摘要
目的观察葛根素滴眼液对家兔高眼压模型的作用和测定房水中葛根素药物浓度。方法兔眼球结膜注射地塞米松形成慢性高眼压模型，兔耳缘静脉注射葡萄糖形成急性高眼压模型，先后滴用10g·L1葛根素滴眼液，观察其降低或抑制高眼压作用；兔眼滴用葛根素滴眼液后。定时抽取房水．用反相高效液相色谱法测定房水中药物浓度。结果10g·L1葛根素滴眼液能降低慢性高眼压兔的眼压；能抑制急性眼压升高；药物滴入兔眼后．能被眼组织吸收进入房水，其高峰浓度（Cmax）为0.963mg·L-1，高峰时间（tmax）为2．0h，半衰期（t1/2β）为8．32h。结论10g·L1葛根素滴眼液通过滴眼用药．能降低地噻米松引起兔眼高压，并能抑制由快速注射葡萄糖引起的眼压升高；药物能被吸收进入房水中．半衰期为8．32h，为该药临床应用提供了依据。
Objective To test wether puerarin eyedrops could lower intraocular pressure (IOP)in animal models and evaluate the level of puerarin in aqueous humor after administration of its topical eyedrops in different times. Methods Chronic ocular hypertension was described previously by dexamethasone (0. 5mg every other day for 3 weeks)injection into the bulbar subconjunctiva of superior comeal margin of rabbit eye; Acute ocular hypertension was induced by rapid intravenous injection of 50g·L-1 glucose 15mg·kg-1. RP-HPLC-UV method was used in determination of the level of puerarin in aqueous humor. Results The potency of IOP hypertension in 10g·L-1 opuerarin group was nearly to that of 5g·L-1 timotimolol, but the effective time maintained for 10 g·L-1 puerarin was longer than that for timolol; The IOP lowering ability of 10g·L-1 puerarin on acute ocular hypertension rabbit was nearly the same as with 5g·L-1 timolol; The pharmackinetic parameters were as following: α＝ 1. 0 h-1,β=0. 083h-1,t1/2α=0. 69h; t/2β=8. 32h. Ka = 5. 06h-1 Cmax=0. 963mg·L-1;AUC=5. 16mg·h-1·L-1; tmax = 2.0 h. Conclusion The 10g·L-1 puerarin eyedrops can decrease IOP hypertention induced by rapidly intravenous injection of glucose and topical dexamethasone. RP-HPLC-UV method is simple and sensitive in the determination of puerarin in aqueons humor.
出处
《眼科新进展》
CAS
1999年第2期73-77,共5页
Recent Advances in Ophthalmology
基金
国家自然科学基金
江苏省科委资助!39570881
关键词
葛根素
滴眼液
眼压
眼房水
药代动力学
puerarin
intraocular pressure
aqueous humor
ocular pharmackinetics
