李瑞,万龙,姜海涛,熊智灵,姜同英,王思玲
LI Rui,WAN Long,JIANG Hai-tao,XIONG Zhi-ling,JIANG Tong-ying,WANG Si-ling*(School of Pharmacy

• 1:沈阳药科大学药学院

摘要(Abstract)：

目的考察不同载药方法对介孔二氧化钛纳米粒载药系统载药和溶出速率的影响。方法通过溶剂挥干法、熔融法、吸附平衡法分别将卡维地洛包载于介孔二氧化钛纳米粒中,用扫描电镜和透射电镜观测样品形貌,氮气吸附-解吸法测量载体的比表面积和孔体积,差示扫描量热法分析药物粒子的存在状态,X-射线衍射法进行物相分析,热失重法分析载药量,最后测定载药系统的溶出速率并进行长期稳定性试验。结果三种载药方法均能通过改变药物的存在状态使药物以非晶型存在于载体中而达到提高溶出速率的目的。其中溶剂挥干法所得的载药系统溶出速率提高显著,并且更具有长期稳定性。结论溶剂挥干法为介孔二氧化钛纳米粒载药的首选。
Objective To test the effect on drug loading and dissolution of mesoporous titania nanoparticles(MTNs)by different drug loading methods.Methods Solvent deposition method,melt method and incipient wetness impregnation method were employed to load the model drug carvedilol(CAR)into MTNs,then scanning electron microscopy(SEM)and transmission electron microscopy(TEM)were employed to observe the morphology and structure of MTNs.Nitrogen adsorption/desorption was recorded to determine the micopore volume and the specific surface area of MTNs.Differential Scanning Calorimetry(DSC)and X-ray diffraction(XRD)test were employed to study the physical state of drug.Thermogravimetric Analysis(TGA)was employed to determine the drug content.At last the in vitro dissolution test and long-lasting stability test were performed.Results All of the three methods could enhance the in vitro dissolution rate by change the physical state of the drug in carriers from crystal to noncrystal.But the carriers loaded with drugs prepared by solvent deposition method obtained a higher dissolution rate and more long-lasting stability.Conclusion The solvent deposition method is the primary choice to load drugs in MTNs.

关键词(KeyWords)： 介孔二氧化钛纳米粒;难溶性药物;载药方法;溶出速率
mesoporous titania nanoparticle;water insoluble drug;drug loading method;in vitro dissolution rate

Abstract:

Keywords:

基金项目(Foundation): 国家基础科学人才培养基金项目(J1103606)

作者(Author): 李瑞,万龙,姜海涛,熊智灵,姜同英,王思玲
LI Rui,WAN Long,JIANG Hai-tao,XIONG Zhi-ling,JIANG Tong-ying,WANG Si-ling*(School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2013.06.010

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