含阿托伐他汀固体分散体的E/R三层基质片的体内外评价

A. Thirupathaiah, R. Sunder
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摘要

研究阿托伐他汀固体分散体缓释片的体内外行为是本研究的重点。采用直接压缩法制备阿托伐他汀三层基质片,中间活性层由不同等级羟丙基甲基纤维素(HPMC)、乙基纤维素和卡波波尔934P组成。屏障层由疏水聚合物巴西棕榈蜡和黄原胶制备。根据评价参数,确定了最佳处方HF16的药物溶出曲线和释放顺序动力学。该给药体系在24 h内具有较长的释药速度。优化后的配方(HF16)的释药曲线为零阶,最符合Higuchi模型。FTIR证实制剂中所用辅料与药物之间无化学相互作用。对优化配方HF16和标准品进行体内生物利用度研究。与参比标准相比,优化后的阿托伐他汀三层基质片血药浓度显著,缓释时间延长,维持24小时,且患者依从性良好,降低给药频率。
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In Vitro - In Vivo Evaluation Of E/R Trilayer Matrix Tablets Containing Solid Dispersion Of Atorvastatin
Investigation of  in vitro/in vivo  behaviour of extended release tablets containing solid dispersions of Atorvastatin is the focus of the present research work. Atorvastatin trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), ethyl cellulose and Carbopol 934P. Barrier layers are prepared with hydrophobic polymers carnauba wax and xanthan gum. Based on the evaluation parameters, drug dissolution profile and release order kinetics HF16 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF16) was described by the Zero-order and best fitted to Higuchi model. FTIR confirmed that there was no chemical interaction between drug and excipients used in the formulation. . In vivo bioavailability studies were conducted for optimized formulation HF16 and reference standard. The optimized formulation of Atorvastatin trilayer matrix tablet was shown significant plasma concentration with extended release and maintained for 24 hrs with patient compliance by reducing the dosage frequency, when compared with reference standard.
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