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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2010, Vol. 15 ›› Issue (11): 1256-1260.

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Pharmacokinetics of minidose nalmefene hydrochloride in healthy chinese volunteers

FU Zhi-min1, YUAN Hong1, TAN Hong-yi1, TAN Zhi-rong2, PEI Qi1, OU YANG Dong-sheng2, HUANG Yuan-yuan1, HUANG Zhi-jun1, YANG Guo-ping1   

  1. 1Center of Clinical Pharmacology, the Third Xiangya Hospital of Central South University, Changsha 410013, Hunan,China;
    2Clinical Pharmacologic Research Institute, Central South University, Changsha 410078, Hunan, China
  • Received:2010-10-06 Revised:2010-11-02 Online:2010-11-26 Published:2020-09-16

Abstract: AIM: To study the pharmacokinetics of minidose Nalmefene hydrochloride in healthy Chinese volunteers. METHODS: In a randomized crossover trial, 12 healthy Chinese subjects received Nalmefene hydrochloride 0.05 and 0.1 mg by intravenous injection.The concentration of Nalmefene in human plasma was determined by LC-MS/MS method and its pharmacokinetic parameters were calculated by DAS 2.0. RESULTS: The main pharmacokinetic parameters of Nalmefene after a single intravenous administration dose of 0.05 and 0.1 mg Nalmefene hydrochloride were as follows: Cmax were (203±99) and (488±350) ng/L; AUC0-8 were (177±94) and (480±194) ng·L-1·h; AUC0-∞ were (282±134) and (649±247) ng·L-1·h; Tmax were (0.08±0.07) and (0.12±0.14) h; t1/2 were(2.0±1.1) and (2.8±1.2) h, respectively. CONCLUSION: The pharmacokinetics of minidose Nalmefene hydrochloride in healthy Chinese volunteer was agreement with the two-compartment mode characteristics and linear kinetics under the intravenous injection dose of 0.05 to 0.1 mg.

Key words: Nalmefene hydrochloride, LC-MS/ MS, Pharmacokinetics

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