Solid self-microemulsifying drug delivery system of Sophoraflavanone G: Prescription optimization and pharmacokinetic evaluation

Eur J Pharm Sci. 2019 Aug 1:136:104953. doi: 10.1016/j.ejps.2019.06.007. Epub 2019 Jun 5.

Abstract

Sophoraflavanone G (SFG) is promising component in clinical treatment. The purpose of this study was to develop a drug delivery system in order to improve oral bioavailability of SFG. The optimum formulation of Self-microemulsifying Drug Delivery System with SFG (SFG-SMEDDS) was selected by the solubility test, self-emulsifying grading test and ternary phase diagram test. The optimized formulation of SFG-S-SMEDDS was composed of Ethyl Oleate (38.5%, w/w), Cremophor RH40 (47.5%, w/w), PEG 400 (14.0%, w/w), and drug loading (20 mg/g). Mannitol as a solid absorbent was added to SFG-SMEDDS formulation with the mass adsorption ratio of 2:1 (w/w). The vitro release rate of SFG-S-SMEDDS reached 60% in 10 min and 80% in 30 min. After SD rats were given SFG and SFG-S-SMEDDS by oral administration, it was found that the area under the curve of SFG-S-SMEDDS was significantly larger than that of SFG suspension and the relative bioavailability of SFG in rats was 343.84%. In addition, the SFG-S-SMEDDS did not change greatly within 3 months. Therefore, the results show that SFG-S-SMEDDS can significantly improve the oral bioavailability of SFG so as to lay a foundation of further research on the new dosage form of SFG.

Keywords: Bioavailability; Pharmacokinetic; Solid Self-microemulsifying Drug Delivery System (S-SMEDDS); Sophoraflavanone G (SFG).

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems / methods
  • Emulsions / chemistry*
  • Emulsions / pharmacokinetics*
  • Flavanones / chemistry*
  • Flavanones / pharmacokinetics*
  • Male
  • Polyethylene Glycols / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Solubility / drug effects
  • Surface-Active Agents / chemistry

Substances

  • Emulsions
  • Flavanones
  • Surface-Active Agents
  • cremophor
  • Polyethylene Glycols
  • vexibinol
  • polyethylene glycol 400