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Journal of Pharmacology and Experimental Therapeutics

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Abstract

Polymer delivery of the active isomer of misoprostol: a solution to the intestinal side effect problem.

W E Perkins, R G Bianchi, S J Tremont, P W Collins, J J Casler, R L Fenton, G M Wagner, M P McGrath, J C Stolzenbach and D L Kowalski
Journal of Pharmacology and Experimental Therapeutics April 1994, 269 (1) 151-156;
W E Perkins
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R G Bianchi
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S J Tremont
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P W Collins
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J J Casler
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R L Fenton
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G M Wagner
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M P McGrath
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J C Stolzenbach
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D L Kowalski
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Abstract

SC-53450 is a new polybutadiene-based polymer system with an acid labile diisopropyl silyl ether linker to which the active isomer of misoprostol (SC-30249) is attached covalently at position C-11. It was studied in rats and dogs to define its profile of gastrointestinal effects relative to misoprostol-hydroxypropyl methylcellulose (HPMC) and the systemic availability of prostaglandin from the polymer. Results of rat studies indicate that SC-53450 has a spectrum of mucosal protective activity similar to misoprostol-HPMC, being protective against indomethacin-induced gastric, cysteamine/indomethacin-induced duodenal and indomethacin-induced lower small bowel damage. SC-53450, in contrast to misoprostol-HPMC, was not diarrheagenic in the rat when administered intragastrically. The observation that SC-53450 is more than 4 times more potent than misoprostol-HPMC suggests the possibility of sustained gastric availability of the prostaglandin SC-30249. SC-53450 exhibited gastric antisecretory activity in histamine-stimulated gastric fistula dogs and protected against acidified aspirin-induced gastric damage in normal fasted beagles. Rat and dog experiments indicate that little, if any, polymer-derived prostaglandin is available systemically, suggesting SC-53450 will have reduced abuse potential in abortion induction. SC-53450 is a potential candidate to replace the present misoprostol formulation in the marketplace for the prevention of nonsteroidal anti-inflammatory drug-induced gastric damage.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 269, Issue 1
1 Apr 1994
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Abstract

Polymer delivery of the active isomer of misoprostol: a solution to the intestinal side effect problem.

W E Perkins, R G Bianchi, S J Tremont, P W Collins, J J Casler, R L Fenton, G M Wagner, M P McGrath, J C Stolzenbach and D L Kowalski
Journal of Pharmacology and Experimental Therapeutics April 1, 1994, 269 (1) 151-156;

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Abstract

Polymer delivery of the active isomer of misoprostol: a solution to the intestinal side effect problem.

W E Perkins, R G Bianchi, S J Tremont, P W Collins, J J Casler, R L Fenton, G M Wagner, M P McGrath, J C Stolzenbach and D L Kowalski
Journal of Pharmacology and Experimental Therapeutics April 1, 1994, 269 (1) 151-156;
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