PMID- 33364947
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20201231
IS  - 1663-9812 (Print)
IS  - 1663-9812 (Electronic)
IS  - 1663-9812 (Linking)
VI  - 11
DP  - 2020
TI  - Pharmacokinetics and Bioequivalence of Rasagiline Tablets in Chinese Healthy 
      Subjects Under Fasting and Fed Conditions: An Open, Randomized, Single-Dose, 
      Double-Cycle, Two-Sequence, Crossover Trial.
PG  - 571747
LID - 10.3389/fphar.2020.571747 [doi]
LID - 571747
AB  - Objective: This study evaluated the pharmacokinetics, safety, and bioequivalence 
      (BE) of two formulations of rasagiline tablets in healthy Chinese subjects under 
      fasting and fed conditions. Methods: An open, randomized, single-dose, 
      double-cycle, two-sequence, self-crossover pharmacokinetic study in healthy 
      Chinese subjects under fasting and high-fat postprandial conditions was 
      performed. A total of 108 healthy subjects (36 in the fasting group and 72 in the 
      postprandial group) were recruited. In each cycle of the study under both 
      conditions, subjects received a single oral dose of 1 mg of a test or reference 
      preparation of rasagiline tablets (1 mg each). A washout period of 3 days was 
      observed. Blood samples were obtained up to 10 h post-intake. Primary endpoints 
      were the BE of major pharmacokinetic parameters (AUC(0-t) and AUC(0-infinity)) and the 
      maximum observed serum concentration (C(max)). Secondary endpoints were safety 
      parameters. Results: The 90% confidence interval (CI) of the geometric mean ratio 
      (GMR) of the test drug vs. the reference drug for rasagiline was 94.16-105.35% 
      for the AUC(0-t) under fasting conditions and 99.88-107.07% under postprandial 
      conditions. The 90% CIs for the AUC(0-infinity) were 93.55-105.01% and 99.59-107.05% 
      under fasting and postprandial conditions, respectively. The 90% CIs for the 
      C(max) were 88.26-108.46% and 89.54-118.23% under fasting and postprandial 
      conditions, respectively. The 90% CIs for the test/reference AUC ratio and C(max) 
      ratio were within the acceptable range (0.80-1.25) for BE. In this BE study, 
      there were no serious adverse events (AEs). Conclusion: BE between the test and 
      the reference products was established in both fasting and postprandial 
      conditions. The two formulations of rasagiline showed good tolerability and a 
      similar safety profile. Clinical Trial Registration: chinaDrugtrials.org.cn, 
      identifier CTR20181466.
CI  - Copyright (c) 2020 Li, Qi, Bai, Liu, Fan, Tu, Sun, Wang, Qi, Feng, Zhou and Wang.
FAU - Li, Yinjuan
AU  - Li Y
AD  - Department of Phase I Clinical Trail Center, Beijing Shijitan Hospital, Capital 
      Medical University, Beijing, China.
FAU - Qi, Lu
AU  - Qi L
AD  - Department of Phase I Clinical Trail Center, Beijing Shijitan Hospital, Capital 
      Medical University, Beijing, China.
FAU - Bai, Haihong
AU  - Bai H
AD  - Department of Phase I Clinical Trail Center, Beijing Shijitan Hospital, Capital 
      Medical University, Beijing, China.
FAU - Liu, Ying
AU  - Liu Y
AD  - Department of Phase I Clinical Trail Center, Beijing Shijitan Hospital, Capital 
      Medical University, Beijing, China.
FAU - Fan, Rongxia
AU  - Fan R
AD  - Department of Phase I Clinical Trail Center, Beijing Shijitan Hospital, Capital 
      Medical University, Beijing, China.
FAU - Tu, Yongrui
AU  - Tu Y
AD  - Changzhou Siyao Pharmaceuticals Co., Ltd., Jiangsu, China.
FAU - Sun, Yongqiang
AU  - Sun Y
AD  - Changzhou Siyao Pharmaceuticals Co., Ltd., Jiangsu, China.
FAU - Wang, Juxiang
AU  - Wang J
AD  - Changzhou Siyao Pharmaceuticals Co., Ltd., Jiangsu, China.
FAU - Qi, Qi
AU  - Qi Q
AD  - Changzhou Siyao Pharmaceuticals Co., Ltd., Jiangsu, China.
FAU - Feng, Xiaohui
AU  - Feng X
AD  - Changzhou Siyao Pharmaceuticals Co., Ltd., Jiangsu, China.
FAU - Zhou, Da
AU  - Zhou D
AD  - Changzhou Siyao Pharmaceuticals Co., Ltd., Jiangsu, China.
FAU - Wang, Xinghe
AU  - Wang X
AD  - Department of Phase I Clinical Trail Center, Beijing Shijitan Hospital, Capital 
      Medical University, Beijing, China.
LA  - eng
PT  - Clinical Trial
DEP - 20201203
PL  - Switzerland
TA  - Front Pharmacol
JT  - Frontiers in pharmacology
JID - 101548923
PMC - PMC7750811
OTO - NOTNLM
OT  - bioequivalence
OT  - food effect
OT  - highly variable drug
OT  - pharmacokinetic
OT  - rasagiline
COIS- YT, YS, JW, QQ, XF, and DZ were employed by the company Changzhou Siyao 
      Pharmaceuticals Co., Ltd.The remaining authors declare that the research was 
      conducted in the absence of any commercial or financial relationships that could 
      be construed as a potential conflict of interest.The authors declare that this 
      study received funding from Changzhou Siyao Pharmaceuticals Co., Ltd. The funder 
      had the following involvement with the study: study design, decision to publish 
      and preparation of the manuscript.
EDAT- 2020/12/29 06:00
MHDA- 2020/12/29 06:01
PMCR- 2020/12/03
CRDT- 2020/12/28 12:05
PHST- 2020/06/11 00:00 [received]
PHST- 2020/10/26 00:00 [accepted]
PHST- 2020/12/28 12:05 [entrez]
PHST- 2020/12/29 06:00 [pubmed]
PHST- 2020/12/29 06:01 [medline]
PHST- 2020/12/03 00:00 [pmc-release]
AID - 571747 [pii]
AID - 10.3389/fphar.2020.571747 [doi]
PST - epublish
SO  - Front Pharmacol. 2020 Dec 3;11:571747. doi: 10.3389/fphar.2020.571747. 
      eCollection 2020.