Bioadhesive tablet containing testosterone/testosterone ester mixtures and method for producing a predetermined testosterone time-release profile with same

US6977083B1 · kind B1 · utility

Assignee

• Jenapharm GmbH & Co. KG · DE

Inventors

• Doris Huebler · Schmieden, DE
• Guenter Kaufmann · Jena, DE
• Michael Oettel · Jena, DE
• Holger Zimmermann · Falkensee, DE
• Michael Dittgen · Apolda, DE
• Sabine Fricke · Jena, DE
• Manfred Boese · Jena, DE
• Ralf Ladwig · Jena, DE
• Sven Claussen · Jena, DE
• Carsten Timpe · Bad Birnbach, DE

Key dates

• Filing date: Sep 30, 1999
• Grant date: Dec 20, 2005
• Expiry date: Sep 30, 2019

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K9/006
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The method of making a bioadhesive tablet for controlling testosterone blood level, especially in elderly men suffering from partial androgen deficiency, includes spray-drying an alcoholic solution or suspension of testosterone and at least one testosterone ester, preferably in a ratio of 1:10 to 1:1.5, separately or together, with an organic polymer and optionally one or more auxiliary ingredient to form an active ingredient premix. Then various other auxiliary ingredients are mixed, as needed, with the active ingredient premix to form the bioadhesive tablet with an active ingredient layer and an adhesive layer. The active ingredient layer contains an effective amount of the active ingredient premix. The adhesive layer includes auxiliary ingredients including the bioadhesive polymer. The bioadhesive tablet may be buccally administered to provide a predetermined timed release profile of testosterone, advantageously varying according to a circadian rhythm.