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探索固体分散体在提高草药提取物、富集成分和生物活性物质的溶解度、溶出度及生物利用度方面的潜力。

Exploring the potential of solid dispersion for improving solubility, dissolution & bioavailability of herbal extracts, enriched fractions, and bioactives.

作者信息

Mohapatra Debadatta, Agrawal Ashish K, Sahu Alakh N

机构信息

Phytomedicine Research Lab., Department of Pharmaceutical Engineering & Technology, IIT (BHU), Varanasi, India.

出版信息

J Microencapsul. 2021 Nov-Dec;38(7-8):594-612. doi: 10.1080/02652048.2021.1963342. Epub 2021 Aug 17.

Abstract

Most drugs' poor aqueous solubility has emerged as a significant challenge in achieving proper therapeutic response following oral administration. Herbal drugs are being used from time immemorial to prevent, mitigate, and cure multiple diseases. However, most of the bioactives phytoconstituents possess limited aqueous solubility & poor oral bioavailability. Solid dispersion (SD) has been realised as an efficient formulation to overcome hydrophobic candidates' solubility issues and improve their oral bioavailability. The current review mainly explores the potential of SD for improving solubility, dissolution & bioavailability of herbal extracts, enriched fractions, and isolated bioactives. Hence, basics of SD, selection of excipients, need for SD of plant products, SD of plant products, selection of preparation method, the chemistry of phytoconstituent-excipient interaction, and hurdles associated with SD of herbal extract/enriched fraction were explored in this review. The SD has the potential to overcome solubility, dissolution, and oral bioavailability issues of poorly soluble phytoconstituents.

摘要

大多数药物的水溶性差已成为口服给药后实现适当治疗反应的重大挑战。自古以来,草药就被用于预防、减轻和治疗多种疾病。然而,大多数生物活性植物成分的水溶性有限且口服生物利用度差。固体分散体(SD)已被认为是一种有效的制剂,可克服疏水性候选物的溶解性问题并提高其口服生物利用度。本综述主要探讨了固体分散体在提高草药提取物、富集组分和分离生物活性成分的溶解度、溶出度和生物利用度方面的潜力。因此,本综述探讨了固体分散体的基本原理、辅料的选择、植物产品固体分散体的必要性、植物产品的固体分散体、制备方法的选择、植物成分与辅料相互作用的化学以及与草药提取物/富集组分固体分散体相关的障碍。固体分散体有潜力克服难溶性植物成分的溶解度、溶出度和口服生物利用度问题。

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