Zaman Muhammad, Hanif Muhammad, Qaiser Asif Ali
Acta Pol Pharm. 2016 Sep;73(5):1351-1360.
Aim of the present work was to design fast dissolving buccal film of meloxicam using central composite rotatable design and to evaluate the effects of polymer and plasticizer on formulation and characterization of the buccal films. Meloxicam was incorporated in film as model drug, HPMC E15 was used as film forming agent and polyethylene glycol (PEG) 400 was used as plasticizer. Films were fabricated using solvent casting technique. Prepared films were subjected to study various evaluation parameters. Dissolution studies were carried out for 30 min, using phosphate buffer of pH 6.8. Drug-excipients compatibility was studied using Fourier transform infra-red spectroscopy (FTIR). X-ray diffractometry (X-RD) was used to observe the crystalline or amorphous nature of the drug. Differential scanning calorimetry was used for thermal analysis of the drug and films. Optical microscopy and scanning electron microscopy were used to study the surface morphology. Results revealed that apparently the films were of smooth surface with uniform mixing of drug and excipients. Folding fortitude was > 100 in all the formulations. Weight variations were in acceptable range. Moisture loss was directly linked with concentration of plasticizer. Although buccal films were showing rapid release of the drug but still it was noticed that increasing concentration of HPMC E15 was the cause of drug retardation as well as delay in the total dissolution time, while PEG 400 was facilitating the drug release from the formulated films. Formulation F5 released approximately 100% drug in 5 min. All formulations individually showed total dissolving time in the range of 48-120 s. There were no noticeable interactions between drug and excipients. Finally, it was concluded that meloxicam containing films can be optimized using statistical tools, and HPMC E15 in combination with PEG 400 as plasticizer can be effectively used in the films formulation.
本研究的目的是采用中心复合旋转设计法设计美洛昔康速溶口腔膜，并评估聚合物和增塑剂对口腔膜制剂和特性的影响。将美洛昔康作为模型药物加入到膜中，使用羟丙甲纤维素E15作为成膜剂，聚乙二醇（PEG）400作为增塑剂。采用溶剂浇铸技术制备薄膜。对制备的薄膜进行各种评价参数的研究。使用pH 6.8的磷酸盐缓冲液进行30分钟的溶出度研究。采用傅里叶变换红外光谱（FTIR）研究药物-辅料相容性。采用X射线衍射法（X-RD）观察药物的结晶或无定形性质。差示扫描量热法用于药物和薄膜的热分析。光学显微镜和扫描电子显微镜用于研究表面形态。结果表明，薄膜表面明显光滑，药物和辅料混合均匀。所有制剂的折叠强度均>100。重量差异在可接受范围内。水分损失与增塑剂浓度直接相关。虽然口腔膜显示出药物的快速释放，但仍注意到羟丙甲纤维素E15浓度的增加是药物延迟释放以及总溶解时间延迟的原因，而PEG 400则促进了药物从制剂薄膜中的释放。制剂F5在5分钟内释放了约100%的药物。所有制剂的总溶解时间均在48-120秒范围内。药物与辅料之间没有明显的相互作用。最后得出结论，含美洛昔康的薄膜可以使用统计工具进行优化，羟丙甲纤维素E15与PEG 400作为增塑剂联合使用可有效地用于薄膜制剂中。
