A pharmacokinetic study of nimesulide in healthy volunteers: Correlation between in vitro dissolution and in vivo absorption

Sheng Fang Su, Jin Ding Huang, Chen Hsi Chou, Chia Wei Chu, Chia Ling Hsiao, Chao Feng Kung, Hwei Ling Lee, Chyun Yu Yang

Research output: Contribution to journalArticle

Abstract

Nimesulide is a non-steroid anti-inflammatory drug (NSAID) used for the treatment of inflammation and pain. Twelve healthy volunteers were recruited for this study to evaluate the bioequivalence of two nimesulide formulations and to further understand the effects of in vitro dissolution on in vivo absorption. After oral administration of 100 mg of nimesulide, maximal concentrations of 4-6 μg/mL were reached after 2-3 hours. A smaller Cmax and longer Tmax was observed in formulation N, but no difference in t1/2 was found between the two formulations. In addition, a 17 % reduction in AUC was observed for formulation N, indicating that the extent and rate of absorption of nimesulide were not equivalent between two formulations. The results from in vitro dissolution tests showed that 80 % of nimesulide was released in 20 minutes from formulation A, while only 60 % was released in 3 hours from formulation N. This study suggests that the differences in dissolution can account for differences in absorption of nimesulide in vivo.

Original languageEnglish
Pages (from-to)281-290
Number of pages10
JournalChinese Pharmaceutical Journal
Volume53
Issue number6
Publication statusPublished - 2001 Dec 1

Fingerprint

nimesulide
Healthy Volunteers
Pharmacokinetics
Therapeutic Equivalency
Area Under Curve
Oral Administration
In Vitro Techniques
Anti-Inflammatory Agents
Inflammation
Pain

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science

Cite this

Su, Sheng Fang ; Huang, Jin Ding ; Chou, Chen Hsi ; Chu, Chia Wei ; Hsiao, Chia Ling ; Kung, Chao Feng ; Lee, Hwei Ling ; Yang, Chyun Yu. / A pharmacokinetic study of nimesulide in healthy volunteers : Correlation between in vitro dissolution and in vivo absorption. In: Chinese Pharmaceutical Journal. 2001 ; Vol. 53, No. 6. pp. 281-290.
@article{09fb34d16b8440c9a3b02b6879be7914,
title = "A pharmacokinetic study of nimesulide in healthy volunteers: Correlation between in vitro dissolution and in vivo absorption",
abstract = "Nimesulide is a non-steroid anti-inflammatory drug (NSAID) used for the treatment of inflammation and pain. Twelve healthy volunteers were recruited for this study to evaluate the bioequivalence of two nimesulide formulations and to further understand the effects of in vitro dissolution on in vivo absorption. After oral administration of 100 mg of nimesulide, maximal concentrations of 4-6 μg/mL were reached after 2-3 hours. A smaller Cmax and longer Tmax was observed in formulation N, but no difference in t1/2 was found between the two formulations. In addition, a 17 {\%} reduction in AUC was observed for formulation N, indicating that the extent and rate of absorption of nimesulide were not equivalent between two formulations. The results from in vitro dissolution tests showed that 80 {\%} of nimesulide was released in 20 minutes from formulation A, while only 60 {\%} was released in 3 hours from formulation N. This study suggests that the differences in dissolution can account for differences in absorption of nimesulide in vivo.",
author = "Su, {Sheng Fang} and Huang, {Jin Ding} and Chou, {Chen Hsi} and Chu, {Chia Wei} and Hsiao, {Chia Ling} and Kung, {Chao Feng} and Lee, {Hwei Ling} and Yang, {Chyun Yu}",
year = "2001",
month = "12",
day = "1",
language = "English",
volume = "53",
pages = "281--290",
journal = "Chinese Pharmaceutical Journal",
issn = "1016-1015",
number = "6",

}

A pharmacokinetic study of nimesulide in healthy volunteers : Correlation between in vitro dissolution and in vivo absorption. / Su, Sheng Fang; Huang, Jin Ding; Chou, Chen Hsi; Chu, Chia Wei; Hsiao, Chia Ling; Kung, Chao Feng; Lee, Hwei Ling; Yang, Chyun Yu.

In: Chinese Pharmaceutical Journal, Vol. 53, No. 6, 01.12.2001, p. 281-290.

Research output: Contribution to journalArticle

TY - JOUR

T1 - A pharmacokinetic study of nimesulide in healthy volunteers

T2 - Correlation between in vitro dissolution and in vivo absorption

AU - Su, Sheng Fang

AU - Huang, Jin Ding

AU - Chou, Chen Hsi

AU - Chu, Chia Wei

AU - Hsiao, Chia Ling

AU - Kung, Chao Feng

AU - Lee, Hwei Ling

AU - Yang, Chyun Yu

PY - 2001/12/1

Y1 - 2001/12/1

N2 - Nimesulide is a non-steroid anti-inflammatory drug (NSAID) used for the treatment of inflammation and pain. Twelve healthy volunteers were recruited for this study to evaluate the bioequivalence of two nimesulide formulations and to further understand the effects of in vitro dissolution on in vivo absorption. After oral administration of 100 mg of nimesulide, maximal concentrations of 4-6 μg/mL were reached after 2-3 hours. A smaller Cmax and longer Tmax was observed in formulation N, but no difference in t1/2 was found between the two formulations. In addition, a 17 % reduction in AUC was observed for formulation N, indicating that the extent and rate of absorption of nimesulide were not equivalent between two formulations. The results from in vitro dissolution tests showed that 80 % of nimesulide was released in 20 minutes from formulation A, while only 60 % was released in 3 hours from formulation N. This study suggests that the differences in dissolution can account for differences in absorption of nimesulide in vivo.

AB - Nimesulide is a non-steroid anti-inflammatory drug (NSAID) used for the treatment of inflammation and pain. Twelve healthy volunteers were recruited for this study to evaluate the bioequivalence of two nimesulide formulations and to further understand the effects of in vitro dissolution on in vivo absorption. After oral administration of 100 mg of nimesulide, maximal concentrations of 4-6 μg/mL were reached after 2-3 hours. A smaller Cmax and longer Tmax was observed in formulation N, but no difference in t1/2 was found between the two formulations. In addition, a 17 % reduction in AUC was observed for formulation N, indicating that the extent and rate of absorption of nimesulide were not equivalent between two formulations. The results from in vitro dissolution tests showed that 80 % of nimesulide was released in 20 minutes from formulation A, while only 60 % was released in 3 hours from formulation N. This study suggests that the differences in dissolution can account for differences in absorption of nimesulide in vivo.

UR - http://www.scopus.com/inward/record.url?scp=30844459696&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=30844459696&partnerID=8YFLogxK

M3 - Article

AN - SCOPUS:30844459696

VL - 53

SP - 281

EP - 290

JO - Chinese Pharmaceutical Journal

JF - Chinese Pharmaceutical Journal

SN - 1016-1015

IS - 6

ER -