Pharmaceutical preparation with an active substance of low solubility in water and gastric juices

US4727109A · kind A · utility

Assignee

• R.P. Scherer Corporation · US

Inventors

• Peter C. Schmidt · Leverkusen, DE
• Bernd Stockebrand · Wittlich, DE
• Gerhard Fischer · Hannover, DE

Key dates

• Filing date: Dec 30, 1985
• Grant date: Feb 23, 1988
• Expiry date: Dec 30, 2005

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K9/4858
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A pharmaceutical preparation having an active substance of low solubility in water and gastric juices that has an initially liquid carrier system consisting of a hydrophilic component, a hydrophobic component and a solubilizer. The solvent mixture contains 9 to 90 parts by weight of solubilizer and 90 to 5 parts by weight of a hydropholic component, such as polyethylene glykol, 1,2-propylene glykol, 1,3-butanediol, 1,4-butanediol, 1,2-propanediol, glycerol, mannitol, sorbitol or polyoxyethylene polyoxypropylene copolymerisate or mixtures of such substances, and 40 to 1 parts by weight of an oleophilic component, such as natural and/or semisynthetic vegetable or animal oils or synthetic oils, such as neutral oil or waxes. The active substance is dissolved in the carrier system or dispersed in a stable way and for an oral application, is filled into drug capsules made of gelatine. In order to achieve a delayed release of the active substance (delayed-action effect), an adjuvant that is soluble in the carrier system is also added to the carrier system in the amount of up to 10 parts by weight, preferably 2 to 5 parts by weight that, after the dissolving of the capsule wall, develops i…