Sengel Ceyda T, Hasçiçek Canan, Gönül Nurşin
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ankara, Tandogan, Ankara, Turkey.
J Microencapsul. 2006 Mar;23(2):135-52. doi: 10.1080/02652040500286474.
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, Cellactose80, Flow-Lac100 and excipients Compritol888 ATO, KollidonSR. 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 180 mg diltiazem hydrochloride and using either Compritol888 ATO or KollidonSR were designed successfully and maintained drug release for 24 h with zero order and Higuchi kinetics, respectively.
在本研究中，尝试开发含盐酸地尔硫䓬微球的缓释片剂制剂，使其每日服用一次而非每日两到三次。为此，采用乳液 - 溶剂蒸发技术制备了乙基纤维素微球。评估了乳化剂类型和药物/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、Cellactose80、Flow - Lac100）和辅料（Compritol888 ATO、KollidonSR）进行压片。从物理和体外药物释放特性的角度对片剂进行了评估。结果表明，辅料的类型和比例在微球压片中起着重要作用。最终，成功设计了两种分别含有180 mg盐酸地尔硫䓬且使用Compritol888 ATO或KollidonSR的片剂制剂，它们分别以零级动力学和Higuchi动力学维持药物释放24小时。
