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1. 发明授权

US06749867B2 Delivery system for omeprazole and its salts 失效
标题翻译：奥美拉唑及其盐的输送系统
公开(公告)号：US06749867B2
公开(公告)日：2004-06-15
申请号：US09991059
申请日：2001-11-21
申请人： Joseph R. Robinson , James W. McGinity
发明人： Joseph R. Robinson , James W. McGinity
IPC分类号： A61K914
CPC分类号： A61K31/4439 , A61K9/2009 , A61K9/2054 , A61K9/282 , A61K9/2846 , A61K9/2866
摘要： The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.
摘要翻译：本发明提供了用于将酸不稳定药物（例如奥美拉唑）输送到胃下游胃肠道上部的时间释放剂型。剂型包括由惰性时间释放涂层包围的药物核心，其延迟药物从核心释放直到给药后一定时间段通常为0.5-5.0小时或1-3小时。当胃肠液接触核心时，药物迅速释放到胃肠道。剂型不含肠溶衣。剂型还可以包括一个或多个在时间释放涂层外部的附加涂层，以提供立即释放的负载剂量的酸不稳定药物或另一种药物的递送。

2. 发明授权

US6071539A Effervescent granules and methods for their preparation 失效
标题翻译：泡腾颗粒及其制备方法
公开(公告)号：US6071539A
公开(公告)日：2000-06-06
申请号：US934109
申请日：1997-09-19
申请人： Joseph R. Robinson , James W. McGinity
发明人： Joseph R. Robinson , James W. McGinity
IPC分类号： A61K9/00 , A61K9/16 , A61K9/46 , A61K9/20
CPC分类号： A61K9/1641 , A61K9/0007 , A61K9/0034 , A61K9/1694
摘要： According to the present invent, effervescent granules having a controllable rate of effervescence are provided. Such granules comprise an acidic agent, an alkaline agent, a hot-melt extrudable binder capable of forming a eutectic mixture with the acidic agent and, optionally, a plasticizer. The effervescent granules are made by a hot-melt extrusion process.
摘要翻译：根据本发明，提供了具有可控的泡腾速率的泡腾颗粒。这种颗粒包括酸性剂，碱性试剂，能够与酸性试剂形成共晶混合物的热熔可挤出粘合剂和任选的增塑剂。泡腾颗粒通过热熔挤出方法制成。

3. 发明授权

US08802130B2 Sublingual buccal effervescent 有权
标题翻译：舌下颊泡腾
公开(公告)号：US08802130B2
公开(公告)日：2014-08-12
申请号：US11511098
申请日：2006-08-28
申请人： S. Indiran Pather , Rajendra K. Khankari , Jonathan D. Eichman , Joseph R. Robinson , John Hontz
发明人： S. Indiran Pather , Rajendra K. Khankari , Jonathan D. Eichman , Joseph R. Robinson , John Hontz
IPC分类号： A61F13/00
CPC分类号： A61K9/0007 , A61K9/0056 , A61K9/006 , A61K31/4468 , A61K31/5415
摘要： A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administrable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.
摘要翻译：一种药物剂型，其适于向口腔中提供药物的口腔，舌下或牙龈吸收，所述药物包含与可用于促进所述药物在口腔中的吸收的泡腾剂相结合的可口服给药的药物。还公开了与泡腾剂结合使用另外的pH调节物质以促进吸收药物。

4. 发明申请

US20110223115A1 SUBLINGUAL BUCCAL EFFERVESCENT 有权
标题翻译：次级效应
公开(公告)号：US20110223115A1
公开(公告)日：2011-09-15
申请号：US13099003
申请日：2011-05-02
申请人： Sathasivan Indiran Pather , Rajendra K. Khankari , Jonathan D. Eichman , Joseph R. Robinson , John Hontz
发明人： Sathasivan Indiran Pather , Rajendra K. Khankari , Jonathan D. Eichman , Joseph R. Robinson , John Hontz
IPC分类号： A61K9/10
CPC分类号： A61K31/4468 , A61K9/0007 , A61K9/0056 , A61K9/006 , A61K31/5415
摘要： A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administrable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.
摘要翻译：一种药物剂型，其适于向口腔中提供药物的口腔，舌下或牙龈吸收，所述药物含有与用于促进口腔中的药物吸收的泡腾剂相结合的可口服给药的药物。还公开了使用额外的pH调节物质与泡腾剂组合以促进吸收药物。

5. 发明授权

US06641838B2 Effervescent drug delivery system for oral administration 有权
公开(公告)号：US06641838B2
公开(公告)日：2003-11-04
申请号：US10021109
申请日：2001-10-29
申请人： S. Indiran Pather , Joseph R. Robinson , Jonathan D. Eichman , Rajendra K. Khankari , John Hontz , Sangeeta V. Gupte
发明人： S. Indiran Pather , Joseph R. Robinson , Jonathan D. Eichman , Rajendra K. Khankari , John Hontz , Sangeeta V. Gupte
IPC分类号： A61K928
CPC分类号： A61K9/2886 , A61K9/0007 , A61K9/2072 , A61K9/2866 , A61K9/5084 , Y10S514/96
摘要： The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

6. 发明授权

US4983392A Bioadhesive compositions and methods of treatment therewith 失效
标题翻译：生物粘合剂组合物及其处理方法
公开(公告)号：US4983392A
公开(公告)日：1991-01-08
申请号：US287464
申请日：1988-12-20
申请人： Joseph R. Robinson
发明人： Joseph R. Robinson
IPC分类号： A61K9/22 , A61K9/50 , A61K9/70
CPC分类号： A61K9/0048 , A61K9/0065 , A61K9/4808 , A61K9/5026 , A61K9/7007
摘要： A controlled release treatment composition and method of use are disclosed. The composition includes a bioadhesive and an effective amount of a treating agent. The bioadhesive is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether.
摘要翻译：公开了一种控释组合物和使用方法。组合物包括生物粘合剂和有效量的处理剂。生物粘合剂是水溶胀性但水不溶性的纤维状交联羧基官能聚合物，其含有（a）多个重复单元，其至少约80％含有至少一个羧基官能团，和（b）约 0.05至约1.5％的交联剂基本上不含聚烯基聚醚。

7. 发明授权

US06649186B1 Effervescent granules and methods for their preparation 有权
公开(公告)号：US06649186B1
公开(公告)日：2003-11-18
申请号：US09553528
申请日：2000-04-20
申请人： Joseph R. Robinson , James William McGinity , Pascal Delmas
发明人： Joseph R. Robinson , James William McGinity , Pascal Delmas
IPC分类号： A61K946
CPC分类号： A61K9/0056 , A61K9/0007 , A61K9/0034 , A61K9/1694 , A61K9/2095
摘要： Disclosed here are effervescent granules having a controllable rate of effervescence. In some embodiments, the such granules comprise an acidic agent, an alkaline agent, a pharmacologically active agent, hot-melt extrudable binder capable of forming a eutectic mixture with the acidic agent and, optionally, a plasticizer. The effervescent granules are made by a hot-melt extrusion process. The present invention also provides a thermal heat process for preparing a pharmacologically active agent containing effervescent granule. In certain aspects, the granules contain pharmacologically active agents such as narcotics, antidiarrheal agents, antiviral agents, anxiolytic agents, a cholesterol lowering agent, an alpha adrenergic blocking agent, a phenanthrene derivative. By way of example, some of the narcotics that may be included in the granules and in the process of preparing the granules include, by way of example: phenanthrene derivatives (e.g., morphine sulfate), and morphine derivatives (e.g., hydromorphone hydrochloride).

8. 发明授权

US06200604B1 Sublingual buccal effervescent 有权
标题翻译：舌下颊泡腾
公开(公告)号：US06200604B1
公开(公告)日：2001-03-13
申请号：US09327814
申请日：1999-06-08
申请人： Sathasivan Indiran Pather , Rajendra K. Khankari , Jonathan D. Eichman , Joseph R. Robinson , John Hontz
发明人： Sathasivan Indiran Pather , Rajendra K. Khankari , Jonathan D. Eichman , Joseph R. Robinson , John Hontz
IPC分类号： A61K946
CPC分类号： A61K31/5415 , A61K9/0007 , A61K9/0056 , A61K9/006 , A61K31/4468
摘要： A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administerable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.
摘要翻译：一种药物剂型，其适于向口腔中提供药物的颊，舌下或牙龈吸收，所述药物包含与用于促进药物在口腔中吸收的口腔可药用组合泡腾剂。还公开了与泡腾剂结合使用另外的pH调节物质以促进吸收药物。

9. 发明授权

US5192535A Ophthalmic suspensions 失效
标题翻译：眼科悬浮液
公开(公告)号：US5192535A
公开(公告)日：1993-03-09
申请号：US544518
申请日：1990-06-27
申请人： Jeffrey P. Davis , Santosh K. Chandrasekaran , Yansheng Su , Roy D. Archibald , Joseph R. Robinson
发明人： Jeffrey P. Davis , Santosh K. Chandrasekaran , Yansheng Su , Roy D. Archibald , Joseph R. Robinson
IPC分类号： A61K9/107 , A61F2/14 , A61K9/00 , A61K9/64 , A61K9/70 , A61K31/765 , A61K47/32
CPC分类号： A61K9/0048 , Y10S514/912 , Y10S514/913 , Y10S514/914 , Y10S514/915 , Y10S514/944 , Y10S514/953 , Y10S514/954
摘要： Lightly crosslinked polymers, preferably ones prepared by suspension or emulsion polymerizing at least about 90% by weight of a carboxyl-containing monoethylenically unsaturated monomer such as acrylic acid with from about 0.1% to about 5% by weight of a polyfunctional, and preferably difunctional, crosslinking agent such as divinyl glycol (3,4-dihydroxy-1,5-hexadiene), having a particle size of not more than about 50 .mu.m in equivalent spherical diameter, when formulated with an ophthalmic medicament, e.g., fluorometholone, into suspensions in aqueous medium in which the amount of polymer ranges from about 0.1% to about 6.5% by weight, based on the total weight of the aqueous suspension, the pH is from about 3.0 to about 6.5, and the osmotic pressure (osmolality or tonicity) is from about 10 mOsM to about 400 mOsM, provide new topical ophthalmic medicament delivery systems having suitably low viscosities which permit them to be easily administered to the eye in drop form, and hence be comfortably administrable in consistent, accurate dosages. These suspension will rapidly gel in the eye after coming into contact with the eye's tear fluid to a substantially greater viscosity than that of the originally-introduced suspension and thus remain in place for prolonged periods of time to provide sustained release of the ophthalmic medicament.
摘要翻译：轻度交联的聚合物，优选通过悬浮或乳液聚合至少约90重量％的含羧基的单烯属不饱和单体如丙烯酸与约0.1重量％至约5重量％的多官能，优选双官能的，当与眼科药物（例如氟米龙）一起配制成悬浮液时，具有当量球形直径不大于约50μm的粒度的二乙烯基二醇（3,4-二羟基-1,5-己二烯）等交联剂在水性介质中，其中聚合物的量为约0.1％至约6.5％（重量），基于水性悬浮液的总重量，pH为约3.0至约6.5，渗透压（渗透压或渗透压）提供了约10mOsM至约400mOsM的新型局部眼科药物递送系统，其具有适当的低粘度，使得它们能够以滴剂形式容易地施用于眼睛，因此是以一致，准确的剂量舒适地管理。在与眼睛的泪液接触之后，这些悬浮液将在眼睛中快速凝胶至比最初引入的悬浮液的粘度显着更大的粘度，并因此保持在适当位置以延长时间以提供眼药物的持续释放。

10. 发明授权

US4992280A Sustained flavorant release composition, method for making same and chewable structure incorporating same 失效
标题翻译：持续的调味剂释放组合物，其制备方法和掺入其的咀嚼结构
公开(公告)号：US4992280A
公开(公告)日：1991-02-12
申请号：US452214
申请日：1989-12-18
申请人： Anita W. Yung Chu , Joseph R. Robinson
发明人： Anita W. Yung Chu , Joseph R. Robinson
IPC分类号： A23G4/00 , A23G4/04 , A23G4/06 , A23G4/10 , A23G4/20 , A23L27/00 , A61K9/68 , A61K47/32
CPC分类号： A23G4/06 , A23G4/043 , A23G4/10 , A23G4/20 , A23L27/74
摘要： A sustained flavorant release composition is provided for use in a chewable structure. The flavorant release composition consists essentially of a homogenous dispersion of a liquid flavorant agent and polyvinyl acetate having a number average molecular weight of about 150,000 to about 200,000 daltons. The weight ratio of the liquid favorant agent to polyvinyl acetate is about 1:5 to about 5:1, respectively. A method of producing the flavorant release composition includes admixing the polyvinyl acetate, dissolved in a volatile, nonreactive organic solvent, with the flavorant release agent at a temperature at which the flavorant release agent does not degrade. The solvent is then removed. The chewable structure includes the flavorant release composition and a gum base composition.
摘要翻译：提供持久的调味剂释放组合物用于可咀嚼结构。调味剂释放组合物基本上由数均分子量为约150,000至约200,000道尔顿的液体食用香料剂和聚乙酸乙烯酯的均匀分散体组成。液体助剂与聚乙酸乙烯酯的重量比分别为约1:5至约5:1。制备调味剂释放组合物的方法包括在调味剂脱模剂不降解的温度下将溶于挥发性非反应性有机溶剂的聚乙酸乙烯酯与调味剂脱模剂混合。然后除去溶剂。咀嚼结构包括调味剂释放组合物和胶基组合物。

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