# US 8,784,878 B2 · Transdermal delivery rate control using amorphous pharmaceutical compositions

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- Number: US 8,784,878 B2
- Document ID: US8784878B2
- Status: Granted
- Kind: B2
- Application number: 13/710,761
- Filed: 2012-12-11
- Published: 2013-11-28
- Granted: 2014-07-22
- Earliest claimed: 2002-06-25
- Assignees: Acrux DDS Pty Ltc.
- Applicants: Acrux DDS Pty Ltd
- Inventors: Timothy Matthias Morgan; Nina Frances Wilkins; Kathryn Traci-Jane Klose; Barrie Charles Finnin; Barry Leonard Reed
- Web page: https://patentgrep.com/patent/US8784878B2

## CPC

- A61K 31/568: substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/12: Aerosols; Foams {(A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015)}
- A61K 9/7015: {Drug-containing film-forming compositions, e.g. spray-on}
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/18: Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 5/26: Androgens
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 11/08: Bronchodilators
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/06: Antimigraine agents
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 33/06: Antimalarials
- 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

A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.

## Claims

### Claim 1

A non-occlusive transdermal pharmaceutical composition for the transdermal delivery of testosterone, comprising:
(a) from 0.1% to 10% by weight of testosterone;
(b) from 0.1% to 10% by weight of one or more dermal penetration enhancers selected from the group consisting of octyl salicylate and Padimate O; and
(c) from 85% to 99.8% by weight of a volatile solvent selected from the group consisting of ethanol, isopropanol, and mixtures thereof;
wherein the combination of testosterone and dermal penetration enhancer(s) is such that the composition, upon application and evaporation of the solvent at physiological temperatures, forms an amorphous deposit comprising an amorphous phase containing the dermal penetration enhancer(s) and testosterone.

### Claim 2 (depends on 1)

A composition according to claim 1, wherein the molar ratio of testosterone to dermal penetration enhancer is from 1:20 to 20:1.

### Claim 3 (depends on 1)

A composition according to claim 1, wherein the composition consists of the testosterone, the penetration enhancer(s), the volatile solvent(s) and, optionally, a gelling agent.

### Claim 4 (depends on 1)

A composition according to claim 1, wherein the penetration enhancer is octyl salicylate.

### Claim 5

A non-occlusive pharmaceutical composition for transdermal delivery of testosterone, consisting of:
(a) from 0.1% to 10% by weight of testosterone;
(b) from 0.1% to 10% by weight of one or more dermal penetration enhancers selected from the group consisting of octyl salicylate and Padimate O; and
(c) from 85% to 99.8% by weight of a volatile solvent selected from the group consisting of ethanol, isopropanol, and mixtures thereof; and
(d) optionally a gelling agent;
wherein the combination of testosterone and dermal penetration enhancer(s) is such that the composition, upon application and evaporation of the solvent at physiological temperatures, forms an amorphous deposit comprising an amorphous phase, containing the dermal penetration enhancer(s) and testosterone.

### Claim 6 (depends on 1)

A method of transdermally delivering testosterone to a subject in need thereof, comprising applying a composition according to claim 1 to the skin of the subject.

### Claim 7 (depends on 6)

The method of claim 6, wherein the composition consists of the testosterone, the penetration enhancer(s), the volatile solvent(s) and, optionally, a gelling agent.