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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 physico-chemical constants of equilibrium solubility, oil-water partition coefficient and other factors of gastrodin, the effects of solvent, temperature and pH on the stability of aqueous solution were investigated. Methods: The equilibrium solubility of gastrodin in different media and the apparent oil-water partition coefficient (Papp) under different pH conditions were determined by HPLC. The stability and stability of gastrodin with different solvents, temperature and pH were investigated by RSD of drug content within 12h influences. Results: The equilibrium solubility of gastrodin in methanol, ethanol, isopropanol, acetone and ethyl acetate was 1.29 × 10-1, 3.20 × 10-2, 8.89 × 10-3, 4.48 × 10-3, 6.25 × 10 -4 g / mL in 0.9% sodium chloride solution, purified water, methanol-water 1: 1, pH 7.8 phosphate buffered saline PBS pH 7.4 PBS pH 5.8 PBS pH 1.2 Equilibrated solubility in HCl 0.334,0.340,0.311,0.302,0.311,0.324,0.328,0.351 g / mL; in water, 0.9% sodium chloride solution, pH 1.2 HCl, pH 3.0 PBS, pH 4.0 PBS, pH 5.0 Papp of PBS, pH 5.8 PBS and pH 7.0 PBS were 0.704,0.269,0.253,0.180,0.485,0.595,0.617,0.757, respectively. Gastrodin was diluted in methanol, ethanol, 0.9% sodium chloride solution, purified water (37 ℃, The RSD of drug content within 12 h in pH 5.8 PBS, pH 7.0 PBS, pH 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: The Papp of gastrodin increased with the increase of pH. The equilibrium solubility of the gastrodin decreased with the increase of pH. The equilibrium solubility in organic solvents increased with the increase of solvent polarity. Sufficient in different solvents, different temperatures and different pH of PBS has good stability.