Study of drug release and tablet characteristics of silicone adhesive matrix tablets

被引:23
|
作者
Tolia, Gaurav [1 ]
Li, S. Kevin [1 ]
机构
[1] Univ Cincinnati, Coll Pharm, Div Pharmaceut Sci, Cincinnati, OH 45267 USA
基金
美国国家科学基金会;
关键词
Controlled release; Silicone adhesive; Ethyl cellulose; Polymers; Tablet strength; Binary mixture; HYDROXYPROPYL METHYLCELLULOSE; DOSAGE FORMS; COMPRESSION; POLYMERS; ETHYLCELLULOSE; PARACETAMOL; PREDICTION; DISPERSION; SUCCINATE; CELLULOSE;
D O I
10.1016/j.ejpb.2012.07.006
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Matrix tablets of a model drug acetaminophen (APAP) were prepared using a highly compressible low glass transition temperature (T-g) polymer silicone pressure sensitive adhesive (PSA) at various binary mixtures of silicone PSA/APAP ratios. Matrix tablets of a rigid high T-g matrix forming polymer ethyl cellulose (EC) were the reference for comparison. Drug release study was carried out using USP Apparatus 1 (basket), and the relationship between the release kinetic parameters of APAP and polymer/APAP ratio was determined to estimate the excipient percolation threshold. The critical points attributed to both silicone PSA and EC tablet percolation thresholds were found to be between 2.5% and 5% w/w. For silicone PSA tablets, satisfactory mechanical properties were obtained above the polymer percolation threshold; no cracking or chipping of the tablet was observed above this threshold. Rigid EC APAP tablets showed low tensile strength and high friability. These results suggest that silicone PSA could eliminate issues related to drug compressibility in the formulation of directly compressed oral controlled release tablets of poorly compressible drug powder such as APAP. No routinely used excipients such as binders, granulating agents, glidants, or lubricants were required for making an acceptable tablet matrix of APAP using silicone PSA. (C) 2012 Elsevier B.V. All rights reserved.
引用
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页码:518 / 525
页数:8
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