Aqueous crystalline suspension of steroid glycoesters

US4794119A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Paul-Eberhard Schulze
• Bernard Acksteiner · Berlin, DE
• Bernd Dusterberg · Berlin, DE

Key dates

• Filing date: Mar 27, 1986
• Grant date: Dec 27, 1988
• Expiry date: Mar 27, 2006

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J1/0096
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

An aqueous crystalline suspension of a 17-tertiary steroid glycoester contains a compound of Formula I ##STR1## wherein X is two hydrogen atoms or an oxygen atom, PA1 Y is two hydrogen atoms or a methylene group, PA1 R.sup.1 is hydrogen or methyl, PA1 Z is hydroxy or --O--CO--R.sup.2 PA1 R.sup.2 is methyl or phenyl, and ##STR2## in the following fractions: 0-30% by weight of a particle size of 3-15 .mu.m, PA1 40-90% by weight of a particle size of 15-60 .mu.m, and PA1 20-60% by weight of a particle size of 30-100 .mu.m. Upon a one-time intramuscular injection of 30-75 mg of steroid glycoester as an aqueous crystalline suspension, a steroid level is achieved in the plasma which, over a period of 4 weeks, is adequately high and shows a uniform course.