Dermal penetration enhancers and drug delivery systems involving the same

• US 8,071,075 B2
• Filed: 10/05/2007
• Issued: 12/06/2011
• Est. Priority Date: 02/19/1996
• Status: Expired due to Fees

• Current Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Original Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Inventors: Reed, Barry Leonard, Morgan, Timothy Matthias, Finnin, Barrie Charles
• Primary Examiner(s): Arnold, Ernst
• Assistant Examiner(s): Yu, Hong
• Application Number:
  US11/905,926
• Publication Number:
  US 20080152597A1
• Time in Patent Office: 1,523 Days
• Field of Search: None
• US Class Current: 424/47
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 8/046 Aerosols; Foams
• CPC Class Codes: A61K 8/37 Esters of carboxylic acids
• CPC Class Codes: A61K 8/445 aromatic, i.e. the carboxylic acid directly linked to the aromatic ring
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• CPC Class Codes: A61K 9/122 Foams; Dry foams edible foams A61K9/0056
• CPC Class Codes: A61M 35/003 Portable hand-held applicators having means for dispensing or spreading integral media hand-held massage devices with liquid delivery A61H7/003
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 15/16 Masculine contraceptives
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61P 17/14 for baldness or alopecia
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 : Anxiolytics
• CPC Class Codes: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/22 : for herpes viruses
• CPC Class Codes: A61P 33/06 : Antimalarials
• CPC Class Codes: A61P 35/00 : Antineoplastic agents
• CPC Class Codes: A61P 39/00 : General protective or antinoxious agents
• CPC Class Codes: A61P 5/24 : of the sex hormones
• CPC Class Codes: A61P 5/26 : Androgens
• CPC Class Codes: A61P 5/30 : Oestrogens
• CPC Class Codes: A61P 7/02 : Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/12 : Antihypertensives
• CPC Class Codes: A61Q 17/04 : Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: Y02A 50/30 : Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The invention relates to a method for treatment or prophylaxis of a disease or condition in an animal comprising administering to a mucosal membrane of said animal in need of such treatment a therapeutically effective amount of a drug delivery system comprising at least one physiologically active agent or prodrug thereof and at least one penetration enhancer selected from safe ester sunscreens.

Claims

1. A transdermal drug delivery system comprising:

(a) a therapeutically effective amount of testosterone;

(b) at least one dermal penetration enhancer present in an amount of from 10 to 10,000 wt % based on the weight of the testosterone;

wherein the dermal penetration enhancer is at least one ester of formula (I);

2. A drug delivery system according to claim 1, wherein said ester is a C₈ to C₁₈ alkyl para-aminobenzoate, C₈ to C₁₈ alkyl dimethyl-para-aminobenzoate, C₈ to C₁₈ alkyl cinnamate, C₈ to C₁₈ alkyl methoxycinnamate or C₈ to C₁₈ alkyl salicylate.

3. A drug delivery system according to claim 2, wherein said ester is octyl dimethyl-para-aminobenzoate, octyl para-methoxycinnamate or octyl salicylate.

4. A drug delivery system according to claim 1, wherein the drug delivery system is not supersaturated with respect to the testosterone.

5. A method for the treatment of a testosterone deficient hypogonadal man which comprises administering to a dermal surface of said man in need of such treatment a therapeutically effective amount of the drug delivery system according to claim 1.

6. The transdermal drug delivery system according to claim 3, wherein said ester is octyl salicylate.

7. The transdermal drug delivery system according to claim 3, wherein said volatile liquid is selected from the group consisting of ethanol, isopropanol, and a mixture thereof.

8. The drug delivery system according to claim 6, wherein said volatile liquid is selected from the group consisting of ethanol, isopropanol, and a mixture thereof.

9. The method according to claim 5, wherein said ester is a C₈ to C₁₈ alkyl para-aminobenzoate, C₈ to C₁₈ alkyl dimethyl-para-aminobenzoate, C₈ to C₁₈ alkyl cinnamate, C₈ to C₁₈ alkyl methoxycinnamate or C₈ to C₁₈ alkyl salicylate.

10. The method according to claim 9, wherein said ester is octyl dimethyl-para-aminobenzoate, octyl para-methoxycinnamate, or octyl salicylate.

11. The method according to claim 10, wherein said ester is octyl salicylate.

12. The method according to claim 10, wherein said volatile liquid is selected from the group consisting of ethanol, isopropanol, and a mixture thereof.

13. The method according to claim 11, wherein said volatile liquid is selected from the group consisting of ethanol, isopropanol, and a mixture thereof.