Department of Physical Chemistry II. Pharmacy Faculty, Biofuncional Studies Institute, Complutense University, Paseo Juan XXIII, 1, 28040 Madrid, Spain.
Center of Biomaterials, University of Havana Ave. Universidad s/n entre G y Ronda, Vedado, 10400 La Habana, Cuba.
Molecules. 2017 Nov 15;22(11):1980. doi: 10.3390/molecules22111980.
Venlafaxine controlled drug delivery systems using different matrixes have been tested to reduce undesirable side effects in the treatment of depression. The legal status of chitosan (Cs) in Pharmacy has dramatically improved after its acceptance as excipient in several and, therefore, there is great interest in pharmaceutical formulations based on this polymer. In this paper, chitosan microcapsules cross-linked with sodium tripolyphosphate (TPP) for oral delivery of venlafaxine were formulated using the spray drying technique. The effect of chitosan physico-chemical properties, TPP concentration and TPP/Cs ratio on drug release was evaluated. The microcapsules were characterized in terms of size, zeta potential and morphology. The physical state of the drug was determined by X-ray diffraction (XRD) and the drug release from the microcapsules was studied in simulated gastric and intestinal fluids. The release pattern fitted well to the Peppas-Koersmeyer model with n exponents indicating anomalous transport.
已测试使用不同基质的文拉法辛控释给药系统,以减少治疗抑郁症的不良副作用。壳聚糖 (Cs) 在药学中的法律地位在被接受为几种药物的赋形剂后得到了显著改善,因此,基于这种聚合物的药物制剂引起了极大的兴趣。在本文中,使用喷雾干燥技术制备了用三偏磷酸钠 (TPP) 交联的壳聚糖微胶囊,用于文拉法辛的口服给药。研究了壳聚糖物理化学性质、TPP 浓度和 TPP/Cs 比对药物释放的影响。微胶囊的粒径、zeta 电位和形态学特征。通过 X 射线衍射 (XRD) 确定药物的物理状态,并研究了微胶囊在模拟胃液和肠液中的药物释放情况。释放模式符合 Peppas-Koersmeyer 模型,指数 n 表明存在异常传递。