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KMID : 0369819970270010011
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Jorunal of Korean Pharmaceutical Sciences
1997 Volume.27 No. 1 p.11 ~ p.14
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Comparison of Diclofenac Sodium and Diclofenac Sodium - β - cyclodextrin Complexation on Gastric Mucosal Injury in Rats
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박재훈/Park JH
김종환/김주일/김승조/서성훈/이경태/Kim JH/Kim JI/Kim SJ/Seo SH/Lee KT
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Abstract
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This laboratory has recently reported the solubility and in vivo absorption enhancement of diclofenac sodium by β?cyclodextrin complexation. The acute gastroduodenal mucosa injury provoked by administration of 34 mg/kg and 68 mg/kg of a diclofenac sodium (DS) and equivalent dose of new formulation [diclofenac sodium-beta-cyclodextrin complexation(DS?β?CD)] was evaluated and compared. Microscopic examinations, performed after 18-hrs treatment, demonstrated that DS?β?CD was less gastrolesive than DS. The drop in gastrophy after a single dose of the assigned drug was considerably greater for DS than for DS?β?CD, which registered similar values to control. Since gastrophy is an expression of the anatomy-functional integrity of the gastric barrier, the results indicate that DS?β?CD exerts less direct acute damage on the gastric mucosa. Therefore, when administered short-term, DS?β?CD appears to be less gastrolesive than the standard DS formulation.
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KEYWORD
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Diclofenac sodium, β?cyclodextrin, Absorption, Complexation, Mucosal injury
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