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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
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| 篇名： | 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 |
| TITLE： | |
| 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 the lurasidone hydrochloride solid dispersion， and improve its dissolution rate. METHODS： Taking povidone K30 as the carrier， solvent method was used to prepare the lurasidone hydrochloride solid dispersion with different drug-load ratios （1 ∶ 0.5， 1 ∶ 1， 1 ∶ 2）. The in vitro dissolution rates of 3 kinds of lurasidone hydrochloride solid dispersion with physical mixture （lurasidone hydrochloride-povidone K30） and original preparation were compared. X-ray powder diffraction method was adopted to analyze the crystal structures of raw material of lurasidone hydrochloride， povidone K30 and accessories， physical mixture （1 ∶ 2） and accessories， and lurasidone hydrochloride solid dispersion （1 ∶ 2） and accessories. RESULTS： Compared with physical mixture， the dissolution rate of lurasidone hydrochloride solid dispersion with drug-load ratios of 1 ∶ 0.5， 1 ∶ 1， 1 ∶ 2 was significantly improved， and the dissolution rate of solid dispersion was increased as the increase of the carrier ratio. The in vitro dissolution rates of lurasidone hydrochloride solid dispersion with drug-load ratio of 1 ∶ 2 and original preparation were respectively 101.2％ and 100.2％ in 20 min. X-ray powder diffraction showed， there were characteristic absorption peaks of lurasidone hydrochloride and accessories in physical mixture； the characteristic absorption peak of lurasidone hydrochloride in solid dispersion disappeared basically， and the characteristic absorption peak of accessories still existed. CONCLUSIONS： The in vitro dissolution of lurasidone hydrochloride solid dispersion with drug-load ratio of 1 ∶ 2 is similar to original preparation， and lurasidone hydrochloride exists in the solid dispersion as amorphous form. |
| 期刊： | 2017年第28卷第34期 |
| 作者： | 赵海涛，宋光西，殷学治，吴沉，王兵 |
| AUTHORS： | ZHAO Haitao，SONG Guangxi，YIN Xuezhi，WU Chen，WANG Bing |
| 关键字： | 盐酸鲁拉西酮；固体分散体；聚维酮K30；溶出度 |
| KEYWORDS： | Lurasidone hydrochloride； Solid dispersion； Povidone K30； Dissolution rate |
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