Pharmaceutical composition in the form of a gel or a solution based on dihydrotestosterone, process for preparing it and uses thereof

• US 20040072810A1
• Filed: 06/06/2003
• Published: 04/15/2004
• Est. Priority Date: 12/07/2001
• Status: Abandoned Application

• Current Assignee: Besins Healthcare Luxemborg SARL (Besins Healthcare, Inc.)
• Original Assignee: Besins International Belgique
• Inventors: Masini-Eteve, Valerie, Taravella, Brigitte
• Application Number:
  US10/456,868
• Publication Number:
  US 20040072810A1
• Time in Patent Office: Days
• US Class Current: 514/177
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• 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 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• 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: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis

Abstract

The present invention relates to a pharmaceutical composition in the form of a hydro-alcoholic gel or a solution for transdermal application, comprising:

from about 0.2% to about 1.5% of dihydrotestosterone;

and from about 0.2 to about 3% of isopropyl myristate.

Claims

1. Pharmaceutical composition in the form of a hydro-alcoholic gel or a solution for transdermal application, comprising:

from about 0.2% to about 1.5% of dihydrotestosterone;

and from about 0.2% to about 3% of isopropyl myristate;

these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.

2. Pharmaceutical composition according to claim 1, having a dihydrotestosterone content of about 0.7%, these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.

3. Pharmaceutical composition of claim 1, having a content of isopropyl myristate from about 0.45 to about 2%, these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.

4. Pharmaceutical composition of claim 2, having a content of isopropyl myristate of about 0.7%, these percentages being expressed by weight relative to 100 g of the pharmaceutical composition.

5. Pharmaceutical composition according to claim 1, wherein the alcoholic solvent is selected from the group consisting of ethanol, isopropanol and mixtures thereof.

6. Pharmaceutical composition according to claim 1, having a content of from about 50 to about 75% of absolute ethanol, these percentages being expressed by weight relative to 100 g of formulation.

7. Pharmaceutical composition according to claim 6, having a content of about 66% of absolute ethanol, these percentages being expressed by weight relative to 100 g of formulation.

8. Pharmaceutical composition according to claim 1, having a content of from about 0.2 and about 2% of a gelling agent, these percentages being expressed by weight relative to 100 g of formulation.

9. Pharmaceutical composition according to claim 1, having a content of about 0.5% of a gelling agent, these percentages being expressed by weight relative to 100 g of formulation.

10. Pharmaceutical composition according to claim 8, wherein the gelling agent is selected from the group consisting of carbomers, cellulose derivatives and mixtures thereof.

11. Pharmaceutical composition according to claim 8, wherein the gelling agent is a carbomer.

12. Pharmaceutical composition according to claim 8, wherein the gelling agent is Carbopol®

980 (carboxyvinyl polymer grade 980, polymerized in an ethyl acetate/cyclohexane system).

13. Pharmaceutical composition according to claim 8, further comprising a neutralizing agent.

14. Pharmaceutical composition according to claim 13, wherein the neutralizing agent is selected from the group consisting of triethanolamine, sodium hydroxide, ammonium hydroxide, potassium hydroxide, arginine, aminomethylpropanol and tromethamine, and mixtures thereof.

15. Pharmaceutical composition according to claim 13, wherein the neutralizing agent/gelling agent ratio is from about 3/1 to about 0.5/1.

16. Pharmaceutical composition according to claim 14, wherein the neutralizing agent is triethanolamine.

17. Pharmaceutical composition according to claim 15, wherein the neutralizing agent/gelling agent ratio is about 1/1.

18. Process for preparing a pharmaceutical composition according to claim 1, comprising the following steps:

a mixture comprising DHT, isopropyl myristate and an alcoholic solvent is prepared;

a gelling agent is optionally added to this mixture, and mixing is again carried out;

a neutralizer is optionally added, and mixing is then again carried out;

the pharmaceutical composition containing DHT is recovered.

19. Process according to claim 18, wherein the alcoholic solvent is selected from the group consisting of ethanol, isopropanol or mixtures thereof.

20. Method for the treatment of physiological conditions associated with insufficiency of dihydrotestosterone, comprising the step of administering a pharmaceutical composition according to claim 1 to a subject.

21. Method according to claim 21, wherein the physiological conditions are selected from the group consisting of permanent hypogonadism, functional hypogonadism, hyperplasia of the prostate, gynaecomasty, balano-preputial sclero-atrophic lichen in men and vulval sclero-atrophic lichen in women, or micropenis in children.