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Abstract

Contribution of the intestine to the first-pass metabolism of felodipine in the rat.

S X Wang, T A Sutfin, C Bäärnhielm and C G Regårdh
Journal of Pharmacology and Experimental Therapeutics August 1989, 250 (2) 632-636;
S X Wang
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T A Sutfin
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C Bäärnhielm
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C G Regårdh
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Abstract

The systemic availability of intraduodenally (i.d.) administered felodipine in the rat is about 10%. The purpose of this study was to determine to what extent intestinal metabolism contributes to the first-pass elimination of felodipine in the rat. Four different types of experiments were performed. 1) [3H]Felodipine was given i.v. and i.p.; 2) the uptake of i.p. administered [3H]felodipine by the lymph was studied for 3 hr after dosing; 3) portal blood was collected quantitatively for 40 min after i.d. administration of [3H]felodipine; and 4) the in vitro metabolism of felodipine was studied in intestinal cell suspensions. The mean bioavailability of the i.p. dose was approximately 48%. The uptake via the lymph was negligible as an insignificant amount of the radioactive i.p. dose was recovered in lymph from a main lymph vessel in the peritoneal cavity. An average of 21 +/- 12% of given radioactive dose was recovered in portal blood during the first 40 min after i.d. dosing. The recovered radioactivity was to 40 to 70% due to felodipine and 9 to 16% was due to dehydro-felodipine. These results indicate that substantial first-pass elimination occurs in the intestine of the rat. Further support for gastrointestinal metabolism of felodipine in the rat was obtained from incubations with intestinal cells.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 250, Issue 2
1 Aug 1989
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Abstract

Contribution of the intestine to the first-pass metabolism of felodipine in the rat.

S X Wang, T A Sutfin, C Bäärnhielm and C G Regårdh
Journal of Pharmacology and Experimental Therapeutics August 1, 1989, 250 (2) 632-636;

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Abstract

Contribution of the intestine to the first-pass metabolism of felodipine in the rat.

S X Wang, T A Sutfin, C Bäärnhielm and C G Regårdh
Journal of Pharmacology and Experimental Therapeutics August 1, 1989, 250 (2) 632-636;
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