Stability in vitro of methylproscillaridin.
The in vitro stability of methylproscillaridin has been compared with that of proscillaridin, the activities of the glycosides being assayed by the 86Rb-technique. After incubation in gastric juice at pH 1,2, and 3, the activity half life of each glycoside was proportional to pH and was approximately 0.25 h, 2.5 h, and 25 h, respectively. The inactivation rate in pure hydrochloric acid at pH 2 did not differ from that in gastric juice of the same pH. The glycosides were stable in bile and enteric juice. In faeces, methylproscillaridin was stable and proscillaridin was inactivated with a half life of 32 h. It is concluded that the difference in biological availability between the two glycosides cannot be explained by differences in gastrointestinal stability.
D001646:Bile / Q000378:metabolism; D002018:Bufanolides / Q000378:metabolism*; D004355:Drug Stability; D005243:Feces / Q000032:analysis; D005750:Gastric Juice / Q000378:metabolism; D006207:Half-Life; D006801:Humans; D006851:Hydrochloric Acid; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007419:Intestinal Secretions / Q000378:metabolism; D011442:Proscillaridin / Q000031:analogs & derivatives / Q000378:metabolism*; D013997:Time Factors
D002018:Bufanolides; D011442:Proscillaridin; D006851:Hydrochloric Acid