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Publication numberUS3108043 A
Publication typeGrant
Publication dateOct 22, 1963
Filing dateMay 9, 1960
Priority dateMay 9, 1960
Publication numberUS 3108043 A, US 3108043A, US-A-3108043, US3108043 A, US3108043A
InventorsMillman Nathan, Homm Roger Edwin
Original AssigneeOrtho Pharma Corp
Export CitationBiBTeX, EndNote, RefMan
External Links: USPTO, USPTO Assignment, Espacenet
Spermicidal sheet-like material
US 3108043 A
Abstract  available in
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Claims  available in
Description  (OCR text may contain errors)

United States Patent 3,108,043 SPERMICIDAL SHEET-LIKE MATERIAL Nathan Millmau, Somerville, and Roger Edwin Homm,

N eshanic, NJ assignors to Ortho Pharmaceutical Corporation, a corporation of New Jersey No Drawing. Filed May 9, 1960, Ser. No. 27,507 7 Claims. (Cl. 167-58) The present invention relates to a novel and improved spermicidal manufacture for treatment of the vaginal cavity to be acted on by the body fluids and provide a convenient and effective spermicidal composition.

Objects and advantages of the invention will be set forth in part hereinafiter and in part will be obvious herefrom, or may be learned by practice with the invention, the same being realized and attained by means of the steps, processes and compositions pointed out in the appended claims.

The invention consists in the novel steps, processes, compositions and improvements herein shown and described.

The present invention has for its object the provision of a novel and improved composition and article of manuiacture for the convenient treatment of the vaginal cavity to provide it with a readily available and regulated amount of a spermicidal material. A further object is the provision of an economical and conveniently usable material which is adapted to dissolve at a controlled rate in the normal fluids available in the vaginal cavity thereby supplying the cavity with a regulated amount of spermicide. Still another object is the provisionv of a solid material which is substantially 'dry, may be inexpensively packaged, which requires no apparatus for its 3,108,043 Patented Oct. 22, 1963 ice 2 a suitable water soluble spermicide, such as a non-ionic detergent.

The weight ratio of spermicide to vehicle may be as great as 121. It has been found that many spermicides are not compatible with the vehicle when present in larger quantities. The minimum amount of spermicide present should not be less than 5 milligrams per application. Thus, if the total weight of a single film or team designed for one application were 720 milligrams, the minimum amount of spermicide present should not be less than 5 milligrams. Another way of expressing this relationship is that the weight ratio of spermicide to total solids is not less than about 1:145.

Any water soluble, non deleterious spermicide may be used, but the non-ionic detergent spermicides are preferred and are selected from the group consisting of diisobutylphenoxypolyethoxyethanol described in United States Patent No. 2,752,284, alkylated aryl polyether alcohols, sodium alkylaryl polyether sulfates, and nonylphenoxypolyethoxyethanol.

It is preferred that a suitable plasticizer or humectant be added to the water soluble vehicle to render the unmoistened sheet material more pliable and less likely to cause damage to any body tissue with which it may come in contact. Suitable materials for this purpose are glycerol, sorbitol, polyethylene :glycols of high molecular weight and other bland, non-deleterious, hygroscopic liquids which are compatible with the film-forming material. The weight ratio of glycerol to vehicle may be as much as 1213 or as little as 1:3. Larger amounts of glycerol are not readily compatible with the vehicle proper and effective use, and which is without deleterious eiiect on the tissues with which it may remain in contact.

According to the present invention the spermicidal manufacture comprises a non-deleterious, bland mass, which is soluble in the body fluids available in the vaginal cavity at a controlled rate of solution and which incorporates within it an effective amount of a spermicide, together, if desired, with a suitable humectant or plasticizing agent for the mass to maintain the mass in a more pliable, less rigid condition. The spermicidal manufacture is formed into sheets or foams in such a manner that it has an extremely large surface area with respect to its mass, thereby increasing not only the rate at which it may be dissolved on contact with the body fluids, but also rendering the mass more pliable and less likely to cause damage to the tissues with which it comes in contact.

The water soluble solid material which forms the vehicle for the spermicide and which forms the mass is a bland, non-deleterious, solid, tilm forming material, which is readily soluble in water and the body fluids with which it comes in contact within the vaginal cavity. Among the soluble materials which havebeen found suitable are the various viscosity grades of sodium carboxymethylcellulose and methylcellulose. The sodium carboxymethylcellulose and methylcellulose used are of grade having a viscosity of from 25 to 10,000 centipoises per second in a 2% aqueous solution at 25 'C., and preferably such that a 2% by weight solution in water at 25 C. has a viscosity of from 25 to 50 centipoises per second, although other grades with similarly measured viscosities of trom 50 to 10,000 centipoises per second are usable in certain formulations. Alternatively, they may be employed as vehicles, if desired, other water soluble nonputrefying, bland, film-forming, sol-id materials such as alginates, cellulose acetate, sorbate, and polyvinyl alcohol (4-6 c.p.s.).

The water soluble vehicle is dissolved and mixed with and smaller amounts of glycerol do not produce the desired flexibility.

The solubility of the composition and articles of the present invention in water and body fluids may be controlled by the presence in the vehicle of urea. The amount of urea should be such that a 3-inch square film of the vehicle will dissolve in water at 37 C. in less than seconds. The weight ratio of urea to vehicle may be as much as 1:3 or as little as 1:4. If the ratio of urea to vehicle is greater than 1:3, discontinuity may appear in the cast film. It the ratio of urea to vehicle is less than 124, the rate of solubility may be too slow.

The spermicidal manufacture may be formed as a filmlike sheet, or as a sheet of foam, but in any event has an extremely large ratio of surface to volume so that it has a large surface which may be acted upon by the solvent fluids to speed the process of dissolution upon contact with the vaginal fluids.

'In use, a suitable quantity of the sheet-like material comprising the water soluble sheet containing the spermicide is compacted, either by rolling or by crumpling, and is introduced into the vaginal cavity and immediately begins to dissolve and thus provides a viscous, retained gel, having effective spermicidal activity, on the vaginal Walls.

In general, the material of the present invention comprises a sheet of the water soluble vehicle, either sodium carboxymethylcellulose or methylcellulose. The sodium carboxymethylcellulose or methylcellulose which forms the vehicle is preferably dissolved in water to form a solution containing from 0.5% to 12.0% of vehicle solids, together with urea, a humectant such as glycerol, ethylene glycol or sorbitol and a spermicide in the proportions described above.

Where the sheet material is to be in the form of a film, the solution may be poured or otherwise fed onto a heated surface to the correct thickness to give the desired film thickness after drying, and the water is then evaporated by gently heating of the support and the solution carried thereby. The solution is deposited in such in the solu- 1grams-- -inches square 0 carboxying:

The ratio of the working examples and the process by ing spec surface, as is customary The ratio of glycerol (or the follow y be cast and dried upon a lar g of continuous webs' of film. re of the present invention ylene glycol) do 220 the dried film to sodium carbox The ratio of urea t um carboxymethylcellulose ch the spermicidal materials of the ither the non-foamed or the foamed g a polished in whi y be prepared,

will function as foaming agents ng now in detail to various mi1liliters 46.2

solution is dried to form a film 3 rri Conveniently, e

A spermicide manufactu This Refe

agents and tion described sheet-like material rna heated cylinder havin in connection with the castin is made from a water solution compris Sodium carboxymethylcellulose mill Nonylphenoxypolyethoxyethanol Glycerine (or polyeth Urea Water and about 0.005 inch in thickness. spermicide present in methylcellulose is methylcellulose is also 1:3.

is about 1:1.36.

of the manner present invention ma which they may be prepared 20 polyethylene glycol) to sodi will be apthe boiling point is a sheet, relatively tion, while its other to assist in the its ingredients, after The heated surface is just slightly below e foam is destro dded strength to the 15 the sheet or film is dried goven or chamber. In the ying, the dried film will have a h to 0.0075 inch and which apidly than films having a greater Sheets of dried foamed material absorb moisture more 5 supple and in many cases may reason. Such foams or foamed lently beating air into the prising all of aterial is poured out onto a hot y eventually be separated, after is dried.

yed immediately adjagive a Thereafter,

, the preferable form inch to 0.240 inch thickness) which has y continuous and not interru -like or cellular forma surface exhibits the normal appearance of a dried foam.

Foaming agents may of course be used manufacture of a foamed spermicide.

ermicides are surface active 2 thickness that after dr thickness of from 0.001 inc will dissolve more I thickness.

be preferred for this sheet may be produced by vio prepared solution com which the foamed m surface from which it ma of water so that th cent the supporting surface to sheet as a whole.

in any conventional dryin case of a foam thin (from 0.005

one of its faces substantiall ed by any foam 0 050 3 730 0000 mnmnohw 00 0 0 2410 0 05 2 L09 11112 3 L1L 1111 6 210 2 11112 7 2 10w 2 n 3 n 4 n n 0 5 0 024: 0 fi v0 332 0 05 0 2410 0000 m. 1 0 .1 1111 2 1111 2 L0 2 11112 3111 2 m 5 3 5 mw73 0 0 0 331." 0 05 0 2410 000 w w 0 0 .0 nl mmmlL W 1 .1 1111 A 2 L0 9 11112 3L1 2 n 11 5 0060 2410 m005 0m2410 000 w 0 m 2 L0 2 11112 2L0 2 11112 M 3 L1 2 n 0 0 000 3445 0 05 0 2410 M000 m m 2 m 43 0 11127 3 2 10 211112 4. 311 2 1 0 0 000 3465 0 06 0 2410 0 00 n m N m 432 11117 M 2 10 2 11112 Q 4 31 m 0 000 KU 0 000 mmeo wa a 0 05 0 WJAJO 0 00 m 2 4; 1 111 7 8 2 13 1 .111 7 0 2 L0 2 11112 1 4 3 L 0 005 mnwnm ro 0 005 34 5 0 030 m m23w0 0 00 N. r 0 050 53 0 0 0 0 n 7310 0 050 m 5450 0 %5 m 5 215 lflflmlnu w 5 3 5 1 115 m 022 n 1.3115 3 2 0 n 0 050 2410 0 060 5110 0 300 m 3320 0 5 0 3410 2 102 11112 5 5 215 12315 7 0 3 3 5 113 .15 8 2 .0 2 11112 1 P| 2 1 u h 3 0 n 1 n u 0 0 0 2415 0 000 MOO O m 535 0 003410 b .2... 6. 0: i 1 11 4 l 6 s 1 5 1 1 1 1 1 m 34 2 052 1 M lflll MM 2 0 211112 n n 1 m 5 um5 m23m0 0 0%0 m0000 m 244 m n n n 0 .0 113 L 3 5 2 .5 5 4 L1 1111 n n n 00 1 1 1 2 v 1 n n u n e nnnu 6 u n n e a n h n a n n n n a n n a u 0 o o o 0 P D. D. .1 1 1 .r. t. t t H D 1 n 1 D l MT" m "II" w e n n 0 0 m I "II nh f M n mM um m wm rm 5 mm i y l 1 1 6M" o. c 0 9R m o n 0 0w ent w m we m n E mm "wh s N mm m mpm mamm" m m m m mm mmIomm m m m mm 0 1H h SM O 1 u h S 0 f h S 6 1 1 a 1 y a t h a N n by. m N H t V.r. N H 1 r m 0H by S 8 0! 92 9 .1 C0 .BXBM F 09 1 1c. yoh .6. oh m 0 V.oh 1c yoh 1 YO 11t m l l t .l th m i th mm 0 i 0 0 t 0 .0 0 0 i m ay lm m m ay u m e m m new i r 1 mwl F 1 mi n d e yylv. Ie X 4 X ..X 0 4. .10 l. 0P c oD e 0D e o c we m 1 r m .1 m l nmrm eunm l nmflm e mwmpimm e fl u m w. m m mt .mned xm. eyy mnmm m m mmwu m um m m mr m mlm wmmar m m .mwmw mafia t um 06 r lnk CC I lnk 09 l n a 81min n We d .vi n l vi s an nyeld vi s m1 w vi ss wL h e hh fi wl h e "h wl .t e ....hiS a SS G 8 1 h 8 06 1 u 4.. M m1 u mt. F 10 U m .0 1 u t 00 myr ma rv m v.r l a rv v.r a rv m myr a v l e e k l 1 mm aamwwm m wm mwmmwm a wa mammam a mem w m m m d6 .1 h 0 6 H h 0 d a efi .0 .10 1T O 11 1 lr h O 1 1 .10. 0 1f 1 1 h sMoUDNsAWoUsT sMoUDNsAwGusr sMoUDNsAWGUsr sMGUDNsAWGPwTT readily, films are more Which the foam or sheet preferably heated preciated that many active sp amples are given. These examples set forth specific solutions from which the articles of the present invention may be produced by evaporation of water in accordance with the procedures described above. In each instance, the composition includes sodium carboxymethylcellulose or methylcellulose as a vehicle, together with urea and other ingredients. The quantities given are by weight and are based upon the grams used with 100 grams of water.

The above compositions were tested for spermicidal eifectiveness, the method followed being that described in A Method of Testing the Relative spermicidal Effectiveness of Contraceptives, and Its Application to Ten Commercial Products, Human Fertility, (4)-97, 1940, by R. L. Brown and C. I. Gamble.

In all instances the materials Were instantly spermicidal at dilutions of 20 times (8/ 20).

Where the sheet-like material is in the form of a foam the area of the film-sheet, in square inches, should be at least 500 and preferably 1000 times or more the thickness of the film, while with a vigorously beaten foam, the area may be as small as or smaller than ten times the thickness of the material. Where a low concentration of spermicide occurs in the vehicle, this ratio will generally be larger than with higher concentnations, but with an unfoamed film 0.005 inch thick that contains about 14% of the spermicide, the area for a single use would be of the order of 9 to 16 square inches. With a film Which had a concentration of 14% of spermicide and a thickness of 0.240 inch, about 2.5 square inches of the material should be used.

The spermicidal film or foamed material of the present invention lends itself readily to easy, inexpensive packaging, and a sufficient amount for a single use may be enclosed and hermetically sealed in an envelope of thermoplastic sheet material, such as polyethylene envelopes, in which case the material need not be completely dried, thereby partially eliminating the need for any hu-mectant, and at the same time increasing the rapidity with which the dissolution of the material may start after application.

The invention in its broader aspects is not limited to the specific steps, processes and compositions shown and described but departures may be made therefrom within the scope of the accompanying claims without departing from the principles of the invention and without sacrificing its chief advantages.

This application is a continuation-in-part of Serial No. 597,861, filed July 16, 1956, and 690,452, filed October 16, 1957, both now abandoned.

What is claimed is:

*1. A spermicidal sheet-like material comprising a sheet of non-deleterious, water soluble sodium carboxymethylcellulose, at least 5 milligrams of nonylphenoxypolyethoxyethanol, from about 20% to about 25% by weight of urea based on vehicle solids and from about 25 to about 45% by weight of glycerol.

2. A spermicidal material as claimed in claim 1 in which the area of the sheet is at least 10 times as great as its thickness.

3. A spermicidal material as claimed in claim 1 in which the sheet material is a foamed material.

4. A spermicidal material as claimed in claim 1 in which the sheet is from 0.001 to 0.0075 inch thick.

5. A spermicidal material as claimed in claim 1 in which the sheet is from 0.005 to 0.240 inch thick and is formed from a foam.

6. A spermicidal sheet like material comprising a sheet of non-deleterious Water soluble, carboxymethylcellulose, containing from 20% to 25% by weight of urea and from 1% to by weight based on the carboxymethylcellulose of a spermicide selected from the group consisting of alkylated aryl polyether alcohols and a sodium alkylaryl polyether surfates and also containing about 25 to 40% by weight based on the carboxymethylcell-ulose of a humectant.

'7. A spermicidal sheet-like material as claimed in claim 6 in which the humectant is glycerol.

References Cited in the file of this patent UNITED STATES PATENTS 2,484637 Mattocks et al Oct. 11, 1949 2,563,593 Engel Aug. 7, 1951 2,602,042 Abbott July 1, 1952 2,693,438 Ward Nov. 2, 1954 FOREIGN PATENTS 150,013 Australia Feb. 12, 1953 OTHER REFERENCES Diserens: The Chemical Technology of Dyeing and Printing, Reinhold Publ. Co., New York (1948), p. 8.

Patent Citations
Cited PatentFiling datePublication dateApplicantTitle
US2484637 *Aug 20, 1946Oct 11, 1949Southern Res InstPowdered ointment base of methyl cellulose and sorbitol
US2563593 *Mar 18, 1949Aug 7, 1951 Surgical bandage
US2602042 *Aug 16, 1947Jul 1, 1952Inez M AbbottProcessing methyl cellulose and the products thereof
US2693438 *Feb 21, 1951Nov 2, 1954Norwich Pharma CoPreformed, nonadherent films for application to open lesions
AU150013B * Title not available
Referenced by
Citing PatentFiling datePublication dateApplicantTitle
US3875300 *Dec 18, 1972Apr 1, 1975Ortho Pharma CorpComposition for sustained release of a medicament and method of using same
US3918452 *Aug 1, 1974Nov 11, 1975Cornfeld EdwardTampons impregnated with contraceptive compositions
US4031202 *Dec 8, 1975Jun 21, 1977The Procter & Gamble CompanyNonhormonal, spermicide
US4193813 *Sep 7, 1976Mar 18, 1980Medi-Coll, Inc.Method for making collagen sponge
US4261969 *May 3, 1979Apr 14, 1981World Health OrganizationControlled drug release composition
US4265875 *Oct 19, 1979May 5, 1981Inveresk Research InternationalHydroxypropyl methyl cellulose
US4292300 *Jul 20, 1977Sep 29, 1981Inveresk Research InternationalControlled release suppositories
US4351338 *May 21, 1980Sep 28, 1982Pierre LangloisA sponge material impregnated(no pun intended) with a spermicidal composition in a time release medium
EP2138162A2Jul 1, 2005Dec 30, 2009Gilead Sciences, Inc.Gel comprising tenofovir or tenofovir disoproxil
EP2138163A2Jul 1, 2005Dec 30, 2009Gilead Sciences, Inc.Suppository formulations comprising tenofovir or tenofovir disoproxil
EP2283812A2Jul 1, 2005Feb 16, 2011Gilead Sciences, Inc.Topical antiviral formulations
EP2546358A1Jul 15, 2011Jan 16, 2013Laboratorios Del. Dr. Esteve, S.A.Methods and reagents for efficient control of HIV progression
WO2011067302A1Dec 1, 2010Jun 9, 2011Seprox Biotech, S.L.Topical use of hydroxytyrosol and derivatives for the prevention of hiv infection
Classifications
U.S. Classification604/286, 424/433, 424/DIG.140, 514/718
International ClassificationA01N25/34, A61K47/00, A61K9/00, A61K9/70, A61F6/06
Cooperative ClassificationA01N25/34, A61F6/06, Y10S424/14, A61K9/7007, A61K9/0034
European ClassificationA01N25/34, A61K9/00M8, A61F6/06