Dose-proportional pharmacokinetic properties of GLA5PR GLARS-NF1 controlled-release pregabalin in healthy Korean volunteers: a randomized, open, single-dose, parallel study

• Published in: Drug design, development and therapy Vol. 12; pp. 3449 - 3457
• Main Authors: Shin, Kwang-Hee, Jeon, Ji-Young, Jang, Kyungho, Kim, Tae-Eun, Kim, Min-Gul
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 2018; Taylor & Francis Ltd; Dove Medical Press
• Subjects: Adult; Analysis; Body Mass Index; Chromatography; Clinical medicine; Clinical trials; Controlled release; Convulsions & seizures; Dosage; Dosage and administration; Dose-Response Relationship, Drug; Drug dosages; FDA approval; Fibromyalgia; GABA; Gamma-aminobutyric acid (GABA) analog; Gender differences; Healthy Volunteers; Hospitals; Humans; Labels; Liquid chromatography; Male; Mass spectrometry; Mass spectroscopy; maximum concentration; Middle Aged; Original Research; Pain; Pharmacokinetics; Pharmacology; Pregabalin; Pregabalin - administration & dosage; Pregabalin - blood; Pregabalin - pharmacokinetics; Randomization; Republic of Korea; Safety; safety evaluation Korean; Spectroscopy; Structure-Activity Relationship; Tablets; Tablets - administration & dosage; Tablets - chemistry; Young Adult; Republic of Korea; New York; United States > US; South Korea; Korean; GABA analog; safety evaluation; maximum concentration; gamma-aminobutyric acid analog
• ISSN: 1177-8881; 1177-8881
• DOI: 10.2147/DDDT.S167668

The aim of this study was to evaluate the dose-proportional pharmacokinetic characteristics of pregabalin following the administration of GLA5PR GLARS-NF1 tablets (150, 300, 450, and 600 mg) in the fed state. An open-label, randomized, single-dose, parallel study was conducted in 40 eligible subjects who were randomly assigned to receive a single 150, 300, 450, or 600 mg dose of GLA5PR GLARS-NF1. Serial blood samples were collected before and after dosing for 36 hours, and plasma concentrations were determined using liquid chromatography-tandem mass spectrometry. Safety profiles were evaluated throughout the study (trial registration number: NCT02327000). Thirty-seven subjects completed the studies. The area under the plasma concentration-time curve up to the last measurable concentration of pregabalin exhibited dose proportionality following administration of GLA5PR GLARS-NF1 tablets from 150 to 600 mg while its maximum plasma concentration showed dose proportionality at a dose range of 150-450 mg. The safety evaluations showed no clinically significant finding after administration of GLA5PR GLARS-NF1 tablets (150, 300, 450, and 600 mg) in the fed state. The dose-proportional properties of GLA5PR GLARS-NF1 150-450 mg tablets were determined.