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81. 发明授权

US06287540B1 Formulation for inhalation 有权
标题翻译：吸入制剂
公开(公告)号：US06287540B1
公开(公告)日：2001-09-11
申请号：US09431916
申请日：1999-11-02
申请人： Jan Trofast
发明人： Jan Trofast
IPC分类号： A61K914
CPC分类号： A61K9/0075 , A61K9/145 , A61K31/137 , A61K31/167 , A61K31/58 , A61K45/06 , Y10S514/826 , A61K31/165 , A61K2300/00
摘要： A dry powder composition comprising one more potent pharmaceutically active substances and a carrier substance, all of which are in finely divided form, wherein the formulation has a poured bulk density of from 0.28 to 0.38 g/ml is useful in the treatment of respiratory disorders.
摘要翻译：一种干粉组合物，其包含一种更有效的药物活性物质和载体物质，所有这些物质均为细碎形式，其中该制剂具有0.28至0.38g / ml的倾倒堆积密度可用于治疗呼吸系统疾病。

82. 发明授权

US06284282B1 Method of spray freeze drying proteins for pharmaceutical administration 有权
标题翻译：喷雾冷冻干燥蛋白质用于药物施用的方法
公开(公告)号：US06284282B1
公开(公告)日：2001-09-04
申请号：US09299377
申请日：1999-04-27
申请人： Yuh-Fun Maa , Phuong-Anh Nguyen
发明人： Yuh-Fun Maa , Phuong-Anh Nguyen
IPC分类号： A61K914
CPC分类号： A61K9/0075 , A61K9/19 , A61K38/30
摘要： The present invention relates to the spray freeze dry preparation of dry powder formulations of therapeutic proteins suitable for administration via pulmonary delivery.
摘要翻译：本发明涉及适用于通过肺部给药施用的治疗性蛋白质的干粉制剂的喷雾冷冻干燥制剂。

83. 发明授权

US06261602B1 Pharmaceutical composition for rapid suspension in aqueous media 有权
标题翻译：用于在水性介质中快速悬浮的药物组合物
公开(公告)号：US06261602B1
公开(公告)日：2001-07-17
申请号：US09297213
申请日：1999-09-21
申请人： Massimo Maria Calanchi , Marco Giuseppe Raffaele Marconi , Luigi Giovanni Mapelli
发明人： Massimo Maria Calanchi , Marco Giuseppe Raffaele Marconi , Luigi Giovanni Mapelli
IPC分类号： A61K914
CPC分类号： A61K9/0095 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5073 , A61K47/36 , A61K47/38
摘要： The invention provides a granular product useful as a pharmaceutical carrier which can be used for the preparation of pharmaceutical compositions that are capable of rapid suspension in water or aqueous media including saliva. The compositions may be used by addition to a glass of water with stirring or taken directly in the mouth. The granular product may be prepared by a process which comprises subjecting a mixture of a thickening agent and a disintegrating agent to wet granulation with an aqueous medium as wetting agent or dry granulation and preparing the pharmaceutical composition from the granular product and the pharmaceutically active ingredient. A water-soluble inert excipient, which may be a sugar, may be mixed with the granular product prior to mixing with the pharmaceutically active ingredient.
摘要翻译：本发明提供了可用作药物载体的颗粒产品，其可用于制备能够在包含唾液的水或含水介质中快速悬浮的药物组合物。组合物可以通过在搅拌下加入一杯水或直接在口中使用。粒状产物可以通过包括使增稠剂和崩解剂的混合物用水性介质湿润造粒作为润湿剂或干法制粒的方法制备，并从颗粒状产品和药物活性成分制备药物组合物。在与药物活性成分混合之前，可将水溶性惰性赋形剂（其可以是糖）与颗粒产物混合。

84. 发明授权

US06242008B1 Spherical pharmaceutical granules comprising microcrystalline cellulose and a process for their production 失效
标题翻译：包含微晶纤维素的球形药物颗粒及其生产方法
公开(公告)号：US06242008B1
公开(公告)日：2001-06-05
申请号：US09029948
申请日：1998-07-07
申请人： Hidero Akiyama , Zene Matsumoto , Takashi Ueno
发明人： Hidero Akiyama , Zene Matsumoto , Takashi Ueno
IPC分类号： A61K914
CPC分类号： A61K9/1652 , A61K9/1694 , Y10S514/951
摘要： A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients comprising at least 5% crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution; a substantially spherical granule for pharmaceutical use comprising famciclovir and 5% or more crystalline cellulose, together with an optional coating; and a sachet containing a unit dose of famciclovir in the form of such granules.
摘要翻译：一种高速搅拌造粒机，其制备用于药物用途的基本上为球形的颗粒，其包含用于药物用途的药物，其中所述药物的水溶解度为0.01至0.30g / ml，所述方法包括引入药物和赋形剂的混合物，其至少包含将5％结晶纤维素加入造粒机中，喷洒在水或乙醇和水的混合物作为粘合剂溶液; 用于药物用途的基本上为球形的颗粒，包括泛昔洛韦和5％或更多结晶纤维素，以及任选的涂层; 和含有这种颗粒形式的泛昔洛韦单位剂量的小袋。

85. 发明授权

US06242006B1 &bgr;-lactam granules free of organic solvents 失效
标题翻译：不含有机溶剂的β-内酰胺颗粒
公开(公告)号：US06242006B1
公开(公告)日：2001-06-05
申请号：US09214245
申请日：1998-12-24
申请人： Gerard Jan Kwant , Nicolaas Henricus Scheffers
发明人： Gerard Jan Kwant , Nicolaas Henricus Scheffers
IPC分类号： A61K914
CPC分类号： A61K9/1688 , A61K31/43
摘要： &bgr;-Lactam granules free of organic solvents have been provided for. Also a process to prepare the same by applying during the granulation only water as binding solvent has been disclosed.
摘要翻译：已经提供了不含有机溶剂的β-内酰胺颗粒。另外，通过在造粒期间施用只制备作为结合溶剂的水的方法也已公开。

86. 发明授权

US06242005B1 Absorbable prophylactic composition for protection against ionizing or non-ionizing electromagnetic waves 失效
标题翻译：用于防止电离或非电离电磁波的可吸收预防组合物
公开(公告)号：US06242005B1
公开(公告)日：2001-06-05
申请号：US09051507
申请日：1998-09-28
申请人： Charles Legrand , Rachid Bouhamidi
发明人： Charles Legrand , Rachid Bouhamidi
IPC分类号： A61K914
CPC分类号： A61Q17/04 , A61K8/97 , A61K36/87 , A61K2300/00
摘要： An absorbable prophylactic composition for protecting against ionizing or nonionizing electromagnetic waves. The composition is derived from a crude extract of residual fractions of crushed grapes, and primarily from solid material comprising pips, stalks and skins of grapes and/or combinations thereof. The crude extract is obtained by first pulverizing the fraction or fractions from the grapes to form a powder, and then subjecting the powder to at least two extraction processes, one with acetone and the other with ethyl acetate. The extract is then ingested in doses between about 20 mg to 3 g for an adult male. Tests have demonstrated the efficacy of this composition against changes induced by ionizing radiation (x-rays) and nonionizing radiation (UV-C).
摘要翻译：一种用于防止电离或非电离电磁波的可吸收预防组合物。组合物衍生自粗碎的葡萄残留部分的粗提取物，主要来自包含荚，茎和葡萄皮和/或其组合的固体材料。通过首先粉碎来自葡萄的级分或级分以形成粉末，然后使粉末至少两次萃取过程，一次用丙酮，另一次用乙酸乙酯进行，得到粗提物。然后，对于成年男性，提取物以约20mg至3g的剂量摄取。测试已经证明了该组合物对电离辐射（x射线）和非离子化辐射（UV-C）诱导的变化的功效。

87. 发明授权

US06235313B1 Bioadhesive microspheres and their use as drug delivery and imaging systems 失效
公开(公告)号：US06235313B1
公开(公告)日：2001-05-22
申请号：US08824172
申请日：1997-03-26
申请人： Edith Mathiowitz , Donald Chickering, III , Jules S. Jacob
发明人： Edith Mathiowitz , Donald Chickering, III , Jules S. Jacob
IPC分类号： A61K914
CPC分类号： A61K9/1641 , A61K9/167 , Y10S514/962 , Y10S977/906 , Y10S977/915 , Y10S977/928
摘要： Bioadhesive polymers in the form of, or as a coating on, microcapsules containing drugs or bioactive substances which may serve for therapeutic, or diagnostic purposes in diseases of the gastrointestinal tract, are described. The polymeric microspheres all have a bioadhesive force of at least 11 mN/cm2 (110 N/m2). Techniques for the fabrication of bioadhesive microspheres, as well as a method for measuring bioadhesive forces between microspheres and selected segments of the gastrointestinal tract in vitro are also described. This quantitative method provides a means to establish a correlation between the chemical nature, the surface morphology and the dimensions of drug-loaded microspheres on one hand and bioadhesive forces on the other, allowing the screening of the most promising materials from a relatively large group of natural and synthetic polymers which, from theoretical consideration, should be used for making bioadhesive microspheres.

88. 发明授权

US06228400B1 Orally administered pharmaceutical formulations of benzimidazole derivatives and the method of preparing the same 失效
标题翻译：口服给药苯并咪唑衍生物的药物制剂及其制备方法
公开(公告)号：US06228400B1
公开(公告)日：2001-05-08
申请号：US09488406
申请日：2000-01-19
申请人： Fang-Yu Lee , Shan-chiung Chen , Han-Chiang Kuo
发明人： Fang-Yu Lee , Shan-chiung Chen , Han-Chiang Kuo
IPC分类号： A61K914
CPC分类号： A61K9/5078 , A61K31/4439
摘要： The present invention provides pharmaceutical formulations which contain (a) an inert core of sugar, sugar and starch, or microcrystalline cellulose, (b) a drug emulsion layer which is made from mixing a free base of benzimidazole derivative (such as omeprazole or lansoprazole) with a nonionic surfactant and water, (c) a protective coating which is made of a film-forming compound, and optionally a plasticizer or excipient, and (d) an enteric coating which is made of a pharmaceutically acceptable polymer and a plasticizer. Optionally, a basic amino acid can be added to the drug emulsion layer or the protective coating. The present invention also provides the method for making the pharmaceutical formulations.
摘要翻译：本发明提供了含有（a）糖，糖和淀粉或微晶纤维素的惰性核心的药物制剂，（b）由苯并咪唑衍生物（如奥美拉唑或兰索拉唑）的游离碱混合制成的药物乳剂层，非离子表面活性剂和水，（c）由成膜化合物和任选的增塑剂或赋形剂制成的保护涂层，和（d）由药学上可接受的聚合物和增塑剂制成的肠溶衣。任选地，可将碱性氨基酸加入到药物乳剂层或保护性涂层中。本发明还提供了制备药物制剂的方法。

89. 发明授权

US06214383B1 Precipitated silicas which contain an active substance 失效
标题翻译：含有活性物质的沉淀二氧化硅
公开(公告)号：US06214383B1
公开(公告)日：2001-04-10
申请号：US09208453
申请日：1998-12-10
申请人： Heinz Esch , Robert Kuhlmann , Matthias Neumüller , Karin Otto , Ralf Rausch , Klaus-Peter Thomas
发明人： Heinz Esch , Robert Kuhlmann , Matthias Neumüller , Karin Otto , Ralf Rausch , Klaus-Peter Thomas
IPC分类号： A61K914
CPC分类号： A61Q11/00 , A61K8/25
摘要： A precipitated silica which contains an active substance with a characteristic, delayed release of active substance is prepared by adding the active substance during preparation of the precipitated silica. The precipitated silica containing the active substance may be added to oral hygiene agents such as toothpastes, topical fluoride preparations, dental materials or medicinal chewing gums.
摘要翻译：通过在沉淀二氧化硅的制备过程中加入活性物质制备含有具有特征的活性物质延迟释放的活性物质的沉淀二氧化硅。含有活性物质的沉淀二氧化硅可以添加到口腔卫生剂如牙膏，局部氟化物制剂，牙科材料或药用口香糖中。

90. 发明授权

US06214379B1 Maximizing effectiveness of substances used to improve health and well being 有权
标题翻译：最大限度地提高用于改善健康和福祉的物质的有效性
公开(公告)号：US06214379B1
公开(公告)日：2001-04-10
申请号：US09323158
申请日：1999-06-01
申请人： Victor M. Hermelin
发明人： Victor M. Hermelin
IPC分类号： A61K914
CPC分类号： A61K31/714 , A61K31/277 , A61K31/4164 , A61K31/4458 , A61K31/517 , A61K31/549 , A61K31/5513 , Y10S514/937
摘要： The present disclosure relates to novel dosage forms, drug delivery regimens, methods and pharmaceutical compositions which optimize the therapeutic effects of active therapeutic substances through the application of the concept of uneven dosing.
摘要翻译：本公开涉及通过应用不均匀给药的概念来优化活性治疗物质的治疗效果的新型剂型，药物递送方案，方法和药物组合物。

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