期刊
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
卷 13, 期 3, 页码 213-220出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/10837450801949509
关键词
alendronate sodium; radiolabeling; technetium-99m; PEG 1500; rectal absorption; in vitro release
Alendronate sodium (ALD) is a bisphosphonate medication used in the treatment and prevention of osteoporosis. Absorption of ALD as oral formulation is very poor (0.5%-1%). Its bioavailability can decrease with food effect. It has some gastrointestinal adverse effects such as gastritis, gastric ulcer, and esophagitis. The aim of this study was to develop a rectal formulation of ALD as an alternative to oral route and to investigate the absorption of it by using gamma scintigraphy. For this reason, ALD was labeled with Technetium-99m (Tc-99m) by direct method. The radiochemical characterization of the Tc-99m-ALD was carried out by paper chromatography, thin layer chromatography, and electrophoresis methods. The labeling efficiency of Tc-99m-ALD was found 99% without significant changes until 6 h postlabeling at room temperature. The rectal suppositories containing Tc-99m-ALD were prepared by fusion method using polyethylene glycol (PEG) 1500. The Tc-99m-labeled ALD suppositories were administrated to rabbits by rectal route. Serial scintigrams over all bodies of the rabbits were obtained at different time intervals using a gamma camera. We found that the rectal absorption of Tc-99m-ALD from suppository formulation was possible. According to our results, this formulation of ALD can be suggested for the therapy of osteoporosis as an alternative route.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据