# US 11,992,472 B2 · Compositions and methods for enhancing the efficacy of contraceptive microbicides

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- Number: US 11,992,472 B2
- Document ID: US11992472B2
- Status: Granted
- Kind: B2
- Application number: 17/823,020
- Filed: 2022-08-29
- Published: 2023-08-03
- Granted: 2024-05-28
- Earliest claimed: 2012-06-13
- Assignees: Evofem, Inc.
- Applicants: Evofem, Inc.
- Inventors: Wendell Guthrie
- Web page: https://patentgrep.com/patent/US11992472B2

## CPC

- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 9/0034: {Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61P 15/18: Feminine contraceptives
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/12: Antivirals
- A61P 31/18: for HIV
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure relates to compositions and methods for contraception that also enhance the efficacy of microbicides. Such compositions serve the dual purpose of preventing pregnancy and lessening the risk of spreading sexually transmitted diseases. More specifically, the compositions and methods relate to syngergistic contraceptive microbicide and antiviral compositions comprising a combination of a contraceptive microbicide and an antiviral agent in an acidic carrier that enhances the efficacy of both the contraceptive microbicide and antiviral agent.

## Claims

### Claim 1

A method for preventing pregnancy comprising intravaginally administering a composition to a subject in need thereof, wherein the composition comprises: a) a matrix-forming compound selected from the group consisting of: alginic acid, chitosan, gellan gum, and poloxamer; b) a bioadhesive compound that is the same or different from the matrix-forming compound; c) L-lactic acid; and d) an aqueous-based pharmaceutically acceptable carrier, wherein the composition has a nonmatrix state when not in contact with ejaculate, and a matrix state when in contact with ejaculate, and wherein the total lactic acid in the composition is not in a form of racemic mixture.

### Claim 2 (depends on 1)

The method of claim 1, wherein the composition further comprises a humectant.

### Claim 3 (depends on 2)

The method of claim 2, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycol, polypropylene glycol, sorbitol, and triacetin.

### Claim 4 (depends on 3)

The method of claim 3, wherein the composition further comprises a preservative.

### Claim 5 (depends on 4)

The method of claim 4, wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benzyalkonium chloride, phenylmercuric nitrate, and chlorhexidine.

### Claim 6 (depends on 5)

The method of claim 5, wherein the matrix-forming compound is alginic acid.

### Claim 7 (depends on 6)

The method of claim 6, wherein the alginic acid has an average molecular weight in the range of about 20,000 to about 300,000 g/mole.

### Claim 8 (depends on 1)

The method of claim 1, wherein the bioadhesive compound is selected from the group consisting of xanthan gum, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, chitosan, polycarbophil, and carbopol.

### Claim 9 (depends on 8)

The method of claim 8, wherein the bioadhesive compound is xanthan gum.

### Claim 10 (depends on 1)

The method of claim 1, wherein the composition comprises about 1-10% of the matrix forming compound, about 1-10% of the bioadhesive compound, and 1-10% L-lactic acid.

### Claim 11 (depends on 1)

The method of claim 1, wherein the composition comprises about 3-5% of the matrix forming compound, 2.5-3.5% of the bioadhesive compound, and 1-7% L-lactic acid.

### Claim 12 (depends on 1)

The method of claim 1, wherein the pH of the composition is 5.0 or below.

### Claim 13 (depends on 1)

The method of claim 1, wherein the composition maintains the pH of the vagina at pH 5.0 or below in the presence of normal amounts of ejaculate.

### Claim 14 (depends on 1)

The method of claim 1, wherein the composition in the matrix state is capable of trapping and inactivating sperms.

### Claim 15 (depends on 1)

The method of claim 1, wherein the composition in the matrix state is capable of immobilizing sperms.

### Claim 16 (depends on 1)

The method of claim 1, wherein the composition is administered at a dosage of from about 1 to about 10 grams.

### Claim 17 (depends on 1)

The method of claim 1, wherein the composition is administered at a dosage of from about 3 to about 7 grams.

### Claim 18 (depends on 1)

The method of claim 1, wherein the composition is administered at a dosage of from about 4 to about 6 grams.
