Phares K, Cho M, Johnson K, Swarbrick J
Pharmaceutics Department, University of North Carolina, Chapel Hill 27599-7360, USA.
Pharm Res. 1995 Feb;12(2):248-56. doi: 10.1023/a:1016235111210.
Nylon 610 is a hydrophilic polymer with considerable potential as a membrane for drug microencapsulation. To better understand drug transport through such membrane, the influence of the solvents and monomers used in the synthesis of nylon films were examined using a full factorial study. Nylon 610 films were synthesized by an interfacial polycondensation reaction using hexamethylenediamine (HD) in the water phase and sebacoyl chloride (SC) in the organic phase, which was a solvent blend of chloroform and trichlorotrifluoroethane at ratios of 1:1, 1:4, and 4:1. Monomer concentrations studied were 0.2, 0.4, and 0.6 M with respect to their appropriate phase, while the monomer ratios were 1:1, 3:1, and 1:3. The molecular weight, porosity, thickness, and crystallinity of the films were characterized. The transport of potassium chloride, hydrocortisone, and m-cresol was studied at 25 degrees C as a function of the synthesis variables. Potassium chloride was selected to measure the porosity of the membrane. Hydrocortisone and m-cresol, a known solvent for nylon 610, were used to study pore and solution-diffusion transport, respectively. The molecular weight of the films was proportional to the chloroform concentration. As the molecular weight increased, film thickness, porosity, and hydrocortisone permeability increased. As the molecular weight decreased, film thickness and porosity decreased, while m-cresol permeability increased. These results can be explained on the basis of HD ability to readily partition into a good solvent such as chloroform permitting high molecular weight polymer to form before precipitation.
尼龙610是一种亲水性聚合物，作为药物微囊化的膜材料具有相当大的潜力。为了更好地理解药物通过这种膜的传输，采用全因子研究考察了尼龙膜合成中所用溶剂和单体的影响。尼龙610膜通过界面缩聚反应合成，水相中使用己二胺（HD），有机相中使用癸二酰氯（SC），有机相是氯仿和三氯三氟乙烷按1:1、1:4和4:1比例混合的溶剂。研究的单体浓度相对于各自的相为0.2、0.4和0.6 M，而单体比例为1:1、3:1和1:3。对膜的分子量、孔隙率、厚度和结晶度进行了表征。在25℃下研究了氯化钾、氢化可的松和间甲酚的传输与合成变量的关系。选择氯化钾来测量膜的孔隙率。氢化可的松和间甲酚（尼龙610的已知溶剂）分别用于研究孔隙传输和溶液扩散传输。膜的分子量与氯仿浓度成正比。随着分子量增加，膜厚度、孔隙率和氢化可的松渗透率增加。随着分子量降低，膜厚度和孔隙率降低，而间甲酚渗透率增加。这些结果可以基于己二胺易于分配到诸如氯仿等良溶剂中，从而在沉淀前形成高分子量聚合物的能力来解释。
