公开(公告)号：US06423344B1

公开(公告)日：2002-07-23

申请号：US09498397

申请日：2000-02-04

申请人： Robert M. Platz ,  Thomas K. Brewer ,  Terence D. Boardman

发明人： Robert M. Platz ,  Thomas K. Brewer ,  Terence D. Boardman

IPC分类号： A61K916

CPC分类号： A61K9/0075 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/1658 ,  A61K9/1694 ,  A61K38/28 ,  A61M15/0086

摘要： A process for preparing ultrafine powders of biological macromolecules comprises atomizing liquid solutions of the macromolecules, drying the droplets formed in the atomization step, and collecting the particles which result from drying. By properly controlling each of the atomization, drying, and collection steps, ultrafine dry powder compositions having characteristics particularly suitable for pulmonary delivery for therapeutic and other purposes may be prepared.

公开(公告)号：US06419960B1

公开(公告)日：2002-07-16

申请号：US09465159

申请日：1999-12-16

申请人： Thinnayam N. Krishnamurthy ,  Andrew Darke

发明人： Thinnayam N. Krishnamurthy ,  Andrew Darke

IPC分类号： A61K916

CPC分类号： A61K9/209 ,  A61K9/0053 ,  A61K9/167 ,  A61K9/2081 ,  A61K9/2086 ,  A61K9/2846 ,  A61K9/2893 ,  A61K9/5026 ,  A61K9/5047 ,  A61K9/5073 ,  A61K9/5078 ,  A61K9/5084 ,  A61K9/5089 ,  A61K31/4458

摘要： The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

摘要翻译： 本发明涉及口服改良/控释药物制剂，其提供快速起效和起效延长。 优选地，峰值浓度低于药物立即释放制剂的参考标准提供的峰值浓度，并且效果持续时间在给药间隔结束时迅速下降。

公开(公告)号：US06379705B1

公开(公告)日：2002-04-30

申请号：US09580551

申请日：2000-05-30

申请人： Carla Patricia Goncalves Mendes ,  Maria Julia Caeiro Ramalho De Oliveira

发明人： Carla Patricia Goncalves Mendes ,  Maria Julia Caeiro Ramalho De Oliveira

IPC分类号： A61K916

CPC分类号： A61K31/4439 ,  A61K9/5078 ,  A61K31/4184

摘要： The present invention relates to oral multi-unitary pharmaceutical preparations containing substituted benzimidazoles being inhibitors of H+, K+-ATPase (i.e. omeprazole, lansoprazole, pantoprazole, leminoprazole and pariprazole) or their pharmaceutically acceptable salts. Such pharmaceutical preparations are stable pellet preparations containing substituted benzimidazole(s) or their salts and they comprise a quantity of active ingredient of between 1 and 50 mg, an inert core of spherical symmetry with a diameter of 600-1000 &mgr;m, constituted by inert excipients, coated with an active layer containing at least one substituted benzimidazole in the micronized form and various pharmaceutically acceptable inert excipients, mixed in suitable proportions in order to allow the disaggregation of the formulations and dissolution of the active ingredient(s) in an appropriate manner, coated in turn with an insulating layer of a strictly polymeric nature, soluble in water, free from alkaline and/or alkaline-earthy metallic salts, of a minimum thickness of 15 &mgr;m, this layer being coated lastly with a gastroresistant or enteric layer of a minimum thickness of 30 &mgr;m. This invention also refers to the process for the preparation of said pharmaceutical preparations.

摘要翻译： 本发明涉及含有取代的苯并咪唑的口服多单一药物制剂，其为H +，K + -ATPase（即奥美拉唑，兰索拉唑，泮托拉唑，依米卡唑和派吡拉唑）或其药学上可接受的盐的抑制剂。 这样的药物制剂是含有取代的苯并咪唑或其盐的稳定的丸剂制剂，它们包含1至50mg的活性成分，一种直径为600-1000μm的球形对称的惰性核心，由惰性赋形剂 涂覆有含有至少一种微粉化形式的取代的苯并咪唑的活性层和各种药学上可接受的惰性赋形剂，以适当的比例混合，以允许制剂的分解和活性成分以适当的方式溶解， 依次具有严格聚合性质的绝缘层，其可溶于最低厚度为15μm的碱土金属盐和/或碱土金属盐的水中，该层最后涂覆有抗胃或肠溶层 最小厚度30 mum。 本发明还涉及制备所述药物制剂的方法。

公开(公告)号：US06368635B1

公开(公告)日：2002-04-09

申请号：US08993314

申请日：1997-12-18

申请人： Yohko Akiyama ,  Naoki Nagahara ,  Shin-ichiro Hirai

发明人： Yohko Akiyama ,  Naoki Nagahara ,  Shin-ichiro Hirai

IPC分类号： A61K916

CPC分类号： A61K9/1635 ,  A61K9/1617 ,  A61K9/5026 ,  A61K9/5047 ,  Y10S514/952

摘要： A solid matrix composition which is solid at ambient temperature, which comprises a viscogenic agent, such as an acrylic acid polymer, capable of developing viscosity on contact with water, as dispersed at least in the neighborhood of the surface layer of a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient. The matrix may be such that a matrix particle containing a polyglycerol fatty acid ester or a lipid and an active ingredient has been coated with a coating composition containing at least one viscogenic agent. Such composition can adhere to the digestive tract and remain there for a prolonged period of time, thereby increasing the bioavailability of the active ingredient. Solid preparations, such as fine granules and granules, contain the above matrix composition.

摘要翻译： 一种在环境温度下为固体的固体基质组合物，其包含能够在与水接触时显现出粘度的粘性剂如丙烯酸聚合物，至少分散在含有 聚甘油脂肪酸酯或脂质和活性成分。 基质可以使得含有聚甘油脂肪酸酯或脂质和活性成分的基质颗粒已经涂覆有含有至少一种粘稠剂的涂料组合物。 这样的组合物可以粘附到消化道上并且长时间保持在那里，从而增加活性成分的生物利用度。 固体制剂，如细颗粒和颗粒，含有上述基质组成。

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。

公开(公告)号：US06346274B1

公开(公告)日：2002-02-12

申请号：US08894796

申请日：1998-01-05

申请人： Hans Koll ,  Gerhard Winter ,  Thomas Kissel ,  Michael Morlock

发明人： Hans Koll ,  Gerhard Winter ,  Thomas Kissel ,  Michael Morlock

IPC分类号： A61K916

CPC分类号： A61K9/1652 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/1658 ,  A61K38/1816

摘要： The invention concerns parenteral pharmaceutical forms of administration containing polypeptide in the form of microparticles and a process for the production thereof. The microparticles according to the invention contain as a biodegradable polymer an ABA triblock copolymer the A block of which is a copolymer of lactic and glycolic acid and the B block of which represents a polyethylene glycol chain, together with additives that are selected from the group comprising serum proteins, polyamino acids, cyclodextrins, cyclodextrin derivatives, saccharides, amino sugars, amino acids, detergents or carboxylic acids as well as mixtures of these additives. The microparticles according to the invention continuously release the polypeptide over a relatively long time period even when the amounts of polypeptide they include are small or susceptible to aggregation.

摘要翻译： 本发明涉及含有微粒形式的多肽的肠胃外药物给药形式及其生产方法。 根据本发明的微粒包含作为生物可降解聚合物的ABA三嵌段共聚物，其中A嵌段是乳酸和乙醇酸的共聚物，其B嵌段代表聚乙二醇链，以及选自以下的添加剂： 血清蛋白，聚氨基酸，环糊精，环糊精衍生物，糖，氨基糖，氨基酸，去污剂或羧酸，以及这些添加剂的混合物。 根据本发明的微粒在相对长的时间段内连续地释放多肽，即使它们包括的多肽的量很小或易于聚集。

公开(公告)号：US06335037B1

公开(公告)日：2002-01-01

申请号：US09526063

申请日：2000-03-15

申请人： Shoji Ichinohe ,  Muneo Kudo ,  Akira Yamamoto

发明人： Shoji Ichinohe ,  Muneo Kudo ,  Akira Yamamoto

IPC分类号： A61K916

CPC分类号： A61Q15/00 ,  A61K8/025 ,  A61K8/25 ,  A61K9/167 ,  A61K2800/412 ,  A61K2800/612 ,  A61Q1/00 ,  A61Q1/02 ,  A61Q1/10 ,  A61Q19/10

摘要： A cosmetic containing spherical hydrophobic fine silica particles having an average particle diameter of from 0.01 to 5 &mgr;m, having been made more highly hydrophobic, is provided. The spherical hydrophobic fine silica particles have been made hydrophobic on their surfaces by introducing an R2SiO3/2 unit (wherein R2 represents a monovalent hydrocarbon group having 1 to 20 carbon atoms) to the surfaces of hydrophilic fine silica particles having an SiO2 unit, and further have been made more highly hydrophobic on their surfaces by introducing to the surfaces of the hydrophobic fine silica particles first treated an R13SiO1/2 unit (wherein R1's may be the same or different and each represent a monovalent hydrocarbon group having 1 to 6 carbon atoms). The cosmetic containing spherical hydrophobic fine silica particles is a product improved in spreadability and inunctionability.

摘要翻译： 提供了具有更高疏水性的平均粒径为0.01〜5μm的球状疏水性二氧化硅微粒的化妆品。 通过将R2SiO3 / 2单元（其中R2表示碳原子数1〜20的一价烃基）引入具有SiO 2单元的亲水性二氧化硅微粒的表面，使球形疏水性二氧化硅微粒表面疏水化， 通过向首先处理的R 13 SiO 1/2单元（其中R 1可以相同或不同并且各自表示具有1至6个碳原子的一价烃基）的疏水性二氧化硅微粒的表面引入其表面而被制成更高疏水性， 。 含有球形疏水性二氧化硅微粒的化妆品是可扩展性和功能性提高的产品。

公开(公告)号：US06270805B1

公开(公告)日：2001-08-07

申请号：US09187319

申请日：1998-11-06

申请人： Chih-Ming Chen ,  Xiu Xiu Cheng

发明人： Chih-Ming Chen ,  Xiu Xiu Cheng

IPC分类号： A61K916

CPC分类号： A61K9/5078 ,  A61K9/5026 ,  A61K9/5084 ,  A61K31/554 ,  Y10S514/97

摘要： A once-a-day controlled release formulation of a water soluble drug is described which includes: (a) from 20 to 50% by weight of enteric polymeric membrane coated pellets comprising a polymer membrane coated core which comprises a biologically inert core which is coated with a first layer which consists essentially of a water soluble drug and a binder; and a second layer which comprises a membrane comprising a pH dependent polymeric material; and (b) from 50% to 80% by weight of delayed pulse polymeric membrane coated pellets comprising a polymeric membrane coated core which comprises a biologically inert core which is coated with a first layer which consists essentially of a water soluble drug and a binder and a second layer which comprises a polymeric membrane and a alkaline earth metal stearate which will substantially maintain its integrity in the varying pH conditions of the gastrointestinal tract but is permeable to said water soluble drug; and (c) a unit dose containment system.

摘要翻译： 描述了一种每日一次的水溶性药物的控释制剂，其包括：（a）20至50重量％的肠溶性聚合物膜包衣的丸剂，其包含聚合物膜包衣的核心，其包含生物惰性核心，其包被 其具有基本上由水溶性药物和粘合剂组成的第一层; 以及第二层，其包括包含pH依赖性聚合物材料的膜; 和（b）50％至80％重量的延迟脉冲聚合物膜包衣的丸粒，其包含聚合物膜包衣芯，其包含生物学惰性芯，其涂覆有基本上由水溶性药物和粘合剂组成的第一层，以及 第二层，其包含聚合物膜和碱土金属硬脂酸盐，其将在胃肠道的变化的pH条件下基本上保持其完整性，但对所述水溶性药物是可渗透的; 和（c）单位剂量遏制系统。

公开(公告)号：US06264989B1

公开(公告)日：2001-07-24

申请号：US09463327

申请日：2000-01-24

申请人： Hisayoshi Kato ,  Nagayoshi Myo ,  Ikuo Tanai ,  Yusuke Suzuki ,  Toshiro Fujii ,  Yoshitaka Tomoda

发明人： Hisayoshi Kato ,  Nagayoshi Myo ,  Ikuo Tanai ,  Yusuke Suzuki ,  Toshiro Fujii ,  Yoshitaka Tomoda

IPC分类号： A61K916

CPC分类号： B01J2/14 ,  A23L27/70 ,  A23L33/15 ,  A23P10/22 ,  A23V2002/00 ,  A61K9/1688 ,  B01J2/16 ,  A23V2250/708 ,  A23V2250/6422 ,  A23V2200/224 ,  A23V2250/204 ,  A23V2250/1614 ,  A23V2250/1582 ,  A23V2250/6418 ,  A23V2250/51086

摘要： The present invention relates to a process for producing a spherical particle comprising an aggregate of particles containing at least 95% of a water-soluble single substance having a viscosity of 10 mPa.s or less as determined in the form of a saturated aqueous solution, the process comprising: preparing moist spherical particles of the single substance by charging, as cores, crystalline particles or granulated particles of the single substance on a rotary disc in a processing vessel of a centrifugal tumbling granulating apparatus, wherein the granulated particles are prepared by granulating a powder of the single substance, and dispersing over the cores a powder of the single substance and simultaneously spraying on the cores a liquid such as water or the like while supplying slit air to provide a fluidized condition; and then fixation treating the moist spherical particles by drying them while spraying an aqueous solution of the single substance or the like on the spherical particles in a fluidized bed apparatus; to the spherical particle produced by the process; and to a pharmaceutical preparation and a food containing the spherical particle.

摘要翻译： 本发明涉及一种球形颗粒的制造方法，其包含以饱和水溶液的形式测定的含有至少95％的粘度为10mPa·s以下的水溶性单一物质的颗粒聚集体， 该方法包括：通过在离心转鼓造粒装置的处理容器中将旋转盘上的单一物质的核心，结晶颗粒或造粒颗粒作为核心，制备单一物质的湿球形颗粒，其中造粒颗粒通过造粒 将该单一物质的粉末分散在芯体上，并且同时在芯体上喷洒诸如水等的液体，同时在狭缝空气中提供流化条件; 然后在流化床装置中将单一物质等的水溶液喷雾在球形颗粒上的同时，通过干燥固定处理湿球形颗粒; 通过该方法生产的球形颗粒; 以及含有球形颗粒的药物制剂和食品。

公开(公告)号：US06207196B1

公开(公告)日：2001-03-27

申请号：US09405166

申请日：1999-09-24

申请人： Luc Rigal ,  Eric Peyrat ,  Vincent Pluquet ,  Antoine Gaset

发明人： Luc Rigal ,  Eric Peyrat ,  Vincent Pluquet ,  Antoine Gaset

IPC分类号： A61K916

CPC分类号： D21B1/00

摘要： A material formed from plant matter granules has the following size distribution, the percentages being expressed by weight of dry matter: between about 5 and 50% of the granules having a size of less than about 0.25 mm, between about 5 and 40% of the granules having a size of between about 0.25 and 0.5 mm, between about 15 and 60% of the granules having a size of between about 0.5 and 1 mm, between about 1 and 10% of the granules having a size of between about 1 and 1.25 mm, between about 0.5 and 7% of the granules having a size of between about 1.25 and 1.4 mm, between about 1 and 10% of the granules having a size of between about 1.4 and 1.7 mm, between about 0.1 and 10% of the granules having a size of between about 1.7 and 2.36 mm, and between about 0 and 10% of the granules having a size greater than about 2.36 mm.

摘要翻译： 由植物物质颗粒形成的材料具有以下尺寸分布，百分比由干物质的重量表示：约5至50％的颗粒的尺寸小于约0.25mm，约5至40％ 尺寸为约0.25至0.5mm的颗粒，约15至60％的颗粒的尺寸为约0.5至1mm，约1至10％的颗粒的尺寸为约1至1.25 约0.5至7％的颗粒的尺寸为约1.25至1.4mm，约1至10％的颗粒的尺寸为约1.4至1.7mm，约0.1至10％ 尺寸为约1.7至2.36mm的颗粒和约0至10％的具有大于约2.36mm的尺寸的颗粒。