Inclusion complexes of clavulanic acid and of potassium salts th

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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424470, 536103, C07D48704, A01K 926

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active

054987881

ABSTRACT:
Described is a new process for the preparation of alkali clavulanate from an aqueous solution of pure clavulanic acid and of pharmaceutically acceptable potassium 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 equimolar amount or up to 10% excess 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 with water and then converted with potassium 2-ethyl hexanate to the potassium clavulanate, which is isolated. Furthermore, there are described new inclusion complexes of clavulanic acid and of its pharmaceutically acceptable potassium salt 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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