苯磺酸左氨氯地平分散片的制备及质量研究

Preparation and Quality Investigation of Levoamlodipine Besylate Dispersible Tablets

目的制备苯磺酸左氨氯地平分散片并评价其质量。方法采用辅料相容性研究和崩解时间为指标筛选崩解剂的种类和用量;采用正交试验设计方案,优化最佳处方和制备工艺,通过初步稳定性考查,认证处方组成的合理性。结果相容性试验表明:乳糖和苯磺酸左氨氯地平具有配伍禁忌;优化处方组成:主药苯磺酸左氨氯地平3.47 mg,微晶纤维素(MCC)70 mg,磷酸氢钙30 mg,淀粉30 mg,崩解剂交取聚乙烯吡轿咯烷酮(PVPP 8%),矫味剂阿斯巴甜5 mg。2.5%聚乙烯吡咯烷酮(PVP-k30)水溶液制粒,硬脂酸镁1%。采用内外加崩解剂(内加4%,外加4%),片剂崩解效果最好。最佳崩解时间<85 s,10 min溶出百分率明显高于普通片(P<0.05),初步稳定性试验结果表明,加速和室温留样6个月制剂质量稳定,各项指标符合质量标准要求。结论苯磺酸左氨氯地平分散片处方组成合理,工艺稳定,体外溶出速率明显优于普通片,可适用于工业化生产。

Objective To prepare Levoamlodipine Besylate dispersible tablets, and evaluate its quality. Methods Different disintegrates were screened, and the best formulation was optimized by orthogonal experiment design using the disintegration time and dissolution as indexes. The best formulation of Levoamlodipine Besylate dispersible tablets was authenticated by the initial stability experiment. Results Lactose is incompatible with Levoamlodipine Besylate. The best formulation of Levoamlodipine Besylate dispersible tablets was composed of Levoamlodipine Besylate 3.47 mg, MCC 70 mg, brushite 30 mg, starch 30 mg, PVPP 8%, aspartame 5 mg, 2. 5% polyvidone k30 queous solution quantity sufficient, and 1% Magnesium stearate. The effect of disintegration was much optimized when PVPP were used in coordinationwith exterior addition （4%） and interior addition （4%）. The result showed that the disintegration time of optimizedprescription formulation was 〈 85 s, and the dissolution percent at 10 min was obviously better than that of conventionaltablets （P 〈 0. 05 ）, and the quality of the dispersible tablets was very well by stability test. Conclusion The dispersible tablets of Levoamlodipine Besylate formulationand technology is simple, reasonable, and have a higher dissolution speed than conventional tablets. Its is suitable for industrialization production.