共查询到4条相似文献,搜索用时 0 毫秒
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Hermens Walter A. J. J. Deurloo Marc J. M. Romeyn Stefan G. Verhoef J. Coos Merkus Frans W. H. M. 《Pharmaceutical research》1990,7(5):500-503
A new formulation for nasal administration containing 17-estradiol (E2) with dimethyl--cyclodextrin (DMC) as a solubilizer and absorption enhancer is described. Nasal administration of this E2-DMC formulation gave a significantly higher E2 absorption than an E2 suspension in both rabbits and rats. Relative to an intravenous injection of the E2-DMC formulation, absolute bioavailabilities of 94.6 and 67.2% were calculated for the nasal E2-DMC formulation in rabbits and rats, respectively. Differences in bioavailability may have resulted from differences in experimental animal conditions. The effects on human nasal ciliary activity of the E2-DMC formulation were studied with an in vitro method. The formulation was found to exert only a minor effect on ciliary beat frequency. Thus, nasal delivery of E2, using a cyclodextrin inclusion formulation, may have potential for clinical application, e.g., in the therapy of postmenopausal disorders. 相似文献
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Arong Gaowa Tomohisa Horibe Masayuki Kohno Koji Kawakami 《Journal of pharmaceutical sciences》2018,107(5):1322-1329
The aim of this study was to improve the oral absorption of epidermal growth factor receptor–targeted hybrid peptide using bile acid as an absorption enhancer. The oral formulation of this peptide was formed through electrostatic interactions between the cationic peptide and anionic bile acid. Comparative studies of in vitro cell permeability and in vivo antitumor effects of peptide and peptide/bile acid complex were performed in Caco-2 cells and in a xenograft mouse model of human gastric cancer. The in vitro permeability of peptide/bile acid complex across Caco-2 cell monolayers was significantly enhanced to about 5.0-fold over those of peptide alone. Furthermore, in vivo mouse xenograft model treated with peptide/bile acid complex showed a 1.6-fold reduction in the mean tumor volume as compared with the peptide alone. A preliminary safety evaluation of blood cells counts, liver enzyme levels, and histopathology of gastrointestinal tissues and main organs showed that the peptide/bile acid complex did not induce any acute toxicity. These results suggest that bile acid is an effective absorption enhancer for improving the oral bioavailability and bioactivity of epidermal growth factor receptor–targeted hybrid peptide. 相似文献
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Ville Vartiainen Luis M. Bimbo Jouni Hirvonen Esko I. Kauppinen Janne Raula 《Pharmaceutical research》2017,34(1):25-35