Studies on pulsatile release tablets of diltiazem hydrochloride in explosion way.
- Author:
Tian-yuan FAN
1
;
Shu-li WEI
;
Wen-wei YAN
;
Wu-xiao DING
Author Information
- Publication Type:Journal Article
- MeSH: Adult; Antihypertensive Agents; administration & dosage; pharmacokinetics; Biological Availability; Chemistry, Pharmaceutical; Delayed-Action Preparations; Diltiazem; administration & dosage; pharmacokinetics; Drug Delivery Systems; Fluorocarbons; chemistry; Humans; Male; Polymethacrylic Acids; chemistry
- From: Acta Pharmaceutica Sinica 2002;37(3):221-225
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo investigate the preparation of pulsatile release tablets, the release of the drug in vitro and the pharmacokinetics in vivo.
METHODSDiltiazem hydrochloride (DIL) was used as model drug. The pulsatile release tablets were prepared by film-coated method using ethylcellulose and Eudragit L. The effect of formulation on pulsatile release of diltiazem hydrochloride was investigated under release rate test. The mechanism of pulsatile release of drug was proved by the test of water-uptake. The pharmacokinetic and bioavailability study in eight human subjects was performed by HPLC method.
RESULTSThe release of diltiazem hydrochloride effected by the formulation of the core tablets and the composition and thickness of the coating film. In vitro, the delayed-release time T10 was 4.4 h, the maximum release time Trm was 8.0 h and the pulsed-release time Trm-10 was 3.6 h. In vivo, the delayed-release time Tlag was 4.9 h, the peak time was 8.0 h and the pulsed-release time was 3.1 h. The relative bioavailability was 105%.
CONCLUSIONThe release of drug from pulsatile release tablets of diltiazem hydrochloride was shown to be in pulsed way both in vitro and in vivo.
