Yamashita N
Second Department of Surgery, Nagasaki University School of Medicine, Japan.
Nihon Shokakibyo Gakkai Zasshi. 1990 May;87(5):1183-90.
Recently, methyl tertiary butyl ether (MTBE) has been evaluated as a new cholesterol gallstone dissolving agent. The dissolution rate of cholesterol monohydrate (ChM) by MTBE was measured and effective types of MTBE administration in vivo were studied. When the dissolution rate of ChM by MTBE was compared with that of d-limonene and monooctanoin used clinically at present, MTBE was found to be the most excellent dissolving agent. However, the dissolving effect of MTBE can be suppressed by water (a component of wet gallstones and 97% of bile) because MTBE is insoluble in water. Therefore, MTBE mixed with a small amount of surfactants (MTBEP) was prepared. The dissolving effect of MTBE alone and MTBEP on dry and wet gallstones were measured. The dissolving effect of MTBE alone on the wet stones was markedly decreased, while MTBEP suppressed the decrease of dissolving effect on wet stones significantly. Furthermore, the dissolving effect of MTBE alone and MTBEP on gallstones in water were measured. MTBEP significantly improved the decrease of dissolving effect on stones by MTBE alone, because the addition of a small amount of a surfactant suppressed the influence of water for dissolving effect of MTBE. MTBE emulsion, newly type of solvent, was prepared. Although the dissolution rate of ChM in MTBE emulsion was low, the dissolving effect of MTBE emulsion was also better than that of MTBE in animal experiments. In this study, emulsion type can be expected to become excellent dissolving agents, because emulsion type suppressed the influence of water for dissolving effect of solvent.
最近,甲基叔丁基醚(MTBE)已被评估为一种新型的胆固醇胆结石溶解剂。测定了MTBE对一水合胆固醇(ChM)的溶解速率,并研究了MTBE在体内的有效给药方式。当将MTBE对ChM的溶解速率与目前临床上使用的d-苎烯和单辛酸甘油酯的溶解速率进行比较时,发现MTBE是最优异的溶解剂。然而,由于MTBE不溶于水,其溶解效果会受到水(湿胆结石的一种成分以及97%胆汁的成分)的抑制。因此,制备了与少量表面活性剂混合的MTBE(MTBEP)。测定了MTBE单独以及MTBEP对干、湿胆结石的溶解效果。MTBE单独对湿结石的溶解效果显著降低,而MTBEP显著抑制了对湿结石溶解效果的降低。此外,还测定了MTBE单独以及MTBEP对水中胆结石的溶解效果。MTBEP显著改善了MTBE单独对结石溶解效果的降低,因为添加少量表面活性剂抑制了水对MTBE溶解效果的影响。制备了新型溶剂MTBE乳剂。尽管ChM在MTBE乳剂中的溶解速率较低,但在动物实验中MTBE乳剂的溶解效果也优于MTBE。在本研究中,乳剂类型有望成为优异的溶解剂,因为乳剂类型抑制了水对溶剂溶解效果的影响。