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

Kwang-Hee Shin, Ji-Young Jeon, Kyungho Jang, Tae-Eun Kim, Min-Gul Kim, Kwang-Hee Shin, Ji-Young Jeon, Kyungho Jang, Tae-Eun Kim, Min-Gul Kim

Abstract

Purpose: 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.

Subjects and methods: 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).

Results: 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.

Conclusions: The dose-proportional properties of GLA5PR GLARS-NF1 150-450 mg tablets were determined.

Keywords: GABA analog; Korean; gamma-aminobutyric acid analog; maximum concentration; safety evaluation.

Conflict of interest statement

Disclosure The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
Mean plasma concentration-time curves of pregabalin by treatment groups. Note: (A) Linear and (B) log scale.
Figure 2
Figure 2
Box-whiskers-plots of pregabalin. Notes: (A) AUClast/dose and (B) Cmax/dose after oral GLA5PR GLARS-NF1 150, 300, 450, and 600 mg administration. Median is indicated by line in the box. Interquartile range box represents the middle 50% of the data. Whiskers represent ranges of bottom and top 25% of data values excluding outliers. Abbreviations: AUClast, area under the serum concentration-time curve from time zero to the time of the last measured concentration; Cmax, maximum serum concentration.
Figure 3
Figure 3
Regression plot of pregabalin. Note: (A) log(AUClast) and (B) log(Cmax). Abbreviations: AUClast, area under the serum concentration-time curve from time zero to the time of the last measured concentration; Cmax, maximum serum concentration.

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