(2015) An insitu crosslinked compression coat comprised of pectin and calcium chloride for colon-specific delivery of indomethacin, Drug Delivery, 22:3, 298-305, DOI: 10.3109/10717544.2013
AbstractThe 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 t max and apparent t 1/2 , as well as a decreased C max and AUC 0-t , compared with the core tablet counterpart. Evaluation with g-scintigraphy verified colonspecific delivery of the compression-coated tablet. In conclusion, the P/Ca in situ crosslinking system worked well for colon-specific drug delivery.