不同工艺制得非洛地平固体分散体的溶解度比较研究

A comparative study on the solubility of felodipine solid dispersions based on different preparation methods

目的应用不同工艺制备非洛地平/PVP VA64固体分散体,通过溶解度的测定,阐明出非洛地平固体分散体制备的最优制备工艺。方法以共聚维酮(PVP VA64)为聚合物载体,通过4种制备工艺(共沉淀法、微波淬冷法、冷冻干燥法及喷雾干燥法)制备非洛地平/PVP VA64固体分散体。考察其在水及PBS(p H6.8)两种介质中的平衡溶解度。结果原形药物及物理混合物中药物溶解度较低(<0.4 mg/L)。微波-淬冷技术产生的药物溶解度最大(>1.4 mg/L),明显高于其他3种方法。结论微波-淬冷技术显著地改善了非洛地平的溶解度,更适合用于非洛地平固体分散体的制备及产业化应用。

Objective To optimized the preparation technology for felodipine solid dispersions by determining its sol-ubility.Methods Solid dispersions were prepared based on polymer carrier of copovidone （ PVP VA64） using four preparation methods （ coprecipitation method , microwave-quenching cooling method , freeze drying method and spray drying method ） .Equilibrium solubility was measured in the water and PBS （ pH 6 .8 ） .Results Pure drug and physical mixtures caused the relatively low solubility （〈0.4 mg/L）.Microwave-quench cooling technology resulted in the highest solubility （〉1.4 mg/L）,which was superior to other three methods .Conclusion Microwave-quench cooling technology improved the solubility of felodipine obviously ,and is more suitable for preparing felodipine solid dispersions in industrialized application .