摘要
目的优化离子交换型缓释微球镶嵌载体蒙脱石对盐酸倍他洛尔的载药条件。方法考察不同的分散方式、载药时间、介质pH值、介质离子浓度及载药温度对盐酸倍他洛尔蒙脱石(betaxolol hydrochloride-montmorillonite,BH-MMT)载药量的影响;设计一系列BH浓度梯度实验拟合BH-MMT的等温吸附模型,筛选出适合的制备条件,并进行体外释放考察BH-MMT缓释性能。结果采用磁力搅拌初步分散,水浴超声30 min的分散方式分散后的粒径为441.9 nm,PDI为0.382;于50℃水浴的条件下,磁力搅拌2 h载药可确保达到载药平衡;介质pH在4~8范围内改变对蒙脱石载药量影响较小,MMT的载药量随着介质离子浓度的增加,逐渐降低。MMT对BH吸附过程属于自发性反应,低温有助于其反应,拟合结果显示Langmuir等温吸附模型对MMT吸附BH的拟合效果更好,R^(2)为0.9998,Freundlich等温吸附模型的R^(2)为0.9739。在体外释放实验中,BH-MMT中的药物于8 h完全释放,释放度达95.25%。结论优化后所制得BH-MMT载药量较大,制备工艺简单易行,能有效延长BH的释放时间,可用作缓释微球的镶嵌载体。
Objective To optimize the drug-loading conditions of ion exchange sustained-release microspheres embedded carrier of montmorillonite for betaxolol hydrochloride.Methods The different dispersion modes,drug loading time,medium pH,ion concentration and drug loading temperature were designed to explore their effects on the drug loading capacity of BH-MMT(betaxolol hydrochloride-montmorillonite,BH-MMT),and a series of BH concentration gradient experiments were designed to fit the isothermal adsorption model of BH-MMT.The suitable preparation conditions were selected,and in vitro release tests was performed to investigate the sustained release performance of BH-MMT.Results The particle size was 441.9 nm and the PDI was 0.382 after initial dispersion with magnetic stirring and water bath ultrasonication for 30 min,and the loading equilibrium was ensured by magnetic stirring for 2 h under the water bath at 50℃.It was found that pH change in the range of 4~8 had a small effect on montmorillonite loading.The drug load of montmorillonite gradually decreased with the increase of ion concentration.MMT was a spontaneous reaction to BH adsorption process,low temperature was helpful for its reaction.The fitting results showed that Langmuir isothermal adsorption model had a better fitting effect on MMT adsorption BH,R²was 0.9998,and the R²of the Freundlich isothermal adsorption model was 0.9739.BH-MMT was completely released in vitro at 8 h,with a release degree of 95.25%.Conclusion The optimized BH-MMT has a large drug loading quantity,a simple and feasible preparation process,which can effectively prolong the release time of BH and be used as the embedded carrier for sustained-release microspheres.
作者
叶菁华
李慧慧
柯远程
秦宏涛
马颖芸
肖梦莎
冼毅盈
侯冬枝
YE Jinghua;LI Huihui;KE Yuancheng;QIN Hongtao;MAYingyun;XIAO Mengsha;XIAN Yiying;HOU Dongzhi(School of Pharmacy,Guangdong Pharmaceutical University/Guangdong Engineering Technology Research Center for Topical Precision Drug Delivery Preparations/Guangdong Key Laboratory of New Drug Dosage Forms,Guangzhou 510006,China)
出处
《广东药科大学学报》
CAS
2023年第5期15-20,共6页
Journal of Guangdong Pharmaceutical University
基金
广东药科大学大学生创新训练计划项目(202210573028)
广东省矿物物理与材料研究开发重点实验室开放课题(GLMPM-047)。
关键词
蒙脱石
盐酸倍他洛尔
离子交换
吸附
释放
montmorillonite
betaxolol hydrochloride
ion exchange
adsorption
release
