羟苯磺酸钙缓释胶囊在大鼠体内的药动学-药效学研究  

Pharmacokinetics-pharmacodynamics of calcium dobesilate in rats

作　　者：赵海山[1] 曾宪鑫[1] 陈秋晨[1] 江茜[1] 魏敏杰[1] 

机构地区：[1]中国医科大学药学院,辽宁沈阳110001

出　　处：《广东药学院学报》2014年第1期11-14,共4页Academic Journal of Guangdong College of Pharmacy

摘　　要：目的考察羟苯磺酸钙缓释胶囊在大鼠体内的药动学参数,并判断其抗血小板聚集作用和防止血栓形成作用。方法采用HPLC-UV法测定大鼠血浆样品中的羟苯磺酸钙质量浓度,DAS 2.0药动学软件处理得到主要药动学参数。用血小板聚集仪测定羟苯磺酸钙缓释胶囊的抗血小板聚集作用,用颈动脉血栓模型测定其抑制血栓形成作用。结果主要药动学参数如下:AUC0-t为(298.32±34.12)μg·h·mL-1,AUC0-∞为(318.54±30.11)μg·h·mL-1,C max为(33.10±8.774)μg·mL-1,t max为(5.64±0.77)h,t1/2为(3.01±0.78)h;当羟苯磺酸钙溶液质量浓度为300μg/mL时,血小板聚集抑制率可达(23.54±15.32)%,且具有剂量依赖关系;羟苯磺酸钙溶液的血栓形成抑制率为(22.72±20.77)%。结论羟苯磺酸钙具有抗血小板聚集功能和抗血栓形成作用。Objective To study the pharmaeokinetics and pharmacodynamics of calcium dobesilate in rats and the effect of calcium dobesilate on platelet aggregation in vitro and thrombosis in vivo. Methods The plasma concentration of calcium dobesilate was determined by HPLC-UV method. The main pharmacokinetic parameters were calculated by DAS 2.0. The inhibit rate of platelet aggregation was determined by platelet aggregometer. The effect of calcium dobesilate on thrombosis was determined by the carotid thrombosis model of rats. Results The main pharmacokinetie parameters of calcium dobesilate were as follows： AUC0-1, was （298.32 ±34.12）μg · h · mL^-1 ,AUC0-∞ was （ 318.54± 30.11 ）μg · h ·mL^-1 , C was （ 33.10± 8.774） μg · mL^-1 , tmax was （ 5.64±0.77 ） h, t 1/2 %3 （ 3.01 ±0.78） h. When the concentration of calcium dobesilate arrived at 300 p.g/mL, the inhibit rate of platelet aggregation was （23.54± 15.32）% ,with dose-dependent manner. The inhibitory rate of thrombosis was （22.72±20.77）%. Conclusion The calcium dobesilate could inhibit thrombosis and platelet aggregatmn

关 键 词：羟苯磺酸钙 HPLC 药动学 血小板聚集 血栓模型 药效学 

分 类 号：R969[医药卫生—药理学]