粉防己碱在兔眼房水中的药物动力学考察

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。

Pharmacokinetics of tetrandrine in aqueous humor of rabbit following subconjunctival administration

Objective To investigate the pharmacokinetic parameters of tetrandrine following subconjunctival administration. Method Sixteen rabbits were given subconjunctival administration by a single dose of tetrandrine 5 mg, the concentrations of tetrandrine in aqueous humor at various time were determined by HPLC, and the pharmacokinetic parameters were analyzed by DSA. Result The concentration-time data of tetrandrinein aqueous humor was subject to two-compartment open model. The pharmacokinetic parameters were as follows: t_1/2α 0.533 h，t_1/2β0.69 h，AUC_(0-∞)17.762 mg·h·L^-1，K₁₀4.087 h-1，K₁₂ 2.787 h-1，K₂₁1.005 h-1，t_1/2Ka0.398 h。Conclusion Tetrandrine can penetrate blood-aqueous barrier to enter aqueous humor, its distribution and clearance are fast.