Development and optimization of intravenous puerarin emulsions formation by a novel complex-phase inversion-homogenization technology.
To decrease the hemolysis side effect of puerarin, a novel approach of Complex-Phase Inversion-Homogenization (CPIH) Technology was established to prepare intravenous puerarin emulsions. Preparation of puerarin submicron emulsion were optimized by central composite design, and the physicochemical properties were evaluated. Puerarin phospholipid complexs prepared by puerarin and phospholipids at a ratio of 1 : 1.2. In order to improve the product quality, a central composite design was applied to optimize the critical process variables, such as emulsification time, stirring velocity and homogenization press, and the results were modeled statistically. Puerarin phospholipid complexs prepared were identified by fourier transform infrared spectrophotometry. The datas showed that the parameters had great effect on the response values. The particle size, span of dispersity and entrapment efficiency of puerarin emulsions prepared using the optimal parameters settings were 218.23 nm, 0.6284 and 87.32%, respectively. These meant that over 87% of the drug was located at the surfactant interface and oil droplet, the concentration of puerarin in aqueous was rarely. And the puerarin emulsion prepared by CPIH technology were sufficient stable for 90 d. The CPIH technology can be used as a general formulation principle for drugs which are slightly soluble in water and poorly soluble in oils.
Yue
Peng-Fei
PF
302 Hospital of PLA&PLA Institute of Chinese Materia Medica, Beijing 100039, China.
Yuan
Hai-Long
HL
Li
Xian-Yi
XY
Yang
Ming
M
Zhu
Wei-Feng
WF
Xiao
Xiao-He
XH
D016503:Drug Delivery Systems / Q000379:methods*; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D007529:Isoflavones / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D046529:Microscopy, Electron, Transmission; D009821:Oils; D010316:Particle Size; D010743:Phospholipids / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D014867:Water / Q000737:chemistry
D045703:Emulsifying Agents; D007529:Isoflavones; D009821:Oils; D010743:Phospholipids; D012997:Solvents; D014665:Vasodilator Agents; D014867:Water; C033607:puerarin