Coating of Oral Beclomethasone Dipropionate Capsules With Cellulose Acetate Phthalate Enhances Delivery of Topically Active Antfinflammatory Drug to the Terminal Ileum

Abstract

Selective delivery of orally administered topically active anti inflammatory drugs to the terminal ileum and ascending colon could be potentially useful for patients with inflammatory bowel disease involving these sites. Because topical beclomethasone dipro= pionate (BDP) enemas have been used successfully in the treatment of distal idiopathic colitis, oral formulations of this drug were studied. Entericcoated 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 ilea] effluent (43.0% ± 24.1%) compared to uncoated BDP capsules (13.5% ± 8.5%, p < 0.05, Student's paired t-test). We conclude that oral cellulose acetate phthalatecoated 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.