Shyu W C, Reilly J, Campbell D A, Wilber R B, Barbhaiya R H
Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Pharmaceutical Research Institute, Syracuse, New York 13221-4755.
Antimicrob Agents Chemother. 1993 May;37(5):1180-3. doi: 10.1128/AAC.37.5.1180.
Penetration of cefprozil into tonsillar and/or adenoidal tissues was investigated for patients undergoing tonsillectomy and/or adenoidectomy. A total of 29 patients ranging in age from 2 to 14 years participated in the study. The tonsils and/or the adenoids were removed at times ranging from 0.33 to 3.17 h after oral administration of a dose of either 7.5 or 20 mg/kg of body weight. A blood sample was also collected as soon as the tissue sample was removed. Plasma, tonsil, and adenoid samples were analyzed for cis and trans isomers of cefprozil by high-performance liquid chromatographic assays. The concentrations of the cis isomer of cefprozil in plasma ranged from 0.60 to 9.87 micrograms/ml at the 7.5-mg/kg dose level and from 1.04 to 20.40 micrograms/ml at the 20-mg/kg dose level. The corresponding concentrations of the cis isomer in tonsil tissue ranged from 0.48 to 2.42 micrograms/g and from 1.00 to 4.29 micrograms/g, respectively. The corresponding concentrations of the cis isomer in adenoid tissue ranged from 0.40 to 4.20 micrograms/g and from 1.74 to 4.94 micrograms/g, respectively. The concentrations of the trans isomer were about 1/10 of those observed for the cis isomer. The median ratios of the cefprozil concentration in tonsillar tissue to that in plasma were 0.37 and 0.47 for patients receiving a 7.5- or a 20-mg/kg oral dose of cefprozil, respectively. The corresponding median ratios for the adenoidal tissue were 0.46 and 0.82, respectively. The cefprozil concentrations in either the tonsillar or the adenoidal tissue at both dose levels over 3.17 h after dosing are much higher than the MICs for common pathogens which cause pharyngitis or tonsillitis.
对接受扁桃体切除术和/或腺样体切除术的患者,研究了头孢丙烯在扁桃体和/或腺样体组织中的渗透情况。共有29名年龄在2至14岁的患者参与了该研究。在口服7.5或20mg/kg体重剂量的头孢丙烯后0.33至3.17小时的不同时间切除扁桃体和/或腺样体。在切除组织样本后立即采集血样。通过高效液相色谱法分析血浆、扁桃体和腺样体样本中的头孢丙烯顺式和反式异构体。在7.5mg/kg剂量水平时,血浆中头孢丙烯顺式异构体的浓度范围为0.60至9.87μg/ml,在20mg/kg剂量水平时为1.04至20.40μg/ml。扁桃体组织中顺式异构体的相应浓度分别为0.48至2.42μg/g和1.00至4.29μg/g。腺样体组织中顺式异构体的相应浓度分别为0.40至4.20μg/g和1.74至4.94μg/g。反式异构体的浓度约为顺式异构体的1/10。接受7.5或20mg/kg口服剂量头孢丙烯的患者,扁桃体组织中头孢丙烯浓度与血浆中浓度的中位数比值分别为0.37和0.47。腺样体组织的相应中位数比值分别为0.46和0.82。给药后3.17小时内,两个剂量水平的扁桃体或腺样体组织中的头孢丙烯浓度均远高于引起咽炎或扁桃体炎的常见病原体的最低抑菌浓度。