# US 2016/0030569 A1 · Low-glycerin formulations for hiv treatment and prevention

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- Number: US 2016/0030569 A1
- Document ID: US20160030569A1
- Status: Published application
- Kind: A1
- Application number: 14/775,503
- Filed: 2014-03-14
- Published: 2016-02-04
- Earliest claimed: 2013-03-15
- Assignees: Conrad
- Applicants: Conrad
- Inventors: David R. FRIEND
- Web page: https://patentgrep.com/patent/US20160030569A1

## CPC

- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 9/0031: {Rectum, anus}
- A61K 9/0034: {Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants}
- A61K 9/02: Suppositories; Bougies; Bases therefor; {Ovules}(apparatus for making A61J3/08; devices for introducing into the body A61M31/00)
- 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 47/38: Cellulose; Derivatives thereof
- 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 invention relates to formulations of nucleotide reverse transcriptase inhibitors (NRTIs), preferably [2-(6-Amino-pur: in-9-yl)-1-methyl-ethoxymethy]-phosphonic acid (tenofivir, PMPA), or a physiologically functional derivative thereof, wherein the formulations contain a low level of glycerin. Human immunodeficiency vims (HIV) infection and related diseases are a major public health problem worldwide. One approach to the problem of HIV/AIDS is to reduce the risk of transmission of HIV and thus reduce the number of individuals who become newly infected.

## Claims

### Claim 1

A pharmaceutical formulation comprising an effective amount of a NRTI in combination with one or more of a lubricant, humectant, preservative, and thickening agent, wherein the formulation comprises less than or equal to about 5% glycerin.

### Claim 2 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the lubricant is in an amount of 1.0% (w/w) to about 10% (w/w).

### Claim 3 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the lubricant is selected from the group consisting of magnesium stearate, stearic acid, vegetable oil, glycerin, mineral oil, PEG4000, PEG6000, Sodium Lauryl Sulfate (SLS), glyceryl palmitostearate, glyceryl behenate, sodium benzoate, and sodium stearyl fumarate.

### Claim 4 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulation comprises about 0.5% (w/w) to about 10% (w/w) of the thickening agent.

### Claim 5 (depends on 4)

The pharmaceutical formulation of claim 4, wherein the thickening agent is hydroxyethylcellulose or methylcellulose.

### Claim 6 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulations comprises about 0.01% (w/w) to about 2.0% (w/w) of one or more preservatives.

### Claim 7 (depends on 6)

The pharmaceutical formulation of claim 6, wherein the one or more preservatives is selected from the group consisting of EDTA, propylparaben and methylparaben.

### Claim 8 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulation is a solid.

### Claim 9 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulation is in the form of a gel, aerosol, or form.

### Claim 10 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulation is a suppository.

### Claim 11 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the amount of glycerin is less than or equal to about 0.1% (w/w).

### Claim 12 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the NRTI is tenofovir.

### Claim 13 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulation comprises about 300 mg of the NRTI.

### Claim 14 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11)

A method for the treatment of the symptoms or effects of an HIV infection in an infected animal which comprises administering to said animal the formulation of any of claims 1-11.