Nova Patents
US2467884A

Spermicides

Abstract

This record has no abstract on file.

Term

Term ended

Expired 19 April 1966, 60.4 years ago.

  1. Priority and filed
  2. Granted
  3. Expired
  4. Today

6 claims: 5 independent, 1 dependent

  1. 1
    Having thus described the range of spermicidal substances coming within the scope of the present invention, I shall now give examples of how they may be used in finished spermicidal compositions. In accordance with the present invention, the said substances are uniformly distributed in vehicles to form various spermicidal compositions, these compositions being generally classified as 8,467,884 β Acid JelliesUsing Wins Soluble Mono Fatty ESTERS AND A WATER SOLUBLE ORGANIC ACID AND No Emulsifier Formula 2 Founds 5 jellies, creams, concentrated foam jellies, concentrated foam producing mixtures, concentrated foam powders, suppositories and tampons. The particle size of the said substances in said vehicles varies from molecular, 1. e., a solution, to β approximately 1.5 microns. JELLIES In general it should be noted that in any of the following jelly formulae glycerine is added to prevent dehydration of the jelly and also to prevent freezing of the composition. The various vegetable gums, such as gum tragacanth, gum karaya and gum arable may be substituted by other gums such as Irish moss, Indian gum, alginates, synthetic cellulose derivatives such as' coJlOresin, locust bean gum, etc. The butyl para hydroxy benzoate may be substituted by other mold preventive material such as the methyl, ethyl or propyl para hydroxy benzoates. The oxyquinoline sulphate may be substituted by other bacteriostatic materials such as the phenols, the alkali alkyl sulphates, etc. The emulsifying agent, sodium lauryl sulphate may be substituted by any of the known alkali, ammonium or substituted ammonium alkyl sulphates or other sulfonated substances such as sulfonated oils, sulfonated hydrocarbons, sulfonated castor oil and similar products. The water soluble acids which may be substituted for lactic or boric acids as shown in the formulae may include acetic acid, tartaric acid and similar acids. The potassium acetate as shown in the formula is a buffer and may be substituted by sodium acetate or by alkali borates, tartrates, phosphates, lactates, etc. It is understood that where the water soluble organic acids are used they exert a certain known spermicidal power, but this spermicidal power alone is Insufficient to achieve the effectiveness now possible with these new compositions. In the case of boric acid, this product has very slight spermicidal efficacy and is used simply for regulating the pH of the composition. The fact that compositions of extremely high spermicidal value, even though neutral, are made possible by this invention, establishes the utility of these compositions regardless of the presence or absence of added acid. The proportion of the gums used indicates the viscosity range chiefly preferred, but such viscosities may range either lower or higher than 55 indicated in the compositions described without seriously affecting the utility of the product. Neutral Jellies Using Water Soluble Mono Fatty Esters With No Emulsifier Formula 1 Pounds Nona ethylene glycol mono laurate_______ 3.0 65 Oxyquinoline sulphate_______________ 0.05 Glycerine_________________10.0 Gum tragacanth____ 2.0 Gum karaya_________;_________ 1.0 Gum arable___________________________0.5 γθ Butyl para hydroxy benzoate_________ 0.05 Perfume_____________________ 0.05 Nona ethylene glycol mono laurate —— 3.0 Oxyquinoline sulphate _—-----------— 0.05 Glycerine_____—;-----------—-10.0 Lactic add—85% 2.35 IO Gum tragacanth _—«.------------------- 2.0 Gum arable-------------------— 0.5 Gum karaya-------------------------- 1-0 Butyl para hydroxy benzoate--------- 0.05 Potassium acetate, sufficient for pH of 3.0______________________About 0.05 10 Perfume------------------------ 0.05 Add sufficient water to make ------------100.00 In this type of formula, using water soluble 20 esters, the approximate equivalence rule given previously applies. Less of the spermicidal ester is used here than in Formula 1, since part of the spermicidal action is provided by the lactic acid. 25 However, more of the ester may be used If a still more spermicidal composition is desired. Acid Jellies Using Water Soluble Mono Esters and Boric Acid Formula 3 Pounds Nonaethylene glycol mono laurate - 2.0 Sodium lauryl sulfate---------------:0.5 Gum tragacanth i_______— 3.0 35 Glycerine--------------------- 10.0 Gum arable__________--------- 0.5 Butyl para hydroxy benzoate -- 0.05 Boric acid—adjust pH to 4.3------About 0.5 Perfume_____-________________ 0.05 40 -----Water sufficient to make a total of______100.00 Here boric acid Is used, and since this contributes little to the spermicidal value, 3 lbs. of the ester are used. In addition, sodium lauryl sul45 phate is used which has a bacteriostatic action as well as a wetting action so the oxyquinoline sulphate may be omitted. The function of the boric acid is simply to bring the composition to a pH value of 4.3. 50 Neutral Jellies Using Water Insoluble Mono Fatty Esters With Added Emulsifier Formula 4 Pounds Glyceryl mono undecylenate3.0 Sodium lauryl sulfate 0.5 Glycerine_____—_________________ 10.0 Gum tragacanth-----------------_____3.0 Gum arable______-- 0.5 Butyl para hydroxy benzoate 0.05 Perfume 0.05 Bring to pH of 7.0 with trace of NaOH if necessary. Add sufficient water to make total of____100.00 The sodium laurly sulfate here assists in the dispersal of the glyceryl mono-undecylenate as well as exerting a bacteriostatic action. Acid Jellies Using Water Insoluble Mono Fatty Esters and an Acid Formula 5 Bring to pH of 7.0 with trace of NaOH. Add sufficient water to make total of ____100 This formula is identical with Formula 3 ex75 cept that the 2 lbs. of nonaethylene glycol lau9,487,884 rate Is replaced by 2 lbs. of glyceryl monorlclnoleate. Acid Jellies Using Water Insoluble Higher Fatty Alcohols With Added Emulsifier Formula 6 Pounds n-Decyl Alcohol 1.0 Sodium lauryl sulfate 0.8 Glycerine____________________- 10.0 Gum tragacanth________ 3.2 Gum arable 0.7 Butyl para hydroxy benzoate 0.05 Perfume 0.05 Boric acid—adjust pH to 4.3______About 0.5 Water sufficient to make total100.0 Acid Jellies Using Water Insoluble Mono Fatty Ether and Boric Acid Formula 7 This formula is identical with Formula 3 except that 2 lbs. of the glyceryl mono ether of octyl alcohol are used instead of 3 lbs. of nonaethylene glycol monolaurate. Jellies in Which Both a Water Soluble and Water Insoluble Ester are Used Formula S Pounds Nona ethylene glycol mono laurate _ 1.5 Glyceryl mono ricinoleate 1.5 Glycerine 10.0 Oxyquinoline sulfate________________ 0.05 Gum Tragacanth 3.0 Gum arable 0.5 Boric acid to adjust pH to 4.3 i_____About 0.5 Perfume 0.05 Water sufficient to make a total of100.0 Here the nonaethylene glycol monolaurate assists in emulsifying the glyceryl monoricinoleate and they both exert spermicidal action, which is additive. Jellies in Which a Water Soluble Mono Fatty Ether is Used Formula SA
  2. 2
    5 lbs. nona ethylene glycol mono ether of octanol is substituted for the 3 lbs. of nona ethylene glycol laurate In Formula 2. CREAMS In forming spermicidal creams, I have found it essential to provide a suitable cream base to carry the spermicidal material. Such a base is made up of a high molecular alcohol such as stearyl alcohol or cetyl alcohol or saturated mono-higher fatty esters of glycerine or sorbitan or glyceryl mono lactate with an emulsifier such as one of the alkyl sulfates and water. I have found it convenient to reduce the cost of such a base by diluting it with stearic acid in which case the more costly high molecular alcohols such as cetyl and stearyl or the saturated mono fatty esters of glycerine or of sorbitan or of glyceryl monolactate are required in less quantity. Because of the necessity for emulsifying the base forming constituents of the creams, it is essential always to have in the composition an emulsifying agent. It must be present in amount sufficient to emulsify the base, and in case a water insoluble non-seif-dispersible spermicidal material is used, there must be sufficient in addition for emulsifying this also. Of course, where the spermicidal agent is self emulsifying some8 what less of the emulsifier will be required than is otherwise the case. This is also true where the sperimlcidal agent Is water soluble. Neutral Cream Using Water Soluble and Water Insoluble Mono Fatty Esters Formula 9 Pounds Glyceryl mono stearate________________ . 18.0 Glyceryl mono laurate 2.0 Glycerine 8.5 Nona ethylene glycol undecylenate 2.0 Sodium lauryl sulfate 0.7 Perfume______________________ 0.05 Adjust to pH of 7.0 with either boric acid or NaOH. Water sufficient to total100.0 Acid Cream Using Water Soluble and Water Insoluble Mono Fatty Esters Formula 10 Pounds Glyceryl mono stearate 5.5 Stearic acid 10.O Sorbitan stearate______________________ 4.5 Nona ethylene glycol mono laurate 3.0 Glycerine 8.5 Sodium lauryl sulfate 0.6 Lactic acid 85% 1.2 Potassium acetate to adjust pH to 3.3------About 0.2 Water sufficient to make total100.0 Acid Cream Using Mixture of Water Insoluble Mono Fatty Esters Formula 11 Pounds Stearic acid is.o Sorbitan stearate 4.5 Glyceryl monoricinoleate 2.0 Glycerine 8.5 Sodium lauryl sulfate 0.6 Boric acid—adjust to pH of 4.3 Perfume 05 Water sufficient to make total100.0 Acid Cream Using Only Water Soluble Mono Fatty Esters Formula 12 Pounds Stearic acid___________________________ 4.0 Stearyl alcohol 8.0 Nona ethylene glycol mono laurate 3.0 Glycerine 8.5 Sodium lauryl sulfate_______________~~~ o^5 Lactic acid 85% 2'0 Potassium acetate to adjust pH to 3.0------About 0.3 Perfume 05 Water sufficient to make total100.0 Other Cream Formulae Showing Variations in the Ingredients for the Base Formula 13 _ . Pounds Stearic acid 19 q Glycol monoricinoleate 1’3 Sodium lauryl sulfate0^8 Stearyl alcohol________________________ Potassium acetate 0 2 Lactic acid 85% _____________ΣΖΖΣΞΖΣΣΣΣΣ 12 Glycerine θ 0 Water sufficient to make total of100.0 8,487,884 Formula 14 Glyceryl monostearate ;---------- 18.0 Nonaethylene glycol laurate 3.0 Sodium lauryl sulfate —----------:— 0.9 Boric acid------ 2.0 Glycerine —-------ύ----------: Water sufficient to make total of100.0 Formula 15 Pound Glyceryl monostearate---------------— 10.0 Stearic acid 10.0 Nonaethylene glycol laurate 2.0 Sodium lauryl sulfate--------______—-0.7 Boric acid - 2.0 Glycerine 8.0 Water sufficient to make total of100.0 Formula 16 Pounds Stearic acid 18.0 Glyceryl monostearate 2.0 Sodium lauryl sulfate----------;———0.8 Glyceryl monoricinoleate 1.3 Boric acid 1.0 Glycerine _ 8.0 Water sufficient to make total of100.0 CONCENTRATED FOAM JELLIES For concentrated foam producing jellies, powders or similar mixtures to be used with moist sponges or moist tampons, it is desirable to have very high concentrations of spermicidal materials, since a small amount only- is used on the sponge or tampon. The sodium alkyl sulfate assists the polyglycol mono ester in foam formation. The following formulae are examples of my new compositions for this purpose. Concentrated Foam Jellies for Use With Moist Sponge or Tampon Using Water Soluble Mono Fatty Ester . Formula 17 Pounds Nonaethylene glycol laurate20.0 Sodium lauryl sulfate 5.0 Gum tragacanth 3.0 Boric acid----------------------------— ‘2.0 Perfume - θ·1 Glycerine 8.5 Water sufficient to make total of —-100.0 Formula 18 This is identical with Formula 17 except that the nonaethylene glycol laurate is replaced with 20 lbs. of glyceryl monoricinoleate, which is Insoluble. Concentrated Foam Producing Mixture Which May be Used With Moist Tampon or Moist Sponge Using Water Soluble Mono Fatty Ester Formula 19 Pounds Nonaethylene glycol laurate20.0 Boric acid-------------Gum arable ---------------------— 2.0 Sodium lauryl sulfate----------------— 5.0 Perfume -------------- θ· Glycerine --------------------Water to make total of---------——------1θθ·° FOAM POWDERS The vehicle in the ease, of the foam powders consists of kaolin and sucrose and lauryl sulfate. The spermicidal material is uniformly mixed 5 throughout the powder. CONCENTRATED FOAM POWDER FOR USE WITH MOIST Sponge or Tampon Formula 20 Pounds Kaolin____ 50 Sucrose ____;_____________2----------30 Sodium lauryl sulfate_____ 5 Glyceryl monoricinoleate _ 15 15 Perfume —_________——------------- 0.1 Formula 21 Same as previous formula except that 15 lbs. of 20 nonaethylene glycol mono laurate is substituted for the 15 lbs. of glyceryl monoricinoleate. SUPPOSITORIES For suppositories, two types may be used. The 25 first is that which melts at body temperature. Here the vehicle used is the higher molecular weight polyglycols themselves :— in which the spermicidal factor is uniformly mixed. Examples are as follows: 30 Formula 22 To 96 parts polyethylene glycol of molecular weight 1500 is added 4 parts of nonaethylene glycol mono undecylenate and both are melted 35 together. This mixture is then adjusted to a melting point of 36.5 by the addition of poly ethylene glycol of molecular weight 4000. The resulting product is melted and cast in sup40 pository molds. Formula 23 To 06 parts of poly ethylene glycol of molecular weight 1500 is added 4 parts of the laurate ester of poly ethylene glycol (molecular weight 400) and 2 lbs. of boric acid, and further adjustments of meltfag point are made by the addition of the poly glycols of molecular weight 4000, to obtain a melting point of 36.5° C. The ingredients are melted together and then cast in suppository molds. For suppositories stable at higher temperatures, the following formulae may be used. These depend on solubility of the vehicle or the spermicidal ingredient or both. Formula 24 To 96 lbs. of a poly ethylene glycol of melting point of 50° C. is added 2 lbs. of boric acid and 4 60 lbs. of a poly ethylene glycol mono laurate having a molecular weight of 800. The mixture is melted together and then cast in suppository molds. ¢5 Spermicidal Tampons to Be Used With Added Moisture Here cotton, lambs wool, or other fibre and the added water constitutes the vehicle through which the spermicidal factor is distributed. 70 Formula 25 Cotton, lambs wool, natural or artificial silk or nylon fluff are impregnated with a water solution containing 50 parts of nonaethylene glycol mono 75 laurate and 3 parts boric acid in a total of 100. 9,467,884 The materia] is pressed until there remains in it only 10% of the solution. It is then cut up into tampons weighing approximately 5 grams each, provided with strings, packaged and sterilized. Formula 26 Identical with formula 25 except that the monoethylene glycol laurate solution is replaced by molten poly ethylene glycol mono laurate of molecular weight of about 1700. Formula 27 Identical with formula 25 except that the mono ethylene glycol laurate solution is replaced by molten polyethylene glycol mono undecylenate of molecular weight of about 1680. I have described what I believe to be the best embodiments of my invention. I do not wish, however, to be confined to the embodiments set forth, but what I desire to cover by Letters Patent is set forth in the appended claims. I claim: 1. A harmless spermicide comprising a nonalkaiine vehicle and a neutral aliphatic hydroxy material of sufficient spermicidal power and in sufficient proportions to constitute the major spermicidal ingredient in total spermicidal effect distributed therein, the size of the particles of the material distributed ranging from molecular to approximately 1.5 microns, said material being selected from the class consisting of (a) straight chain fatty monohydroxy alcohols having from 8 to 11 carbon atoms in the chain, (b) branched chain fatty alcohols from 8 to 18 carbon atoms in the chain, (c) glyceryl, ethylene glycol and propylene-glycol monoethers of the alcohols mentioned in (a) and (b), (d) polyethylene glycol and polypropylene glycol mono ethers of these alcohols, the poly glycols ranging from the diglycol up to polyglycols of molecular weight of about 4000, (e) glyceryl, ethylene glycol and propylene glycol monoesters of unsaturated fatty acids having from 10 to 18 carbons in the chain, (/) the polyethylene glycol and the polypropylene-glycol monoesters of fatty acids, saturated and unsaturated, having from 10 to 18 carbons in the chain, the polyglycols ranging in molecular weight from diglycol to polyglycol of molecular weight of about 4000, (p) glyceryl monolactate monoesters of unsaturated fatty acids of 10 to 18 carbon atoms, and mixtures thereof, the consistency of the vehicle being such that when the material is distributed throughout It, the resulting composition may be positioned for effective action in a body cavity. 2. The spermicide as defined in claim 1, in S which the vehicle is an aqueous vehicle.
  3. 3
    The spermicide as defined in claim 1 and containing a water soluble acid for bringing the pH of the resulting composition within the range of 7.0 to approximately 1.0. 10
  4. 5
    The spermicide as defined in claim 1 and containing a substance for reducing the surface 20 tension of the composition.
  5. 6
    The spermicide as defined in claim 1 and containing a buffer. NATHANIEL M. KT .TAS 25 REFERENCES CITED The following references are of record in the file of this patent:UNITED STATES PATENTS 30 Number Name Date 2,052,025 Harris_____________Aug. 25, 1936 2,055,063 Bird _______________Sept. 22, 1936 2,149,240 Crossley____________Feb. 28, 1939 2,173,203 Harris_____________Sept. 19,1939 33 2,192,907 Harris______________Mar. 12,1940 2,269,529 Goldsmith__________Jan. 13,1942 2,302,121 Harris______________Nov. 17,1942 FOREIGN PATENTS 40 Number Country Date 110,600 Australia___________May 23,1940 OTHER REFERENCES Journal of Contraception, Sept. 1938, pages 149 45 to 153, article by Climenko. Human Fertility, Feb. 1941, pages 1-7, article by Brown and Gamble. Drug and Cosmetic Ind., Oct. 1943, pages 388, 389 and 395 by Glickman. 60 Garrell, Clin. Med., July 1941, pages 163-166. Spans and Tweens pamphlet, Atlas Powder Co. Nov. 1942,20 pages.
Independent claims5