PMID- 38226890
OWN - NLM
STAT- MEDLINE
DCOM- 20240405
LR  - 20240416
IS  - 2160-7648 (Electronic)
IS  - 2160-763X (Linking)
VI  - 13
IP  - 4
DP  - 2024 Apr
TI  - Pharmacokinetics, Bioequivalence, and Safety Evaluation of Two Oral Formulations 
      of Calcium Dobesilate Capsules in Healthy Chinese Volunteers Under Fasting and 
      Fed Conditions.
PG  - 360-366
LID - 10.1002/cpdd.1376 [doi]
AB  - To determine the pharmacokinetics (PK), safety, and bioequivalence profiles of 
      0.5-g calcium dobesilate capsules in both fasting and fed states for the test 
      drug and reference drug. 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: CTR202000268-01). The fasting and 
      fed studies, both involving 24 subjects, were conducted. A single dosage of 
      either the reference or the test preparation was given to each eligible subject 
      in a 1:1 ratio, followed by a 7-day rest interval before the administration of 
      the alternative formulation. After taking the capsules, plasma samples were taken 
      for 48 hours, and using liquid chromatography-tandem mass spectrometry, the 
      calcium dobesilate level was determined. The PK parameters evaluated in the study 
      included the maximum serum concentration (C(max)), area under the plasma 
      concentration-time curve (AUC) from time 0 to the last quantifiable 
      concentration, AUC from time 0 to infinity, half-life, time to C(max), and 
      terminal elimination rate constant. In addition, the safety evaluation 
      encompassed monitoring fluctuations in vitals (temperature, pulse, and blood 
      pressure) and laboratory tests (urinalysis, hepatic function, blood biochemistry, 
      and hematology), as well as recording the emergence of adverse events (AEs). The 
      geometric mean ratio (GMR) of the test/reference medications was used to assess 
      bioequivalence by determining if the 90% confidence intervals of the GMR fell 
      within the predefined range of 80%-125%. AEs were assessed as safety end points. 
      The study included 48 healthy Chinese volunteers (with n = 24 each for the 
      fasting and the fed conditions), and no subjects dropped out for any reason. The 
      differences in the PK metrics for the test and reference drugs for both 
      conditions were insignificant (P > .05). For bioequivalence, irrespective of 
      whether the food was consumed or not, the range of the 90% confidence intervals 
      of the GMR for C(max), AUC from time 0 to the last quantifiable concentration, 
      and AUC from time 0 to infinity was between 80% and 125%. In the experiment, no 
      serious AEs were recorded. Our findings revealed that the calcium dobesilate 
      capsules used as the reference and the test drugs were both bioequivalent. 
      Irrespective of whether the healthy Chinese volunteers consumed food or not, the 
      PK and safety profiles were comparable.
CI  - (c) 2024, The American College of Clinical Pharmacology.
FAU - Wang, Yanrong
AU  - Wang Y
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Liu, Ying
AU  - Liu Y
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Tang, Liyuan
AU  - Tang L
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Gao, Jie
AU  - Gao J
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Li, Hongmin
AU  - Li H
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Dai, Xinya
AU  - Dai X
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Chen, Ran
AU  - Chen R
AD  - GCP Office of Cangzhou Central Hospital, Cangzhou, Hebei, People's Republic of 
      China.
FAU - Wang, Fengqin
AU  - Wang F
AD  - Research Center of Hainan Linheng Pharmaceutical Co. LTD, Haikou, Hainan, 
      People's Republic of China.
LA  - eng
GR  - Hainan Linheng Pharmaceutical Co. LTD/
GR  - 20200340/Hebei Province medical science/
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20240116
PL  - United States
TA  - Clin Pharmacol Drug Dev
JT  - Clinical pharmacology in drug development
JID - 101572899
RN  - 5921X1560Q (Calcium Dobesilate)
SB  - IM
MH  - Humans
MH  - Area Under Curve
MH  - Biological Availability
MH  - *Calcium Dobesilate
MH  - China
MH  - Cross-Over Studies
MH  - Fasting
MH  - Therapeutic Equivalency
MH  - Volunteers
MH  - East Asian People
OTO - NOTNLM
OT  - bioequivalence
OT  - calcium dobesilate capsules
OT  - pharmacokinetics
OT  - safety
EDAT- 2024/01/16 13:42
MHDA- 2024/04/05 06:44
CRDT- 2024/01/16 09:53
PHST- 2023/09/05 00:00 [received]
PHST- 2023/12/19 00:00 [accepted]
PHST- 2024/04/05 06:44 [medline]
PHST- 2024/01/16 13:42 [pubmed]
PHST- 2024/01/16 09:53 [entrez]
AID - 10.1002/cpdd.1376 [doi]
PST - ppublish
SO  - Clin Pharmacol Drug Dev. 2024 Apr;13(4):360-366. doi: 10.1002/cpdd.1376. Epub 
      2024 Jan 16.