【摘要】：目的以維生素E聚乙二醇琥珀酸酯(VE-TPGS)和聚乙二醇硬脂酸酯15(Solutol HS 15,SHS15)為載體制備姜黃素膠束,并研究該膠束對(duì)姜黃素溶解度和口服生物利用度的影響。方法采用薄膜分散法制備姜黃素膠束;通過(guò)膠束平均粒徑、載藥量、包封率等指標(biāo)表征該膠束,同時(shí)測(cè)定姜黃素的溶解度;通過(guò)體外釋放考察該膠束的釋放特性;進(jìn)一步通過(guò)大鼠實(shí)驗(yàn)評(píng)估膠束對(duì)姜黃素口服生物利用度的影響。結(jié)果當(dāng)VE-TPGS與SHS15加入質(zhì)量比為3∶7時(shí),膠束粒徑為(35.79±1.23)nm,多分散性指數(shù)(PDI)為0.12±0.03;在該條件下,膠束的載藥量和包封率分別為9.34%和90.03%,姜黃素的溶解度達(dá)到2.03 mg/m L;體外釋放實(shí)驗(yàn)中,膠束組較姜黃素組有緩慢釋放特性;大鼠口服生物利用度實(shí)驗(yàn)中,膠束組較姜黃素組的相對(duì)生物利用度提高到303.5%(P0.01)。結(jié)論本實(shí)驗(yàn)制備的膠束不僅有較好的緩釋特性,還提高了姜黃素的溶解度和口服生物利用度。利用藥物-膠束體系來(lái)改善難溶性藥物的溶解度,具有較高的臨床應(yīng)用潛力。
[Abstract]:Objective to prepare curcumin micelles with vitamin E polyethylene glycol succinate (VE-TPGS) and polyethylene glycol stearate (15 (Solutol HS 15 SHS15) as carriers, and to study the effects of the micelles on the solubility and oral bioavailability of curcumin. Methods the curcumin micelles were prepared by thin-film dispersion method. The micelles were characterized by the mean particle size, drug loading and encapsulation efficiency, and the solubility of curcumin was also determined, and the release characteristics of curcumin micelles were investigated by in vitro release. The effects of micelles on oral bioavailability of curcumin were further evaluated in rats. Results when the mass ratio of VE-TPGS to SHS15 was 3:7, the particle size of micelle was (35.79 鹵1.23) nm, polydispersity index (PDI) was 0.12 鹵0.03.The drug loading and entrapment efficiency of micelle were 9.34% and 90.03%, respectively, and the solubility of curcumin was 2.03 mg/m L in vitro release experiment. The relative bioavailability of micelle group was increased to 303.5% compared with curcumin group (P0.01). Conclusion the micelles prepared in this study not only have good sustained-release properties, but also improve the solubility and oral bioavailability of curcumin. It has high clinical application potential to improve the solubility of insoluble drugs by using drug-micelle system.
【作者單位】： 南通市中醫(yī)院;江蘇省中醫(yī)藥研究院;
【分類號(hào)】：R943

【參考文獻(xiàn)】

相關(guān)期刊論文 前10條

1 劉碧林;石明芯;朱照靜;晏聲蕾;張景R，

本文編號(hào)：2212809