Influence of beta-cyclodextrin complexation on carbamazepine release from hydroxypropyl methylcellulose matrix tablets.
The in vitro release profiles of carbamazepine and beta-cyclodextrin either complexed or simply mixed and subsequently incorporated in hydrophilic matrix tablets containing 15 or 30% hydroxypropyl methylcellulose were evaluated. Solubility studies revealed a linear relationship between the increase in carbamazepine solubility and the increase in beta-cyclodextrin concentration. Drying methods (spray-drying and freeze-drying) were used to obtain carbamazepine/beta-cyclodextrin solid complexes in order to prepare tablets. The results demonstrated that matrix tablets containing carbamazepine/beta-cyclodextrin solid complexes displayed faster carbamazepine and beta-cyclodextrin release compared to that containing simple physical mixture. Gelling and matrix formation was impaired in formulation containing 15% hydroxypropyl methylcellulose and spray-dried complex. The comparison of spray-drying and freeze-drying revealed no significant influence of both drying methods on carbamazepine and beta-cyclodextrin dissolution rate when carbamazepine/beta-cyclodextrin complexes were incorporated in 30% hydroxypropyl methylcellulose matrix tablets. The results point to the possibility of modulating carbamazepine release using a hydroxypropyl methylcellulose matrix associated to the drug complexed with beta-cyclodextrin.
Koester
Letícia S
LS
Programa de Pós-graduação em Ciências Farmacêuticas, Porto Alegre, RS, Brazil.
Xavier
Clarissa R
CR
Mayorga
Paulo
P
Bassani
Valquiria L
VL
D000927:Anticonvulsants / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002220:Carbamazepine / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003505:Cyclodextrins / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D012995:Solubility; D013055:Spectrophotometry, Infrared; D013607:Tablets; D047392:beta-Cyclodextrins
D000927:Anticonvulsants; D003505:Cyclodextrins; D005079:Excipients; D013607:Tablets; D047392:beta-Cyclodextrins; D002220:Carbamazepine; D065347:Hypromellose Derivatives; D008747:Methylcellulose; C031215:betadex