Al-Mogherah Arwa Ibrahim, Ibrahim Mohamed Abbas, Hassan Maha Abdelazeem
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University 71526 Assiut, Egypt.
Saudi Pharm J. 2020 Nov;28(11):1374-1382. doi: 10.1016/j.jsps.2020.09.001. Epub 2020 Sep 12.
Three factors, three levels (3) full factorial design was used to develop venlafaxine HCl fast dissolving oral films (FDOFs) to optimize the concentrations of the film forming polymer; hydroxypropyl methylcellulose HPMC (X1), superdisintegrant; sodium starch glycolate SSG, (X2) and glycerol as the film plasticizer (X3). Effects of the three factors on the disintegration time (Y1), swelling index (Y2), and dissolution efficiency at 15 min; DE%15 (Y3) of the prepared FDOFs were evaluated by using statistical models. The optimized film formula was characterized in term of x-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and morphological characteristics. Disintegration time was found to increase with the increase in HPMC (X1) concentration, and the shortest disintegration time (21.67 ± 2.08 s) was observed in case of F2 formula (lowest HPMC level and highest glycerol level in absence of SSG). The highest swelling index (3.64 ± 0.59) was observed in case of film formula F1 (medium concentrations of both HPMC and glycerol and highest SSG concentration. The results also indicated that as the concentration of HPMC increased the DE%15 decreased. SSG (X2), with highest value (72.33 ± 1.71%) was recorded for in case of F12 (using 2% HPMC, 5%SSG and 1.5% glycerol). The optimized FDOF formula derived by the statistical models suggested 2% HPMC, 5% SSG, and 1% glycerol. The data obtained from DSC and XRPD revealed no interaction between drug and FDOT excipients. In addition, XRPD studies proved that the venlafaxine HCl was homogeneously dispersed in the film matrix.
采用三因素三水平（3³）全因子设计来制备盐酸文拉法辛速溶口腔膜（FDOFs），以优化成膜聚合物羟丙基甲基纤维素（HPMC，X1）、超级崩解剂淀粉乙醇酸钠（SSG，X2）和作为膜增塑剂的甘油（X3）的浓度。通过统计模型评估这三个因素对所制备FDOFs的崩解时间（Y1）、溶胀指数（Y2）和15分钟时的溶出效率DE%15（Y3）的影响。通过X射线粉末衍射（XRPD）、差示扫描量热法（DSC）和形态学特征对优化后的膜配方进行表征。发现崩解时间随HPMC（X1）浓度的增加而增加，在F2配方（在无SSG时HPMC水平最低且甘油水平最高）的情况下观察到最短崩解时间（21.67±2.08秒）。在膜配方F1（HPMC和甘油浓度均为中等且SSG浓度最高）的情况下观察到最高溶胀指数（3.64±0.59）。结果还表明，随着HPMC浓度的增加，DE%15降低。在F12（使用2%HPMC、5%SSG和1.5%甘油）的情况下记录到SSG（X2）的最高值（72.33±1.71%）。由统计模型得出的优化FDOF配方为2%HPMC、5%SSG和1%甘油。从DSC和XRPD获得的数据表明药物与FDOF辅料之间无相互作用。此外，XRPD研究证明盐酸文拉法辛均匀分散在膜基质中。
