Medicament containing a 2-arylpropionic acid derivative in nanosol form and its preparation

US5560924A · kind A · utility

Assignees

• ALFATEC-Pharm GmbH · DE
• Paz Arzneimittelentwicklungsgesellschaft mbH · DE

Inventors

• Jens-Christian Wunderlich · Heidelberg, DE
• Ursula Schick · Schriesheim, DE
• Jurgen Werry · Ludwigshafen, DE
• Jurgen Freidenreich · Schriesheim, DE
• Helmut H. Lukas · Carleton Place, CA
• Otto Schuster · Bad Soden, DE

Key dates

• Filing date: Sep 29, 1994
• Grant date: Oct 1, 1996
• Expiry date: Sep 29, 2014

Classification

• Technology area (CPC G): Physics
• CPC primary: G03C2001/0471
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Immediate-effect medicaments containing a pharmacologically active 2-arylpropionic acid derivate as a pharmaceutically applicable nanosol have a considerably improved action start and bioavailability of the active substance. The 2-arylpropionic acid derivates, for example ibuprofen, flurbiprofen and ketoprofen, that are scarcely soluble in an aqueous medium, are present in a gelatine-stabilized nanosol in a form that allows these active substances to be quickly and completely resorbed already in the stomach. The disclosed colloidal disperse system composed of a 2-arylpropionic acid derivate is prepared by selecting a gelatine or gelatine derivate according to their isoelectric point (IEP), so that their IEP is adapted to the charge of the 2-arylpropionic acid derivate particles, leading to a neutral charge when the gelatine or its derivate is combined with the undissolved 2-arylpropionic acid derivate at a determined pH value. The gelatine or its derivate are converted into an aqueous sol form, their pH value is set according to the IEP of the gelatine at a value that stabilizes the nanoparticles of 2-arylpropionic acid derivate at an approximately or totally neutral charge. Before…