|
KMID : 0369820040340050385
|
|
Jorunal of Korean Pharmaceutical Sciences
2004 Volume.34 No. 5 p.385 ~ p.391
|
|
|
Solubilization of IH-901, a Novel Intestinal Metabolite of Ginseng Saponin, in Aqueous Solution
|
|
권오승/Kwon OS
정연복/Chung YB
|
|
|
Abstract
|
|
|
|
The purpose of the present study was to formulate the aqueous solution of 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol (IH-901), an intestinal bacterial metabolic derivative from Ginseng protopanaxadiol saponin. For this pur-pose, the effects of various solubilization agents such as cosolvents [ethanol, propylene glycol (PG), polyethylene glycol 300 (PEG 300). polyethylene glycol 400 (PEG 400), glycerin], surfactants (Tween 80, Cremophor RH40, Cremophor？EL, Poloxamer 407, Poloxamer 188) and a complexation agent [hydroxypropyl-β-cyclodextrin (HPBCD)], on the solubility of IH-901 in aqueous solution were evaluated. The solubility of IH-901 in water was under 1 μg/ml at 20℃. Cosolvents such as ethanol, PG, PEG 300, PEG 400 and glycerin did not enhance the solubility of IH-901 at the 0 - 40% concentration range. The solubility of IH-901 was significantly elevated by the addition of cosolvents over the 80% concentration range. On the other hand. tween 80, Cremophor" EL, Cremophor" RH40 and HPBCD showed enhanced effects on the solubility of IH-901. The enhanced effects of Poloxamer 407 or Poloxamer 188 on the IH-901 solubility were less pronounced compared with Cremophor" EL or Cremophor` RH40. As a results. Cremophor"` aqueous solution was selected as an optimum solvent system. The aqueous solutions containing 10% Cremophor EL and 7% Cremophor` RH40 were formulated as dosing solutions containing 5.0 mg/ml of IH-901 for its intravenous and oral administration, respectively. The formular showed physical stability after stored for 7 days at 4℃.
|
|
|
KEYWORD
|
|
|
20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol (IH-901), Solubility, Stability, Cosolvent, Surfactant
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
|
|