摘要
Temocillin的犬药代动力学及组织浓度研究是用微生物法测定血清及组织中药物浓度。静注和肌注本品20mg/kg后,体内药物转运过程分别符合开放型二室和一室模型。静注本品后即刻血浓度为141.1± 38.4μg/ml,分布相半衰期仅为0.06小时,故可迅速达到有效杀菌浓度。肌注后0.49小时达峰值,为47.8μg/ml。肌注与静注后血浆清除半衰期分别为1.23 ±0.14和1.08±0.13小时。总表观分布容积分别为0.29±0.01和0.26±0.05L/kg。生物利用度为93.1％。 4只犬分别单次静脉注射本品20gm/kg,测定1小时后各组织浓度。结果显示,胆汁中药物浓度高达176.7±123.4μg/ml, 为血清浓度的5倍,其次肝组织浓度为43.45±9.91μm/ml,略高于血浓度。按浓度递减顺序,其它组织分别为骨骼肌、肺、子宫、肾、胰腺、前列腺、脾、小肠和心肌。脑组织和脑脊液药物浓度未测出。
The pharmacokinetics and tissue concentration of temocillin in healthy dogs were reported. The drug concentration were measured by bioassay method. The serum drug concentration-time profile conformed to the two-compartment open modle by IV injection and one-compartment open model after IM injection.For IV injection of 20mg/kg, the mean peak level was 141.1 ± 38.4μg/ml, Tl/2α was 0.06 hour. Thus,the effective bactericidal concentration can be attained rapidly.By the same dose, after IM injection, the mean peak level was 47.8±4.3 μg/ml and was obtained at
(Tmax) 0.49± 0.104 hour. The elimination halflives after IM and TV injection were 1.23 ± 0.14 and 1.08± 0.01 hours, respectively. The apparent volume of distribution were 0.29 ±0.01 and 0.26 ± 0.05L/kg, respectively. The bioavailility for IM injection was 93.1%.
Tissue concentrations were measured in 4 dogs 1 hour after IV injection of 20 mg/kg. The results showed that the concentration in the bile was the highest, reaching 176.7±123.4 Mg/ml. Hepatic drug-concentration was 33.45± 9.91 μg/ml, which was
slightly higher than that of the serum.The concentrations in decreasing order in other tissues were muscle, lung, uterus, kidney, pancreas, prostate, spleen, small intestine and heart. The concentrations in the brain and cerebrospinal fluid were less than 2μg/ ml.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
1990年第4期275-280,共6页
Chinese Journal of Antibiotics
