Previous studies have shown the beneficial effect of rebamipide, a novel anti-ulcer drug, on experimental colitis. The permeabilities of rebamipide in different intestinal segments remained unknown.
A research article to be published on August 21, 2008 in the World Journal of Gastroenterology addresses this question. The research team led by Guo-Feng Li from Nanfang Hospital, Southern Medical University in China investigated the permeability of rabamipide across different intestinal membranes, analyzed potential transportation mode, and observed the effect of sodium laurate (C12) as an absorption enhancer on the permeability of rebamipide across colonic tissues. Furthermore, the effectiveness of chitosan on the colon-specific delivery of rebamipide and the influence of combination chitosan with absorption enhancers on colon specific delivery of rebamipide were explored.
The permeabilities of rebamipide across the jejunal and ileal membranes were higher than the colonic membranes, as monitored by using chamber experiment. Both C12 and labrasol significantly increased permeability of rebamipide across the colon membranes. The release of rebamipide from chitosan capsule was less than 10% totally within 6 h. The areas under concentration-time curve (AUC) in the colon mucosa (AUCLI, 16011.2 ng•h/g) were 2.5 times and 4.4 times greater than using gelatin capsules and CMC suspension, respectively. Meanwhile, AUC in the plasma (AUCPL) were 1016.0 ng•h/mL for chitosan capsule, 1887.9 ng•h/mL for CMC suspension and 2163.5 ng•h/mL for gelatin capsule. The results suggested that both AUCLI and AUCPL increased when C12 was administrated simultaneously, but the increase of AUCLI was much greater; drug delivery index (DDI) was higer in C12 + chitosan than in chitosan capsule group.
Since the present experiments have demonstrated the possibility of chitosan capsule as a specific colon delivery carrier of rebamipide in rats, study of the drug-filled chitosan capsule should be the next step, including large scale preparation and clinical usage. It can be expected that chitosan capsule of rebamipide compounded with absorption enhancer, C12, can be used to treat colnitis effectively in the future.
Reference: Huang BB, Li GF, Luo JH, Duan L, Nobuaki K, Akira Y. Permeabilities of rebamipide via the rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier. World J Gastroenterol 2008; 14(31): 4928-4937
http://www.wjgnet.com/1007-9327/14/4928.asp
Correspondence to: Guo-Feng Li, Department of Pharmacy, Nanfang Hospital, Southern Medical University, 1838 Guangzhou AVE(N), Guangzhou 510515, Guangdong Province, China. lgfnf@fimmu.com
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About World Journal of Gastroenterology
World Journal of Gastroenterology (WJG), a leading international journal in gastroenterology and hepatology, has established a reputation for publishing first class research on esophageal cancer, gastric cancer, liver cancer, viral hepatitis, colorectal cancer, and H pylori infection and provides a forum for both clinicians and scientists. WJG has been indexed and abstracted in Current Contents/Clinical Medicine, Science Citation Index Expanded (also known as SciSearch) and Journal Citation Reports/Science Edition, Index Medicus, MEDLINE and PubMed, Chemical Abstracts, EMBASE/Excerpta Medica, Abstracts Journals, Nature Clinical Practice Gastroenterology and Hepatology, CAB Abstracts and Global Health. ISI JCR 2003-2000 IF: 3.318, 2.532, 1.445 and 0.993. WJG is a weekly journal published by WJG Press. The publication dates are the 7th, 14th, 21st, and 28th day of every month. WJG is supported by The National Natural Science Foundation of China, No. 30224801 and No. 30424812, and was founded with the name of China National Journal of New Gastroenterology on October 1, 1995, and renamed WJG on January 25, 1998.
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World Journal of Gastroenterology