Development of oral controlled-release tablet formulations based on diltiazem-carrageenan complex

被引:25
作者
Bonferoni, MC [1 ]
Rossi, S [1 ]
Ferrari, F [1 ]
Caramella, C [1 ]
机构
[1] Univ Pavia, Dept Pharmaceut Chem, I-27100 Pavia, Italy
关键词
lambda carrageenan; diltiazem HCl; drug-polymer complex; controlled release;
D O I
10.1081/PDT-120027428
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Diltiazem HCl and lambda carrageenan react in distilled water to give a slightly soluble interaction product. The aim of this work was to verify the possible employment of lambda carrageenan-diltiazem (DTZ) complex in controlled-release formulations. The influence of complex particle size, compression force, pH of the dissolution medium, and tablet dimensions on drug release has been evaluated. The results confirm the suitability of the DTZ-carrageenan interaction product for controlled-release formulations. Good compaction properties allow tablets to slowly erode, with only the addition of the amount of hydroxypropyl methylcellulose (HPMC) necessary as a binding agent. The use of the finest sieve fraction results in the highest crushing strength values and in the slowest release rate, both in pH 1.2 and in pH 6.8. The force of compression does not affect the drug release for values over 16 kN. The release rate increases when the geometry of the tablet is varied so the surface/volume ratio of the tablet is increased, suggesting a release mechanism involving surface dissolution/erosion.
引用
收藏
页码:155 / 162
页数:8
相关论文
共 24 条
[1]  
AGUZZI C, 2002, AAPS PHARM SCI TECH, V3
[2]   ON THE EMPLOYMENT OF LAMBDA-CARRAGEENAN IN A MATRIX SYSTEM .2. LAMBDA-CARRAGEENAN AND HYDROXYPROPYLMETHYLCELLULOSE MIXTURES [J].
BONFERONI, MC ;
ROSSI, S ;
TAMAYO, M ;
PEDRAZ, JL ;
DOMINGUEZGIL, A ;
CARAMELLA, C .
JOURNAL OF CONTROLLED RELEASE, 1994, 30 (02) :175-182
[3]   ON THE EMPLOYMENT OF LAMBDA-CARRAGEENAN IN A MATRIX SYSTEM .1. SENSITIVITY TO DISSOLUTION MEDIUM AND COMPARISON WITH NA CARBOXYMETHYLCELLULOSE AND XANTHAN GUM [J].
BONFERONI, MC ;
ROSSI, S ;
TAMAYO, M ;
PEDRAZ, JL ;
DOMINGUEZGIL, A ;
CARAMELLA, C .
JOURNAL OF CONTROLLED RELEASE, 1993, 26 (02) :119-127
[4]   On the employment of λ carrageenan in a matrix system.: III.: Optimization of a λ carrageenan-HPMC hydrophilic matrix [J].
Bonferoni, MC ;
Rossi, S ;
Ferrari, F ;
Bertoni, M ;
Bolhuis, GK ;
Caramella, C .
JOURNAL OF CONTROLLED RELEASE, 1998, 51 (2-3) :231-239
[5]   Characterization of a diltiazem-lambda carrageenan complex [J].
Bonferoni, MC ;
Rossi, S ;
Ferrari, F ;
Bettinetti, GP ;
Caramella, C .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 200 (02) :207-216
[6]  
BONFERONI MC, 2000, AAPS PHARM SCI TECH, V1
[7]  
BONFERONI MC, 2001, TIMOLOL MALEATE OPHT
[8]  
CARAMELLA C, 2002, Patent No. 6355272
[9]  
DAVIDSONS RL, 1980, HDB WATER SOLUBLE GU
[10]  
Edmundson I C, 1967, Adv Pharm Sci, V2, P95