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Development of an improved oral drug delivery system for the absorbable active components of Danshen.

机译：开发了用于丹参可吸收活性成分的改进的口服药物递送系统。

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摘要

Background. Danshen, the dried root of Salvia miltiorrhiza Bge, is used for treating coronary heart disease. In China, numerous pharmaceutical dosage forms of Danshen are commercially available. Although the pharmacological effects of different components of Danshen are well identified, its absorption as well as pharmacokinetics studies are still insufficient and inconsistent. The current study aims to: (1) screen for the major absorbable active components of Danshen; (2) interpret the absorption mechanism and pharmacokinetics characteristics of the identified components; (3) develop an improved oral drug delivery system for the identified components of Danshen.;Methods. Six major active components in commercially available Danshen products were identified and quantified. In vitro human Caco-2 cell monolayer model, rat in situ intestinal perfusion model as well as rat in vivo pharmacokinetic model were used to investigate the intestinal absorption and pharmacokinetics profiles of the identified Danshen components. Effect of the absorption enhancer on the oral absorption and bioavailabilities of the studied Danshen components was further evaluated.;Results. Danshensu, salvianolic acid B (SAB) and protocatechuic aldehyde (PCA) were identified as the major components in Danshen products. Investigations using in vitro, in situ and in vivo model found that both danshensu and SAB had poor permeabilities and low bioavailabilities (Danshensu: 11.09%; SAB: 3.90%), which may be due to their absorption via the paracellular transport pathways. Studies of PCA suggested that it may have a intestinal first pass metabolism with an oral bioavailability of only 18.02%. It was found that the permeabilities of both danshensu and SAB were significantly increased upon addition of sodium caprate, a paracellular absorption enhancer. The oral bioavailabilities of both danshensu and SAB in pure compound form as well as Danshen extract form were also increased in the presence of sodium caprate in rats.;Conclusion. Both danshensu and SAB have limited intestinal permeability and oral bioavailabilities. Our results demonstrated the usefulness of sodium caprate as a potential absorption enhancer for danshensu and SAB in Danshen product.
机译：背景。丹参，丹参干根，用于治疗冠心病。在中国，丹参的多种药物剂型是可商购的。尽管已很好地确定了丹参不同成分的药理作用，但其吸收以及药代动力学研究仍不足且不一致。目前的研究旨在：（1）筛选丹参的主要可吸收活性成分； （2）解释所鉴定成分的吸收机理和药代动力学特征； （3）为丹参中已确定的成分开发了一种改进的口服药物递送系统。鉴定和定量了市售丹参产品中的六种主要活性成分。使用体外人Caco-2细胞单层模型，大鼠原位肠灌注模型以及大鼠体内药代动力学模型来研究已鉴定的丹参成分的肠道吸收和药代动力学特征。进一步评估了吸收促进剂对所研究的丹参成分口服吸收和生物利用度的影响。丹参素，丹酚酸B（SAB）和原儿茶醛（PCA）被确定为丹参产品的主要成分。使用体外，原位和体内模型进行的研究发现，丹参素和SAB的渗透性均很差，生物利用度较低（丹参素：11.09％； SAB：3.90％），这可能是由于它们通过旁细胞运输途径吸收了。 PCA的研究表明，它可能具有肠道首过代谢，口服生物利用度仅为18.02％。结果发现，加入碳酸氢钠（一种旁细胞吸收促进剂）后，丹参素和SAB的通透性均显着增加。在大鼠中加入碳酸氢钠时，丹参素和SAB的纯化合物形式以及丹参提取物形式的口服生物利用度也均增加。丹参素和SAB的肠道通透性和口服生物利用度均有限。我们的结果证明了癸酸钠作为丹参素和丹参产品中SAB的潜在吸收促进剂的有用性。

著录项

  • 作者

    Zhou, Limin.;

  • 作者单位

    The Chinese University of Hong Kong (Hong Kong).;

  • 授予单位 The Chinese University of Hong Kong (Hong Kong).;
  • 学科 Health Sciences Pharmacology.
  • 学位 Ph.D.
  • 年度 2008
  • 页码 218 p.
  • 总页数 218
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药理学;
  • 关键词

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