title: Pulsatile systems for colon targeting of budesonide: in vitro and in vivo evaluation.
abstract: The purpose of this study is to increase the lag time and prevent release of budesonide, a corticosteroid drug used in Crohn's disease for the first 5 h and efficiently deliver it to the colon. Eudragit S100 spray-coated capsules and pulsatile systems using tablet plugs of cellulose acetate butyrate (CAB), HPMC K4M, guar gum, and pectin were prepared. Eudragit S100-coated capsules released 80.62% after 5 h. In pulsatile systems, decreasing the ratio of the polymer significantly increased the rate and extent of drug release. Spray-coating with EUD S100 decreased the extent of drug release to 48.41%, 69.94%, 80.58%, and 45.23% in CAB, HPMC K4M, pectin, and guar gum, respectively; however, the entire amount was released in the target area. In the presence of bacterial enzymes, selected formulas showed nearly 100% release. X-ray imaging performed to monitor the capsules throughout the GIT in human volunteers of the capsules and spray-coated pulsatile systems with 25% guar gum in the plug showed bursting in the transverse and ascending colon, respectively. Both formulations showed marked reduction in induced rabbit colitis model.
authors: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors: Soad A
authors: SA
authors: Yehia
authors: Ahmed H
authors: AH
authors: Elshafeey
authors: Ibrahim
authors: I
authors: Elsayed
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000818:Animals; D001682:Biological Availability; D019819:Budesonide / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D002214:Capsules; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003092:Colitis / Q000139:chemically induced / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D003106:Colon / Q000000981:diagnostic imaging / Q000187:drug effects / Q000378:metabolism* / Q000473:pathology; D044684:Colon, Transverse / Q000000981:diagnostic imaging / Q000378:metabolism; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*; D005685:Galactans / Q000737:chemistry / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D007082:Ileum / Q000000981:diagnostic imaging / Q000378:metabolism; D007785:Lactose / Q000737:chemistry; D008297:Male; D008351:Mannans / Q000737:chemistry / Q000378:metabolism; D008361:Mannosidases / Q000378:metabolism; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D010368:Pectins / Q000737:chemistry / Q000378:metabolism; D009195:Peroxidase / Q000378:metabolism; D053149:Plant Gums / Q000737:chemistry / Q000378:metabolism; D011096:Polygalacturonase / Q000378:metabolism; D011109:Polymethacrylic Acids / Q000737:chemistry; D011817:Rabbits; D011859:Radiography; D012007:Rectum / Q000000981:diagnostic imaging / Q000378:metabolism; D013270:Stomach / Q000000981:diagnostic imaging; D013607:Tablets; D014302:Trinitrobenzenesulfonic Acid / Q000494:pharmacology; D055815:Young Adult
chemical_list: D002214:Capsules; D003692:Delayed-Action Preparations; D005685:Galactans; D008351:Mannans; D053149:Plant Gums; D011109:Polymethacrylic Acids; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; D065347:Hypromellose Derivatives; D019819:Budesonide; C013517:ethyl cellulose; D010368:Pectins; D014302:Trinitrobenzenesulfonic Acid; D002482:Cellulose; C014396:cellulose acetate-butyrate; D008747:Methylcellulose; C007894:guar gum; D009195:Peroxidase; D008361:Mannosidases; C109435:galactomannanase; D011096:Polygalacturonase; D007785:Lactose