Biopharmaceutical Studies of Lonazolac Acetic Acid Ester and Lonazolac Argininate

로나졸락 초산에스테르 및 로나졸락 알지니네이트의 생물약제학적 연구

  • Ham, Kwang-Su (College of Pharmacy, Sung Kyun Kwan University) ;
  • Lee, Wan-Ha (College of Pharmacy, Sung Kyun Kwan University) ;
  • Yang, Jae-Heon (College of Pharmacy, Jeon Ju Woosuk University)
  • 함광수 (성균관대학교 약학대학) ;
  • 이완하 (성균관대학교 약학대학) ;
  • 양재헌 (전주우석대학교 약학과)
  • Published : 1991.06.20

Abstract

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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