Coating of oral beclomethasone dipropionate capsules with cellulose acetate phthalate enhances delivery of topically active antiinflammatory drug to the terminal ileum.
Selective delivery of orally administered topically active antiinflammatory drugs to the terminal ileum and ascending colon could be potentially useful for patients with inflammatory bowel disease involving these sites. Because topical beclomethasone dipropionate (BDP) enemas have been used successfully in the treatment of distal idiopathic colitis, oral formulations of this drug were studied. Enteric-coated or uncoated capsules containing BDP were administered in a single-dose protocol on separate days to 6 healthy volunteers with postcolectomy ileostomies. Ileostomy effluent was collected for a minimum of 8 h and analyzed by high-performance liquid chromatography for BDP, its pharmacologically active derivative beclomethasone monopropionate (BMP), and inactive beclomethasone alcohol. Cellulose acetate phthalate coating of oral BDP capsules significantly increased the mean percentage recovery of BDP + BMP in ileal effluent (43.0% +/- 24.1%) compared to uncoated BDP capsules (13.5% +/- 8.5%, p less than 0.05, Student's paired t-test). We conclude that oral cellulose acetate phthalate-coated BDP capsules may merit clinical trial in Crohn's ileitis and ileocolitis or in conjunction with BDP enemas for topical treatment of ulcerative colitis involving the whole colon.
D000284:Administration, Oral; D000328:Adult; D000368:Aged; D001507:Beclomethasone / Q000008:administration & dosage* / Q000032:analysis; D002214:Capsules; D002482:Cellulose / Q000031:analogs & derivatives* / Q000627:therapeutic use; D002851:Chromatography, High Pressure Liquid; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D007079:Ileitis / Q000188:drug therapy; D007081:Ileostomy; D007082:Ileum; D066298:In Vitro Techniques; D008875:Middle Aged; D012116:Resins, Plant; D013608:Tablets, Enteric-Coated
D002214:Capsules; D012116:Resins, Plant; D013608:Tablets, Enteric-Coated; D002482:Cellulose; C011708:cellulose acetate phthalate; D001507:Beclomethasone