NOVEL COMPLEXES AND THEIR COMPOSITIONS

摘要

This invention provides inclusion complexes of Taxol {[2aR-[a alpha ,4 beta ,4 alpha beta ,6 beta ,9 alpha ( alpha R*, beta S*,) 11 alpha ,12 alpha , 12a alpha , 12b alpha ,]]- beta -(benzoylamino)- alpha -hydroxy-benzene-propanoic acid 6,12-b-bis(acetyloxy)-12-(benzoyloxy)-2a, 3, 4, 4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclo-deca-[3,4]-benz-[1,2-b]-oxeth-9-yl-ester]} or Taxotere (butoxycarbonyl-10-desacethyl-N-debenzoyl-Taxol) or Taxus extracts formed with a cyclodextrin derivative and a co-solvent. The molar ratio of Taxol, Taxotere or Taxus extract to cyclodextrin is 1:(10-65), preferably 1:(30-40). This invention relates to pharmaceutical composition with increased water-solubility and stability. This invention provides the process for the preparation of an inclusion complex of Taxol or Taxotere or a brevifolia extract of Taxus formed with a cyclodextrin derivatice and a co-solvent. This invention relates to pharmaceutical composition, containing as active ingredient an effective amount of an inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with a cyclodextrin derivative, preferably heptakis-2,6-0-dimethyl- beta -cyclodextrin, random methylated beta -cyclodextrin, succinylmethyl- beta -cyclodextrin and a co-solvent together with usual filling, diluting and other auxiliaries generally used in the pharmaceutical industry. This invention provides pharmaceutical compositions comprising an inclusion complex of Taxol, Taxotere or Taxus extracts formed with a cyclodextrin or a cyclodextrin derivative as active ingredient, they further contain ethanol or an ethanol-water mixture. Accordingly composition of this invention may be administered for the treatment of human cancer.