Pharmacokinetic and bioequivalence study of itopride HCl in healthy volunteers

Kyung Jin Cho, Wonkyung Cho, Kwang Ho Cha, Junsung Park, Min Soo Kim, Jeong Soo Kim, Sung Joo Hwang

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

In the present study two different formulations containing 50 mg itopride HCl (N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide HCl, CAS 122898- 67-3) were compared in 28 healthy male volunteers in order to compare the bioavailability and prove the bioequivalence. The study was performed in an open, single dose randomized, 2-sequence, crossover design in 28 healthy male volunteers with a one-week washout period. Blood samples for pharmacokinetic profiling were drawn at selected times during 24 h. The serumconcentrations of itopride HCl were determined using a specific and sensitive HPLC method with fluorescence detection. The detection limit of itopride HCl was 5 ng/ml and no endogenous compounds were found to interfere with analysis. The mean AUC 0→24h , AUC 0→∞ , C max , T max and T 1/2 were 865.28 ng · h/ml, 873.04 ng · h/ml, 303.72 ng/ml, 0.75 h, and 2.95 h, respectively, for the test formulations, and 833.00 ng · h/ml, 830.97 ng · h/ml, 268.01 ng/ml, 0.78 h, and 2.83 h, respectively, for the reference formulation. Both primary target parameters AUC 0→∞ and C max were log-transformed and tested parametrically by analysis of variance (ANOVA). 90% confidence intervals of AUC 0→∞ and C max were 100.57%-109.56% and 105.46%-121.18%, respectively, and were in the range of acceptable limits of bioequivalence (80-125%). Based on these results, the two formulations of itopride HCl are considered to be bioequivalent.

Original languageEnglish
Pages (from-to)137-140
Number of pages4
JournalArzneimittel-Forschung/Drug Research
Volume60
Issue number3
Publication statusPublished - 2010 Apr 15

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Therapeutic Equivalency
Area Under Curve
Healthy Volunteers
Pharmacokinetics
Cross-Over Studies
Biological Availability
Limit of Detection
Analysis of Variance
Fluorescence
High Pressure Liquid Chromatography
Confidence Intervals
itopride

All Science Journal Classification (ASJC) codes

  • Drug Discovery

Cite this

Cho, K. J., Cho, W., Cha, K. H., Park, J., Kim, M. S., Kim, J. S., & Hwang, S. J. (2010). Pharmacokinetic and bioequivalence study of itopride HCl in healthy volunteers. Arzneimittel-Forschung/Drug Research, 60(3), 137-140.
Cho, Kyung Jin ; Cho, Wonkyung ; Cha, Kwang Ho ; Park, Junsung ; Kim, Min Soo ; Kim, Jeong Soo ; Hwang, Sung Joo. / Pharmacokinetic and bioequivalence study of itopride HCl in healthy volunteers. In: Arzneimittel-Forschung/Drug Research. 2010 ; Vol. 60, No. 3. pp. 137-140.
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abstract = "In the present study two different formulations containing 50 mg itopride HCl (N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide HCl, CAS 122898- 67-3) were compared in 28 healthy male volunteers in order to compare the bioavailability and prove the bioequivalence. The study was performed in an open, single dose randomized, 2-sequence, crossover design in 28 healthy male volunteers with a one-week washout period. Blood samples for pharmacokinetic profiling were drawn at selected times during 24 h. The serumconcentrations of itopride HCl were determined using a specific and sensitive HPLC method with fluorescence detection. The detection limit of itopride HCl was 5 ng/ml and no endogenous compounds were found to interfere with analysis. The mean AUC 0→24h , AUC 0→∞ , C max , T max and T 1/2 were 865.28 ng · h/ml, 873.04 ng · h/ml, 303.72 ng/ml, 0.75 h, and 2.95 h, respectively, for the test formulations, and 833.00 ng · h/ml, 830.97 ng · h/ml, 268.01 ng/ml, 0.78 h, and 2.83 h, respectively, for the reference formulation. Both primary target parameters AUC 0→∞ and C max were log-transformed and tested parametrically by analysis of variance (ANOVA). 90{\%} confidence intervals of AUC 0→∞ and C max were 100.57{\%}-109.56{\%} and 105.46{\%}-121.18{\%}, respectively, and were in the range of acceptable limits of bioequivalence (80-125{\%}). Based on these results, the two formulations of itopride HCl are considered to be bioequivalent.",
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Cho, KJ, Cho, W, Cha, KH, Park, J, Kim, MS, Kim, JS & Hwang, SJ 2010, 'Pharmacokinetic and bioequivalence study of itopride HCl in healthy volunteers', Arzneimittel-Forschung/Drug Research, vol. 60, no. 3, pp. 137-140.

Pharmacokinetic and bioequivalence study of itopride HCl in healthy volunteers. / Cho, Kyung Jin; Cho, Wonkyung; Cha, Kwang Ho; Park, Junsung; Kim, Min Soo; Kim, Jeong Soo; Hwang, Sung Joo.

In: Arzneimittel-Forschung/Drug Research, Vol. 60, No. 3, 15.04.2010, p. 137-140.

Research output: Contribution to journalArticle

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AU - Cho, Kyung Jin

AU - Cho, Wonkyung

AU - Cha, Kwang Ho

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AU - Kim, Jeong Soo

AU - Hwang, Sung Joo

PY - 2010/4/15

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Cho KJ, Cho W, Cha KH, Park J, Kim MS, Kim JS et al. Pharmacokinetic and bioequivalence study of itopride HCl in healthy volunteers. Arzneimittel-Forschung/Drug Research. 2010 Apr 15;60(3):137-140.