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

• Published in: Drug development and industrial pharmacy 2013-01, Vol.39 (1), p.109-116
• Main Authors: Luo, Yanfei, Xu, Lishuang, Xu, Ming, Tao, Xiaoguang, Ai, Ruiting, Tang, Xing
• Format: Article
• Language: English
• Subjects: Animals; bioavailability; Biological Availability; cogrinding; dissolution; Dogs; Drug Compounding - methods; Female; Ginsenosides; Ginsenosides - chemistry; Ginsenosides - pharmacokinetics; hot melt extrusion; Hot Temperature; Male; Solubility
• ISSN: 0363-9045; 1520-5762
• DOI: 10.3109/03639045.2012.659189

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 AUC0→48 of PPD were 1439.9 ± 435.71, 1618.2 ± 571.9 and 1089.8 ± 359.9 ng·h/mL, and the AUC0→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.