龚双, 朱春柳, 丁劲松, 甘勇. 聚合物型过饱和给药系统的促吸收机制及研究进展J. 药学学报, 2018,53(8): 1310-1317. doi: 10.16438/j.0513-4870.2018-0159
引用本文: 龚双, 朱春柳, 丁劲松, 甘勇. 聚合物型过饱和给药系统的促吸收机制及研究进展J. 药学学报, 2018,53(8): 1310-1317. doi: 10.16438/j.0513-4870.2018-0159
GONG Shuang, ZHU Chun-liu, DING Jin-song, GAN Yong. Absorption-enhancing mechanisms and advances of polymer-based supersaturated drug delivery systemJ. Acta Pharmaceutica Sinica, 2018,53(8): 1310-1317. doi: 10.16438/j.0513-4870.2018-0159
Citation: GONG Shuang, ZHU Chun-liu, DING Jin-song, GAN Yong. Absorption-enhancing mechanisms and advances of polymer-based supersaturated drug delivery systemJ. Acta Pharmaceutica Sinica, 2018,53(8): 1310-1317. doi: 10.16438/j.0513-4870.2018-0159

聚合物型过饱和给药系统的促吸收机制及研究进展

Absorption-enhancing mechanisms and advances of polymer-based supersaturated drug delivery system

  • 摘要: 过饱和给药系统(supersaturated drug delivery system,SDDS)是利用药物的高能态形式或快速溶出在胃肠道中形成过饱和溶液并维持足够长时间以促进难溶性药物口服吸收的一类给药系统。过饱和溶液属于热力学不稳定体系,易出现药物结晶析出而达不到促吸收的目的。因此,有效维持过饱和溶液稳定是SDDS研发的重点之一。聚合物型过饱和给药系统是以聚合物为沉淀抑制剂的SDDS,聚合物的存在能有效抑制药物结晶沉淀的发生,对于维持过饱和溶液的稳定具有显著作用。然而不同的聚合物有着不同的沉淀抑制能力,目前对于聚合物维持药物溶液过饱和态的机制尚不清楚。因此,本文对聚合物型过饱和给药系统的促吸收机制、体外评价及其研究现状进行综述,以期为SDDS的理性化设计提供参考。

     

    Abstract: Supersaturated drug delivery systems (SDDS) are defined as systems that are able to generate and maintain a sustained drug supersaturation in the gastrointestinal tract, facilitating the oral absorption of drugs with poor water solubility. Supersaturated drug solution is generated from a higher energy form of the drug or rapid dissolution through various formulation options. However, supersaturated solution is a thermodynamically unstable system that can easily lead to drug precipitation, missing the aim of improving the absorption. Therefore, maintenance of the supersaturated state is essential for the development of SDDS. Polymer-based SDDS take polymers as the precipitation inhibitor,which can effectively prevent the precipitation of drugs, generating an excellent effect on maintenance of the stability of supersaturated solution. However, different polymers have distinct anti-precipitation ability, and the mechanisms of such activity supported by the polymer remain unrevealed. In this review, we summarize the research advances in the absorption-enhancing mechanisms and in vitro evaluations of polymers-based SDDS. This review provides a reference for the design of rational SDDS.

     

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