马来酸噻吗洛尔眼用即型凝胶的制备及体内外评价  

Preparation, in vitro and in vivo Evaluation of Timolol Maleate Ophthalmic in situ Gel

作　　者：郭家旺[1] 马洋[1] 王健[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2015年第5期477-481,共5页Chinese Journal of Pharmaceuticals

基　　金：国家"重大新药创制"科技重大专项(2012ZX09304004)

摘　　要：联用结冷胶和黄原胶为凝胶基质,制备马来酸噻吗洛尔眼用即型凝胶制剂。采用旋转流变仪测定了制品及其与人工泪液混合物的黏度与模量变化。流变学测定结果显示,以0.4%结冷胶和0.1%黄原胶为基质的载药凝胶的零剪切黏度为2.89 Pa·s,储能模量(G?)小于损耗模量(G?),易于给药;与人工泪液混合后G?大于G?,发生了相转变,形成了凝胶。体内药效试验结果表明,健康Beagle犬眼部给予自制即型凝胶后降眼压效果维持时间大于9 h。An ophthalmic in situ gel loaded with timolol maleate was prepared with gellan gum and xanthan gum as gel matrix. The viscosities and modulus of the gel and a mixture of the gel and simulated tear fluid （STF） were measured by rotary rheometer. The zero-shear viscosity of the drug-loaded product with 0.4% gellan gum and 0.1% xanthan gum as gel matrix was 2.89 Pa·s, and the storage modulus （G） was smaller than the loss modulus （G＂）. After mixed with STF, the G′ increased to be larger than G＂, indicating phase transition occurred and the gel formed. The intraocular pressure-reducing effect of the product was investigated with healthy Beagle dogs as models. The results showed that the effect could maintain for more than 9 h after administration.

关 键 词：马来酸噻吗洛尔 即型凝胶 结冷胶 眼用 降眼压效果 

分 类 号：R944.9[医药卫生—药剂学]