[Optimize preparation of compound licorice microemulsion with D-optimal design]

Zhongguo Zhong Yao Za Zhi. 2018 Mar;43(6):1131-1138. doi: 10.19540/j.cnki.cjcmm.20180105.010.
[Article in Chinese]

Abstract

In order to increase the solubility of essential oil in compound licorice microemulsion and improve the efficacy of the decoction for treating chronic eczema, this experiment intends to prepare the decoction into microemulsion. The essential oil was used as the oil phase of the microemulsion and the extract was used as the water phase. Then the microemulsion area and maximum ratio of water capacity was obtained by plotting pseudo-ternary phase diagram, to determine the appropriate types of surfactant and cosurfactant, and Km value-the mass ratio between surfactant and cosurfactant. With particle size and skin retention of active ingredients as the index, microemulsion prescription was optimized by D-optimal design method, to investigate the in vitro release behavior of the optimized prescription. The results showed that the microemulsion was optimal with tween-80 as the surfactant and anhydrous ethanol as the cosurfactant. When the Km value was 1, the area of the microemulsion region was largest while when the concentration of extract was 0.5 g·mL⁻¹, it had lowest effect on the particle size distribution of microemulsion. The final optimized formulation was as follows: 9.4% tween-80, 9.4% anhydrous ethanol, 1.0% peppermint oil and 80.2% 0.5 g·mL⁻¹ extract. The microemulsion prepared under these conditions had a small viscosity, good stability and high skin retention of drug; in vitro release experiment showed that microemulsion had a sustained-release effect on glycyrrhizic acid and liquiritin, basically achieving the expected purpose of the project.

Keywords: D-optimal design method; compound licorice microemulsion; essential oil; in vitro release; prescription optimization; skin retention.

MeSH terms

  • Delayed-Action Preparations
  • Drugs, Chinese Herbal / chemistry*
  • Emulsions*
  • Ethanol
  • Flavanones
  • Glucosides
  • Glycyrrhiza / chemistry*
  • Glycyrrhizic Acid
  • Polysorbates
  • Solubility
  • Surface-Active Agents

Substances

  • Delayed-Action Preparations
  • Drugs, Chinese Herbal
  • Emulsions
  • Flavanones
  • Glucosides
  • Polysorbates
  • Surface-Active Agents
  • Ethanol
  • Glycyrrhizic Acid
  • liquiritin