固体分散技术提高雷米普利片的溶出度

A. M. Hay, S. Adawy
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摘要

雷米普利是一种ACE抑制剂,主要用于治疗轻至重度高血压和心肌梗死。雷米普利的溶解度和润湿性差,导致溶解性差,因此显示出生物利用度的变化。本研究旨在利用固体分散体(SD)技术改善药物的理化性质。以聚乙烯吡咯烷酮(PVP K25、PVP K30和PVP K90)、聚乙二醇(PEG 4000和PEG 6000)为载体,以三种药物载体比(1:1)、(1:2)和(1:3)制备雷米普利固体分散体[SDs]。采用熔炼法和揉捏法等不同的方法。采用x射线衍射、傅里叶变换红外光谱和体外溶出度研究对配方进行了表征。与纯雷米普利缓慢的溶出速度相比,药物在PEG4000或peg6000中的分散大大提高了药物的溶出速度。此外;雷米普利10mg速释片按1:1(药物:载体)的比例用融合法制备,溶出度可接受;雷米普利peg4000和雷米普利peg6000分别为91%和97%。
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Enhancement of Dissolution Rate of Ramipril Tablets by Solid Dispersion Technique
Ramipril is an ACE inhibitor mainly used for management of mild to severe hypertension and myocardial infarction. The poor solubility and wettability of Ramipril leads to poor dissolution and hence showing variations in bioavailability.The present study is aimed to improve the physicochemical properties of the drug using solid dispersion [SD] techniques. Solid dispersions [SDs] of ramipril were prepared with different polymers or carriers such as polyvinylpyrrolidone (PVP K25, PVP K30 and PVP K90), polyethylene glycol (PEG 4000 and PEG 6000) at three drug : carrier ratios (1:1), (1:2) and (1:3). Different methods such as melting and kneading methods were used. The formulations were characterized by X-Ray Diffractometry studies, Fourier transform infrared spectroscopy and in vitro dissolution rate studies. In contrast to the slow dissolution rate of pure Ramipril, the dispersion of the drug in the PEG4000 or 6000 considerably enhanced the dissolution rate. Furthermore; Ramipril 10 mg immediate release tablets prepared in a ratio of 1:1 (drug: carrier) by the fusion method has been resulted in an acceptable dissolution results; 91% and 97% for ramiprilPEG4000 and ramipril-PEG6000 respectively.
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