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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2023, Vol. 28 ›› Issue (2): 171-177.doi: 10.12092/j.issn.1009-2501.2023.02.007

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Bioequivalence study of cinacalcet hydrochloride tablets in healthy Chinese volunteers

YAN Qiangyong1,2, XIANG Daxiong1,2, ZHU Ronghua1,2, YANG Lingfeng2,3, YANG Xiding1,2, LI Jingjing1,2, FAN Xiao1,2, LIU Sai4, XIONG Shoujun4, FANG Pingfei1,2   

  1. 1Department of Pharmacy, the Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, China; 2Phase I Clinical Trial Center, the Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, China; 3Department of Metabolism & Endocrinology, the Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, China; 4Nanjing Hencer Pharmaceutical Co., Ltd., Nanjing 211200, Jiangsu, China
  • Received:2022-04-11 Revised:2023-02-08 Online:2023-02-26 Published:2023-03-10

Abstract:

AIM: To evaluate the bioequivalence of cinacalcet hydrochloride tablets in healthy Chinese volunteers. METHODS: A randomized, open, double-period and crossover trial was conducted, 48 healthy volunteers were administered a single dose of cinacalcet test tablets or reference tablets orally under each fasting and fed condition. The concentration of cinacalcet was determined by validated LC-MS/MS method. Pharmacokinetic parameters were calculated by Phoenix WinNonlin 8.0 to study its bioequivalence. RESULTS: The main pharmacokinetic parameters of test tablets and reference tablets under fasting condition were as follows: Cmax (5.96±4.15) and (6.11±4.08) ng/mL, AUC0-72h (45.82±30.20) and (46.11±29.50) ng·h·mL-1, AUC0-∞  (49.65±33.64) and (49.63±32.01) ng·h·mL-1, Tmax (4.5[1.0, 6.0]) and (4.5[1.0, 6.0]) h, t1/2 (23.15±9.23) and (22.43±8.81) h, respectively. Under fed condition, the main pharmacokinetic parameters of test tablets and reference tablets were as follows: Cmax (11.14±5.24) and  (10.24±5.39) ng/mL, AUC0-72h (76.70±39.34) and (75.18±34.36) ng·h·mL-1, AUC0-∞ (83.28±43.00) and (81.38±38.03) ng·h·mL-1, Tmax (3.0[1.5,5.0]) and (4.3[1.5,7.0]) h, t1/2 (28.07±6.37) and (27.46±5.44) h, respectively. The 90%confidence intervals of the geometric average ratios of Cmax, AUC0-72h and AUC0-∞ were all within the equivalent interval of 80.00%-125.00%. CONCLUSION: Two formulations of cinacalcet tablets are bioequivalent and safe.

Key words: cinacalcet, bioequivalence, LC-MS/MS, pharmacokinetics

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