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目的测定雷公藤甲素及其氨基糖结合物的表观溶解度、表观油水分配系数和解离常数(pK_a~T)。方法采用平衡溶解度法、摇瓶法测定雷公藤甲素及其氨基糖结合物的表观溶解度和油水分配系数;采用分光光度指示剂法测定雷公藤甲素-氨基糖结合物的解离常数。结果雷公藤甲素的表观溶解度随p H的增加而增加,其表观油水分配系数随p H的增加而降低,但变化并不显著。雷公藤甲素-氨基葡萄糖结合物的表观油水分布系数随p H的增加而增加,在纯水中的表观溶解度为1.9325±0.1373 g,pK_a~T=5.938±0.191。结论雷公藤甲素是一个难溶性的亲脂性化合物,而雷公藤甲素-氨基葡萄糖结合物是一个弱碱性的亲水性化合物。
Objective To determine the apparent solubility, apparent oil water partition coefficient and dissociation constant (pK_a ~ T) of triptolide and its amino sugar conjugate. Methods The apparent solubility and oil-water partition coefficient of triptolide and its amino-sugar conjugate were determined by equilibrium solubility method and shake flask method. The dissociation constants of triptolide-aminosugar conjugate were determined by spectrophotometric method. Results The apparent solubility of triptolide increased with the increase of p H, and its apparent oil-water partition coefficient decreased with the increase of p H, but the change was insignificant. The apparent oil-water distribution coefficient of triptolide-glucosamine conjugate increased with the increase of p H, the apparent solubility in pure water was 1.9325 ± 0.1373 g, pK_a ~ T = 5.938 ± 0.191. Conclusion Triptolide is a poorly soluble lipophilic compound, and triptolide-glucosamine conjugate is a weakly basic hydrophilic compound.