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二氢杨梅素胃漂浮缓释片:研制、表征及药代动力学研究

Gastric floating sustained-release tablet for dihydromyricetin: Development, characterization, and pharmacokinetics study.

作者信息

Liu Hao, Zhao Wenmei, Hu Qi, Zhao Ling, Wei Yumeng, Pi Chao, Yang Yuhan, Yang Xuerong, Yuan Hang, Zhang Yuhan, Qu Kunyan, Shi Xinyu, Huang Yao, Shi Houyin

机构信息

School of Pharmacy, Southwest Medical University, Luzhou City, Sichuan, People's Republic of China.

School of Clinical Medicine, Southwest Medical University, Luzhou City, Sichuan, People's Republic of China.

出版信息

Saudi Pharm J. 2019 Nov;27(7):1000-1008. doi: 10.1016/j.jsps.2019.08.002. Epub 2019 Aug 8.

Abstract

Dihydromyricetin (DHM) is a natural dihydroflavonol compound with quite a number of important pharmacological properties. However, its low solubility in water and poor stability in aqueous environment, have compromised drug efficacy of DHM, thus hindering its clinical use. The present study was to develop DHM-loaded gastric floating sustained-release tablet (DHM-GFT) to improve the bioavailability of DHM. DHM-GFT was prepared via powder direct compression. The formulation of tablet was optimized in terms of the floating ability and drug release rate. The optimized DHM-GFT exhibited short floating lag time of less than 10 s and long floating duration of over 12 h in acidic medium. It had a 12-hour sustained release of DHM, which proved its potential to develop as a twice-a-day dosing preparation. The physicochemical properties of DHM-GFT well satisfied the pharmacopoeial requirements. In addition, the results from pharmacokinetic studies demonstrated that, DHM-GFT could considerably prolong the residence time of drug and improve the bioavailability via good gastric floating ability and sustained drug release when compared to DHM powder. Therefore, DHM-GFT is promising to promote the application of DHM and merits studies for further development.

摘要

二氢杨梅素(DHM)是一种具有众多重要药理特性的天然二氢黄酮醇化合物。然而,其在水中的低溶解度以及在水性环境中的稳定性较差,削弱了DHM的药物疗效,从而阻碍了其临床应用。本研究旨在开发载有二氢杨梅素的胃漂浮缓释片(DHM-GFT)以提高二氢杨梅素的生物利用度。DHM-GFT通过粉末直接压片法制备。片剂的配方在漂浮能力和药物释放速率方面进行了优化。优化后的DHM-GFT在酸性介质中表现出小于10秒的短漂浮滞后时间和超过12小时的长漂浮持续时间。它具有12小时的二氢杨梅素缓释效果,证明了其作为每日两次给药制剂开发的潜力。DHM-GFT的理化性质完全符合药典要求。此外,药代动力学研究结果表明,与二氢杨梅素粉末相比,DHM-GFT通过良好的胃漂浮能力和持续药物释放可显著延长药物的驻留时间并提高生物利用度。因此,DHM-GFT有望促进二氢杨梅素的应用,值得进一步开展研究以进行深入开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/91d8/6978620/3f61687bbd86/gr1.jpg

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