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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 pharmacokinetics of tetrandrine in aqueous humor of rabbit eyes and to provide basis for local rational drug use. Methods 16 rabbit eyes were subconjunctivally injected with tetrandrine 5 mg. Aqueous humor was drawn on time. After treatment, the concentration of tetrandrine in aqueous humor was determined by HPLC. The data were fitted by DSA pharmacokinetic software and the pharmacokinetic parameters were obtained. . Results The concentration of tetrandrine in the aqueous humor after subconjunctival injection of 5 mg of tetrandrine was higher, and the drug-time curve was consistent with the two-compartment model. The main kinetic parameters were: t1/2α0.533 h, t1/2β0.69 h, AUC(0-∞) 17.762 mg.hL-1, K104.087 h-1, K122.787 h-1, K211. 005 h-1, t1/2Ka0.398 h. Conclusion The subconjunctival injection of tetrandrine in rabbit eyes can pass through the blood water barrier, and it distributes rapidly in the aqueous humor, and the metabolic elimination rate is also faster.