Bioequivalence study of sidenafil citrate tablets in Chinese healthy subjects
10.13699/j.cnki.1001-6821.2024.03.026
- VernacularTitle:枸橼酸西地那非片在中国健康受试者体内的生物等效性研究
- Author:
Xiao-Bin LI
1
;
Lu CHEN
;
Xiu-Jun WU
;
Yu-Xin GE
;
Wen-Chao LU
;
Ting XIAO
;
He XIE
;
Hua-Wei WANG
;
Wen-Ping WANG
Author Information
1. 辽宁中医药大学附属医院GCP中心Ⅰ期临床病房,辽宁沈阳 110032
- Keywords:
sidenafil citrate tablet;
N-desmethyl sildenafil;
bioequivalence;
safety
- From:
The Chinese Journal of Clinical Pharmacology
2024;40(3):430-434
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the bioequivalence of oral sidenafil citrate tablets manufactured(100 mg)test preparations and reference preparations in healthy subjects under fasting and fed conditions.Methods Using a single-dose,randomized,open-lable,two-period,two-way crossover design,36 healthy subjects respectively for fasting and fed study were enrolled,and randomized into two groups to receive a single dose of test 100 mg with 7-day washout period.Plasma concentration of sidenafil and N-demethylsildenafil was determined by liquid chromatography-tandem mass spectrometry(LC-MS/MS)method.The pharmacokinetic parameters were calculated by Analyst 1.6.3(AB Scie)using non-compartmental model,and bioequivalence evaluation was performed for the two preparations.Relevant safety evaluations were performed during the trial.Results The main pharmacokinetic parameters of sidenafil after a single oral dose of sidenafil citrate tablets under fasting condition for test and reference were as follows:Cmax were(494.69±230.94)and(558.78±289.83)ng·mL-1,AUC0-t were(1 336.21±509.78)and(1 410.82±625.99)h·ng·mL-1,AUC0-were(1 366.49±512.16)and(1 441.84±628.04)h·ng·mL-1,respectively.The main pharmacokinetic parameters of sidenafil under fed condition for T and R were as follows:Cmax were(381.89±126.53)and(432.47±175.91)ng·mL-1,AUC0-t were(1 366.34±366.99)and(1 412.76±420.37)h·ng·mL-1,AUC0-were(1 403.28±375.32)and(1 454.13±429.87)h·ng·mL-1,respectively.The results demonstrated the bioequivalence of sidenafil citrate tablets between T and R.The incidence of adverse events in fasting and fed tests were 33.33％and 25.00％,respectively.No serious adverse event was reported.Conclusion The test and reference formulation of sidenafil citrate tablets were equivalent and was safe.
