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卡波姆940眼用制剂的配方以及模拟泪液对其物理化学性质影响的体外评价

Formulation of Carbopol 940 ophthalmic vehicles, and in vitro evaluation of the influence of simulated lacrimal fluid on their physico-chemical properties.

作者信息

Unlü N, Ludwig A, van Ooteghem M, Hincal A A

机构信息

Department of Pharmaceutical Sciences, UIA, Antwerpen, Belgium.

出版信息

Pharmazie. 1991 Nov;46(11):784-8.

PMID:1811229
Abstract

Carbopol 940 ophthalmic vehicles were prepared in order to investigate the interaction between the simulated lacrimal fluid and the polymer, and to examine the influence of sodium fluorescein - a tracer for the fluorophotometric studies - on the physico-chemical properties of the polymer vehicles. Four kinds of vehicles containing mannitol (5%), sodium fluorescein (0.05%) and disodium edetate (0.01%) were formulated. Physicochemical properties of the preparations including pH, osmolality, surface tension and viscosity were measured after neutralization and sterilization, and also after 1 and 2 weeks, 1, 2 and 3 months of storage at 4 degrees C. The viscosity significantly decreased by adding sodium fluorescein and disodium edetate to Carbopol 940 vehicles. It was observed no significant effect of sterilization and storage on the viscosity, pH and osmolality. Significant change in the flow property of the vehicles was observed when the simulated lacrimal fluid was added. Three concentrations of Carbopol 940 vehicles (0.20%, 0.15% and 0.10%) both containing and not containing disodium edetate were proposed for in vivo evaluation.

摘要

制备了卡波姆940眼用载体,以研究模拟泪液与聚合物之间的相互作用,并考察荧光素钠(用于荧光光度研究的示踪剂)对聚合物载体物理化学性质的影响。配制了四种含有甘露醇(5%)、荧光素钠(0.05%)和依地酸二钠(0.01%)的载体。在中和、灭菌后,以及在4℃下储存1周和2周、1个月、2个月和3个月后,测量制剂的物理化学性质,包括pH值、渗透压、表面张力和粘度。向卡波姆940载体中添加荧光素钠和依地酸二钠后,粘度显著降低。观察到灭菌和储存对粘度、pH值和渗透压没有显著影响。添加模拟泪液后,观察到载体的流动性质发生了显著变化。提出了三种浓度的卡波姆940载体(0.20%、0.15%和0.10%)用于体内评价,其中两种含有依地酸二钠,一种不含依地酸二钠。

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