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혈소판 응집 억제제의 효과 측정법에 대한 고찰과 지원자에서 Triflusal의 혈소판 응집 억제능 평가
이병요,장힘찬,백인환,윤휘열,권광일 충남대학교 약학대학 의약품개발연구소 2010 藥學論文集 Vol.25 No.-
The anti-platelet agent is a member of a class of pharmaceuticals that decreases platelet aggregation and inhibits thrombus formation. They are effective in the arterial circulation and widely used in primary and secondary prevention of thrombotic cerebrovascular or cardiovascular disease. As a method for estimating the effects of anti-platelet agent, platelet aggregation was conventionally measured using the optical method or the impedance method. Several alternate methods currently in development or recently developed were considered, including luminescence method, flow cytometry, laser-light scattering method, and Verify Now-P2Y12 assay. Principles, advantages, and disadvantages of the optical method, impedance method, and the other alternate platelet aggregation methods were discussed in this report. 15 human volunteers were recruited for the evaluation of the efficacy of triflusal using the optical method. After the oral administration of a single dose of 900mg, 15 subjects received eight doses administered at 24-hour intervals of 600mg triflusal. Using platelet rich-plasma from above subjects, we performed baseline platelet aggregation test induced by adenosine diphosphate(ADP), collagen, and arachidonic acid. The results of platelet aggregation test after triflusal administration were compared with the baseline study. Triflusal significantly inhibited platelet aggregation induced by ADP (33.0±21.3%) and arachidonic acid (99.1±1.2%), respectively. Therefore, we concluded that anti-platelet aggregation effect of triflusal can be studied successfully with the optical method. Each of the platelet aggregation methods has value for evaluating the effects by various mechanisms of the anti-platelet agents. The ideal method for estimating the platelet aggregation as it relates to safety and efficacy in patients treated with anti-platelet agents will need to be determined in clinical trials.
암브록솔과 세티리진의 Cytochrome P450 저해 활성 평가
김봉희,류창선,장힘찬,이상윤,이지윤,채정우,권광일,김상겸 대한약학회 2013 약학회지 Vol.57 No.3
In the present study we evaluated drug-drug interaction potential of ambroxol and cetirizine mediated by inhi-bition of CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 using pooled human liver microsomes (HLMs). As measured by liquid chromatography-electrospray ionization tandem mass pec- trometry, cetirizine and ambroxol inhibited significantly CYP2E1 but the maximal inhibition was approximately 36% at 10 µM cetirizine and 28% at 3 µM ambroxol. In addition, CYP2D6 activity was decreased to approximately 83% of ontrol activity in pooled HLM incubated with 3 µM ambroxol. Activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, and CYP3A4 were not significantly inhibited by cetirizine and ambroxol. Considering their maximal plasma concentration in human (Cmax of cetirizine is approximately 0.67 µM and Cmax of ambroxol is 0.044 µM), these two drugs have very low pos- sibility in drug-drug interaction by CYP inhibition in clinical situations.