KC-404缓释片在健康志愿者体内的药代动力学及相对生物利用度

[Pharmacokinetics and relative bioavailability of KC-404 sustained release tablets in healthy volunteers].

作者信息

Li Tongling, Pang Yinuo, Wang Zhixiao, Jia Yurong, Cheng Qiang, Sun Jian

机构信息

Department of Clinic Pharmacy, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

出版信息

Sichuan Da Xue Xue Bao Yi Xue Ban. 2003 Jul;34(3):541-3.

PMID:12910715

Abstract

OBJECTIVE

To study the pharmacokinetics and relative bioavailability of KC-404 sustained release tablets and capsules in healthy volunteers.

METHODS

The concentration of KC-404 in serum was determined by HPLC method after a single oral dose (20 mg) of tablet or capsule was administered to 19 healthy male volunteers respectively in an open randomized cross-over test.

RESULTS

After being processed by 3P87 pharmacokinetics program, the experiment data showed that the pharmacokinetic parameters of the tablets and the capsules were AUC0-->infinity: 740.12 ng.h/ml and 724.04 ng.h/ml; tmax: 5.37 h and 5.11 h; Cmax: 46.98 ng/ml and 46.29 ng/ml; T1/2: 7.4 h and 7.0 h; MRT0-->infinity: 14.78 h and 14.39 h respectively. There were no significant differences in AUC, tmax, Cmax, T1/2 and MRT0-->infinity between these two preparations (P > 0.05). The relative bioavailability of KC-404 sustained release tablets was 102.6%.

CONCLUSION

These two preparations are bioequivalent.

摘要

目的

研究KC - 404缓释片和胶囊在健康志愿者体内的药代动力学及相对生物利用度。

方法

采用开放随机交叉试验，分别给19名健康男性志愿者单次口服20mg片剂或胶囊后，用高效液相色谱法测定血清中KC - 404的浓度。

结果

经3P87药代动力学程序处理后，实验数据表明，片剂和胶囊的药代动力学参数分别为：AUC0→∞：740.12ng·h/ml和724.04ng·h/ml；tmax：5.37h和5.11h；Cmax：46.98ng/ml和46.29ng/ml；T1/2：7.4h和7.0h；MRT0→∞：14.78h和14.39h。两种制剂在AUC、tmax、Cmax、T1/2和MRT0→∞方面均无显著差异（P＞0.05）。KC - 404缓释片的相对生物利用度为102.6%。