CAJ | 학술논문

为了制备具有蛋白药物结肠靶向释放性能的新型药物载体，采用了水相溶液滴定反应法，分别以牛血清白蛋白(BSA)和乳铁蛋白(LF)为模型蛋白质药物，制得壳聚糖/纤维素磷酸钠(NaCS)/三聚磷酸钠(TPP)载药微球。利用电镜SEM和显微镜观测拍照，对微球的表面和截面形貌进行了表征，发现微球球形规则且颗粒大小均一。同时进行了体外药物模拟释放试验，考察了载药微球先后经过模拟胃液、模拟小肠液和模拟结肠液时的释药性能，及不同的释放条件和制造条件对于微球释药性能的影响，尤其考察了不同蛋白药物和不同干燥方式的影响。结果表明由临界点干燥法制得的负载乳铁蛋白(LF)微球在模拟胃液和小肠液释放量中5 h内只释放出不到20%的蛋白药物，而后在结肠模拟液中4 h内释放出蛋白药物80%以上。这些结果表明，壳聚糖/NaCS/TPP体系具有一定的作为结肠靶向药物释放载体的应用潜力。
위료제비구유단백약물결장파향석방성능적신형약물재체，채용료수상용액적정반응법，분별이우혈청백단백(BSA)화유철단백(LF)위모형단백질약물，제득각취당/섬유소린산납(NaCS)/삼취린산납(TPP)재약미구。이용전경SEM화현미경관측박조，대미구적표면화절면형모진행료표정，발현미구구형규칙차과립대소균일。동시진행료체외약물모의석방시험，고찰료재약미구선후경과모의위액、모의소장액화모의결장액시적석약성능，급불동적석방조건화제조조건대우미구석약성능적영향，우기고찰료불동단백약물화불동간조방식적영향。결과표명유림계점간조법제득적부재유철단백(LF)미구재모의위액화소장액석방량중5 h내지석방출불도20%적단백약물，이후재결장모의액중4 h내석방출단백약물80%이상。저사결과표명，각취당/NaCS/TPP체계구유일정적작위결장파향약물석방재체적응용잠력。
In order to develop a novel carrier for the oral colon-specific drug delivery system, a microcapsule composed of chitosan, sodium cellulose sulfate (NaCS) and sodium tripolyphosphate(TPP) was prepared by reaction in aqueous phase. The microscope and SEM observation results show that the microcapsules are in the same size and in spherical form. In vitro protein drug release studies, three kinds of simulated fluids, i.e. simulated gastric fluid (SGF), simulated small intestinal fluid (SIF) and simulated colonic fluid (SCF), were used to evaluate the effects of preparation parameters and delivery conditions on the release performance, especially the effects of drying methods and protein kinds. The results indicate that the microcapsule carrying lactoferrin (LF) dried by critical point drying method shows the best release performance. Less than 20%of LF is released after staying in the SGF and SIF for 5 hours, and then more than 80%of LF is released in the SCF for next 4 hours. The experiments results suggest that chitosan/NaCS/TPP microcapsule is a promising system for protein drug colon-specific delivery.