title: A combination of pH-sensitive caplet coatings may be an effective noninvasive strategy to deliver bioactive substances, nutrients, or their precursors to the colon.
abstract: We hypothesize that bacterially synthesized nutrients in the large intestine may significantly influence the nutritional status of humans and, specifically, that of the colonocytes. In vivo research with human subjects in this area has been extremely limited because of the absence of a noninvasive means to quantitatively deliver test doses of nutrients, or their precursors, to the colon. The purpose of this study was to design and test the effectiveness of a pH-dependent coating in delivering intact placebo caplets to the large intestine. Barium sulphate caplet cores (19.1 mm x 9.7 mm) were coated with 2 different pH-dependent acrylic copolymer products, Eudragit L100 and S100, in either a 1:0 ratio (100% Eudragit L100) or 3:1 ratio (75% Eudragit L100 and 25% S100). The disintegration profile of each formulation was determined through in vitro testing, then caplets were sequentially administered to 10 healthy volunteers, and monitored in vivo via serial abdominal fluoroscopic images. Test caplets with the 3:1 coating formulation had a 40% higher colon-targeting specificity compared with the 1:0-coated caplets, and tended to begin disintegrating at a later time after administration (p = 0.09). The total time from administration to complete disintegration was also significantly longer for the 3:1-coated caplets (p = 0.003). These results suggest that barium sulphate caplets with a 3:1 acrylic copolymer coating formulation ratio (Eudragit L100 and S100) may be a suitable delivery system for quantifying the biosynthesis of nutrients in the human large intestine and measuring their absorption across the colonic epithelium.
authors: Department of Nutritional Sciences, University of Toronto, Toronto, ON, Canada.
authors: Ashley M
authors: AM
authors: Aimone
authors: Bairbre
authors: B
authors: Connolly
authors: Surinder
authors: S
authors: Chaudhary
authors: Jamie
authors: J
authors: Lugtu-Pe
authors: Frank
authors: F
authors: Martinuzzi
authors: Paul
authors: P
authors: Pencharz
authors: Deborah L
authors: DL
authors: O'Connor
mesh_terms: D000328:Adult; D002626:Chemistry, Pharmaceutical; D003106:Colon / Q000378:metabolism*; D003692:Delayed-Action Preparations; D019587:Dietary Supplements; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D008875:Middle Aged; D055815:Young Adult
chemical_list: D003692:Delayed-Action Preparations