CAJ | 학술논문

目的:探讨在不同pH值条件下羟基喜树碱的油/水分配系数与大鼠小肠吸收之间的相关性.方法:缓冲溶液水相pH值依次为2.2、4.0、6.0、7.4、9.16及11,正辛醇为油相,采取"摇瓶法"使药物在油相/水相中达到平衡后,用高效液相测定油/水相中药物的浓度,计算药物的油/水分配系数.以酚红为体积校正剂,测定不同 pH值条件下,大鼠小肠吸收系数.将药物油/水分配系数与大鼠小肠吸收系数进行线性回归.结果:药物的油/水分配系数与大鼠小肠吸收系数随分散介质的pH值不同而改变,两者之间的线性关系为:y=0.001 3x+0.009 1,相关系数R~2为0.959 7.结论:羟基喜树碱的油/水分配系数与小肠吸收之间存在良好的线性关系,可以油/水分配系数预测大鼠小肠吸收.
목적:탐토재불동pH치조건하간기희수감적유/수분배계수여대서소장흡수지간적상관성.방법:완충용액수상pH치의차위2.2、4.0、6.0、7.4、9.16급11,정신순위유상,채취"요병법"사약물재유상/수상중체도평형후,용고효액상측정유/수상중약물적농도,계산약물적유/수분배계수.이분홍위체적교정제,측정불동 pH치조건하,대서소장흡수계수.장약물유/수분배계수여대서소장흡수계수진행선성회귀.결과:약물적유/수분배계수여대서소장흡수계수수분산개질적pH치불동이개변,량자지간적선성관계위:y=0.001 3x+0.009 1,상관계수R~2위0.959 7.결론:간기희수감적유/수분배계수여소장흡수지간존재량호적선성관계,가이유/수분배계수예측대서소장흡수.
AIM:To explore the eorrelativity of the oil/water partition of hydroxycamptothecin and its absorption coefficieney in small intestine in rats.METHODS:pH value of water phase in buffer solution in turn took 2.2,4.6,7.4,9.6 and 11,while octanol was adopted as oil phase.After phase equilibrium,HPLC wag used to determine the concentration of hydro-xycamptothecin,and oil/water partition coefficient Was calculated with the phenol red as volume calibration agent,small intestinal absorption coefficients of rats in different pH were plotted against its oil/water partition coefficients.RESULTS:Oil/water partition coefficient(x)of hydroxyeamptotheein and small intestinal absorption(y)altered with the change of pH value of the dispension medium.The linear regress equation was constructed as y=0.001 3x+0.009 1 with its correlation coefficient R~2 being 0.959 7.CONCLUSION:There exists a good linear dependence between oil/water partition coefficient of hydroxycamptothecin and its absorption coefficient in small intestines of rats.Oil/water partition coefficient Can be used to design the new oral preparations.