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1. 发明申请

US20110201680A1 FORMULATION OF SILYMARIN WITH HIGH EFFICACY AND PROLONGED ACTION AND THE PREPARATION METHOD THEREOF 有权
标题翻译：具有高效和延长作用的硅藻土配方及其制备方法
公开(公告)号：US20110201680A1
公开(公告)日：2011-08-18
申请号：US13126071
申请日：2009-11-23
申请人： Ximing Xu , Jiangnan Yu , Shanshan Tong , Yuan Zhu , Xia Cao
发明人： Ximing Xu , Jiangnan Yu , Shanshan Tong , Yuan Zhu , Xia Cao
IPC分类号： A61K31/353 , A61P1/00 , A61P9/00 , A61P7/02 , B29B9/12 , B82Y5/00
CPC分类号： A61K31/357 , A61K9/146 , A61K9/5115 , A61K31/353 , A61K47/02 , A61K47/24 , A61K47/30 , A61K47/32 , Y10S977/773 , Y10S977/888 , Y10S977/906
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.
摘要翻译：包含水飞蓟素固体分散体，含水飞蓟马的二氧化硅纳米颗粒，缓释基质材料和释放增强剂的高效，长效的水飞蓟素制剂，其中这些组分的质量比是水飞蓟素固体分散体：载有水飞蓟马的二氧化硅纳米颗粒：缓释基质材料：释放增强剂= 1：0.5〜1.25：0.1〜0.3：0.1〜0.3; 所述载有水飞粒的二氧化硅纳米粒子的药物负载率为51.95％〜52.87％。所述水飞蓟素固体分散体含有聚维酮K30，大豆卵磷脂和丙烯酸树脂IV，水飞蓟素等水飞蓟素固体分散体中的其他医疗配件的质量比为水飞蓟素：聚维酮K30：大豆卵磷脂：丙烯酸树脂IV = 1：1〜3：0.3 〜0.8：0.2〜0.5。与现有制剂相比，本发明公开的水飞蓟素的高效长效制剂的半衰期为2.3倍，平均停留时间（MRT）为9.94倍; 当在Beagle犬体内测试时，这种水飞蓟素的新制剂呈现出更平滑的浓度 - 时间曲线并达到连续释放72小时。本发明公开了其制备方法。

2. 发明授权

US09023388B2 Formulation of silibinin with high efficacy and prolonged action and the preparation method thereof 有权
标题翻译：具有高效和长效作用的水飞蓟宾制剂及其制备方法
公开(公告)号：US09023388B2
公开(公告)日：2015-05-05
申请号：US13126251
申请日：2009-11-23
申请人： Ximing Xu , Jiangnan Yu , Xia Cao , Yuan Zhu
发明人： Ximing Xu , Jiangnan Yu , Xia Cao , Yuan Zhu
IPC分类号： A61K31/357 , B29C35/16 , B82Y5/00 , B82Y40/00 , A61K9/16 , A61K9/20 , A61K9/48
CPC分类号： A61K31/357 , A61K9/1617 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2068 , A61K9/2095 , A61K9/4866 , A61K9/4875 , Y10S977/773 , Y10S977/888 , Y10S977/906
摘要： A high-efficacy, long-acting formulation of silibinin, comprising silibinin solid dispersion, silibinin-loaded silica nanoparticles, slow-release matrix material and release enhancer, wherein the mass ratio of these components is silibinin solid dispersion:silibinin-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 silibinin-loaded silica nanoparticles is 51.29˜51.77%; the said silibinin solid dispersion contains povidone K30, soybean lecithin, acrylic resin IV, wherein the mass ratio between silibinin and other medical accessories is silibinin: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 silibinin disclosed in this invention is 14.8 times longer while the mean residence time (MRT) of which is 4.52 times longer; when tested in vivo in Beagle dogs, this new formulation of silibinin presents a smoother concentration-time curve and reaches the continuous release for 72 hours. This invention discloses its preparation method.
摘要翻译：含有水飞蓟宾固体分散体，含有载脂蛋白的二氧化硅纳米粒子，缓释基质材料和释放增强剂的高效长效制剂，其中这些组分的质量比为硅胶蛋白固体分散体：载有载脂蛋白的二氧化硅纳米粒子：缓释基质材料：释放增强剂= 1：0.5〜1.25：0.1〜0.3：0.1〜0.3; 所述含有载脂蛋白的二氧化硅纳米粒子的药物加载速率为51.29〜51.77％; 所述的水飞蓟宾固体分散体含有聚维酮K30，大豆卵磷脂，丙烯酸树脂IV，其中水飞蓟宾与其他医用附件之间的质量比为硅胶蛋白：聚维酮K30：大豆卵磷脂：丙烯酸树脂IV = 1：1〜3：0.3〜0.8：0.2 ~0.5。与现有制剂相比，本发明公开的高效，长效制剂的水飞蓟宾的半衰期为14.8倍，平均停留时间（MRT）为4.52倍; 当在Beagle犬体内进行体内测试时，这种新的配制的水飞蓟宾提供更平滑的浓度 - 时间曲线并达到连续释放72小时。本发明公开了其制备方法。

3. 发明申请

US20110250269A1 HIGHLY EFFICIENT AND LONG-ACTING SLOW-RELEASE FORMULATION OF POORLY SOLUBLE DRUGS AND PREPARATION METHOD THEREOF 有权
标题翻译：高效和长效缓释配方不溶性药物及其制备方法
公开(公告)号：US20110250269A1
公开(公告)日：2011-10-13
申请号：US13126183
申请日：2009-11-23
申请人： Ximing Xu , Jiangnan Yu , Yuan Zhu , Xia Cao
发明人： Ximing Xu , Jiangnan Yu , Yuan Zhu , Xia Cao
IPC分类号： A61K9/52 , A61K9/26 , B29B9/12 , A61K31/7048 , A61K31/4422 , A61K9/00 , A61K36/28
CPC分类号： A61K9/2054 , A61K9/143 , A61K9/146 , A61K9/2077 , A61K31/357 , A61K31/4422 , A61K31/7048
摘要： A high-efficacy, long-acting, slow-release formulation of the poorly soluble drug, comprising solid dispersion of the poorly soluble drug, silica nanoparticles loaded with the poorly soluble drug, matrix material, and release enhancer, wherein the mass ratio of these components is solid dispersion of the poorly soluble drug: silica nanoparticles loaded with the poorly soluble drug: matrix material: release enhancer=1: 0.5˜1.25: 0.1˜0.3: 0.1˜0.3; the said solid dispersion of the poorly soluble drug contains povidone K30, soybean lecithin, and acrylic resin IV, wherein the mass ratio of the drug and the accessory materials is poorly soluble drug: povidone K30: soybean lecithin: acrylic resin IV=1: 1-3: 0.3˜0.8: 0.2˜0.5. Compared with the existing formulations, the in vivo half life of the high-efficacy, long-acting formulation of the poorly soluble drug disclosed in this invention is 2.3˜14.8 times longer while the mean residence time (MRT) of which is 7.94˜4.52 times longer; when tested in vivo in Beagle dogs, this new formulation of the poorly soluble drug presents a smoother concentration-time curve and reaches a continuous release for 72 hours. This invention discloses its preparation method.
摘要翻译：难溶性药物的高效，长效，缓释制剂，包括难溶性药物的固体分散体，负载有难溶性药物的二氧化硅纳米粒子，基质材料和释放增强剂，其中这些组分是难溶性药物的固体分散体：载有难溶性药物的二氧化硅纳米粒子：基体材料：释放增强剂= 1:0.5〜1.25:0.1〜0.3:0.1〜0.3; 所述难溶性药物的固体分散体含有聚维酮K30，大豆卵磷脂和丙烯酸树脂IV，其中药物和辅助材料的质量比是难溶性药物：聚维酮K30：大豆卵磷脂：丙烯酸树脂IV = 1：1 -3：0.3〜0.8：0.2〜0.5。与现有制剂相比，本发明公开的难溶性药物的高效长效制剂的体内半衰期为2.3〜14.8倍，平均停留时间（MRT）为7.94〜4.52 时间更长当在Beagle犬体内进行体内测试时，这种新的低溶解性药物的制剂呈现出更平滑的浓度 - 时间曲线，达到连续释放72小时。本发明公开了其制备方法。

4. 发明授权

US09283190B2 Highly efficient and long-acting slow-release formulation of poorly soluble drugs and preparation method thereof 有权
标题翻译：难溶性药物的高效长效缓释制剂及其制备方法
公开(公告)号：US09283190B2
公开(公告)日：2016-03-15
申请号：US13126183
申请日：2009-11-23
申请人： Ximing Xu , Jiangnan Yu , Yuan Zhu , Xia Cao
发明人： Ximing Xu , Jiangnan Yu , Yuan Zhu , Xia Cao
IPC分类号： A61K9/20 , A61K31/357 , A61K31/4422 , A61K31/7048 , A61K9/14
CPC分类号： A61K9/2054 , A61K9/143 , A61K9/146 , A61K9/2077 , A61K31/357 , A61K31/4422 , A61K31/7048
摘要： A high-efficacy, long-acting, slow-release formulation of the poorly soluble drug, comprising solid dispersion of the poorly soluble drug, silica nanoparticles loaded with the poorly soluble drug, matrix material, and release enhancer, wherein the mass ratio of these components is solid dispersion of the poorly soluble drug: silica nanoparticles loaded with the poorly soluble drug: matrix material: release enhancer=1: 0.5˜1.25: 0.1˜0.3: 0.1˜0.3; the said solid dispersion of the poorly soluble drug contains povidone K30, soybean lecithin, and acrylic resin IV, wherein the mass ratio of the drug and the accessory materials is poorly soluble drug: povidone K30: soybean lecithin: acrylic resin IV=1: 1˜3: 0.3˜0.8: 0.2˜0.5. Compared with the existing formulations, the in vivo half life of the high-efficacy, long-acting formulation of the poorly soluble drug disclosed in this invention is 2.3˜14.8 times longer while the mean residence time (MRT) of which is 7.94˜4.52 times longer; when tested in vivo in Beagle dogs, this new formulation of the poorly soluble drug presents a smoother concentration-time curve and reaches a continuous release for 72 hours. This invention discloses its preparation method.
摘要翻译：难溶性药物的高效，长效，缓释制剂，包括难溶性药物的固体分散体，负载有难溶性药物的二氧化硅纳米粒子，基质材料和释放增强剂，其中这些组分是难溶性药物的固体分散体：载有难溶性药物的二氧化硅纳米粒子：基体材料：释放增强剂= 1:0.5〜1.25:0.1〜0.3:0.1〜0.3; 所述难溶性药物的固体分散体含有聚维酮K30，大豆卵磷脂和丙烯酸树脂IV，其中药物和辅助材料的质量比是难溶性药物：聚维酮K30：大豆卵磷脂：丙烯酸树脂IV = 1：1 〜3：0.3〜0.8：0.2〜0.5。与现有制剂相比，本发明公开的难溶性药物的高效长效制剂的体内半衰期为2.3〜14.8倍，平均停留时间（MRT）为7.94〜4.52 时间更长当在Beagle犬体内进行体内测试时，这种新的低溶解性药物的制剂呈现出更平滑的浓度 - 时间曲线，达到连续释放72小时。本发明公开了其制备方法。

5. 发明授权

US08962017B2 Formulation of silymarin with high efficacy and prolonged action and the preparation method thereof 有权
标题翻译：具有高效和长效作用的水飞蓟素的制备及其制备方法
公开(公告)号：US08962017B2
公开(公告)日：2015-02-24
申请号：US13126071
申请日：2009-11-23
申请人： Ximing Xu , Jiangnan Yu , Shanshan Tong , Yuan Zhu , Xia Cao
发明人： Ximing Xu , Jiangnan Yu , Shanshan Tong , Yuan Zhu , Xia Cao
IPC分类号： A61K31/353 , A61P1/00 , A61P9/00 , A61P7/02 , B29B9/12 , B82Y5/00 , A61K31/357 , A61K9/14 , A61K9/51 , A61K47/02 , A61K47/24 , A61K47/30 , A61K47/32
CPC分类号： A61K31/357 , A61K9/146 , A61K9/5115 , A61K31/353 , A61K47/02 , A61K47/24 , A61K47/30 , A61K47/32 , Y10S977/773 , Y10S977/888 , Y10S977/906
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.
摘要翻译：包含水飞蓟素固体分散体，含水飞蓟马的二氧化硅纳米颗粒，缓释基质材料和释放增强剂的高效，长效的水飞蓟素制剂，其中这些组分的质量比是水飞蓟素固体分散体：载有水飞蓟马的二氧化硅纳米颗粒：缓释基质材料：释放增强剂= 1：0.5〜1.25：0.1〜0.3：0.1〜0.3; 所述载有水飞粒的二氧化硅纳米粒子的药物负载率为51.95％〜52.87％。所述水飞蓟素固体分散体含有聚维酮K30，大豆卵磷脂和丙烯酸树脂IV，水飞蓟素等水飞蓟素固体分散体中的其他医疗配件的质量比为水飞蓟素：聚维酮K30：大豆卵磷脂：丙烯酸树脂IV = 1：1〜3：0.3 〜0.8：0.2〜0.5。与现有制剂相比，本发明公开的水飞蓟素的高效长效制剂的半衰期为2.3倍，平均停留时间（MRT）为9.94倍; 当在Beagle犬体内测试时，这种水飞蓟素的新制剂呈现出更平滑的浓度 - 时间曲线并达到连续释放72小时。本发明公开了其制备方法。

6. 发明申请

US20120029064A1 FORMULATION OF SILIBININ WITH HIGH EFFICACY AND PROLONGED ACTION AND THE PREPARATION METHOD THEREOF 有权
标题翻译：具有高效和延长作用的硅胶的制备及其制备方法
公开(公告)号：US20120029064A1
公开(公告)日：2012-02-02
申请号：US13126251
申请日：2009-11-23
申请人： Ximing Xu , Jiangnan Yu , Xia Cao , Yuan Zhu
发明人： Ximing Xu , Jiangnan Yu , Xia Cao , Yuan Zhu
IPC分类号： A61K31/357 , B29C35/16 , B82Y5/00 , B82Y40/00
CPC分类号： A61K31/357 , A61K9/1617 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2068 , A61K9/2095 , A61K9/4866 , A61K9/4875 , Y10S977/773 , Y10S977/888 , Y10S977/906
摘要： A high-efficacy, long-acting formulation of silibinin, comprising silibinin solid dispersion, silibinin-loaded silica nanoparticles, slow-release matrix material and release enhancer, wherein the mass ratio of these components is silibinin solid dispersion:silibinin-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 silibinin-loaded silica nanoparticles is 51.29˜51.77%; the said silibinin solid dispersion contains povidone K30, soybean lecithin, acrylic resin IV, wherein the mass ratio between silibinin and other medical accessories is silibinin: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 silibinin disclosed in this invention is 14.8 times longer while the mean residence time (MRT) of which is 4.52 times longer; when tested in vivo in Beagle dogs, this new formulation of silibinin presents a smoother concentration-time curve and reaches the continuous release for 72 hours. This invention discloses its preparation method.
摘要翻译：含有水飞蓟宾固体分散体，含有载脂蛋白的二氧化硅纳米粒子，缓释基质材料和释放增强剂的高效长效制剂，其中这些组分的质量比为硅胶蛋白固体分散体：载有载脂蛋白的二氧化硅纳米粒子：缓释基质材料：释放增强剂= 1：0.5〜1.25：0.1〜0.3：0.1〜0.3; 所述含有载脂蛋白的二氧化硅纳米粒子的药物加载速率为51.29〜51.77％; 所述的水飞蓟宾固体分散体含有聚维酮K30，大豆卵磷脂，丙烯酸树脂IV，其中水飞蓟宾与其他医用附件之间的质量比为硅胶蛋白：聚维酮K30：大豆卵磷脂：丙烯酸树脂IV = 1：1〜3：0.3〜0.8：0.2 ~0.5。与现有制剂相比，本发明公开的高效，长效制剂的水飞蓟宾的半衰期为14.8倍，平均停留时间（MRT）为4.52倍; 当在Beagle犬体内进行体内测试时，这种新的配制的水飞蓟宾提供更平滑的浓度 - 时间曲线并达到连续释放72小时。本发明公开了其制备方法。

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