Preparation, characterization, and pharmacokinetic evaluation of puerarin submicron emulsion.
A novel formulation of puerarin was studied. Puerarin submicron emulsion was prepared by complex phase inversion-high-pressure homogenization technology. Characterization, distribution of drug in emulsion, short-term stability, and pharmacokinetics of emulsion were evaluated. The mean diameter and zeta potential of puerarin emulsion were 188.14 nm and -29.45 mv, respectively. The distribution range of puerarin emulsion was very narrow. The concentration of puerarin in the interfacial surface, oil droplet, water, and liposome-micelles were 7.821, 1.079, 0.637 and 0.423 mg/mL, respectively. Puerarin submicron emulsion was stable for a period of 3 months. The area under the whole blood concentration-time curve of rabbits after intravenous administration of puerarin emulsion was 1.718-fold higher than that of rabbits of intravenous administration of puerarin (P < 0.05). And compared with the puerarin group, the elimination rate of puerarin emulsion group was significantly decreased (P < 0.05), and the biological half-life and the mean retention time of puerarin emulsion were markedly increased (P < 0.05).
Yue
Peng-Fei
PF
302 Hospital of People Liberation Army, People Liberation Army Institute of Chinese Materia Medica, Beijing 100039, China. ypfpharm@gmail.com
Yuan
Hai-Long
HL
Yang
Ming
M
You
Rong-Hui
RH
Cong
Long-Bo
LB
Zhu
Jun
J
Wang
Qi
Q
Zhu
Wei-Feng
WF
Xiao
Xiao-He
XH
D000818:Animals; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004655:Emulsions; D006207:Half-Life; D007529:Isoflavones / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008657:Metabolic Clearance Rate; D010316:Particle Size; D011817:Rabbits; D017550:Spectroscopy, Fourier Transform Infrared; D014018:Tissue Distribution; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D004655:Emulsions; D007529:Isoflavones; D014665:Vasodilator Agents; C033607:puerarin