Pharmacokinetics study of ferulic acid in rats after oral administration of γ-oryzanol under combined use of Tween 80 by LC/MS/MS.
OBJECTIVE
γ-oryzanol (OZ) is a rich source of commercially-important bioactive phytochemicals, most of them of interest in nutrition, pharmacy and cosmetics. However, the poor solubility of OZ limited the use. In the paper, ultraviolet-visible (UV-Vis) analysis was conducted to analysis the solubilization of OZ under combined use of Tween 80 in vitro. In addition, to further confirm the solubilizing effect of Tween 80, a pharmacokinetic study of ferulic acid (FA) in rats after oral administration of OZ 100 mg/kg under combined use of Tween 80 though LCMS/MS was carried out.


RESULTS
Solubility enhancement as high as 100-fold is achieved using 1% Tween 80 in vitro. Following oral administration of OZ-Tween 80 100 mg/kg, the values of Tmax, Cmax, AUC0-∞, T1/2Ka and MRT0-∞ were 46.667 ± 39.328, 129.498 ± 27.025, 63738.28 ± 599, 14.274 ± 7.309 and 859.592 ± 108.780 respectively. The values of T1/2Ka, AUC0-∞, MRT0-t, and Tmax showed up to increase 16%, 58%, 44% and 47% while Cmax and CL/F decreased 22% and 12%, respectively. The decreased Cmax value indicated that Tween 80 can hardly enhance the absorption of FA in rats. However, T1/2Ka and Tmax values showed that the absorption of FA was extended, which resulted the increased values of AUC0-∞ and MRT0-∞.


CONCLUSIONS
Our results reveal that Tween 80 improves solubility of OZ in vitro and could enhance the bioavailability of OZ by extending its absorption and elimination.
Department of Pharmacy, and Department of Hepatobiliary Surgery; Zhujiang Hospital, Southern Medical University, Guangzhou, PR China. zhang43499@sohu.com  
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Zhang
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002853:Chromatography, Liquid / Q000379:methods; D003373:Coumaric Acids / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D005260:Female; D008297:Male; D010666:Phenylpropionates / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D011136:Polysorbates / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D053719:Tandem Mass Spectrometry
D003373:Coumaric Acids; D010666:Phenylpropionates; D011136:Polysorbates; C004999:ferulic acid; C013172:gamma-oryzanol