摘要
目的:考察天麻素的平衡溶解度、油水分配系数等理化常数,研究溶剂、温度及pH对其水溶液稳定性的影响。方法:HPLC测定天麻素在不同介质中的平衡溶解度以及不同pH条件下的表观油水分配系数(Papp),以12h内药物含量的RSD为指标考察不同溶剂、温度、及pH对其稳定性的影响。结果:天麻素在甲醇、乙醇、异丙醇、丙酮、乙酸乙酯中的平衡溶解度为1.29×10-1、3.20×10-2、8.89×10-3、4.48×10-3、6.25×10-4 g/mL,在0.9%氯化钠溶液、纯化水、甲醇-水(1:1)、pH 7.8磷酸盐缓冲液(PBS)、pH 7.4 PBS、pH6.8 PBS、pH 5.8 PBS、pH 1.2 HCl中的平衡溶解度为0.334、0.340、0.311、0.302、0.311、0.324、0.328、0.351g/mL;在水、0.9%氯化钠溶液、pH 1.2 HCl、pH 3.0 PBS、pH 4.0 PBS、pH 5.0 PBS、pH 5.8 PBS、pH 7.0 PBS下的Papp分别为0.704、0.269、0.253、0.180、0.485、0.595、0.617、0.757;天麻素在甲醇、乙醇、0.9%氯化钠溶液、纯化水(37℃、40℃、55℃、75℃)、pH 5.8 PBS、pH 7.0 PBS、pH 7.6 PBS中的12h内药物含量的RSD分别为1.86%、0.91%、0.76%、0.78%、0.49%、0.92%、0.70%、0.75%、0.64%、0.39%。结论:天麻素的Papp随着pH增大而增大;在水性介质中的平衡溶解度随着pH增大而减小,在有机溶剂中的平衡溶解度随溶剂极性的增大而增大;天麻素在不同溶剂、不同温度及不同pH的PBS中具有很好的稳定性。
Objective： To investigate the physicochemical constants such as equilibrium solubility and apparent partition coefficients （Papp）, and to study the effects of solvent, temperature and pH value on the stability of gastrodin solution. Methods： The equilibrium solubility of gastrodin in various medium and the Papp of gastrodin under different pH conditions were measured by RP-HPLC, and the effects of solvent, temperature and pH value on the stability of solution were investigated by taking the RSD of drug content in 12h as detection index. Results： The equilibrium solubility of gastrodin in methanol, ethanol, isopropyl, acetone and ethyl acetate were 1.29x10-l, 3.20x10-2, 8.89x10-3, 4.48x10-3, 6.25x10-4g/mL, and in 0.9% sodium chloride solution, purified water, methanol-water （1：1）, pH value 7.8, 7.4, 6.8, 5.8 phosphate buffer solution （PBS） and pH value 1.2 HC1 were 0.334, 0.340, 0.311, 0.302, 0.311, 0.324, 0.328 and 0.35 lg/mL respectively; While in purified water, 0.9% sodium chloride solution, pH value 1.2 HCI and pH value 3.0, 4.0, 5.0, 5.8, 7.0 PBS, the Papp were 0.704, 0.269, 0.253, 0.180, 0.485, 0.595, 0.617, 0.757; The RSD of drug content in 12h in methanol, ethanol, 0.9% sodium chloride solution, purified water （37℃, 40℃, 55℃, 75℃ ） and pH value 5.8, 7.0, 7.6 PBS were 1.86%, 0.91%, 0.76%, 0.78%, 0.49%, 0.92%, 0.70%, 0.75%, 0.64%, 0.39%. Conclusion： Papp of gastrodin increased as pH value increased, and the equilibrium solubility of gastrodin in the aqueous solution decreased with the pH increased, while in organic solvents decreased with the polarity decreased. The stability of gastrodin solution in different solvents, temperatures and pH values PBS is good.
出处
《中华中医药杂志》
CAS
CSCD
北大核心
2014年第3期851-854,共4页
China Journal of Traditional Chinese Medicine and Pharmacy
基金
卫生部科学研究基金--浙江省医药卫生重大科技计划项目(No.WKJ2012-2-035)~~
