头孢克肟口腔崩解片在健康人体的生物等效性

Bioequivalence of cefixime orally disintegrating tablets in healthy volunteers

目的：观察头孢克肟口腔崩解片在健康人体的生物等效性。方法：18名健康受试者随机双交叉单剂量口服头孢克肟口腔崩解片受试制剂和头孢克肟胶囊参比制剂200mg．用HPLC法测定头孢克肟血药浓度。用DAS2．0药动学程序计算主要药动学参数并评价：种制剂生物等效性。AUC0-24、AUG0-∞和Cmax经方差分析和双单侧t检验，tmax进行非参数法检验。结果：单剂量口服受试制刹和参比制剂后血浆中头孢克肟的Cmax分别为（3．0±0．9）mg·L^-1和（2．8±0．9）mg·L^-1；tmax分别为（3．5±0．8）h和（4．4±1．1）h；t1/2分别为（2．9±0．8）h和（2．7±0．7）h；AUG0-24分别为（22．0±7．1）mg·h·L^-1和（22．6±7．1）mg·h·L^-1；AUG0-∞分别为（22．7±7．0）mg·h·L^-1和（23．2±7．0）mg·h·L^-1；Cmax、AUGⅧ和AUC0-∞的90%可信区间分别88．9％～127．1％，82．8％～116．3％和83．7％～115．5％，相对生物利用度F0-24、F0-∞分别为（106．6±52．2）％和（105．9±48．3）％。结论：头孢克肟口腔崩解片与头孢克肟胶囊的Cmax、AUG0-24和AUC0-∞一致,吸收程度等效；头孢克肟口腔崩解片吸收速度明显快于头孢克肟胶囊。

OBJECTIVE To study the bioequivalence of cefixime orally disintegrating tablets in comparison with cefixime capsules in healthy volunteers.METHODS A single oral dose （200 mg of test and reference preparations） were given to 18 healthy volunteers in a randomized crossover study. The concentrations of cefixime in serum were determined by HPLC. The pharmacokinetics parameters were calculated and the bioequivalence of two preparations were evaluated by DAS 2. 0 program. RESULlS The main pharmacokinetics parameters of the tested and reference cefixime were as follows： Cmax were （3. 0 ± 0. 9） mg·L ^-1and （2.8±0. 9） mg·L^-1; Tmax were （3.5±0.8）h and （4.4± 1.1）h; t1/2 were （2.9±0.8）h and （2.7±0. 7）h; AUC0-24were （22.0±7. 1） mg·h·L^-1 and （22.6±7.1） mg·h·L^-1 ; AUG0-∞were （22.7±7.11）mg·h·L^-1 and （23.2±7.0） mg·h·L^-1; The 90% confidential interval of Cmax, AUC0-24; and AUC0-∞ were 88. 9%- 127. 1,82.8%-116. 3% and 83.7% 115.5% ,respectively; F0-24and F0-∞ were （ 106. 6 ± 52.2） % and （ 105.9 ± 48. 3） %, respectively. CONCLUSION The results of statistical analysis for Cmax AUC0-24 and AUC0-∞ show that the two preparations are bioequivalent. There are singnificant differences in Tmax between two preparations and the cefixime orally disintegrating tablets are absorbed faster.