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Bioequivalence of Tylicol ER Tablet to Tylenol® ER Tablet (Acetaminophen 650 mg)

타이레놀이알서방정(아세트아미노핀 650 mg)에 대한 타이리콜이알정의 생물학적동등성

  • Kang, Hyun-Ah (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University) ;
  • Kim, Dong-Ho (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University) ;
  • Park, Sun-Ae (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University) ;
  • Yun, Hwa (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University,Clinical Trial Center, Chonnam National University Hospital) ;
  • Kim, Kyung-Ran (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University) ;
  • Park, Eun-Ja (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University) ;
  • Cho, Hea-Yeong (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University,Clinical Trial Center, Chonnam National University Hospital) ;
  • Lee, Yong-Bok (Institute of Bioquivalence and, Bridging Study, College of Pharmacy, Chonnam National University,Clinical Trial Center, Chonnam National University Hospital)
  • 강현아 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소) ;
  • 김동호 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소) ;
  • 박선애 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소) ;
  • 윤화 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소,전남대학교 병원 임상시험센터) ;
  • 김경란 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소) ;
  • 박은자 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소) ;
  • 조혜영 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소,전남대학교 병원 임상시험센터) ;
  • 이용복 (전남대학교 약학대학 부속 생물학적동등성 및 가교시험연구소,전남대학교 병원 임상시험센터)
  • Published : 2006.06.21

Abstract

Acetaminophen (paracetamol), a para-aminophenol derivative, has analgesic and antipyretic properties and weak anti-inflammatory activity. The purpose of the present study was to evaluate the bioequivalence of two acetaminophen tablets, $Tylenol^{\circledR}$ ER (Janssen Korea Ltd.) and Tylicol ER (Hana Pharmaceutical Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of acetaminophen from the two acetaminophen formulations in vitro was tested using KP VIll Apparatus II method with pH 1.2 buffer solution. Twenty six healthy male subjects, $22.8{\pm}1.99$ years in age and $65.6{\pm}8.03$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single tablet containing 650 mg as acetaminophen was orally administered, blood samples were taken at predetermined time intervals and the concentrations of acetaminophen in serum were determined using HPLC with UV detector. The dissolution profiles of two formulations were similar in pH 1.2 buffer solution. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Tylenol^{\circledR}$ ER, were 2.84, 1.89 and -1.36% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log $0.987{\sim}log$ 1.08 and log $0.944{\sim}log$ 1.17 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Tylicol ER tablet was bioequivalent to $Tylenol^{\circledR}$ ER tablet.

Keywords

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