Influence of β-cyclodextrin complexation on carbamazepine release from hydroxypropyl methylcellulose matrix tablets

被引:45
作者
Koester, LS [1 ]
Xavier, CR [1 ]
Mayorga, P [1 ]
Bassani, VL [1 ]
机构
[1] Univ Fed Rio Grande Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
关键词
carbamazepine; beta-cyclodextrin; hydroxypropyl methylcellulose; complexes; in vitro dissolution; matrix tablets; spray-drying; freeze-drying;
D O I
10.1016/S0939-6411(02)00127-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. (C) 2002 Published by Elsevier Science B.V.
引用
收藏
页码:85 / 91
页数:7
相关论文
共 19 条
[1]  
[Anonymous], 1992, APPL PHARMACOKINETIC
[2]   Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate [J].
Bettini, R ;
Catellani, PL ;
Santi, P ;
Massimo, G ;
Peppas, NA ;
Colombo, P .
JOURNAL OF CONTROLLED RELEASE, 2001, 70 (03) :383-391
[3]   Mechanisms by which cyclodextrins modify drug release from polymeric drug delivery systems [J].
Bibby, DC ;
Davies, NM ;
Tucker, IG .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 197 (1-2) :1-11
[4]   STUDIES ON THE BEHAVIOR OF ALPHA-CYCLODEXTRINS, BETA-CYCLODEXTRINS AND GAMMA-CYCLODEXTRINS AND SOME DERIVATIVES UNDER REVERSED-PHASE LIQUID-CHROMATOGRAPHIC CONDITIONS [J].
BIELEJEWSKA, A ;
KOZBIAL, M ;
NOWAKOWSKI, R ;
DUSZCZYK, K ;
SYBILSKA, D .
ANALYTICA CHIMICA ACTA, 1995, 300 (1-3) :201-206
[5]  
ElNahhas SA, 1996, PHARMAZIE, V51, P960
[6]   CARBAMAZEPINE MODIFIED RELEASE DOSAGE FORMS [J].
GIUNCHEDI, P ;
CONTE, U ;
LAMANNA, A .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1991, 17 (13) :1753-1764
[7]  
Higuchi T., 1965, Interscience, New York, V4, P117
[8]  
ICH Steering Committee, INT C HARM TECHN REQ
[9]  
Ikinci G, 1999, PHARMAZIE, V54, P139
[10]   Simultaneous determination of α, β and γ cyclodextrins by LC [J].
Kinalekar, MS ;
Kulkarni, SR ;
Vavia, PR .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 2000, 22 (04) :661-666