A new oral formulation for the release of sodium butyrate in the ileo-cecal region and colon

• Published in: World journal of gastroenterology : WJG Vol. 13; no. 7; pp. 1079 - 1084
• Main Author: Roda, Aldo
• Format: Journal Article
• Language: English
• Published: United States Department of Pharmaceutical Sciences,University of Bologna,Via Belmeloro 6,Bologna 40126,Italy%Department of Internal Medicine and Gastroenterology,University of Bologna,via Massarenti 9,Bologna 40126,Italy 21.02.2007; Baishideng Publishing Group Co., Limited
• Subjects: Administration, Oral; Adolescent; Adult; Aged; Butyrates - administration & dosage; Butyrates - metabolism; Butyrates - therapeutic use; Carbon Dioxide - metabolism; Carbon Isotopes; Cecum - metabolism; Chemistry, Pharmaceutical; Colon - metabolism; Crohn Disease - drug therapy; Female; Humans; Ileum - metabolism; Male; Middle Aged; Rapid Communication; Sodium - administration & dosage; Sodium - metabolism; Sodium - therapeutic use; Tablets, Enteric-Coated; Taurochenodeoxycholic Acid - blood; 丁酸钠; 公式化; 列方程式; Sodium butyrate; Inflammatory bowel diseases; Controlled release formulation; Stable isotope; Breath test; Crohn's disease; Pharmacokinetics; Ulcerative colitis
• ISSN: 1007-9327; 2219-2840
• DOI: 10.3748/wjg.v13.i7.1079

AIM： To develop a new formulation with hydroxy propyl methyl cellulose and Shellac coating for extended and selective delivery of butyrate in the ileo-caecal region and colon. METHODS： One-gram sodium butyrate coated tablets containing ^13C-butyrate were orally administered to 12 healbhy subjects and 12 Crohn＇s disease patients and the rate of ^13C-butyrate absorption was evaluated by t3CO2 breath test analysis for eight hours. Tauroursodeoxycholic acid （500 rag） was co-administered as a biomarker of oro-ileal transit time to determine also the site of release and absorption of butyrate by the time of its serum maximum concentration. RESULTS： The coated formulation delayed the ^13C-butyrate release by 2-3 h with respect to the uncoated tablets. Sodium butyrate was delivered in the intestine of all subjects and a more variable transit time was found in Crohn＇s disease patients than in healthy subjects. The variability of the peak ^13CO2 in the kinetic release of butyrate was explained by the inter-subject variability in transit time. However, the coating chosen ensured an efficient release of the active compound even in patients with a short transit time. CONCLUSION： Simultaneous evaluation of breath ^13CO2 and tauroursodeoxycholic acid concentrationtime curves has shown that the new oral formulation consistently releases sodium butyrate in the ileo-cecal region and colon both in healthy subjects and Crohn＇s disease patients with variable intestinal transit time. This formulation may be of therapeutic value in inflammatory bowel disease patients due to the appropriate release of the active compound.