琥珀酸甲泼尼龙兔眼球周注射的药代动力学研究  

Pharmacokinetics of methylprednisolone sodium succinate after periocular injection into rabbits

作　　者：车松天[1] 李旭 

机构地区：[1]吉林大学第二医院眼底病科,中国吉林省长春市130041

出　　处：《国际眼科杂志》2018年第2期235-238,共4页International Eye Science

摘　　要：目的:检测琥珀酸甲泼尼龙(methylprednisolone sodium succinate,MPS)兔眼球周注射后,MPS和其在眼内的代谢产物甲泼尼龙(methylprednisolone,MP)的分布及药代动力学情况。方法:兔眼球周注射琥珀酸甲泼尼龙钠10mg,采用质谱-液相色谱方法检测MPS和MP在巩膜、脉络膜和视网膜、玻璃体、虹膜、房水、晶状体、视神经和血浆中的浓度。结果:球周注射琥珀酸甲泼尼龙钠后,MPS浓度在眼内组织中的达峰时间为注药后0.25~1h,在血浆中的达峰时间为注药后0.25h;MP浓度在眼内组织中的达峰时间为0.5~6h,在血浆中的达峰时间为注药后0.5h。MPS和MP在眼内各组织的达峰浓度由高到低依次为巩膜、视神经、脉络膜和视网膜、虹膜、晶状体,二者在晶状体内的浓度均为所有眼部组织中最低,且远远低于眼内其它组织的含量,但平均驻留时间最长。结论:球周注射MPS是一种有效的向眼组织传递药物的方式,且该药在眼内的分布有利于向巩膜、视神经和脉络膜视网膜给药,而不易被晶状体吸收。AIM： To determine the pharmacokinetics and distrubution of methylprednisolone sodium succinate（MPS）and its metabolic product methylprednisolone（MP）in eye tissues and blood plasma after MPS periocular injection in rabbits.METHODS： After periocular injection of MPS 10mg, the concentrations for MP and its prodrug conmpound were quantified at different time points using mass spectrum-liquid chromatography in plasma and ocular tissues-slera, choroid and retina, vitreous, iris, aqueous humor, lens and optic nerve.RESULTS： After periocular injection, the time of maximum concentration（Tmax）for MPS in ocular tissues was 0.25 to 1h, in blood plasma was 0.25h. Tmax for its metablite MP in ocular tissues was 0.5 to 6h, in blood plasma was 0.5h. The maximum MPS and MP concentration（Cmax）and the area under the curve（AUC0-t）in ocular tissues from high to low in turn was sclera, optic nerve, the choroid and the retina, iris and lens. The drug concentration of lens was not only the lowest among all tissues, but also much lower than others by far the content, and its mean residence time was the longest.CONCLUSION： Periocular administration of MPS is an effective way to intraocular drug transmission. It achieves a satisfactory drug distribution in sclera, optic nerve, choroid and retina. It is not easily absorbed by lens.

关 键 词：球周注射 琥珀酸甲泼尼龙 药代动力学 

分 类 号：R969[医药卫生—药理学]