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用于马来酸噻吗洛尔控释的聚合物眼用水凝胶和眼用插入剂。

Polymeric ocular hydrogels and ophthalmic inserts for controlled release of timolol maleate.

作者信息

Singh Vinod, Bushetti S S, Raju S Appala, Ahmad Rizwan, Singh Mamta, Ajmal Mohammad

机构信息

SBS PG Institute of Biomedical Sciences and Research, Dehradun, Uttrankhand, India.

出版信息

J Pharm Bioallied Sci. 2011 Apr;3(2):280-5. doi: 10.4103/0975-7406.80773.

Abstract

BACKGROUND

Ophthalmic drug delivery systems are the challenging subject for the researchers because of delicate nature of ocular membrane and preventive barriers leading to less than 1 % of Bioavailability. Reasons for reduced bioavailability are due to rapid pre corneal elimination, tear turnover, lacrimal drainage, blinking and degradation by enzymes. Less bioavailability causes short duration of action and increased frequency of administration.

MATERIALS AND METHODS

Timolol maleate was used as model drug. Dynamic drug release studies were used to study the polymeric hydrogels and ophthalmic inserts. Rheological studies were carried out by Brookfield Viscometer LVDV- II+.

RESULT AND DISCUSSION

Viscosity value lies in the range of 4.08 to 31.8 cps. Drug release data was fitted to various kinetic equations such as First order plots, Higuchi plots, Peppa's exponential plots. The results shows fairly linear curve and the slope value of the Peppa's equation is less than 0.5 and hence follows the fickian diffusion.

CONCLUSION

The developed hydrogels and inserts were therapeutically effacious, stable, non irritant and provide a sustained release of drug over 8 hours time period.

摘要

背景

由于眼膜性质脆弱以及存在预防性屏障,导致生物利用度低于1%,眼科药物递送系统一直是研究人员面临的具有挑战性的课题。生物利用度降低的原因包括角膜前快速消除、泪液更新、泪液引流、眨眼以及酶降解。生物利用度降低会导致作用时间缩短和给药频率增加。

材料与方法

使用马来酸噻吗洛尔作为模型药物。采用动态药物释放研究来研究聚合物水凝胶和眼科插入剂。通过布鲁克菲尔德LVDV-II+粘度计进行流变学研究。

结果与讨论

粘度值在4.08至31.8厘泊范围内。药物释放数据拟合到各种动力学方程,如一级图、 Higuchi图、Peppa指数图。结果显示出相当线性的曲线,Peppa方程的斜率值小于0.5,因此遵循菲克扩散。

结论

所开发的水凝胶和插入剂具有治疗效果、稳定性好、无刺激性,并能在8小时内持续释放药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2342/3103925/14cd79eecaab/JPBS-3-280-g006.jpg

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