介孔二氧化锡纳米粒改善非洛地平溶出速率的研究  

Research on Mesoporous SnO2 Nanoparticles in Enhancing Dissolution Rate of Felodipine

作　　者：尚文静 吴超 Shang Wenjing;Wu Chao(Jinzhou Medical University,Jinzhou 121000 China)

机构地区：[1]锦州医科大学

出　　处：《锦州医科大学学报》2020年第1期4-9,共6页Journal of Jinzhou Medical University

基　　金：辽宁省教育厅青年科技人才“育苗”项目，项目编号:JYTQN201919

摘　　要：目的将非洛地平吸附到介孔二氧化锡纳米粒的介孔孔道以改善它的溶解度和体外溶出速率。方法采用模板法制备介孔二氧化锡(μmesoporous SnO 2,MSn)。利用吸附法将非洛地平(felodipine,FDP)载入MSn的介孔孔道中以制备FDP-Msn粉末。通过透射电子显微镜(TEM)分析和表征MSn的形态结构和孔径大小。采用差式扫描量热法(differential scanning calorimetry,DSC)表征药物在介孔孔道中的存在状态。通过体外溶出实验考察MSn对FDP的增溶能力。采用粉末直接压片法制备FDP-MSn片剂,并对粘合剂和崩解剂的种类进行筛选以达到优化处方的目的。结果MSn能够显著减小非洛地平的结晶度,药物是以无定形的状态存在于载体的孔道中。体外溶出实验表明MSn可以使FDP达到非常理想的溶出速率。FDP-MSn自制片剂的质量检查结果符合药典要求。结论MSn作为一种新型安全无机纳米介孔载体,具有改善难溶性药物溶出速率的潜力。Objective To absorb felodipine(FDP)in the pore of mesoporous SnO 2(MSn)nanoparticles to improve the solubillity and dissolution rate in vitro.Methods MSn was synthesized by template method.Adsorption method was used to load FDP into the pore of MSn to prepare FDP-Msn powder.The morphology and pore size of MSn was analyzed and characterized by transmission electron microscopy(TEM).The physical state of FDP in the pore was measured by differential scanning calorimetry(DSC).The dissolution experiments in vitro were carried out to determine the solubilization capacity of MSn for FDP.The direct compression method was used to obtain FDP-MSn tablets.Besides,we screened the types of adhesive and disintegrant to optimize the prescription.Results MSn could significantly reduce the crystallinity of felodipine.The drug existed in the pore of the carrier in an amorphous state.The dissolution experiments in vitro indicated that MSn could make FDP achieve an ideal dissolution rate.The quality inspection results of self-made FDP-MSn tablets were in compliance with the pharmacopoeia requirements.Conclusion As a new type of safe inorganic mesoporous nano-carrier,MSn has the potential to improve the dissolution rate of insoluble drugs.

关 键 词：非洛地平 介孔二氧化锡纳米载体 体外溶出速率 

分 类 号：R91[医药卫生—药学]