Hanson L H, Stevens D A
Department of Medicine, Santa Clara Valley Medical Center, San Jose, California.
Antimicrob Agents Chemother. 1992 Feb;36(2):486-8. doi: 10.1128/AAC.36.2.486.
Complexing amphotericin B (AmB) with lipids or entrapping it in liposomes may increase its efficacy by reducing toxicity and affecting distribution. However, depending on the lipids involved, interference with antifungal activity has been shown. We compared the in vitro activity of AmB colloidal dispersion by cholesteryl sulfate (ABCD) to the standard AmB deoxycholate suspension (ABDS) against 41 isolates of 15 pathogenic species. Broth dilution MIC and minimum fungicidal concentration (MFC) ranges were similar, and the same number of isolates had lower MICs and MFCs with one drug as with the other. Differences between species were noted. In less than a third of comparisons, there were large (fourfold or more) decreases in ABCD activity relative to that of ABDS, and in approximately 1/10, there were large increases. Thus, ABCD complexing variably affects AmB activity. As ABCD pharmacokinetics and toxicology differ from those of ABDS, the significance of these results for in vivo activity needs to be determined.
将两性霉素B(AmB)与脂质复合或包裹于脂质体中,可能会通过降低毒性和影响分布来提高其疗效。然而,根据所涉及的脂质不同,已显示出其对抗真菌活性存在干扰。我们比较了硫酸胆固醇两性霉素B胶体分散液(ABCD)与标准两性霉素B脱氧胆酸盐混悬液(ABDS)对15种致病菌种的41株分离株的体外活性。肉汤稀释法测得的最低抑菌浓度(MIC)和最低杀菌浓度(MFC)范围相似,且两种药物对相同数量的分离株具有相同的较低MIC和MFC。不同菌种之间存在差异。在不到三分之一的比较中,相对于ABDS,ABCD的活性大幅降低(四倍或更多),而在约十分之一的比较中,活性大幅增加。因此,ABCD复合对AmB活性的影响各不相同。由于ABCD的药代动力学和毒理学与ABDS不同,这些结果对体内活性的意义有待确定。