Orodispersible Carbamazepine/Hydroxypropyl-beta-Cyclodextrin Tablets Obtained by Direct Compression with Five-in-One Co-processed Excipients

• Tipo: Artigo em Revista Científica Internacional
• Data: 2020

Autores

Conceicao, J (Autor) Outra; Adeoye, O (Autor) Outra; Cabral Marques, H (Autor) Outra; Concheiro, A (Autor) Outra; Alvarez Lorenzo, C (Autor) Outra; Sousa Lobo, JMS (Autor) Outra

Revista

Título: AAPS PharmSciTech

Vol. 21

ISSN: 1530-9932

Editora: Springer Nature

Indexação

ISI Web of Knowledge - 0 Citações

Scopus - 0 Citações

Outras Informações

ID Authenticus: P-00R-RAT

DOI: 10.1208/s12249-019-1579-5

Abstract (EN): The development of orodispersible tablets (ODTs) for poorly soluble and poorly flowable drugs via direct compression is still a challenge. This work aimed to develop ODTs of poorly soluble drugs by combining cyclodextrins that form inclusion complexes to improve wetting and release properties, and directly compressible co-processed excipients able to promote rapid disintegration and solve the poor flowability typical of inclusion complexes. Carbamazepine (CBZ) and hydroxypropyl-beta -cyclodextrin (HP beta CD) were used, respectively, as a model of a poorly soluble drug with poor flowability and as a solubilizing agent. Specifically, CBZ-an antiepileptic and anticonvulsant drug-may benefit from the studied formulation approach, since some patients have swallowing difficulties or fear of choking and are non-cooperative. Prosolv (R) ODT G2 and F-Melt (R) type C were the studied five-in-one co-processed excipients. The complex was prepared by kneading. Flow properties of all materials and main properties of the tablets were characterized. The obtained results showed that ODTs containing CBZ/HP beta CD complex can be prepared by direct compression through the addition of co-processed excipients. The simultaneous use of co-processing and cyclodextrin technologies rendered ODTs with an in vitro disintegration time in accordance with the European Pharmacopoeia requirement and with a fast and complete drug dissolution. In conclusion, the combination of five-in-one co-processed excipients and hydrophilic cyclodextrins may help addressing the ODT formulation of poorly soluble drugs with poor flowability, by direct compression and with desired release properties.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 10