| Disease | THE PHARMACOKINETICS OF Z-GUGGULSTERONE AND ITS METABOLITE, E-GUGGULSTERONE WAS STUDIED IN RATS AFTER ORAL (50 MG/KG) AND INTRAVENOUS (18 MG/KG) ADMINISTRATION, IT WAS OBSERVED THAT 1A WAS ISOMERIZED TO 1B IN TREATED RAT SERUM SAMPLES. SERUM
LEVELS OF GUGGULSTERONE AFTER INTRAVENOUS ADMINISTRATION SHOWED A BIEXPONENTIAL ELIMINATION PHASE WITH A MEAN +/- S.D. TERMINAL HALF-LIFE OF 10-02 +/- 4.74 H AND 9.24 +/- 3.32 H FOR 1A AND 1B ISOMERS, RESPECTIVELY. THE VALUES OF SYSTEMIC CLEARENCE AND
AUC FOR BOTH 1A AND 1B WERE OBSERVED TO BE 0.71 L/HR, 4.99 MCG/H/ML AND 1.04 L/HR, 3.65 MCG/H/ML, RESPECTIVELY. AFTER ORAL ADMINISTRATION, THE CONCENTRATION-TIME PROFILE DECLINED IN A MONOEXPONENTIAL FASHION WITH THE VALUE OF C-MAX,
TERMINAL HALF-LIFE, CLEARANCE AND AUC FOR 1A AND 1B BEING 1.07 MCG/ML, 4.48 HR, 1.76 L/HR, 5.95 MCG/H/ML AND 0.97 MCG/ML, 3.56 HR, 2.24 L/HR AND 4.75 MCG/HR/ML, RESPECTIVELY. ABSOLUTE BIOAVAILABILITY OF PARENT COMPOUND (1A) AFTER ORAL
ADMINISTRATION WAS 42.9%. |