CA1139221A - Antacid compositions - Google Patents

Antacid compositions

Info

Publication number
CA1139221A
CA1139221A CA000337031A CA337031A CA1139221A CA 1139221 A CA1139221 A CA 1139221A CA 000337031 A CA000337031 A CA 000337031A CA 337031 A CA337031 A CA 337031A CA 1139221 A CA1139221 A CA 1139221A
Authority
CA
Canada
Prior art keywords
organopolysiloxane
composition
antacid
powder
silica
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
CA000337031A
Other languages
French (fr)
Inventor
Vijay B. Surpuriya
Colleen A. Gonyo
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wyeth LLC
Original Assignee
American Home Products Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by American Home Products Corp filed Critical American Home Products Corp
Application granted granted Critical
Publication of CA1139221A publication Critical patent/CA1139221A/en
Expired legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08KUse of inorganic or non-macromolecular organic substances as compounding ingredients
    • C08K3/00Use of inorganic substances as compounding ingredients
    • C08K3/34Silicon-containing compounds
    • C08K3/36Silica

Abstract

ABSTRACT OF THE DISCLOSURE

An antacid chewable tablet containing an antacid, an organopolysilo-xane and silica, present in specified amounts, is described.

The disclosed formulation provides a product which has rapid defoatn-ing action; The tablet is prepared by adding the organopolysiloxane and silica, premixed in powder form, to an antacid. Additionally, the premixed powder can be used as an antiflatulent alone or in combination with other medicinal agents.

Description

113~aZZl ANTACID COMPOSITIONS

BACKGROUND OF THE INVENTION

a) Field of the Invention This invention relates to irnproved antacid compositions containing an organopolysiloxane. More specifically, this invention relates to a method for 10 combining the organopolysiloxane with silica resulting in a powder. This powder is then combined with an antacid and compressed into tablets. The powder can also be used as an antiflatulent alone or in combination with other medicinal agents.

b) Description of the Prior Art The use of organopolysiloxanes in antacid compositions is old in the art. For instance, U.S. Reissue Patent 25,205 describes the use of organopolysiloxanes with antacids. U.S. Patents 3,210,208 and 3,382,150 20 describe methods for preparing coated organopolysiloxane particles. Both of these patents utilize an emulsion of organopolysiloxane, a nontoxic coating material and water. The emulsion is spray-dried to form particles of organopolysiloxane which is then coated with the coating material. U.S.
3,501,571 describes a method for absorbing organopolysiloxanes on an inert 25 absorbent filler such as sugar or mannitol, granulating the resulting mixture and then drying the mixture which results in the organopolysiloxane in a powder form.

, ~ 39~22:~

All of the above methods require either some form of liquid to form an emulsion or granulation of the organopolysiloxane material and use of an inert absorbent filler. The above methods then require a spray drier or oven to dry the material. This is both time consuming and costly.

U. S. 3,422,189 describes anti-flatulent compositions which contain an organopolysiloxane and finely divided silica or a silica aerogel. The finely divided silica is used in amounts sufficient to form a viscous mixture with the organopolysiloxane resulting in a honey-like or salve-like consistency.
A weight range, based on the organopolysiloxane employed, of 1-10% is 10 employed with a range of about 3 - 7% being preferred. British Patent 1,047,470 describes defoaming compositions which are prepared by adding finely divided silica to a polysiloxane component and heating this mixture to disperse the silica. The silica is disclosed as being present in an amount of at least 3% by weight.

SUMMARY OF THE INVENTION

It has now been discovered that substantially uniform and spherical particles in powder form comprising an organopolysiloxane and silica can be prepared without the use of liquid or heat. The novel silica and organopolysiloxane powder of this invention consists essentially of organo-20 polysiloxanes, from about 1% to 70%, preferably from about 5% to about6n%, and more particularly about 15% to about 60% by weight of the final powder. The novel powder can then be formulated with suitable excipients to form an antiflatulent tablet composition or can be mixed with an antacid and compressed into tablets. The novel powder of the invention can also be 25 mixed with excipients or other medicinal agents and excipients and used in 1~39221 various pharmaceutical forms. The use of this amount of silica results in a uniform powder and distinguishes~this formulation from prior combinations of silica and organopolysiloxanes.

Detailed Description of the Invention The organopolysiloxane type compound that is utilized in this novel formulation is usually a liquid, oily or semi-solid organopolysiloxane represented~by the following formula.

R R R

R - Si - O - Si - O - Si - R

R R n wherein R is a lower alkyl group having from 1 to 5 carbon atoms or an organic radical such as phenyl and n can be 0 to 2000. A preferred organopolysiloxane is simethicone which is a mixture of fully methylated 15 linear siloxane polymers containing repeating units of the formula [-(CH3)2-Si ~]n' stabilized with trimethylsiloxy end-blocking units of the formula UCH3)3-Si O-] and silicon dioxide. Simethicone contains at least 93.0 percent and not more than 99.0 percent of [ ~CH3)2-Si ~] n (dimethylpolysiloxane), and at least 4.0 percent and not more than 7.0 20 percent of silicon dioxide.

~,..

1~39ZZl r Suitable antacids which can be utilized in this invention include magaldrate, magnesium hydroxidè, aluminum hydroxide, magnesium carbo-nate, calcium carbonate, magnesium oxide, magnesium trisilicate, alumi-num phosphate, dihydroxy aluminum aminoacetate, bismuth subcarbonate 5 and combinations thereof. The preferred antacid of this invention is magaIdrate.

The finely divided silica used in this invention are available from various commercial sources. A preferred source of silica is sold under the trademark CAB-O-SIL and is a submicroscopic fire-dried fumed silica. The 10 particle size can vary from 70 to 500 angstroms in diameter.

As has been noted before, the organopolysiloxane powder of this invention can be incorporated with an antacid in the formulation of a chewable antacid tablet. A preferred method of preparation of this tablet is to add sucrose to a simethicone-silica powder before mixing with the 15 antacid. A preferred formula for 1000 tablets is listed below:

In~redient Amount Magaldrate, U.S.P. 470.0 g Simethicone N.F. 23.2 g Silica, Colloidal 17.37 g Sucrose, Powdered 153.0 g Methylcellulose, U.S.P., 15 cps 1.34 g Dextrates, Hydrous 500.0 g Polyethylene Glycol 6000, U.S.P., Milled 120.0 g Spearmint, Aromalok 26380, Fritzsche 4.0 g Magnesium Stearate, U.S.P. 5.4 g Water, U.S.P., Purified 28.0 ml Theoretical Tablet Weight 1,294. mg ~13~Z2~

The term "theoretical tablet weight" is used because all commercial dimethylpolysiloxanes are somewhat volatile. Recently, low volatility dimethylpolysiloxane has been introduced on the market and this product appears to perform better.
As can be seen from the above formulation, pharmaceutically inert ingredients such as extenders, binders, lubricants, coloring agents, flavo-rings and the like can be added to the antacid formulation. Examples of pharmaceutically inert ingredients which can be added to the antacid formulation include extenders or diluents such as lactose, mannitol, 10 sorbitol, microcrystalline cellulose and starch. Examples of binders that can be added to the formulation of this invention are natural gums and gum constituents such as acacia, tragacanth, agar, and pectin; proteinaceous materials such as gelatin, casein, and zein; polyvinylpyrrolidone; cellulose compounds; and starch. Examples of lubricants that can be used are 15 calcium stearate, talc, stearic acid, sodium benzoate or mixtures thereof.
The uniform powder of this invention is simply prepared by blending the simethicone with the silica in a suitable blender until uniform. The simethicone silica powder is then as, previously noted preferrably granu-lated with sucrose prior to formulation of an antiflatulent dosage form 20 alone or formulation of a combination antacid anti~latulent dosage form.
More specifically, the above formulation is prepared in the following manner and is illustrative of the manner of preparation for all the compo-sitions encompassed by this invention.

~39~

1. Heat about 14 ml of Purified Water to 80 - 90 C. Add Methylcellulose, 15 cps, and stir until uniformly dispersed. Bring up to a volume of 28 ml with Purified Water and cool to room temperature.
2. Blend the simethicone with Colloidal Silica in a suitable blender 5until uniform.
3. Blend the mixture from Step #2 with Powdered Sucrose in a suitable blender until uniform.
4. Granulate the blend from Step #3 with the solution prepared in Step #1, adding additional Purified Water if necessary to obtain suitable 10granulation.
5. Dry the granulation from Step #4 overnight at 45 C in a forced draft dryer and pass through a Fit2 Mill using a #20 screen, medium speed, knives forward.
6. Blend Magaldrate Powder, Dextrates Hydrous, Polyethylene Glycol 156000 Milled and Spearmint Aromalok 26380. Pass through a Fitz Mill using a #16 screen, medium speed, knives forward.
7. Blend the ingredients from Step #5 and #6 in a suitable blender until uniform.
%. Add the Magnesium Stearate and blend.
209. Compress to make a tablet.
Rxamples of other medicinal agents which can be used in combination with an organopolysiloxane powder include the following:

113922~

l. Digestants such as bile constituents, pancreatin, pepsin, and digestive enzymes such as amylase, lipase and protease.

2. Antichoïinergic Agents such as atropine sulfate, hyoscyamine sulfate, scopolamine hydrobromide and mixed alkaloidal extracts.

3. Barbiturates such as phenobarbital and butabarbital sodium.

The following examples further illustrate the above described invention:

EXAMPLE I

Simethicone 800 g Colloidal Silica 600 g Mix simethicone and the colloidal silica together in a suitable mixer with high shear. The resulting mixture is a powder. It is understood that this powder can be prepared by dissolving simethicone in a suitable solvent as taught by the prior art, dispersing the simethicone on the silica and evaporating the solvent.
EXAMPLE II
The powder as prepared in Example I can be mixed with antacids such as magaldrate and pharmaceutically inert ingredients and compressed into tablets. This example illustrates such a preparation.
Simethicone Powder from Example I 35.0 g 20 Magaldrate 470.0 g Powdered Sucrose 70.0 g PEG 6000 120.0 g Dextrates, Hydrous 425.0 g Sorbitol 100.0 g 25 Saccharin 0.3 g Spearmint 4.0 g Magnesium Stearate 5.4 g Theoretical Tablet Weight 1229.7 mg 1139ZZl All the ingredients except magnesium stearate were mixed in a suitable mixer. The magnesium stearate was blended in and all the ingredients were compressed.

EXAMPLE III

Simethicone powder as described in Example I can first be mixed with d pharmaceutically inert ingredient, granulated with a binder and dried and sized to convert the mixture into granules Simethicone - 400.0 g Colloidal Silica - 300.0 g 10 Powdered Sucrose - 2625 g 5% Methylcellulose (15 cps) Aq. Sol. - 450.0 ml The simethicone and colloidal silica were mixed in a suitable mixer with high shear. The powdered sucrose was added and mixed well. Granulate the mixture with 450 ml of 5% methylcellulose aqueous solution and dry it 15 in a forced air oven at 45 C. Size the dried material by passing through a suitable screen.

EXAMPLE IV

Simethicone granules as prepared in Example III can be mixed with antacids and pharmaceutically inert ingredients and compressed to make 20 tablets as follows:
Simethicone Granules from Example III 167.38 g Magaldrate 470.0 g Dextrates, Hydrous 500.0 g PEG 6000 120.0 g 25 Spearmint 4.0 g Magnesium Stearate 5.4 g Theoretical Tablet Weight1266.7~ mg This formulation is prepared as in Example II.

~39ZZl EXAMPLE V
Simethicone Powder from Example I 140.0 g Dextrates, Hydrous 600.0 g Polyethylene Glycol 6000 80.0 g Spearmint Elavor 2.7 g Magnesium Stearate 2.0 g Theoretical Tablet Weight824.7 mg All the ingredients except Magnesium Stearate were mixed in a suita-ble mixer. The Magnesium Stearate was blended in and all the ingredients 10 were compressed.

EXAMPLE VI

Simethicone Granulation from Example III 669.5 g Spearmint Flavor 2.7 g Magnesium Stearate 2.0 g Theoretical Tablet Weight 674.2 mg The Simethicone Granulation and Spearmint were mixed in a suitable mixer. The Magnesium Stearate was blended in and all the ingredients were compressed.
Examples V and VI illustrate anti-flatulent formulations.

Claims (15)

The embodiments of the invention in which an exclusive property or priviledge is claimed are defined as follows:
1. A pharmaceutical composition comprising a uniform and spherical powder consisting essentially of an organopolysiloxane and finely divided silica wherein the organopolysiloxane is present in an amount from 1% to about 70%
based on the weight of the final powder and a pharmaceutically acceptable excipient.
2. The composition of claim 1 wherein the organopolysiloxane is present in an amount from about 5% to about 60%.
3. The composition of claim 1 wherein the organopolysiloxane is present in an amount from about 15% to about 60%.
4. The composition of claim 1 wherein said excipient is sucrose.
5. The composition of claim 1 wherein the organopolysiloxane is simethicone.
6. The composition of claim 1 and a medicinal agent.
7. The composition of claim 6 wherein said medicinal agent is an antacid.
8. A compressed tablet comprising the composition of claim 1 and an antacid.
9. The tablet of claim 8 wherein the antacid is magaldrate.
10. A method for preparing the composition of claim 1 which com-prises blending in the absence of heat or a solvent about 1% to about 70% of an organopolysiloxane with silica to obtain a uniform and spherical powder com-prising from about 1% to 70% of the organopolysiloxane and granulating the powder with a pharmaceutically acceptable excipient.
11. The method of claim 10 wherein said pharmaceutically acceptable excipient is sucrose.
12. The method of claim 10 in which the organopolysiloxane is simethi-cone.
13. The method of claim 10,11 or 12 wherein the organopolysiloxane is present in an amount from about 15% to 60%.
14. A pharmaceutical composition comprising a uniform and spherical powder consisting essentially of an organopolysiloxane and finely divided silica wherein the organopolysiloxane is present in an amount from about 1% to about 70% based on the weight of the final powder and a medicinal agent.
15. The composition of claim 14 wherein said medicinal agent is an antacid.
CA000337031A 1978-10-10 1979-10-04 Antacid compositions Expired CA1139221A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US95033278A 1978-10-10 1978-10-10
US950,332 1978-10-10

Publications (1)

Publication Number Publication Date
CA1139221A true CA1139221A (en) 1983-01-11

Family

ID=25490285

Family Applications (1)

Application Number Title Priority Date Filing Date
CA000337031A Expired CA1139221A (en) 1978-10-10 1979-10-04 Antacid compositions

Country Status (7)

Country Link
CA (1) CA1139221A (en)
CY (1) CY1314A (en)
DE (1) DE2940905A1 (en)
GB (1) GB2033915B (en)
HK (1) HK102585A (en)
KE (1) KE3574A (en)
MY (1) MY8600315A (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5599577A (en) * 1992-05-21 1997-02-04 Mcneil-Ppc, Inc. Simethicone containing pharmaceutical compositions
US6038608A (en) * 1996-11-25 2000-03-14 Nec Corporation Virtual LAN system
US7341742B2 (en) 2002-09-30 2008-03-11 L. Perrigo Company Simethicone containing tablet composition and method

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0068566B1 (en) * 1981-06-30 1984-11-21 Sociéte d'Importation de Parfumerie et de Produits Pharmaceutiques en abrégé "Sipar-Pharma" Société Anomyme Edible pharmaceutical form of a composition of matter containing a fluid dimethyl polysiloxane
US4396604A (en) * 1982-05-17 1983-08-02 Norcliff Thayer, Inc. Simethicone antacid lozenge
FR2559063B1 (en) * 1984-02-08 1987-03-06 Leribault Loic COMPOSITIONS FOR THERAPEUTIC USE COMPRISING ORGANO-SILICATED COMPOUNDS
US5173305A (en) * 1985-03-06 1992-12-22 Grimberg Georges Serge Composition for protection of oesogastroduodenal mucous membrane
FR2578423B1 (en) * 1985-03-06 1988-12-30 Grimberg Georges GUAR GUM-BASED PHARMACEUTICAL COMPOSITION FOR THE PROTECTION OF THE OESO-GASTRO-DUODENAL MUCOSA
MD407C2 (en) * 1989-01-19 1996-06-30 Schmidt Alfred Remedy for gullet inflammation and stomach-intestinal tract inflammatory and ulcerated diseases treatmen
KR920002149A (en) * 1990-07-03 1992-02-28 안드레아 엘. 콜비 Pharmaceutical compositions for alleviating the symptoms of gastrointestinal disorders caused by nonsteroidal anti-inflammatory drugs and methods for alleviating the same
DE4140116A1 (en) * 1991-12-05 1993-06-09 Bolder Arzneimittel Gmbh DIMETICON PASTILLES
GB9310412D0 (en) * 1993-05-20 1993-07-07 Danbiosyst Uk Nasal nicotine system
FR2705966B1 (en) * 1993-06-04 1995-08-25 Dow Corning Sa Antifoam compositions useful in particular for the treatment of gastric disorders.
DE4415999A1 (en) * 1994-05-06 1995-11-09 Bolder Arzneimittel Gmbh Gastric acid-binding chewing pastilles
AU3968697A (en) * 1996-07-26 1998-02-20 Kristine A. Bateman Dietetic one-to-one sugar substitute composition for table top, baking and cooking applications

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5599577A (en) * 1992-05-21 1997-02-04 Mcneil-Ppc, Inc. Simethicone containing pharmaceutical compositions
US5679376A (en) * 1992-05-21 1997-10-21 Mcneil-Ppc, Inc. Simethicone containing pharmaceutical compositions
US5716641A (en) * 1992-05-21 1998-02-10 Mcneil-Ppc, Inc. Simethicone containing pharmaceutical compositions
US5980944A (en) * 1992-05-21 1999-11-09 Mcneil-Ppc, Inc. Simethicone containing pharmaceutical compositions
US6038608A (en) * 1996-11-25 2000-03-14 Nec Corporation Virtual LAN system
US7341742B2 (en) 2002-09-30 2008-03-11 L. Perrigo Company Simethicone containing tablet composition and method

Also Published As

Publication number Publication date
HK102585A (en) 1986-01-03
KE3574A (en) 1985-11-22
MY8600315A (en) 1986-12-31
GB2033915A (en) 1980-05-29
CY1314A (en) 1986-03-28
DE2940905A1 (en) 1980-04-30
GB2033915B (en) 1983-02-09

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