| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject compound useful as e.g. an antitumor agent by clathration of a fluoroprogesterone derivative with a cyclodextrin so as to improve absorbability of the above antineoplastic derivative by oral administration. SOLUTION: This clathrate compound is obtained by reaction of a mixture of a fluoroprogesterone derivative of the formula (R<1> is a 1-23C hydrocarbon group)(e.g. 9α-fluoro-6αmethylprogesterone), cyclodextrin (e.g. dimethylβ- cyclodextrin) and water under agitation for 24 h using a stirrer at room temperature followed by centrifugal separation to remove insolubles and then lyophilizing the resultant supernatant. Next, this clathrate compound is incorporated with cornstarch as vehicle, croscarmellose sodium as disintegrant, sodium laurel sulfate as disintegrating auxiliary and 5% aqueous solution of hydroxypropyl ctellulose to conduct granulation followed by drying and then addition of magnesium stearate as lubricant, thus obtaining art antitumor agent.
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