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KMID : 0369819910210020103
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Jorunal of Korean Pharmaceutical Sciences
1991 Volume.21 No. 2 p.103 ~ p.110
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Biopharmaceutical Studies of Lonazolac Acetic Acid Ester and Lonazolac Argininate
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함광수/Ham KS
이완하/양재헌/Lee WH/Yang JH
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Abstract
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Two new prodrugs of lonazolac, lonazolac acetic acid ester and lonazolac argininate, were prepared and examined for physicochemical properties and biopharmaceutical characteristics. The prodrugs were stable in solid state and lonazolac argininate showed higher dissolution rate than lonazolacca in both artificial gastric and intestinal juices. These prodrugs have higher analgegic effect than that of lonazolac-Ca in mice, and increased anti-inflammatory activities in rats. In addition, ulcerogenic effects and acute toxicity of these prodrugs were lower than those of lonaaolac-Ca. Lonazolac acetic acid ester showed larger area under the plasma concentration-time curves (AUC) than that of lonazolac. Therefore, it was suggested that these prodrugs of lonazolac have advantages over lonzolac-Ca for not only enhanced bioavailability but also decreased ulcerogenic and toxic effects.
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KEYWORD
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#prodrugs #anti-inflammatory activity #bioavailability #AUC #ulcerogenicity #acute toxicity #lonazolac-Ca(LAC) #lonazolac acetic acid ester(LAA) #lonazolac arginate(LAR)
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