pH-independent release of a basic drug from pellets coated with the extended release polymer dispersion Kollicoato® SR 30 D and the enteric polymer dispersion Kollicoato® MAE 30 DP

被引:59
作者
Dashevsky, A
Kolter, K
Bodmeier, R
机构
[1] Free Univ Berlin, Coll Pharm, D-12169 Berlin, Germany
[2] BASF AG, Dev Pharma Ingredients, Ludwigshafen, Germany
关键词
enteric polymers; extended release; multiparticulates; pH-independent release; polyvinyl acetate; Kollicoat((R))SR 30 D;
D O I
10.1016/j.ejpb.2004.03.013
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The objective of this study was to obtain pH-independent release profiles from coated pellets containing drugs with pH-dependent solubility. pH-independent release of the basic model drug verapamil HCl was achieved by coating with a combination of the neutral polymer dispersions Kollicoat(R) SR 30 D (aqueous dispersion of polyvinyl acetate) and the enteric polymer dispersion Kollicoat(R) MAE 30 DP (aqueous dispersion of methacrylic acid and ethyl acrylate copolymer; methacrylic acid copolymer type C). The two polymers where applied either as separate layers (enteric polymer + extended release polymer or vice versa) or as a polymer blend. A careful balance of the ratios of the polymers allowed the achievement of a pH-independent release. Higher amounts of the enteric polymer in the polymer blend resulted in a reversal of the pH-dependency, e.g. a faster release at pH 6.8 than in 0.1 N HCl. (C) 2004 Elsevier B.V. All rights reserved.
引用
收藏
页码:45 / 49
页数:5
相关论文
共 16 条
[1]   PH-INDEPENDENT CONTROLLED-RELEASE MICROSPHERES USING POLYGLYCEROL ESTERS OF FATTY-ACIDS [J].
AKIYAMA, Y ;
YOSHIOKA, M ;
HORIBE, H ;
HIRAI, S ;
KITAMORI, N ;
TOGUCHI, H .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1994, 83 (11) :1600-1607
[2]  
BENEDIKT G, 1987, Patent No. 0275444
[3]  
DASHEVSKY A, 1999, AAPR ANN M, V30, P384
[4]   MICROENVIRONMENTAL PH CONTROL OF DRUG DISSOLUTION [J].
DOHERTY, C ;
YORK, P .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 50 (03) :223-232
[5]   Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms [J].
Dressman, JB ;
Amidon, GL ;
Reppas, C ;
Shah, VP .
PHARMACEUTICAL RESEARCH, 1998, 15 (01) :11-22
[6]   Influence of admired citric acid on the release profile of pelanserin hydrochloride from HPMC matrix tablets [J].
Espinoza, R ;
Hong, E ;
Villafuerte, L .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 201 (02) :165-173
[7]  
GABR KE, 1992, EUR J PHARM BIOPHARM, V38, P199
[8]   An organic acid-induced sigmoidal release system for oral controlled-release preparations .3. Elucidation of the anomalous drug release behavior through osmotic pumping mechanism [J].
Narisawa, S ;
Nagata, M ;
Hirakawa, Y ;
Kobayashi, M ;
Yoshino, H .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 148 (01) :85-91
[9]   AN ORGANIC ACID-INDUCED SIGMOIDAL RELEASE SYSTEM FOR ORAL CONTROLLED-RELEASE PREPARATIONS [J].
NARISAWA, S ;
NAGATA, M ;
DANYOSHI, C ;
YOSHINO, H ;
MURATA, K ;
HIRAKAWA, Y ;
NODA, K .
PHARMACEUTICAL RESEARCH, 1994, 11 (01) :111-116
[10]   An organic acid-induced sigmoidal release system for oral controlled-release preparations .2. Permeability enhancement of Eudragit RS coating led by the physicochemical interactions with organic acid [J].
Narisawa, S ;
Nagata, M ;
Hirakawa, Y ;
Kobayashi, M ;
Yoshino, H .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1996, 85 (02) :184-188