|
KMID : 0369820010310040289
|
|
Jorunal of Korean Pharmaceutical Sciences
2001 Volume.31 No. 4 p.289 ~ p.295
|
|
|
Bioequivalence of Carvelol Tablet to Dilatrend Tablet ( Carvedilol 25mg )
|
|
조혜영/Cho HY
이문석/박순철/임동구/문재동/이용복/Lee MS/Park SC/Lim DK/Moon JD/Lee YB
|
|
|
Abstract
|
|
|
|
Carvedilol is an antihypertensive and antianginal compound that combines nonselective beta-adrenoceptor blocking and vasodilation properties and is devoid of intrinsic sympathomimetic activity. The purpose of the present study was to evaluate the bioequivalence of two carvedilol tablets, DilatrendTM (Chong Kun Dang Pharmaceutical Co., Ltd.) and CarvelolTM (Dae Won Pharmaceutical Co., Ltd.), according to the prior and revised guidelines of Korea Food and Drug Administration (KFDA). The carvedilol release from the two carvedilol tablets in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution, water and blend of PSB80 into water). Eighteen normal male volunteers, 24.22±1.86 years in age and 64.81±4.56kg in body weight, were divided into two groups and a randomized 2×2 cross-over study was employed. After one tablet containing 25 mg of carvedilol was orally administered, blood was taken at predetermined time intervals and the concentrations of carvedilol in serum were determined using HPLC method with fluorescence detector. The dissolution profiles of two carvedilol tablets were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as AUCt, Cmax and Tmax were calculated and ANOVA test was utilized for the statistical analysis of the parameters using non-transformed and logarithmically transformed AUCt and Cmax. The results showed that the differences in AUCt, Cmax and Tmax between two tablets based on the DilatrendTM were 2.23%, -2.00% and 0.00%, respectively. Minimum detectable differences (Δ) at α=0.05 and 1?β=0.8 were less than 20% (e.g., 13.55% and 17.61% for AUCt and Cmax, respectively). The powers (l?β) at α=0.05, Δ=0.2 for AUCt and Cmax were 98.08% and 88.81%, respectively. The 90% confidence intervals were within ±20 (e.g., ?5.69∼10.16 and ?12.30∼8.30 for AUCt and Cmax, respectively). There were no sequence effect between two tablets in logarithmically transformed AUCt and Cmax. The 90% confidence intervals using logarithmically transformed were within the acceptance range of log(0.8) to log(1.25) (e.g., 0.95∼1.11 and 0.89∼1.09 for AUCt and Cmax, respectively). Two parameters met the criteria of prior and revised KFDA guideline for bioequivalence, indicating that CarvelolTM tablet is bioequivalent to DilatrendTM tablet.
|
|
|
KEYWORD
|
|
|
Carvedilol, DilatrendTM, CarvelolTM, Bioequivalence, HPLC
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|
|