Inclusion complexes of butylphthalide with cyclodextrin or...

Details Inclusion complexes of butylphthalide with cyclodextrin or... Inclusion complexes of butylphthalide with cyclodextrin or...

C - Chemistry, Metallurgy

08

L

C08L 5/16 (2006.01) A61K 31/343 (2006.01) A61K 31/724 (2006.01) A61K 47/48 (2006.01) C07D 307/88 (2006.01) C08B 37/16 (2006.01)

Patent

CA 2494157

The present invention relates to the inclusion complexes of butylphthalide, which is D, L-mixed or levorotatory, with cyclodextrin or cyclodextrin derivatives, to a process for their preparation and the use thereof. In the invention, the butylphthalide is complexed with cyclodextrin or cyclodextrin derivatives, preferably with hydroxypropyl- .beta.-cyclodextrin, in order to increase the water-solubility of butylphthalide, develop clinical solid or liquid formulations and improve the therapeutic effect of butylphthalide. The inclusion complex, in which the molar ratio of butylphthalide to cyclodextrin or cyclodextrin derivatives is in the range of 1:1-10, can be used to prepare infusion, injection, injectable powder, liquids for oral administration, syrup, tablets, granules, dispersible tablets and others.

Clathrates de phtalide butylique, sous forme de mélange dextrogyre / lévogyre ou lévogyres, qui sont associés à de la cyclodextrine ou à ses dérivés, procédé de préparation desdites compositions et leur utilisation. Selon la présente invention, le phtalide butylique est associé à la cyclodextrine ou à ses dérivés, afin d'améliorer l'hydrosolubilité du phtalide butylique, et mettre au point des formulations cliniques solides ou liquides de manière que l'effet curatif du phtalide butylique puisse être amélioré. Le clathrate dans lequel le rapport molaire du phtalide butylique à la cyclodextrine ou à ses dérivés est de 1/1-10, peut être utilisé pour la préparation de transfusions, d'injections, de poudre injectable, de liquides à administration orale, de sirops, de comprimés, de granules, de comprimés dispersibles et autres.

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