Department of Ocular Pharmacology and Pharmacy, Dr Rajendra Prasad Centre for Ophthalmic Sciences, All India Institute of Medical Sciences, New Delhi, India.
Drugs R D. 2010;10(2):93-6. doi: 10.2165/11539310-000000000-00000.
Neuroprotection for glaucoma is a therapeutic approach that aims to prevent optic nerve damage or cell death. An appropriate drug that reaches an adequate concentration across the blood retinal barrier is expected to shield the retina in glaucoma. Several in vitro and in vivo attempts in experimental models indicate the possibility of successful neuroprotection. However, clinical trials might not show the same level of neuroprotection as a result of subtherapeutic concentrations of the drug in the eye. The study by Zhong et al. in this issue of Drugs in R&D could not attribute the observed improvement in visual field indices to any one of the individual active constituents of Erigeron breviscapus (vant.) Hand. Mazz. (EBHM). One of the major constituents of EBHM is scutellarin, which is known to have poor oral bioavailability and an unclear ability to penetrate inside the eye. Therefore, before recognizing EBHM as a neuroprotectant in glaucoma for further clinical studies and practice, its active constituents and their pharmacokinetics (systemic as well as ocular) need to be explored.
神经保护治疗青光眼是一种旨在预防视神经损伤或细胞死亡的治疗方法。人们期望一种合适的药物能够穿过血视网膜屏障达到足够的浓度,从而保护青光眼患者的视网膜。在实验模型中,已经进行了一些体外和体内的尝试,表明神经保护是可行的。然而,临床试验可能不会显示出相同水平的神经保护效果,因为药物在眼部的浓度低于治疗水平。本期《研发中的药物》杂志中 Zhong 等人的研究表明,观察到的视野指数的改善不能归因于短葶飞蓬(vant.)Hand. Mazz.(EBHM)的任何一种单一活性成分。EBHM 的主要成分之一是野黄芩苷,已知其口服生物利用度差,进入眼睛内部的能力也不清楚。因此,在将 EBHM 确认为治疗青光眼的神经保护剂并进一步进行临床研究和实践之前,需要探索其活性成分及其药代动力学(全身和眼部)。