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目的进行两种双氯芬酸缓释片的单次给药的生物利用度比较研究和多次给药的峰谷浓度波动研究。方法12位健康男性受试者按交叉试验单剂量服用试验片和对照片,采用HPLC方法测定人血清中的药物浓度 ,并比较其生物利用度。结果两种片剂的Cmax 和AUC无显著差异(P>0.05),但试验片给药后的达峰时间(Tpeak)显著小于对照片 ,与对照片相比有非常显著差异(P<0.01)。试验片相对于对照片的相对生物利用度为98 11 %,经统计学检验证明这两种制剂具有生物等效性。12位受试者连续服用试验片和对照片的交叉试验表明 ,两种缓释片在稳态时的峰浓度(Cmax)、谷浓度(Cmax)、平均浓度(Cavg)、峰谷比(r)和峰谷波动度(DF)均无显著差异(P>0.05) ,最小有效浓度持续时间(Tmec50)也基本一致 ,说明两种缓释片在稳态时的峰谷浓度波动程度相当 ,具有较好的缓释特征。在多次给药时 ,试验片的达峰时间同样显著小于对照片(P<0.01)。结论试验结果表明两种缓释片具有生物等效性 ,都具有峰谷浓度差异小 ,波动幅度小的特点 ,与对照片相比 ,无论单次给药还是多次给药 ,试验片的达峰时间都显著缩短。
OBJECTIVE To compare the bioavailability of single diclofenac sustained-release tablets and the fluctuation of peak-to-trough concentrations in multiple administrations. Methods Twelve healthy male subjects were given a single dose of test and control tablets in a crossover test. The concentration of the drug in human serum was determined by HPLC and its bioavailability was compared. Results There was no significant difference in Cmax and AUC between the two tablets (P> 0.05). However, the Tpeak of the two tablets was significantly lower than that of the control (P <0.01) . The relative bioavailability of the test piece relative to the control was 98 11%, which was confirmed by statistical tests to be bioequivalent. The crossover tests of 12 consecutive subjects and the control subjects showed that the Cmax, Cmax, Cavg, r (P> 0.05), and the minimum effective concentration duration (Tmec50) were also basically the same, indicating that the two kinds of sustained-release tablets in the steady-state peak trough concentration fluctuations, with Better slow release characteristics. At multiple administrations, the peak time of the test piece was also significantly less than that of the control (P <0.01). Conclusion The results showed that the two sustained-release tablets were bioequivalent and both had the characteristics of small difference in peak-trough concentration and small fluctuation range. Compared with the control group, no matter single or multiple administration, Peak times are significantly shorter.