Hainan Hdeton Science and Technology Co., Ltd.

Meridian Laboratories, Inc.

Shuqin Yu

Yong Ren

Jianfeng Gao

Ling Wu

Xiaodong Sun

Xueqin Ma

A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056 M-13051 M), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 &#x3bc;m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

Pharmaceutical composition containing docetaxel-cyclodextrin inclusion complex and its preparing process

A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056M-13051M), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 &#x3bc;m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

A pharmaceutical composition comprising cyclodextrin/paclitaxel inclusion, which consists of paclitaxel, cyclodextrin and a pharmaceutically acceptable excipient, wherein the mass ratio of the paclitaxel to cyclodextrin is 1:10-150, the said cyclodextrin is hydroxylpropyl-sulfobutyl-7-&#x3b2;-cyclodextrin, or sulfobutylether-7-&#x3b2;-cyclodextrin, or their mixture; the stability constant of the cyclodextrin/paclitaxel inclusion is Ka=5396M&#x2212;1&#x2212;1412M&#x2212;1. The preparation method of the pharmaceutical composition is as follow: (a) A solution of cyclodextrin is added dropwise to a solution of paclitaxel in ethanol. (b) The resulting mixture is filtered through microporous membrane of 0.2-0.4 &#x3bc;m after being dissolved. (c) Ethanol is removed under reduced pressure to give a liquid inclusion which has the ethanol level of less than 2%, or alternatively water is also removed under reduced pressure, the resulting product is dried giving a solid inclusion.

Pharmaceutical composition comprising cyclodextrin paclitaxel inclusion and preparation method thereof

Hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin, the preparation method, analytical method, and the pharmaceutical application thereof. The hydroxypropyl-sulfobutyl-&bgr;-cyclodextrin is a derivate of cyclodextrin which is substituted by hydroxypropyl group and sulfobutyl group: n-(2,3,6-O-2-hydroxypropyl)-m-(2,3,6-O-sulfobutyl)-&bgr;-cyclodextrin. The number of substituent groups per mole cyclodextrin is n hydroxypropyl groups and m sulfobutyl groups. 'n' represents the average substituent degree of hydroxypropyl groups; 'm' represents the average substituent degree of sulfobutyl groups; &#x201c;n+m=z&#x201d; is the gross average substituent degree, in which n is a random integer chosen from 1,2,3,4,5,6,7,8,9; m is a random integer chosen from 1,2,3,4,5,6,7,8,9; and the gross average substituent degree z is a random integer chosen from 2,3,4,5,6,7,8,9,10. The present invention shows low haemolysis and low toxicity.

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Jiangsu, China

Shuqin Yu