Int J Pharm. 2009 Jun 6; Han SF, Yao TT, Zhang XX, Gan L, Zhu C, Yu HZ, Gan YThis study has explored the use of lipid-based formulations to enhance the oral bioavailability of the poorly water-soluble drug anethol trithione (ATT), and compared the performance of different formulations. Two groups of lipid-based formulations, sub-microemulsion (SME) and oil solution, were prepared using short (SCT), medium (MCT) and long (LCT) chain triglycerides respectively; aqueous suspension was used as the reference formulation. In vitro and in vivo studies were conducted to investigate the impact of lipid composition and formulation on drug absorption. In vitro digestion was used to analyze lipid digestion rates and drug distribution/solubilization. After in vitro digestion, the performance rank order for drug solubilization was SCT < MCT < LCT. SME formulations were digested more rapidly in vitro than oil solutions. The bioavailability of the drug from different formulations was investigated in rats. All six lipid-based formulations enhanced drug absorption compared to the aqueous suspension. For the SMEs, which were rapidly digested, in vivo bioavailability increased in accordance with the increase of solubilization data obtained by in vitro digestion, with the rank order SCT-SME < MCT-SME < LCT-SME. For the oil solutions, which were digested more slowly, there was no significant difference in drug bioavailability for the different formulations. In conclusion, lipid-based formulations can enhance the oral bioavailability of ATT, and for this BCS class II drug, both the lipid composition and type of lipid formulation are likely to govern in vivo performance.
J Asian Nat Prod Res. 2009; 11(5): 397-400Lu X, Xu N, Dai HF, Mei WL, Yang ZX, Pei YHThree new compounds, 4-hydroxyphenethyl-2'-hydroxypropanoate (1), 6-(1',2'-dimethyloxiran-1'-yl)-4-methoxy-3-methyl-2H-pyran-2-one (2), 6-(1-hydroxyethyl)-4-methoxy-3-methyl-2H-pyran-2-one (3), along with the two known compounds, nectriapyrone (4) and wermopyrone (5), have been isolated from the endophytic fungus of Cephalotaxus hainanensis. Their structures were determined on the basis of chemical and spectroscopic methods.
J Asian Nat Prod Res. 2009; 11(5): 426-32Li ZL, Li DY, Hua HM, Chen XH, Kim CSThree new flavone C-glycosides with the substitution of the unusual acyl, 2''-O-veratroylisoswertisin (1), 3''-O-2-methylbutyrylisoswertiajaponin (2), and 3''-O-2-methylbutyrylvitexin (3), together with the known compounds of 2''-O-2-methylbutyrylisoswertisin (4), 3''-O-2-methylbutyrylisoswertisin (5), and trollisin I (6) were isolated from the antibacterial fraction of the aqueous extract of the flowers of Trollius chinensis. The structural elucidations of these compounds were carried out by a detailed analysis of the NMR and MS spectra.
J Asian Nat Prod Res. 2009; 11(5): 433-8Gao HM, Liu JX, Wang ZM, Wang WHPhytolacacinoside A (1), a novel triterpenoid saponin, together with the seven known compounds, was isolated from 75% ethanol extract of the root of Phytolacca acinosa Roxb (Phytolaccaceae). Their structures were elucidated on the basis of analysis of spectroscopic data and physicochemical properties as 3-O-beta-[(beta-d-glucopyranosyl-(1 --> 4)-O-beta-D-xylopyranosyl)]-11beta-methoxy-jaligonic acid 30-methyl ester 28-O-beta-D-glucopyranoside (1), 3-O-beta-[(beta-D-glucopyranosyl-(1 --> 4)-O-beta-D-xylopyranosyl)]-jaligonic acid 30-methyl ester 28-O-beta-D-glucopyranoside (2, esculentoside G), 3-O-beta-[(beta-D-glucopyranosyl-(1 --> 4)-O-beta-D-xylopyranosyl)]-jaligonic acid 30-methyl ester (3, phytolaccoside E), 3-O-beta-D-xylopyranosyl-jaligonic acid 30-methyl ester (4, phytolaccoside B), hypaphorine (5), palmitic acid monoglyceride (6), beta-sitosterol (7), and daucosterol (8).