Inclusion complexes of clavulanic acid and of alkali salts there

Details Inclusion complexes of clavulanic acid and of alkali salts there Inclusion complexes of clavulanic acid and of alkali salts there

1995-06-06

1997-03-25

Venkat, Jyothsna

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

424451, 424461, 424464, 424465, 424479, A61K 900

Patent

active

056141998

ABSTRACT:
Described is a new process for the preparation of alkali clavulanate from an aqueous solution of crude clavulanic acid, which is obtained in a conventional manner after the fermentation with a clavulanic-acid-producing microorganism, extracted with an ethyl acetate solution of a hydrophobic .beta.-CD derivative such as heptakis-(2,3,6-tri-O-acetyl)-.beta.-CD in at least equimolar ratio with regard to clavulanic acid. The resulting novel inclusion complexes of clavulanic acid and hydrophobic .beta.-CD derivative in a molar ratio about 1:1 are isolated, purified and then converted with an alkali base or alkali alkanoate to the desired alkali clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable alkali salts both with hydrophilic .beta.-CD derivatives and with hydrophobic .beta.-CD derivatives, processes for the preparation thereof and the use thereof for the preparation of galenic forms with immediate as well as with sustained action, in combination with amoxicillin trihydrate, which are valuable medicaments in the therapy of infectious diseases.

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