Cymipristone solid preparation and preparation methods thereof

Abstract

The invention discloses preparation methods of a cymipristone solid preparation. A method 1 comprises the following steps: dissolving cymipristone in a solvent to obtain a drug-containing solution, then evenly mixing auxiliary materials with the drug-containing solution, and performing wet granulation, wherein, the solvent is an organic solvent or an aqueous solution containing more than 85% of an organic solvent by mass percent. A method 2 comprises the following steps: dissolving the cymipristone in an acid solution containing an acidulant to obtain a drug-containing acid solution, then evenly mixing the auxiliary materials with the drug-containing acid solution, and performing wet granulation. The invention further discloses the cymipristone solid preparation prepared by the methods. The preparation methods disclosed by the invention avoid the defects such as serious pollution, great loss and serious potential safety hazard caused by mechanical pulverization, and the methods are simple and feasible in operation and have a high safety factor, thus being applicable to industrial production. The cymipristone solid preparation prepared by the methods has the advantages of excellent leaching property, better stability and better content uniformity.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid preparation of cymipristone and a preparation method thereof. Background technique [0002] Cymipristone belongs to steroidal compounds, chemical name: 11β-(4-(N-methyl-N-cyclohexylamino)phenyl)-17β-hydroxy-17α-(1-propynyl)-estr Ste-4,9-dien-3-one, with a molecular weight of 497.71, has dual effects of progesterone receptor antagonism and glucocorticoid receptor antagonism. Chinese patent document CN1287123 discloses its preparation method and its pharmaceutical composition and application. [0003] Cymipristone is a weak base drug and is insoluble in water. When preparing solid preparations, cymipristone needs to be pulverized to a certain fineness to ensure that the solid preparations can dissolve rapidly after oral administration. At present, mechanical pulverization is generally used for the pulverization of poorly water-soluble drugs. Howeve...

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Problems solved by technology

[0008] The technical problem to be solved by the present invention is to overcome the existing method for preparing cymipristone solid preparations by selecting and controlling the particle size of cymipristone through mechanical crushing, which will cause environmental pollution, large loss, and serious potential safety hazards. And the dissolution characteristics of cymipristone solid pharmaceutical preparations are still not ideal enough defects, and provide easier operation, less pollution, no aforementioned safety hazards, and can significantly improve the dissolution characteristics of the obtained cymipristone solid preparations, and ensure better A preparation method with good stability and content uniformity, and a solid preparation of cymipristone prepared by the method

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