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AssigneeChinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
InventorsJosef Szejtli, Lajos Szente, Agoston David, Sandor Virag, Gyula Sebestyen, Attila Mandi
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The invention relates to an inclusion complex of 1-(p-chloro-benzoyl)-5-methoxy-2-methyl-indol-3-yl-acetic acid (indomethacin) and cyclodextrin of a molar ratio of about 2:1. The inclusion complex can be prepared by reacting about 2 moles of alpha or beta cyclodextrin with about 1 mole of 1-(p-chloro-benzoyl)-5-methoxy-2-methyl-indol-3-yl-acetic acid under heating in the presence of an organic solvent which dissolves indomethacin and does not form a stable complex with cyclodextrin. The new complex is at least as active antiinflammatory agent as indomethacin and at the same time shows substantially less ulcerative side-effect.
An inclusion complex of cyclodextrin and Indomethacin in a molar ratio of about 2:1.
An inclusion complex of cyclodextrin and Indomethacin in a molar ratio of 1.9:1 to 2.1:1.
A process for the preparation of an inclusion complex in a molar ratio of about 2:1 of cyclodextrin to 1-(p-chloro-benzoyl)-5-methyl-2-methyl-indol-3-yl-acetic acid (Indomethacin) which comprises reacting about 2 moles of .alpha.- or .beta.-cyclodextrin with about 1 mole of 1-(p-chloro-benzoyl)-5-methoxy-2-methyl-indol-3-yl-acetic acid with heating to a temperature sufficient to form the inclusion complex in the presence of an inert organic solvent dissolving Indomethacin and not forming a stable complex with cyclodextrin, and isolating the formed complex.
A pharmaceutical composition of antiinflammatory activity containing an effective amount of an inclusion complex of cyclodextrin and Indomethacin in a molar ratio of about 2:1 and a pharmaceutically acceptable inert solid or liquid carrier.
Dependencies are inferred from the claim text.