# US 11,439,610 B2 · Compositions and methods for enhancing the efficacy of contraceptive microbicides

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- Number: US 11,439,610 B2
- Document ID: US11439610B2
- Status: Granted
- Kind: B2
- Application number: 16/738,868
- Filed: 2020-01-09
- Published: 2020-05-14
- Granted: 2022-09-13
- Earliest claimed: 2012-06-13
- Assignees: Evofem, Inc.
- Applicants: Evofem Biosciences, Inc.
- Inventors: Wendell Guthrie
- Web page: https://patentgrep.com/patent/US11439610B2

## 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 synergistic 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 composition comprising:
a) 3-5% alginic acid;
b) 2.5-3.5% xanthan gum;
c) 1-7% L-lactic acid; and
d) an aqueous-based pharmaceutically acceptable carrier,
wherein the composition is essentially free of D-lactic acid.

### Claim 2 (depends on 1)

The composition of claim 1, further comprising a humectant.

### Claim 3 (depends on 2)

The composition 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 composition of claim 3, further comprising a preservative.

### Claim 5 (depends on 4)

The composition 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 1)

The composition of claim 1, wherein the alginic acid has an average molecular weight in the range of 20,000 to 300,000 g/mole.

### Claim 7 (depends on 1)

The composition of claim 1 comprising 3.5-4.5% alginic acid, 2.5-3.5% xanthan gum, and 1-4% L-lactic acid.

### Claim 8 (depends on 1)

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

### Claim 9 (depends on 1)

The composition 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 10

A composition consisting essentially of:
a) 3-5% alginic acid;
b) 2.5-3.5% xanthan gum;
c) 1-7% L-lactic acid;
d) potassium bitartrate;
e) glycerin;
f) benzoic acid;
g) citric acid; and
h) water,
wherein the composition is essentially free of D-lactic acid.

### Claim 11 (depends on 10)

The composition of claim 10, wherein the alginic acid has an average molecular weight in the range of 20,000 to 300,000 g/mole.

### Claim 12 (depends on 10)

The composition of claim 10, wherein the pH of the composition is 5.0 or below.

### Claim 13 (depends on 10)

The composition of claim 10 comprising 3.5-4.5% alginic acid, 2.5-3.5% xanthan gum, and 1-4% L-lactic acid.

### Claim 14 (depends on 1)

The composition of claim 1, further comprising potassium bitartrate, glycerin, benzoic acid, and citric acid, wherein the pH of the composition is 5 or below.

### Claim 15 (depends on 14)

The composition of claim 14, further comprising water.

### Claim 16 (depends on 7)

The composition of claim 7, further comprising potassium bitartrate, glycerin, benzoic acid, and citric acid, wherein the pH of the composition is 5 or below.

### Claim 17 (depends on 16)

The composition of claim 16, further comprising water.