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目的:测定葛根芩连片中主要活性成分(葛根素、黄芩苷和盐酸小檗碱)及其在复方多成分环境下,于不同p H磷酸缓冲液中的溶解度及油水分配系数。方法:采用HPLC法测定葛根素、黄芩苷和盐酸小檗碱在不同p H介质中的溶解度,以及在正辛醇-水和正辛醇-缓冲液体系中的油水分配系数。结果:葛根素、黄芩苷和盐酸小檗碱的溶解度与油水分配系数随p H的变化而变化,在复方多成分背景下也会发生改变。在p H为7.4时溶解度最大,葛根素为7.56 mg·m L-1,黄芩苷为17.07 mg·m L-1,盐酸小檗碱为3.57 mg·m L-1;3者油水分配系数P在p H为1.0时较大,葛根素为0.420(lgP=-0.38),黄芩苷为10.783(lgP=1.03),盐酸小檗碱为0.267(lgP=-0.57)。结论:葛根素、黄芩苷和盐酸小檗碱在p H为1.0时脂溶性均较好,推测在胃里吸收较好,在其它p H介质下脂溶性较低,推测脂溶性可能是影响其肠吸收的原因之一。
OBJECTIVE: To determine the solubility and oil-water partition coefficients of the main active components (puerarin, baicalin and berberine) and their solubility in p H phosphate buffer solution in the multi-component environment of Puerarin. Methods: The solubility of puerarin, baicalin and berberine hydrochloride in different p H media and the oil-water partition coefficient in n-octanol-water and n-octanol-buffer system were determined by HPLC. Results: The solubility, oil-water partition coefficients of puerarin, baicalin and berberine changed with p H, and also changed under the multi-component background. The solubility of pG was 7.4, puerarin was 7.56 mg · mL-1, baicalin was 17.07 mg · mL-1 and berberine hydrochloride was 3.57 mg · mL-1. The coefficients of oil-water partition coefficient P PH was 1.0, puerarin was 0.420 (lgP = -0.38), baicalin was 10.783 (lgP = 1.03) and berberine hydrochloride was 0.267 (lgP = -0.57). CONCLUSION: Puerarin, baicalin and berberine have better liposolubility at a p H of 1.0, better assimilation in the stomach and lower lipophilicity in other p H media, suggesting that liposolubility may be affected by puerarin One of the reasons intestinal absorption.