Edmonds L C, Davidson L, Bertino J S
Department of Medicine, Mary Imogene Bassett Hospital, Cooperstown, New York 13326.
Ther Drug Monit. 1989;11(3):323-6. doi: 10.1097/00007691-198905000-00015.
The solubility and stability of amphotericin B in human serum in vitro was assessed using a sensitive high performance liquid chromatographic technique. The solubility of amphotericin B at concentrations ranging from 0.5 micrograms/ml to 10 micrograms/ml in human serum at pH 7.4, at 37 degrees C, and in 5% CO2 (simulated in vivo conditions) showed no significant difference compared with the solubility at 23 degrees C in room air after a 1 h incubation period. Dissolution of the colloidal suspension at a concentration of 2 micrograms/ml reached 81% in 3 min with a small increase in solubility by 60 min. Amphotericin B was very stable (less than 5% loss) in human serum at -20 degrees C for up to 14 days with only a 10% loss of drug at 6 months. In dimethylsulfoxide, however, losses at 6 months were greater than 60%. We conclude that amphotericin B solubilizes, but not completely, from a colloidal form in human serum under simulated in vivo conditions at 37 degrees C and at 23 degrees C in room air over 1 hour. Additionally, amphotericin B is stable in frozen serum for 6 months.
采用灵敏的高效液相色谱技术评估了两性霉素B在人血清中的体外溶解度和稳定性。在pH 7.4、37℃及5%二氧化碳（模拟体内条件）下，两性霉素B在人血清中浓度为0.5微克/毫升至10微克/毫升时的溶解度，与在室温空气中23℃孵育1小时后的溶解度相比，无显著差异。浓度为2微克/毫升的胶体悬浮液在3分钟内的溶解率达到81%，60分钟时溶解度略有增加。两性霉素B在-20℃的人血清中非常稳定（损失小于5%），长达14天，6个月时药物损失仅为10%。然而，在二甲基亚砜中，6个月时的损失大于60%。我们得出结论，在模拟体内条件下，37℃时以及室温空气中23℃孵育1小时后，两性霉素B可从人血清中的胶体形式溶解，但不完全溶解。此外，两性霉素B在冷冻血清中6个月内稳定。
