阿替洛尔鼻用凝胶体外释药影响因素考察

Factors Influencing the Release in Vitro of Atenolol Nasal Gel

目的:对影响阿替洛尔鼻用凝胶制剂处方体外释药的因素进行考察,为处方筛选提供依据。方法:考察处方中不同用量的基质卡波姆941(0.8%、1.0%、1.2%)、表面活性剂吐温-80(0、6%、8%)及不同的吸收促进剂二甲基-β-环糊精(DM-β-CD)、β-CD对阿替洛尔鼻用凝胶体外释放度的影响。结果:3种因素对凝胶的体外释放度均有显著影响,以卡波姆941与吐温-80的用量分别为0.8%、6%及10%DM-β-CD作为吸收促进剂可显著提高凝胶的体外释放度。结论:本试验结果可为阿替洛尔鼻用凝胶处方筛选提供依据。

OBJECTIVE： To investigate the factors influencing the drug release of atenolol nasal gel for references of optimization of its formulation. METHODS： The effects of carbopol 941 （0.8%, 1.0% and 1.2% ） which used as the gel stroma, the amount of surface acting agent Tween- 80 （0, 6% and 8% ）, and absorption enhancer （DM-β- CD vs. β- CD） on the in vitro release of atenolol nasal gel were investigated. RESULTS： All the above- mentioned 3 factors had marked effects on the in vitro release of atenolol nasal gel. The in vitro release of atenolol nasal gel was markedly enhanced by 0.8% carbopol 941, 6% Tween- 80 and 10% DM-β- CD absorption enhancer. CONCLUSION： The results in the study serve as references for the optimization of the formulation of atenolol nasal gel.