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Hydroxypropyl-β-Cyclodextrin and β-Cyclodextrin as Tablet Fillers for Direct Compression.
AAPS PharmSciTech. 2018 Aug; 19(6):2710-2718.AP

Abstract

Cyclodextrins are cyclic carbohydrates widely used as complexing and non-complexing excipients in drug delivery systems. The purpose of this work was to study the ability of hydroxypropyl-β-cyclodextrin and β-cyclodextrin to act as tablet fillers for direct compression. In this way, several parameters of the cyclodextrins were evaluated, namely: (i) the flow properties such as angle of repose, flow time, Carr index, and Hausner ratio; (ii) the compaction behavior, specifically the energies and forces exerted during tableting, the plasticity index, the lubrication efficiency, and compression profiles (force/time and work/displacement of the upper punch); and (iii) the influence on carbamazepine release characteristics from uncoated tablets, i.e., dissolution rate and disintegration time. In addition, these properties of the cyclodextrins were compared with those from other commonly used direct compression fillers (lactose monohydrate, mannitol, calcium hydrogen phosphate dihydrate, and microcrystalline cellulose) and co-processed excipients (microcrystalline cellulose/mannitol and lactose monohydrate/cellulose). Three main conclusions can be drawn: (i) the studied cyclodextrins can be used as tablet fillers for direct compression; (ii) hydroxypropyl-β-cyclodextrin showed better properties than β-cyclodextrin mainly at the level of the physics of compression (higher values of plasticity index and lubrication efficiency) and of the drug release characteristics (faster and greater dissolution rate and a shorter disintegration time); and (iii) lactose monohydrate and hydroxypropyl-β-cyclodextrin displayed the best results. As there are people intolerant to lactose, hydroxypropyl-β-cyclodextrin, although its cost is higher, can be considered a good substitute for lactose.

Authors+Show Affiliations

UCIBIO-ReQuimTe, Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, n.° 228, 4050-313 Oporto, Porto, Portugal. jmgmconceicao@ff.up.pt.Research Institute for Medicines (iMed.ULisboa), Department of Galenic Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal. Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.Research Institute for Medicines (iMed.ULisboa), Department of Galenic Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Universidade de Lisboa, Lisbon, Portugal.UCIBIO-ReQuimTe, Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, n.° 228, 4050-313 Oporto, Porto, Portugal.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29978292

Citation

Conceição, Jaime, et al. "Hydroxypropyl-β-Cyclodextrin and β-Cyclodextrin as Tablet Fillers for Direct Compression." AAPS PharmSciTech, vol. 19, no. 6, 2018, pp. 2710-2718.
Conceição J, Adeoye O, Cabral-Marques HM, et al. Hydroxypropyl-β-Cyclodextrin and β-Cyclodextrin as Tablet Fillers for Direct Compression. AAPS PharmSciTech. 2018;19(6):2710-2718.
Conceição, J., Adeoye, O., Cabral-Marques, H. M., & Sousa Lobo, J. M. (2018). Hydroxypropyl-β-Cyclodextrin and β-Cyclodextrin as Tablet Fillers for Direct Compression. AAPS PharmSciTech, 19(6), 2710-2718. https://doi.org/10.1208/s12249-018-1115-z
Conceição J, et al. Hydroxypropyl-β-Cyclodextrin and β-Cyclodextrin as Tablet Fillers for Direct Compression. AAPS PharmSciTech. 2018;19(6):2710-2718. PubMed PMID: 29978292.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hydroxypropyl-β-Cyclodextrin and β-Cyclodextrin as Tablet Fillers for Direct Compression. AU - Conceição,Jaime, AU - Adeoye,Oluwatomide, AU - Cabral-Marques,Helena Maria, AU - Sousa Lobo,José Manuel, Y1 - 2018/07/05/ PY - 2018/05/12/received PY - 2018/06/24/accepted PY - 2018/7/7/pubmed PY - 2018/10/20/medline PY - 2018/7/7/entrez KW - compaction KW - cyclodextrins KW - disintegration KW - dissolution KW - flow SP - 2710 EP - 2718 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 19 IS - 6 N2 - Cyclodextrins are cyclic carbohydrates widely used as complexing and non-complexing excipients in drug delivery systems. The purpose of this work was to study the ability of hydroxypropyl-β-cyclodextrin and β-cyclodextrin to act as tablet fillers for direct compression. In this way, several parameters of the cyclodextrins were evaluated, namely: (i) the flow properties such as angle of repose, flow time, Carr index, and Hausner ratio; (ii) the compaction behavior, specifically the energies and forces exerted during tableting, the plasticity index, the lubrication efficiency, and compression profiles (force/time and work/displacement of the upper punch); and (iii) the influence on carbamazepine release characteristics from uncoated tablets, i.e., dissolution rate and disintegration time. In addition, these properties of the cyclodextrins were compared with those from other commonly used direct compression fillers (lactose monohydrate, mannitol, calcium hydrogen phosphate dihydrate, and microcrystalline cellulose) and co-processed excipients (microcrystalline cellulose/mannitol and lactose monohydrate/cellulose). Three main conclusions can be drawn: (i) the studied cyclodextrins can be used as tablet fillers for direct compression; (ii) hydroxypropyl-β-cyclodextrin showed better properties than β-cyclodextrin mainly at the level of the physics of compression (higher values of plasticity index and lubrication efficiency) and of the drug release characteristics (faster and greater dissolution rate and a shorter disintegration time); and (iii) lactose monohydrate and hydroxypropyl-β-cyclodextrin displayed the best results. As there are people intolerant to lactose, hydroxypropyl-β-cyclodextrin, although its cost is higher, can be considered a good substitute for lactose. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/29978292/Hydroxypropyl_β_Cyclodextrin_and_β_Cyclodextrin_as_Tablet_Fillers_for_Direct_Compression_ L2 - https://dx.doi.org/10.1208/s12249-018-1115-z DB - PRIME DP - Unbound Medicine ER -