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用微生物测定法对阿米卡星脂质体在小鼠体内各组织中的药物浓度进行测定,研究了给药后组织浓度及分布情况,并将其与游离阿米卡星作比较。结果表明:小鼠单剂量静脉注射52mg/kg游离的或脂质体硫酸阿米卡星后,测定0.5、1、3、7、12、24h各组织中药物浓度,以肾脏浓度为最高。与游离药物相比,阿米卡星脂质体明显提高了心(6.2倍)、肝(9.5倍)、脾(284倍)、肺(3倍)、脑(14.7倍)、血清(3倍)中的药物分布,降低了肾脏的分布(1/2)。阿米卡星脂质体不仅改变了该游离药物的体内组织分布,而且延长了半衰期,血药浓度可维持24h(游离药物仅7h)。说明阿米卡星脂质体具有靶向和缓释的双重作用。
The concentration of amikacin liposomes in each tissue of mice was determined by microbiological assay. The concentration and distribution of the amikacin liposomes after administration were studied and compared with free amikacin. The results showed that after single-dose intravenous injection of 52mg / kg amikacin or liposomal amikacin sulfate in mice, the drug concentration in each tissue at 0.5, 1, 3, 7, 12 and 24 hours was determined, . Compared with the free drug, liposomes of amikacin significantly improved heart (6.2 times), liver (9.5 times), spleen (284 times), lung (3 times), brain (14.7 times ), Serum (3 times) drug distribution, reducing the distribution of the kidneys (1/2). Liposomal amikacin not only changed the in vivo tissue distribution of the free drug, but also prolonged the half-life, and the plasma concentration could be maintained for 24 h (free drug only 7 h). This shows that the liposomes have the dual role of targeting and sustained release.