DEVELOPMENT OF A ZERO-ORDER RELEASE ORAL COMPRESSED TABLET WITH POTENTIAL FOR COMMERCIAL TABLETTING PRODUCTION

DEVELOPMENT OF A ZERO-ORDER RELEASE ORAL COMPRESSED TABLET WITH POTENTIAL FOR COMMERCIAL TABLETTING PRODUCTION
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DOI:
10.1016/0378-5173(94)90259-3
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发表时间:
1994-11-04
影响因子:
5.8
通讯作者:
DANCKWERTS, MP
DANCKWERTS, MP
中科院分区:
医学2区
文献类型:
--
作者:
DANCKWERTS, MP

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以咖啡因和布洛芬为模型药物,研究了它们从独特的杯芯口服给药系统中的释放,以确定它们的时间指数(t(n))与释放曲线。杯内芯药物递送系统由不同浓度的两种等级的羟丙基甲基纤维素(HPMC)的芯组成。使用HPMC K4 M和HPMC K15 M作为核心基质中的聚合物。然后将平的盘形芯Tvas与先前压制的杯形片剂一起压制,所述杯形片剂由惰性和不可渗透的巴西棕榈蜡和乙基纤维素组成。这些药物递送系统以零级速率释放活性药物8至23小时。然后将释放速率与仅含核心的系统进行比较。t(n)指数从最低芯系统的0.477变化到布洛芬杯芯系统中的5%w/w HPMC K4 M的0.997。由于芯、杯和杯中芯在自动压片机上压缩,因此该药物递送系统可以容易地按比例放大到商业生产。
The release of caffeine and ibuprofen as model drugs from a unique core-in-cup oral drug delivery system has been examined to determine their time exponent (t(n)) vs release profiles. The core-in-cup drug delivery system consisted of cores of various concentrations of two grades of hydroxypropylmethylcellulose (HPMC). HPMC K4M and HPMC K15M were used as the polymers in the core matrix. The flat disc-shaped core Tvas then compressed with a previously compressed cup-shape tablet consisting of inert and impermeable carnauba wax and ethylcellulose. These drug delivery systems released active drug at a zero-order rate for periods of time between 8 and 23 h. The release rate was then compared to core only systems. The t(n) exponents varied from 0.477 for the lowest core system to 0.997 for a 5% w/w HPMC K4M in ibuprofen core-in-cup system. Because the core, the cup, and the core-in-cup are compressed on an automated tabletting press, this drug delivery system can be easily scaled up to commercial production.