Formulation of silymarin with high efficacy and prolonged action and the preparation method thereof

US8962017B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-8962017-B2
Application numberUS-200913126071-A
CountryUS
Kind codeB2
Filing dateNov 23, 2009
Priority dateDec 31, 2008
Publication dateFeb 24, 2015
Grant dateFeb 24, 2015

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Abstract

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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.

First claim

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What is claimed is: 1. A formulation of silymarin, comprising: a silymarin solid dispersion, silymarin-loaded silica nanoparticles, a slow-release matrix material and a release enhancer, wherein a mass ratio of the silymarin solid dispersion:the silymarin-loaded silica nanoparticles:the slow-release matrix material:the release enhancer is 1:0.5-1.25:0.1-0.3:0.1-0.3; wherein the silica nanoparticles are a mesoporous material including a plurality of pores having a diameter of 1.5…

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What does patent US8962017B2 cover?
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…
Who is the assignee on this patent?
Xu Ximing, Yu Jiangnan, Tong Shanshan, and 3 more
What technology area does this patent fall under?
Primary CPC classification A61K31/357. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Feb 24 2015 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).