Tsuda Y, Yamanouchi K, Okamoto H, Yokoyama K, Heldebrant C
Green Cross Corporation, Osaka, Japan.
J Pharmacobiodyn. 1990 Mar;13(3):165-71. doi: 10.1248/bpb1978.13.165.
The purpose of this study was to clarify the reason why two similar perfluorochemical (PFC) emulsions, namely a mixed PFC (perfluorodecalin: FDC and perfluorotripropylamine: FTPA) and an FDC emulsion, resulted in a very different survival time for the exchange-transfused rats. Supposing that some difference in the intravascular behavior of both emulsions would account for such a difference in efficacy, experiments on behavior of PFC emulsions were carried out focusing on the particle size. It was reconfirmed that larger PFC particles were eliminated from the blood stream much more rapidly than smaller particles with three FMIQ (perfluoro-N-methyldecahydroisoquinoline) emulsions. After the FDC + FTPA emulsion or the FDC emulsion were injected into rabbits, PFC particles in the blood tended to decrease in size. When each of the collected blood samples was incubated at 37 degrees C for 24 h, the FDC emulsion enlarged in size markedly, but the FDC + FTPA emulsion showed no change. The retention of PFC particles appeared to depend on the emulsion stability rather than simply on the emulsifying agent alone. These data showed that some differences were observed in intravascular persistence of the FDC + FTPA emulsion and the FDC emulsion, and suggested that the efficacy of PFC emulsions would reflect their behavior in the circulation.
本研究的目的是阐明两种相似的全氟化合物(PFC)乳剂,即混合PFC(全氟萘烷:FDC和全氟三丙胺:FTPA)和FDC乳剂,为何会使换血大鼠的存活时间有很大差异。假设两种乳剂在血管内行为上的某些差异可解释这种疗效差异,于是围绕粒径开展了PFC乳剂行为的实验。通过三种FMIQ(全氟-N-甲基十氢异喹啉)乳剂再次证实,较大的PFC颗粒比小颗粒从血流中清除得更快。将FDC + FTPA乳剂或FDC乳剂注入兔子体内后,血液中的PFC颗粒尺寸往往会减小。当将采集的每份血样在37℃孵育24小时时,FDC乳剂尺寸明显增大,但FDC + FTPA乳剂无变化。PFC颗粒的留存似乎取决于乳剂稳定性,而非仅仅取决于乳化剂。这些数据表明,FDC + FTPA乳剂和FDC乳剂在血管内的持久性存在一些差异,并表明PFC乳剂的疗效将反映其在循环中的行为。