Development, Optimization and In Vitro Evaluation of Buccal Tablet of Posaconazole

Buccal route of administration has many advantages such as improving patient compliance, bypassing the GIT and hepatic first pass effect. The objectives are to formulate Mucoadhesive buccal tablet using Posaconazole and compatible excipients, and to evaluate the product using quality control tests and in vitro tests. In the development of buccal tablet of antifungal drug Posaconazole to treat oral thrush locally and to improve the solubility and bioavailability of drug, simultaneously enhances the erosion rate of tablet Mucoadhesive dosage forms have long been employed to improve the bioavailability of drugs undergoing significant hepatic first-pass metabolism and control the release of drugs from hydrophilic matrices. Therefore, it is needed to develop suitable controlled release Mucoadhesive buccal tablets containing an antifungal agent, Posaconazole. The present study has been planned to formulate the Mucoadhesive buccal tablets of posaconazole by using xanthan gum and carbopol 940. This formulation used for the treatment of oral candidiasis. In vitro drug release results of all the formulations were conducted for 12 h which indicated that, tablet formulations, F1- F9 were found to be following non- fickian diffusion. The formulation F5 was taken as an optimized batch. Stability studies were conducted at 400C and 75 % RH as per ICH guidelines.口腔黏膜给药途径具备多项优势，可提升患者顺应性，规避胃肠道（gastrointestinal tract, GIT）与肝脏首过效应（hepatic first-pass effect）。本研究旨在以泊沙康唑（Posaconazole）与适配药用辅料制备黏膜黏附型口腔颊片，并通过质量控制试验与体外试验对该制剂开展评价。在开发用于局部治疗鹅口疮的抗真菌药物泊沙康唑口腔颊片的过程中，需同步改善药物溶解度与生物利用度，并提升片剂的溶蚀速率。黏膜黏附给药剂型长期应用于提升存在显著肝脏首过代谢的药物的生物利用度，同时可调控亲水凝胶骨架型药物的释放行为。因此，开发含抗真菌药物泊沙康唑的适宜控释型黏膜黏附口腔颊片具有现实必要性。本研究计划采用黄原胶（xanthan gum）与卡波姆940（carbopol 940）制备泊沙康唑黏膜黏附口腔颊片，该制剂用于治疗口腔念珠菌病。对全部制剂开展了12小时的体外药物释放试验，结果显示F1至F9的片剂制剂均符合非菲克扩散（non-Fickian diffusion）行为特征。其中处方F5被确定为最优处方批次。稳定性考察按照人用药品注册技术要求国际协调会（International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use, ICH）指导原则，在40℃与75%相对湿度（RH）条件下进行。