公开(公告)号：US06194005B1

公开(公告)日：2001-02-27

申请号：US09269468

申请日：1999-03-23

申请人： Nabil Farah ,  Philippe Barthelemy ,  Joseph Joachim

发明人： Nabil Farah ,  Philippe Barthelemy ,  Joseph Joachim

IPC分类号： A61K922

CPC分类号： A61K9/2013 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/2009 ,  A61K9/2077 ,  A61K9/5015

摘要： The invention concerns a method for preparing a modified release of active principle. The method comprises the steps of mixing a powder composed of active principle, adjuvant or combinations thereof while heating and fluidizing in order to obtain individual grains, liquefying a lipid matrix agent composed of partial esters of alcohol with at least one fatty acid, coating the powder by spraying from 1 to 15% by weight of the final composition liquid lipid matrix agent over the individual grains, the spraying air pressure, and optionally the spraying rate varying throughout the coating operation and lowering the temperature of the combined product to allow the lipid matrix agent to solidify around the grains.

摘要翻译： 本发明涉及制备活性成分的改性释放的方法。 该方法包括以下步骤：将由活性成分组成的粉末，佐剂或其组合混合，同时加热和流化以获得单个颗粒，将由醇的偏酯与至少一种脂肪酸组成的脂质基质剂液化， 通过在单个颗粒上喷雾1至15重量％的最终组合物液体脂质基质剂，喷雾空气压力和任选的喷雾速率在整个涂布操作中变化并降低组合产物的温度，以允许脂质基质 药剂在谷物周围固化。

公开(公告)号：US06375987B1

公开(公告)日：2002-04-23

申请号：US09718613

申请日：2000-11-22

申请人： Nabil Farah ,  Philippe Bärthelemy ,  Joseph Joachim

发明人： Nabil Farah ,  Philippe Bärthelemy ,  Joseph Joachim

IPC分类号： A61K914

CPC分类号： A61K9/1694 ,  A61K9/1617

摘要： The invention relates to a process for the manufacture of a pharmaceutical composition with modified release of active principle comprising at least one active principle, a lipid matrix agent composed of ester of alcohol with at least one fatty acid and at least one adjuvant. This process is characterized in that: a powder composed of at least one component selected in the group comprising the active principle and the adjuvant, is mixed, while heating and fluidizing, in order to obtain individual grains; the said lipid matrix agent is liquefied separately under warm conditions; the said powder is then coated under warm conditions by spraying the said lipid matrix agent over the individual grains; finally, the temperature of the combined product is lowered in order to allow the lipid matrix agent to solidify.

摘要翻译： 本发明涉及一种制备具有改性释放活性成分的药物组合物的方法，其包含至少一种活性成分，由醇酯与至少一种脂肪酸和至少一种佐剂组成的脂质基质剂。该方法是 其特征在于：将由选自活性成分的组中选择的至少一种组分的粉末和佐剂混合，同时加热和流化，以获得单个颗粒;所述脂质基质剂在温热条件下分别液化 然后在温热条件下通过将所述脂质基质剂喷雾到单个颗粒上来涂覆所述粉末;最后，降低组合产品的温度，以使脂质基质剂固化。

公开(公告)号：US06379700B2

公开(公告)日：2002-04-30

申请号：US09733668

申请日：2000-12-08

申请人： Joseph Joachim ,  Pascal Prindirre ,  Nabil Farah

发明人： Joseph Joachim ,  Pascal Prindirre ,  Nabil Farah

IPC分类号： A61K922

CPC分类号： A61K9/2095 ,  A61K31/196 ,  A61K31/522

摘要： The invention concerns a method for making tablets with active principle sustained-release which consists in: preparing a fluid oil-in-water emulsion; spraying the resulting emulsion on a powder mixture containing at least the active principle; subjecting said treated powder to a compressing step, to obtain tablets.

摘要翻译： 本发明涉及一种制备具有主动缓释的片剂的方法，该方法包括：制备流体水包油乳液; 将所得乳液喷雾至至少含有活性成分的粉末混合物; 对所述处理的粉末进行压缩步骤，得到片剂。

公开(公告)号：US6054136A

公开(公告)日：2000-04-25

申请号：US838893

申请日：1997-04-11

申请人： Nabil Farah ,  Joel Denis

发明人： Nabil Farah ,  Joel Denis

IPC分类号： A61K8/06 ,  A61K8/39 ,  A61K9/107 ,  A61Q19/00 ,  A61K9/00

CPC分类号： A61K8/375 ,  A61K8/068 ,  A61K8/39 ,  A61K9/1075 ,  A61Q19/00 ,  A61K2800/92

摘要： Composition for pharmaceutical or cosmetic use, capable of forming a microemulsion, comprising at least:an active principle,a lipophilic phase consisting of a mixture of fatty acid esters and glycerides,a surfactant (SA),a cosurfactant (CoSA),a hydrophilic phase,characterized:in that the lipophilic phase consists of a mixture of C.sub.8 to C.sub.18 polyglycolized glycerides having a hydrophilic-lipophilic balance (HLB) of less than 16, this lipophilic phase representing from 30 to 75% of the total weight of the composition;in that the surfactant (SA) is chosen from the group comprising saturated C.sub.8 -C.sub.10 olyglycolized glycerides and oleic esters of polyglycerol, this surfactant having an HLB of less than 16;in that the cosurfactant (CoSA) is chosen from the group comprising lauric esters of propylene glycol, oleic esters of polyglycerol and ethyl diglycol;in that the SA/CoSA ratio is between 0.5 and 6;and in that the hydrophilic phase of the final microemulsion is supplied after ingestion by the physiological fluid of the digestive milieu.

摘要翻译： 能够形成微乳液的组合物，其至少包含：活性成分，由脂肪酸酯和甘油酯的混合物组成的亲油相，表面活性剂（SA），辅助表面活性剂（CoSA），亲水相 其特征在于：亲脂相由亲水 - 亲油平衡（HLB）小于16的C8-C18聚乙二醇化甘油酯的混合物组成，该亲油相占组合物总重量的30-75％ 表面活性剂（SA）选自饱和的C8-C10乙二醇化的甘油酯和聚甘油的油酸酯的组，该表面活性剂的HLB小于16; 辅助表面活性剂（CoSA）选自丙二醇的月桂酸酯，聚甘油的油酸酯和乙基二甘醇; 因为SA / CoSA比率在0.5和6之间; 并且由消化环境的生理液体吸收后提供最终微乳液的亲水相。

公开(公告)号：US06312704B1

公开(公告)日：2001-11-06

申请号：US09487391

申请日：2000-01-18

申请人： Nabil Farah ,  Joel Denis

发明人： Nabil Farah ,  Joel Denis

IPC分类号： A61K600

CPC分类号： A61K8/068 ,  A61K8/375 ,  A61K8/39 ,  A61K9/1075 ,  A61Q19/00

摘要： Composition for pharmaceutical or cosmetic use, capable of providing enhanced bioavailability when ingested, comprising at least a pharmaceutical active ingredient, a lipophilic phase consisting of a mixture of fatty acid esters and glycerides, a surfactant (SA), and a cosurfactant (CoSA). The lipophilic phase consists of a mixture of C8 to C18 polyglycolized glycerides having hydrophilic-lipophilic balance (HLB) of less than 16, this lipophilic phase representing from 32 to 75% of the total weight of the composition. The surfactant (SA) is chosen from the group comprising saturated C8-C10 polyglycolized glycerides and oleic esters of polyglycerol, this surfactant having an HLB of less than 16. The cosurfactant (CoSA) is chosen from the group comprising lauric esters of propylene glycol, oleic esters of polyglycerol and ethyl diglycol. The SA/CoSA ratio is between 0.5 and 6 and the hydrophilic phase of the final microemulsion is supplied after ingestion by the physiological fluid of the digestive milieu.

摘要翻译： 用于药物或化妆品用途的组合物，其能够在摄入时提供增强的生物利用度，其包含至少一种药物活性成分，由脂肪酸酯和甘油酯的混合物组成的亲油相，表面活性剂（SA）和辅助表面活性剂（CoSA）。 亲油相由具有小于16的亲水亲油平衡（HLB）的C8至C18聚乙二醇化甘油酯的混合物组成，该亲油相占组合物总重量的32-75％。 表面活性剂（SA）选自饱和C8-C10聚乙二醇化甘油酯和聚甘油油酸酯的组，该表面活性剂的HLB小于16.辅助表面活性剂（CoSA）选自丙二醇月桂酸酯， 聚甘油和乙基二甘醇的油酸酯。 SA / CoSA比值在0.5和6之间，并且最终微乳液的亲水相由消化环境的生理液体摄取后供应。