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中国临床药理学与治疗学 ›› 2021, Vol. 26 ›› Issue (3): 299-304.doi: 10.12092/j.issn.1009-2501.2021.03.009

• 临床药理学 • 上一篇    下一篇

琥珀酸索利那新片在中国健康受试者的生物等效性研究#br#

王晖1,2，崔畅1,2，杨双1,2，姚安1,2，吴淑婷1,2，阳晓燕1,2，叶玲1,2，邹志3，唐智3，阳国平1,2，黄洁1,2，欧阳冬生3
  

  1. 1中南大学湘雅三医院临床药理中心，2中南大学临床试验研究中心，长沙 410013，湖南；3长沙都正生物科技有限公司，长沙 410000，湖南

  • 收稿日期:2020-12-07 修回日期:2021-02-05 出版日期:2021-03-26 发布日期:2021-04-06
  • 通讯作者: 黄洁，通信作者，女，硕士，助理研究员，主要从事临床药理学方向研究。 Tel: 15116469024 E-mail: cellahuang1988@163.com 欧阳冬生，共同通信作者，男，教授，主要从事临床药理学方向研究。 Tel: 13307313736 E-mail: dongsheng.ouyang@duxact.com
  • 作者简介:王晖，男，博士研究生在读，主要从事临床药理学方向研究。 Tel: 13875759809 E-mail: wang.hui@csu.edu.cn
  • 基金资助:
    国家自然科学基金（81673519）；国家十三五重大新药创制课题（2020ZX09201010）；湖南省青年基金项目（2020JJ5852）

Bioequivalence of solifenacin succinate tablets in healthy Chinese volunteers

WANG Hui1,2, CUI Chang1,2, YANG Shuang1,2, YAO An1,2, WU Shuting1,2, YANG Xiaoyan1,2, YE Ling1,2, ZOU Zhi3, TANG Zhi3, YANG Guoping1,2, HUANG Jie1,2, OUYANG Dongsheng3   

  1. 1 Center of Clinical Pharmacology, the Third Xiangya Hospital, Central South University, Changsha 410013, Hunan, China; 2 Research Center of Drug Clinical Evaluation of Central South University, Changsha 410013, Hunan, China; 3 Changsha Duxact Biotech Co, Ltd., Changsha 410000, Hunan, China
  • Received:2020-12-07 Revised:2021-02-05 Online:2021-03-26 Published:2021-04-06

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摘要： 目的：评价中国健康受试者空腹及餐后单次口服琥珀酸索利那新受试制剂和参比制剂的生物等效性。方法：采用单中心、随机、开放、两周期交叉设计，空腹组和餐后组受试者各24例，每周期口服受试制剂或参比制剂10 mg，采用LC-MS/MS法测定索利那新血药浓度，WinNonlin 7.0软件计算药动学参数，并进行生物等效性评价。结果：空腹组受试制剂与参比制剂的药动学参数分别为：Cmax（13.99±3.34）和（13.27±3.20）ng/mL，AUC0-t（675.60±210.46）和（653.31±238.59）h·ng·mL-1，AUC0-∞（728.28±240.20）和（718.14±275.63）h·ng·mL-1，tmax（5.00±1.41）h和（4.98±1.07）h，t1/2（39.19±9.29）和（42.44±12.66）h，相对生物利用度按AUC0-t计算为105.06%，按AUC0-∞计算为104.07%。餐后组受试制剂与参比制剂的药动学参数分别为：Cmax（15.65±5.30）和（15.02±4.42） ng/mL，AUC0-t（808.85±271.19）和（793.76±256.78） h·ng·mL-1，AUC0-∞（917.02±347.82）和（875.49±310.77）h·ng·mL-1，tmax（4.29±1.48）h和（5.69±4.10）h，t1/2（49.47±20.08）和（45.29±12.24）h，相对生物利用度按AUC0-t计算为100.91%，按AUC0-∞计算为102.97%。空腹/餐后条件下两制剂的主要药动学参数Cmax、AUC0-t、AUC0-∞几何均数比值的90%置信区间均在80.00%～125%。结论：琥珀酸索利那新的受试制剂和参比制剂在空腹和餐后条件下，均生物等效。

关键词: 琥珀酸索利那新, LC-MS/MS, 生物等效性, 药代动力学

Abstract: AIM: To evaluate the bioequivalence of the test and reference preparations of solifenacin succinate tablets administered once orally under fasting and fed conditions in Chinese healthy volunteers.  METHODS: The study was designed as single-center, randomized, open, self-crossover and twenty four healthy volunteers were recruited respectively in fasting and fed conditions. Subjects were assigned to receive a single oral of the test or reference formulation per period at a dose of 10 mg. The plasma concentration of solifenacin was analyzed by LC-MS/MS. The major pharmacokinetic parameters were calculated by WinNonlin 7.0, then the bioequivalence was evaluated.RESULTS: The main pharmacokinetic parameters of a single oral solifenacin succinate under fasting condition for test and reference preparation were as follows: Cmax (13.99±3.34) and (13.27±3.20) ng/mL, AUC0-t (675.60±210.46) and (653.31±238.59) h·ng·mL-1, AUC0-∞(728.28±240.20) and (718.14±275.63) h·ng·mL-1, tmax (5.00±1.41) h and (4.98±1.07) h, t1/2 (39.19±9.29) and (42.44±12.66) h. The relative bioavailability was 105.06% for AUC0-t, 104.07% for AUC0-∞. The main pharmacokinetic parameters of a single oral solifenacin succinate under fed condition for test and reference preparation were as follows: Cmax (15.65±5.30), (15.02±4.42) ng/mL; AUC0-t (808.85±271.19), (793.76±256.78) h·ng·mL-1; AUC0-∞ (917.02±347.82), (875.49±310.77) h·ng·mL-1. tmax (4.29±1.48) h and (5.69±4.10) h, t1/2 (49.47±20.08) and (45.29±12.24) h. The relative bioavailability was 100.91% for AUC0-t, 102.97% for AUC0-∞. The 90% confidence intervals of the geometric mean ratios of the main pharmacokinetic parameters Cmax, AUC0-t, AUC0-∞ of the two preparations under fasting/feding conditions were all within 80%-125%.CONCLUSION: The test and reference preparation of solifenacin succinate tablets are bioequivalent under fasting and fed conditions.

Key words: solifenacin succinate, LC-MS/MS, bioequivalence, pharmacokinetic

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