安石榴苷平衡溶解度与油水分配系数的测定
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摘要
目的考察安石榴苷在不同pH值磷酸盐缓冲液中的平衡溶解度(S)和油水分配系数(PO/W),为其制剂开发提供参考。方法采用摇瓶-紫外分光光度法测定安石榴苷在不同温度(25℃、37℃)、pH为1.2、2.5、5.0、5.8、6.8、7.4、7.8~8.0的磷酸盐缓冲液中的S值和在正辛醇-缓冲液中的PO/W值。结果在pH为1.2~8.0条件下,安石榴苷在25℃时的S值和lgPO/W分别为775.00~2 789.00mg/mL和-3.07~-3.85,在37℃时的S值和lgPO/W分别为1 006.00~2 684.00mg/mL和-1.32~-3.81;在pH 1.2~8.0范围,均有lgPO/W<0,pH为1.2时,安石榴苷的S值较低。结论安石榴苷水溶性较好,亲脂性差,在胃内的溶解性不好,表明透膜性差是影响胃肠道吸收的限速因素。
Objective To determine the equilibrium solubility(S)and the apparent oil/water partition coefficient(PO/W)of punicalagin in different pH phosphate buffer solution,so as to provide the basis for the exploitation of preparations.Methods The S values and the PO/Wvalues of punicalagin in pH1.2,2.5,5.0,5.8,6.8,7.4,7.8-8.0 of phosphate buffer solutions at 25℃ or 37℃ were measured by shaking flask-UV spectrophotometry.Results In pH 1.2-8.0 phosphate buffer solutions,the Svalues of punicalagin were775.00~2 789.00 mg/mL and the PO/Wvalues were-3.07~-3.85 at 25℃,and the Svalues of punicalagin was 1 006.00~2 684.00 mg/mL and the PO/Wvalues were-1.32~-3.81 at 37℃.The lgPO/W values were<0 at the pH range from 1.2 to 8.0.The Svalue of punicalagin in pH1.2 is markedly lower than the others.Conclusion Punicalagin has good watersolubility,but its solubility is bad in stomach.Punicalagin has poor liposolubility.It may be poor absorption in the gastrointestinal tract for the poor membrane permeability.
Objective To determine the equilibrium solubility(S)and the apparent oil/water partition coefficient(PO/W)of punicalagin in different pH phosphate buffer solution,so as to provide the basis for the exploitation of preparations.Methods The S values and the PO/Wvalues of punicalagin in pH1.2,2.5,5.0,5.8,6.8,7.4,7.8-8.0 of phosphate buffer solutions at 25℃ or 37℃ were measured by shaking flask-UV spectrophotometry.Results In pH 1.2-8.0 phosphate buffer solutions,the Svalues of punicalagin were775.00~2 789.00 mg/mL and the PO/Wvalues were-3.07~-3.85 at 25℃,and the Svalues of punicalagin was 1 006.00~2 684.00 mg/mL and the PO/Wvalues were-1.32~-3.81 at 37℃.The lgPO/W values were<0 at the pH range from 1.2 to 8.0.The Svalue of punicalagin in pH1.2 is markedly lower than the others.Conclusion Punicalagin has good watersolubility,but its solubility is bad in stomach.Punicalagin has poor liposolubility.It may be poor absorption in the gastrointestinal tract for the poor membrane permeability.
引文
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[2]JIMENEZ DRM,RAMAZANOV A,SIKORSKI S,et al.A new method of standartization of health-promoting pomegranate fruit(Pu-nicagranatum)extract[J].J Georgian Med News,2006,140:70-77.
[3]张杰,崔艳娜,刘绣华,等.安石榴苷的研究进展[J].化学研究,2014,25(6):551-562.
[4]SU D S,WANG S L.Physical Pharmacy[M].Beijing:Chemical Industry Press,2004:98-117.
[5]孙进.口服药物吸收与转运[M].人民卫生出版社,北京,2006,352-395.
[6]施洋,孙芸,谢莉,等.石榴皮中活性成分鞣花酸的平衡溶解度和油水分配系数的测定[J].新疆医科大学学报,2016,39(2):145-148.
[7]熊璐琪,李国锋,苏碧雅,等.醋酸地塞米松和地塞米松磷酸钠的油水分配系数与其经皮渗透行为之间的相关性研究[J].中国药学杂志,2011,46(6):439-446.
[8]国家药典委员会.中华人民共和国药典(四部)[S].北京:中国医药科技出版社,2015:325-326.
[9]陆慧,贾晓斌,韦英杰,等.灵芝三萜表观油水分配系数的测定及其在体肠吸收[J].中国实验方剂学杂志,2011,21(17):12-16.
[10]ABRAHAM D.Burger′s medicinal chemistry and drug discovery[M].USA:Wiley Online Library,2003:249-293