Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, People's Republic of China.
Drug Dev Ind Pharm. 2013 Jan;39(1):109-16. doi: 10.3109/03639045.2012.659189. Epub 2012 Feb 18.
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.
本文的主要目的是通过两种方法提高含有 20(S)-原人参二醇（PPD）和 20(S)-原人参三醇（PPT）的人参皂苷（GS）的溶解和生物利用度，并将其与 GS 提取物的体外和体内性能进行比较。通过热熔挤出（HME）制备 GS 固体分散体（SD），通过共研磨制备 GS 共研磨混合物。在 500 mL 0.1%十二烷基硫酸钠（SDS）水溶液中，与 GS 提取物相比，GS-SD 和 GS 共研磨混合物的溶解都得到了改善。并且 GS-SD 的溶解度超过 90%，优于溶解度约为 70%的 GS 共研磨混合物。在 GS-SD、GS 共研磨混合物和 GS 提取物中，PPD 的 AUC(0 → 48)分别为 1439.9 ± 435.71、1618.2 ± 571.9 和 1089.8 ± 359.9 ng·h/mL，PPT 的 AUC(0 → 48)分别为 683.1 ± 197.7、736.0 ± 226.0 和 439.8 ± 193.6 ng·h/mL。结果表明，GS-SD 和 GS 共研磨混合物的生物利用度优于 GS 提取物，但 GS-SD 的生物利用度低于 GS 共研磨混合物，这与溶解度的结果不一致。这一结果可能是由于 GS 共研磨混合物中的磷脂起到了促进吸收的作用。显然，热熔挤出和共研磨都可以提高 GS 的溶解和生物利用度。
