Pharmaceutical preparation with an active substance of low solub

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules

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424456, 514781, 514786, 514789, A61K 900, A61K 966

Patent

active

047271094

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 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.

REFERENCES:
patent: 3197369 (1965-07-01), Widmann et al.
patent: 4177254 (1979-12-01), Khan et al.
patent: 4198391 (1980-04-01), Grainger
patent: 4572833 (1986-02-01), Pedersen et al.
patent: 4574080 (1986-03-01), Roswall et al.
patent: 4595583 (1986-06-01), Eckenhoff et al.
patent: 4605548 (1986-08-01), Ushiyama et al.

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