Forster D, Washington C, Davis S S
Department of Pharmacy, University of Nottingham, UK.
J Pharm Pharmacol. 1988 May;40(5):325-8. doi: 10.1111/j.2042-7158.1988.tb05260.x.
The toxicity of a number of solubilized or colloidal amphotericin B formulations to human erythrocytes has been studied in-vitro. All the solubilized formulations studied, using poloxamer F127 or L92, or sodium deoxycholate as solubilizing agents, showed similar toxicity, erythrocyte lysis being greater than 90% for amphotericin B concentrations between 4 to 8 micrograms mL-1. Emulsion formulations stabilized by poloxamers showed reduced toxicity, while those stabilized by egg lecithin showed less than 5% erythrocyte lysis up to an amphotericin B concentration of 200 micrograms mL-1. The mechanisms of the differential toxicity is considered to be due to the differences in the equilibrium concentration of free amphotericin B in the aqueous phase.
已在体外研究了多种增溶或胶体两性霉素B制剂对人红细胞的毒性。所有使用泊洛沙姆F127或L92或脱氧胆酸钠作为增溶剂的增溶制剂均表现出相似的毒性，当两性霉素B浓度在4至8微克/毫升之间时，红细胞裂解率大于90%。由泊洛沙姆稳定的乳剂制剂毒性降低，而由卵磷脂稳定的制剂在两性霉素B浓度高达200微克/毫升时红细胞裂解率小于5%。毒性差异的机制被认为是由于水相中游离两性霉素B的平衡浓度不同。
