结膜下给药兔眼玻璃体内维拉帕米的药代动力学研究

姜彩辉; 张卯年; 张鲲; 赵玉兰; 廖杰

结膜下给药兔眼玻璃体内维拉帕米的药代动力学研究

The study of pharmacokinetics of verapamil in vitreous following subconjunctival administration in an experimental model of PVR

摘要

摘要: 目的：研究结膜下给药兔眼玻璃体内维拉帕米(Verapamil，Ver)的药代动力学参数。方法：制备外伤性PVR动物模型，结膜下注射1.25mg/0.5ml Ver，按时抽取玻璃体样品。样品经提取、浓缩处理后，采用美国HP1050HPLC系统测定样品中Ver的浓度，计算其药代动力学参数。结果：结膜下注射Ver后，吸收半衰期t_1/2(Ka)=(0.54±0.16) h，达到峰浓度的时间T (peak)=(2.10±0.84) h，峰浓度Cmax=(17.65±4.64)μg/ml，消除半衰期t_1/2(Ke)=(7.29±1.46) h，药-时曲线下面积AUC=(208.07±40.22)μg/(ml·h)。结论：结膜下注射Ver可以进入玻璃体并能达到有效治疗浓度，为结膜下注射Ver防治PVR提供了理论依据。

Abstract: Objective: To study the pharmacokinetic parameters of verapamil in vitreous following subconjunctival administration. Methods: An experimental model of traumatic proliferative vitreoretinopathy was produced in pigment rabbits，which received subconjunctival verapamil injection.The concentrations of verapamil in vitreous at various times were determined by a reversed- phase HPLC， and the pharmacokinetic parameters were analyzed by 3P87.Results: The pharmacokinetic parameters were as follows: lagtime=(12.6±4.4)min，T (peak)=(2.10±0.84)h，Cmax =(17.65±4.64(g)/ml，Ka=(1.34± 0.26)/h，t_1/2(Ka)=(0.54±0.16)h，Ke=(0.09±0.03)/h，t_1/2(Ke)=(7.29(1.46)h，AUC=(208.07(40.22±μg/(ml· h).Conclusion: Verapamil penetrates into the vitreous following subconjunctival administration and reaches potentially therapeutic concentrations for 24hours.The results provide the basis of subconjunctival verapamil for the treatment of PVR.

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