Pharmaceutical dosage form for transdermal administration

• US 6,538,039 B2
• Filed: 10/31/1996
• Issued: 03/25/2003
• Est. Priority Date: 04/29/1994
• Status: Expired due to Fees

• Current Assignee: Laboratoire L. Lafon
• Original Assignee: Laboratoire L. Lafon
• Inventors: Laurent, Philippe
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): TRAN, SUSAN T
• Application Number:
  US08/741,967
• Publication Number:
  US 20020111387A1
• Time in Patent Office: 2,336 Days
• Field of Search: 514/772.2, 424/60, 424/401, 424/63
• US Class Current: 514/772.2
• CPC Class Codes: A61K 9/7015 Drug-containing film-forming compositions, e.g. spray-on

Abstract

The present invention relates to a process for administering an active principle to a patient transdermally, which comprises the formation of a film on the patient'"'"'s skin, by applying to the skin a liquid solution which consists essentially of:

a) a lipophilic active principle,

b) from 2.5 to 25% by weight of a silicone-based adhesive polymer composition,

c) from 0 to 25% by weight of an absorption promoter, and

d) from 25 to 95% by weight of volatile solvents comprising volatile silicones.

Claims

1. Process for transdermally administering a lipophilic active ingredient, comprising applying to the skin of a patient a liquid solution to effect formation of a film on the patient'"'"'s skin, wherein the liquid solution comprises:

a) a lipophilic active ingredient selected form the group consisting of hormones, steroids, and lipophilic vitamins,

b) from 2.5 to 25% by weight of a polydimethylsiloxane-oil-based adhesive polymer composition,

c) from 5 to 25% by weight of an absorption promoter, and

d) from 25 to 95% by weight of volatile silicone solvent,

said liquid solution being free of water, whereby, after evaporation of said volatile silicone solvent, a polydimethylsiloxane-oil-based film forms on the skin, which film transdermally delivers said lipophilic active ingredient to the patient.

2. Process as claimed in claim 1, in which the polydimethylsiloxane oils are selected from dimethicones of formula:

where n is an integer below 5000, and dimethiconols.

3. Process as claimed in claim 1, in which the adhesive polymer composition represents 2.5 to 12% of the weight of the solution.

4. Process as claimed in claim 1, in which the adhesive polymer composition represents 2.5 to 10% of the weight of the solution.

5. Process as claimed in claim 1, comprising 50 to 95% by weight of volatile silicones.

6. Process as claimed in claim 1, in which the volatile silicone is selected from the group consisting of polydimethylcyclosiloxanes and polysiloxanes of low molecular weight.

7. Process according to claim 1, said solution further comprising 0 to 25% by weight of a volatile solvent other than a volatile silicone.

8. Process as claimed in claim 1, in which the lipophilic active ingredient is selected from the group consisting of vitamin D₃ and its hydroxylated derivatives.

9. Process as claimed in claim 1, in which a defined dose of said solution is delivered on the skin and said dose is spread on the skin.

10. Process as claimed in claim 1, said liquid solution comprising:

a) the lipophilic active ingredient selected from the group consisting of oestrogens, progestogens and mixtures thereof,

b) from 2.5 to 25% by weight of the polydimethylsiloxane oil-based adhesive polymer composition,

c) from 5 to 25% by weight of the absorption promoter, and

d) from 35 to 55% by weight of the volatile silicone, and

e) from 0 to 35% by weight of the volatile polar solvent.

11. Composition for transdermally administering a lipophilic active ingredient, said composition being a liquid solution comprising:

a) a lipophilic active ingredient selected from the group consisting of hormones, steroids, and lipophilic vitamins,

b) from 2.5 to 25% by weight of a polydimethylsiloxane-oil-based adhesive polymer composition,

c) from 5 to 25% by weight of an absorption promoter, and

d) from 35 to 95% by weight of volatile silicone solvent,

said liquid solution being free from water and said solution forms, upon applying to the skin of a patient and evaporation of said volatile silicone solvent, a polydimethylsiloxane-oil-based film transdermally delivering said lipophilic active ingredient to the patient.

12. Composition as claimed in claim 11, for the formation of a film on the skin for the transdermal administration of a lipophilic active ingredient selected from the group consisting of oestrogens, progestogens, and mixtures thereof, said composition being a liquid solution which comprises:

a) the lipophilic active ingredient, selected from oestrogens, progestogens and mixtures thereof,

b) from 2.5 to 25% by weight of the polydimethylsiloxane-oil-based adhesive polymer composition,

c) from 5 to 25% by weight of the absorption promoter,

d) from 35 to 55% by weight of the volatile silicone solvent, and

e) from 0 to 35% by weight of a volatile polar solvent,

said liquid solution being free from water.

13. Composition for transdermally administering a lipophilic active ingredient, said composition being a liquid solution consisting essentially of:

a) a lipophilic active ingredient selected from the group consisting of hormones, steroids, and lipophilic vitamins,

b) from 2.5 to 25% by weight of a polydimethylsiloxane-oil-based adhesive polymer composition,

c) from 5 to 25% by weight of an absorption promoter, and

d) from 35 to 95% by weight of volatile silicone solvent,

said liquid solution being free from water and said solution forms, upon applying to the skin of a patient and evaporation of said volatile silicone solvent, a polydimethylsiloxane-oil-based film transdermally delivering said lipophilic active ingredient to the patient.