Nair Anroop B, Al-Dhubiab Bandar E, Shah Jigar, Jacob Shery, Saraiya Vismay, Attimarad Mahesh, SreeHarsha Nagaraja, Akrawi Sabah H, Shehata Tamer M
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Department of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, Gujarat, India.
Saudi Pharm J. 2020 Feb;28(2):201-209. doi: 10.1016/j.jsps.2019.11.022. Epub 2019 Dec 7.
Administration of almotriptan as an oral therapy is largely limited because of poor aqueous solubility and rather low bioavailability. The aim of present investigation was to formulate oral mucoadhesive film of almotriptan to improve the drug delivery and desired therapeutic effects. Placebo films (F1-F8) were prepared by varying the concentrations of Proloc 15 (7.5-15% w/v) and Eudragit RL 100/RS 100 (15-30% w/v) polymers. Physicomechanical and pharmaceutical characteristics of drug loaded films (FA1-FA4) were examined. Selected FA4 film was evaluated by assessing the pharmacokinetic profile and compared with oral therapy in rabbits. FA1-FA4 films exhibited excellent physicomechanical properties and rapid hydration. A biphasic and considerably greater drug release (p < 0.05) was observed in FA3 and FA4 films contain higher amount of hydrophilic polymer. The rate of permeation of almotriptan was found to be significantly higher in FA4 than FA3 film (p < 0.005). Fourier transform infrared spectral scan indicates no incompatibility exists between the drug and polymers used. Differential scanning calorimetry thermogram represents the evidence of almotriptan amorphization and molecular dispersion of it in the film. Scanning electron microscopy images shows that FA4 possess good morphological features and hence suitable for use in the buccal application. data demonstrated rapid and efficient absorption (p < 0.005) of almotriptan with greater AUC (>2 folds, p < 0.0001) by FA4 film as compared to oral (control). In general, the data established the potential of FA4 film to improve the therapeutic delivery of almotriptan and offers a promising option in migraine therapy.
阿莫曲坦作为口服疗法的应用在很大程度上受到限制，因为其水溶性差且生物利用度较低。本研究的目的是制备阿莫曲坦口腔黏膜黏附膜，以改善药物递送和达到预期的治疗效果。通过改变普罗洛克15（7.5 - 15% w/v）和尤特奇RL 100/RS 100（15 - 30% w/v）聚合物的浓度制备了空白膜（F1 - F8）。对载药膜（FA1 - FA4）的物理机械和药学特性进行了研究。通过评估药代动力学特征对选定的FA4膜进行评价，并与兔口服疗法进行比较。FA1 - FA4膜表现出优异的物理机械性能和快速水合作用。在含有较高亲水性聚合物的FA3和FA4膜中观察到双相且显著更高的药物释放（p < 0.05）。发现阿莫曲坦在FA4膜中的渗透速率明显高于FA3膜（p < 0.005）。傅里叶变换红外光谱扫描表明所用药物与聚合物之间不存在不相容性。差示扫描量热法热谱图显示了阿莫曲坦非晶化及其在膜中的分子分散的证据。扫描电子显微镜图像表明FA4具有良好的形态特征，因此适用于口腔给药。数据表明，与口服（对照）相比，FA4膜能使阿莫曲坦快速有效吸收（p < 0.005），且AUC更大（>2倍，p < 0.0001）。总体而言，数据证实了FA4膜在改善阿莫曲坦治疗递送方面的潜力，并为偏头痛治疗提供了一个有前景的选择。
