丹参静脉注射后在兔血浆和眼玻璃体中的药代动力学研究  

Pharmacokinetic research of Salvia miltiorrhiza in rabbits plasma and vitreous body after intravenous injection

作　　者：张丽琼[1] 廖敏华 李明生 高丽园[1] 刘子睿[1] 于永斌[1] 

机构地区：[1]哈尔滨医科大学附属第一医院眼科,黑龙江哈尔滨150001 [2]海南农垦三亚医院眼科,海南三亚572009 [3]黑龙江省眼科医院,黑龙江哈尔滨150001

出　　处：《哈尔滨医科大学学报》2012年第5期415-419,共5页Journal of Harbin Medical University

基　　金：黑龙江省自然科学基金资助项目(D200949);哈尔滨市科技局资助项目(2007RFQXS090);黑龙江省教育厅科学技术研究项目(11541219);黑龙江省卫生厅科研项目(2007-222)

摘　　要：目的建立测定兔血浆和玻璃体中丹参素含量的高效液相色谱方法,研究丹参通过血眼屏障进入玻璃体的能力及药代动力学特点。方法白兔72只,随机分为对照组6只;血浆组6只;玻璃体组60只。对照组0.85%生理盐水20 mL,静脉注射。其余两组丹参1.0 g/kg静脉注射。取血浆和玻璃体检测丹参素的含量。色谱柱Hypersil BDS,C18柱(5μm,4.6 mm×250 mm);预柱:自填国产YWGC18;流动相为乙腈:0.01 mol/L磷酸二氢钾(8:92);紫外检测波长279 nm;流速1.0 mL/min;柱温为室温。结果丹参素血浆质量浓度符合三室模型。t1/2β(消除半衰期):5.661 min;Cmax(锋浓度):727.29mg/L;Tmax(达峰时间):0 min。玻璃体质量浓度符合二室模型。t1/2β:499.521 min;Cmax:0.998 mg/L;Tmax:25 min。对照组血浆、玻璃体中未检测到丹参素。结论本方法灵敏、特异、准确。丹参静脉注射后可以通过血眼屏障,丹参素在玻璃体内的含量较少。在玻璃体中丹参吸收比较慢,消除也较慢。Objective To establish high performance liquid chromatography（HPLC） in order to determine the concentration of Danshensu in blood plasma and vitreous body of the rabbits;to study the capacity of Danshensu penetrating vitreous body through blood-ocular barrier and its characterics of pharmacokinetics.Methods Seventy-two white rabbits were divided into three groups： control group（n=6）,plasma group（n=6）,vitreous body group（n=60）.Rabbits of control group were injected 20 mL physiological saline of 0.85% through auri-edge vein.Salvia miltiorrhiza 1.0 g/kg were injected through vein of auri-edge.In plasma group, blood and vitreous body were obtained.The analytical column was a BDS C18 stainless steed column（5μm,4.6 mm× 250 mm）;precolumn：YWGC18;the mobile phase consists of acetonitrile and 0.01 mol/L KH2PO4（8：92,adjusted to pH=2.8 with phosphoric acid）.The UV detector was set at 279 nm;the flow rate was 1.0 mL/min;and the column temperature was ordinary temperature.Results The plasma concentration-time curves of Salvia miltiorrhiza fitted three-compartment model.t1/2β（elimination half time）：5.661 min;Cmax（peak concentration）： 727.29 mg/L;Tmax（peak time）： 0 min.Concentration-time curves of vitreous body fitted two compartment model.t1/2β： 499.521 min;Cmax： 0.998 mg/L;Tmax： 25 min.Conclusion HPLC is sensitive,specific and accurate.After intravenous injection through auri-edge vein,Salvia miltiorrhiza can penetrate blood-ocular barrier and the concentration of Salvia miltiorrhiza in the vitreous body is less.The absorption of Salvia miltiorrhiza in vitreous body is slower and the elimination is slower.

关 键 词：丹参 高效液相色谱法 药代动力学 兔 玻璃体 

分 类 号：R917.101[医药卫生—药物分析学]