头孢克洛干混悬剂的药动学及生物等效性研究.doc

头孢克洛干混悬剂的药动学及生物等效性研究 薛洪源，杨汉煜，侯艳宁，杨荣慧，贾丽霞，楚波1.白求恩国际和平医院临床药理室，河北 石家庄 050082；2.石药集团中奇制药技术有限公司，河北 石家庄 050011；3.河北医科大学，河北 石家庄健康男性志愿者单剂量口服两种头孢克洛干混悬剂250 mg，用液相色谱-串联质谱法测定血浆中头孢克洛的浓度，将20名受试者的经时血药浓度录入DAS（ver 1.0）程序，进行统计分析。结果 单剂量口服试验与参比制剂后头孢克洛的Cmax分别为（9.00±1.68）和（9.59±1.61）(g·mL-1，Tmax分别为（0.37±0.12）和（0.35±0.05）h，t1/2分别（0.88±0.16）和（0.87±0.11）h，AUC0-5 h分别为（7.91±1.00）和（7.91±1.10）(g·h·mL-1，AUC0-∞分别为（7.98±1.02）和（7.98±1.11）(g·h·mL-1，max进行非参数秩和检验，Cmax、AUC0-5 h、AUC0-∞经对数转换后做方差分析，并经双向单侧t检验；两制剂的Tmax、Cmax、AUC0-5 h、AUC0-∞均无显著性差异，受试制剂的AUC0-5 h、AUC0-∞的90 %可信限落在参比制剂的80 %～125 %范围内；Cmax的90%可信限落在参比制剂的70 %～143 %范围内。试验制剂的相对生物利用度为（100.7±12.5）%。结论 试验制剂与参比制剂具有生物等效性。 [关键词] 头孢克洛；干混悬剂；相对生物利用度；生物等效性；药动学；高效液相色谱-串联质谱法 Pharmacokinetic properties and bioequivalence of cefaclor for suspension after single dose administration in healthy volunteers XUE Hong-yuan1, YANG Han-yu2, HOU Yan-ning1,YANG Rong-hui1, JIA Li-xia1, CHU Bo3 (1 Department of pharmacology, Bethune International Peace Hospital, Hebei Province, Shijiazhuang, 050082, China;2 Shijiazhuang Pharmaceutical Group Co. Ltd. Zhongqi Corporation, Shijiazhuang 050011, China; Hebei Medical University Pharmacy School, Hebei Province, Shijiazhuang, 050017) ABSTRACT：AIM To study the bioequivalence and relative bioavailability of two cefaclor for suspensions. METHODS A single oral adminstration of 250 mg test and reference suspensions were given to 20 healthy male volunteers according to a randomized crossover design. The concentrations of cefaclor in plasma were determined by a HPLC/MS/MS method. The pharmacokinetic parameters were calculated and the bioequivalence were compared by DAS (ver 1.0) program. RESULTS The pharmacokinetic parameters of test and reference preparations were as follows: Cmax were (9.00?.68) cand (9.59?.61) .(g·mL-1，Tmax were (0.37±0.12) and (0.35±0.05) h，t1/2 were (0.88±0.16) and (0.87±0.11) h，AUC0-5 h were (7.91±1.00) and (7.91±1.10) (g·h·mL-1，AUC0-∞were (7.98±1.02) and (7.98±1.11), respectively. There were no significant d