Preparation of lipophile:hydroxypropylcyclodextrin complexes by a method using co-solubilizers

US5120720A · kind A · utility

Assignee

• The United States of America as Represented by the Secretary of the Department of Health and Human Services · US

Inventors

• Josef Pitha · Baltimore, US
• Juan J. Torres-Labandeira · Coruña, ES
• Tetsumi Irie · Kumamoto, JP

Key dates

• Filing date: Sep 20, 1990
• Grant date: Jun 9, 1992
• Expiry date: Sep 20, 2010

Classification

• Technology area (CPC B): Performing Operations; Transporting
• CPC primary: B82Y5/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The dissolution of lipophilic compounds in aqueous solutions of hydroxypropylcyclodextrins can be accelerated by the addition of co-solubilizers, such as ethanol or ammonia, which again can be removed, together with water, by evaporation or by freeze-drying leaving lipophile: hydroxypropylcyclodextrin complexes as a residue. The co-solubilizer method was used successfully with steroid drugs (5-androstene-3.beta.,17.beta.-diol, 4-androstene-3,17-dione, dehydroepiandrosterone, dexamethasone, 5-.alpha.-dihydro-testosterone, 6-methylprednisolone, and testosterone), peptides (gramicidin S) and a macrocyclic antibiotic (amphotericin B). The complexes prepared in this manner were amorphous and possessed satisfactory stability.