Self administrable anti-fertility composition

• US 4,310,510 A
• Filed: 10/03/1980
• Issued: 01/12/1982
• Est. Priority Date: 12/27/1976
• Status: Expired due to Term

• Current Assignee: Arnold Jacobson, Kenneth N. Sherman
• Original Assignee: Arnold Jacobson, Kenneth N. Sherman
• Inventors: Sherman, Kenneth N., Jacobson, Arnold
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/193,628
• Time in Patent Office: 466 Days
• Field of Search: 424/238-243, 424/45
• US Class Current: 424/45
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/122 Foams; Dry foams edible foams A61K9/0056

Abstract

A self-administrable anti-fertility composition comprising a progestational compound in an amount effective for alteration of cervical mucus secretions in a manner unfavorable to fertility without systemic absorption and a pharmaceutically acceptable vehicle. A typical composition is a foamable aqueous emulsion containing an anionic surfactant, propylene glycol and an amount of progesterone effective to provide a dose of from about 10 micrograms to about 5 milligrams. The composition may be foamed by dispensing with a syringe or by dispensing from an aerosol container.

Claims

1. A self-administrable antifertility composition comprising a progestational compound for topical non-systemic application to the cervix in an amount effective for alteration of cervical mucous secretions in a manner unfavorable to fertility and a non-rigid pharmaceutically acceptable viscous gel, cream, foam or effervescent type suppository vehicle which is sufficiently viscous to keep the progestational compound in effective contact with the cervical tissue for sufficient time to bring about the desired modification of the cervical mucous secretions when formulated for self-administrable use, care being taken that the carrier is not so viscous that administration becomes difficult and the contact time required between the reactive progestational ingredient and the cervical tissue becomes overly long for the effective dose to be administered, said vehicle excluding solid or rigid type ampoules or capsules as well as liquid carriers and ordinary suppositories which have an undesirable propensity to flow and run out of the vagina, said progestational compound being contained in said vehicle in a concentration selected according to the progestational compound and the dosage quantity and schedule so as to apply to the cervix substantially only a non-systemic quantity of the progestational compound to produce substantially only a local effect without changing in significant measure the amount of said compound in the blood stream of the user and thereby without generating side effects resulting from increased blood levels in the user of said progestational compound.

2. A composition as in claim 1 wherein said vehicle comprises a foam base containing a thickening agent in an amount effective to substantially prevent said composition from flowing when foamed.

3. A composition as in claim 1 further comprising a foam containing a stabilizing agent.

4. A composition as in claim 2 wherein said thickening agent is an aliphatic, straight chain, monohydroxy alcohol containing 14-22 carbon atoms.

5. A composition as in claim 1 wherein said composition is an aqueous emulsion, said emulsion containing about 1-5% by weight of a thickening agent comprising an aliphatic, straight chain monohydroxy alcohol containing 14-22 carbon atoms, and an anionic surfactant as a foaming agent in an amount of about 5-20% by weight.

6. A composition as in claim 5 further including a fatty acid-dialkanolamine condensate in an amount of about 1-5% by weight.

7. A composition as in claim 1 further comprising a foam containing a stabilizing agent.

8. A composition as in claim 7 wherein said foam stabilizing agent is a glycol, a polyalkylene glycol or glycerol, present in said composition in an amount of about 10-50% by weight.

9. A composition as in claim 6 further including a foam stabilizing agent selected from a glycol, a polyalkylene glycol and glycerol, said foam stabilizing agent being present in an amount of about 10-50% by weight.

10. A composition as in claim 1 wherein the amount of progestational compound is insufficient to provide a dose of greater than about 5 milligrams per application.

11. A composition as in claim 1 wherein the amount of said progestational compound is sufficient to provide a dose of from about 10 micrograms to about 5 milligrams.

12. A composition as in claim 1 wherein said composition is an aqueous emulsion, said composition containing triethanolamine lauryl sulfate as a foaming agent and said progestational compound is progesterone, said composition further containing about 10-50% of propylene glycol or ethylene glycol, about 1-5% by weight of coconut-diethanolamine condensate, about 1-5% by weight of cetyl alcohol, about 0.1-2% by weight of hydroxyethyl cellulose or hydroxypropyl cellulose, and about 20-50% by weight of water.

13. A composition as in claim 1 wherein said composition containing as a foaming agent a surfactant selected from triethanolamine lauryl sulfate, sorbitain monolaurate, N-(lauroyl colamino formyl methyl) pyridinium chloride, a carboxylic acid derivative of an imidazolinium compound, and sodium lauryl ether sulfate, the amount of said surfactant being about 5-20%, and wherein the progestational compound is progesterone, said composition further containing about 10-50% by weight of ethylene glycol, propylene glycol, a polyalkylene glycol or glycerol, about 1-5% by weight of coconut-diethanolamine condensate or oleic acid-diethanolamine condensate, about 1-5% by weight of cetyl alcohol, myristyl alcohol or stearyl alcohol, about 0.1-2% by weight of hydroxyethyl cellulose, hydroxypropyl cellulose, carboxymethyl cellulose, or methyl cellulose, and about 20-50% by weight of water.

14. A composition as in claim 1 wherein the amount of said progestational compound is about 1.25% by weight.

15. A composition as in claim 1 wherein said progestational compound is progesterone.

16. A composition as in claim 1 wherein said progestational compound is natural progesterone, synthetic progesterone, chloromadinone, medroxyprogesterone acetate, norgestrel, or cyproterone acetate.