Two kinds of Ipriflavone tablets (IP) were orally cross administered to 8 healthy volunteers. The serum level of IP at different time was determined by HPLC, 3P87 pharmacokinetic package was used in the analysis of ...Two kinds of Ipriflavone tablets (IP) were orally cross administered to 8 healthy volunteers. The serum level of IP at different time was determined by HPLC, 3P87 pharmacokinetic package was used in the analysis of the time course of serum concentration and it had shown that the data well fitted a 2 compartment model. Pharmacokinetic parameters and area under curve (AUC) were calculated. The relative bioavailability of Tabellae IP made in China vs that made in Japan (as a reference) was 1.003( P >0.05). The values of AUC T max and C max of the two preparations were also comparable by the statistical analysis, so they were bioequivalent.展开更多
Two novel compounds,3,8-dibromo-2-methoxyl-7-isopropoxyisoflavanone (1) and 3,6-dibromo-2-methoxyl-7-isopropoxyisoflavanone (2),are synthesized via bromination reaction of their precursor ipriflavone in methanol.The m...Two novel compounds,3,8-dibromo-2-methoxyl-7-isopropoxyisoflavanone (1) and 3,6-dibromo-2-methoxyl-7-isopropoxyisoflavanone (2),are synthesized via bromination reaction of their precursor ipriflavone in methanol.The mixture of 1 and 2 co-crystallizes in ethanol and forms two different crystal shapes,the shape of 1 being block and 2 prism,they can be separated manually.1 and 2 are characterized by IR,1H NMR and single crystal X-ray diffraction.The mechanism of bromination reaction is also discussed.1 crystallizes in the monoclinic space group P 21/n with cell parameters a = 1.3569(3) nm,b = 0.6706(2) nm,c = 2.0704(4) nm,?= 97.50(2)°,V = 1.8678(6) nm3,Z = 4,Dc = 1.672 Mg/m3,R = 0.0455,wR = 0.0779,F(000) = 936.2 crystallizes in the monoclinic space group P 21/c with cell parameters a =1.3854(17) nm,b = 1.1215(14) nm,c = 1.3038(17) nm,? = 103.71(2)°,V = 1.968(4) nm3,Z = 4,Dc = 1.587 Mg/m3,R = 0.0306,wR = 0.0619,F(000) = 936.The Br…p interactions,hydrogen bonds,aromatic hy-drogen bonds and aromatic stacking interactions exist in the crystal structures of 1 and 2,which lead them into supramolecular compounds with a three-dimensional network structure,respec-tively.1 and 2 are the isoflavanone derivatives halogenated at C3 and this kind of isoflavanone halides has not been reported yet.展开更多
文摘Two kinds of Ipriflavone tablets (IP) were orally cross administered to 8 healthy volunteers. The serum level of IP at different time was determined by HPLC, 3P87 pharmacokinetic package was used in the analysis of the time course of serum concentration and it had shown that the data well fitted a 2 compartment model. Pharmacokinetic parameters and area under curve (AUC) were calculated. The relative bioavailability of Tabellae IP made in China vs that made in Japan (as a reference) was 1.003( P >0.05). The values of AUC T max and C max of the two preparations were also comparable by the statistical analysis, so they were bioequivalent.
文摘Two novel compounds,3,8-dibromo-2-methoxyl-7-isopropoxyisoflavanone (1) and 3,6-dibromo-2-methoxyl-7-isopropoxyisoflavanone (2),are synthesized via bromination reaction of their precursor ipriflavone in methanol.The mixture of 1 and 2 co-crystallizes in ethanol and forms two different crystal shapes,the shape of 1 being block and 2 prism,they can be separated manually.1 and 2 are characterized by IR,1H NMR and single crystal X-ray diffraction.The mechanism of bromination reaction is also discussed.1 crystallizes in the monoclinic space group P 21/n with cell parameters a = 1.3569(3) nm,b = 0.6706(2) nm,c = 2.0704(4) nm,?= 97.50(2)°,V = 1.8678(6) nm3,Z = 4,Dc = 1.672 Mg/m3,R = 0.0455,wR = 0.0779,F(000) = 936.2 crystallizes in the monoclinic space group P 21/c with cell parameters a =1.3854(17) nm,b = 1.1215(14) nm,c = 1.3038(17) nm,? = 103.71(2)°,V = 1.968(4) nm3,Z = 4,Dc = 1.587 Mg/m3,R = 0.0306,wR = 0.0619,F(000) = 936.The Br…p interactions,hydrogen bonds,aromatic hy-drogen bonds and aromatic stacking interactions exist in the crystal structures of 1 and 2,which lead them into supramolecular compounds with a three-dimensional network structure,respec-tively.1 and 2 are the isoflavanone derivatives halogenated at C3 and this kind of isoflavanone halides has not been reported yet.
