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Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained by Direct Compression with Five-in-One Co-processed Excipients.
AAPS PharmSciTech. 2020 Jan 02; 21(2):39.AP

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.

Authors+Show Affiliations

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.Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal.Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal.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.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.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.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31897724

Citation

Conceição, Jaime, et al. "Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained By Direct Compression With Five-in-One Co-processed Excipients." AAPS PharmSciTech, vol. 21, no. 2, 2020, p. 39.
Conceição J, Adeoye O, Cabral-Marques H, et al. Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained by Direct Compression with Five-in-One Co-processed Excipients. AAPS PharmSciTech. 2020;21(2):39.
Conceição, J., Adeoye, O., Cabral-Marques, H., Concheiro, A., Alvarez-Lorenzo, C., & Sousa Lobo, J. M. (2020). Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained by Direct Compression with Five-in-One Co-processed Excipients. AAPS PharmSciTech, 21(2), 39. https://doi.org/10.1208/s12249-019-1579-5
Conceição J, et al. Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained By Direct Compression With Five-in-One Co-processed Excipients. AAPS PharmSciTech. 2020 Jan 2;21(2):39. PubMed PMID: 31897724.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained by Direct Compression with Five-in-One Co-processed Excipients. AU - Conceição,Jaime, AU - Adeoye,Oluwatomide, AU - Cabral-Marques,Helena, AU - Concheiro,Angel, AU - Alvarez-Lorenzo,Carmen, AU - Sousa Lobo,José Manuel, Y1 - 2020/01/02/ PY - 2019/07/27/received PY - 2019/11/12/accepted PY - 2020/1/4/entrez PY - 2020/1/4/pubmed PY - 2020/3/28/medline KW - F-Melt® type C KW - Prosolv® ODT G2 KW - carbamazepine/hydroxypropyl-β-cyclodextrin complexes KW - direct compression KW - orally disintegrating tablets SP - 39 EP - 39 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 21 IS - 2 N2 - 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. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/31897724/Orodispersible_Carbamazepine/Hydroxypropyl-β-Cyclodextrin_Tablets_Obtained_by_Direct_Compression_with_Five-in-One_Co-processed_Excipients L2 - https://dx.doi.org/10.1208/s12249-019-1579-5 DB - PRIME DP - Unbound Medicine ER -