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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 investigate the pharmacokinetics of 2% pilocarpine sodium hyaluronate in rabbit eyes and evaluate its relative bioavailability. Design experimental research. 48 healthy rabbits. Methods 48 rabbits were randomly divided into experimental group and control group, each group of 24 rabbits. Respectively to the rabbit eye conjunctival sac embedded 2% pilocarpine sodium hyaluronate membrane and dropping 4% pilocarpine gel eye drops. Evaluation of rabbits eye irritation symptoms after treatment, pupil size, and at 0.5,1,3,6,12,24,48 and 72h after administration of aqueous humor, each group at each time point randomly selected 3 rabbits (6 eyes ), And the concentration of pilocarpine in aqueous humor was determined by reversed-phase high performance liquid chromatography (HPLC). The main indicators Rabbit eye irritation symptoms, pupil size, aqueous humor concentration. Results Compared with the control group, there was no significant difference in conjunctival hyperemia (P> 0.05). The duration of miosis was (54.78 ± 4.52) h and (21.33 ± 2.28) h respectively (P <0.01) The peak time was 30min and 3h, respectively. The peak concentrations were (18.44 ± 9.56) μg / ml and (16.61 ± 4.92) μg / ml, respectively. Conclusion 2% pilocarpine sodium hyaluronate film can significantly improve the bioavailability of pilocarpine, reduce the frequency of medication, and has the prospect of clinical development and application.