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制药技术可将传统药物地塞米松转变为一线眼科用药。全球视角与未来趋势。

Pharmaceutical technology can turn a traditional drug, dexamethasone into a first-line ocular medicine. A global perspective and future trends.

作者信息

Rodríguez Villanueva Javier, Rodríguez Villanueva Laura, Guzmán Navarro Manuel

机构信息

Biomedical Sciences Department, Pharmacy and Pharmaceutical Technology Unit, Faculty of Pharmacy, University of Alcalá, Ctra. de Madrid-Barcelona (Autovía A2) Km. 33,600, 28805 Alcalá de Henares, Madrid, Spain; Faculty of Pharmacy, University of Alcalá, Ctra. de Madrid-Barcelona (Autovía A2) Km. 33,600 28805 Alcalá de Henares, Madrid, Spain.

Faculty of Pharmacy, University of Alcalá, Ctra. de Madrid-Barcelona (Autovía A2) Km. 33,600 28805 Alcalá de Henares, Madrid, Spain.

出版信息

Int J Pharm. 2017 Jan 10;516(1-2):342-351. doi: 10.1016/j.ijpharm.2016.11.053. Epub 2016 Nov 23.

Abstract

Dexamethasone is one of the most prescribed glucocorticoids. It is effective and safe in the treatment of a wide variety of ocular conditions, including anterior and posterior segment inflammation. However, its half-life in the vitreous humor is very short, which means that it typically requires frequent administrations, thus reducing patient adherence and causing therapeutic failure. Innovative dexamethasone delivery systems have been designed in an attempt to achieve sustained release and targeting. The FDA has approved dexamethasone implants for the treatment of macular edema secondary to retinal vein occlusion and posterior segment noninfectious uveitis. Lenses, micro- and nanoparticles, liposomes, micelles and dendrimers are also proving to be adequate systems for maintaining optimal dexamethasone levels in the site of action. Pharmaceutical technology is turning a classical drug, dexamethasone, into a fashionable medicine.

摘要

地塞米松是最常用的糖皮质激素之一。它在治疗多种眼部疾病(包括眼前段和眼后段炎症)方面有效且安全。然而,它在玻璃体液中的半衰期非常短,这意味着通常需要频繁给药,从而降低了患者的依从性并导致治疗失败。已设计出创新的地塞米松给药系统,试图实现持续释放和靶向给药。美国食品药品监督管理局(FDA)已批准地塞米松植入剂用于治疗视网膜静脉阻塞继发的黄斑水肿和眼后段非感染性葡萄膜炎。此外,透镜、微米和纳米颗粒、脂质体、胶束和树枝状大分子也被证明是在作用部位维持最佳地塞米松水平的合适系统。制药技术正在将经典药物地塞米松转变为一种时尚药物。

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