Carbamazepine bilayer tablets combining hydrophilic and hydrophobic cyclodextrins as a quick/slow biphasic release system

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

Authors

Conceição, J (Author) Other; Adeoye, O (Author) Other; Cabral Marques, H (Author) Other; Concheiro, A (Author) Other; Alvarez Lorenzo, C (Author) Other; Sousa Lobo JM (Author) FFUP

Journal

Title: Journal of Drug Delivery Science and Technology

Vol. 57

ISSN: 1773-2247

Publisher: Editions de Sante

Indexing

Scopus - 0 Citations

Other information

Authenticus ID: P-00R-WFY

DOI: 10.1016/j.jddst.2020.101611

Abstract (EN): This work aimed to explore the combination of hydrophilic and hydrophobic cyclodextrins to prepare bilayer tablets that can perform as quick/slow biphasic release systems of a poorly soluble drug. This formulation approach is of particular interest for treatments that require a rapid action followed by sustained therapeutic levels. Carbamazepine (CBZ), an antiepileptic and anticonvulsant agent, was used as a model of a BCS Class 2 drug. Hydroxypropyl-ß-cyclodextrin (HPßCD) was chosen as complexing agent in the rapid release layer. Differently, triacetyl-ß-cyclodextrin (TAßCD) was tested as controlling release agent in the sustained release layer. Croscarmellose sodium was utilized as superdisintegrant in the rapid release layer, and sodium stearyl fumarate was applied as anti-adherent lubricant in both layers. Bilayer tablets were characterized through several techniques. The results highlighted the feasibility of the combination of HPßCD/CBZ inclusion complex with croscarmellose sodium in the rapid release layer to achieve fast dissolution for the first 30¿45 min, and TAßCD as controlling agent in the sustained release layer of the bilayer tablets to obtain a prolonged release during 720 min. In conclusion, combinations of hydrophilic and hydrophobic cyclodextrins may help addressing the formulation of poorly soluble drugs in bilayer tablets as a fast/slow biphasic release system. © 2020 Elsevier B.V.

Language: English

Type (Professor's evaluation): Scientific