Özakar Emrah, Sevinç-Özakar Rukiye, Yılmaz Bilal
Department of Pharmaceutical Technology, Faculty of Pharmacy, Atatürk University, 25240 Erzurum, Turkey.
Department of Analytical Chemistry, Faculty of Pharmacy, Atatürk University, 25240 Erzurum, Turkey.
Gels. 2023 Feb 9;9(2):147. doi: 10.3390/gels9020147.
The oral availability of many drugs is problematic due to the pH of the stomach, enzymes, and first-pass effects through the liver. However, especially geriatric, pediatric, bedridden, or mentally handicapped patients and those with dysphagia have difficulty swallowing or chewing solid dosage forms. Oral Thin Films (OTFs) are one of the new drug delivery systems that can solve these problems. Pregabalin (PG) and Methylcobalamin (MC), which are frequently preferred for pain originating in the central nervous system, were brought together for the first time using OTF technology in this study. In this study, a quantification method for PG and MC was developed and validated simultaneously. Optimum formulations were selected with organoleptic and morphological controls, moisture absorption capacity, swelling capacity, percent elongation, foldability, pH, weight variability, thickness, disintegration time, and transparency tests on OTFs prepared by the solvent pouring method. Content uniformity, dissolution rate, determination of release kinetics, SEM, XRD, FT-IR, DSC, long-term stability, and cytotoxicity studies on the tongue epithelial cell line (SCC-9) were performed on selected OTFs. As a result, OTFs containing PG-MC, which are non-toxic, highly flexible, transparent, compatible with intraoral pH, with fast disintegration time (<30 s), and acceptable in taste and appearance, have been developed successfully.
由于胃的pH值、酶以及肝脏的首过效应,许多药物的口服可用性存在问题。然而,尤其是老年、儿科、卧床或智障患者以及吞咽困难者,吞咽或咀嚼固体剂型存在困难。口腔薄膜(OTF)是能够解决这些问题的新型药物递送系统之一。本研究首次使用OTF技术将常用于中枢神经系统疼痛的普瑞巴林(PG)和甲钴胺(MC)组合在一起。在本研究中,同时开发并验证了PG和MC的定量方法。通过对溶剂浇铸法制备的OTF进行感官和形态控制、吸湿能力、溶胀能力、伸长率百分比、可折叠性、pH值、重量变异性、厚度、崩解时间和透明度测试,选择了最佳配方。对选定的OTF进行了含量均匀度、溶出速率、释放动力学测定、扫描电子显微镜(SEM)、X射线衍射(XRD)、傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)、长期稳定性以及舌上皮细胞系(SCC-9)的细胞毒性研究。结果成功开发出了含有PG-MC的OTF,其无毒、高度柔韧、透明、与口腔内pH值相容、崩解时间快(<30秒),且口感和外观均可接受。