| 摘要: |
| 目的：将盐酸尼卡地平制成肠溶缓释固体分散体，以促进其在肠道内溶出，提高制剂的生物利用度。方法：以水溶性材料（PEG6000）和肠溶性材料(Ⅱ丙烯酸树脂)为混合载体，采用溶剂法制备了盐酸尼卡地平固体分散体。通过正交实验设计，筛选得到了具有理想肠溶缓释效果的处方。结果：盐酸尼卡地平制成的肠溶缓释固体分散体在人工肠液中3 h释放量为54.33％，10 h释放量为80.18％。其体外释药方式符合Higuchi 方程。DTA分析和X-射线粉末衍射证实药物以无定形态分散于载体中。结论：以固体分散体制备的肠溶缓释微丸具有促进药物溶出、定位缓慢释放的作用。 |
| 关键词: 盐酸尼卡地平 固体分散体 迟效制剂 |
| DOI： |
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| 基金项目: |
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| Study on nicardipine hydrochloride intestinal-dissolved sustained-release pellets |
| 崔孟,孙其荣,钟延强,刘善奎 |
| () |
| Abstract: |
| Objective: To prepare nicardipine hydrochloride solid dispersion to promote the dissolution and improve bioavailability of drugs in vivo and in vitro. Methods: Nicardipine hydrochloride solid dispersion was developed using Ⅱ acrylic resin and PEG6000 as mixed carrier by the solvent evaporating method. The orthogonal test was employed in the design of the formulations. Results: The percentage released of nicardipine hydrochloride solid dispersion in artificial intestinal liquid was 54.33%and 80.18%at 3 h and 10 h, respectively. The DTA and X-ray powder diffractometry showed that nicardipine hydrochloride was amorphously dispersed in the solid dispersion. The released profiles in vitro of the solid dispersion followed Higuchi equation. Conclusion: Nicardipine hydrochloride intestinal-dissolved sustained-release pellets are prepared by traditional method which combine the advantages of pellets and solid dispersion. |
| Key words: nicardipine hydrochloride solid dispersion sustained-release pellets |
