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含填充剂的水胶体载体用于盐酸地尔硫卓的释放。

Hydrocolloid carriers with filler inclusion for diltiazem hydrochloride release.

作者信息

Gal A, Nussinovitch A

机构信息

Institute of Biochemistry, Food Science and Nutrition, The Hebrew University of Jerusalem, Faculty of Agricultural, Food and Environmental Quality Sciences, Rehovot, 76100, Israel.

出版信息

J Pharm Sci. 2007 Jan;96(1):168-78. doi: 10.1002/jps.20775.

Abstract

Hydrocolloid beads based on agarose, alginate (both 3%, w/w), or gellan (2%, w/w) were produced to study their potential as drug carriers. The beads included various fillers: talc, kaolin, calcium carbonate, potato, or corn starch (10%, w/w). After gelation, the carriers were subjected to either freeze- or vacuum-drying. The dried carriers were spheroids. The diameters of freeze- and vacuum-dried carriers ranged from 2.4 to 4.1 mm and 1.5 to 2.8 mm, respectively. The porosity values of the freeze-dried carriers were significantly higher than those of their vacuum-dried counterparts. Scanning electron microscopy (SEM) revealed that all dried carriers included internal voids that were partially occupied by the filler particles. Upon their introduction into simulated gastric fluid (3 h), followed by 6 h in intestinal fluid, all carriers were stable and underwent swelling. Release profiles of diltiazem hydrochloride from different carriers were obtained during immersion in dissolution medium. Filler inclusion (but not the type of filler) contributed to the stability of the carriers and prolonged the time of drug release (6.5-8.5 h) relative to the faster drug release from carriers that contained no filler (3.5 h). In summary, alginate, agar, and gellan beads with filler inclusion may be useful for slow drug release.

摘要

制备了基于琼脂糖、海藻酸盐(均为3%,w/w)或结冷胶(2%,w/w)的水胶体珠,以研究其作为药物载体的潜力。这些珠子包含各种填充剂:滑石粉、高岭土、碳酸钙、土豆或玉米淀粉(10%,w/w)。凝胶化后,载体进行冷冻干燥或真空干燥。干燥后的载体呈球体。冷冻干燥和真空干燥载体的直径分别为2.4至4.1毫米和1.5至2.8毫米。冷冻干燥载体的孔隙率值显著高于真空干燥载体。扫描电子显微镜(SEM)显示,所有干燥载体都有内部空隙,部分被填充颗粒占据。将它们放入模拟胃液中3小时,然后在肠液中放置6小时后,所有载体都保持稳定并发生膨胀。在溶解介质中浸泡期间,获得了不同载体上盐酸地尔硫䓬的释放曲线。填充剂的加入(而非填充剂的类型)有助于载体的稳定性,并相对于不含填充剂的载体更快的药物释放(3.5小时)延长了药物释放时间(6.5 - 8.5小时)。总之,含有填充剂的海藻酸盐、琼脂和结冷胶珠可能有助于药物缓释。

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