Relationship Between Gelation Rate of Controlled-release Acetaminophen Tablets Containing Polyethylene Oxide and Colonic Drug Release in Dogs
Relationship Between Gelation Rate of Controlled-release Acetaminophen Tablets Containing Polyethylene Oxide and Colonic Drug Release in Dogs
复制标题
含聚环氧乙烷的对乙酰氨基酚控释片的凝胶化率与犬结肠药物释放的关系
DOI：
10.1023/a:1016006423601
复制
发表时间：
1996
影响因子：
3.7
通讯作者：
Muneo Fukui
中科院分区：
文献类型：
--
作者：
Kazuhiro Sako;H. Nakashima;T. Sawada;Muneo Fukui
目的。我们假设，由于凝胶基质的连续侵蚀，口服给药的亲水性基质片剂在到达结肠之前的充分凝胶化可以防止结肠药物释放的减少，这通常发生在这里。本研究的目的是阐明含有聚氧化乙烯的亲水性基质的凝胶化对使用控释（CR）对乙酰氨基酚片剂的犬结肠药物释放的影响。
方法.制备了两种类型的CR片剂，缓慢胶凝片剂（SG）和快速胶凝片剂（RG），其中含有额外的高度水溶性填充剂。检查了体外和体内性能。
结果SG和RG的体外释药行为相似。在犬经口给药中，两种制剂显示出相似的胃肠道转运，在经口给药后2-4 h内到达结肠。此外，它们显示出相似的最大血浆浓度（Cmax）和达到Cmax的时间（Tmax）。然而，相比之下，两种片剂从给药后2小时产生不同的血浆水平，RG的血浆水平高于SG的血浆水平，个体差异较小。直接观察到的RG结肠释药行为与体外释药行为相似，而SG结肠释药行为受到抑制。
结论.结肠药物释放与亲水性基质的凝胶化密切相关，快速凝胶化提供了药物在体内的持续释放。
AbstractPurpose. We hypothesized that sufficient gelation of orally administered hydrophilic matrix tablets before they reach the colon could, as a result of continuous erosion of the gelated matrix, prevent the decrease in colonic drug release which normally occurs here. The purpose of this study was to elucidate the effect of gelation of hydrophilic matrices containing polyethylene oxide on colonic drug release in dogs using controlled-release (CR) acetaminophen tablets.
Methods. Two types of CR tablets were prepared, a slow gelling tablet (SG) and a rapid gelling tablet (RG) containing an extra highly water soluble filler. In vitro and in vivo performance were examined.
Results. SG and RG showed similar drug release behavior in vitro. In oral administration to dogs, the two formulations showed similar gastrointestinal transit, reaching the colon within 2–4 h after oral dosing. Further, they showed similar maximum plasma levels (Cmax) and time to Cmax (Tmax). In contrast, however, the two tablets produced different plasma levels from 2 h post-dosing, with plasma levels of RG higher than those of SG and with smaller individual variation. Directly observed colonic drug release behavior of RG was similar to in vitro drug release, whereas that from SG was suppressed.
Conclusions. Colonic drug release is closely related to the gelation of hydrophilic matrix, and rapid gelation provides continuous in vivo drug release.
高效液相色谱法测定血浆中对乙酰氨基酚：单剂量药代动力学研究。
DOI：
10.1016/s0378-4347(00)84226-7
发表时间：
1981
期刊：
Journal of chromatography
影响因子：
--
作者：
Ameer,B;Greenblatt,DJ;Divoll,M;Abernethy,DR;Shargel,L
通讯作者：
Shargel,L