Koland M, Sandeep Vp, Charyulu Nr
Department of Pharmaceutics, Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences, Mangalore - 574 160, Karnataka, India.
J Young Pharm. 2010 Jul;2(3):216-22. doi: 10.4103/0975-1483.66790.
Ondansetron hydrochloride, a 5 HT3 antagonist is a powerful antiemetic drug which has oral bioavailability of 60% due to hepatic first pass metabolism and has a short half-life of 5 h. To overcome the above draw back, the present study was carried out to formulate and evaluate fast dissolving films of ondansetron hydrochloride for sublingual administration. The films were prepared from polymers such as polyvinylalcohol, polyvinyl pyrrolidone, Carbopol 934P in different ratios by solvent casting method. Propylene glycol or PEG 400 as plasticizers and mannitol or sodium saccharin as sweeteners were also included. The IR spectral studies showed no interaction between drug and polymer or with other additives. Satisfactory results were obtained when subjected to physico-chemical tests such as uniformity of weight, thickness, surface pH, folding endurance, uniformity of drug content, swelling index, bioadhesive strength, and tensile strength. Films were also subjected to in vitro drug release studies by using USP dissolution apparatus. Ex vivo drug permeation studies were carried out using porcine membrane model. In vitro release studies indicated 81-96% release within 7 min and 66-80% within 7 min during ex vivo studies. Drug permeation of 66-77% was observed through porcine mucosa within 40 min. Higher percentage of drug release was observed from films containing the sweeteners. The stability studies conducted for a period of 8 weeks showed no appreciable change in drug content, surface pH, and in vitro drug release.
盐酸昂丹司琼是一种5-羟色胺3（5 HT3）拮抗剂，是一种强效止吐药，由于肝脏首过代谢，其口服生物利用度为60%，半衰期短，仅5小时。为克服上述缺点，本研究开展了盐酸昂丹司琼口腔崩解膜的研制与评价，用于舌下给药。采用溶剂浇铸法，以不同比例的聚乙烯醇、聚乙烯吡咯烷酮、卡波姆934P等聚合物制备薄膜。还加入了丙二醇或聚乙二醇400作为增塑剂，甘露醇或糖精钠作为甜味剂。红外光谱研究表明，药物与聚合物或其他添加剂之间没有相互作用。薄膜进行重量均匀性、厚度、表面pH值、耐折性、药物含量均匀性、溶胀指数、生物粘附强度和拉伸强度等理化测试时，结果令人满意。薄膜还采用美国药典溶出装置进行体外药物释放研究。采用猪膜模型进行离体药物渗透研究。体外释放研究表明，7分钟内释放率为81-96%，离体研究中7分钟内释放率为66-80%。40分钟内通过猪黏膜的药物渗透率为66-77%。含有甜味剂的薄膜药物释放率更高。为期8周的稳定性研究表明，药物含量、表面pH值和体外药物释放均无明显变化。
