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Developing a mechanism to measure the absorption of bacterially‐synthesized folate across the colon: Testing of caplets with a pH‐sensitive coating designed for colon targeting
Author(s) -
Aimone Ashley,
Connolly Bairbre,
Chaudhary Surinder,
Lugtu Jamie,
Martinuzzi Frank,
O'Connor Deborah L
Publication year - 2008
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.22.1_supplement.296.7
Subject(s) - placebo , in vivo , gastroenterology , chemistry , absorption (acoustics) , medicine , materials science , biology , pathology , microbiology and biotechnology , alternative medicine , composite material
We hypothesize that bacterially synthesized folate in the large intestine may significantly influence the folate status of humans and, specifically, colonocytes. Research in this area has been limited due to the absence of a non‐invasive means to quantitatively deliver test doses of folate to the colon. The purpose of this study was to design and test the effectiveness of two pH‐dependent coatings in delivering intact placebo caplets to the large intestine. Barium sulphate caplet cores (19.1 x 9.7mm) were coated with Eudragit ® L100 and S100, in either a 1:0 or 3:1 ratio. Each formulation was administered to ten healthy volunteers, and monitored in‐vivo via serial abdominal fluoroscopic images. Test caplets with 3:1 coating formulations had 40% higher colon‐targeting specificity compared to 1:0 caplets, and tended to begin dissolving at a later time after administration (p=0.09). The total time from administration to complete dissolution was also significantly longer for 3:1 coated caplets (p=0.003). These results suggest that barium sulphate caplets with a 3:1 (Eudragit L100:S100) coating formulation ratio would be a suitable delivery system for investigating the absorption of folate across the large intestine. Sponsored by NSERC and the CIHR Training Program in Clinical Research.