Sustained-release forms of alpha-(2,5-dimethoxy phenyl)-beta-glycinamidoethanol and process for their preparation

Abstract

Abstract 1. Claims for the Contracting States : BE CH DE FR GB IT LI LU NL SE Oral sustained-release forms of alpha-(2,5-dimethoxyphenyl)-beta-glycinamidoethanol (midodrin) in the form of solid shaped pharmaceutical articles, produced by compressing, and consisting of the active compound, a polymeric support material and, if appropriate, auxiliaries and additives customary in pharmaceutical formulation, characterized in that the sustained-release form contains 1 to 15 parts by weight of poly-D(-)-3-hydroxybutyric acid having a molecular weight of at least 50,000 and a selected particle size fraction in the range from 0.05 to 0.6 mm to one part by weight of alpha-(2,5-dimethoxyphenyl)-beta-glycinamidoethanol in the form of the hydrochloride (midodrin hydrochloride) in a homogeneous mixture. 1. Claims for the Contracting State : AT Process for the preparation of oral sustained-release forms of alpha-(2,5-dimethoxyphenyl)-beta-glycinamidoethanol (midodrin) in the form of solid shaped pharmaceutical articles, produced by compressing, and consisting of the active compound, a polymeric support material and, if appropriate, auxiliaries and additives customary in pharmaceutical formulation, characterized in that the active compound alpha-(2,5-dimethoxyphenyl)-beta-glycinamidoethanol in the form of the hydrochloride (midodrin hydrochloride) is mechanically mixed in a weight ratio of 1:1 to 1:15 with poly-D(-)-3-hydroxybutyric acid having a molecular weight of at least 50,000, which has been obtained from the fermentation product in a selected particle size fraction in the range from 0.05 to 0.6 mm by grinding and sieve analysis, homogenized and compressed to give shaped pharmaceutical articles, if appropriate with the addition of auxiliaries and additives customary in pharmaceutical formulation, under a pressure of 0.1 to 10 tonnes/cm**2 , corresponding to 9.81 to 981 N/mm**2 .

Inventors

• 👤 Werner Dr. Korsatko
• 👤 Brigitta Korsatko-Wabnegg

Bibliographic Details