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用于口服格列美脲的固体自乳化药物递送系统(S-SNEDDS):在白化兔中的研发及抗糖尿病活性

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits.

作者信息

Mohd Abdul Bari, Sanka Krishna, Bandi Srikanth, Diwan Prakash V, Shastri Nalini

机构信息

Department of Pharmaceutics, School of Pharmacy, Anurag Group of Institutions , Hyderabad, Andhra Pradesh , India and.

出版信息

Drug Deliv. 2015;22(4):499-508. doi: 10.3109/10717544.2013.879753. Epub 2014 Jan 29.

Abstract

CONTEXT

This study presents novel self-nanoemulsifying drug delivery system potential of oral delivering which leads poorly aqueous soluble drug glimepiride.

OBJECTIVE

The objective of this study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) for the improved oral delivery of glimepiride and to evaluate its therapeutic efficacy in albino rabbits.

RESULTS AND DISCUSSION

The droplet size analyses revealed a droplet size of less than 200 nm. The solid state characterization of S-SNEDDS by scanning electron microscopy (SEM), X-ray powder diffraction and differential scanning calorimetry (DSC) revealed the absence of crystalline glimepiride in the S-SNEDDS. The in vitro dissolution studies revealed that the significant improvement in glimepiride release characteristics. The effect of S-SNEDDS on therapeutic efficacy of glimepride was assessed in albino rabbits by monitoring blood glucose levels and compared with free drug suspension, L-SNEDDS. The S-SNEDDS showed significant (p < 0.05) increase in in vitro drug release and therapeutic efficacy as compared with free drug.

CONCLUSION

This study demonstrated that S-SNEDDS is a promising novel drug delivery system of glimepride to enhance oral delivery.

摘要

背景

本研究提出了一种新型的自纳米乳化药物递送系统,具有口服递送难溶性药物格列美脲的潜力。

目的

本研究的目的是制备固体自纳米乳化药物递送系统(S-SNEDDS)以改善格列美脲的口服递送,并评估其在白化兔中的治疗效果。

结果与讨论

液滴尺寸分析显示液滴尺寸小于200nm。通过扫描电子显微镜(SEM)、X射线粉末衍射和差示扫描量热法(DSC)对S-SNEDDS进行固态表征,结果显示S-SNEDDS中不存在结晶格列美脲。体外溶出度研究表明,格列美脲的释放特性有显著改善。通过监测血糖水平,在白化兔中评估S-SNEDDS对格列美脲治疗效果的影响,并与游离药物混悬液、L-SNEDDS进行比较。与游离药物相比,S-SNEDDS的体外药物释放和治疗效果显著提高(p<0.05)。

结论

本研究表明,S-SNEDDS是一种有前景的新型格列美脲药物递送系统,可增强口服递送效果。

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