PMID- 33727797
OWN - NLM
STAT- MEDLINE
DCOM- 20211011
LR  - 20221207
IS  - 1177-8881 (Electronic)
IS  - 1177-8881 (Linking)
VI  - 15
DP  - 2021
TI  - Pharmacokinetics and Bioequivalence Evaluation of Two Montelukast Sodium Chewable 
      Tablets in Healthy Chinese Volunteers Under Fasted and Fed Conditions.
PG  - 1091-1099
LID - 10.2147/DDDT.S298355 [doi]
AB  - PURPOSE: The aim of this study was to assess and compare the pharmacokinetic (PK) 
      properties and bioequivalence of montelukast sodium chewable tablets prepared by 
      two different manufacturers in healthy Chinese volunteers to obtain adequate PK 
      evidence for the registration approval of the test formulation. PATIENTS AND 
      METHODS: A randomized-sequence, single-dose, open-label, 2-period crossover study 
      was conducted in fasted and fed healthy Chinese volunteers (Chinese Clinical 
      Trials Registry identifier: CTR20182362). Eighteen subjects each were selected 
      for a fasted study and a fed study. Eligible participants were randomly assigned 
      in a 1:1 ratio to receive a single dose of the reference formulation or the test 
      formulation, followed by a 5-day washout period and the administration of the 
      alternate formulation. Plasma samples were collected over a 24-hour period 
      following tablet administration and analyzed for montelukast contents by 
      high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). The 
      PK parameters, such as maximum serum concentration (C(max)), area under the curve 
      (AUC) from t = 0 to the last quantifiable concentration (AUC(0-t)), AUC from t = 
      0 to infinity (AUC(0-infinity)), half-life (t(1⁄2)), time to C(max) (T(max)), and 
      terminal elimination rate constant (lambda(z)), were evaluated. The safety assessment 
      included changes in vital signs (blood pressure, pulse, and temperature) or 
      laboratory tests (hematology, blood biochemistry, hepatic function, and 
      urinalysis) and the incidence of adverse events (AEs). RESULTS: The geometric 
      mean ratios (GMRs) between the two formulations for the primary pharmacokinetic 
      parameters (C(max), AUC(0-24), and AUC (0-infinity)) and the corresponding 90% 
      confidence intervals (Cis) were all within the range of 80.00-125.00% for both 
      the fasting and fed states. The safety profiles for both treatments were 
      comparable. CONCLUSION: The PK analysis revealed that the test and reference 
      formulations of montelukast sodium chewable tablets were bioequivalent and 
      well-tolerated by healthy Chinese subjects.
CI  - (c) 2021 Li et al.
FAU - Li, Weihong
AU  - Li W
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, 061000, People's 
      Republic of China.
FAU - Wang, Yanrong
AU  - Wang Y
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, 061000, People's 
      Republic of China.
FAU - Pei, Yingzi
AU  - Pei Y
AD  - Research Center of Beijing Fuyuan Pharmaceutical Co., Ltd. (Formerly Beijing 
      Wansheng Pharmaceutical Co., Ltd.), Beijing, 101113, People's Republic of China.
FAU - Xia, Yue
AU  - Xia Y
AD  - Research Center of Beijing Fuyuan Pharmaceutical Co., Ltd. (Formerly Beijing 
      Wansheng Pharmaceutical Co., Ltd.), Beijing, 101113, People's Republic of China.
LA  - eng
PT  - Clinical Trial, Phase I
PT  - Journal Article
PT  - Randomized Controlled Trial
DEP - 20210309
PL  - New Zealand
TA  - Drug Des Devel Ther
JT  - Drug design, development and therapy
JID - 101475745
RN  - 0 (Acetates)
RN  - 0 (Cyclopropanes)
RN  - 0 (Quinolines)
RN  - 0 (Sulfides)
RN  - 0 (Tablets)
RN  - MHM278SD3E (montelukast)
SB  - IM
MH  - Acetates/administration & dosage/blood/*pharmacokinetics
MH  - Administration, Oral
MH  - Adolescent
MH  - Adult
MH  - Asian People
MH  - Cross-Over Studies
MH  - Cyclopropanes/administration & dosage/blood/*pharmacokinetics
MH  - Drug Compounding
MH  - *Fasting
MH  - Female
MH  - Healthy Volunteers
MH  - Humans
MH  - Male
MH  - Middle Aged
MH  - Quinolines/administration & dosage/blood/*pharmacokinetics
MH  - Sulfides/administration & dosage/blood/*pharmacokinetics
MH  - Tablets
MH  - Therapeutic Equivalency
MH  - Young Adult
PMC - PMC7955749
OTO - NOTNLM
OT  - HPLC-MS/MS
OT  - adverse events
OT  - bioequivalence
OT  - montelukast sodium
OT  - pharmacokinetic profile
COIS- Yingzi Pei and Xia Yue are affiliated with Beijing Fuyuan Pharmaceutical Co., 
      Ltd. (formerly Beijing Wansheng Pharmaceutical Co., Ltd.). The authors report no 
      other conflicts of interest in this work.
EDAT- 2021/03/18 06:00
MHDA- 2021/10/12 06:00
PMCR- 2021/03/09
CRDT- 2021/03/17 06:44
PHST- 2020/12/24 00:00 [received]
PHST- 2021/02/23 00:00 [accepted]
PHST- 2021/03/17 06:44 [entrez]
PHST- 2021/03/18 06:00 [pubmed]
PHST- 2021/10/12 06:00 [medline]
PHST- 2021/03/09 00:00 [pmc-release]
AID - 298355 [pii]
AID - 10.2147/DDDT.S298355 [doi]
PST - epublish
SO  - Drug Des Devel Ther. 2021 Mar 9;15:1091-1099. doi: 10.2147/DDDT.S298355. 
      eCollection 2021.