含苯并咪唑速释片工艺优化及评价

N. Sudarshan Rao, Budda Leena
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奥美沙坦是一种用于治疗高血压的血管紧张素II拮抗剂。本研究尝试研制奥美沙坦固体口服制剂。本研究的目的是通过实验设计,以辅料为辅料,研制奥美沙坦速释片配方。采用直接压缩法制备片剂。HPLC法测定奥美沙坦在296 nm,流速为0.7 ml/min,注射量为5L时的相关系数为0.993。采用USPⅱ型仪器进行硬度、厚度、溶出度校准研究、药物含量测定,体外研究均采用磷酸盐缓冲液,温度为37°C±0.5°C。优化后的制剂体外释放度为96。与其他ARB药物相比,显示出高亲和力的血管紧张素II型1 (AT1)受体,作用时间长。奥美沙坦的最长半衰期为24小时,其中最大半衰期为0.5 - 1小时,并且它可以如此迅速地达到所需的血浆浓度。稳定性研究是根据ICH指南进行的。所有结果均在ICH限定范围内获得。
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Process Optimization and Evaluation of Immediate Release Tablet containing Benzimidazoles
Olmesartan is an angiotensin II antagonist used in the treatment of hypertension. In present investigation an attempt was made to develop solid oral formulation of Olmesartan. The purpose of this study was to develop the formulation as immediate release tablet of Olmesartan by using excipients by design of experiment. Tablets were prepared by using direct compression method. In HPLC study of Olmesartan the correlation coefficient was found to be 0.993 at 296 nm at flow rate of 0.7 ml/min at injection volume of 5 L Tablets were evaluated for hardness, thickness, dissolution calibration study, drug content and all the in-vitro studies were performed using USP apparatus type II All in-vitro studies were carried out using Phosphate buffer at 37°C ± 0.5°C. The optimized formulation showed in- vitro drug release of 96. 80 % at the end of 60 min. Comparing to other ARB’s drug shows high affinity Angiotensin II type 1 (AT1) receptors has long duration of action. Olmesartan has longest half life of 24 hrs where, T max is 0.5 – 1 hr, and it was so rapidly achieving desired plasma concentrations. Stability studies were carried out according to ICH guidelines. All the results were obtained within given ICH limits.
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