粉防己碱在兔眼房水中的药物动力学考察

Pharmacokinetics of tetrandrine in aqueous humor of rabbit following subconjunctival administration

目的探讨粉防己碱在兔眼房水中的药物动力学过程,为临床局部合理用药提供依据。方法16只兔眼结膜下注射粉防己碱5 mg,按时抽取房水,经处理后,用HPLC法测定房水中粉防己碱质量浓度,通过DSA药物动力学软件拟合数据,获得药物动力学参数。结果粉防己碱5 mg结膜下注射后房水内有较高的药物浓度,药-时曲线符合二室模型。其主要动力学参数为:t1/2α0.533 h,t1/2β0.69 h,AUC(0-∞)17.762 mg.h.L-1,K104.087 h-1,K122.787 h-1,K211.005 h-1,t1/2Ka0.398 h。结论粉防己碱兔眼结膜下注射能通过血房水屏障,其在房水内分布较快,代谢消除速度也较快。

Objective To investigate the pharmacokinetic parameters of tetrandrine following subconjunctival administration. Methods Sixteen rabbits were given subconjunctival administration by a single dose of tetrandrine 5 rag, the concentrations of tetrandrine in aqueous humor at various time were determined by HPLC, and the pharmacokinetic parameters were analyzed by DSA. Results The concentration-time data of tetrandrinein aqueous humor was subject to two-compartment open model. The pharmacokinetic parameters were as follows： t1/2α0.533h,t1/2β 0.69h,AUC（0-∞）17.762mg·h·L^-1,K10 4.087h^-1,K12 2.787h^-1,K21 1.005h^-1,t1/2Ka 0.368h. Conclusions Tetrandrine can penetrate blood-aqueous barrier to enter aqueous humor, its distribution and clearance are fast.