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AAPS PharmSciTech
Jan 02, 2020;21 (2): 39.

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

Jaime Conceição, Oluwatomide Adeoye, Helena Cabral-Marques, Angel Concheiro, Carmen Alvarez-Lorenzo, José Manuel Sousa Lobo
Author Information
  1. Jaime Conceição: UCIBIO/REQUIMTE, MedTech-Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, no. 228, 4050-313, Porto, Portugal. jmgmconceicao@ff.up.pt.
  2. Oluwatomide Adeoye: Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal.
  3. Helena Cabral-Marques: Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal.
  4. Angel Concheiro: Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma Group (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
  5. Carmen Alvarez-Lorenzo: Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma Group (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
  6. José Manuel Sousa Lobo: UCIBIO/REQUIMTE, MedTech-Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, no. 228, 4050-313, Porto, Portugal.
PMID: 31897724 DOI: 10.1208/s12249-019-1579-5

Abstract

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-β-cyclodextrin (HPβCD) 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® ODT G2 and F-Melt® 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/HPβCD 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.

Keywords

F-Melt® type C Prosolv® ODT G2 carbamazepine/hydroxypropyl-β-cyclodextrin complexes direct compression orally disintegrating tablets

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MeSH Term

2-Hydroxypropyl-beta-cyclodextrin
Anticonvulsants
Calorimetry, Differential Scanning
Carbamazepine
Drug Compounding
Drug Liberation
Excipients
Tablets
X-Ray Diffraction

Chemicals

Anticonvulsants
Excipients
Tablets
2-Hydroxypropyl-beta-cyclodextrin
Carbamazepine
Journal Article

Word Cloud

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