|
KMID : 0370019990130000005
|
|
Chung-Ang Journal of Pharmacal Sciences
1999 Volume.13 No. 0 p.5 ~ p.15
|
|
|
Analytic Conditions of Lovatatin Acid in Plasma and Bioequivalence of Lovastatin Preparations
|
|
|
|
|
Abstract
|
|
|
|
Lovastatin acid (LVA), a lovastatin(LV) hydroxy acid biotransformed by liver microsomal CYP3A, is a specific and potent inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate limiting enzyme in the de novo synthesis of cholesterol. A fast, simple and accurate method for determining of LVA in human plasma has been developed and validated. This HPLC method involves column switching system with UV detection. The procedure was linear from 0.5 to 50ng/㎖ for LVA. The interday and intraday validations for coefficient of variation(CV(%)) and relative error(RE) were less than 10%. Based on this analysis methods, bioequivalence of two lovastatin tablets, the Mevacor^TM(Choong-Wae Phrmaceutival Co., Ltd.) and the Lovarex^TM(Sam-A Pharmaceutical Co., Ltd.), was evaluated according to the guideline of KFDA. Sixteen normal male volunteers (age 21∼27 years old) were divided into two groups and a randomized 2×2 cross-over study was employed. After oral administrations of four lovastatin tablets(80㎎ of lovastatin), blood sample was taken at predetermined time intervals and the concentration of lovastatin acid in plasma was determined by HPLC with column switching system. The pharmacokinetic parameters(AUCo→_12h, C_max, T_max) were calculated and ANOVA was introduced for the statistical analysis of parameters. The results showed that the differences in AUCo→_12h, C_max, and T_max between two tablets were 0.17%, -10.14% and 9.67%, respectively. The power (1-β) for AUCo→_12h, C_max, and T_max were 89.6%, 93.1% and 89.1%, respectively. Detectable differences(Δ) and confidence intervals were all less than ±20%. All of these parameters met the criteria of KFDA guidelines for bioequivalence, indicating that Lovarex^TM tablet is bioequivalent to Mevacor^TM tablet.
|
|
|
KEYWORD
|
|
|
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|
|
|