Process optimization, characterization and pharmacokinetic evaluation in rats of ursodeoxycholic Aci
May 1st, 2008 | by admin |Process optimization, characterization and pharmacokinetic evaluation in rats of ursodeoxycholic Acid-phospholipid complex.
The purpose of this research was to study whether the bioavailability of ursodeoxycholic acid could be improved by administering ursodeoxycholic acid-phospholipid complex (UDCA-PLC) orally to rats. A central composite design approach was used for process optimization in order to obtain the acceptable UDCA-PLC. The physicochemical properties of the complex obtained by optimal parameters were investigated by means of scanning electron microscopy and X-ray diffraction. The pharmacokinetic parameters and bioavailability studies were conducted in rats of UDCA after oral administration of UDCA-PLC and UDCA tablet. Multiple linear regression analysis for process optimization revealed that the acceptable UDCA-PLC was obtained wherein the optimal values of X (1), X (2) and X (3) were 3, 60 degrees C and 3 h, respectively. The XRD studies of UDCA-PLC obtained by the optimal parameters demonstrated that UDCA and phospholipids in the UDCA-PLC were combined by non-covalent bonds, not form new compounds. But pharmacokinetic parameters of the complex in rats were T (max) 1.6 h, C (max) 0.1346 mug/ml, [Formula: see text]11.437 mug.h/ml, respectively. The relative bioavailability of UDCA of UDCA-PLC was increased by 241%,compared with the reference ursodeoxycholic acid tablet.
Yue PF, Zhang WJ, Yuan HL, Yang M, Zhu WF, Cai PL, Xiao XH.
302 Hospital of PLA&PLA Institute of Chinese Materia Medica, Beijing, 100039, China.