毛果芸香碱透明质酸钠药膜药代动力学研究  

Pharmacokinetics of pilocarpine membrane with sodium hyaluronate in rabbit eyes

作　　者：黄丽娜[1] 翁宏[1] 成洪波[1] 赖铭莹[1] 

机构地区：[1]暨南大学附属深圳市眼科医院,深圳518001

出　　处：《眼科》2008年第4期283-285,共3页Ophthalmology in China

基　　金：深圳市科技计划项目(JH200505310588A)

摘　　要：目的探讨2%毛果芸香碱透明质酸钠药膜在兔眼的药代动力学特征,评价其相对生物利用度。设计实验性研究。研究对象48只健康白兔。方法48只兔随机分成实验组和对照组,每组24只兔。分别给兔眼结膜囊内嵌入2%毛果芸香碱透叫质酸钠药膜和滴入4%毛果芸香碱凝胶滴眼液。评价用药后兔眼刺激症状得分、瞳孔大小,并于给药后0.5、1、3、6、12、24、48及72h时抽取房水,每组各时间点随机选取3只兔(6眼),用反相高效液相色谱法(HPLC)测定房水中的毛果芸香碱浓度。主要指标兔眼刺激症状,瞳孔大小,房水药物浓度。结果实验组与对照组比较兔结膜充血症状无显著性差异(P>0.05);瞳孔缩小持续时间分别为(54.78±4.52)h、(21.33±2.28)h(P<0.01);药物房水达峰时间分别为30min和3h,达峰浓度分别为(18.44±9.56)μg/ml、(16.61±4.92)μg/ml。结论2%毛果芸香碱透明质酸钠药膜可明显提高毛果芸香碱的生物利用度,减少用药频率,并具有临床开发应用的前景。Objective To study the pharmacokinetics of 2% pilocarpine membrane with sodium hyaluronate in rabhit eyes. Design Experimental study. Participants 48 albino rabbits. Methods 48 albino rabbits were divided into 2 groups randomly, received respec- tively pilocarpine membrane with sodium hyaluronate, pilocarpine hydrochloride ophthalmic gel. The aqueous humor was withdrawn from 3 rabbits （6 eyes） respectively at 0.5, 1, 3, 6, 12, 24, 48 and 72 hours after instillation. The drug was analyzed with reversed phase high pressure liquid chromatography （HPLC）. Main Outcome Measures The conjunctival congestion symptoms of rabbit, the size of pupil, concentration of piloearpine in aqueous humor. Results The conjunctiva congestion symptoms of rabbit between two groups had no statistical significance （P〉0.05）. The duration of pupil contraction in experimental group （54.78±4.52 hours） was longer than that in control group （21.33±2.28 hours）（P〈0.01）. The peak concentration of pilocarpine in aqueous humor were （18.437±9.560） μg/ml at 3 hours in the experimental group. Whereas in the control group the peak concentration of pilocarpine in aqueous humor were （16.610±4. 924） μg/ml at 30 minutes. Measurable amounts of drug were still observed at 72 hours in the experimental group. Conclusion 2% pilocarpine membrane with sodium hyaluronate significantly increases ocular bioavailability. It shows that 2% pilocarpine membrane might prolong the drug activity, decrease frequency of administration.

关 键 词：毛果芸香碱 透明质酸钠 药代动力学 生物利用度 

分 类 号：R96[医药卫生—药理学]