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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >AmBisome (liposomal amphotericin B): a comparative review (see comments) (published erratum appears in J Clin Pharmacol 1999 Apr;39(4):428)
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AmBisome (liposomal amphotericin B): a comparative review (see comments) (published erratum appears in J Clin Pharmacol 1999 Apr;39(4):428)

机译：AmBisome（脂质体两性霉素B）：一项比较性评论（请参阅评论）（发表的勘误出现在J Clin Pharmacol 1999 Apr; 39（4）：428）

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摘要

AmBisome (NeXstarPharmaceuticals, San Dimas, CA) is a unilamellar liposomal formulation of amphotericin B that was recently approved for use as empirical treatment for presumed fungal infections in febrile neutropenic patients and for aspergillosis, candidiasis, and cryptococcosis infections refractory to amphotericin B. It is a small closed microscopic sphere (<100 nm in diameter) with an inner aqueous core (i.e., a true liposome). AmBisome remains as an intact sphere in vitro and for prolonged periods of time in vivo during the processes of systemic transport and pharmacologic action. As a consequence of its size and in vivo stability, AmBisome has physiochemical properties and a pharmacokinetic profile that are considerably different from those of currently available lipid-complexed amphotericin B formulations, with greatly increased area under the plasma concentration-time curve and much lower clearance at equivalent doses. AmBisome liposomes can be seen to accumulate at sites of fungal infection. Disruption of AmBisome liposomes occurs after attachment to the fungal cell wall and results in amphotericin B binding to fungal cell membrane ergosterol with subsequent cell lysis. AmBisome has been shown to penetrate the cell wall of both extracellular and intracellular forms of susceptible fungi.
机译：AmBisome（NeXstarPharmaceuticals，San Dimas，CA）是两性霉素B的单层脂质体制剂，最近被批准用作高热中性粒细胞减少症患者的真菌感染以及对两性霉素B难治的曲霉病，念珠菌病和隐球菌感染的经验治疗。具有内部水核心（即真正的脂质体）的小型封闭的微观球体（直径小于100 nm）。在系统转运和药理作用过程中，AmBisome在体外和在体内的完整时间都保持完整。由于其大小和体内稳定性，AmBisome的理化特性和药代动力学特征与目前可得的脂质复合两性霉素B制剂大不相同，血浆浓度-时间曲线下的面积大大增加，并且清除率低得多剂量相等。可以看到AmBisome脂质体积聚在真菌感染部位。 AmBisome脂质体的破坏在附着到真菌细胞壁后发生，并导致两性霉素B与真菌细胞膜麦角固醇结合，随后发生细胞裂解。已显示AmBisome可以穿透易感真菌的细胞外和细胞内形式的细胞壁。

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