溴莫尼定
苯扎溴铵
色谱法
药物输送
化学
药品
眼压
医学
药理学
眼科
有机化学
作者
A. J. Khopade,Arindam Halder,Vinod Burade,Bharat Pateliya,Kaushal Jani,Vivek Patel,Sudhaker Upadhyay
标识
DOI:10.1016/j.jddst.2022.103594
摘要
Brimonidine is used to lower intraocular pressure (IOP) in glaucoma patients. An ophthalmic Brimonidine formulation was developed to reduce the dosing frequency from three times a day to once a day using a drug/nanoresin complex suspension. Cationic Brimonidine forms complex with Amberlite™ IRP69 resin in an aqueous medium. The resin was milled to nanosize range and characterized for simulated mucous interaction and drug complexation. The drug/nanoresin complex was amorphous and showed ion-triggered release of Brimonidine in presence of tear salts. Nano-resin/drug ophthalmic suspension of 0.35% strength was formulated with excipients that did not interfere with drug/nanoresin complexation. The Brimonidine ophthalmic suspension had a pH value of 6.8–7.2, viscosity value ∼40–80cps, osmolality ∼280–350 mOsm/kg, D50 of 0.190 μm and complied with pharmacopoeial antimicrobial efficacy test. In-vitro release of Brimonidine from nano-resin complex formulation was slower in water than simulated tear fluid. The suspension was stable for 18 months at room temperature. In-vivo animal study showed comparable efficacy of once a day 0.35% nano-resin formulation to three times a day 0.15% solution formulation. There was improved absorption of the drug in aqueous humor which translated to a significantly high peak IOP reduction for a sustained period.
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