盐酸鲁拉西酮固体分散体的制备、表征及体外溶出行为研究

发布时间：2018-05-28 17:47

本文选题：盐酸鲁拉西酮 + 固体分散体　；参考：《中国药房》2017年34期

【摘要】：目的:制备盐酸鲁拉西酮固体分散体,提高其溶出度。方法:选用聚维酮K30为载体,以溶剂法制备不同药载比(1:0.5、1:1、1:2)的盐酸鲁拉西酮固体分散体。比较3种盐酸鲁拉西酮固体分散体与物理混合物(盐酸鲁拉西酮-聚维酮K30)、原研制剂的体外溶出度;采用X射线粉末衍射法对盐酸鲁拉西酮原料药、聚维酮K30与外加辅料、物理混合物(1:2)与外加辅料、盐酸鲁拉西酮固体分散体(1:2)与外加辅料的晶体结构进行分析。结果:药载比1:0.5、1:1、1:2的盐酸鲁拉西酮固体分散体溶出速率较物理混合物有显著提高,且载体比例越大,固体分散体溶出越快;药载比为1:2的盐酸鲁拉西酮固体分散体与原研制剂20 min时体外溶出度分别为101.2%、100.2%。X射线粉末衍射结果显示,物理混合物中存在盐酸鲁拉西酮和辅料的特征吸收峰;盐酸鲁拉西酮固体分散体中的盐酸鲁拉西酮特征吸收峰基本消失,辅料特征吸收峰仍存在。结论:以药载比1:2制得的盐酸鲁拉西酮固体分散体与原研制剂体外溶出行为相似,且其中盐酸鲁拉西酮以无定形存在。
[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.
【作者单位】：常州制药厂有限公司;
【分类号】：R943

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