Shi Li-Li, Xu Wei-Juan, Cao Qing-Ri, Yang Mingshi, Cui Jing-Hao
Pharmazie. 2014 May;69(5):327-34.
In this work, we developed a sildenafil citrate (SC)-loaded polyvinyl alcohol (PVA)/sodium alginate (ALG-Na) based orodispersible film (ODF) using a solvent casting method. Formulation factors such as the type and amount of plasticizers and disintegrants were optimized on the basis of characteristics of blank ODF, including the disintegration time, elastic modulus (EM) and percentage of elongation (E%). SC-loaded ODF with a loading capacity up to 25 mg in an area of 6 cm2 was prepared and evaluated in terms of mechanical properties, disintegration time and dissolution rate. The surface morphology of ODF was visualized under a scanning electron microscope (SEM). The physicochemical properties of ODF were investigated using X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The blank ODF composed of PVA, polyethylene glycol 400 (PEG 400) and ALG-Na (20:5:2, w/w) had a remarkably short disintegration time of about 20 s. However, the loading of drug extended the disintegration time (100 s) of ODF, while it still maintained satisfactory mechanical properties. SC was homogenously dispersed throughout the films and the crystalline form of drug changed, with strong hydrogen bonding between the drug and carriers. The PVA/ALG-Na based ODF containing SC prepared by the simple solvent casting method might be an alternative to conventional SC tablets for the treatment of male erectile dysfunction.
在本研究中，我们采用溶剂浇铸法制备了一种载有枸橼酸西地那非（SC）的聚乙烯醇（PVA）/海藻酸钠（ALG-Na）口腔崩解膜（ODF）。基于空白ODF的特性，如崩解时间、弹性模量（EM）和伸长率（E%），对增塑剂和崩解剂的类型及用量等配方因素进行了优化。制备了在6 cm²面积上载药量高达25 mg的载SC的ODF，并对其机械性能、崩解时间和溶解速率进行了评估。在扫描电子显微镜（SEM）下观察ODF的表面形态。使用X射线衍射（XRD）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FT-IR）研究ODF的物理化学性质。由PVA、聚乙二醇400（PEG 400）和ALG-Na（20:5:2，w/w）组成的空白ODF崩解时间非常短，约为20 s。然而，药物的载入延长了ODF的崩解时间（100 s），同时仍保持令人满意的机械性能。SC均匀分散在整个薄膜中，药物的晶型发生了变化，药物与载体之间形成了强氢键。通过简单的溶剂浇铸法制备的含SC的PVA/ALG-Na基ODF可能是治疗男性勃起功能障碍的传统SC片剂的替代物。
