国产丙戊酸钠无糖口服液人体生物等效性研究
孙培红，崔一民，刘玉旺，赵东方，孙忠民
(北京大学第一医院药剂科，北京100034)
[摘要] 目的：评价国产丙戊酸钠无糖口服液和进口丙戊酸钠糖浆两种制剂的生物等效性。方法：20例健康男性志愿者双周期随机交叉口服单剂量1000mg(25mL) 国产丙戊酸钠无糖口服液和进口丙戊酸钠糖浆两种制剂，分别于服药前及服药后0.33，0.67，1，1.5，2，4，8，12，24，36，48及72h采集血样。用高效液相-荧光色谱法测定血清中丙戊酸钠的浓度，并用3P97程序对试验数据进行处理。结果：单次口服国产及进口丙戊酸钠制剂的Cmax分别为(112.65±16.91)和(110.22±15.20)μg·mL-1；Tmax分别为(0.86±0.38)和(1.09±0.48)h；AUC0~72h分别为(1980.24±275.82)和(1950.11±305.60)μg·h·mL-1；AUC0~¥分别为(2088.19±313.25)和(2075.30±367.58)μg·h·mL-1；单次口服国产丙戊酸钠无糖口服液的相对生物利用度F0~72h为(102.96±15.37)%，F0~¥为(102.25±15.61)%。结论：单次口服国产丙戊酸钠无糖口服液和进口丙戊酸钠糖浆具有生物等效性。
, 百拇医药
[关键词] 丙戊酸钠；生物等效性；高效液相-荧光色谱法；相对生物利用度
[中图分类号] R971.6；R969.4 [文献标识码] B [文章编号]1003-3734(2001)
Study on bioequivalence of domestic sodium valproic oral liquid in healthy volunteers
SUN Pei-Hong，CUI Yi-Min，LIU Yu-Wang，ZHAO Dong-Fang，SUN Zhong-Min
(Department of Pharmacy, First Medical School，Peking University, Beijing 100034,China)
, 百拇医药
[Abstract] Objective：To evaluate relative bioavailability and bioequivalence of domestic sodium valproic oral liquid and imported sodium valproic syrup in healthy volunteers. Methods：A single oral administration of 1000mg(25mL) domestic sodium valproic oral liquid and imported sodium valproic syrup were given to 20 healthy male volunteers in randomized crossover study respectively. A high performance liquid chromatographic assay with fluorimetric detection was developed to determine the concentration of sodium valproic in human serum. The dada were analyzed by 3P97 program. Results：The pharmacokinetics parameters after a single oral administration of 1000mg domestic sodium valproic oral liquid and imported sodium valproic syrup were as follows：Cmax (112.65±16.91 )and( 110.22±15.20 )μg·mL-1；Tmax (0.86±0.38 )and(1.09±0.48)h；AUC0~72h (1980.24±275.82 )and (1950.11±305.60)μg·h·mL-1；AUC0~¥ (2088.19±313.25) and (2075.30±367.58)μg·h·mL-1；F0~72h (102.96±15.37)%、F0–¥(102.25±15.61)% respectively. Variance analysis and two-onesided test were performed to parameters：Cmax , AUC0~72h , AUC0–¥. There were no significant difference. Conclusion： The relative bioavailability of single oral administration group was (102.96±15.37)%. The two preparations were of bioequivalence
, 百拇医药
[Key words] sodium valproic；bioequivalence；fluorimetric-HPLC；relative bioavailability
[作者简介] 孙培红(1965-)，女，副主任药师，主要从事临床药学及药代动力学方面的研究。联系电话：(010)66171122转2043，E-mail：speihong@263.net。
[参考文献]
[1] 郁健，王广基，杜春波，等. 高效液相色谱法测定人血清中丙戊酸钠的含量[J]. 中国药科大学学报, 1998,29(1):45-48.
[2] Bressolle F, Gomeni R, Airic R，et al. A double weibull input function describes the complex absorption of sustained-release oral sodium valproate[J]. J Pharm Sci, 1994, 83(10):1461-1464., 百拇医药
(北京大学第一医院药剂科，北京100034)
[摘要] 目的：评价国产丙戊酸钠无糖口服液和进口丙戊酸钠糖浆两种制剂的生物等效性。方法：20例健康男性志愿者双周期随机交叉口服单剂量1000mg(25mL) 国产丙戊酸钠无糖口服液和进口丙戊酸钠糖浆两种制剂，分别于服药前及服药后0.33，0.67，1，1.5，2，4，8，12，24，36，48及72h采集血样。用高效液相-荧光色谱法测定血清中丙戊酸钠的浓度，并用3P97程序对试验数据进行处理。结果：单次口服国产及进口丙戊酸钠制剂的Cmax分别为(112.65±16.91)和(110.22±15.20)μg·mL-1；Tmax分别为(0.86±0.38)和(1.09±0.48)h；AUC0~72h分别为(1980.24±275.82)和(1950.11±305.60)μg·h·mL-1；AUC0~¥分别为(2088.19±313.25)和(2075.30±367.58)μg·h·mL-1；单次口服国产丙戊酸钠无糖口服液的相对生物利用度F0~72h为(102.96±15.37)%，F0~¥为(102.25±15.61)%。结论：单次口服国产丙戊酸钠无糖口服液和进口丙戊酸钠糖浆具有生物等效性。
, 百拇医药
[关键词] 丙戊酸钠；生物等效性；高效液相-荧光色谱法；相对生物利用度
[中图分类号] R971.6；R969.4 [文献标识码] B [文章编号]1003-3734(2001)
Study on bioequivalence of domestic sodium valproic oral liquid in healthy volunteers
SUN Pei-Hong，CUI Yi-Min，LIU Yu-Wang，ZHAO Dong-Fang，SUN Zhong-Min
(Department of Pharmacy, First Medical School，Peking University, Beijing 100034,China)
, 百拇医药
[Abstract] Objective：To evaluate relative bioavailability and bioequivalence of domestic sodium valproic oral liquid and imported sodium valproic syrup in healthy volunteers. Methods：A single oral administration of 1000mg(25mL) domestic sodium valproic oral liquid and imported sodium valproic syrup were given to 20 healthy male volunteers in randomized crossover study respectively. A high performance liquid chromatographic assay with fluorimetric detection was developed to determine the concentration of sodium valproic in human serum. The dada were analyzed by 3P97 program. Results：The pharmacokinetics parameters after a single oral administration of 1000mg domestic sodium valproic oral liquid and imported sodium valproic syrup were as follows：Cmax (112.65±16.91 )and( 110.22±15.20 )μg·mL-1；Tmax (0.86±0.38 )and(1.09±0.48)h；AUC0~72h (1980.24±275.82 )and (1950.11±305.60)μg·h·mL-1；AUC0~¥ (2088.19±313.25) and (2075.30±367.58)μg·h·mL-1；F0~72h (102.96±15.37)%、F0–¥(102.25±15.61)% respectively. Variance analysis and two-onesided test were performed to parameters：Cmax , AUC0~72h , AUC0–¥. There were no significant difference. Conclusion： The relative bioavailability of single oral administration group was (102.96±15.37)%. The two preparations were of bioequivalence
, 百拇医药
[Key words] sodium valproic；bioequivalence；fluorimetric-HPLC；relative bioavailability
[作者简介] 孙培红(1965-)，女，副主任药师，主要从事临床药学及药代动力学方面的研究。联系电话：(010)66171122转2043，E-mail：speihong@263.net。
[参考文献]
[1] 郁健，王广基，杜春波，等. 高效液相色谱法测定人血清中丙戊酸钠的含量[J]. 中国药科大学学报, 1998,29(1):45-48.
[2] Bressolle F, Gomeni R, Airic R，et al. A double weibull input function describes the complex absorption of sustained-release oral sodium valproate[J]. J Pharm Sci, 1994, 83(10):1461-1464., 百拇医药