含琥珀酸前药的氢化可的松口腔崩解薄膜的研制。

Development of a Hydrocortisone Orodispersible Thin Film Containing Its Succinate Prodrug.

作者信息

Boisseillier Clément, Demange-Labriet Lucas, Kariyawasam Dulanjalee, Marchadour Pauline, Fauqueur Anne-Sophie, Annereau Maxime, Denis Lucas, Cotteret Camille, Cisternino Salvatore, Schweitzer-Chaput Arnaud

机构信息

Service Pharmacie, Hôpital Universitaire Necker-Enfants Malades, Assistance Publique des Hôpitaux de Paris (AP-HP), 149 Rue de Sèvres, F-75015 Paris, France.

Service d'Endocrinologie, Diabétologie, Gynécologie Pédiatriques, Hôpital Universitaire Necker-Enfants Malades, Assistance Publique des Hôpitaux de Paris (AP-HP), 149 Rue de Sèvres, F-75015 Paris, France.

出版信息

Pharmaceuticals (Basel). 2025 Jan 13;18(1):86. doi: 10.3390/ph18010086.

DOI:10.3390/ph18010086

PMID:39861149

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11768698/

Abstract

UNLABELLED

Orodispersible thin film (ODF) is an innovative dosage form that allows for adjustable dosing and improved patient compliance. It is administered by mouth, where it dissolves, making it suitable for children.

OBJECTIVES

The aim of the study was to develop and characterize an optimal ODF formulation containing equivalent hydrocortisone at 0.5 mg/cm using the solvent-casting method. A stability-indicating assay for the simultaneous quantification of hydrocortisone and hydrocortisone 21-hemissucinate (HMS) was developed. ODFs were characterized by organoleptic properties and by testing for uniformity of mass, content, stability, thickness, and dissolution.

RESULTS

When optimized, ODF is thin, flexible, and transparent, making it suitable for production in hospital pharmacies using standard equipment. In contrast to the water-insoluble hydrocortisone, the HMS-loaded cast gel successfully satisfied the tests, including content uniformity. Disintegration appeared acceptable as compared to the commercial grade ondansetron ODF (Setofilm). The physicochemical stability of the active ingredients (i.e., HMS, hydrocortisone) contained in the ODF at 0.5 mg/cm is demonstrated for at least 84 days at 23 °C.

CONCLUSION

The ODF formulated with the water-soluble hydrocortisone prodrug HMS allows accurate drug level to be achieved, thus opening up new opportunities for use in pediatric patients.

摘要

未标注

口腔崩解薄膜（ODF）是一种创新剂型，可实现剂量调整并提高患者依从性。它通过口服给药，在口腔中溶解，适用于儿童。

目的

本研究旨在采用溶剂浇铸法开发并表征一种含有0.5mg/cm等量氢化可的松的最佳ODF制剂。开发了一种同时定量氢化可的松和氢化可的松21-半琥珀酸酯（HMS）的稳定性指示测定法。通过感官特性以及质量、含量、稳定性、厚度和溶出度测试对ODF进行表征。

结果

优化后的ODF薄、柔韧且透明，适合使用标准设备在医院药房生产。与水不溶性氢化可的松不同，负载HMS的浇铸凝胶成功通过了包括含量均匀度在内的各项测试。与市售级昂丹司琼ODF（Setofilm）相比，崩解情况可接受。ODF中含有的活性成分（即HMS、氢化可的松）在23℃下至少84天的物理化学稳定性得到了证明。