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KMID : 0614020000160010078
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Journal of Pharmaceutical Sciences (C.N.U.)
2000 Volume.16 No. 1 p.78 ~ p.83
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Antiplatelet Effect of Cilostazol and Effect of Sodium Citrate on Platelet Aggregation
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Woo Su-Kyung
Kim Young-Ri
Kwon Kwang-II
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Abstract
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Cilostazol, 6- 〔4- (1-cyclohexyl- 1H-tetrazol -5-yl) butoxy〕 - 3, 4-dihydro- 2(1H)- quinolinone, is an antiplatelet/antithrombotic agent that has been used for treatment of chronic peripheral arterial occlusion. Cilostazol was studied for its inhibitory effects on platelet aggregation in vitro in rabbit plasma and in human plasma, and also for its antiplatelet effects ex vivo in rabbit after single oral administration. At time t=0, the rabbits were given a single oral dose of 14 ㎎/㎏ cilostazol. At 1, 2, 4, 8, 12, and 24 hours after drug administration, blood samples were taken for measurements of antiplatelet aggregation effect. Before the study of antiplatelet effects of cilostazol in rabbits, the effect of sodium citrate on platelet aggregation in various concentrations was studied to determine the optimal treatment. Cilostazol produced a potent inhibitory effect on platelet aggregation induced by adenosine diphosphate (ADP) in vitro. The maximum effect on antiplatelet aggregation was 14.4% and was appeared at 1 hour after drug administration. The optimum blood/anticoagulant (3.8% sodium citrate) ratio was 9 to 1, and 16 to 1 in human plasma and in rabbit plasma, respectively.
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KEYWORD
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Cilostazol, platelet aggregation, sodium citrate in rabbit and human
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