盐酸坦洛新肠溶缓释微丸的制备及其体内外评价  

Preparation of tamsulosin hydrochloride enteric-coated sustained-release pellets and the evaluation in vitro and in vivo

作　　者：胡佳[1] 张涛 黄华[1] 欧云国[3,4] 林羽[3,4] 唐波[3,4] 

机构地区：[1]重庆医科大学药学院药剂学教研室,重庆400016 [2]福安药业集团重庆礼邦药物开发有限公司,重庆401121 [3]重庆医药工业研究院有限责任公司,重庆400061 [4]重庆市化学制药工程技术研究中心,重庆400061

出　　处：《中国新药杂志》2015年第2期221-227,共7页Chinese Journal of New Drugs

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。Objective： To prepare tamsulosin hydrochloride enteric-coated sustained-release pellets,and investigate the consistency with reference preparation in vitro and in vivo. Methods： The core pellets were coated by fluidized bed bottom spray coating technology. EC and HPMC were used as sustained-release coating materials,and Eudragit as enteric-coated coating material. The main factors influencing the drug release characteristics were evaluated. Multiple dissolution profile was used to investigate the in vitro consistency of the test and reference preparations. Double-period crossover trial design was used to compare the plasma concentrations of drug after single oral doses of the test and reference preparations in dogs. The in vivo consistency was investigated,and the in vitro and in vivo correlation was evaluated. Results： The main factors affecting drug release were identified. Multiple dissolution profile showed that the test preparation has good in vitro consistency with the reference preparation. The pharmacokinetic study in dogs showed that the test preparation were bioequivalent with the reference preparation,and had a close in vitro and in vivo correlation. Conclusion： The tamsulosin hydrochloride enteric-coated sustainedrelease pellets have been successfully achieved by our method,and have good in vitro and in vivo consistency with reference preparation.

关 键 词：盐酸坦洛新 肠溶缓释微丸 生物等效 体内外一致性 体内外相关性 

分 类 号：R943.41[医药卫生—药剂学] R971.9[医药卫生—药学]