Improvement of dissolution and bioavailability of Ginsenosides by hot melt extrusion and cogrinding

Drug Dev Ind Pharm. 2013 Jan;39(1):109-16. doi: 10.3109/03639045.2012.659189. Epub 2012 Feb 18.

Abstract

The main purpose of this paper was to improve the dissolution and bioavailability of Ginsenosides (GS) which contained 20(S)-protopanaxadiol (PPD) and 20(S)-protopanaxatriol (PPT) by two methods, and to compare their performance in vitro and in vivo with GS extracts. GS-solid dispersion (SD) were prepared by hot melt extrusion (HME), and GS coground mixture were prepared by cogrinding. In 500 mL 0.1% sodium dodecyl sulfate (SDS) aqueous solution, dissolution of GS-SD and GS coground mixture were both improved comparing with GS extracts. And dissolution of GS-SD was above 90%, which was better than GS coground mixture whose dissolution was about 70%. In GS-SD, GS coground mixture and GS extracts, the AUC(0 → 48) of PPD were 1439.9 ± 435.71, 1618.2 ± 571.9 and 1089.8 ± 359.9 ng · h/mL, and the AUC(0 → 48) of PPT were 683.1 ± 197.7, 736.0 ± 226.0 and 439.8 ± 193.6 ng · h/mL. The results revealed that bioavailability of GS-SD and GS coground mixture was better than GS extracts, but bioavailability of GS-SD was lower than GS coground mixture, which was not consistent with the results of dissolution. The results perhaps caused by the phospholipid in GS coground mixture which played a role as absorption enhancement. It is apparent that both HME and cogrinding can improve the dissolution and bioavailability of GS.

MeSH terms

  • Animals
  • Biological Availability
  • Dogs
  • Drug Compounding / methods*
  • Female
  • Ginsenosides / chemistry
  • Ginsenosides / pharmacokinetics*
  • Hot Temperature
  • Male
  • Solubility

Substances

  • Ginsenosides