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目的:研究阿苯达唑(ABZ)固体分散体体外溶出以及体内药动学规律。方法:固体分散体的制备采用溶剂法;采用3种方程对溶出度数据进行拟合,并比较固体分散体及3个参比样品溶出度情况;采用HPLC法测定大鼠血浆药物浓度,考察ABZ固体分散体在大鼠体内药动学规律。结果:在20min时固体分散体、市售片剂、简单混合物及原料药的溶出度分别达到:92.8%,76.5%,40.8%和2.9%,溶出规律均符合Weibull模型。大鼠体内药动学研究结果表明:固体分散体与市售片剂相比Cmax和AUC均有很大提高;采用隔室模型和统计矩2种模型进行计算固体分散体相对生物利用度,均能达到230%。结论:固体分散体可以显著提高阿苯达唑(ABZ)体外溶出及体内吸收。
Objective: To study the in vitro dissolution of albendazole (ABZ) solid dispersion and its pharmacokinetics in vivo. Methods: The solid dispersion was prepared by the solvent method. The three kinds of equations were used to fit the dissolution data. The dissolution of the solid dispersion and the three reference samples were compared. The plasma concentration of the drug was measured by HPLC. Pharmacokinetics of solid dispersions in rats. Results: The dissolution rates of solid dispersions, commercial tablets, simple mixtures and APIs reached 92.8%, 76.5%, 40.8% and 2.9% respectively at 20min. The dissolution laws were in line with the Weibull model. Pharmacokinetic studies in rats showed that both the Cmax and AUC of solid dispersions were greatly improved compared with those of commercial tablets. The relative bioavailability of solid dispersions was calculated using two compartments model and statistical moment model Can reach 230%. Conclusion: Solid dispersions can significantly improve the dissolution and absorption of albendazole (ABZ) in vitro.