赖诺普利迟释型缓释片的制备及其体外释放研究

发布时间：2019-06-20 09:54

【摘要】：目的:制备赖诺普利迟释型缓释片,并对其体外释放度进行测定。方法:以羟丙甲纤维素(HPMC)为片芯骨架材料,乙基纤维素为阻滞材料,聚乙二醇(PEG)为致孔剂,利用包衣技术制备赖诺普利迟释型缓释片。以6、10、16、22 h的累积释放度(Q6 h、Q10 h、Q16 h、Q22 h)为指标,采用正交试验优化HPMC型号、用量和PEG用量,并进行验证。比较自制赖诺普利迟释型缓释片、自制赖诺普利缓释片芯和市售赖诺普利片在0.1 mol/L盐酸溶液中22 h内的Q。结果:最优处方为HPMC型号为K100M,占片芯质量比例为35%,PEG比例为40%,即600片赖诺普利迟释型缓释片中含赖诺普利18 g、乳糖54 g、HPMC(K100M)48 g、PEG 1.6 g、10%聚维酮乙醇溶液适量、硬脂酸镁1%、微粉硅胶1%、乙基纤维素2.4 g;所制3批赖诺普利迟释型缓释片的Q6 h、Q10 h、Q16 h、Q12 h的均值分别为11.17%、29.55%、62.38%、82.63%。自制赖诺普利缓释片芯Q10 h达80%以上,Q14 h为95.60%;市售赖诺普利片的Q5 min即达80%以上,Q1 h为97.95%;自制赖诺普利迟释型缓释片Q6 h仅为13.97%,Q22 h为84.12%,其释放特征符合零级动力学模型。结论:成功制得体外延迟4 h释放药物,并可缓慢释放22 h的赖诺普利迟释型缓释片。
[Abstract]:Objective: to prepare and determine the release rate of lisinopril sustained-release tablets in vitro. Methods: using hydroxypropyl methylcellulose (HPMC) as core skeleton material, ethyl cellulose as blocking material and polyethylene glycol (PEG) as pore-forming agent, the slow-release sustained-release tablets of lisinopril were prepared by coating technique. Taking the cumulative release rate of 6, 10, 16, 22 h (Q6 h, Q10 h, Q16 h, Q22 h) as the index, the HPMC model, dosage and PEG dosage were optimized by orthogonal test and verified. The self-made lisinopril sustained-release tablets were compared with those of the self-made lisinopril sustained-release tablets in 0.1 mol/L hydrochloric acid solution within 22 h with those of the self-made lisinopril sustained-release tablets and the marketed lisinopril tablets in 0.1 mol/L hydrochloric acid solution within 22 h. Results: the optimal prescription of HPMC was K100M, accounting for 35% of the core mass, and 40% of HPMC, that is, 600 tablets of lisinopril sustained-release tablets contained 18 g of lisinopril, 54 g of lactose, 48 g of HPMC (K100M), 1.6 g of PEG, 10% of povidone ethanol solution, 1% of magnesium stearate, 1% of silica gel and 2.4 g of ethyl cellulose. The results showed that the optimal prescription was as follows: Lainopril 18 g, lactose 54 g, PEG 1.6 g, 10% povidone ethanol solution, magnesium stearate 1%, silica gel 1%, ethyl cellulose 2.4 g. The Q6 h, Q16 h and Q12 h mean values of three batches of lisinopril sustained-release tablets were 11.17%, 29.55%, 62.38% and 82.63%, respectively. The Q5 min and Q1h of the self-made lisinopril sustained-release tablets were more than 80% and 95.60% at 10 h and 95.60%, 80% and 97. 95% respectively, and those of the self-made lisinopril sustained-release tablets were only 13.97% at Q6 h and 84.12% at Q22 h. The release characteristics were in accordance with the zero-order kinetic model. Conclusion: the sustained release tablets of lisinopril with delayed release in vitro for 4 hours and slow release for 22 hours were successfully prepared.
【作者单位】：台州职业技术学院;浙江华海药业股份有限公司;
【基金】：浙江省高技能人才培养和技术创新活动计划项目(No.2011R30051)
【分类号】：R943

【参考文献】