Higaki K, Kishimoto I, Komatsu H, Hashida M, Sezaki H
J Pharmacobiodyn. 1986 Jun;9(6):532-9. doi: 10.1248/bpb1978.9.532.
The effect of medium chain glyceride (MGK) emulsion on the intestinal absorption and the biliary excretion of bromthymol blue (BTB) was investigated in rats. Extensive tissue accumulation of BTB was reduced when BTB was administered with MGK emulsion formulation. HCO-100, an emulsifier, was also important for the decrease in the tissue accumulation of BTB. The ratios of absorption percent to tissue accumulation percent and to free fraction, not contained in the droplet of emulsion, in MGK emulsion were much greater than that of the control. Pretreatment with BTB-free emulsion reduced BTB absorption under the control, although tissue accumulation was not affected. The absorption appeared to decrease with increase in the time of pretreatment. The effect of leaving treatment after pretreatment on the absorption of BTB was also investigated. With the increase in leaving time after pretreatment, reduced absorption tended to resume to the level of control. The change in monocaprylate content from 54 to 60% in MGK made a difference in BTB absorption and it was suggested that monocaprylate content in MGK was one of the significant factors of MGK emulsion on drug absorption. Bile recovery study was simultaneously carried out with an in situ recirculation experiment. The recovery of BTB into bile tended to decrease. The ratio of recovery percent of BTB into bile to the absorption percent of BTB also decreased extensively, which is possibly another effect of MGK on drug disposition.
在大鼠中研究了中链甘油酯（MGK）乳剂对溴麝香草酚蓝（BTB）肠道吸收及胆汁排泄的影响。当BTB与MGK乳剂制剂一起给药时，BTB在组织中的大量蓄积减少。乳化剂HCO - 100对BTB组织蓄积的减少也很重要。MGK乳剂中吸收百分比与组织蓄积百分比以及与乳剂液滴中不含的游离部分的比率远大于对照组。用不含BTB的乳剂预处理会降低对照组下的BTB吸收，尽管组织蓄积不受影响。吸收似乎随着预处理时间的增加而降低。还研究了预处理后停止处理对BTB吸收的影响。随着预处理后停止时间的增加，降低的吸收倾向于恢复到对照水平。MGK中辛酸单酯含量从54% 变为60% 对BTB吸收产生了影响，提示MGK中辛酸单酯含量是MGK乳剂影响药物吸收的重要因素之一。同时通过原位再循环实验进行胆汁回收研究。BTB进入胆汁的回收率趋于降低。BTB进入胆汁的回收率与BTB吸收百分比的比率也大幅降低，这可能是MGK对药物处置的另一个影响。
