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Purpose <p>Andrographolide (AG), a phytopharmaceutical maker from <i>Andrographis paniculata</i>, is a BCS Class II compound with limited solubility, dissolution, and bioavailability. The present study aimed to investigate the physicochemical properties, dissolution, stability, pharmacokinetics, and acute toxicity of <i>Andrographis paniculata</i> extract (APE). Effects of liquid vehicles were systematically investigated.</p> Methods <p>Solubility of AG was determined. APE liquisolid powders were fabricated using different solvents. Their flowability, AG content, FTIR, PXRD, ESEM, dissolution, and storage stability were investigated. Oral absorption and acute oral toxicity were evaluated in Wistar rats.</p> Results <p>APE liquisolid powders based on N-methyl-2-pyrrolidone (NMP, AG solubility 38.12%), diethylene glycol monoethyl ether (DG, AG solubility 1.3%), and NMP/DG mixtures exhibited acceptable flowability and a uniform content. Inclusion of volatile solvent ethanol, together with DG, during manufacture of liquisolid powder significantly improved the dissolution and bioavailability of DG-based powder to levels comparable to those of NMP-based formulation. Compared with that of the physical mixture, the dissolution efficiency improvements ranged between 2.7−3.6-fold, and bioavailability improvements at an AG dose of 30&#xa0;mg/kg body weight ranged between 4.9−6.2-fold. A stability study indicated that only liquisolid powder made of NMP maintained the noncrystalline state and dissolution characteristics of AG component after 3-month storage. APE and liquisolid powder formulations exhibited an LD<sub>50</sub> &gt; 5000&#xa0;mg/kg body weight.</p> Conclusion <p>Liquisolid systems successfully increased the dissolution and bioavailability of AG. These research findings underscore the promise of liquisolid systems with a suitable liquid vehicle for increasing the effectiveness with low toxicity of oral formulations of AG and APEs.</p>

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Liquisolid powders of Andrographis paniculata extract: physicochemical attributes, dissolution, oral bioavailability, stability, and acute toxicity

  • 期刊论文

  • 发表日期：

    2026年1月8日

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  • Peera Tabboon,
  • Ekapol Limpongsa,
  • Rarinthorn Samrid,
  • Supawan Wechprakhon,
  • Jidapa Niyommoh,
  • Napaphak Jaipakdee

摘要

Purpose

Andrographolide (AG), a phytopharmaceutical maker from Andrographis paniculata, is a BCS Class II compound with limited solubility, dissolution, and bioavailability. The present study aimed to investigate the physicochemical properties, dissolution, stability, pharmacokinetics, and acute toxicity of Andrographis paniculata extract (APE). Effects of liquid vehicles were systematically investigated.

Methods

Solubility of AG was determined. APE liquisolid powders were fabricated using different solvents. Their flowability, AG content, FTIR, PXRD, ESEM, dissolution, and storage stability were investigated. Oral absorption and acute oral toxicity were evaluated in Wistar rats.

Results

APE liquisolid powders based on N-methyl-2-pyrrolidone (NMP, AG solubility 38.12%), diethylene glycol monoethyl ether (DG, AG solubility 1.3%), and NMP/DG mixtures exhibited acceptable flowability and a uniform content. Inclusion of volatile solvent ethanol, together with DG, during manufacture of liquisolid powder significantly improved the dissolution and bioavailability of DG-based powder to levels comparable to those of NMP-based formulation. Compared with that of the physical mixture, the dissolution efficiency improvements ranged between 2.7−3.6-fold, and bioavailability improvements at an AG dose of 30 mg/kg body weight ranged between 4.9−6.2-fold. A stability study indicated that only liquisolid powder made of NMP maintained the noncrystalline state and dissolution characteristics of AG component after 3-month storage. APE and liquisolid powder formulations exhibited an LD50 > 5000 mg/kg body weight.

Conclusion

Liquisolid systems successfully increased the dissolution and bioavailability of AG. These research findings underscore the promise of liquisolid systems with a suitable liquid vehicle for increasing the effectiveness with low toxicity of oral formulations of AG and APEs.