An in situ crosslinked compression coat comprised of pectin and calcium chloride for colon-specific delivery of indomethacin. (May 2015)

• Record Type: Journal Article
• Authors: Wei, Xiuli; Lu, Yi; Qi, Jianping; Wu, Baojian; Chen, Jian; Xu, Huinan; Wu, Wei
• Is Part Of: Drug delivery. Volume 22:Number 3(2015:Apr.)
• Page Start: 298
• Page End: 305
• Publication Date: 2015-05
• Subjects: Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.3109/10717544.2013.879965
• Languages: English
• ISSNs: 1071-7544

Abstract

<abstract> <title>Abstract</title> <p>The use of pectin for colon-specific drug delivery has been extensively investigated; however, when used alone, pectin is often compromised due to its high solubility. This study explored the feasibility of using an <italic>in situ</italic> compression-coated crosslinking system, composed of pectin and calcium chloride, for colon-specific drug delivery. A pectin/calcium chloride (P/Ca) coating was compressed onto a core tablet. The colon specificity of the compression-coated tablet was verified by dissolution, pharmacokinetics and scintigraphy with ^99mTc labeling. The <italic>in situ</italic> pectin and calcium chloride gel slowed the release of indomethacin. The lag time varied between 3 h and 7 h depending on the amount of calcium chloride and the coating weight. Pectinase triggered the release of indomethacin from the compression-coated tablet, which was then accelerated by the calcium chloride in the coating layer. The compression-coated tablet had a prolonged <italic>t</italic>_max and apparent <italic>t</italic>_1/2, as well as a decreased <italic>C</italic>_max and <italic>AUC</italic>_0–t, compared with the core tablet counterpart. Evaluation with γ-scintigraphy verified colon-specific delivery of the compression-coated tablet. In conclusion, the P/Ca <italic>in situ</italic> crosslinking system worked well for colon-specific drug delivery.</p> </abstract>