盐酸坦洛新肠溶缓释微丸的制备及其体内外评价

发布时间：2018-04-27 05:18

本文选题：盐酸坦洛新 + 肠溶缓释微丸　；参考：《中国新药杂志》2015年02期

【摘要】：目的:制备盐酸坦洛新肠溶缓释微丸,并与参比制剂进行体内外一致性评价。方法:分别以乙基纤维素和羟丙甲纤维素为缓释包衣材料,以聚丙烯酸树脂为肠溶性包衣材料,采用流化床底喷包衣技术对载药微丸包衣,制备肠溶缓释微丸;考察释放度主要影响因素;采用多条释放曲线对比考察受试制剂与参比制剂体外一致性;双周期交叉试验设计,考察Beagle犬口服单剂量受试制剂与参比制剂后血浆中的药物浓度,评价受试制剂与参比制剂的体内一致性;考察受试制剂的体内外相关性。结果:确定了影响盐酸坦洛新释放的主要处方工艺因素;多条释放曲线测定结果表明,所制备的微丸与参比制剂体外一致性较好;Beagle犬体内药动学研究结果表明,受试制剂与参比制剂生物等效且体内外相关性良好。结论:成功制备了盐酸坦洛新肠溶缓释微丸,且与参比制剂体内外一致性良好。
[Abstract]:Aim: to prepare Tanluoxin hydrochloride sustained-release pellets and evaluate their consistency with reference preparation in vitro and in vivo. Methods: using ethylcellulose and hydroxypropylcellulose as sustained-release coating materials and polyacrylic acid resin as enteric-soluble coating materials, pellets were coated with fluidized bed bottom spray technique to prepare enteric-soluble sustained-release pellets. To investigate the main influencing factors of release rate, to compare the consistency of test preparation and reference preparation with multiple release curves, to investigate the plasma concentration of Beagle canine after oral single dose test preparation and reference preparation, and to investigate the in vitro consistency of test preparation and reference preparation. To evaluate the consistency of test preparation and reference preparation in vivo and to investigate the correlation between in vivo and in vitro. Results: the main prescription factors affecting the release of Tanluo hydrochloride were determined, and the results of multiple release curves showed that the prepared pellets were in good agreement with the reference preparation in vitro, and the pharmacokinetics of the prepared pellets was better than that of the reference preparation in vivo. The bioequivalence of the tested preparation and the reference preparation is good in vivo and in vitro. Conclusion: Tanluoxin hydrochloride sustained-release pellets have been successfully prepared and have good consistency with reference preparation in vivo and in vitro.
【作者单位】：重庆医科大学药学院药剂学教研室;福安药业集团重庆礼邦药物开发有限公司;重庆医药工业研究院有限责任公司;重庆市化学制药工程技术研究中心;
【分类号】：R96

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