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首页> 外文期刊>Acta ophthalmologica >The penetration and distribution of topical atropine in animal ocular tissues
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The penetration and distribution of topical atropine in animal ocular tissues

机译:动物眼组织局部阿托品的渗透与分布

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Abstract Purpose To conduct a multi‐tissue investigation on the penetration and distribution of topical atropine in myopia treatment, and determine if atropine is detectable in the untreated contralateral eye after uniocular instillation. Methods Nine mature New Zealand white rabbits were evenly divided into three groups. Each group was killed at 5, 24 and 72?hr, respectively, following uniocular instillation of 0.05?ml of 1% atropine. Tissues were sampled after enucleation: conjunctiva, sclera, cornea, iris, ciliary body, lens, retina, aqueous, and vitreous humors. The assay for atropine was performed using liquid chromatography‐mass spectrometry ( LC ‐ MS ), and molecular tissue distribution was illustrated using matrix‐assisted laser desorption ionization‐imaging mass spectrometry ( MALDI ‐ IMS ) via an independent experiment on murine eyes. Results At 5?hr, the highest (mean?±?SEM) concentration of atropine was detected in the conjunctiva (19.05?±?5.57?ng/mg, p??0.05) with a concentration gradient established anteriorly to posteriorly, as supported by MALDI ‐ IMS . At 24?hr, preferential binding of atropine to posterior ocular tissues occurred, demonstrating a reversal of the initial concentration gradient. Atropine has good ocular bioavailability with concentrations of two magnitudes higher than its binding affinity in most tissues at 3?days. Crossing‐over of atropine to the untreated eye occurred within 5?hr post‐administration. Conclusion Both transcorneal and transconjunctival‐scleral routes are key in atropine absorption. Posterior ocular tissues could be important sites of action by atropine in myopic reduction. In uniocular atropine trials, cross‐over effects on the placebo eye should be adjusted to enhance results reliability. Combining the use of LC ‐ MS and MALDI ‐ IMS can be a viable approach in the study of the ocular pharmacokinetics of atropine.
机译:摘要目的是对近视治疗中局部阿托品渗透和分布进行多组织调查,并确定在单轴滴注后未经处理的对侧眼中可检测到阿托品。方法九个成熟的新西兰白兔均匀分为三组。每组在5,24和72℃下杀死,分别在单轴滴注0.05?ml的1%阿托品后。组织在enucleation后取样:结膜,巩膜,角膜,鸢尾,睫状体,镜片,视网膜,水性和玻璃体幽默。使用液相色谱 - 质谱(LC - MS)进行阿托嘌呤的测定,并使用基质辅助激光解吸离子化 - 成像质谱(MALDI-IMS)通过鼠眼的独立实验说明分子组织分布。结果在5?小时,在结膜(19.05→±5.57→Ng / mg,p≤m2 5.57,p 1 5.57×5.57℃)中检测到最高(平均值?±ΔMem)浓度的浓度浓度梯度。马尔迪 - IMS支持。在24℃下,发生阿托哌妥的优先结合到后眼部组织,证明了初始浓度梯度的逆转。阿托品具有良好的眼部生物利用度,其浓度高于其在3℃的大多数组织中的结合亲和力。在施用后5μlHR后,阿巴罗过度的过度接触发生在未经治疗的眼内。结论跨划​​伤和跨跨度 - 巩膜途径都是阿托品吸收的关键。后眼部组织可能是阿托品在近视减少中的重要作用。在无奇曲线试验中,应调整安慰剂眼的交叉影响,以提高结果可靠性。结合LC - MS和MALDI - IMS的使用可以是在阿托品的眼镜药代动力学研究中成为一种可行的方法。

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