稳态试验丙戊酸镁缓释片人体生物利用度的研究

Study on Biological Availability of Magnesium Valprote Extended Action Tablet

目的 比较稳态下丙戊酸镁缓释片与普通片的相对生物利用度和药代动力学参数。方法 采用气相色谱(GC)法测定人体血中丙戊酸浓度。结果 达峰浓度Cmax 普通片为(69. 57±12.80)μg/ml,缓释片为(58.45±11.83)μg/ml;达峰时间Tmax普通片为(1.8±0.7)h,缓释片为(3.9±1.8)h;峰谷浓度普通片为(48.91±12.00)mg/ml,缓释片为(52.87±11.03)mg/ml,波动系数DF普通片为(37±9)%,缓释片为(10±4)%,Csavg普通片为(57.12±11.93)μg/ml,缓释片为(59.16±24.22)μg/ml,相对生物利用度为103.97%。结论 丙戊酸镁缓释片与其普通片比较具有缓释特征,血药浓度稳定,其生物利用度与其普通片剂相似。

Objective To compare the pharmacokinetics parameters and relative biological availabilities of magnesium valprote extended action tablet and common tablet. Methods Using gas chromatogram (GC), The blood concentrations of valproic acid in human body were detected. Results The peak concentration of common tablet was (69.57±12.80) μg/ml, that of the extended action tablet was (58.45± 11.83)μg/ml, the peak times of them were (1.8±0.7)h, (3.9±1.8)h respectively; The peak valley concentrations of common and extended action tablet were (48.91±12.00)mg/ml, (52.87± 11.03) mg/ml respectively. The fluctuated quotieties of common and extended action tablet were (37±9)%, (10±4)%. The averages of steady state concentration of common and extended action tablet were (57.12±11.93) μg/ml, (59.16±24.22) μg/ml. The relative biological availability was 103.97%. Conclusions Compared with common tablet, magnesium valprote extended action tablet has the character of extending action, the concentration is steady, and the biological availability is similar to common tablet.