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载有三七总皂苷的 BSP/海藻酸钠微球治疗酒精性胃溃疡的疗效改善。

Improved efficacy of Panax notoginseng saponin loaded into BSP/alginate microspheres for the treatment of alcoholic gastric ulcers.

机构信息

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing City, Jiangsu Province 210023, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing City, Jiangsu Province 210023, China.

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing City, Jiangsu Province 210023, PR China; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing City, Jiangsu Province 210023, China.

出版信息

Int J Pharm. 2021 Mar 1;596:120218. doi: 10.1016/j.ijpharm.2021.120218. Epub 2021 Jan 23.

Abstract

Previously, we have reported the evaluations of alginate and Bletilla striata polysaccharide (BSP) in formulation of microsphere, which is a muco-adhesive carrier and can achieve a long duration of gastric retention. The combination of Panax notoginseng (Burk.) and B. striata is a traditional Chinese herbal formula that is used to treat gastric ulcers. BSP, an effective ingredient of B. striata, possesses both medicinal and excipient functions. Panax notoginseng saponin (PNS), which can easily dissolve in water, is the main effective ingredient in P. notoginseng (Burk.) for the treatment of gastric ulcers. However, microspheres containing PNS could directly cause drug leakage, ultimately reducing the encapsulation rate. In this study, PNS was fabricated into a hydrophobic dispersion with slow-release characteristics. Subsequently, PNS was packaged into BSP/alginate microspheres to improve the encapsulation rate. The prepared PNS-loaded microspheres were round, the release characteristics aligned with the Weibull equation, and the active ingredients were released by diffusion and erosion. The developed microspheres improved the effects of PNS and synergistically exerted the pharmaceutical effects of BSP on acute gastric ulcers.

摘要

先前,我们报道了海藻酸钠和白及多糖(BSP)在微球制剂中的评价,BSP 是一种具有黏膜黏附性的载体,可以实现胃滞留时间的延长。三七和白及的组合是一种传统的中药方剂,用于治疗胃溃疡。BSP 是白及的有效成分,具有药用和赋形剂的双重功能。人参皂苷(PNS),易溶于水,是三七(Burk.)治疗胃溃疡的主要有效成分。然而,含有 PNS 的微球可能会直接导致药物泄漏,最终降低包封率。在本研究中,将 PNS 制成具有缓释特性的疏水性分散体。随后,将 PNS 包封到 BSP/海藻酸钠微球中,以提高包封率。制备的载 PNS 微球呈圆形,释放特性符合 Weibull 方程,活性成分通过扩散和侵蚀释放。开发的微球提高了 PNS 的效果,并协同发挥了 BSP 对急性胃溃疡的药效作用。

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