Yıldız Simay, Aytekin Eren, Yavuz Burçin, Bozdağ Pehlivan Sibel, Ünlü Nurşen
a Department of Pharmaceutical Technology , Hacettepe University, Faculty of Pharmacy , Ankara , Turkey.
Drug Dev Ind Pharm. 2016;42(6):1008-17. doi: 10.3109/03639045.2015.1104345. Epub 2015 Nov 4.
Orally disintegrating tablets (ODTs) recently have gained much attention to fulfill the needs for pediatric, geriatric, and psychiatric patients with dysphagia. Aim of this study was to develop new ODT formulations containing mirtazapine, an antidepressant drug molecule having bitter taste, by using simple and inexpensive preparation methods such as coacervation, direct compression and to compare their characteristics with those of reference product (Remereon SolTab).
Coacervation method was chosen for taste masking of mirtazapine. In vitro characterization studies such as diameter and thickness, weight variation, tablet hardness, tablet friability and disintegration time were performed on tablet formulations. Wetting time and in vitro dissolution tests of developed ODTs also studied using 900 mL 0.1 N HCl medium, 900 mL pH 6.8 phosphate buffer or 900 mL pH 4.5 acetate buffer at 37 ± 0.2 °C as dissolution medium.
Ratio of Eudragit® E-100 was chosen as 6% (w/w) since the dissolution profile of A1 (6% Eudragit® E-100) was found closer to the reference product than A2 (4% Eudragit® E-100) and A3 (8% Eudragit® E-100). Group D, E and F formulations were presented better results in terms of disintegration time. Dissolution results indicated that Group E and F formulations showed optimum properties in all three dissolution media.
Formulations D1, D4, D5, E3, E4, F1 and F5 found suitable as ODT formulations due to their favorable disintegration times and dissolution profiles.
Developed mirtazapine ODTs were found promising in terms of showing the similar characteristics to the original formulation.
口腔崩解片（ODT）最近备受关注，以满足儿科、老年科和吞咽困难的精神科患者的需求。本研究的目的是通过凝聚法、直接压片法等简单且廉价的制备方法，开发含有米氮平（一种有苦味的抗抑郁药物分子）的新型口腔崩解片制剂，并将其特性与参比产品（瑞美隆速溶片）进行比较。
选择凝聚法对米氮平进行掩味。对片剂制剂进行体外特性研究，如直径、厚度、重量差异、片剂硬度、片剂脆碎度和崩解时间。还使用900 mL 0.1 N盐酸介质、900 mL pH 6.8磷酸盐缓冲液或900 mL pH 4.5醋酸盐缓冲液在37±0.2°C作为溶出介质，对所开发的口腔崩解片进行湿润时间和体外溶出试验。
选择Eudragit® E - 100的比例为6%（w/w），因为发现A1（6% Eudragit® E - 100）的溶出曲线比A2（4% Eudragit® E - 100）和A3（8% Eudragit® E - 100）更接近参比产品。D组、E组和F组制剂在崩解时间方面表现出更好的结果。溶出结果表明，E组和F组制剂在所有三种溶出介质中均表现出最佳性能。
制剂D1、D4、D5、E3、E4、F1和F5因其良好的崩解时间和溶出曲线而被认为适合作为口腔崩解片制剂。
所开发的米氮平口腔崩解片在显示出与原制剂相似的特性方面很有前景。
