CA2101779C - Defoaming composition - Google Patents

Abstract

A defoaming or antifoaming composition comprises a free flowing granular combinate of 50 to 90 weight percent of a wax soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin agglomerates, maltodextrin/
dextrose co-agglomerates, dextrose agglomerates; maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbito agglomerates; agglomerates of hydrolyzed cereal solids,and agglomerates of corn syrup solids and about 10 to 50 weight percent of a liquid, non aqueous, defoaming or antifoaming composition such as simethicone, hydrocarbon-based oils or silicone oils. The composition may be combined with one or more suitable excipients and prepared as a unit dosage in the form of a compressed tablet, filled capsule, packet, or granule for various defoaming applications.

Description

2 ~ ~ ~ ~ ~ ~ ~ PCf/US92/10491 _1_ DESCRIPTTON
DEFORMING COMPOSITION
Backctround of the Invention 1. Technical Field This invention relates to a composition whereby fluid, nonaqueous, defoaming or antifoaming compositions are prepared as relatively free flowing granular combinates by intermixing them with a low density, highly porous, generally spherical, water soluble carbohydrate-based agglomerate such as maltodextrin to form adjuvant agglomerate combinates suitable for addition to products or processes wherever a rapid dispersion of the antifoaming or defoaming compound in an aqueous medium is indicated or desired.
2. Backctround Art The following listing and characterization of fluid, nonaqueous, antifoaming or defoaming compositions or compounds used in the practice of this invention is given to, more precisely and particularly illustrate applicable compositions and compounds. The listing is not meant to limit or to specifically define the category of fluid, nonaqueous, antifoaming or def naming compositions, but rather to illustrate the scope of compositions applicable to the formation of the adjuvant agglomerate combinates.
Fluid hydrocarbon oil-based antifoaming or defoaming compositions containing a hydrocarbon-silicon copolymer, a hydrophobic filler, an organo-silicone surfactant, a . hydrocarbon~.carrier~oil, and, optionally; a silicone oil are discloss:d in U.S. Patent No. 4,514,319 to Kulcarni et al.
Fluid antifoaming or defoaming compositions comprising mineral oil-containing dispersed hydrophobic solid particles are well known in the art. The~use of hydrophobic silica in fluid hydrocarbon oil based WO 93/11752 Pf.'T/US92/104Q1 _2_ antifoam or defoaming compositions is disclosed in U.S.
Patent Nos. 3,076,768; 3,207,698; 3,388,073; and 3,714,068.
Fluid antifoaming or defoaming.compositions comprising polyoxyethylene-polypropylene copolymers containing dispersed hydrophobic silica are disclosed in U.S. Patent Nos. 3,912,652 and 3,959,176.
Fluid antifoaming or defoaming compositions in a non-silicone oil and containing activated insitu hydrophobic silica particles are disclosed in U.S. Patent No. 3,304,266.
Fluid antifoaming or defoaming compositions comprising a non-silicone water insoluble polyalkylene containing an alkoxysilicon chloride as the hydrophobic agent are disclosed in G.B. Patent No. 1,166,877.
Fluid antifoaming or defoaming compositions employing the use of other intrinsically hydrophobic fillers in organic liquids are also well known. For example, Canadian Patent No. 508,856 discloses N,N~-distearyl ethylene-diamide in white spirits, while the use of finely divided polyolefin polymers or polyesters dispersed in organic liquids is disclosed in U.S. Patent No. 3,705,859. The use of fatty acid salts is disclosed in G.B. Patent No. 1,267,482 and low molecular weight polyethylenes in combination with mineral oil and conventional organic nonionic emulsifiers is disclosed in U.S. Patent No. 3,909,445.
Fluid antifoam or defoaming compositions comprising silicone oil-silica compounds containing organo silicone 30- compounds to improve perfarmance are disclosed in U.S.
Patent No. 3,691,091.
Fluid antifoam or defoaming compositions comprising the use of silicone-glycol copolymers in association with WQ 93/11752 1'Cf/US92/14491 -3_ silicone oil and silica are disclosed in U.S. Patent Nos.
3,746,653; 3,784,479; and 3,Et65,544.
Simethecone is a fluid antifoam or defoaming composition comprised of po:Lydimethylsiloxane and silica suitably purified for its intended application. The preparation of liquid methylsiloxane polymers is delineated in U.S. Patent No. 2,441,098, the disclosure of which is hereby incorporated by reference. The normal physical state of the simethicone is a water white to .
grey translucent, viscous, oil-like liquid with a density of 0.965-0.970 grams/cubic centimeter having demonstrable immiscibility with water and alcohol.
The medically established therapeutic use for simethicone is as an ointment base ingredient, topical drug vehicle, skin protectant, but most particularly as an antigas and antiflatulent agent for human application as well as an antibloating agent for veterinary (animal) application. A combinate of simethicone and calcium silicate useful for such latter applications is disclosed in U.S. Patent No. 4,906,478 to Valentine et al.
Various antigas or antifoam formulations, some containing simethicone, are disclosed in the prior art.
The pharmaceutical and medicinal applications include U.S. Patent Nos. 4,605,551 to Buehler et al; 3,326,754 to Prussin et al; 2,774,710 to Thompson et al; 4,115,553 to Rubino et al; 4, 396, 604 to Mitra; 3, 767, 794 to McVean et al; and 4,581,381 to Morris et al. Non°pharmaceutical and non-medicinal antifoaming applications, such as powdered cleaning agents, are disclosed in U.S. Patent Nos. 3,843,558 to Faiminer et al; 4,180,485 to Llenado;

4,264,465 to Abel; 4,102,823 t~ Matheson et al; and European Patent 213,953 to Iley et al.
The preferred pharmaceutical solid dose delivery system for simethicone is a chewable tablet. Such chewable tablets often contain antacid ingredients such WO 93/11752 PCT/US92/10~121 r as calcium carbonate, aluminum hydroxide, magnesium hydroxide and magnesium carbonate. 1'he article by F.
Maksond et al, ~'Simethicone use in Antacid Medications' as published in Manufacturincl" Chemist and Aerosol News, Vol. 47, No. 5, 1976, pp 36-36 discloses instability problems when simethicone is intermixed with aluminum or magnesium bases. It is extremely troublesome to distribute the oil-like, viscous, water and alcohol immiscible simethicone expeditiously and uniformly throughout a tablet granulation prior to compression. It is equally difficult to be certain that the simethicone is in a sufficiently divided and dispersed state so that its action will be quick and effective when administered per os as a chewable or swallowable tablet or powder filled capsule.
Similar problems are encountered in distributing the other anitfoaming compositions in an expeditious and uniform manner in their liquid form.
Bearing in mind the problems and deficiencies of the prior art, it is therefore an object of the present invention to provide an improved dry, granular combinate for dispersing liquid antifoaming or defoaming compounds in an aqueous medium.
It is another object of the present invention to provide an effective simethicone containing granule for use in gastric antacid, antigas, and/or antiflatulent formulations.
It is a further object of the present invention to provide granules to be added to aqueous based products or processes .wherever antifbaming or defoaming is indicated . or desired.
It is yEa another object of the present invention to provide a facile method of producing an effective simethicone-containing foam controlling granule utilizing conventional equipment at relatively low cost.
It is a further object of the present invention to provide a-free flowing~simethicone containing granule for 1~0 93/11752 PCT/US92/10491 use in conventional formulations which, after processing, retains acceptable defoaming activity.
It is yet another obj ect of the present invention to provide an antifoaming or defoaming compound combinate which retains its properties and activity after extended storage and at elevated temperatures.
The present invention achieves these objects and satisfies the long felt need to overcome the difficulties in expeditious utilization of antifoaming or defoaming compounds in an aqueous medium. A larger amount of antifoaming or defoaming compound can be incorporated with the carbohydrate-based agglomerate of this invention for dispersion than has previously been disclosed in the prior art. The carbohydrate-based agglomerate portion of the combinate makes it possible to effect rapid and uniform distribution of the antifoaming/defoaming compound by simple mixing.
Disclosure of Invention The present invention relates to fluid, nonaqueous, antifoaming or defoaming compositions prepared as a dry, solid, flawable granule by intermixing a fluid, nonaqueous, antifoaming or defoaming compound or composition and a low density, highly porous, generally spherical, water soluble, carbohydrate-based agglomerate such as a maltodextrin agglomerate, maltodextrin/dextrose co-agglomerate, dextrose agglomerate, maltodextrin/
sucrose c.o-agglomerate, maltodextrin/fructose co-agglomerate, sucrose agglomerate, fructose agglomerate, mannitol agglomerate, sorbitol agglomerate, agglomerated hydrolyzed cereal solids, agglomerated corn syrup solids, and combinations thereof to form a functional combinate. The preferred agglomerate is maltodextxin, a low conversion starch hydrolyzate having a D.E. (dextrose equidalent) less than 20. The fluid, nonaqueous, antifoaming or defo.aming compound or wo 93imsz Pcrius~znoAm _6_ composition is added, in liquid form, to the water soluble carbohydrate agglomerate and blended to form a uniform, relatively free flowing combinate in which the base structure is water soluble. The combinate may be readily added to conventional products and processes where a rapid dispersion of the fluid, nonaqueous, antifoaming or defoaming compound is indicated. It is preferred that the fluid, nonaqueous, antifoaming or defoaming combinate have from about 10 to 50 weight percent antifoaming or defoaming composition or compound, and from about 90 to 50 weight percent carbohydrate agglomerate. It is more preferred that the fluid, nonaqueous, antifoaming or defoaming composition or compound represents 30 weight percent and the water soluble, highly porous, low density, generally spherical, carbohydrate agglomerate represents 70 weight percent of the admixture combinate. Unless otherwise specified, all references to percentages are in weight percent. The terms "antifoaming" and "defoaming" are generally used interchangably throughout the specification. The antifoaming compositions or compounds useful in this invention may be any of those discussed in the background section of the specification, particularly simethicone (for pharmaceutical and medicinal applictions) and silicone, mineral or other oils containing silica.
Modes for Carrvincr Out Invention The preferred fluid, nonaqueous, antifoaming or defoaming compound~prepared as a flowable granule used herein is simethicone.and, more specifically, si~aethicone U.S.P. as defined in the United States Pharmacopeia, incorporated herein by reference, which has the chemical structure:
(CH3)3Si [OSi(CH3)2]nCH3 + SiO2 and the chemical formula:

WO 93/11752 2 ~ fl ~ ~ ~ ~ PC'I'/~JS92/10491 Alpha(trimethylsilyl)-omega-methylpoly[oxy (dimethylsilylene)] in mixture with silicon dioxide.
Simethicone is a mixture of fully methylated linear siloxane polymers contain~.ng repeating units of the formula [-(CH3)2 Sz0-]n, stabilized with trimethylsiloxy end-blocking units of the formula [(CH3)3Si0-], and silicon dioxide. It is preferred to contain not less than 90.5 percent and not more than 99.0 percent of polydimethylsiloxane ([-(CH3)2 Si0-]n)), and not less than 4.0 percent and not more than 7.O percent of silicon dioxide.
Maltodextrins are composed of water soluble glucose polymers obtained from the reaction of starch with acid and/or enzymes in the presence of water. The starch is hydrolyzed to produce hydrolyzate products containing sugars. 'The production of starch hydrolyzates, and, in particular, low conversion starch hydrolyzat~s, is described in U.S. Patent Nos. 3,663,369; 3,849,194;
4,298,400; and Re. 30,880, the disclosures of which are hereby incorporated by reference. The starch used for the preparation of maltodextrins can be any of a variety of commercially available starches such as maize, potato, or tapioca. Further, the U.S. Food and Drug Adminis-tration defines maltodextrins, (C6H12~5)nH20, as nonsweet nutritive saccharide polymers that consist of D-glucose units linked primarily by alpha l-4 bonds and 30~ having' a D.E.' (total ~reduCing sugars expressed as dextrose equivalents) of less than 20.
Maltode:xtrin is usually produced as a fine, white powder and is generally recognized as safe (gras) as a direct human food ingredient at levels consistent with - good manufacturing practices. Agglomerated maltodextrin is available from a variety of commercial sources and in _8_ a larger, more porous, faster dissolving, and more free flowing form.
The preferred commercial source for low density, highly porous, generally spherical, water soluble maltodextrin agglomerates is the product family sold by Valentine Enterprises, Inc. of Lawrenceville, Georgia under the trademark VELite. The preferred VELite is VELite 20/40 which is prepared from 9-12 D.E.
maltodextrin, derived from corn starch, and having the following typical analysis: a particle size distribution of about 100 percent less than 850 microns and a majority (98 percent) greater than 420 microns; an apparent density of from about 10 to about 12 pounds per cubic food; a maximum moisture content of 6 percent; and a total surface area of between about 9.5 q 1 and 10.5 q 1 square meters per gram as determined by a 3 point nitrogen B.E.T. analysis.
A preferred embodiment of the present invention is directed toward the admixture of simethicone and maltodextrin agglomerate to form a uniform, relatively free flowing, granular combinate containing 3o percent by weight of simethicone and 70 percent by weight maltodextrin for incorporation into tablets or for use "as is" for addition to an aqueous medium whenever antifoaming or defoaming is desired.
The 30 percent by weight simethicone/70 percent by weight agglomerated maltodextrin combinate is readily formulated into, for example, antacid or antigas farmulations by adding the 30% simethicone active granule combinate to a compressible granule base without sacrif icing or compromising the compressibility of the base granule. . It is a further feature of the present invention that the simethicone is contained in or on a water soluble agglomerated maltodextrin and, as such, is available and stable in the formulations.

W~ 93/11752 ~ ~ ~ ,,~ "l ~ PC1'/US92/10a91 _g_ The process of the present invention may be practiced by obtaining desired quantities of agglomerated maltodextrin, such as VE:Lite 20/40 available from Valentine Enterprises, Inc., and consumable simethicone, such as Sentry simethicone available from Union Carbide Corporation. These two starting materials are then mixed employing low shear mixing such as that encountered in a planetary, ribbon or plow mixer in order to effect a uniform combinate agglomerate suitable for use without further processing.
The relative amounts of the simethicone and the maltodextrin agglomerate may range from about ZO to about 50 weight percent simethicone and from about 90 to about 50 percent by weight of agglomerated maltodextrin. This range of the ingredients has been found to provide optimum performance of the final s.~.aethicone/agglomerated maltodextrin combinate. If more than about 50~ by weight percent simethicone is used, the product tends to be too moist and exhibits poor flow. If more than 90o by weight of agglomerated maltodextrin is used the product tends to exhibit non-uniform distribution of the simethicone.
Exceeding either extreme will tend to result in less than optimum product performance, most particularly in final tableting. A 30~ by weight simethicone to 70% by weight agglomerated maltodextrin ratio represents the preferred product performance whether for tableting or for general purpose aqueous antifoaming or defoaming application.
The combinate maltodextrin and the antifoaming or defoaming composition preferably has a particle size in which essentially all of the particles are less than about 20 mesh (-20 mesh) and greater than 40 mesh (+40 mesh) and a total typical surface area of less than about 1 square meter per gram.
While not wishing to be limited to a particular combinate formation theory, it is believed that sorption, i.e., absorption or adsorption, takes place during the W~ 93/11752 PCi~/US92/laa~a i;

blending whereupon the liquid simethicone or other defoaming compound or composition (the sorbate) is taken up by the agglomerated maltodextrin or other carbohydrate (the sorbent). It is further theorized that the rapid water solubility of the carbohydrate moiety of the combinate helps to explain the speed of action of the product since the simethicone or other defoaming compound is liberated in dispersed particles.
The antifoaming and/or defoaming containing adjuvant l0 combinate granules of the present invention have been found to be equal in foam inhibition and foam breaking to an equivalent quantity of the starting simethicone. This means, for example, that 66.7 mg of the 30~ simethicone combinate granule is equivalent in performance to 20 mg of simethicone. The equivalent performance is demonstrable even after the simethicone/agglomerated maltodextrin combinates have been stored at 45°C far a period of two months.
Defoaming activity of the simethicone/agglomerated maltodextrin combinate or of the monadic simethicone or of the simethicone/agglomerated maltodextrin combinate contained as part of an antacid and/or antigas tablet, i.e., foam breaking (defoaming) and/or foam inhibition (antifoaming),, may be defined and measured by the procedure given in the United States Pharmacopeia.
First, a foaming solution and test preparation are prepared as follows:
Foaming solution - dissolve 1g of octoxylnol 9 in 100 ml of distilled water.
~30 ~ Test preparation - transfer 200 mg of simethicone .to a 60 ml bottle, add 50 m1 of tertiary butyl alcohol, cap the bottle, and shake vigorously. The preparation may be warmed slightly, if necessary, to effect the solution.
The procedure for determining defoaming activity as follows: For each test, a clean, unused 250 ml glass jar fitted with a 50 mm cap should be employed. Add, - WO 93/11752 ~ ~ ~ ~ PCT/t.J592/10491 dropwise, 0.5 ml of the test preparation (i.e., equivalent to 2.0 mg simethicone) to the 250 ml glass gar containing 100 ml of the foaming solution. Cap the jar and clamp it in an upright poi>ition on a wrist action shaker. Employing a radius of 13.3 q 0.4 cm (measured from the center of the shafi~ to the center of the bottle), shake for 10 seconds through an arc of 10° at a frequency of 300 q 30 strokes per minute. Record the time required for the foam to collapse. The time, in seconds, for foam collapse is determined at the instant the first portion of foam-free liquid surface appears, measured from the end of the shaking period. This time is the defoaming activity time and should not exceed 15 seconds for acceptable simethicone activity. To evaluate the simethicone/maltodextrin agglomerate combinate activity, a quantity of the combinate equivalent to 2.0 mg of simethicone (i.e. 6.7 mg of a 30~ simethicone/
maltodextrin combinate) is introduced directly into the test solution and the defoaming time is determined as described above.
There is no fixed quantity of simethicone, supplied by the simethicone/maltodextrin combinate, which must be used to prepare an antacid%antigas preparation. A
typical formulation would contain:
Aluminum hydroxide dried gel 200 mg Magnesium hydroxide, dried 200 mg Simethicone/maltodextrin combinate 85 mg 3Jot only will the simethicone/maltodextrin agglomerate release the simethicone by virtue of the water~solubility of the mal4. =_xtrin moiety, but, when the combinate is added tG .:ablet granulations, no deleterious compression effects are evidenced. 6~hether or not the foam inhibition attributes of the simethicone/m~altodextrin agglomerate combinates are measured from the combinate alone or combined with standard antacid ingredients, in tablet or granule form, ;:

defoaming results are obtained which are equivalent to simethicone alone. Significantly, the same defoaming test results are evidenced even after accelerated storage stability at 37°C, and 60°C, for periods up to 2 months.
Therefore, the simethicone/agglomerated maltodextrin adjuvant combinate demonstrates itself as a uniquely stable product capable of being combined with. antacid ingredients such as aluminum and magnesium bases in a single layer tablet without compromising the acid' neutralizing or the defoaming or antifoaming capacity of the dose form.
Standard excipients can be combined with the simethicone/agglomerated maltodextrin combinate granules in order to prepare pharmaceutical preparations in the form of tablets or capsules. In order to prepare tablets, the simethicone/agglomerated maltodextrin combinate may be combined and blended with standard compression granules comprising, for example, calcium carbonate, dextrose, sucrose, mannitol, sorbitol, aluminum hydroxide dried gel; magnesium hydroxide, any compatible spray dried flavor, and magnesium stearate.
The blended preparation may be pressed by standard, well known techniques to form tablets of desired weight, potency, and hardness. A single layer homogeneous unit dosage tablet or capsule may preferably contain from about 80 mg to about 280 mg of the simethicone/
agglomerated maltodextrin combinate (i.e., from about 25 to about 80 mg of simethicone), but any desired amouait outside this range may be used far specific applications.
w A general ranking order of the water soluble carbohydrate agglomerate/simethicone U.S.P. combinates, beginning with the most satisfactory, is as follows:
maltodextrin agglomerate maltodextrin/dextrose co-agglomerate dextrose agglomerate maltodextrin/suarose co-agglomerate bV0 93/11752 PCT/US92/10491 maltodextrin/fructose co-agglomerate sucrose agglomerate fructose agglomerate Additionally, mannitol agglomerate, sorbitol agglomerate, agglomerated hydrolyzed cereal solids, and agglomerated corn syrup solids, 1.e., those having a D.E.
of 20 or greater, may be employed. Any of these agglomerates, either alone or in combination, may be obtained, combined with simethicone, and utilized in the same manner as described above for the embodiment utilizing agglomerated maltodextrin alone. The combinate will preferrably comprise at least about 50 weight percent, and up to about 90 weight percent, of the carbohydrate-based agglomerate. The particle side of substantially all of the carbohydrate- based agglomerate is preferably less than about 850 microns, with the majority (up to about 98 wt.%) greater than about 9:20 microns.
The maltodextrin/dextrose, maltodextrin/sucrose and maltodextrin/fructose co-agglomerates are preferably prepared by well known fluid bed agglomeration techniques in which maltodextrin in solution (e. g., a 10% aqueous solution or 5% povidone (K 29/32) U.S.P. solution) is combined with the dextrose, sucrose or fructose in ~n agglomerator bed. The specific ratio of maltodextrin to dextrose, sucrose or fructose may' vary according to use, and may be determined without undue experimentation. The co-agglomerate is produced by standard spray granulation techniques. The carbohydrate-based agglomerates will ~30 preferably have a. particle~size range of less than 20 mesh and greater than 60 mesh (U. S. Standard), more preferably less than 20 mesh and greater than 40 masts.
Other antifoaming compositions or compounds useful in' this invention with maltodextrin or any of the other aforementi~ned carbohydrate-based agglomerates may be any of those organic liquid defoamers discussed in the background section of the specification, including WO 93/11752 PCI'/US92/104~1 l::

hydrocarbon-based liquids, such as mineral oils and other hydrocarbon oil-based liquids, and silicone oils. These liquids may optionally contain silica. The carbohydrate-based agglomerate and liquid antifoaming composition may be mixed by low shear mixing techniques in a planetary, ribbon or plow mixer in order to effect a uniform combinate agglomerate suitable for use without further processing. The combinate will preferrably comprise at least about 10 weight percent, and no greater than about 50 weight percent, of the liquid antifoaming composition. Lower amounts of liquid antifoaming composition may be employed, although there tends to be non-uniform distribution of the antifoaming agent in amounts less than about 10 wt.~. The particle size range of the combinate is not substantially different from the particle size range of the carbohydrate-based agglomerate prior to mixing with the liquid antifoaming composition.
The combinate of carbohydrate-based agglomerate and antifoaming or defoaming composition of the present invention may be used by contacting the aqueous medium in which defoaming is desired with the combinate. In the case of simethicone for use in pharmaceutical or medicinal applications, the carbohydrate-based agglomerate/simethicone combinate would be ingested by the user in tablet, capsule, granule or other unit dose form to provide antigas and/or antiflatulent treatment.
In the case of other defoaming compositions or compounds, the combinate may be prepared as granules in bulk filled packages or in unit dose forms such as compressed tablets or water soluble pouches for application to the aqueous medium..
.Acid neutralizing capacity may be measured by the procedure set forth in the United States Pharmacopeia.
The analytical procedure, to be conducted at 37°C ~
35~ 3°C, is as followsi First, :standardize a pH meter using 0.05M potassium biphthalate and 0.05M potassium-tetraoxalate ~rVO 93/11752 PC.'T/US92/10491 ~lQ~h~~~
°15-standardizing buffers. Next, transfer 100 ml of water to a 250 ml beaker containing a 40 x 10 mm magnetic stirring bar that is coated with solid perfluorocarbon and has a spin ring at its center. The power setting of the magnetic stirrer shou:Ld be adjusted to produce a stirring rate of 300 rpm when the stirring bar is centered in the beaker, as determined by a suitable optical tachometer.
The test preparations are prepared as follows:
powders - transfer the accurately weighed portion of the substance to be tested to a 250 ml beaker, add 70 ml of water, and mix in the magnetic stirrer for one minute.
Tablets - weigh not less than 20 tablets and determine the average tablet weight Grind the tablets to a powder that passes through a no. 20 sieve and is retained on a 100 sieve. Mix the material on the no. 100 sieve to obtain a uniform mixture, transfer an accurately weighed quantity of it, equivalent to the minimum dosage, to a 250 ml beaker. If wetting is desired, add not more than 5m1 of alcohol (neutralized to an apparent pH of 3.5), and mix to wet the specimen thoroughly. Add 70 ml of water, and mix on the magnetic stirrer for one minute.
The test procedure is as follows: Pipet 30.0 m1 of 1.0 N hydrochloric acid vs into the test preparatian prepared earlier while continuing to stir with the magnetic stirrer. Magnetic stirring should continue for 15 minutes (accurately timed) after the addition of the acid. Thereafter, begin to Citrate immediately, in a period not to exceed 5 minutes, the excess hydrochloric ~30 acid with 0.5 N sodium hydroxide vs to attain a stable .pH
of 3.5 for not less than Z5 seconds. Calculate the number of mEq of acid consumed per gram of the substance tested. Ea~;h ml of 1.0 N hydrochloric acid is equal to 1 mEq of acid consumed.

WO 93/11752 P(_T/US92/10491 EXAMPLES
The following illustrative examples are given to more precisely and particular7.y illustrate the specific details of the present invention. Equivalent procedures and quantities will occur to those skilled in the art and therefore, the following examples are not meant to define the limits of the present invention, these being defined by the scope of the appended claims.
Example 1 Starting Materials:
Simethicone U.S.P.
(Sentry simethicone) 40 g Agglomerated Maltodextrin (VELite 20/40) 160 g The VELite 20/40 was charged into a 1000 cc stainless steel beaker and the simethicone was added. The total materials were blended with a spatula until~uniform. The resulting granular combinate was lump free, less than 850 microns (20 mesh) in size, and contained 20~ simethieone.
A portion of the sample was used to prepare chewable antacid tablets containing 125 mg of the simethicone/agglomerated maltodextrin combinate per tablet (equivalent to 25 mg of simethicone per tablet).
Example 2 Starting materials:
Simethicone U.S.P.
3'0 (Seaztz°y simethicone) 300 g Agglomer<~ted maltadextrin (VEl~ite 20/40) 700 g The VELite 20/40 was charged into a 5000 ml stainless steel beaker and the simethicone was added. The total materials were blended with a spatula until uniform. The resulting granular combinate was lump free; less thin 850 microns (20 mesh) in size and contained 30~ simethicone.

iWaD 93/11752 PCf/U~92/1 x491 A portion of the sample was used to prepare chewable antacid tablets containing 84 mg of the simethicone/ag-glomerated maltodextrin combinate per tablet (equivalent to 25 mg simethicone per tablet).
Examt~le 3 Starting materials:
Simethicone U.S.P.
(Sentry simethicone) 400 g Agglomerated maltodextrin (VELite 20/40) 600 g VELite 20/40 was charged into a 5000 ml stainless steel beakex and the simethicone was added. The total materials were blended with a spatula until uniform. The resulting granular combinate was lump free, less than 850 microns (20 mesh) in size and contained 40% simethicone.
A portion of the sample.was used to prepare chewable antacid tablets containing 63 mg of the simethicone/agglomerated maltodextrin combinate per tablet (equivalent to 25 mg of simethicone per tablet).
Example 4 Starting materials:
Simethicone U.S.P.
(Sentry simethicone) 1.5 kg Agglomerated maltodextrin (VELite 20/40) 3.5 kg VELite 20/40 was charged into a 5 gallon stainless steel Hobart mixer and the simethicone was added. The mixer was energized and mixing~was effected for a period of l0 .minutes. The resulting granular combinate was found to be lump free, less than 850 microns (20 mesh) in size, and contained 30% simethicone.
A portion of the product was used to prepare chewable antacid tablets containing 84 mg of the sim~thicone/
agglomerated .maltodextrin combinate per tablet (equivalent to 25 mg of simethicone per tablet).

o'VO 93/11752 PCT/U~92/10491 a ~,~~~~'; 9 Example 5 Starting materials:
Simethicone U.S.P.
(Sentry simethicone) 30 kg Agglomerated maltodextrin (VELite 20/40) 70 kg VELite 20/40 was charged into a 20 cubic foot capacity ribbon blender and the simethicone was added.
The mixer was energized and mixing was effected for a period of IO minutes. The resulting granular combinate was discharged into drums and found to be lump free, less than 850 microns (20 mesh) in size, and contained 30%
simethicone.
A portion of the product was used to prepare chewable antacid tablets containing 84 mg of the simethicone/
agglomerated maltodextrin combinate per tablet (equivalent to 25 mg of simethicone per tablet).
Example 6 Starting materials:
Simethicone U.S.P.
(Sentry simethicone) 3.0 kg Agglomerated maltodextrin (VELite 20/40) 7.0 kg VELite 20/40 was charged into a 3 cubic foot capacity stainless steel Lodige blender and the simethicon~ was added. The plow blades of the mixer were energized and mixing effected for a period of l0 minutes. The resulting granular, coanbinate~ was discharged into a drum and found to be lump free, less than 850 microns (20 mesh) in size, and contained 30% simethicone.
A portion of the product was used to prepare chewable antacid tablets containing 84 mg of the simethicone/
agglomerated-maltodextrin combinate per tablet (equivalent to 25 mg of simethicone per tablet).

~O 93/11752 2 ~ ~ ~ ~ ~ ~ PCT/U x92/10491 Examule 7 Starting materials:
Simethicone U.S.P.
(Sentry simethicone) 90 kg Agglomerated maltodextrin (VELite 20/40) 210 kg VELite 20/40 was charged into a 1200 1 stainless steel Lodige blender and the simethicone added. The plow blades of the mixer were energized an mixing was effected fox a period of 10 minutes. The resulting granular combinate was discharged into drums and found to be lump free, less than 850 microns (20 mesh) in size, and contained 30% simethicone.
A portion of the product was used to prepare chewable antacid tablets containing 84 mg of the simethicone/
agglomerated maltodextrin combinate per tablet (equivalent to 25 mg of simethicone per tablet).
Example 8 Each of the simethicone/maltodextrin combir,ates produced in Examples 1-7. were evaluated in the following manner:
A quantity of the simethicone/agglomerated maltodextrin combinates were evaluated in the standard U.S.P, defoaming test at a level equivalent to 2 mg of simethicone.
Quantity of the Simethicone Time Example No. Combinate Used Equivalent to Defoam (mgj (mg) (sec.) 1 10.0 2 3-4 2 6.7 2 3-4 3 . 5.0 . 2 3-4 4 6.7 2 3-4 6.7 2 3-4 6 6.7 2 3-4 7 6.7 2 3-4 Controls-Simethicone U.SoP 2.0 2 3-4 Sim~thicone U.S.P 6.7 ' 2 ' 3-4 (a~ 30~ emulsion) iW~ 93/11752 PC1'/U592/10491 f..

The data suggests that ec;uivalent quantities of simethicone derived from either the simethicone/
maltodextrin combinates or from the simethicone U.S.P. or from the commercial 30~ silicone emulsion demonstrate equivalent defoaming action.
Stability samples stored for, periods up to 2 months at 37°C and 45°C evidence no change in defoaming times and are unchanged in physical appearance.
It is observed that when the simethicone/agglomerated maltodextrin combinates (Examples 1-7) are added to water at a level calculated to liberate 100 mg of samethicone, the maltodextrin moiety dissolves in the water and the silicone forms a surface oil layer.
Example 9 Each of the simethicone/agglomerated maltodextrin combinates produced in Examples 1-7 were evaluated in a typical chewable antacid tablet formulation as follows (all values in mg):
EX.1 EX.4 EX.S EX.6 EX.7 EX.2 EX.3 Compression Dextrose 661702 723 702 702 702 702 Aluminum Hydroxide Dried Gel 200200 200 200 200 200 200 Magnesium Hydroxide ' Powder 200200 200 200 200 200 200 Simethicone/

Maltodextrin Combinate Equivalent to 25 mg of Simethicone 12584 63 84 84 84 84 Spray Dried Flavor 5 5 5 5 5 5 5 Magnesium Stearate 9 9 9 g 9 9 9 Each of the formulations re produced as single we layer. 9/16 inc h, flat-faced, edge chewable beveled tablets, compressed at a~weight 1200 and of mg a hardness i. .. WO 93/11752 ~ ~' PCT/US92/1a491 of 7-9 Kp. Tablets without simethicone were also produced under the same conditions to serve as a control.
All of the tablets produced for the trials satisfied the criteria for taste acceptance, mouth feel, hardness, friability, and acid neutralization, Each of the tablet formulations were evaluated for defoaming in accordance with the U.S.P. method for antacid tablets with the following results:
Test Storage Condition: Tnitial 45° for 2 Months Tablets produced with Simethicone/Malto- Time to Defoam Time to Defoam dextrin Combinate From: L n Seconds L ~In Seconds) EX.1 5-7 5-7 EX.2 5-7 5-7 EX.3 5°7 5-7 EX.4 5-7 5-7 EX.S 5-7 5-7 EX.6 5-7 5-7 EX.7 5-7 5-7 Control No Defoaming No Defoaming After storage at 45°C for a period of two months all of the tablets still satisfied the acid neutralization criteria for extra strength antacid tablets.
Examble 10 Calcium carbonate-based antacid tablets were prepared with and without simethicone/agglomerated maltodextrin combinat.e as follows (all values in mg):
With Without Formula: Combinate Combinate Calcium Carbonate .

compression Granules (53% Calcium Carbonate 47% Dextrose) 1000 1000 Compression Dextrose 104 188 Simethicone/Agglomerated Maltodextrin Cambinate From Example ~7 84 - -Spray Dried Flavor 3 3 Magnesium Stearate 9 9 WO 93/11752 PC'I'/US92/104~1 t Each of the formulations were processed into single layered 9/16 inch, flat faced, beveled edge chewable tablets compressed at a weight of 1200 mg and a hardness of 7-9 Kp.
Each of the chewable tablet formulations produced for the trial s satisfied the criteria for chewable tablets with respect to taste acceptance, mouth feel, hardness, friability, and acid neutralization.
Each of the chewable tablet formulations were evaluated f or defoaming in accordance with the U.S.P.
method for antacid tablets with the following results:
Defoamina Time Formulation With Combinate 4-6 sec.
Formulation Without Combinate No Defoaming Example 11 Magaldrate (aluminum magnesium hydrate with magnesium sulf ate) based antacid tablets were prepared with and without simethicone/agglomerated maltodextrin combinate as follows (all values in mg):
With Without Formula Combinate Combinate Dextrose Compression Granules 702 786 Magaldrate 400 400 Simethicone/Agglomerated Maltodextri.n Combinate From Example 7 84 ---Spray Dried Flavor . " 5 5 Magnesium Stearate 9 g, Both of the formulation s were processed into single layered 9/16 inch, flat-f aced, beveled edge chewable antacid tablets at a weightof 1200 mg a hardness and of 7-9 Kp.

-.:lWO 93/11752 PCT/US92/10491 The chewable antacid tablets produced for the trials, i.e., with and without the simethicone/agglomerated maltodextrin combinate, satisfied the criteria for taste acceptance, mouth feel, hardness, friability, and acid neutralization.
Each. of the formulations were evaluated for defoaming in accordance with the U.S.:P. method for antacid tablets with the following results:
Defoamina Time Formulation With Combinate 4-6 sec.
Formulation Without Combinate No Defoaming Examble 12 An antigas chewable tablet formulation was prepared to demonstrate the utility of simethicone/agglomerated maltodextrin combinate in such an application as follows (all values in mg):
Compression Dextrose 946 Simethicone/Agglomerated Maltodextrin Combinate From Example 7 240 Spray Dried Flavor 5 Magnesium Stearate 9, ~ The fag~naulation was produced as a single layered 9/16 inch, flat-faced, beveled edged chewable tablet compressed at a weight of 1200 mg and a hardness of '~~-9 Kp.
The tablets produced satisfied the criteria for taste acceptance, mouth feel, hardness, friability, and foam suppression..

WO 93/11752 PCT/IJ~92/10491 j.

Example 13 To further illustrate the utility of the invention, a general standard fluid silicone oil defoamer/ agglomerated maltodextrin combinate was prepared:
Starting Materials Used:
Fluid Silicone Oil Containing Silica 1.05 kg Agglomerated Maltodextrin (VELite 20/40) 2.45 kg The VELite 20/40 was charged into a 5 gallon stainless steel Hobart mixer and the fluid silicone oil containing silica added. The mixer was energized and mixing was effected for a period of 10 minutes. The resulting granular combinate was lump free, less than 850 microns (20 mesh) in size and contained 30~ of the fluid silicone oil containing silica defoaming compound.
The above described combinate demonstrated satisfactory antif oaming/defoaming properties when subjected to the standard U.S.P. defoaming test.
Example 14 To further illustrate the utility of the invention,. a general standard fluid mineral oil defoamer/agglomerated maltodextrin combinate was prepared as fol3.ows:
Starting Materials Used:
Fluid Mineral Oil Containing silica 1.05 kg V6'O 93/11752 "~ f~ PCT/US92/1On91 Agglomerated Maltodextrin (VELite 20/40) 2.45 kg The VELite 20/40 was charged into a 5 gallon stainless steel Hobart mixer and the fluid mineral oil containing silica added. The mixer was energized and mixing was effected for a period of 10 minutes. The resulting granular combinate was lump free, less than 850 microns (20 mesh) in size and contained 30% of the fluid silicone oil containing silica defoaming compound.
The above described combinate demonstrated satisfactory antifoaming/defoaming properties when subjected to the stardard U.S.P. defoaming test.
The following Examples illustrate the use of other water soluble carbohydrate-based agglomerates in combination with simethicone.
Example Z5 A granular or agglomerated product comprised of dextrose monohydrate 95% and maltodextrin (10 D.E.) 5% was obtained from Corn Products Corporation under the trademark Unidex 2034. The Unidex product had a particle size range of -20/+60 mesh and an apparent bulk density of 0.58 g/cc.
Sample products were prepared by adding simethicone U.S.P. to the Unidex dextrose monohydrate/maltodextrin mixture in the following amounts, followed by 10 minute mixing to produce relatively free flowing Unidex produot/
simethicone combinates:
3 0' ' ' ' ~ ' ' 1 2 3 Unidex 2034 (-20/+6o Mesh) 80% w/w ~o% w/w ~o% w/w ~'VO 93/11752 PCT/US92/10~491 ~.~~~~~ 9 Sentry Simethicone U.S.P.
(Union carbide) 20% w/w 30% w/w 40% w/w The Unidex product/simethicone U.S.P. combinates evidenced rapid defaaming characteristics, i.e., 2 seconds by the U.S.P. test.
Standard antacid tables containing 200 mg of aluminum hydroxide, 200 mg of magnesium hydroxide, and 25 mg of simethicone, in the form of the Unidex productj simethicone combinate, also evidenced satisfactory defoaming charcteristics when tested by the U.S.P.
defoaming method, i.e. 6-8 seconds.
Example 16 Dextrose monohydrate-maltodextrin agglomerates were prepared by fluid bed agglomeration as follows:
In the fluid bed agglomertor bed:
Dextrose Monohydate 95%
(Clintose 'F' Granluation, Archer Daniels Midland) In aqueous solution:
Maltodextrin, 10 D.E. 5%
(Maltrin M-100, Grain Processing Corporation) The dextrose monohydate-maltodextrin co-agglomerate was processed by standard spray granulation techniques to produce an agglomerate for sorption trials. After processing, the agglomerated dextrose-maltodextrin particles had a particle size range of about -20/+60 mesh and an apparent density of 0.42 g/cc.:
Saanpl~: products were prepared by adding the simethicone U.S.P. to the agglomerated dextrose-2~0.~~'~~
_27_ maltodextrin in the following amounts (percentages by weight):

Dextrose/maltodextrin Co-agglomerate (-20/+60 Mesh) 80% 70~ 60$
Sentry Simethicone U.S.P.
(Union Carbide) 20~ 30% 40~
The samples were mixed for 10 minutes to produce relatively free flowing simethicone/dextrose-maltodextrin agglomerate combinates.
The agglomerated dextrose-maltodextrin/simethicone combinates evidenced rapid defoaming charcteristics, i.e., 2 seconds by the e.S.P. defoaming test.
Standard single l~~:er antacid tables containing 200 mg of aluminum hydroxi;:,e, 200 mg of magnesium hydroxide, and 25 mg of simethicone, in the form of the dextrose agglomerate/simethicone U.S.P. combinate, evidenced rapid defoaming characteristics, i.e. 6-8 seconds by the U.S.P.
defoaming test.
Example 17 Sucrose-maltodextrin co-agglomerates were prepared by fluid bed agglomeration as follows:
In fluid bed agglomerator bed:
Milled sucrose (-50 Mesh) 95%
In pump solution:
3 0 ~ Maltodextrin, 1~0 ' D. E .
(as 10~ aqueous solution) 5~
The sucrose-maltodextrin co-agglomerate was effected by standar~'l spray granulation techniques to produce an agglomerate for sorption. trials. After processing, the WO 93/11752 PCT/U592/1~D491 r:. .

sucrose-maltodextrin particles had a particle size range of about -20/+60 mesh and an apparent density of 0.45 g/cc.
Sample products were prepared by adding simethicone U. S. P. to the sucrose-maltod~extrin co-agglomerates in the following amounts:

Sucrose-maltodextrin to co-agglomerate (-20/+60 Mesh) 80% 70% 60%
Sentry Simethicone U.S.P.
(Union Carbide) 20% 30% 40%
The samples were mixed for 10 minutes to produce relatively free flowing simethicone/sucrose-maltodextrin agglomerate combinates.
The agglomerated sucrose-maltodextrin/simethicone combinates evidenced rapid defoaming characteristics, i.e., 2 seconds by the U.S.P. d~foaming test.
Standard single layer chewable antacid tablets containing 200 mg aluminum hydroxide, 200 mg magnesium hydroxide, and 25 mg of simethicone in the form of the sucrose-maltodextrin co-agglomerate/simethicone combinate, also evidenced staisfactory defoaming characteristics when tested by the U.S.P. defoaming method, i.e., 6-8 seconds.
~ ~xamgle 18 Sucrose 10x-maltodextrin co°agglomerates were prepared by fluid bed agglomeration as follows. Sucrose loX is a widely available finely milled sucrose which contains 2% corn starch to assure free-flow:

WO 93/11752 ~ ~ ~ ~ ~ ~ ~ PCT/U592/10491 In fluid bed agglomerator bed:
Sucrose 10x 95%
In pump solution:
Maltodextrin, 10 D.E. 5%
(as aqueous solution) The sucrose lOX-maltodextrin co-agglomerate was effected by standard spray granluation techniques to produce an agglomerate for sorption trials. After processing, the agglomerated sucrose 10X-maltodextrin particles had a particle size range of about -20/+60 mesh and an apparent density of 0.40 g/cc.
Sample products were prepared by adding the simethicone U.S.P. to the sucrose lOX-maltodextrin co-agglomerate in the following amounts:

Sucrose lOX-maltodextrin Co-agglomerate (-20/+60 Mesh) 80% 70% 60%
Sentry Simethicone U.S.P.
(Union Carbide) 20% 30% 40%
The samples were produced by mixing for 10 minutes to produce relatively free flowing simethicone/sucrose 10X
maltodextrin agglomerate combinates.
The agglomerated sucrose 10X-maltodextrin/simethicone U.S.P. combinates evidenced rapid defoaming characteristics, i.e. 2 seconds by the U.S.P. defoaming test.
Examgle 19 Dextrose monohydate-maltodextrin co-agglomerates were prepared by fluid bed agglomeration as followss wo ~3imsz rcrius9zmo4Q~
-30_ In fluid bed agglomerator_ bed:
Dextrose monohydate 42.5%
Maltodextrin, 10 D.E. 42.5%
In pump solution:
Maltodextrin, 1U D.~'s. 5.0%
(in aqueous solution) The dextrose monohydate-maltodextrin co-agglomerate was effected by standard spray granulation techniques to produce an agglomerate for sorption trials. After processing, the dextrose-maltodextrin co-agglomerate particles had a particle size range of about -20/+60 mesh and an apparent density of 0.30 g/cc.
Sample products were prepared by adding '~lae simethicone U.S.P. to the dextrose-maltodextrin co-agglomerate in the following amounts:

Dextrose-maltodextrin Co-agglomerate (-20/+60 Mesh) 80% 70% 60%
Sentry simethicone U.S.P.
(Union Carbide) 20% 30% 40%
The samples were produced by mixing for 10 minutes to produce relatively free flowing simethicone/dextrose maltodextrin co-agglomerate combinates.
The agglomerated dextrose-maltodextrin/simethicone U.S.P. combinates evidenced rapid defoaming characteristics, i.e. 2 seconds by the U.S.P. defoaming 30' test.' ' Standard single layer chewable antacid tablets containing 200 mg of aluminum hydroxide, 200 mg of magnesiuan h;Ydroxide and 25 mg of simethicone, in the form of agglomerated dextrose-maltodextrin/simethicone U.S.P.
combinates, evidenced rapid defoaming characteristics, i.e. 6-8 seconds by the U.S.P. defoaming test.

WO 93111752 ~ ~ ~ PC1'/US92/10491 Examx~le 20 Sucrose-maltodextrin co-agglomerates were prepared by fluid bed agglomeration as follows:
In fluid bed agglomerator bed:
Sucrose lOX 42.5%
Maltodextrin, 10 D.E. 42.5%
In pump solution:
Maltodextrin, 10 D.E. 5.0%
(in aqueous solution) The sucrose-maltodextrin co-agglomerate was effected by standard spray granulation techniques to produce an agglomerate for sorption trials. After processing, the sucrose-maltodextrin co-agglomerate particles had a particle size range of about -20/+60 mesh and an apparent density of 0.32 g/cc.
Sample products were prepared by adding simethicone U.S.P. to the sucrose-maltodextrin co-agglomerates in the following amounts:

Sucrose-maltodextrin co-agglomerate (-20/+60 Mesh) 80% 70% 60%
Sentry Simethicone (Union Carbide) 20% 30% 40%
The samples were produced by mixing for 10 minutes to produce re~.atively free flowing simethicone/sucrose maltodextrin co-agglomerate combinates.
The sucrose-maltodextrin co-agglomerate/simethicone combinate5 evidenced rapid defoaming characteristics, i.e. 2 seconds by the U.S.P. defoaming test.

WO 93/11752 PC'f/US92/10491 d~~~

Standard single layer chewable antacid tablets containing 200 mg of aluminum hydroxide, 200 mg of magnesium hydroxide and 25 mg of simethicone, in the form of the sucrose 10X-maltodextrin/simethicone combinate, evidenced rapid defoaming characteristics, i.e. 6-8 seconds by the U.S.P. defoam:ing test.
Example 21 Dextrose monohydate-maltodextrin co-agglomerates were prepared as in Example 19 except that the pump solution was 5% povidone (K 29/32) U.S.P.
Similar trial products were prepared and similar results were observed as in Example 19.
Example 22 Sucrose-maltodextrin co-agglomerates were prepared as in example 20 except that the pump solution was 5%
povidone (K 29/32) U.S.P.
Similar trial products were prepared and similar results were observed as in example 20.
Example 23 Fructose-maltodextrin co-agglomerates were prepared by fluid bed agglomeration as follows:
In fluid bed agglomerator bowl:
Fructose (powder) 50%
Maltodextrin, 10 D.E. 47.5%
In pump solution:
~ Maltadextrin, 10'D.E.
(as 10% water solution) 2.5%

W~ 93/13752 PCT/US92/10491 A fructose-maltodextrin co-agglomerate was effected by standard spray granulation techniques to produce an agglomerate for sorption trials. After processing, the fructose-maltodextrin co-agglomerate particles had a particle size range of about -20+60 mesh and an apparent density of 0.42 g/cc.
Sample products were prepared by adding simethicone U.S.P. to the fructose-maltodextrin agglomerates in the following amounts:

Fructose/maltodextrin co-agglomerate (-20/+60 Mesh) 80% 70% 60%
Sentry Simethicone U.S.P.
(Union Carbide) 20% 30% 40%
The samples were produced by mixing for 10 minutes to produce relatively free flowing simethicone/fructose maltodextrin co-agglomerate combinates.
The co-agglomerated fructose-maltodextrin/simethicone combinates evidenced rapid defoaming characteristics, i.e. 2 seconds by the U.S.P. defoaming test.
Single layer chewable antacid tablets containing 200 mg of aluminum hydroxide, 200 mg of magnesium hydroxide and 25 mg of simethicone, in the form of the fructose maltodextrin/simethicone U.S.P. combinate, evidenced rapid defoaming characteristics, i.e. 6-8 seconds by the U.S.P. defoaming test.
. While the invention has been described with reference to specific embadiments, it will be recognized by those skilled in the art that variations are possible without WO 93/11752 Pt.'T/U592/10491 e;._.

departing fromthe spirit scope of the invention, and and that it is intended to cover all changes and modificati ons of the invent:ian disclosed herein for the purposes of illustration which do not constitute departure fromthe spirit scope of the invention.
and Having thu s described invention, what is claimed the is:

Claims (61)

The embodiments of the invention in which an exclusive property or privilege is claimed are defined as follows:

1. An antifoaming or defoaming composition comprising a dry, uniform, free flowing granular combinate of a water soluble carbohydrate-based agglomerate and a liquid, nonaqueous, antifoaming or defoaming composition selected from the group consisting of hydrocarbon-based oils and silicone oils, wherein said carbohydrate-based agglomerate is selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids and agglomerates of corn syrup solids having a D.E. of at least 20.

2. The composition of claim 1, wherein said carbohydrate-based agglomerate is selected from the group consisting of dextrose agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of at least 20.

3. The composition of claim 1, wherein said liquid antifoaming or defoaming composition is taken up by the agglomerated carbohydrate particles by sorption.

4. The composition of claim 1, wherein said combinate is comprised of one or more carbohydrate-based agglomerates having a particle size of less than about 850 microns with a majority greater than about 420 microns.

5. The composition of claim 1, wherein said combinate further includes one or more excipients.

6. The composition of claim 1, comprising about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent liquid antifoaming or defoaming composition.

7. The composition of claim 1, wherein said liquid antifoaming or defoaming composition comprises a hydrocarbon-based oil.

8. The composition of claim 1, wherein said liquid antifoaming or defoaming composition comprises mineral oil.

9. The composition of claim 1 wherein said liquid antifoaming or defoaming composition comprises silicone oil.

10. The composition of claim 1, wherein said liquid, nonaqueous, antifoaming or defoaming composition is a silicone oil containing silica in an amount up to about 50 weight percent of the composition.

11. The composition of claim 1, wherein said liquid, nonaqueous, antifoaming or defoaming composition is a hydrocarbon-based oil containing silica in an amount up to about 50 weight percent of the composition.

12. An antifoaming or defoaming composition comprising a dry, uniform, free flowing granular combinate of at least about 50 weight percent water soluble carbohydrate-based agglomerate select ed from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerated sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of least 20, substantially having a particle size of less than about 850 microns and simethicone in an amount up to about 50 weight percent.

13. The composition of claim 12, wherein said simethicone is taken up by the agglomerated carbohydrate-based particles by sorption.

14. The composition of claim 12, comprising about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent simethicone.

15. The composition of claim 12, wherein said combinate further includes one or more excipients.

16. The composition of claim 12, wherein said combinate is prepared as a unit dose compressed tablet, capsule, or granule.

17. The composition of claim 12, wherein said water soluble carbohydrate-based agglomerate is selected from the group consisting of maltodextrin/dextrose co-agglomerates, maltodextrin/sucrose co-agglomerates, and maltodextrin/fructose co-agglomerates.

18. The composition of claim 12, wherein said water soluble carbohydrate-based agglomerate is selected from the group consisting of dextrose agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of at least 20.

19. An antifoaming or defoaming composition consisting essentially of a dry, uniform, free flowing granular combinate of: 1) a water soluble carbohydrate-based agglomerate selected from the group consisting combinations of maltodextrin with dextrose, sucrose or fructose, and 2) a liquid, nonaqueous, antifoaming or defoaming composition selected from the group consisting of hydrocarbon-based oils containing silica and silicone oils containing silica in an amount up to about 50 weight percent of the composition.

20. The composition of claim 19, wherein said combinate is comprised of one or more carbohydrate-based agglomerates having a particle size of less than about 850 microns with a majority greater than about 420 microns.

21. The composition of claim 19, comprising about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent liquid antifoaming or defoaming composition.

22. An antifoaming or defoaming composition consisting essentially of a dry, uniform, free flowing granular combinate of at least about 50 weight percent water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, maltodextrin/sucrose co-agglomerates, and maltodextrin/fructose co-agglomerates, substantially having a particle size of less than about 850 microns and simethicone in an amount up to about 50 weight percent.

23. An antifoaming or defoaming composition consisting essentially of: 1) a dry, uniform, free flowing granular combinate of a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E of a least 20; and 2) an antifoaming or defoaming composition comprising silicone oil.

24. The composition of claim 23, wherein said antifoaming or defoaming composition comprises silicone oil containing silica.

25. The composition of claim 23, wherein said combinate comprised of one or more carbohydrate-based agglomerates having a particle size of less than about 850 microns with a majority greater than about 420 microns.

26. The composition of claim 23, comprising about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent liquid antifoaming or defoaming composition.

27. A process for producing an antifoaming or defoaming combinate, comprising mixing a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates sorbitol agglomerates, agglomerates of hydrolyzed cereal solids and agglomerates of corn syrup solids having a D.E. of at least 20, with a liquid, nonaqueous, antifoaming or defoaming composition selected from the group consisting of hydrocarbon-based oils, mineral oils and silicone oils to form a dry, uniform, free flowing granular combinate.

28. The process of claim 27, wherein said carbohydrate-based agglomerate is selected from the group consisting of dextrose agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of at least 20.

29. The process of claim 27, wherein said liquid antifoaming or defoaming composition is taken up by the carbohydrate-based agglomerate particles by sorption.

30. The process of claim 27, wherein said combinate is comprised of one or more carbohydrate-based agglomerates having a particle size of less than about 850 microns with a majority greater than about 420 microns.

31. The process of claim 27, further including the step of blending one or more excipients with said combinate.

32. The process of claim 27, comprising mixing about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent liquid antifoaming or defoaming composition.

33. The process of claim 27, wherein said liquid antifoaming or defoaming composition comprises a hydrocarbon-based oil.

34. The process of claim 27, wherein said liquid antifoaming or defoaming composition comprises mineral oil.

35. The process of claim 27, wherein said liquid antifoaming or defoaming composition comprises silicone oil.

36. The process of claim 27, wherein said liquid, nonaqueous, antifoaming or defoaming composition is a silicone oil containing silica in an amount up to about 50 weight percent of the composition.

37. The process of claim 27, wherein said liquid, nonaqueous, antifoaming or defoaming composition is a hydrocarbon-based oil containing silica in an amount up to about 50 weight percent of the composition.

38. A process for producing an antifoaming or defoaming combinate, comprising mixing at least about 50 weight percent of a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E, of at least 20, substantially having a particle size of less than 850 microns with simethicone in an amount up to about 50 weight percent to form a dry, uniform, free flowing granular combinate.

39. The process of claim 38, wherein said simethicone is taken up by the carbohydrate-based agglomerate particles by sorption.

40. The process of claim 38, further including the step of blending one or more excipients with said combinate.

41. The process of claim 38, comprising mixing about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent simethicone.

42. The process of claim 38, further including the step of preparing said combinate as a unit dose compressed tablet, capsule, or granule.

43. The process of claim 38, wherein said water soluble carbohydrate-based agglomerate is selected from the group consisting of maltodextrin/dextrose co-agglomerates, maltodextrin/sucrose co-agglomerates, and maltodextrin/fructose co-agglomerates.

44. The process of claim 38, wherein said water soluble carbohydrate-based agglomerate is selected from the group consisting of dextrose agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of at least 20.

45. A process for producing an antifoaming or defoaming combinate consisting essentially of mixing a water soluble carbohydrate-based agglomerate selected from the group consisting of combinations of maltodextrin with dextrose, sucrose or fructose, with a liquid, nonaqueous, antifoaming or defoaming composition selected from the group consisting of hydrocarbon-based oils containing silica and silicone oils containing silica in an amount up to about 50 weight percent of the composition to form a dry, uniform, free flowing granular combinate.

46. The process of claim 45, wherein said combinate is comprised of one or more carbohydrate-based agglomerates having a particle size of less than about 850 microns with a majority greater than about 420 microns.

47. The process of claim 46, comprising about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent liquid antifoaming or defoaming composition.

48. A process for producing an antifoaming or defoaming combinate consisting essentially of mixing at least about 50 weight percent of a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, maltodextrin/sucrose co-agglomerates, and maltodextrin/fructose co-agglomerates, substantially having a particle size of less than 850 microns with simethicone in an amount up to about 50 weight percent to form a dry, uniform, free flowing granular combinate.

49. A process for producing an antifoaming or defoaming combinate consisting essentially of mixing a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/fructose co-agglomerates, dextrose agglomerates, maltodextrin-sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E of at least 20 with a liquid, nonaqueous, antifoaming or defoaming composition comprising silicone oil to form a dry, uniform, free flowing granular combinate.

50. The process of claim 49, wherein said antifoaming or defoaming composition comprises silicone oil containing silica.

51. The process of claim 49, wherein said combinate is comprised of one or more carbohydrate-based agglomerates having a particle size of less than about 850 microns with a majority greater than about 420 microns.

52. The process of claim 49, comprising about 50 to 90 weight percent carbohydrate-based agglomerate and about 10 to 50 weight percent liquid antifoaming or defoaming composition.

53. A method of defoaming an aqueous medium comprising contacting said aqueous medium with an antifoaming or defoaming composition comprising a dry, uniform, free flowing granular combinate of a water soluble carbohydrate-based agglomerate and a liquid, nonaqueous, antifoaming or defoaming composition selected from the group consisting of hydrocarbon-based oils and silicone oils, wherein said carbohydrate-based agglomerate is selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids and agglomerates of corn syrup solids having a D.E. of at least 20.

54. The method of claim 53, wherein said carbohydrate-based agglomerate is selected from the group consisting of dextrose agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of at least 20.

55. The method of claim 53, wherein said liquid, nonaqueous, antifoaming or defoaming composition is selected from the group consisting of hydrocarbon-based oils containing silica and silicone oils containing silica.

56. The method of claim 55, wherein said liquid, nonaqueous, antifoaming or defoaming composition is a silicone oil containing silica.

57. The method of claim 55, wherein said liquid, nonaqueous, antifoaming or defoaming composition is a hydrocarbon-based oil, containing silica.

58. A method of defoaming an aqueous medium comprising contacting said aqueous medium with an antifoaming or defoaming composition comprising a dry, uniform, free flowing granular combinate of at least about 50 weight percent water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E. of at least 20, substantially having a particle size of less than about 850 microns and simethicone in an amount up to about 50 weight percent.

59. The method of claim 58, wherein said combinate further includes one or more excipients.

60. The method of claim 58, wherein said combinate is in the form of a unit dose compressed tablet, capsule, or free flowing granules.

61. Use of an antifoaming or defoaming composition of an antifoaming or defoaming composition for treating flatulence, wherein said antifoaming or defoaming composition comprises a dry, uniform, free flowing granular combinate of at least about 50 weight percent water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids having a D.E of at least 20, substantially having a particle size of less than about 850 microns and simethicone in an amount up to about 50 weight percent.