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Arzneimittelforschung 2012; 62(05): 247-251
DOI: 10.1055/s-0032-1304649
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Pharmacokinetic and Bioequivalence Studies of Trospium chloride after a Single-dose Administration in Healthy Chinese Volunteers

R. Zhang
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
G. Yuan
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
R. Li
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
X. Liu
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
C. Wei
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
B. Wang
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
H. Gao
2   Department of Health Care, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
,
R. Guo
1   Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, Shandong, PR China
› Author Affiliations
Further Information

Publication History

received 10 December 2011

accepted 08 February 2012

Publication Date:
01 March 2012 (online)

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Abstract

The study aimed to compare and evaluate the bioequivalence of a new generic preparation of trospium chloride (CAS NO:10405-02-4) capsule (20 mg, test) and the available import tablet (20 mg , reference) for the requirement of state regulatory criteria in China. A randomized- sequence, 2-period crossover study was conducted in 20 healthy Chinese male volunteers in the fasted state. Blood samples were collected before and 1, 2, 3, 4, 5, 6, 7, 8, 12, 24, 36, 48, 60 h after administration of a single oral dose of 40 mg trospium chloride capsules or tablets, followed by a 7-day washout period. The concentration of trospium chloride was determined by a LC-MS/MS method. Drug And Statistical-Version 2.0 was used to caculate the pharmacokinetics parameters and assess bioequivalence of the two preparations. It was considered bioequivalent if the 90% CIs of the mean ratios (test: reference) for Cmax, AUC0–t and AUC0–∞ were within the range from 80% to 125%, respectively. The main pharmacokinetics parameters of test and reference were as follows: t1/2 was (15.11±3.24) h and (16.00±3.96) h; Tmax was (4.0±1.2) h and (4.1±0.9) h; Cmax was (3.76±1.87) ng·mL − 1 and (3.70±1.89) ng·mL − 1; AUC0–t was (33.51±14.39) ng·mL − 1·h and (33.33±14.88) ng·mL − 1·h, and the AUC0–∞ was (35.20±14.88) ng·mL − 1·h and (35.16±15.17) ng·mL − 1·h. The ratios (test: reference) for Cmax, AUC0–t, and AUC0–∞ were 94.0%~111.7%, 96.4%~106.8%, and 96.1%~105.3%, respectively. No significant differences in pharmacokinetic parameters were found between preparations and periods (p>0.05). No obvious adverse events were monitored throughout the study based on clinical parameters and patient reports.

Key words

trospium chloride - LC-MS/MS - pharmacokinetic - bioequivalence
 

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