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Article

Influence of In Situ Calcium Pectinate Coating on Metoprolol Tartrate Pellets for Controlled Release and Colon-Specific Drug Delivery

Department of Manufacturing Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
*
Author to whom correspondence should be addressed.
Ampol Mitrevej passed away.
Academic Editor: M. Violante De Paz
Pharmaceutics 2022, 14(5), 1061; https://doi.org/10.3390/pharmaceutics14051061
Received: 13 April 2022 / Revised: 9 May 2022 / Accepted: 12 May 2022 / Published: 15 May 2022
(This article belongs to the Special Issue Advances in Gastro-Retentive Drug Delivery Systems)
In situ calcium pectinate-coated pellets were proposed by applying an alternate coating method to drug-layered pellets to achieve colon-specific drug delivery. Solution layering of metroprolol tartrate, a water-soluble model drug, on inert core pellets was achieved using a centrifugal granulator followed by successive alternate coating with pectin and calcium chloride layers using a fluidized bed bottom spray coater. The effect of the coating sequence on the drug release was studied in phosphate buffer pH 7.4 and 6.0. These test conditions were used to mimic the physiological environments in the distal small intestine and proximal colon, respectively. The results showed that the in situ calcium pectinate layer was successfully generated from the alternate coating of pectin and calcium layers after hydration to form gelation, which was able to control the drug release. The coating sequence played an important role in the drug release. The outermost pectin layer tended to retard the drug release whilst the outermost calcium layer accelerated the release regardless of the number of coating layers. These findings indicate that the release behavior followed the Higuchi model, with the drug release from the coated pellets described by a diffusion control mechanism. It is concluded that the success of the in situ calcium pectinate-coated pellets in controlling the drug release is due to the coating of the outermost layer with pectin and the maintenance of the optimum ratio of calcium to pectin upon hydration. View Full-Text
Keywords: in situ calcium pectinate; pellets; pectin; calcium chloride; alternate coating; fluidized bed in situ calcium pectinate; pellets; pectin; calcium chloride; alternate coating; fluidized bed
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MDPI and ACS Style

Wanasawas, P.; Mitrevej, A.; Sinchaipanid, N. Influence of In Situ Calcium Pectinate Coating on Metoprolol Tartrate Pellets for Controlled Release and Colon-Specific Drug Delivery. Pharmaceutics 2022, 14, 1061. https://doi.org/10.3390/pharmaceutics14051061

AMA Style

Wanasawas P, Mitrevej A, Sinchaipanid N. Influence of In Situ Calcium Pectinate Coating on Metoprolol Tartrate Pellets for Controlled Release and Colon-Specific Drug Delivery. Pharmaceutics. 2022; 14(5):1061. https://doi.org/10.3390/pharmaceutics14051061

Chicago/Turabian Style

Wanasawas, Pimphaka, Ampol Mitrevej, and Nuttanan Sinchaipanid. 2022. "Influence of In Situ Calcium Pectinate Coating on Metoprolol Tartrate Pellets for Controlled Release and Colon-Specific Drug Delivery" Pharmaceutics 14, no. 5: 1061. https://doi.org/10.3390/pharmaceutics14051061

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