Inclusion complexes of taxol or taxotere or taxus extract formed with cyclodextrins, its preparation and use
AssigneeChinoin Ltd.
InventorsLajos Szente, József Szejtli, Andrasne Vikmon
Life of this patent
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Abstract
The present invention relates to an active inclusion complex of Taxol, Taxotere or a Taxus extract formed with a cyclodextrin-derivative, a pharmaceutical composition containing the same, a process of preparation and a method of treatment.
Claims18
Inclusion complex of Taxol [2aR-[2aα,4β;4αβ,6β,9α(αR*,βS*), 11α-12α,12aα,12bα]]-β-(Benzoylamino)-α-hydroxybenzene-propanoic acid 6,12-b-bis (acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihyroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca [3,4]-benz-[1,2-b]oxet-9-yl ester or Taxotere (butoxycarbonyl-10-deacetyl-N-debenzoyl taxol) or Taxus extracts formed with a cyclodextrin derivative.
Inclusion complex of Taxol with a cyclodextrin derivative.
Inclusion complex of a Taxus brevifolia solvent free extract comprising besides Taxol other diterpene taxan-derivatives with a cyclodextrin derivative.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with heptakis-2,6-0-dimethyl-β-cyclodextrin.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with randomly methylated-β-cyclodextrin.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with succinyl-methyl-β-cyclodextrin.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with 2-hydroxy propyl-β-cyclodextrin.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with a soluble anionic-β-cyclodextrin-polymer.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with β-cyclodextrin.
Inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with γ-cyclodextrin.
Process for the preparation of the inclusion complex of Taxol or Taxotere or a Taxus brevifolia extract formed with a cyclodextrin-derivative which comprises:
- a.) reacting Taxol or Taxotere or a Taxus brevifolia extract in an aqueous medium with a cyclodextrin derivative and isolating the complex from the mixture,
- b.) reacting Taxol or Taxotere or a Taxus brevifolia extract with a cyclodextrin derivative in a solid form, or
- c.) high energy milling of Taxol or Taxotere or a Taxus brevifolia extract with a cyclodextrin derivative.
Pharmaceutical composition comprising as active ingredient an effective amount of the inclusion complex of Taxol or Taxotere or a Taxus extract formed with a cyclodextrin derivative, and conventional pharmaceutical filling, diluting and further auxiliary materials.
Method of treatment of cancer in humans orally, parenterally which comprises administering to the human an effective amount of an inclusion complex of Taxol or Taxotere or Taxus extract formed with a cyclodextrin derivative.
Dependencies are inferred from the claim text.