PHARMACOKINETIC ANALYSIS OF 2 NEW SUSTAINED-RELEASE PRODUCTS OF DILTIAZEM DESIGNED FOR TWICE-DAILY AND ONCE-DAILY TREATMENT

被引:4
|
作者
BIALER, M
HADAD, S
GOLOMB, G
BAREL, S
SAMARA, E
ABUSALACH, O
BERKMAN, N
DANENBERG, HD
BENDAVID, J
CARON, D
KAPLAN, R
TAMIR, A
FRIEDMAN, M
机构
[1] HADASSAH UNIV HOSP,DIV MED,JERUSALEM,ISRAEL
[2] LADY DAVIES CARMEL HOSP,DEPT CARDIOL,HAIFA,ISRAEL
[3] ABIC LTD,PHARMACEUT & CHEM IND,NETANYA,ISRAEL
关键词
DILTIAZEM; SUSTAINED-RELEASE PRODUCTS; PHARMACOKINETIC ANALYSIS; HIGHLY VARIABLE DRUGS; SATURABLE FIRST-PASS EFFECT;
D O I
10.1002/bdd.2510150104
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The pharmacokinetics of two new sustained-release (SR) products of diltiazem, Dilapress 120 mg tablets and Dilapress 240 mg tablets, was analysed and characterized in three different studies, in comparison to the following diltiazem SR formulations: Cardizem Retard, Cardizem SR, and Cardizem CD. Dilapress 120, designated for twice-daily dosing, was found to be bioequivalent to Cardizem SR and to Cardizem Retard with mean (+/- SD) relative bioavailability values of 99 +/- 27% and 113 +/- 38%, respectively. Dilapress 240, designed for once-a-day treatment, was found to have a slower absorption rate than Cardizem SR and its extent of absorption was 56 +/- 19% relative to that of Cardizem SR. However, the bioavailability of Dilapress 240 relative to that of Cardizem CD was 118 +/- 46%, indicating that the bioavailability of Cardizem CD relative to that of Cardizem SR was only 54 +/- 29%. Diltiazem is partially available due to a saturable liver first-pass effect. A high dose of Cardizem SR may partially escape this first-pass effect and, thus, achieve a higher extent of absorption than a slower SR product. Consequently, SR products of diltiazem designed for once-daily treatment may not reach the saturation stage in the liver first-pass effect process that diltiazem is susceptible to. Consequently, a twice-daily SR product of diltiazem cannot serve as a reference for extent of absorption assessments of a once-daily SR product.
引用
收藏
页码:45 / 52
页数:8
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