马来酸噻吗洛尔凝胶的制备及体外透皮性  

Preparation and in vitro transdermal of Timolol maleate gel

作　　者：接丽莉 杨跃辉[2] 魏斌斌[1] JIE Lili;YANG Yuehui;WEI Binbin(School of Pharmacy,China Medical University,Shenyang,Liaoning,110122 P.R.China;Shengjing Hospital of China Medical University,Shenyang,Liaoning,110004 P.R.China)

机构地区：[1]中国医科大学药学院,辽宁沈阳110122 [2]中国医科大学附属盛京医院,辽宁沈阳110004

出　　处：《华西药学杂志》2022年第4期365-369,共5页West China Journal of Pharmaceutical Sciences

摘　　要：目的以马来酸噻吗洛尔为模型药物制备凝胶剂,考察其体外透皮性和稳定性。方法采用处方单因素考察和正交设计的方法,筛选出性质稳定、安全无刺激的辅料,确定凝胶的最优处方和工艺;以离体动物皮肤24 h累积透过量为指标,考察凝胶的体外透皮性。结果马来酸噻吗洛尔凝胶的最优处方为:0.5%马来酸噻吗洛尔、1%卡波姆940、5%甘油、10%丙二醇、0.1%羟苯乙酯、1.35%三乙醇胺和适量蒸馏水,制备的凝胶剂均匀细腻,稳定性好,具有较好的体外释放能力。结论马来酸噻吗洛尔凝胶的处方设计合理,性质稳定,体外释药性强,可提高患者的依从性,满足临床实际需求。OBJECTIVE To prepare a gel by using timolol maleate(TM)as model drug,and to investigate its in vitro transdermal performance and stability.METHODS Through formula single factor investigation and orthogonal design experiment,stable and safe gel excipients were found,and the optimal prescription and process were decided.The in vitro transdermability of TM gel was investigated by using the cumulative transdermability of animal skin at 24 h in vitro.RESULTS The optimal formulation of TM gel was as 0.5%TM,1%carbopol 940,5%glycerol,10%propylene glycol,phenethyl estere 0.1%,triethanolamine 1.35%and a proper amount of distilled water.The prepared TM gel was uniform,delicate and stable,as well as of good in vitro release ability.CONCLUSION TM gel has a reasonable prescription design and stable properties,and is satisfying in vitro release ability,which can improve patient compliance and meet clinical needs.

关 键 词：马来酸噻吗洛尔 凝胶 单因素考察 正交设计 经皮给药 影响因素试验 加速试验 长期试验 

分 类 号：R94[医药卫生—药剂学] R917[医药卫生—药学]