Comparative Study of Selected Excipients' Influence on Carvedilol Release from Hypromellose Matrix Tablets

被引:2
作者
Ojstersek, Tadej [1 ,2 ]
Hudovornik, Grega [1 ]
Vrecer, Franc [1 ,2 ]
机构
[1] KRKA Dd, Smarjeska Cesta 6, Novo Mesto 8501, Slovenia
[2] Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia
关键词
hypromellose; HPMC; controlled release; modified release; extended release; prolonged release; direct compression; excipient; filler; drug release modifier; LOCALLY WEIGHTED REGRESSION; DRUG-RELEASE; MICROCRYSTALLINE CELLULOSE; SURFACE-ENERGY; HPMC MATRICES; DISSOLUTION; FORMULATION; LACTOSE; KINETICS; AMORPHIZATION;
D O I
10.3390/pharmaceutics15051525
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Solid dosage forms based on hypromellose (HPMC) with prolonged/extended drug release are very important from the research and industrial viewpoint. In the present research, the influence of selected excipients on carvedilol release performance from HPMC-based matrix tablets was studied. A comprehensive group of selected excipients was used within the same experimental setup, including different grades of excipients. Compression mixtures were directly compressed using constant compression speed and main compression force. LOESS modelling was used for a detailed comparison of carvedilol release profiles via estimating burst release, lag time, and times at which a certain % of carvedilol was released from the tablets. The overall similarity between obtained carvedilol release profiles was estimated using the bootstrapped similarity factor (f(2)). In the group of water-soluble carvedilol release modifying excipients, which produced relatively fast carvedilol release profiles, POLYOX?? WSR N-80 and Polyglykol((R)) 8000 P demonstrated the best carvedilol release control, and in the group of water-insoluble carvedilol release modifying excipients, which produced relatively slow carvedilol release profiles, AVICEL((R)) PH-102 and AVICEL((R)) PH-200 performed best.
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页数:23
相关论文
共 58 条
[1]  
ALDERMAN D A, 1984, International Journal of Pharmaceutical Technology and Product Manufacture, V5, P1
[2]  
[Anonymous], 2014, HYDROPHILIC MATRIX T
[3]  
[Anonymous], ?About us"
[4]   Maltodextrin molecular weight distribution influence on the glass transition temperature and viscosity in aqueous solutions [J].
Avaltroni, F ;
Bouquerand, PE ;
Normand, V .
CARBOHYDRATE POLYMERS, 2004, 58 (03) :323-334
[5]   Properties of sugar, polyol, and polysaccharide water-ethanol solutions [J].
Bouchard, Andreanne ;
Hofland, Gerard W. ;
Witkamp, Geert-Jan .
JOURNAL OF CHEMICAL AND ENGINEERING DATA, 2007, 52 (05) :1838-1842
[6]  
Bruschi M.L., 2015, STRATEGIES MODIFY DR, P63, DOI [10.1016/B978-0-08-100092-2.00005-9, DOI 10.1016/B978-0-08-100092-2.00005-9]
[7]  
Buhler V, 2005, POLYVINYLPYRROLIDONE, P5
[8]   Controlled-release carvedilol [J].
Carter, Natalie J. ;
Keating, Gillian M. .
AMERICAN JOURNAL OF CARDIOVASCULAR DRUGS, 2008, 8 (04) :271-282
[9]   ROBUST LOCALLY WEIGHTED REGRESSION AND SMOOTHING SCATTERPLOTS [J].
CLEVELAND, WS .
JOURNAL OF THE AMERICAN STATISTICAL ASSOCIATION, 1979, 74 (368) :829-836
[10]   LOCALLY WEIGHTED REGRESSION - AN APPROACH TO REGRESSION-ANALYSIS BY LOCAL FITTING [J].
CLEVELAND, WS ;
DEVLIN, SJ .
JOURNAL OF THE AMERICAN STATISTICAL ASSOCIATION, 1988, 83 (403) :596-610