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Drug Deliv. 2015 May;22(3):298-305. doi: 10.3109/10717544.2013.879965. Epub 2014 Jan 29.

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

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  • 1Key Laboratory of Smart Drug Delivery of Ministry of Education and PLA, School of Pharmacy, Fudan University , Shanghai , China and.

Abstract

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 in situ 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 (99m)Tc labeling. The in situ 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 tmax and apparent t1/2, as well as a decreased Cmax and AUC0-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 in situ crosslinking system worked well for colon-specific drug delivery.

KEYWORDS:

Calcium chloride; colon; compression coated; in situ crosslinking; indomethacin; pectin; tablet

[PubMed - indexed for MEDLINE]
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