Korting H C, Schäfer-Korting M, Haag R, Mutschler E
Int J Clin Pharmacol Ther Toxicol. 1984 Apr;22(4):218-20.
Following a single intramuscular application of 1 g ceftizoxime, levels of the drug were determined in plasma as well as in suction blister fluid (SBF) and cantharides blister fluid (CBF). This regimen invariably led to both high and long-lasting plasma levels: 81 +/- 16 min post dose maximum plasma levels of 17.5 +/- 3.1 micrograms/ml were reached; 6 h post dose levels of 4.6 +/- 0.4 micrograms/ml were still found, i.e., 4375 and 1150 times, respectively, the MIC90% of Neisseria gonorrhoeae. The high plasma levels were parallelled by high concentrations in SBF, with peaks amounting to 8.4 +/- 1.0 micrograms/ml. Peak concentrations in CBF ranged from 8.1 to 15.7 micrograms/ml. Thus, the pharmacokinetic behavior of ceftizoxime given as a single intramuscular injection of 1 g explained the excellent clinical results of this regimen in uncomplicated gonorrhea.
单次肌内注射1克头孢唑肟后,测定了血浆、吸疱液(SBF)和斑蝥水疱液(CBF)中的药物水平。该给药方案总是导致血浆水平高且持久:给药后81±16分钟达到最大血浆水平17.5±3.1微克/毫升;给药后6小时仍可检测到4.6±0.4微克/毫升的水平,分别是淋病奈瑟菌MIC90%的4375倍和1150倍。血浆中的高浓度与SBF中的高浓度平行,峰值达8.4±1.0微克/毫升。CBF中的峰值浓度在8.1至15.7微克/毫升之间。因此,单次肌内注射1克头孢唑肟的药代动力学行为解释了该方案在单纯性淋病中优异的临床效果。