Pharmaceutical composition containing lipophilic drugs

• US 5,514,673 A
• Filed: 04/07/1994
• Issued: 05/07/1996
• Est. Priority Date: 04/07/1993
• Status: Expired due to Fees

• Current Assignee: Astra AB (Astrazeneca PLC)
• Original Assignee: Astra AB (Astrazeneca PLC)
• Inventors: Kutz, Gerd, Heckenmuller, Harald
• Primary Examiner(s): Griffin, Ronald W.
• Application Number:
  US08/224,164
• Time in Patent Office: 761 Days
• Field of Search: 424/450, 424/434, 514/938, 514/899, 514/177, 514/182, 552/607, 552/625
• 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 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system

Abstract

A pharmaceutical composition having a form suitable for transmucosal administration containing progesterone and/or 17-β-estradiol as an active ingredient.

Claims

1. A pharmaceutical composition for transmucosal administration based on progesterone and/or 17-β

-estradiol as an active ingredient characterized in that the active ingredient is dissolved in an oil constituting the incoherent inner phase of an oil-water two-phase system.

2. A pharmaceutical composition according to claim 1 characterized in that at least one of progesterone or 17-β

-estradiol is a natural sex hormone.

3. A pharmaceutical composition according to claim 1 characterized in that the oil is a natural oil.

4. A pharmaceutical composition according to claim 1 characterized in that the oil is an artificial oil.

5. A pharmaceutical composition according to claim 1 characterized in that the oil is a mixture of a natural oil and an artificial oil.

6. A pharmaceutical composition according to claim 1 characterized in that the solubility of progesterone in the oil phase is at least 2% by weight.

7. A pharmaceutical composition according to claim 1 characterized in that the solubility of 17-β

-estradiol in the oil phase is at least 0.5% by weight.

8. A pharmaceutical composition according to claim 1 characterized in that it contains 3 μ

g to 0.5 mg of estradiol and/or 0.1-10 mg of progesterone.

9. A pharmaceutical composition according to claim 1 for nasal administration.

10. A pharmaceutical composition according to claim 1 containing pharmaceutically acceptable excipients together with the active compound(s).

11. A pharmaceutical composition according to claim 1 in unit dosage form.

12. A process for the manufacture of a pharmaceutical preparation according to claim 1 characterized in that progesterone and/or 17-β

-estradiol is dissolved in an oil phase whereby the inner phase of an oil in water two phase system for transmucosal administration is obtained.

13. A process for the manufacture of a pharmaceutical preparation according to claim 1 wherein the oil phase is admixed with the water phase.

14. A method of administering progesterone and/or 17-β

-estradiol to a mammal by transmucosal delivery comprising applying an effective amount of the composition of claim 1 to the mucosal membrane of the mammal.