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Development and in-vitro evaluation of modified release tablets including ethylcellulose microspheres loaded with diltiazem hydrochloride

机译:载有盐酸地尔硫卓的乙基纤维素微球等缓释片的研制和体外评价

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摘要

In this study,development of modified release tablet formulations containing diltiazem hydrochloride-loaded microspheres to be taken once rather than two or three times a day was attempted.For this purpose,ethylcellulose microspheres were prepared by emulsion-solvent evaporation technique.The influence of emulsifier type and drug/polymer ratio on production yield,encapsulation efficiency,particle size,surface morphology and in-vitro release characteristics of the microspheres was evaluated.Suitable microspheres were selected and tabletted using different tabletting agents,Ludipress~R,Cellactose~R 80,Flow-Lac~R 100 and excipients Compritol~R 888 ATO,Kollidon~R SR.Tablets were evaluated from the perspective of physical and in-vitro drug release characteristics.It was seen that type and ratio of the excipients played an important role in the tabletting of the microspheres.As a result,two tablet formulations containing 180mg diltiazem hydrochloride and using either Compritol~R 888 ATO or Kollidon~R SR were designed successfully and maintained drug release for 24 h with zero order and Higuchi kinetics,respectively.
机译:在这项研究中,尝试开发含有盐酸地尔硫卓的微球的控释片剂,而不是每天服用两到三次,而是每天服用一次。为此目的,通过乳液-溶剂蒸发技术制备了乙基纤维素微球。评估了微球的类型和药物/聚合物比例对微球的产率,包封效率,粒径,表面形态和体外释放特性的影响。选择合适的微球并使用不同的压片剂(Ludipress〜R,Cellactose〜R 80, Flow-Lac〜R 100和辅料Compritol〜R 888 ATO,Kollidon〜R SR。从物理和体外药物释放特性的角度评估了片剂,发现辅料的类型和比例在其中起着重要的作用。结果,两种含180mg盐酸地尔硫卓的片剂均使用Compritol〜R 888 ATO或K成功设计了ollidon〜R SR,并分别以零级和Higuchi动力学将药物释放保持24小时。

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