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通过GastroPlus软件探索和验证芒果苷的物理化学性质。

Exploring and validating physicochemical properties of mangiferin through GastroPlus software.

作者信息

Khurana Rajneet Kaur, Kaur Ranjot, Kaur Manninder, Kaur Rajpreet, Kaur Jasleen, Kaur Harpreet, Singh Bhupinder

机构信息

University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160014, India; University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160014, India.

Centre with Potential for Excellence in Biomedical Sciences, Panjab University, Chandigarh 160014, India; Centre with Potential for Excellence in Biomedical Sciences, Panjab University, Chandigarh 160014, India.

出版信息

Future Sci OA. 2017 Jan 16;3(1):FSO167. doi: 10.4155/fsoa-2016-0055. eCollection 2017 Mar.

Abstract

AIM

Mangiferin (Mgf), a promising therapeutic polyphenol, exhibits poor oral bioavailability. Hence, apt delivery systems are required to facilitate its gastrointestinal absorption. The requisite details on its physicochemical properties have not yet been well documented in literature. Accordingly, in order to have explicit insight into its physicochemical characteristics, the present work was undertaken using GastroPlus™ software.

RESULTS

Aqueous solubility (0.38 mg/ml), log P (-0.65), P (0.16 × 10 cm/s) and ability to act as P-gp substrate were defined. Potency to act as a P-gp substrate was verified through Caco-2 cells, while P was estimated through single pass intestinal perfusion studies. Characterization of Mgf through transmission electron microscopy, differential scanning calorimetry, infrared spectroscopy and powder x-ray diffraction has also been reported.

CONCLUSION

The values of physicochemical properties for Mgf reported in the current manuscript would certainly enable the researchers to develop newer delivery systems for Mgf.

摘要

目的

芒果苷(Mgf)是一种很有前景的治疗性多酚,但其口服生物利用度较差。因此,需要合适的给药系统来促进其胃肠道吸收。关于其物理化学性质的必要细节在文献中尚未得到充分记载。因此,为了深入了解其物理化学特性,本研究使用GastroPlus™软件进行。

结果

确定了其水溶性(0.38毫克/毫升)、log P(-0.65)、渗透率(0.16×10厘米/秒)以及作为P-糖蛋白底物的能力。通过Caco-2细胞验证了其作为P-糖蛋白底物的潜力,同时通过单通道肠道灌注研究估算了渗透率。还报道了通过透射电子显微镜、差示扫描量热法、红外光谱和粉末X射线衍射对芒果苷进行的表征。

结论

本手稿中报道的芒果苷物理化学性质的值肯定会使研究人员能够开发出芒果苷的新型给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a9f/5351510/882dc71ee2b1/fsoa-03-167-g1.jpg

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