NOVEL COMPLEXES OF TAXOL OR TAXOTERE AND PHARMACEUTICAL COMPOSITIONS

• Main Authors: SZEMAN, JULIANNA, SZEJILI, JOZSEF, SZENTE, LAJOS, VIKMON, ANDRASNE
• Format: Patent
• Language: English; French; German
• Published: 23.04.2003
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

This invention provides inclusion complexes of Taxol ((2aR-(aalpha,4beta,4alphabeta,6beta,9alpha(alphaR*,betaS*),11alpha,12alpha,12aalpha,12balpha))-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-desacetyl-N-debenzoyl-Taxol) or Taxus extracts formed with a cyclodextrin derivative and a co-solvent. 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 derivative 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.