A novel approach to formulation factor of aceclofenac eye drops efficiency evaluation based on physicochemical characteristics of in vitro and in vivo permeation
A novel approach to formulation factor of aceclofenac eye drops efficiency evaluation based on physicochemical characteristics of in vitro and in vivo permeation
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DOI：
10.1016/j.jsps.2013.03.001
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发表时间：
2014-07-01
影响因子：
4.1
通讯作者：
Paliwal, Sarvesh
中科院分区：
文献类型：
--
作者：
Dave, Vivek;Paliwal, Sarvesh
本研究的目的是通过切除的山羊角膜来评估醋氯芬酸滴眼剂。将配方的pH值从6.0提高到8.0，不同防腐剂的作用或粘度增强剂的作用会降低表观渗透系数。局部眼科非甾体抗炎药用于治疗眼表和眼前节炎症以及术后疼痛和炎症的治疗。醋氯芬酸独特的化学结构使其既是一种有效的抗炎药，又是一种可渗透眼组织的亲脂性分子，可确保缓解白内障、屈光手术和角膜擦伤时的疼痛。醋氯芬酸药物的辛醇/水分配系数为1.86+/-0.75。通过将 1 ml 制剂放置在新鲜切除的山羊角膜上（固定在全玻璃改进的 Franz 扩散池的供体和受体室之间）并在 120 分钟后通过分光光度法在 275 nm 处测量受体中渗透的药物来评估药物的渗透特性。结果表明，含有 BAC 的醋氯芬酸眼用溶液（pH 7）可增加通过山羊角膜的体外眼部利用率。在磷酸盐缓冲液中配制的醋氯芬酸滴眼液 0.1% 中对羟基苯甲酸甲酯和对羟基苯甲酸丙酯 MP-PP 防腐剂的组合可增加经角膜渗透。通过体内测量研究，评估了所开发制剂在白化兔中的药效学，并与市售的 voltrane 眼用溶液进行比较。 (C) 2013 年由 Elsevier B.V. 代表沙特国王大学制作和主办。
The purpose of the present study was to evaluate aceclofenac eye drop through excised goat cornea. Raising pH of the formulation from 6.0 to 8.0, effect of different preservatives or effect of viscosity enhancer decreases apparent permeability coefficient. Topical ophthalmic NSAID are used to treat ocular surface and anterior segment inflammation as well as post operative management of pain and inflammation. Aceclofenac's unique chemical structure makes it both a potent anti inflammatory drug and lipophilic molecule that penetrates ocular tissue, ensuring relief of pain in cataract and refractive surgery and corneal abrasion. The octanol/water partition coefficient of aceclofenac drug is 1.86 +/- 0.75. Permeation characteristics of the drug were evaluated by putting 1 ml formulation on freshly excised goat cornea fixed between donor and receptor compartments of an all-glass modified Franz diffusion cell and measuring the drug permeated in the receptor by spectrophotometry at 275 nm, after 120 min The results suggest that aceclofenac ophthalmic solution (pH 7) containing BAC provides increased in vitro ocular availability through goat corneas. The combination of methyl paraben and propyl paraben MP-PP preservative in aceclofenac ophthalmic eye drop 0.1% formulated in phosphate buffer increases transcorneal permeation. The developed formulations were evaluated for their pharmacodynamics in albino rabbits, by measuring in-vivo study and were compared to a marketed voltrane ophthalmic solution. (C) 2013 Production and hosting by Elsevier B.V. on behalf of King Saud University.