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Abstract

Preparation and Evaluation of Timolol Maleate Ophthalmic (Resin) In Situ Gel

Author(s): Xiaofeng Yu, Ze He, Ying Bao, Hongfei Liu*, Dandan Zhang and Haibing He
Department of Pharmacy, Jiangsu University, Zhenjiang 212013, 1Department of Pharmacy and Food Engineering, Wuyi University, 2Jiangmen Hongxiao Biomedical Co. Ltd., Jiangmen 529000, 3College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, 4Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, 5Jiangsu Haizhihong Biomedical Co. Ltd., Nantong 226001, China

Correspondence Address:
Hongfei Liu, Department of Pharmacy and Food Engineering, Wuyi University, Jiangmen 529000, China, E-mail: articlepharmacyliu@163.com


This study aimed to develop a cation-exchange resin suitable for pharmaceutical excipients, with an appropriate particle size to create an in situ gel of timolol maleate, enhancing its safety and efficacy for ophthalmic use. A cation-exchange resin was prepared using dispersion seed swelling and sulfonation. This resin served as a carrier to form timolol maleate drug resin complexes by bath method. The star design effect surface method was employed to optimize the gel formulation, resulting in an in situ thermosensitive gel. Additionally, the intraocular hypertension model of New Zealand rabbits was investigated with the objective of reducing intraocular pressure. The study successfully produced cation-exchange resins with a particle size below 10 μm, suitable for ophthalmic application. The drug content of homemade gel drug content ranged from 97.69 % to 99.37 %, with a cumulative release of 93.07 % over 10 h. Compared to commercially available eye drops, the homemade gel demonstrated prolonged residence time and better sustained intraocular pressure reduction effect.

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