本文選題：鹽酸魯拉西酮 + 固體分散體　； 參考：《中國藥房》2017年34期

【摘要】：目的:制備鹽酸魯拉西酮固體分散體,提高其溶出度。方法:選用聚維酮K30為載體,以溶劑法制備不同藥載比(1:0.5、1:1、1:2)的鹽酸魯拉西酮固體分散體。比較3種鹽酸魯拉西酮固體分散體與物理混合物(鹽酸魯拉西酮-聚維酮K30)、原研制劑的體外溶出度;采用X射線粉末衍射法對鹽酸魯拉西酮原料藥、聚維酮K30與外加輔料、物理混合物(1:2)與外加輔料、鹽酸魯拉西酮固體分散體(1:2)與外加輔料的晶體結(jié)構(gòu)進(jìn)行分析。結(jié)果:藥載比1:0.5、1:1、1:2的鹽酸魯拉西酮固體分散體溶出速率較物理混合物有顯著提高,且載體比例越大,固體分散體溶出越快;藥載比為1:2的鹽酸魯拉西酮固體分散體與原研制劑20 min時體外溶出度分別為101.2%、100.2%。X射線粉末衍射結(jié)果顯示,物理混合物中存在鹽酸魯拉西酮和輔料的特征吸收峰;鹽酸魯拉西酮固體分散體中的鹽酸魯拉西酮特征吸收峰基本消失,輔料特征吸收峰仍存在。結(jié)論:以藥載比1:2制得的鹽酸魯拉西酮固體分散體與原研制劑體外溶出行為相似,且其中鹽酸魯拉西酮以無定形存在。
[Abstract]:Objective: to prepare Lurassetron hydrochloride solid dispersion and improve its dissolution. Methods: solid dispersions of roxidone hydrochloride with different drug loading ratios of 1: 0. 5 and 1: 1: 1: 2 were prepared by solvent method using polyvidone K30 as carrier. To compare the dissolution of three kinds of solid dispersion and physical mixture of Lurassetron hydrochloride with physical mixture (Lurassetron Hydrochloride and Polyvinylidene K30), the dissolution rate of the original preparation was studied by X-ray powder diffraction (XRD) method for the determination of raw material drug, polyvinylethone K30 and excipients for Lurassetron Hydrochloride. The crystal structure of the physical mixture (1: 2) and the adjunct, and the solid dispersion of Lurassetron hydrochloride (1: 2) were analyzed. Results: the dissolution rate of the solid dispersion of Lurassetron hydrochloride at the ratio of 1: 0.5 to 1: 1: 2 was significantly higher than that of the physical mixture, and the larger the carrier ratio, the faster the dissolution rate of the solid dispersion. The dissolution in vitro of the solid dispersion of Lurassetron hydrochloride at 1:2 was 101.2% and 100.2% at 20 min. The X-ray powder diffraction results showed that there were characteristic absorption peaks of roxidone hydrochloride and excipients in the physical mixture. The characteristic absorption peak of roxidone hydrochloride in the solid dispersion of Lurassetron hydrochloride is almost disappeared, and the characteristic absorption peak of excipient still exists. Conclusion: the solid dispersion of Lurassetron hydrochloride prepared by 1:2 drug loading ratio is similar to that of the original preparation in vitro, and there is an amorphous form of Lurassetron hydrochloride.
【作者單位】： 常州制藥廠有限公司;
【分類號】：R943

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