J Korean Soc Clin Pharmacol Ther.  2013 Dec;21(2):120-129. 10.12793/jkscpt.2013.21.2.120.

Bioequivalence of HCP1104, a New Fixed Dose Combination Drug and Co-administration of Eperisone 50 mg and Aceclofenac 100 mg: A Partial Replicated Crossover Study Design to Estimate the Pharmacokinetics of Highly Variable Drugs

• Kim MJ
• Kim YH
• Choi HY
• Jeon HS
• Noh YH
• Lim HS
• Bae KS

• KMID: 2203225
• DOI: http://doi.org/10.12793/jkscpt.2013.21.2.120

Abstract

BACKGROUND
This clinical study was conducted to compare pharmacokinetics of eperisone and aceclofenac of HCP1104, a new fixed dose combination drug with those in co-administration of eperisone 50 mg and aceclofenac 100 mg. The study used a partial replicated study design to characterize intra-subject variability of eperisone when co-administrated with aceclofenac.
METHODS
A partial replicated crossover design was employed in 30 subjects. Each subject received a single dose of co-administration of eperisone 50 mg and aceclofenac 100 mg on two occasions and a single dose of 1 capsule of HCP1104. Blood samples were obtained for 24 hrs after dosing, and plasma was assayed for eperisone and aceclofenac by Liquid chromatography-electrospray ionization-mass spectrometry.
RESULTS
Using an average bioequivalence criterion, the 90 % confidence limits for Ln-transformed Cmax and AUClast for aceclofenac fell wihin the acceptable range of 80 - 125 %. Point estimates of eperisone AUClast and Cmax were 1.0152 and 1.0490, respectively and the 90 % confidence interval for Cmax was 0.8499 - 1.3025. The within-subject coefficient of variation of Cmax for the reference was 50.198 %. Acceptance range for eperisone Cmax based on new bioequivalence guidance for highly variable drugs was extended to 0.6984 - 1.4319.
CONCLUSION
The extent of exposure and rate of absorption of both eperisone and aceclofenac with a single dose of HCP1104 capsule were equivalent to those with co-administration of a marketed eperisone 50 mg tablet and a marketed aceclofenac 100 mg tablet under fasting conditions in healthy adult males.

Keyword

Highly variable drugs; Bioequivalence; Eperisone; Aceclofenac

MeSH Terms

Absorption
Adult
Cross-Over Studies*
Fasting
Humans
Male
Pharmacokinetics*
Plasma
Spectrum Analysis
Therapeutic Equivalency*

Figure

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  Figure 1. Plasma eperisone concentration - time curve (A) and plasma aceclofenac concentration - time curve (B) when administrated eperisone 50 mg with aceclofenac 100 mg or HCP1104 alone. Mean and standard deviation are presented as point and bars, respectively.

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