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DOI: 10.1055/s-0031-1298375
© Georg Thieme Verlag KG Stuttgart · New York
Intestinal Permeability of Forskolin by In Situ Single Pass Perfusion in Rats
Publication History
received October 31, 2011
revised February 21, 2012
accepted February 23, 2012
Publication Date:
12 March 2012 (online)
Abstract
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 µg/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 (Peff) of forskolin was in the range of drugs with high intestinal permeability. The Peff was highest in the duodenum as compared to other intestinal segments. The decreases of Peff 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 Peff. 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.
Key words
forskolin - intestine - permeability - single pass perfusion - Plectranthus barbatus - Coleus forskohlii - Lamiaceae
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Dr. Jian-Ming Huang
Department of Pharmacognosy
School of Pharmacy
Fudan University
826 Zhangheng Road
201203 Shanghai
China
Phone: +86 21 51 98 01 32
Fax: +86 21 51 98 01 32
Email: jmhuang@shmu.edu.cn
Dr. Wei-Yu Weng
Department of Pharmaceutics
School of Pharmacy
East China University of Science and Technology
130 Meilong Road
200237 Shanghai
China
Phone: +86 21 64 25 01 87
Fax: +86 21 64 25 32 50
Email: wyweng@ecust.edu.cn