PDF(Pubmed)
Abstract：
Eosinophilic Esophagitis is an antigen-mediated inflammatory disease characterized by thickening of the esophageal wall, leading to dysphagia, vomiting, reflux, and abdominal pain. This disease can be treated with a therapeutic approach ranging from diet to pharmacological therapy. Jorveza® (budesonide) and Dupixent® (dupilumab) are treatments for Eosinophilic Esophagitis approved by the European Medicines Agency in adults but not in children. Budesonide-based extemporaneous oral liquid suspensions could be prepared for pediatric use. The main limit of this formulation is that budesonide needs a longer residence time on the esophageal mucosa to solubilize and diffuse in it to exert its local anti-inflammatory effect. Herein, we propose the development of an extemporaneous mucoadhesive oral budesonide solution for the pediatric population. A liquid vehicle containing hydroxypropyl-beta-cyclodextrin as a complexing agent and carboxymethylcellulose sodium as a mucoadhesive excipient was used to prepare budesonide-based formulations. A stable solution at a concentration of 0.7 mg/mL was successfully prepared and characterized. The formulation showed rheological and mucoadhesive properties suitable for an Eosinophilic Esophagitis local prolonged treatment. In this way, pharmacists can prepare stable budesonide-based mucoadhesive solutions, providing both patients and physicians with a new therapeutic option for Eosinophilic Esophagitis pediatric treatment.
摘要：
嗜酸性粒细胞性食管炎是一种抗原介导的炎症性疾病，其特征是食管壁增厚，导致吞咽困难,呕吐,反流,和腹痛。这种疾病可以用从饮食到药物治疗的治疗方法来治疗。Jorveza®（布地奈德）和Dupixent®（dupilumab）是欧洲药品管理局批准的成人而非儿童嗜酸性食管炎的治疗方法。基于布地奈德的临时口服液混悬液可用于儿科使用。该制剂的主要限制是布地奈德需要在食管粘膜上更长的停留时间以在其中溶解和扩散以发挥其局部抗炎作用。在这里，我们建议为儿科人群开发一种临时粘膜粘附性口腔布地奈德溶液。使用含有羟丙基-β-环糊精作为络合剂和羧甲基纤维素钠作为粘膜粘附赋形剂的液体载体来制备基于布地奈德的制剂。成功制备并表征浓度为0.7mg/mL的稳定溶液。该制剂显示出适用于嗜酸性食管炎局部延长治疗的流变学和粘膜粘附特性。这样,药剂师可以制备稳定的基于布地奈德的粘膜粘附溶液，为患者和医生提供一种新的治疗选择，用于嗜酸性食管炎儿科治疗。
