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Topical composition for follicular delivery of an ornithine decarboxylase inhibitor

A technology of ornithine decarboxylase and composition, which is applied in drug combination, pill delivery, aerosol delivery, etc., and can solve problems such as difficult to distinguish the efficacy of DFMO preparations

Inactive Publication Date: 2007-06-13
SKINMEDICA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Complicating the situation is the fact that the analysis of hair masses makes it difficult to differentiate the efficacy of different DFMO formulations

Method used

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  • Topical composition for follicular delivery of an ornithine decarboxylase inhibitor
  • Topical composition for follicular delivery of an ornithine decarboxylase inhibitor
  • Topical composition for follicular delivery of an ornithine decarboxylase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

Method to measure drug delivery to hair follicles

[0040] Dead body scalp or bearded skin with hair was collected within 24 hours of death. The removed skin was stored at -70°C. The refrigerated skin was thawed in normal saline maintained at 30°C before use. After thawing, excess subcutaneous fat was clipped from the skin, and the hair was trimmed using electric scissors so that the hair length on the skin surface was 1-2 mm. The skin was then cut into slices of appropriate size and placed in a Franz diffusion cell (0.63 cm 2 ), maintained at 37°C, as the acceptor phase. 30 [mu]l of radiolabeled preparation (1-3 [mu]Ci of radiolabeled eflornithine hydrochloride, 99% minimum radiochemical purity) was gently applied to the skin surface with a glass rod. In vitro diffusion studies were performed 3 to 24 hours after application of the formulation, with Vaniqa in each study  as a positive control. The amount of drug delivered to the hair follicle can be measured by epilati...

Embodiment 2

Lotion A

components ％

Stearyl ether-20 5

Stearyl ether-100 5

Mineral oil 1.9

Stearyl Alcohol 3

Simethicone-200 1

Cetyl Alcohol 1

Eflornithine Hydrochloride Monohydrate * 15

water 68.1

* Equivalent to 13.9% eflornithine hydrochloride

[0045] The preparation of above-mentioned lotion composition is as follows:

[0046] The aqueous phase consisting of eflornithine hydrochloride monohydrate and water is heated to 65-70°C. Heat the oil phase consisting of the remaining ingredients to 65-70°C. The oil and water phases were mixed under stirring and the mixing was continued until the temperature was 30-35°C.

Embodiment 3

Lotion B

components ％

Stearyl ether-20 5

Stearyl ether-100 5

Mineral oil 1.9

Stearyl Alcohol 3

Simethicone-200 0.5

Glyceryl Stearate and PEG-100 Stearate 2.5

Cetearyl Alcohol and Ceteareth-20 2.5

Eflornithine Hydrochloride Monohydrate * 15

water 64.6

* Equivalent to 13.9% eflornithine hydrochloride

[0047] The above-mentioned lotion composition was prepared according to the method of Example 2.

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Abstract

Use the general formula CH 3 (CH 2 ) x CH 2 (OCH 2 CH 2 ) n Polyglycol ethers of alkyl alcohols of OH, wherein x is 8-20 (wherein ceteareth-20, stearyl ether-20 and stearyl ether-100 are preferred), poloxamer 185, Poloxamer 407, N, N-dimethyldodecylamine N-oxide and mixtures thereof to improve the hair follicle transport and / or hair follicle residence time of certain water-soluble ornithine decarboxylase inhibitors, preferred inhibitors are 2-(difluoromethyl)-2,5-diaminovaleric acid and its pharmaceutically acceptable salts, hydrates, optical enantiomers and racemic mixtures.

Description

field of invention [0001] The present invention relates to a topical formulation capable of enhancing the delivery, preferably increasing the residence time, of ornithine decarboxylase inhibitors (hereinafter referred to as "ODC inhibitors") in hair follicles of mammalian skin, preferably human skin, for regulating , preferably to reduce the rate of hair growth. A preferred ODC inhibitor is 2-(difluoromethyl)-2,5-diaminopentanoic acid, also known as alpha-(difluoromethyl)ornithine (hereinafter "DFMO"). DFMO hydrochloride is the most preferred inhibitor, which will be referred to hereafter by the USAN (United States Adopted Name) nomenclature "Eflornithine Hydrochloride". Eflornithine HCl is a highly charged compound that does not readily penetrate the skin or hair follicles. The composition of the present invention includes ODC inhibitors, preferably DFMO, its pharmaceutically acceptable salts and hydrates, optical enantiomers (R, S) and racemic mixtures (RS), more preferabl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K8/44A61Q7/02A61K8/00A61K9/06A61K8/02A61K8/06A61K8/30A61K8/36A61K8/39A61K8/40A61K8/41A61K8/43A61K8/49A61K8/60A61K8/64A61K8/66A61K8/72A61K8/86A61K9/00A61K9/08A61K9/107A61K9/12A61K9/20A61K9/70A61K31/13A61K31/132A61K31/155A61K31/198A61K31/7076A61K47/10A61K47/18A61K47/34A61P17/14A61P43/00A61Q5/00A61Q5/02A61Q7/00
CPCA61K8/39A61K31/198Y10S514/947Y10S514/937A61K8/41A61K9/0014A61K8/40A61Q7/02Y10S514/969Y10S514/946Y10S514/944A61K8/86A61K2800/782A61K47/10A61K31/13Y10S514/945A61K8/44A61P17/14A61P43/00A61K8/69A61K8/81
Inventor 乔伊斯T·周普拉卡什·帕拉博
Owner SKINMEDICA INC
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