Ximing Xu,Jiangnan Yu,Shanshan Tong,Yuan Zhu,Xia Cao
申请号：
US13126071
公开号：
US08962017B2
申请日:
2009.11.23
申请国别(地区):
US
年份:
2015
代理人:
摘要：
A high-efficacy, long-acting formulation of silymarin, comprising silymarin solid dispersion, silymarin-loaded silica nanoparticles, slow-release matrix material and release enhancer, wherein the mass ratio of these components is silymarin solid dispersion:silymarin-loaded silica nanoparticles:slow-release matrix material:release enhancer=1:0.5˜1.25:0.1˜0.3:0.1˜0.3； the drug loading rate of the said silymarin-loaded silica nanoparticles is 51.95%-52.87%； the said silymarin solid dispersion contains povidone K30, soybean lecithin and acrylic resin IV, and the mass ratio between silymarin and other medical accessories in silymarin solid dispersion is silymarin:povidone K30:soybean lecithin:acrylic resin IV=1:1˜3:0.3˜0.8:0.2˜0.5. Compared with the existing formulations, the half life of the high-efficacy, long-acting formulation of silymarin disclosed in this invention is 2.3 times longer while the mean residence time (MRT) of which is 9.94 times longer； when tested in vivo in Beagle dogs, this new formulation of silymarin presents a smoother concentration-time curve and reaches a continuous release for 72 hours. This invention discloses its preparation method.
