Evaluation on the Colon-Targeting Characteristics of Budesonide Colonic Localization Tablet in Rat
LIU Hui1，PAN Wei-san2
Author information+
1. Department of Pharmacy，Wuhan General Hospital of Guangzhou Military Command，Wuhan 430070，China；2. School of Pharmacy，Shenyang Pharmaceutical University，Shenyang 110016，China
OBJECTIVE To evaluate the colon-targeting effects of budesonide colonic localization tablet by comparing the budesonide concentration in gastrointestinal tissue after oral administration of different budesonide preparations.METHODS The different tissue fluids were sampled and the HPLC method was used to determine the budesonide concentration in stomach,small intestine,large intestine tissue after budesonide localization tablet,budesonide tablet and budesonide suspension were administrated in rats,respectively.RESULTS With oral administration of budesonide localization tablets,the peak concentration of budesonide [cmax=(7.17±2.32)μg·g-1] in large intestine tissue was reached at the 6 h and it was significantly higher than that of suspension group(1.37±0.82) μg·g-1 and common tablet group(0.47±0.18) μg·g-1.By investigating the effects of different oral preparations on the gastrointestinal tissue distribution of budesonide in rats at the same time,budesonide was found only in the large intestine tissue,but no drug was distributed in the stomach and the small intestine tissue with oral administration of budesonide localization tablet.CONCLUSION The budesonide colonic localization tablet has conspicuous colon-targeting property.
LIU Hui;PN Wei-sn.
Evaluation on the Colon-Targeting Characteristics of Budesonide Colonic Localization Tablet in Rat [J]. Chinese Pharmaceutical Journal, 2008, 43(23): 1804-1806
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1] EDWARD J O C. Review of the unique properties of budesonide[J] . Clin Ther，2003，25(Suppl c)： 42-66.
[2] LAMERS C B H W，WAGTMANS M J，VAN DER SLUYS VEER A，et al. Budesonide in inflammatory bowel disease[J] . Nether J Med，1996，48： 60-63.
[3] LIU H，YANG X G，NIE S F，et al. Chitosan-based controlled porosity osmotic pump for colon-specific delivery system：Screening of formulation variables and in vitro investigation[J] . Int J Pharm，2007，331：115-124.
[4] LI Y N，TATTAM B，BROWN K F，et al. Quantification of epimeric budesonide and fluticasone propionate in human plasma by liquid chromatography atmospheric pressure chemical ionization tandem mass spectrometry[J] . J Chromatogr B，2001，761： 177-185.
[5] LIU H，DU R，PAN W S. Determination of budesonide concen- tration in tissue distribution after oral administration of the budesonide colonic localization tablet with HPLC[J] . Chin Hosp Pharm J(中国医院药学杂志)，2008，28 (7)： 520-522.
[6] TOZAKI H，ODORIBA T，OKADA N，et al. Chitosan capsules for colon-specific drug delivery enhanced localization of 5-aminosalicylic acid in the large intestine accelerates healing of TNBS-induced colitis in rats[J] . J Controlled Release，2002，82： 51-61.
