【摘要】 为了制订给药方案，作者对第一、二、三代９种头孢菌素在健康志愿者中的药物动力学进行了研究，包括头孢唑啉、头孢拉定、头孢羟氨苄、头孢呋辛、头孢噻肟、头孢唑肟、头孢曲松、头孢他啶和头孢克肟。测定了单剂给药后的血尿浓度，计算了药动学参数，并进行了比较，全部注射给药头孢菌素血药浓度均高，以头孢曲松为最高，口服者头孢克肟最低。消除半减期多为１～２小时，然头孢曲松长达８小时。大部分头孢菌素自肾排泄，给药后２４小时内自尿中排出给药量的８６％￣９６％，而头孢曲松、头孢克肟和头孢噻肟则分别排出３７％、２４％和５１％。根据本研究中获得的药动学资料，提出不同头孢菌素类治疗各种感染的给药方案。更多还原

【Abstract】 n order to propose the therapeutic regimens, clinical pharmacokinetic study of 9cephalosporins, including cefazolin,cefradine, cefadroxil,cefuroxime,cefotaxime,cefti- zoxime, ceftriaxone, ceftazidime, cefixime, was carried out in normal volunteers.Blood and urine concentrations of the drugs were determined after single dose administra- tions. Pharmacokinetic parameters were calculated and compared. The peak Serum con- centrations (Cmaxs)of all parenteral cephalosporins were high, ceftriazone was the highest.The Cmaxs of oral cephalosporins were much lower than those of parentera1 cephalosporins, cefixime was the lowest.Most cephalosporins Were eliminated rapidly, with serum half-lives(t1/2Ke)of 1-2h,the exception was ceftriaxone with the tl/2Ke of 8h。The drugs were eliminaed mostly by the kidneys. The urinary recovery rates within 24 hours were 86-96% for cefazolin, cefradine, cefadroxil, cefuroxime,ceftizo-xime and ceftazidime. However ceftriaxone, cefixime and cefotaxime were el iminated partially through kidneys, the recovery rates were 37%,24% and 51% respectively.Based on the pharmacokinetic data obtained, the therapeutic regimens of different cepha- losporins were proposed for the treatment of Various infections.更多还原