Merck Patent Gesellschaft MIT Beschrankter Haftung

Behringwerke Aktiengesellschaft

R.p. Scherer Corporation

Peter C Schmidt

Hartmut Hartner

Hans Bardonner

Arno Basedow

Friedrich Reiff

Hans-Wolfgang Hugenbusch

Hans P Kraemer

Hans H Sedlacek

Gerhard Fischer

Bernd Stockebrand

Harald Perschbacher

Klaus-Jurgen Steffens

Paul H List

A pharmaceutical formulation for the parenteral, in particular intravenous, administration of sparingly soluble substances is obtained when the very finely ground substance, with a maximum particle diameter of 3 .mu.m, is dispersed in an oil phase which contains emulsifier, and this mixture is emulsified with water for injection, is rendered isotonic and is homogenized using a high-pressure homogenizer, so that the resultant product is a solid/liquid/liquid disperse system.

Pharmaceutical formulation and process for its preparation

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 in contact with the gastric juices a renewing permeable membrane. Suitable adjuvants are ethylcellulose, cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate and vinylacetate crotonic acid copolymers or mixtures thereof.

Pharmaceutical preparation with an active substance of low solubility in

A modified sorbitol with improved tableting properties, viz, has a melting point of about 96.degree. C., a bulk density of 0.3-0.6 g/ml, a .gamma.-sorbitol content of at least 90%, a purity of at least 98%, a specific surface area of 0.7-1.5 m.sup.2 /g, a bending strength of at least 7 N/mm.sup.2 at a compressive force of at least 10,000 N, and a friability of less than 1% at a compressive force of at least 10,000 N, can be prepared by obtaining a sorbitol solution by hydrogenation of crystallized glucose at a temperature below 170.degree. C., and spray-drying this solution at a temperature of 140.degree. to 170.degree. C. The sorbitol thus obtained has a water content of less than 1%. The sorbitol is useful for the production of compressed formulations.

Sorbitol, process for its preparation, and use thereof

Growing community of inventors

Marburg, Germany

Peter C Schmidt