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目的:考察室温下不同pH介质中鬼臼毒素的油水分配系数以及羟丙基-β-环糊精对鬼臼毒素的增溶作用。方法:采用摇瓶法测定鬼臼毒素在不同pH介质中的溶解度和油水分配系数;采用正交设计试验优选羟丙基-β-环糊精包合鬼臼毒素的最佳工艺;以相溶解度法考察羟丙基-β-环糊精对鬼臼毒素的增溶作用。结果:鬼臼毒素在水中溶解度为0.09 g.L-1,在正辛醇中的溶解度为12.91 g.L-1。在水和正辛醇两相中5 min即可达到分配平衡,油水分配系数P=179.067,疏水常数logP=2.249。相溶解度图属于AL型,包合常数为1 022.65 L.mol-1。结论:鬼臼毒素亲脂性较强,在油水两相分配平衡快;羟丙基-β-环糊精对鬼臼毒素具有很好的增溶作用,且可与之形成较稳定的包合物。
Objective: To investigate the oil-water partition coefficient of podophyllotoxin and the solubilization of podophyllotoxin by hydroxypropyl-β-cyclodextrin in different pH media at room temperature. Methods: The solubility and oil-water partition coefficients of podophyllotoxin in different pH media were determined by shake-flask method. The orthogonal design was applied to optimize the inclusion of podophyllotoxin by hydroxypropyl-β-cyclodextrin. Law investigated hydroxypropyl-β-cyclodextrin solubilization of podophyllotoxin. Results: Podophyllotoxin had a solubility of 0.09 g.L-1 in water and 12.91 g.L-1 in n-octanol. In water and n-octanol two phase in 5min to achieve the distribution equilibrium, oil and water partition coefficient P = 179.067, hydrophobic constant logP = 2.249. Phase solubility diagram belongs to the AL type, inclusion constant is 1 022.65 L.mol-1. CONCLUSION: Podophyllotoxin is relatively lipophilic and has a fast equilibrium between oil and water phases. Hydroxypropyl-β-cyclodextrin has a good solubilizing effect on podophyllotoxin and can form a more stable inclusion complex .