当前位置: X-MOL 学术Saudi Pharm. J. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Optimization and evaluation of venlafaxine hydrochloride fast dissolving oral films
Saudi Pharmaceutical Journal ( IF 3.0 ) Pub Date : 2020-09-12 , DOI: 10.1016/j.jsps.2020.09.001
Arwa Ibrahim Al-Mogherah , Mohamed Abbas Ibrahim , Maha Abdelazeem Hassan

Three factors, three levels (33) 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.



中文翻译:

盐酸文拉法辛快速溶解口腔膜的优化与评价

使用三因素,三水平(3 3)全因子设计来开发盐酸文拉法辛快速溶解口腔膜(FDOF),以优化成膜聚合物的浓度;羟丙基甲基纤维素HPMC(X1),超崩解剂;淀粉乙醇酸钠SSG(X2)和甘油作为薄膜增塑剂(X3)。这三个因素对15分钟时的崩解时间(Y1),溶胀指数(Y2)和溶出效率的影响;使用统计模型评估了制备的FDOF的DE%15(Y3)。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的薄膜配方进行了表征。

发现崩解时间随着HPMC(X1)浓度的增加而增加,并且在F2配方的情况下观察到最短的崩解时间(21.67±2.08 s)(在没有SSG的情况下,最低的HPMC水平和最高的甘油水平)。薄膜配方为F1时,溶胀指数最高(3.64±0.59)(HPMC和甘油的中浓度和SSG浓度最高)。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,记录的最高值(72.33±1.71%)。统计模型得出的优化FDOF公式建议为2%HPMC,5%SSG和1%甘油。

从DSC和XRPD获得的数据表明药物与FDOT赋形剂之间没有相互作用。此外,XRPD研究证明文拉法辛HCl均匀分散在薄膜基质中。

更新日期:2020-11-17
down
wechat
bug