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1. 发明授权

US5648095A Preparation of microparticles 失效
标题翻译：微粒的制备
公开(公告)号：US5648095A
公开(公告)日：1997-07-15
申请号：US190022
申请日：1994-07-08
申请人： Lisbeth Illum , Olufunmiloyo Lilly Johnson
发明人： Lisbeth Illum , Olufunmiloyo Lilly Johnson
IPC分类号： A61K9/16 , A61K9/50 , A61K47/36 , A61K49/00 , A61K49/22 , B01J13/02 , B01J13/12 , A61K9/66
CPC分类号： B82Y15/00 , A61K49/223 , A61K49/225 , A61K9/1694 , A61K9/5036 , A61K9/5052 , A61K9/5089 , B01J13/125
摘要： Hollow microcapsules or solid microspheres for use in diagnostic procedures, as well as methods for making the microcapsules, are provided, which are formed by combining a volatile oil with an aqueous phase including a water soluble material such as a starch, modified starch or proteinaceous material, or a polyethylene glycol (PEG) conjugate, to form a primary emulsion. The primary emulsion then is combined with a second oil, to form a secondary emulsion, and the material is permitted to harden and to form microcapsules around a liquid core of the volatile oil. At least part of the volatile oil then may be removed by evaporation to produce hollow microcapsules. Optionally, all of the volatile oil may be removed prior to hardening of the material, which produces solid microspheres. The The microcapsules can be used in a variety of applications for diagnostic purposes and for drug delivery.
摘要翻译： PCT No.PCT / GB92 / 01421 Sec。 371日期：1994年7月8日 102（e）日期1994年7月8日PCT提交1992年8月3日PCT公布。出版物WO93 / 02712 日期1993年2月18日提供了用于诊断程序的微胶囊或固体微球，以及制备微胶囊的方法，其通过将挥发性油与包含水溶性物质如淀粉的水相组合而形成，改性淀粉或蛋白质材料，或聚乙二醇（PEG）缀合物，以形成初级乳液。然后将初级乳液与第二种油组合以形成二级乳液，并允许该材料硬化并在挥发性油的液芯周围形成微胶囊。然后可以通过蒸发除去至少部分挥发性油以产生中空微胶囊。任选地，在产生固体微球的材料硬化之前，所有的挥发油都可以被去除。微胶囊可用于各种诊断用途和药物递送应用。

2. 发明申请

US20110189299A1 PHARMACEUTICAL COMPOSITION CONTAINING SURFACE-COATED MICROPARTICLES 审中-公开
标题翻译：含有表面涂层微量元素的药物组合物
公开(公告)号：US20110189299A1
公开(公告)日：2011-08-04
申请号：US13001751
申请日：2009-07-01
申请人： Katsuyuki Okubo , Chieko Kitaura , Kenjiro Minomi , Elizabeth Pearson , Clive J. Roberts , Martyn C. Davies , Snjezana Stolnik-Trenkic , Lisbeth Illum
发明人： Katsuyuki Okubo , Chieko Kitaura , Kenjiro Minomi , Elizabeth Pearson , Clive J. Roberts , Martyn C. Davies , Snjezana Stolnik-Trenkic , Lisbeth Illum
IPC分类号： A61K9/14 , A61K39/00 , A61K38/02 , A61K38/28 , A61K31/711 , A61K31/713 , A61K31/715 , A61K31/422 , A61K31/137 , A61K31/7105 , A61P37/04
CPC分类号： A61K9/1676 , A61K9/0043 , A61K9/19 , A61K31/137 , A61K31/195 , A61K31/4045 , A61K31/715 , A61K47/32 , A61K47/34 , A61K47/42
摘要： The invention provides a pharmaceutical composition that can be used for efficient administration of low-molecular weight drugs and polymeric compounds such as peptides and proteins by methods other than injection, as well as a method for producing the composition. The pharmaceutical composition is for transmucosal administration and comprises (a) a drug having a positive or negative charge at a predetermined pH, (b) a pharmaceutically acceptable small particle and (c) a pharmaceutically acceptable surface-coating polymer capable of being electrically charged at the pH, wherein the surface of the small particle is coated by the surface-coating polymer, the drug is immobilized on the surface of the small particle via the surface-coating polymer, and a complex is formed by a noncovalent interaction between the small particle and the surface-coating polymer and a concurrent electrostatic interaction between the surface-coating polymer and the drug.
摘要翻译：本发明提供了一种可用于通过注射以外的方法有效施用低分子量药物和聚合物如肽和蛋白质的药物组合物，以及制备该组合物的方法。所述药物组合物用于经粘膜给药，并且包含（a）在预定pH下具有正电荷或负电荷的药物，（b）药学上可接受的小颗粒和（c）能够被电荷充电的药学上可接受的表面包衣聚合物 pH值，其中小颗粒的表面被表面涂层聚合物涂覆，药物通过表面涂层聚合物固定在小颗粒的表面上，并且通过小颗粒之间的非共价相互作用形成络合物表面涂层聚合物和表面涂层聚合物与药物之间的并发静电相互作用。

3. 发明申请

US20070110677A1 DELIVERY OF DRUGS TO MUCOSAL SURFACES 审中-公开
标题翻译：将药物递送到粘膜表面
公开(公告)号：US20070110677A1
公开(公告)日：2007-05-17
申请号：US11562002
申请日：2006-11-21
申请人： Peter Watts , Lisbeth Illum
发明人： Peter Watts , Lisbeth Illum
IPC分类号： A61K9/12 , A61K31/445 , A61K9/14
CPC分类号： A61K9/06 , A61K9/0043 , A61K9/12 , A61K47/36
摘要： Liquid pharmaceutical compositions for administration to a mucosal surface, including fentanyl and a pectin with a low degree of esterification are described. Such compositions gel, or can be adapted to gel, at the site of application in the absence of an extraneous source of divalent metal ions.
摘要翻译：描述了用于给予粘膜表面的液体药物组合物，包括芬太尼和低酯化程度的果胶。这种组合物在不存在二价金属离子的外来源的情况下，在施用部位凝胶化或者可以适应凝胶化。

4. 发明授权

US06355276B1 Adhesive drug delivery composition 失效
标题翻译：胶粘剂药物输送组合物
公开(公告)号：US06355276B1
公开(公告)日：2002-03-12
申请号：US08234723
申请日：1994-04-28
申请人： Lisbeth Illum , Paul Williams , Antony James Caston
发明人： Lisbeth Illum , Paul Williams , Antony James Caston
IPC分类号： A61K916
CPC分类号： A61K9/5052 , A61K9/167 , Y02A50/473
摘要： Adhesive material from the fimbriae (esp. Type 1) of bacteria or synthetic analogues or fragments thereof is combined with a drug to provide for attachment to the gut of a mammal, thereby prolonging the transit time of the drug through the gut. The 28 kDa polypeptide from E. coli Type 1 fimbriae is the preferred adhesive material (“adhesin”). The drug is presented in a carrier such as albumin, a polylactide/glycolide copolymer or alginate microcapsules. The adhesin may be incorporated in the carrier during preparation thereof, adsorbed onto the carrier after preparation, or covalently linked thereto, for example with carbodiimide.
摘要翻译：来自细菌（特别是1型）的细菌或合成类似物或其片段的粘合剂材料与药物组合以提供与哺乳动物的肠道连接，从而延长药物通过肠道的通过时间。来自大肠杆菌1型菌毛的28kDa多肽是优选的粘合剂材料（“粘附素”）。药物存在于载体如白蛋白，聚丙交酯/乙交酯共聚物或藻酸盐微胶囊中。粘附素可以在其制备过程中加入到载体中，在制备后吸附到载体上或与其共价连接，例如与碳二亚胺形成。

5. 发明授权

US5744166A Drug delivery compositions 失效
标题翻译：药物输送组合物
公开(公告)号：US5744166A
公开(公告)日：1998-04-28
申请号：US576877
申请日：1995-12-21
申请人： Lisbeth Illum
发明人： Lisbeth Illum
IPC分类号： A61K9/00 , A61K47/36 , A61K47/48 , A61K9/50 , A61K9/14 , A61K9/20
CPC分类号： A61K9/0014 , A61K47/36 , A61K47/4823 , A61K9/0043
摘要： Compositions for delivery of pharmacologically active agents and methods for their administration are provided. In one embodiment, the compositions include a complex of a polycationic polymer and a pharmacologically active agent in a pharmaceutically acceptable carrier. The compositions in one embodiment permit transport of pharmacologically active compounds across mucosal membranes for systemic delivery. The polycationic polymer may be, for example, a polycationic carbohydrate such as a chitosan or a chitosan salt or derivative. The therapeutic agent a preferred embodiment is a vaccine or a nucleic acid, such as a gene or antisense oligonucleotide. The composition may be provided in different forms such as a solution, dispersion, powder or in the form of microspheres.
摘要翻译：提供用于递送药理学活性剂的组合物及其给药方法。在一个实施方案中，组合物包括在可药用载体中的聚阳离子聚合物和药理活性剂的复合物。在一个实施方案中的组合物允许药物活性化合物跨越粘膜进行系统递送。聚阳离子聚合物可以是例如聚阳离子碳水化合物如壳聚糖或壳聚糖盐或衍生物。治疗剂优选的实施方案是疫苗或核酸，例如基因或反义寡核苷酸。组合物可以以不同形式提供，例如溶液，分散体，粉末或微球形式。

6. 发明授权

US5725871A Drug delivery compositions comprising lysophosphoglycerolipid 失效
标题翻译：包含溶血磷脂糖脂的药物递送组合物
公开(公告)号：US5725871A
公开(公告)日：1998-03-10
申请号：US260611
申请日：1994-06-15
申请人： Lisbeth Illum
发明人： Lisbeth Illum
IPC分类号： A61K9/00 , A61K47/24 , A61K9/08 , A61K9/16 , A61K38/00
CPC分类号： A61K47/24 , A61K9/0034 , A61K9/0043 , Y10S514/866 , Y10S514/964
摘要： Compositions for trans-mucosal delivery, e.g. intranasal, include a lysophosphatidyl-glycerol compound as the adsorption enhancer. The preferred compounds for delivery are insulin and calcitonin.
摘要翻译：用于反式粘膜递送的组合物鼻内，包括溶血磷脂酰甘油化合物作为吸附增强剂。用于递送的优选化合物是胰岛素和降钙素。

7. 发明授权

US5707644A Small particle compositions for intranasal drug delivery 无效
标题翻译：用于鼻内药物递送的小颗粒组合物
公开(公告)号：US5707644A
公开(公告)日：1998-01-13
申请号：US359937
申请日：1994-12-20
申请人： Lisbeth Illum
发明人： Lisbeth Illum
IPC分类号： A61K9/00 , A61K9/16 , A61K9/51 , A61K47/24
CPC分类号： A61K9/5161 , A61K47/24 , A61K9/0043 , A61K9/1652 , A61K9/1658 , Y10S514/866
摘要： A drug delivery composition for intranasal delivery comprises a plurality of bioadhesive microspheres and active drug associated with each microsphere, at least 90 wt % of the microspheres having a diameter in the range 0.1 .mu.m to 10 .mu.m. The microspheres may be of starch, gelatin, dextran, collagen or albumin. Suitable drags include peptides, such as insulin, and antigenic vaccine ingredients. The composition may additionally comprise an absorption enhancer. The microspheres are administered m the nasal cavity by a means such that the product of the square of the microsphere diameter and the flow rate is greater than 2000 .mu.m.sup.2.liters/min.
摘要翻译：用于鼻内递送的药物递送组合物包含多个生物粘附微球体和与每个微球体相关联的活性药物，至少90重量％的微球体的直径在0.1μm至10μm的范围内。微球可以是淀粉，明胶，葡聚糖，胶原蛋白或白蛋白。合适的药物包括肽，例如胰岛素和抗原性疫苗成分。该组合物可另外包含吸收增强剂。通过使微球直径的平方和流速的产物大于2000微米/分钟的方式在鼻腔内施用微球体。

8. 发明申请

US20120244196A1 PHARMACEUTICAL COMPOSITION CONTAINING MEDICAMENT-CONTAINING FINE PARTICLES AND METHOD FOR PRODUCING SAME 审中-公开
标题翻译：含有药物的精细颗粒的药物组合物及其生产方法
公开(公告)号：US20120244196A1
公开(公告)日：2012-09-27
申请号：US13499876
申请日：2010-10-01
申请人： Katsuyuki Okubo , Toshihiko Okazaki , Chieko Kitaura , Kenjiro Minomi , Elizabeth Pearson , Clive J. Roberts , Martyn C. Davies , Snjezana Stolnik-Trenkic , Lisbeth Illum
发明人： Katsuyuki Okubo , Toshihiko Okazaki , Chieko Kitaura , Kenjiro Minomi , Elizabeth Pearson , Clive J. Roberts , Martyn C. Davies , Snjezana Stolnik-Trenkic , Lisbeth Illum
IPC分类号： A61K9/14 , A61K38/38 , A61K38/28
CPC分类号： A61K9/19 , A61K9/146 , A61K31/7105 , A61K31/711 , A61K31/713 , A61K31/715 , A61K33/00 , A61K33/14 , A61K33/30 , A61K38/28 , A61K39/385 , A61K39/39 , A61K45/06 , A61K48/00 , A61K2039/55555 , C12N15/88 , A61K2300/00
摘要： The invention provides a pharmaceutical composition that can be used for an efficient administration of a water-soluble polymer drug by a method other than injection, and a method for production of the pharmaceutical composition. The pharmaceutical composition contains a small particle comprised of (a) a water-soluble drug and (b) a pharmaceutically acceptable ionic crystalline compound which is solid at room temperature, wherein the ionic crystalline compound is crystallized in the small particle.
摘要翻译：本发明提供了可以通过除了注射以外的方法有效施用水溶性聚合物药物的药物组合物和药物组合物的制造方法。药物组合物含有由（a）水溶性药物和（b）在室温下为固体的药学上可接受的离子结晶化合物组成的小颗粒，其中离子结晶化合物在小颗粒中结晶。

9. 发明申请

US20080248991A1 Chitosan Containing Solution 审中-公开
标题翻译：壳聚糖包含溶液
公开(公告)号：US20080248991A1
公开(公告)日：2008-10-09
申请号：US10598212
申请日：2005-02-18
申请人： Ann Margaret Dyer , Patricia Pastor , Lisbeth Illum
发明人： Ann Margaret Dyer , Patricia Pastor , Lisbeth Illum
IPC分类号： A61K38/02 , A61K47/36 , A61K31/7052 , A61M31/00 , A61K31/485 , A61K31/375
CPC分类号： A61K47/36 , A61K9/0034 , A61K9/0043 , A61K9/0048 , A61K9/06 , A61K9/08 , A61K31/485 , A61K38/23 , A61K47/26
摘要： The invention provides a composition comprising (i) chitosan, a salt or derivative thereof or a salt of a derivative thereof, (ii) a polyol-phosphate or sugar-phosphate salt, (iii) a plasticizer, and (iv) a therapeutic agent. Typically, the composition is a solution or suspension at ambient temperature but forms a gel at physiological temperatures.
摘要翻译：本发明提供了包含（i）壳聚糖，其盐或衍生物或其衍生物的盐，（ii）多元醇 - 磷酸盐或糖 - 磷酸盐，（iii）增塑剂和（iv）治疗剂。通常，组合物是环境温度下的溶液或悬浮液，但在生理温度下形成凝胶。

10. 发明申请

US20060115525A1 Pharmaceutical compositions 审中-公开
标题翻译：药物组合物
公开(公告)号：US20060115525A1
公开(公告)日：2006-06-01
申请号：US11271403
申请日：2005-11-12
申请人： Michael Leane , Alan Smith , Lisbeth Illum
发明人： Michael Leane , Alan Smith , Lisbeth Illum
IPC分类号： A61K38/28 , A61K38/22 , A61K38/21 , A61K38/20 , A61K38/19 , A61K38/18 , A61K9/48
CPC分类号： A61K9/4808 , A61K9/1617 , A61K9/1652 , A61K9/205 , A61K9/5047 , A61K9/5084 , A61K31/19 , A61K31/722 , A61K38/00
摘要： The present invention provides a solid composition for oral administration comprising: (i) a drug compound; (ii) chitosan or a derivative thereof or a salt of chitosan or salt of a derivative of chitosan; and (iii) an organic acid. Preferably the drug compound is a polar molecule having a molecular weight of 1 KDa or less, a peptide, a protein or a polysaccharide. The compositions of the invention provide enhance absorption of the drug compound.
摘要翻译：本发明提供一种用于口服给药的固体组合物，其包含：（i）药物化合物; （ii）壳聚糖或其衍生物或壳聚糖的盐或壳聚糖衍生物的盐; 和（iii）有机酸。优选地，药物化合物是分子量为1KDa或更小的极性分子，肽，蛋白质或多糖。本发明的组合物提供药物化合物的增强吸收。

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