Hydroxypropyl-ß-Cyclodextrin and ß-Cyclodextrin as Tablet Fillers for Direct Compression

• Type: Article in International Scientific Journal
• Date: 2018-07-05

Authors

Jaime Conceição (Author) FFUP; Oluwatomide Adeoye (Author) Other; Helena Maria Cabral-Marques (Author) Other; Sousa Lobo JM (Author) FFUP

Journal

Title: AAPS PharmSciTech

Pages: 1-9

ISSN: 1530-9932

Publisher: Springer Nature

Indexing

Scopus - 0 Citations

Other information

Authenticus ID: P-00P-1DM

DOI: 10.1208/s12249-018-1115-z

Abstract (EN): 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-ß-cyclodextrin and ß-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-ß-cyclodextrin showed better properties than ß-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-ß-cyclodextrin displayed the best results. As there are people intolerant to lactose, hydroxypropyl-ß-cyclodextrin, although its cost is higher, can be considered a good substitute for lactose. © 2018 American Association of Pharmaceutical Scientists

Language: English

Type (Professor's evaluation): Scientific