水飞蓟素增溶方法的比较研究

PREPARATION AND IN VITRO EVALUATION OF SILYMARIN SOLID DISPERTIONS AND COMPLEXATION

目的：优选增加水飞蓟素溶解度和溶出速度的最佳方法和条件。方法：以聚乙烯吡咯烷酮（ＰＶＰ），聚乙二醇６０００（ＰＥＧ－６０００），ＰＥＧ－６０００与Ｔｗｅｅｎ－８０混合载体，制备固体分散体；以β－ＣＤ，ＨＰ－β－ＣＤ制包合物，测定溶解度及体外溶出速度。结果：水中溶解度ＰＶＰ固体分散体大于包合物，载体比例越大，药物溶出愈快；比例相同时，ＰＶＰ固体分散体溶出最快。结论：ＰＶＰ Ｋ３０作为水飞蓟素固体分散体的载体，载药量大。增溶效果显著。

OBJECTIVE: To improve the dissolution of Sily- marin(SL).METHODS: Silymarin solid dispertions were pre- pared using solvent-melting and coevaporation methods with PEG 6000, PEG-Tween (3:1), PVP as driers. Silymarin com- plexation was also prepared with β－CD, HP-β－CD. Solubility and in vitro dissolution characteristics were studied. RESULTS: Dissolution results in vitro showed that higher drier-SL ratio led to faster drug dissolution. PVP was superior to PEG 6000, PEG-Tween, β－CD, HP-β-CD in its ability to accelerate the dis- solution of SL. CONCLUSION: PVP was potent in improving the solubility and dissolution of SL and had the potentiatial for practical utilligation.