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1. 发明专利

JP2013231051A Method for producing taste-masked immediate release fexofenadine microcapsule 有权
标题翻译：生产立体释放快速释放微生物的方法
公开(公告)号：JP2013231051A
公开(公告)日：2013-11-14
申请号：JP2013138080
申请日：2013-07-01
申请人： Aptalis Pharma Ltd , アプタリスファーマリミテッド
发明人： MAPELLI LUIGI , FABIANI FLAVIO , BOLTRI LUIGI , GATTI PAOLO , SERRATONI MAURO , CASSANMAGNAGO ROBERTO
IPC分类号： A61K31/445 , A61K9/10 , A61K9/16 , A61K9/26 , A61K9/32 , A61K9/50 , A61K47/10 , A61K47/14 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/32 , A61K47/36 , A61K47/38 , A61P11/02 , A61P17/04 , A61P37/08 , A61P43/00
CPC分类号： A61K31/445 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5089
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a plurality of microencapsulated fexofenadine particles, by a simple process, having taste-masked immediate release properties.SOLUTION: A method for producing microcapsules includes: (a) a dissolution step of dissolving a water-insoluble polymer in an organic solvent; (b) a suspension step of suspending fexofenadine in the organic solvent as an active component; (c) a covering step of applying a coating of the water-insoluble polymer onto the fexofenadine by phase separation to thereby obtain a plurality of microcapsules, in each of which the fexofenadine is coated with the water-insoluble polymer; (d) a separation step of separating the obtained plurality of microcapsules from the organic solvent; and (e) a wetting step of wetting the separated plurality of microcapsules using a surfactant so that these plurality of microcapsules thereby have suspendability in water, thereby obtaining the plurality of particles.
摘要翻译：要解决的问题：提供一种通过简单的方法生产多个微胶囊化非索非那定颗粒的方法，其具有掩味的立即释放特性。解决方案：一种生产微胶囊的方法包括：（a）溶解水不溶性聚合物在有机溶剂中; （b）将非索非那定悬浮在有机溶剂中作为活性成分的悬浮步骤; （c）通过相分离将非水解聚合物的涂层施加到非索非那定的覆盖步骤，从而获得多个微胶囊，其中每个微胶囊中的非索非那那均涂覆有不溶于水的聚合物; （d）从所述有机溶剂中分离得到的多个微胶囊的分离步骤; 和（e）使用表面活性剂润湿分离的多个微胶囊的润湿步骤，使得这些微胶囊因此在水中具有悬浮性，从而获得多个颗粒。

2. 发明专利

JP2014139231A Method for producing taste-masked immediate release fexofenadine microcapsule 有权
标题翻译：生产立体释放快速释放微生物的方法
公开(公告)号：JP2014139231A
公开(公告)日：2014-07-31
申请号：JP2014076950
申请日：2014-04-03
申请人： Aptaris Pharma Ltd , アプタリスファーマリミテッド
发明人： MAPELLI LUIGI , FABIANI FLAVIO , BOLTRI LUIGI , GATTI PAOLO , SERRATONI MAURO , CASSANMAGNAGO ROBERTO
IPC分类号： A61K31/445 , A61K9/10 , A61K9/16 , A61K9/26 , A61K9/32 , A61K9/50 , A61K47/10 , A61K47/14 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/32 , A61K47/36 , A61K47/38 , A61P11/02 , A61P17/04 , A61P37/08 , A61P43/00
CPC分类号： A61K31/445 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5089
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a plurality of microencapsulated fexofenadine particles, by a simple process, having taste-masked immediate release properties.SOLUTION: A method for producing microcapsules comprises: (a) a dissolution step of dissolving a water-insoluble polymer in an organic solvent; (b) a suspension step of suspending fexofenadine in the organic solvent as an active component; (c) a covering step of applying a coating of the water-insoluble polymer onto the fexofenadine by phase separation to thereby obtain a plurality of microcapsules, in each of which the fexofenadine is coated with the water-insoluble polymer; (d) a separation step of separating the obtained plurality of microcapsules from the organic solvent; and (e) a wetting step of wetting the separated plurality of microcapsules using a surfactant so that these plurality of microcapsules thereby have suspendability in water, thereby obtaining the plurality of particles.
摘要翻译：要解决的问题：提供一种通过简单的方法制备多种微胶囊化非索非那定颗粒的方法，其具有掩味的立即释放性质。解决方案：一种生产微胶囊的方法包括：（a）溶解水不溶性聚合物在有机溶剂中; （b）将非索非那定悬浮在有机溶剂中作为活性成分的悬浮步骤; （c）通过相分离将非水解聚合物的涂层施加到非索非那定的覆盖步骤，从而获得多个微胶囊，其中每个微胶囊中的非索非那那均涂覆有不溶于水的聚合物; （d）从所述有机溶剂中分离得到的多个微胶囊的分离步骤; 和（e）使用表面活性剂润湿分离的多个微胶囊的润湿步骤，使得这些微胶囊因此在水中具有悬浮性，从而获得多个颗粒。

3. 发明专利

NZ600256A Fexofenadine microcapsules and compositions containing them 未知
公开(公告)号：NZ600256A
公开(公告)日：2014-05-30
申请号：NZ60025610
申请日：2010-12-01
申请人： APTALIS PHARMA LTD
发明人： MAPELLI LUIGI , FABIANI FLAVIO , BOLTRI LUIGI , GATTI PAOLO , SERRATONI MAURO , CASSANMAGNAGO ROBERTO
IPC分类号： A61K9/50 , A61K31/445
摘要： Disclosed herein is a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating such as ethylcellulose, polyvinyl acetate, cellulose acetate, cellulose acetate butyrate, polyvinyl acetate, ammonio-methacrylate copolymers and mixtures thereof. In one embodiment the microcapsules are co-granulated with an inactive ingredient such as surcrose or xylitol. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

4. 发明专利

CO6541583A2 MICROCAPSULAS DE FEXOFENADINA Y COMPOSICIONES QUE LAS CONTIENEN 未知
公开(公告)号：CO6541583A2
公开(公告)日：2012-10-16
申请号：CO12095687
申请日：2012-06-06
申请人： APTALIS PHARMA LTD
发明人： MAPELLI LUIGI , FABIANI FLAVIO , BOLTRI LUIGI , GATTI PAOLO , SERRATONI MAURO , CASSANMAGNAGO MACHERIO
IPC分类号： A61K9/50 , A61K31/445
摘要： La presente invención proporciona una composición farmacéutica que comprende microcápsulas de liberación inmediata con sabor enmascarado, que comprende fexofenadina y un revestimiento polímero insoluble en agua. Estas microcápsulas y las composiciones farmacéuticas que las comprenden tienen un contenido adecuado en fármacos y propiedades farmacéuticas deseables, que incluyen una rápida tasa de disolución de fexofenalina combinada con un efecto enmascarador del sabor.

5. 发明专利

MX2012006240A MICROCAPSULAS DE FEXOFENADINA Y COMPOSICIONES QUE CONTIENEN LAS MISMAS. 未知
公开(公告)号：MX2012006240A
公开(公告)日：2012-10-03
申请号：MX2012006240
申请日：2010-12-01
申请人： APTALIS PHARMA LTD
发明人： MAPELLI LUIGI , FABIANI FLAVIO , BOLTRI LUIGI , GATTI PAOLO , SERRATONI MAURO , CASSANMAGNAGO ROBERTO
IPC分类号： A61K9/50 , A61K31/445
摘要： La presente invención proporciona una composición farmacéutica que comprende microcápsulas de liberación inmediata con sabor enmascarado, que comprende fexofenadina y un revestimiento polímero insoluble en agua. Estas microcápsulas y las composiciones farmacéuticas que las comprenden tienen un contenido adecuado en fármacos y propiedades farmacéuticas deseables, que incluyen una rápida tasa de disolución de fexofenalina combinada con un efecto enmascarador del sabor.

6. 发明专利

CA2820437A1 PHARMACEUTICAL COMPOSITES OF POORLY WATER SOLUBLE DRUGS AND POLYMERS 未知
公开(公告)号：CA2820437A1
公开(公告)日：2012-06-28
申请号：CA2820437
申请日：2011-12-22
申请人： APTALIS PHARMA LTD
发明人： GATTI PAOLO , COLOMBO ITALO , GERVASONI DARIO , PIRONTI VINCENZA , ALBORGHETTI LIA , FABIANI FLAVIO , BOLTRI LUIGI
IPC分类号： A61K9/14 , A61K31/18 , A61K31/216 , A61K31/44
摘要： The invention provides a composite of drug, polymeric carrier and at least one not cross linked polymer useful to improve the solubility of poorly water soluble drugs. The present invention comprises manufacturing process of this composite material. The manufacturing process is carried out by the solvent induced activation process, wherein the not cross-linked polymer is loaded into the composite from organic solution, possibly together with the drug. Pharmaceutical compositions comprising said composite in combination with pharmaceutical acceptable excipients are also described herein.

7. 发明专利

NZ713487A Pharmaceutical composites of poorly water soluble drugs and polymers 未知
公开(公告)号：NZ713487A
公开(公告)日：2017-04-28
申请号：NZ71348711
申请日：2011-12-22
申请人： APTALIS PHARMA LTD
发明人： GATTI PAOLO , COLOMBO ITALO , GERVASONI DARIO , PIRONTI VINCENZA , ALBORGHETTI LIA , FABIANI FLAVIO , BOLTRI LUIGI
IPC分类号： A61K9/14 , A61K31/18 , A61K31/216 , A61K31/44
摘要： Disclosed herein is a process for the preparation of a composite comprising at least one poorly soluble drug of Class II according to Biopharmaceutics Classification System (BCS) having low solubility and high gastrointestinal permeability, at least one polymeric carrier selected from the group consisting of cross-linked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose, cross-linked cyclodextrins, cross-linked dextran, cross-linked starch, cross-linked methylcellulose and at least one not chemically cross-linked polymer, which is both soluble in water and organic solvent selected from the group consisting of hydroxypropylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethycellulose acetate succinate, cellulose acetate trimellitate, acrylic and methacrylic polymers and their copolymers, methacrylic acid-methylmethacrylate copolymer, polyaminoalkyl methacrylate-methacrylic esters copolymer, dimethylaminoethyl methacrylate-butylmethacrylate-methylmethacrylate copolymer, vinylpyrrolidone-vinyl acetate copolymer, methylvinylether-maleic acid copolymer, polyethyleneglycol- caprolactame- vinylpyrrolidone copolymer, comprising the following steps: (1) Dissolving at least one poorly water soluble drug in a process solvent or process solvent mixture, wherein the solvent may is selected from methanol, ethanol, higher alcohols, acetone, chlorinated solvents, formamide, dimethylformamide, fluorinated hydrocarbons or mixture thereof; (2) Dissolving at least one not cross-linked polymer, which is both water and organic solvent soluble, into the drug solution of step (1); (3) Swelling at least one polymeric carrier with the solution prepared in step (2), thus obtaining a swollen composite; (4) Removing the process solvent from the swollen composite of step (3), wherein step (4) is carried out for a period of time which is equal or shorter than about 410 minutes and at a temperature from 35 to 60°C and wherein the process solvent is able to swell the polymeric carrier or to be absorbed by the polymeric carrier and to dissolve the poorly soluble drug and the water and organic solvent soluble not chemically cross-linked polymer.

8. 发明专利

ZA201304731B PHARMACEUTICAL COMPOSITES OF POORLY WATER SOLUBLE DRUGS AND POLYMERS 未知
公开(公告)号：ZA201304731B
公开(公告)日：2015-10-28
申请号：ZA201304731
申请日：2013-06-25
申请人： APTALIS PHARMA LTD
发明人： BOLTRI LUIGI , FABIANI FLAVIO , ALBORGHETTI LIA , PIRONTI VINCENZA , GERVASONI DARIO , COLOMBO ITALO , GATTI PAOLO
摘要： The invention provides a composite of drug, polymeric carrier and at least one not cross linked polymer useful to improve the solubility of poorly water soluble drugs. The present invention comprises manufacturing process of this composite material. The manufacturing process is carried out by the solvent induced activation process, wherein the not cross-linked polymer is loaded into the composite from organic solution, possibly together with the drug. Pharmaceutical compositions comprising said composite in combination with pharmaceutical acceptable excipients are also described herein.

9. 发明专利

ZA201203983B FEXOFENADINE MICROCAPSULES AND COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：ZA201203983B
公开(公告)日：2013-08-28
申请号：ZA201203983
申请日：2012-05-31
申请人： APTALIS PHARMA LTD
发明人： CASSANMAGNAGO ROBERTO , SERRATONI MAURO , FABIANI FLAVIO , MAPELLI LUIGI , BOLTRI LUIGI , GATTI PAOLO
摘要： The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

10. 发明专利

AU2011347179A1 Pharmaceutical composites of poorly water soluble drugs and polymers 未知
公开(公告)号：AU2011347179A1
公开(公告)日：2013-06-27
申请号：AU2011347179
申请日：2011-12-22
申请人： APTALIS PHARMA LTD
发明人： GATTI PAOLO , COLOMBO ITALO , GERVASONI DARIO , PIRONTI VINCENZA , ALBORGHETTI LIA , FABIANI FLAVIO , BOLTRI LUIGI
IPC分类号： A61K9/14 , A61K31/18 , A61K31/216 , A61K31/44
摘要： The invention provides a composite of drug, polymeric carrier and at least one not cross linked polymer useful to improve the solubility of poorly water soluble drugs. The present invention comprises manufacturing process of this composite material. The manufacturing process is carried out by the solvent induced activation process, wherein the not cross-linked polymer is loaded into the composite from organic solution, possibly together with the drug. Pharmaceutical compositions comprising said composite in combination with pharmaceutical acceptable excipients are also described herein.

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