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Bioequivalence of a Generic Nateglinide Formulation in Healthy Chinese Volunteers under Fasting and Fed Conditions: A Randomized, Open-Label, Double-Cycle, Double-Crossover Study.
- Source :
-
Pharmacology [Pharmacology] 2021; Vol. 106 (7-8), pp. 418-425. Date of Electronic Publication: 2021 Apr 16. - Publication Year :
- 2021
-
Abstract
- Introduction: Nateglinide or N-(trans-4-isopropylcyclohexyl-1-carbonyl)-D-phenylalanine is a drug with a rapid hypoglycemic effect that is mainly used in the treatment of type 2 diabetes. Very few studies have assessed bioequivalence based on feeding status. This study aimed to assess the pharmacokinetic bioequivalence and safety of nateglinide-containing tablets (0.12 g) in healthy Chinese volunteers under fasting and fed conditions.<br />Methods: The studies were performed in 2017-2018 in the Phase I Clinical Trial Ward of the Affiliated Hospital of Liaoning University of Traditional Chinese Medicine, China. Eligible Chinese volunteers received a single 0.12-g dose of the test or reference formulation, followed by a 7-day washout period and administration of the alternate formulation. Blood samples were collected at various time intervals, and plasma nateglinide concentrations were analyzed by liquid chromatography-tandem mass spectrometry. Then, the adverse events, laboratory test results, vital signs, and physical exam findings were compared between the 2 groups.<br />Results: The ratios of the geometric means of Cmax, AUC0-t, and AUC0-inf of the tested to reference preparations under fasting conditions were 105.03% (90% confidence interval [CI]: 99.53-110.83%), 104.02% (90% CI: 101.37-106.74%), and 104.04% (90% CI: 101.38-106.77%), respectively. The same ratios under fed conditions were 96.55% (90% CI: 85.80-108.65%), 103.08% (90% CI: 100.07-106.18%), and 103.07% (90% CI: 100.21-106.01%), respectively. The 90% CI values for Cmax, AUC0-t, and AUC0-inf fell within the accepted range of bioequivalence (80.00-125.0%). Common adverse events included hypoglycemia, heart rate increase, palpitation, sweating, dizziness, and diarrhea.<br />Conclusions: The test formulation (0.12 g) met the CFDA's regulatory definition for bioequivalence to the reference formulation. Both formulations were well tolerated by healthy Chinese subjects.<br />Trial Registration: This trial has been registered in the Chinese Clinical trial registry (ChiCTR2000030694), March 10, 2020.<br /> (© 2021 S. Karger AG, Basel.)
- Subjects :
- Adolescent
Adult
Area Under Curve
Asian People
Chromatography, Liquid
Cross-Over Studies
Drugs, Generic administration & dosage
Drugs, Generic adverse effects
Fasting
Female
Food-Drug Interactions
Humans
Hypoglycemic Agents administration & dosage
Hypoglycemic Agents adverse effects
Male
Middle Aged
Nateglinide administration & dosage
Nateglinide adverse effects
Tablets
Tandem Mass Spectrometry
Therapeutic Equivalency
Young Adult
Drugs, Generic pharmacokinetics
Hypoglycemic Agents pharmacokinetics
Nateglinide pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1423-0313
- Volume :
- 106
- Issue :
- 7-8
- Database :
- MEDLINE
- Journal :
- Pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 33866315
- Full Text :
- https://doi.org/10.1159/000512851