Immediate release dosage form for HRT

• US 20040229854A1
• Filed: 02/18/2004
• Published: 11/18/2004
• Est. Priority Date: 11/28/2000
• Status: Abandoned Application

• Current Assignee: Haan D.E. Pieter
• Original Assignee: Haan D.E. Pieter
• Inventors: Haan De, Pieter
• Application Number:
  US10/781,493
• Publication Number:
  US 20040229854A1
• Time in Patent Office: Days
• US Class Current: 514/178
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61K 9/2004 Excipients; Inactive ingredients

Abstract

It has been recognized that tibolone, which is an agent in the treatment of menopausal complaints and osteoporosis, if formulated with a particle size in a defined range, displays an unexpectedly high bioavailability of one of its estrogenic metabilites, Org A.

Claims

1-12. -12. (Cancelled, without prejudice or disclaimer)

13. A method of treatment or prevention of menopausal complaints, comprising administering to a patient in need thereof an effective amount of a pharmaceutical formulation in the form of an immediate-release peroral dosage unit, comprising tibolone, wherein the pharmaceutical formulation has a bioavailability, in vivo, of 3^α

-OH tibolone at a level above that provided by a solution of tibolone, wherein the amount of tibolone in the immediate-release peroral dosage unit and in the tibolone solution are substantially the same.

14. The method of claim 13, wherein the tibolone in the immediate-release peroral dosage unit has a mean particle size below about 22.8 μ

m.

15. The method of claim 14, wherein the tibolone in the immediate-release peroral dosage unit has a mean particle size below about 20 μ

m.

16. The method of claim 13, wherein the rate of dissolution of tibolone from the pharmaceutical formulation is such that when the pharmaceutical formulation is subjected to a dissolution-test, wherein a sample of said pharmaceutical formulation containing 2.5 mg of tibolone is exposed to a 0.25% sodium lauryl sulfate solution and the dissolution rate is measured, a t₅₀% value about 23.1 minutes is obtained.

17. The method of claim 16, wherein the tibolone in the immediate-release peroral dosage unit has a mean particle size below about 22.8 μ

m.