Development of a Bionic System for the Simultaneous Prediction of the Release/Absorption Characteristics of Enteric-Coated Formulations

• Published in: Pharmaceutical research 2013-02, Vol.30 (2), p.596-605
• Main Authors: Liu, Weijun, He, Xin, Li, Ziqiang, Gao, Xiumei, Ma, Yetao, Xun, Mingjin, Liu, Changxiao
• Format: Article
• Language: English
• Subjects: Animals; Anti-Ulcer Agents - administration & dosage; Anti-Ulcer Agents - chemistry; Anti-Ulcer Agents - pharmacokinetics; Bioavailability; Biochemistry; Biological and medical sciences; Biomedical and Life Sciences; Biomedical Engineering and Bioengineering; Biomedicine; Chemistry, Pharmaceutical - instrumentation; Dissolution; Dogs; Drug delivery systems; Equipment Design; General pharmacology; Hydrogen-Ion Concentration; Linear Models; Male; Medical Law; Medical sciences; Models, Biological; Omeprazole - administration & dosage; Omeprazole - chemistry; Omeprazole - pharmacokinetics; Pharmaceutical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Pharmacology/Toxicology; Pharmacy; Rats; Research Paper; Solubility; Tablets, Enteric-Coated
• ISSN: 0724-8741; 1573-904X
• DOI: 10.1007/s11095-012-0905-3

ABSTRACT Purpose To develop a new bionic system from an existing drug dissolution/absorption simulating system (DDASS) to simultaneously predict the release and absorption of enteric-coated formulations. Methods In accordance with the pH-dependent characteristics of enteric-coated formulations, the modified DDASS was designed to effectively imitate the pH change process of the formulations' transfer from stomach to intestine in vivo . Omeprazole enteric-coated tablets were chosen as the model drug to verify the rationality and feasibility of the modified DDASS. The correlations between USP I system release and beagle dog absorption, as well as between modified DDASS elution/permeation and beagle dog absorption, were investigated by linear and nonlinear regression analyses, respectively. Results In vitro - in vivo correlation between the modified DDASS elution/permeation method and beagle dog absorption was higher than between the USP I system release and beagle dog absorption in both analytical methods. The ratio of first-order permeation rate constant to first-order release rate constant was consistent with that from modified DDASS. Conclusions The modified DDASS provided more information than the USP I system did in the evaluation of enteric-coated formulations. The proposed bionic system model could serve as a new method for improving drug effectiveness.