文献类型：期刊文献

英文题名：Intestinal Permeability of Forskolin by In Situ Single Pass Perfusion in Rats

作者：Liu, Zhen-Jun[2];Jiang, Dong-bo[2];Tian, Lu-Lu[1];Yin, Jia-Jun[1];Huang, Jian-Ming[1];Weng, Wei-Yu[2]

机构：[1]Fudan Univ, Sch Pharm, Dept Pharmacognosy, Shanghai 201203, Peoples R China;[2]E China Univ Sci & Technol, Sch Pharm, Dept Pharmaceut, Shanghai 200237, Peoples R China

年份：2012

卷号：78

期号：7

起止页码：698

外文期刊名：PLANTA MEDICA

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000303838000009)】；

基金：Financial support from the Science and Technology Commission of the Shanghai Municipality (09dZ1973200) is gratefully acknowledged.

语种：英文

外文关键词：forskolin; intestine; permeability; single pass perfusion; Plectranthus barbatus; Coleus forskohlii; Lamiaceae

摘要：The intestinal permeability of forskolin was investigated using a single pass intestinal perfusion (SPIP) technique in rats. SPIP was performed in different intestinal segments (duodenum, jejunum, ileum, and colon) with three concentrations of forskolin (11.90, 29.75, and 59.90 mu g/mL). The investigations of adsorption and stability were performed to ensure that the disappearance of forskolin from the perfusate was due to intestinal absorption. The results of the SPIP study indicated that forskolin could be absorbed in all segments of the intestine. The effective permeability (P-eff) of forskolin was in the range of drugs with high intestinal permeability. The P-eff was highest in the duodenum as compared to other intestinal segments. The decreases of P-eff in the duodenum and ileum at the highest forskolin concentration suggested a saturable transport process. The addition of verapamil, a P-glycoprotein inhibitor, significantly enhanced the permeability of forskolin across the rat jejunum. The absorbed fraction of dissolved forskolin after oral administration in humans was estimated to be 100% calculated from rat P-eff. In conclusion, dissolved forskolin can be absorbed readily in the intestine. The low aqueous solubility of forskolin might be a crucial factor for its poor oral bioavailability.