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家兔肌肉和静脉注射20mg/kg国产氨噻肟头孢菌素药代动力学研究结果表明,两种给药途径的药代动力学均符合二室开放式模型,其数学表达式分别为C_1=58.5e~(-12.14t)+39.4e~(-2.48t)+19.1e~(-0.46t)(肌肉注射)和C_t=148.6e_(-5.28t)+30.6e~(-1.25t)(静脉注射)。家兔肌肉注射氨噻肟头孢菌素的消除半衰期(T(1/2)β)为1.51小时,表观分布容积(Vd)为1.77L,高峰血清浓度(C_(max))为35.3μg/ml,达峰时间(T_(max))为15分钟,24小时尿中回收率为67.39%;肌肉注射的生物利用度为91.6%,表明家兔肌注该药后被其机体吸收利用的程度较高;静脉注射的消除半衰期为0.55小时,表观分布容积为0.47L,24小时尿中回收率为61.45%。 家兔静脉注射氨噻肟头孢菌素与第一代头孢菌素噻吩头孢菌素、唑啉头孢菌素的药代动力学比较结果表明,氨噻肟头孢菌素的药代动力学性质同噻吩头孢菌素相似,具有半衰期短,室间转运速率快,体内分布、消除迅速,肾清除率高等特点;而与唑啉头孢菌素不同。 药代动力学的研究结果还表明,肌注和静注两种途径给药,均能得到高于临床常见致病菌的最低抑菌浓度(MIC)的数十倍到上百倍的血、尿药物浓度,可以有效地控制这些细菌所致的各种感染疾患。
The results of pharmacokinetics study of domestic cefotaxime with 20mg / kg intramuscular and intravenous injection in rabbits showed that the pharmacokinetics of the two routes of administration were in accordance with the two-compartment open model and the mathematical expressions were C_1 = 58.5e ~ -12.14t + 39.4e ~ -2.48t + 19.1e ~ -0.46t (intramuscular injection) and C_t = 148.6e_ (-5.28t) + 30.6e ~ (-1.25t) ( Intravenous injection). The elimination half-life (T (1/2) β) of rabbit intramuscular injection of cefotaxime was 1.51 hours, the apparent volume of distribution (Vd) was 1.77L and the peak serum concentration (C max) was 35.3μg / ml, the peak time (T max) was 15 minutes, the urinary recovery rate was 67.39% after 24 hours; the bioavailability of intramuscular injection was 91.6%, indicating that the degree of absorption and utilization by the body after intramuscular injection of the drug High; intravenous elimination half-life of 0.55 hours, the apparent volume of distribution of 0.47L, 24-hour urine recovery was 61.45%. Pharmacokinetics of intravenous injection of cefotaxime with first-generation cephalosporin and cefazolin in rabbits showed that the pharmacokinetics of cefotaxime was consistent with that of thiophene Cephalosporins are similar, with a short half-life, fast room transport rate, distribution in the body, to eliminate rapidly, high rate of renal clearance; and unlike azole cephalosporins. Pharmacokinetic studies also showed that intramuscular and intravenous injection of both ways, can get higher than the common clinical pathogenic bacteria minimum inhibitory concentration (MIC) several times to hundreds of times the blood, urine Drug concentration, can effectively control these bacteria caused by a variety of infectious diseases.