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1.发明授权Topical formulation including diclofenac, or a pharmaceutically acceptable salt thereof 有权包括双氯芬酸或其药学上可接受的盐的局部制剂公开(公告)号：US07795309B2
公开(公告)日：2010-09-14
申请号：US12281561
申请日：2007-03-06
IPC分类号： A61K31/195
CPC分类号： A61K9/0014 , A61K31/196 , A61K45/06 , A61K2300/00
摘要： There is described a topical formulation. The topical formulation comprises: (i) diclofenac or a pharmaceutically acceptable salt thereof, (ii) a first compound, and (iii) a second compound. The first compound and second compound are different, and each is selected from the group consisting essentially of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate. It has been discovered that certain combination of compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of diclofenac or a pharmaceutically acceptable salt thereof. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation.
摘要翻译： 描述了一种局部制剂。 局部制剂包括：（i）双氯芬酸或其药学上可接受的盐，（ii）第一化合物和（iii）第二化合物。 第一化合物和第二化合物是不同的，并且各自选自基本上由N-月桂酰肌氨酸，辛基硫酸钠，月桂酸甲酯，肉豆蔻酸异丙酯，油酸，油酸甘油酯和月桂基磺基乙酸钠组成的组。 已经发现，化合物的某些组合是优异的渗透增强剂，因此，可以掺入局部制剂以促进双氯芬酸或其药学上可接受的盐的给药。 渗透增加的增加也可能导致制剂中皮肤刺激物的总浓度降低。
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公开(公告)号：US08343962B2
公开(公告)日：2013-01-01
申请号：US12848792
申请日：2010-08-02
IPC分类号： A61K31/19 , A61K31/195 , A61K31/40 , A61K31/444 , A61K31/5415
CPC分类号： A61K47/20 , A61K9/2886 , A61K31/19 , A61K31/195 , A61K31/40 , A61K31/444 , A61K31/5415 , A61K47/12 , A61K47/14 , A61K47/16
摘要： It has been discovered that certain combinations compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.
摘要翻译： 已经发现，某些组合化合物是优异的渗透增强剂，因此，可以掺入局部制剂以促进活性剂的给药。 渗透增加的增加也可能导致制剂中皮肤刺激物的总浓度降低。 本文描述了局部制剂，其包含（i）至少一种活性剂; （ii）第一化合物和（iii）第二化合物，其中第一化合物和第二化合物不同，并且各自选自N-月桂酰肌氨酸，辛基硫酸钠，月桂酸甲酯，肉豆蔻酸异丙酯，油酸 酸，油酸甘油酯和月桂基磺基乙酸钠。
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公开(公告)号：US20110028460A1
公开(公告)日：2011-02-03
申请号：US12848792
申请日：2010-08-02
IPC分类号： A61K31/19 , A61K31/195 , A61K31/40 , A61K31/444 , A61K31/5415 , A61P29/00
CPC分类号： A61K47/20 , A61K9/2886 , A61K31/19 , A61K31/195 , A61K31/40 , A61K31/444 , A61K31/5415 , A61K47/12 , A61K47/14 , A61K47/16
摘要： It has been discovered that certain combinations compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first compound, and (iii) a second compound, wherein the first compound and second compound are different, and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate.
摘要翻译： 已经发现，某些组合化合物是优异的渗透增强剂，因此可以掺入局部制剂以促进活性剂的给药。 渗透增加的增加也可能导致制剂中皮肤刺激物的总浓度降低。 本文描述了局部制剂，其包含（i）至少一种活性剂; （ii）第一化合物和（iii）第二化合物，其中第一化合物和第二化合物不同，并且各自选自N-月桂酰肌氨酸，辛基硫酸钠，月桂酸甲酯，肉豆蔻酸异丙酯，油酸 酸，油酸甘油酯和月桂基磺基乙酸钠。
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公开(公告)号：US20100029769A1
公开(公告)日：2010-02-04
申请号：US12281561
申请日：2007-03-06
IPC分类号： A61K31/196 , A61Q19/00 , A61P29/00
CPC分类号： A61K9/0014 , A61K31/196 , A61K45/06 , A61K2300/00
摘要： There is described a topical formulation. The topical formulation comprises: (i) diclofenac or a pharmaceutically acceptable salt thereof, (ii) a first compound, and (iii) a second compound. The first compound and second compound are different, and each is selected from the group consisting essentially of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate. It has been discovered that certain combination of compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of diclofenac or a pharmaceutically acceptable salt thereof. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation.
摘要翻译： 描述了一种局部制剂。 局部制剂包括：（i）双氯芬酸或其药学上可接受的盐，（ii）第一化合物和（iii）第二化合物。 第一化合物和第二化合物是不同的，并且各自选自基本上由N-月桂酰肌氨酸，辛基硫酸钠，月桂酸甲酯，肉豆蔻酸异丙酯，油酸，油酸甘油酯和月桂基磺基乙酸钠组成的组。 已经发现，化合物的某些组合是优异的渗透增强剂，因此，可以掺入局部制剂以促进双氯芬酸或其药学上可接受的盐的给药。 渗透增加的增加也可能导致制剂中皮肤刺激物的总浓度降低。
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公开(公告)号：US20080221212A1
公开(公告)日：2008-09-11
申请号：US11682412
申请日：2007-03-06
IPC分类号： A61K31/195 , A61P17/00 , A61P29/00
CPC分类号： A61K31/195 , A61K9/0014 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/20
摘要： There is described a topical formulation. The topical formulation includes: (i) diclofenac or a pharmaceutically acceptable salt thereof, (ii) a first compound, and (iii) a second compound. The first compound and second compound are different, and each is selected from the group consisting essentially of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate and sodium lauryl sulfoacetate. It has been discovered that certain combination of compounds are excellent penetration enhancers and, as such, can be incorporated in a topical formulation to facilitate administration of diclofenac or a pharmaceutically acceptable salt thereof. The increased penetration enhancement can also lead to a reduction in the total concentration of skin irritants in the formulation.
摘要翻译： 描述了一种局部制剂。 局部制剂包括：（i）双氯芬酸或其药学上可接受的盐，（ii）第一化合物和（iii）第二化合物。 第一化合物和第二化合物是不同的，并且各自选自基本上由N-月桂酰肌氨酸，辛基硫酸钠，月桂酸甲酯，肉豆蔻酸异丙酯，油酸，油酸甘油酯和月桂基磺基乙酸钠组成的组。 已经发现，化合物的某些组合是优异的渗透增强剂，因此，可以掺入局部制剂以促进双氯芬酸或其药学上可接受的盐的给药。 渗透增加的增加也可能导致制剂中皮肤刺激物的总浓度降低。
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6.发明申请公开(公告)号：US20090105260A1
公开(公告)日：2009-04-23
申请号：US11883606
申请日：2006-01-17
申请人： Samir Mitragotri , Pankaj Karande , Amit K. Jain
发明人： Samir Mitragotri , Pankaj Karande , Amit K. Jain
IPC分类号： A61K31/53 , C07D251/26 , C07C43/30 , C07D211/06 , A61K31/445 , A61K31/03 , G06F19/00 , G01N21/25 , A61K31/495 , A61K31/075 , C07D241/04 , C07C17/00
CPC分类号： A61B5/411 , A61B5/0075 , A61B5/445 , G01N21/35 , G16C20/30
摘要： An IR spectroscopic technique provides methods for measuring the irritation potential of a formulation and to assess the ability of molecules to enhance the permeability of substances into and through skin using samples comprising stratum corneum. Molecules are screened for their performance as chemical penetration enhancers using a unique in silico procedure that may be applied iteratively in an attempt to generate molecules showing successively higher performance. Both the irritation potential and the ability of the molecule to enhance penetration are considered in the in silico approach. The invention provides specific molecules that may be used in topical or transdermal formulations to improve the delivery of actives. The structures of compounds of the invention include: Formulas (I), (II), (III), (IV), (V), (IV) and analogs thereof.
摘要翻译： IR光谱技术提供了用于测量制剂的刺激电位的方法，并评估分子通过包含角质层的样品增强物质进入皮肤和通过皮肤的渗透性的能力。 使用独特的计算机程序筛选分子作为化学渗透增强剂的性能，其可以迭代地施用以试图产生显示连续更高性能的分子。 在计算机方法中考虑了刺激潜能和分子增强渗透能力。 本发明提供可用于局部或透皮制剂以改善活性物质递送的特定分子。 本发明化合物的结构包括：式（I），（II），（III），（IV），（V），（IV）及其类似物。
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公开(公告)号：US20070269379A1
公开(公告)日：2007-11-22
申请号：US10560571
申请日：2004-07-21
申请人： Samir Mitragotri , Pankaj Karande , Amit Jain
发明人： Samir Mitragotri , Pankaj Karande , Amit Jain
CPC分类号： G01N33/5082
摘要： A high throughput screening and isolation system identifies rare enhancer mixtures from a candidate pool of penetration enhancer combinations. The combinations are screened for high penetration but low irritation potential using a unique data mining method to find new potent and safe chemical penetration enhancer combinations. The members of a library of chemical penetration enhancer combinations are screened with a high throughput device to identify “hot spots”, particular combinations that show higher chemical penetration enhancement compared to neighboring compositions. The irritation potentials of the hot spot combinations are measured to identify combinations that also show low irritation potential. A active component, such as a drug, is then combined with the combination in a formulation which is tested for the ability of the drug to penetrate into or through skin. It is then assessed whether the formulation can deliver the quantity of drug required, and animal tests are conducted to confirm in vivo the ability of the chemical penetration enhancer combinations to facilitate transport of sufficient active molecules across the skin to achieve therapeutic levels of the active molecule in the animal's blood. The invention provides specific unique and rare mixtures of chemical penetration enhancers that enhance skin permeability to hydrophilic macromolecules by more than 50-fold without inducing skin irritation, such as combinations of sodium laurel ether sulfate and 1-phenyl piperazine, and combinations of N-lauryl sarcosine and Span 20/sorbitan monolaurate.
摘要翻译： 高通量筛选和分离系统识别来自渗透促进剂组合的候选库的稀有增强剂混合物。 使用独特的数据挖掘方法筛选出高渗透性和低刺激潜力的组合，以发现新的有效和安全的化学渗透增强剂组合。 化学渗透增强剂组合库的成员用高通量装置进行筛选以鉴定“热点”，与相邻组合物相比显示出更高的化学渗透增强的特定组合。 测量热点组合的刺激电位以识别也显示低刺激潜能的组合。 然后将活性成分（例如药物）与组合物组合在一种制剂中，该制剂被测试药物穿透或穿过皮肤的能力。 然后评估制剂是否可以递送所需药物的量，并进行动物试验以确认体内化学渗透增强剂组合的能力，以促进足够的活性分子穿过皮肤的转运，以达到治疗水平的活性分子 在动物的血液中。 本发明提供了特异的独特稀有的化学渗透增强剂混合物，其增强了亲水性大分子的皮肤渗透性超过50倍而不诱导皮肤刺激，例如月桂醚硫酸钠和1-苯基哌嗪钠的组合，以及N-月桂基 肌氨酸和Span 20 /脱水山梨醇单月桂酸酯。
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公开(公告)号：US20050181029A1
公开(公告)日：2005-08-18
申请号：US10782155
申请日：2004-02-18
申请人： Samir Mitragotri , Pankaj Karande
发明人： Samir Mitragotri , Pankaj Karande
IPC分类号： A61K9/70
CPC分类号： A61K9/7084 , A61K9/7092
摘要： A transdermal drug delivery patch with an array of spatially organized reservoirs. The invention provides greater penetration of drug into the skin compared to current transdermal drug delivery systems, and facilitates the delivery of drugs that are presently refractory to transdermal delivery due to high molecular weight.
摘要翻译： 具有阵列空间有组织的储库的透皮药物递送贴片。 与目前的透皮药物递送系统相比，本发明提供了药物进入皮肤的更大的渗透性，并且由于高分子量而促进了目前难于透皮递送的药物的递送。
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公开(公告)号：US10246489B2
公开(公告)日：2019-04-02
申请号：US15446253
申请日：2017-03-01
申请人： Jeffrey D. Rimer , Pankaj Karande
发明人： Jeffrey D. Rimer , Pankaj Karande
摘要： In an embodiment, the present disclosure pertains to a composition for inhibiting calcium oxalate monohydrate crystal growth comprising at least one isolated polypeptide comprising a plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal; and a plurality of amino acids spacers, wherein the amino acid spacers are arranged in varying sequences between the plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal. In some embodiments, the present disclosure related to a method of controlling calcium oxalate monohydrate crystal growth in a subject in need thereof comprising administering to the subject therapeutically effective amount of the calcium oxalate monohydrate inhibiting polypeptide. In some embodiments, the present disclosure relates to a method of identifying calcium oxalate monohydrate inhibiting peptides. Such a method may comprise designing a peptide library of potential calcium oxalate inhibiting peptides; screening the peptide library for high efficacy inhibitor peptides for inhibition of calcium oxalate monohydrate crystallization; and conducting molecular characterization of the high efficacy inhibitor to determine specificity.
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公开(公告)号：US09617306B2
公开(公告)日：2017-04-11
申请号：US14326908
申请日：2014-07-09
申请人： Jeffrey D. Rimer , Pankaj Karande
发明人： Jeffrey D. Rimer , Pankaj Karande
CPC分类号： C07K7/08 , A61K38/00 , G01N33/53 , G01N33/6893 , G01N2500/04 , G01N2500/20 , G01N2800/345
摘要： In an embodiment, the present disclosure pertains to a composition for inhibiting calcium oxalate monohydrate crystal growth comprising at least one isolated polypeptide comprising a plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal; and a plurality of amino acids spacers, wherein the amino acid spacers are arranged in varying sequences between the plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal. In some embodiments, the present disclosure related to a method of controlling calcium oxalate monohydrate crystal growth in a subject in need thereof comprising administering to the subject therapeutically effective amount of the calcium oxalate monohydrate inhibiting polypeptide. In some embodiments, the present disclosure relates to a method of identifying calcium oxalate monohydrate inhibiting peptides. Such a method may comprise designing a peptide library of potential calcium oxalate inhibiting peptides; screening the peptide library for high efficacy inhibitor peptides for inhibition of calcium oxalate monohydrate crystallization; and conducting molecular characterization of the high efficacy inhibitor to determine specificity.
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