title: Improvement of dissolution and bioavailability of Ginsenosides by hot melt extrusion and cogrinding.
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.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, People's Republic of China.
authors.forename: Yanfei
authors.initials: Y
authors.lastname: Luo
authors.forename: Lishuang
authors.initials: L
authors.lastname: Xu
authors.forename: Ming
authors.initials: M
authors.lastname: Xu
authors.forename: Xiaoguang
authors.initials: X
authors.lastname: Tao
authors.forename: Ruiting
authors.initials: R
authors.lastname: Ai
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D000818:Animals; D001682:Biological Availability; D004285:Dogs; D004339:Drug Compounding / Q000379:methods*; D005260:Female; D036145:Ginsenosides / Q000737:chemistry / Q000493:pharmacokinetics*; D006358:Hot Temperature; D008297:Male; D012995:Solubility
chemical_list: D036145:Ginsenosides