| 杨 茜,张新蕊,李 蒙,刘 婷,郑爱萍.乙酰唑胺缓释胶囊的制备与体外释放评价[J].,2024,(17):3201-3204 |
| 乙酰唑胺缓释胶囊的制备与体外释放评价 |
| Preparation and in vitro Release of Acetazolamide Extended-release Capsules |
| 投稿时间：2024-03-27 修订日期：2024-04-23 |
| DOI：10.13241/j.cnki.pmb.2024.17.001 |
| 中文关键词: 乙酰唑胺 缓释 挤出滚圆 体外释放 |
| 英文关键词: Acetazolamide Extended-release Extrusion-spheronization Release in vitro |
| 基金项目:国家重大新药创制项目（2013ZX09402103） |
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| 中文摘要: |
| 摘要 目的：采用挤出滚圆工艺制备乙酰唑胺缓释微丸，并进行体外释放评价。方法：采用离子交换色谱法测定参比制剂中功能性辅料十二烷基硫酸钠的处方含量。参照参比制剂处方组成，以水不溶性的微晶纤维素作为缓释微丸的骨架材料，羟丙基纤维素水溶液作为粘合剂，通过挤出和滚圆过程使得微丸成为致密的类球体，从而缓慢的释放药物。以软材粘性和释放曲线作为主要考察指标，采用挤出滚圆工艺制备乙酰唑胺缓释微丸，微丸干燥后灌装硬胶囊。分别测定自制制剂和参比制剂在pH 1.2盐酸水溶液、pH 4.5 乙酸盐缓冲液、pH 6.8 磷酸盐缓冲液和纯水介质中的释放曲线，采用相似因子（f2）法比较释放曲线的相似性。结果：自制制剂与参比制剂的辅料种类和用量基本一致，微丸的制备工艺较为简便，在不同介质中均能缓慢释放药物，且自制制剂和参比制剂在不同介质中的释放曲线趋势相似，释放曲线的相似因子（f2）数值均大于50。结论：自制制剂的体外释放行为与参比制剂相比具有一致性。 |
| 英文摘要: |
| ABSTRACT Objective: To prepare acetazolamide extended-release pellets by extrusion-spheronization process and assess its release behavior in vitro. Methods: Ion exchange chromatography was applied to determine the content of sodium lauryl sulfate as the functional excipient in the formulation of the reference listed drug. According to the formulation analysis of the reference listed drug, the water-insoluble microcrystalline cellulose was used as the matrix material of extended-release pellets, and the hydroxy propyl cellulose aqueous solution was used as the adhesive excipient. Through extrusion-spheronization process, the pellets became dense spheroids, so as to slowly release the drug. When viscosity of damp mass and release curves of capsules were considered as the main indexes, acetazolamide extended-release pellets were prepared by extrusion-spheronization process, dried and filled into capsules. The release curves of the self-made preparation and the reference drug in pH1.2 hydrochloric acid solution, pH 4.5 acetate buffer, pH 6.8 phosphate buffer and water were determined respectively. And the similarity factor (f2) method was used to compare the similarity of the release curves between two formulations. Results: The types and amounts of excipients of the self-made preparation and the reference listed drug are basically the same. The preparation process of the pellets is relatively simple. And drugs can be released slowly from the self-made preparation in four different media. The release curve trends of the self-made preparation and the reference listed drug in four different media were basically similar, and the similarity factor (f2) values of the release curve between two formulations were all above 50. Conclusion: The release behavior in vitro of the self-made preparation was consistent with that of the reference listed drug. |
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