心得安一日一次缓释片的研制及体外评价

 Rashmi Shivaji Tambare, Minal Chaudhari, S. Kakade
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引用次数: 0

摘要

本研究的目的是开发每日一次的普萘洛尔缓释基质片,用于治疗高血压、心绞痛和许多其他心血管疾病。采用约束混合实验设计制备了由Eudragit RSPO和不同粘度等级的HPMC (Methocel E50和Methocel K15M CR)组成的系统模型配方。采用直接压缩法制备基质片。对所制片剂进行了理化参数评价。通过24h的体外释放检查,评价普萘洛尔SR基质片的质量。增加乌龙茶RSPO和HPMC浓度或增加HPMC聚合物(Methocel E50和Methocel K15M CR)的粘度等级导致心得安释放显著减少。缓释剂量的心得安通过维持药物的血浆浓度远高于治疗浓度来达到更理想的降压效果。体外溶出度分析表明,F4批次由espo (80 mg)、E50 (60 mg)和K15M CR (80 mg)混合制备,释药率为98.11%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and in Vitro Evaluation: Once-Daily Sustained Release Matrix Tablets of Propranolol
The objective of the present study was to develop once-daily sustained-release matrix tablets of propranolol used in the treatment of hypertension, angina pectoris, and many other cardiovascular disorders. The constrained mixture experimental design was used to prepare systematic model formulations, which were composed of Eudragit RSPO and different viscosity grades of HPMC (Methocel E50 and Methocel K15M CR). The matrix tablets were prepared by direct compression process. The prepared tablets were evaluated for various physico-chemical parameters. In vitro release profile was check for 24 hrs to evaluate the SR matrix tablet of propranolol. Increase in Eudragit RSPO and HPMC concentrations or increase in viscosity grades of HPMC polymers (Methocel E50 and Methocel K15M CR) resulted in a significant decrease in propranolol release. Administration of propranolol in a sustained release dosage would be more desirable for antihypertensive effects by maintaining the plasma concentrations of the drug well above the therapeutic concentration. From in vitro dissolution profile, Batch F4 was prepared with blend of Eudragit RSPO (80 mg), Methocel E50 (60 mg) and Methocel K15M CR (80 mg) where drug release was about 98.11%.
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