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

• Type: Article in International Scientific Journal
• Date: 2020

Authors

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

Journal

Title: AAPS PharmSciTech

Vol. 21

ISSN: 1530-9932

Publisher: Springer Nature

Indexing

ISI Web of Knowledge - 0 Citations

Scopus - 0 Citations

Other information

Authenticus ID: 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 10