Suppr超能文献

通过乳化溶剂蒸发法和冷冻干燥法相结合制备并表征的花旗松素-γ-环糊精包合物具有高水溶性。

The high water solubility of inclusion complex of taxifolin-γ-CD prepared and characterized by the emulsion solvent evaporation and the freeze drying combination method.

作者信息

Zu Yuangang, Wu Weiwei, Zhao Xiuhua, Li Yong, Zhong Chen, Zhang Yin

机构信息

Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, Heilongjiang, China.

Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, Heilongjiang, China.

出版信息

Int J Pharm. 2014 Dec 30;477(1-2):148-58. doi: 10.1016/j.ijpharm.2014.10.027. Epub 2014 Oct 16.

Abstract

This study selected γ-cyclodextrin (γ-CD) as the inclusion material and prepared inclusion complex of taxifolin-γ-CD by the emulsion solvent evaporation and the freeze drying combination method to achieve the improvement of the solubility and oral bioavailability of taxifolin. We selected ethyl acetate as the oil phase, deionized water as the water phase. The taxifolin emulsion was prepared using adjustable speed homogenate machine in the process of this experiment, whose particle size was related to the concentration of taxifolin solution, the volume ratio of water phase to oil phase, the speed and time of homogenate. We knew through the single-factor test that, the optimum conditions were: the concentration of taxifolin solution was 40 mg/ml, the volume ratio of water phase to oil phase was 1.5, the speed of homogenate was 5,000 rpm, the homogenate time was 11 min. Taxifolin emulsion with a MPS of 142.5 nm was obtained under the optimum conditions, then the high-concentration taxifolin solution (3mg/ml) was obtained by the rotary evaporation process. Finally, the inclusion complex of taxifolin-γ-CD was prepared by vacuum freeze-dry. The characteristics of the inclusion complex of taxifolin-γ-CD were analyzed using SEM, FTIR, XRD, DSC, and TG. The FTIR results analyzed the interaction of taxifolin and γ-CD and determined the molecular structure of the inclusion complex of taxifolin-γ-CD. The analysis results of XRD, DSC and TG indicated that the inclusion complex of taxifolin-γ-CD was obtained and showed significantly different characteristics with taxifolin. In addition, dissolving capability test, antioxidant capacity test, solvent residue test were also carried out. The experimental datas showed that the solubility of inclusion complex of taxifolin-γ-CD at 25°C and 37°C were about 18.5 times and 19.8 times of raw taxifolin, the dissolution rate of inclusion complex of taxifolin-γ-CD were about 2.84 times of raw taxifolin, the bioavailability of inclusion complex of taxifolin-γ-CD increased 3.72 times compared with raw taxifolin, and the antioxidant capacity of inclusion complex of taxifolin-γ-CD was also superior to raw taxifolin. Furthermore, the amounts of residual solvent of the inclusion complex of taxifolin-γ-CD were suitable for pharmaceutical use. These results suggested that inclusion complex of taxifolin-γ-CD may have potential value to become a new oral taxifolin formulation with high solubility.

摘要

本研究选用γ-环糊精(γ-CD)作为包合材料,采用乳化溶剂蒸发法与冷冻干燥法相结合制备了花旗松素-γ-CD包合物,以提高花旗松素的溶解度和口服生物利用度。我们选用乙酸乙酯作为油相,去离子水作为水相。在本实验过程中,使用可调速匀质机制备花旗松素乳液,其粒径与花旗松素溶液浓度、水相与油相的体积比、匀质速度和时间有关。通过单因素试验可知,最佳条件为:花旗松素溶液浓度为40mg/ml,水相与油相的体积比为1.5,匀质速度为5000rpm,匀质时间为11min。在最佳条件下获得了平均粒径为142.5nm的花旗松素乳液,然后通过旋转蒸发法得到高浓度花旗松素溶液(3mg/ml)。最后,通过真空冷冻干燥制备花旗松素-γ-CD包合物。采用扫描电子显微镜(SEM)、傅里叶变换红外光谱仪(FTIR)、X射线衍射仪(XRD)、差示扫描量热仪(DSC)和热重分析仪(TG)对花旗松素-γ-CD包合物的特性进行分析。FTIR结果分析了花旗松素与γ-CD的相互作用,并确定了花旗松素-γ-CD包合物的分子结构。XRD、DSC和TG的分析结果表明,已获得花旗松素-γ-CD包合物,且其与花旗松素表现出显著不同的特性。此外,还进行了溶解能力试验、抗氧化能力试验和溶剂残留试验。实验数据表明,花旗松素-γ-CD包合物在25℃和37℃时的溶解度分别约为花旗松素原料药的18.5倍和19.8倍,花旗松素-γ-CD包合物的溶出速率约为花旗松素原料药的2.84倍,花旗松素-γ-CD包合物的生物利用度比花旗松素原料药提高了3.72倍,且花旗松素-γ-CD包合物的抗氧化能力也优于花旗松素原料药。此外,花旗松素-γ-CD包合物的残留溶剂量符合药用要求。这些结果表明,花旗松素-γ-CD包合物可能具有成为一种高溶解度新型口服花旗松素制剂的潜在价值。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验