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1. 发明申请

WO2008033024A2 DOSAGE UNIT FOR SUBLINGUAL, BUCCAL OR ORAL ADMINISTRATION OF WATER-INSOLUBLE PHARMACEUTICALLY ACTIVE SUBSTANCES 审中-公开
标题翻译：剂量单位用于水不溶性药物活性物质的分类，结构或口服施用
公开(公告)号：WO2008033024A2
公开(公告)日：2008-03-20
申请号：PCT/NL2007/050449
申请日：2007-09-14
申请人： ECHO PHARMACEUTICALS B.V. , PELLIKAAN, Hubert, Clemens , VERMEULEN, Pieter, Sebastiaan , BENDER, Johannes, Caspar, Mathias, Elizabeth , WOERLEE, Geert, Feye
发明人： PELLIKAAN, Hubert, Clemens , VERMEULEN, Pieter, Sebastiaan , BENDER, Johannes, Caspar, Mathias, Elizabeth , WOERLEE, Geert, Feye
IPC分类号： A61K9/00 , A61K9/20 , A61K31/352
CPC分类号： A61K9/2077 , A61K9/0056
摘要： One aspect of the invention relates to a pharmaceutical dosage unit for sublingual, buccal, pulmonary or oral administration, said dosage unit having a weight of 20-500 mg and comprising 1-80 wt.% of a microgranulate that is distributed throughout a solid hydrophilic matrix; said microgranulate being characterised in that it: has a volume weighted average diameter of 5-100 m; contains at least 0.01 wt.%, preferably at least 0.1 wt.% of one or more water-insoluble pharmaceutically active substances; contains at least 10 wt.%, preferably at least 20 wt.% of an emulsifier component; and is capable of forming a micro-emulsion upon contact with saliva or water. The dosage units of the present invention achieve the inherent benefits of oral delivery whilst at the same time realising a high transmucosal absorption rate of the cannabinoids contained therein. Other aspects of the present invention relate to the use of the aforementioned dosage units in the therapeutic or prophylactic treatment and to a process for the manufacture of said dosage units.
摘要翻译：本发明的一个方面涉及用于舌下，口腔，肺或口服给药的药物剂量单位，所述剂量单位的重量为20-500mg，并且包含1-80wt。％的微粒，其分布在整个固体亲水性矩阵; 所述微粒的特征在于：具有5-100μm的体积加权平均直径; 含有至少0.01重量％，优选至少0.1重量％的一种或多种水不溶性药物活性物质; 含有至少10重量％，优选至少20重量％的乳化剂组分; 并且能够在与唾液或水接触时形成微乳液。本发明的剂量单位实现口服递送的固有益处，同时实现其中所含的大麻素的高透粘膜吸收速率。本发明的其它方面涉及上述剂量单位在治疗或预防治疗中的用途以及制备所述剂量单位的方法。

2. 发明申请

WO2008033023A3 GRANULATE CONTAINING A PHARMACEUTICALLY ACTIVE SUBSTANCE AND ANEMULSIFIER AND METHOD FOR ITS MANUFACTURE 审中-公开
标题翻译：含有药物活性物质的颗粒和其制造方法及其制造方法
公开(公告)号：WO2008033023A3
公开(公告)日：2008-09-12
申请号：PCT/NL2007050448
申请日：2007-09-14
申请人： ECHO PHARMACEUTICALS BV , PELLIKAAN HUBERT CLEMENS , VERMEULEN PIETER SEBASTIAAN , BENDER JOHANNES CASPAR MATHIAS , FERNANDEZ CID MARIA VANESA
发明人： PELLIKAAN HUBERT CLEMENS , VERMEULEN PIETER SEBASTIAAN , BENDER JOHANNES CASPAR MATHIAS , FERNANDEZ CID MARIA VANESA
IPC分类号： A61K9/00 , A61K9/16
CPC分类号： A61K9/2059 , A61K9/1617 , A61K9/1623 , A61K9/1694 , A61K9/2013 , A61K9/2018
摘要： One aspect of the present invention relates to a granulate having a volume weighted mean diameter of 1-200 m and containing: at least 0.1 wt.% of a pharmaceutically active substance; at least 10 wt.% of emulsifier 0-89.9 wt.% of a water-dispersible saccharide; the combination of the pharmaceutically active substance, the emulsifier and the water-dispersible saccharide together represening at least 60 wt.% of the granulate; wherein the granulate is monophasic or wherein the granulate comprises a dispersed phase containing the pharmaceutically active substance, said dispersed phase having a volume weighted mean diameter of less than 300 nm. Another aspect of the invention relates to a process for the preparation of said granulate containing a pharmaceutically active substance, which process employs.
摘要翻译：本发明的一个方面涉及体积加权平均直径为1-200μm并含有至少0.1wt％的药物活性物质的颗粒; 至少10重量％的乳化剂0-89.9重量％的水分散性糖; 药物活性物质，乳化剂和水分散性糖的组合共同表示至少60重量％的颗粒; 其中所述颗粒是单相的或其中所述颗粒包含含有所述药物活性物质的分散相，所述分散相的体积加权平均直径小于300nm。本发明的另一方面涉及一种制备含有药物活性物质的所述颗粒的方法，该方法使用。

3. 发明申请

WO2011112082A1 STERILE ALGINATE-BASED AQUEOUS COMPOSITION FOR MEDICAL USE AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：用于医疗用途的基于ALT的碱性水性组合物及其制备方法
公开(公告)号：WO2011112082A1
公开(公告)日：2011-09-15
申请号：PCT/NL2011/050160
申请日：2011-03-08
申请人： BENDER ANALYTICAL HOLDING B.V. , BENDER, Johannes Caspar Mathias Elizabeth , PELLIKAAN, Hubert Clemens
发明人： BENDER, Johannes Caspar Mathias Elizabeth , PELLIKAAN, Hubert Clemens
IPC分类号： A61K31/734
CPC分类号： A61K31/734 , A61K9/0024 , A61K47/02 , A61K47/36
摘要： The present invention relates to ready-to-use sterile, alginate-based, aqueous compositions for medical use. More particularly, the invention relates to an aqueous composition for medical use that has been sterilized by heat sterilization and having a viscosity at 25 ºC of at least 300 cP (Helipath® T F spindle, 100 rpmat 25 °C), said composition having a pH in the range of 6.5-7.5; containing 0.5-10 wt.% of an alginate salt; and further containing 10-500 mM of one or more dissolved C 2 -C 7 mono-or dicarboxylates that are optionally substituted with up to 2 hydroxyl groups. The alginate-based composition of the present invention has excellent storage stability and is easy to manufacture. The alginate-based aqueous compositions of the present invention can advantageously be used, for instance, to prevent adhesions between a healing trauma site and adjacent surrounding tissue. These compositions can further be used in implants or in pharmaceutical preparations for oral administration.
摘要翻译：本发明涉及用于医疗用途的即用型无菌藻酸盐基水性组合物。更具体地说，本发明涉及用于医疗用途的水性组合物，其已经通过热灭菌灭菌，并且在25℃下的粘度为至少300cP（Helipath？TF锭子，25 rpm，100 rpm），所述组合物具有pH 在6.5-7.5的范围内; 含有0.5-10重量％的藻酸盐; 并进一步含有10-500mM的一个或多个可任选被至多2个羟基取代的溶解的C 2 -C 7单或二羧酸酯。本发明的基于藻酸盐的组合物具有优异的储存稳定性，易于制造。本发明的藻酸盐基水性组合物可以有利地用于例如防止愈合创伤部位和相邻的周围组织之间的粘连。这些组合物还可以用于植入物或用于口服给药的药物制剂中。

4. 发明申请

WO2004006893A1 METHOD FOR PARTICLE PRECIPITATION USING NEAR-CRITICAL AND SUPERCRITICAL ANTISOLVENTS 审中-公开
标题翻译：使用临界和超临界反应的颗粒沉降的方法
公开(公告)号：WO2004006893A1
公开(公告)日：2004-01-22
申请号：PCT/NL2003/000516
申请日：2003-07-15
申请人： FEYECON DEVELOPMENT & IMPLEMENTATION B.V. , UNIVERSITEIT LEIDEN , PELLIKAAN, Hubert, Clemens , BORCHARD, Gerrit
发明人： PELLIKAAN, Hubert, Clemens , BORCHARD, Gerrit
IPC分类号： A61K9/16
CPC分类号： A61K9/5161 , A61K9/1652 , A61K9/1694 , A61K9/5192 , A61K48/0008 , A61K48/0041 , A61K2039/55555
摘要： The present invention is concerned with a continuous or semi-continuous process for the preparation of small particles through precipitation, which process employs (i) a fluid solution comprising a solvent and a solute to be precipitated and (ii) a non-gaseous antisolvent, said solvent being soluble in or miscible with the antisolvent and said solute being substantially insoluble in the antisolvent, said process comprising the successive steps of: a. combining the fluid solution and the antisolvent so as to achieve a condition of super saturation; b. allowing nucleation to commence and the nuclei formed to grow to particles with a volume weighted average diameter of between 5 nm and 50,000 nm, c. collecting the resulting particles and separating them from the antisolvent; wherein the solvent contains an organic solvent and less than 20 wt.% water and the solute comprises a charged carbohydrate polymer in combination with a second biopolymer component selected from the group consisting of polynucleotides, amino acid polymers and mixtures thereof; and wherein step a. and b. are carried out under a substantially constant pressure. Suitable examples of the charged carbohydrate polymer include chitosan polymers, heparin, hyaluronic acid polymers and derivatives thereof. The particles obtained from the above process may suitably be used for intracellular delivery of a polynucleotide and/or a polyamino acid in animals and humans.
摘要翻译：本发明涉及通过沉淀制备小颗粒的连续或半连续方法，该方法使用（i）包含溶剂和待沉淀的溶质的流体溶液，和（ii）非气态反溶剂，所述溶剂可溶于抗溶剂或与溶液混溶，所述溶质基本上不溶于抗溶剂，所述方法包括以下连续步骤：a。结合流体溶液和抗溶剂，以达到超饱和状态; 湾允许成核开始，并且形成的细胞核生长成体积加权平均直径在5nm和50,000nm之间的颗粒，c。收集所得颗粒并将其与抗溶剂分离; 其中所述溶剂含有有机溶剂和少于20重量％的水，并且所述溶质包含带电荷的碳水化合物聚合物与选自多核苷酸，氨基酸聚合物及其混合物的第二生物聚合物组分; 并且其中步骤a。和b。在基本恒定的压力下进行。带电碳水化合物聚合物的合适实例包括壳聚糖聚合物，肝素，透明质酸聚合物及其衍生物。从上述方法获得的颗粒可适合用于动物和人体中多核苷酸和/或多氨基酸的细胞内递送。

5. 发明申请

WO2008033023A2 GRANULATE CONTAINING A PHARMACEUTICALLY ACTIVE SUBSTANCE AND METHOD FOR ITS MANUFACTURE 审中-公开
标题翻译：含有药物活性物质的颗粒及其制造方法
公开(公告)号：WO2008033023A2
公开(公告)日：2008-03-20
申请号：PCT/NL2007/050448
申请日：2007-09-14
申请人： FEYECON DEVELOPMENT & IMPLEMENTATION B.V. , PELLIKAAN, Hubert Clemens , VERMEULEN, Pieter Sebastiaan , BENDER, Johannes Caspar Mathias Elizabeth , FERNANDEZ CID, Maria, Vanesa
发明人： PELLIKAAN, Hubert Clemens , VERMEULEN, Pieter Sebastiaan , BENDER, Johannes Caspar Mathias Elizabeth , FERNANDEZ CID, Maria, Vanesa
CPC分类号： A61K9/2059 , A61K9/1617 , A61K9/1623 , A61K9/1694 , A61K9/2013 , A61K9/2018
摘要： One aspect of the present invention relates to a granulate having a volume weighted mean diameter of 1-200 m and containing: at least 0.1 wt.% of a pharmaceutically active substance; at least 10 wt.% of emulsifier selected from the group consisting of sugar fatty acid esters, mono-glycerides, di-glycerides, diacetyl tartaric acid ester of monoglyceride, diacetyl tartaric acid esters of diglyceride, polyglycerol esters, calcium stearoyl lactylate, sodium stearoyl lactylate and combinations thereof; and 0-89.9 wt.% of a water-dispersible saccharide; the combination of the pharmaceutically active substance, the emulsifier and the water-dispersible saccharide together represening at least 60 wt.% of the granulate; wherein the granulate is monophasic or wherein the granulate comprises a dispersed phase containing the pharmaceutically active substance, said dispersed phase having a volume weighted mean diameter of less than 300 nm. The granulates of the present invention enable the manufacture of transmucosal dosage units that exhibit improved solubility and/or bioavailability of the pharmaceutically active substance. Another aspect of the invention relates to a process for the preparation of a granulate containing a pharmaceutically active substance, which process employs: a pumpable emulsion comprising (i) a continuous phase containing a polar solvent and (ii) a dispersed phase containing an emulsifier and a pharmaceutically active substance; an extractant comprising a supercritical, subcritical or liquefied gas; said solvent being substantially more soluble in the extractant than said emulsifier; the process comprising the successive steps of : a. combining the pumpable emulsion with the extractant under mixing conditions; b. allowing the formation of granules containing the emulsifier and the pharmaceutically active substance; c. collect ing the granules and separating them from the extractant.
摘要翻译：本发明的一个方面涉及体积加权平均直径为1-200μm并含有至少0.1wt％的药物活性物质的颗粒; 至少10重量％的选自糖脂肪酸酯，单甘油酯，二甘油酯，甘油单酯的二乙酰酒石酸酯，甘油二酯的二乙酰酒石酸酯，聚甘油酯，硬脂酰乳酸钙，硬脂酰基硬脂酸钠乳酸盐及其组合; 和0-89.9重量％的水分散性糖; 药物活性物质，乳化剂和水分散性糖的组合共同表示至少60重量％的颗粒; 其中所述颗粒是单相的或其中所述颗粒包含含有所述药物活性物质的分散相，所述分散相的体积加权平均直径小于300nm。本发明的颗粒能够制造显示改善的药物活性物质的溶解度和/或生物利用度的经粘膜剂量单位。本发明的另一方面涉及一种制备含有药物活性物质的颗粒的方法，该方法采用：可泵送乳液，其包含（i）含有极性溶剂的连续相和（ii）含有乳化剂的分散相和药物活性物质; 包括超临界，亚临界或液化气体的萃取剂; 所述溶剂比所述乳化剂在萃取剂中更可溶; 该过程包括以下连续步骤：a。将可泵送乳液与萃取剂在混合条件下结合; 湾允许形成含有乳化剂和药物活性物质的颗粒; C。收集颗粒并将其与萃取剂分离。

6. 发明申请

WO2003086606A1 PROCESS FOR SMALL PARTICLE FORMATION 审中-公开
标题翻译：小粒子形成过程
公开(公告)号：WO2003086606A1
公开(公告)日：2003-10-23
申请号：PCT/NL2003/000168
申请日：2003-03-06
申请人： FEYECON DEVELOPMENT & IMPLEMENTATION B.V. , PELLIKAAN, Hubert, Clemens , WUBBOLTS, Frank, Emile
发明人： PELLIKAAN, Hubert, Clemens , WUBBOLTS, Frank, Emile
IPC分类号： B01J2/04
CPC分类号： B01J2/04
摘要： The present invention is concerned with a process for the preparation of small particles through precipitation. More particularly, the present invention relates to such a process which employs a fluid solution comprising a solvent and solute to be precipitated and a non-gaseous antisolvent, said solvent being soluble in or miscible with the antisolvent and said solute being substantially insoluble in the antisolvent, wherein the process comprises the successive steps of: a. feeding a stream of the fluid solution and a stream of the antisolvent into a mixing zone (5) where both streams are thoroughly mixed to achieve a condition of super saturation whilst ensuring that hardly any nucleation occurs during the mixing; b. feeding the resulting mixture of the fluid solution and the antisolvent into a nucleation zone (6) allowing nucleation to commence; c. allowing the nuclei formed in the nucleation zone the grow to particles with a volume weighted average diameter of no more than 50 µm, preferably of no more than 7 µm. d. collecting the particles and separating them from the antisolvent.
摘要翻译：本发明涉及通过沉淀制备小颗粒的方法。更具体地说，本发明涉及使用包含溶剂和溶质沉淀的流体溶液和非气态反溶剂的方法，所述溶剂可溶于抗溶剂或与抗溶剂混溶，所述溶质基本上不溶于抗溶剂，其中所述方法包括以下连续步骤：a。将流体溶液流和反应溶剂流流入混合区（5），其中两个流充分混合以实现超饱和状态，同时确保在混合期间几乎不发生任何成核; 湾将所得到的流体溶液和抗溶剂的混合物进料到允许成核开始的成核区域（6）中; C。允许在成核区域中形成的核生长成体积加权平均直径不超过50μm，优选不大于7μm的颗粒。天。收集颗粒并将其与抗溶剂分离。

7. 发明申请

WO2013039380A1 STERILE ALGINATE-BASED AQUEOUS COMPOSITION FOR MEDICAL USE AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：用于医疗用途的基于ALT的碱性水性组合物及其制备方法
公开(公告)号：WO2013039380A1
公开(公告)日：2013-03-21
申请号：PCT/NL2012/050318
申请日：2012-05-10
申请人： Bender Analytical Holding B.V. , Bender, Johannes Caspar Mathias Elizabeth , Pellikaan, Hubert Clemens
发明人： Bender, Johannes Caspar Mathias Elizabeth , Pellikaan, Hubert Clemens
IPC分类号： A61K31/19 , A61K47/36
CPC分类号： A61K9/0019 , A61K31/721 , A61K31/734 , A61K47/36
摘要： The present invention relates to ready-to-use sterile, alginate-based, aqueous compositions for medical use. More particularly, the invention relates to an aqueous composition for medical use that has been sterilized by heat sterilization and having a viscosity at 25 °C of at least 300 cP (Helipath® T F spindle, 100 rpm at 25 °C), said composition having a pH in the range of 6.5-7.5; containing 0.5-10 wt.% of an alginate salt; and further containing 10-500 mM of one or more dissolved C 8 -C 12 fatty acid salts. The alginate-based composition of the present invention has excellent storage stability and is easy to manufacture. The alginate-based aqueous compositions of the present invention can advantageously be used, for instance, to prevent adhesions between a healing trauma site and adjacent surrounding tissue. These compositions can further be used in implants or in pharmaceutical preparations for oral administration.
摘要翻译：本发明涉及用于医疗用途的即用型无菌藻酸盐基水性组合物。更具体地说，本发明涉及用于医疗用途的水性组合物，其已经通过热灭菌消毒并且在25℃下具有至少300cP的粘度（Helipath TF锭子，25℃下100rpm），所述组合物具有 pH在6.5-7.5的范围内; 含有0.5-10重量％的藻酸盐; 并进一步含有10-500mM的一种或多种溶解的C8-C12脂肪酸盐。本发明的基于藻酸盐的组合物具有优异的储存稳定性，易于制造。本发明的藻酸盐基水性组合物可以有利地用于例如防止愈合创伤部位和相邻的周围组织之间的粘连。这些组合物还可以用于植入物或用于口服给药的药物制剂中。

8. 发明申请

WO2008033024A3 DOSAGE UNIT FOR SUBLINGUAL, BUCCAL OR ORAL ADMINISTRATION OF WATER-INSOLUBLE PHARMACEUTICALLY ACTIVE SUBSTANCES 审中-公开
标题翻译：用于口服，口腔或口服给药不溶于水的药物活性物质的剂量单位
公开(公告)号：WO2008033024A3
公开(公告)日：2008-05-22
申请号：PCT/NL2007050449
申请日：2007-09-14
申请人： ECHO PHARMACEUTICALS BV , PELLIKAAN HUBERT CLEMENS , VERMEULEN PIETER SEBASTIAAN , BENDER JOHANNES CASPAR MATHIAS , WOERLEE GEERT FEYE
发明人： PELLIKAAN HUBERT CLEMENS , VERMEULEN PIETER SEBASTIAAN , BENDER JOHANNES CASPAR MATHIAS , WOERLEE GEERT FEYE
IPC分类号： A61K9/00 , A61K9/20 , A61K31/352
CPC分类号： A61K9/2077 , A61K9/0056
摘要： One aspect of the invention relates to a pharmaceutical dosage unit for sublingual, buccal, pulmonary or oral administration, said dosage unit having a weight of 20-500 mg and comprising 1-80 wt.% of a microgranulate that is distributed throughout a solid hydrophilic matrix; said microgranulate being characterised in that it: has a volume weighted average diameter of 5-100 m; contains at least 0.01 wt.%, preferably at least 0.1 wt.% of one or more water-insoluble pharmaceutically active substances; contains at least 10 wt.%, preferably at least 20 wt.% of an emulsifier component; and is capable of forming a micro-emulsion upon contact with saliva or water. The dosage units of the present invention achieve the inherent benefits of oral delivery whilst at the same time realising a high transmucosal absorption rate of the cannabinoids contained therein. Other aspects of the present invention relate to the use of the aforementioned dosage units in the therapeutic or prophylactic treatment and to a process for the manufacture of said dosage units.
摘要翻译：本发明的一个方面涉及一种用于舌下，口腔，肺或口服给药的药物剂量单位，所述具有20-500毫克重量的剂量单位和包括被在整个固体亲水性分布微粒（microgranulate）的1-80％（重量）矩阵; 所述微粒的特征在于：具有5-100μm的体积加权平均直径; 含有至少0.01重量％，优选至少0.1重量％的一种或多种水不溶性药物活性物质; 含有至少10重量％，优选至少20重量％的乳化剂组分; 并且能够在与唾液或水接触时形成微乳液。本发明的剂量单位实现口服递送的固有益处，同时实现其中所含大麻素的高透粘膜吸收速率。本发明的其它方面涉及前述剂量单位在治疗性或预防性治疗中的用途和制造所述剂量单位的方法。

9. 发明申请

WO2002102947A1 A METHOD OF PROCESSING LIPID MATERIALS 审中-公开
标题翻译：一种加工脂肪材料的方法
公开(公告)号：WO2002102947A1
公开(公告)日：2002-12-27
申请号：PCT/NL2002/000404
申请日：2002-06-19
申请人： FEYECON DEVELOPMENT & IMPLEMENTATION B.V. , WOERLEE, Geert, Feye , PELLIKAAN, Hubert, Clemens , PETERS RIT, Antonius, Wilhelmus, Petrus, Gerardus
发明人： WOERLEE, Geert, Feye , PELLIKAAN, Hubert, Clemens , PETERS RIT, Antonius, Wilhelmus, Petrus, Gerardus
IPC分类号： C11B3/10
CPC分类号： C11C1/06 , C11B3/10 , C11C1/106 , C11C3/123
摘要： The present invention is concerned with a new method of processing lipid materials, such as triglycerides and waxes, which process involves contacting such lipid materials with a reactive granulate in the presence of a gas in near supercritical state. More particularly the present invention relates to a method of processing lipid material comprising the steps of a) dissolving into the lipid material from 5-95 wt.% of a gas selected from the group consisting of carbon dioxide, ethane, propane, or nitrous oxide and mixtures thereof, at a temperature and a pressure at which the gas per se would be near its supercritical state, b) contacting the lipid material containing the dissolved gas with a reactive granulate, c) separating the granulate from the lipid material and d) allowing the gas to evaporate from the lipid material by reducing the pressure. The reactive granulate employed in the present process may suitably be a catalyst, such as bleaching earth or hydrogenation catalyst, or an adsorbent, such as active carbon.
摘要翻译：本发明涉及一种加工脂质物质如甘油三酸酯和蜡的新方法，该方法包括在近乎超临界状态的气体存在下使这种脂质物质与反应性颗粒接触。更具体地说，本发明涉及一种处理脂质材料的方法，包括以下步骤：a）将5-95重量％的选自二氧化碳，乙烷，丙烷或一氧化二氮的气体溶解在脂质材料中气体本身的温度和压力将接近其超临界状态，b）使含有溶解气体的脂质材料与反应性颗粒接触，c）将颗粒分离，从脂质材料和d）通过降低压力使气体从脂质材料蒸发。本方法中使用的反应性颗粒可以适当地为催化剂，如漂白土或氢化催化剂，或吸附剂，如活性炭。

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