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1. 发明申请

WO2010083035A3 TRANSDERMAL ADMINISTRATION OF TAMSULOSIN 审中-公开
公开(公告)号：WO2010083035A3
公开(公告)日：2010-07-22
申请号：PCT/US2010/000081
申请日：2010-01-14
申请人： CORIUM INTERNATIONAL, INC. , SINGH, Parminder , LEE, Eun, Soo , JAIN, Amit, K.
发明人： SINGH, Parminder , LEE, Eun, Soo , JAIN, Amit, K.
IPC分类号： A61K9/70 , A61K31/18 , A61K31/137 , A61K47/06
摘要： In an aspect of the invention, a composition for making a patch for the transdermal delivery of tamsulosin is provided. The composition comprises (a) at least about 1 wt% tamsulosin or a pharmaceutically acceptable salt of tamsulosin, (b) at least about 40 wt% polyisobutylene adhesive or hydrophobic synthetic rubber adhesive, (c) about 1 -20 wt% of an aprotic solvent in which tamsulosin dissolves readily, (d) about 1-20 wt% of an unsaturated fatty acid or an alpha-hydroxy acid or a mixture of unsaturated fatty acids or alpha-hydroxy acids or of both unsaturated fatty acids and alpha-hydroxy acids, (e) a lipophilic permeation enhancer, and (f) a matrix modifier.

2. 发明申请

WO2006091297A2 MOLECULES TO ENHANCE PERCUTANEOUS DELIVERY AND METHODS FOR DISCOVERY THEREFOR 审中-公开
标题翻译：分析加强PERCUTANEOUS交付及其发现方法
公开(公告)号：WO2006091297A2
公开(公告)日：2006-08-31
申请号：PCT/US2006001964
申请日：2006-01-17
申请人： UNIV CALIFORNIA , MITRAGOTRI SAMIR , KARANDE PANKAJ , JAIN AMIT K
发明人： MITRAGOTRI SAMIR , KARANDE PANKAJ , JAIN AMIT K
IPC分类号： G06F19/00
CPC分类号： A61B5/411 , A61B5/0075 , A61B5/445 , G01N21/35 , G06F19/704
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。

3. 发明申请

WO2005009510A3 PENETRATION ENHANCER COMBINATIONS FOR TRANSDERMAL DELIVERY 审中-公开
标题翻译：穿透增强器组合用于透皮递送
公开(公告)号：WO2005009510A3
公开(公告)日：2005-04-07
申请号：PCT/US2004023634
申请日：2004-07-21
申请人： UNIV CALIFORNIA , MITRAGOTRI SAMIR , KARANDE PANKAJ , JAIN AMIT K
发明人： MITRAGOTRI SAMIR , KARANDE PANKAJ , JAIN AMIT K
IPC分类号： A61K31/00 , A61M20060101 , G01N33/53 , G01N33/543
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从候选渗透促进剂组合中识别稀有增强剂混合物。使用独特的数据挖掘方法来筛选高渗透性但低刺激性的组合，以找到新的有效和安全的化学渗透增强剂组合。用高通量装置筛选化学渗透增强剂组合库的成员以鉴定“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潜能以鉴定也显示低刺激潜力的组合。然后将活性成分如药物与所述组合在制剂中组合，所述制剂经测试药物渗入或穿过皮肤的能力。然后评估制剂是否可以递送所需药物的量，并且进行动物试验以确认体内化学渗透促进剂组合的促进足够活性分子穿过皮肤的运输以实现治疗水平的活性分子的能力在动物的血液中。本发明提供化学渗透促进剂的特定独特和稀有混合物，其增强皮肤对亲水性大分子的渗透性超过50倍而不诱导皮肤刺激，例如月桂基醚硫酸钠和1-苯基哌嗪的组合，以及N-月桂基肌氨酸和司盘20 /失水山梨糖醇单月桂酸酯。

4. 发明申请

WO2010083035A2 TRANSDERMAL ADMINISTRATION OF TAMSULOSIN 审中-公开
标题翻译：透皮给药TAMSULOSIN
公开(公告)号：WO2010083035A2
公开(公告)日：2010-07-22
申请号：PCT/US2010000081
申请日：2010-01-14
申请人： CORIUM INT INC , SINGH PARMINDER , LEE EUN SOO , JAIN AMIT K
发明人： SINGH PARMINDER , LEE EUN SOO , JAIN AMIT K
IPC分类号： A61K9/70 , A61K31/137 , A61K31/18 , A61K47/06
CPC分类号： A61K9/70 , A61K9/0014 , A61K9/7023 , A61K9/7053 , A61K31/137 , A61K31/18 , A61K47/02 , A61K47/12 , A61K47/14
摘要： In an aspect of the invention, a composition for making a patch for the transdermal delivery of tamsulosin is provided. The composition comprises (a) at least about 1 wt% tamsulosin or a pharmaceutically acceptable salt of tamsulosin, (b) at least about 40 wt% polyisobutylene adhesive or hydrophobic synthetic rubber adhesive, (c) about 1 -20 wt% of an aprotic solvent in which tamsulosin dissolves readily, (d) about 1-20 wt% of an unsaturated fatty acid or an alpha-hydroxy acid or a mixture of unsaturated fatty acids or alpha-hydroxy acids or of both unsaturated fatty acids and alpha-hydroxy acids, (e) a lipophilic permeation enhancer, and (f) a matrix modifier.
摘要翻译：在本发明的一个方面，提供了一种用于制造透皮递送坦洛新的贴剂的组合物。该组合物包含（a）至少约1重量％的坦洛新或坦洛新的药学上可接受的盐，（b）至少约40wt％的聚异丁烯粘合剂或疏水性合成橡胶粘合剂，（c）约1-20wt％的非质子（d）约1-20重量％的不饱和脂肪酸或α-羟基酸或不饱和脂肪酸或α-羟基酸或不饱和脂肪酸和α-羟基酸的混合物，（e）亲脂性渗透促进剂，和（f）基质改性剂。

5. 发明申请

WO2005009510A2 PENETRATION ENHANCER COMBINATIONS FOR TRANSDERMAL DELIVERY 审中-公开
标题翻译：渗透增强剂组合用于转运
公开(公告)号：WO2005009510A2
公开(公告)日：2005-02-03
申请号：PCT/US2004/023634
申请日：2004-07-21
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , MITRAGOTRI, Samir , KARANDE, Pankaj , JAIN, Amit, K.
发明人： MITRAGOTRI, Samir , KARANDE, Pankaj , JAIN, Amit, K.
IPC分类号： A61M
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。

6. 发明申请

WO2006091297A3 MOLECULES TO ENHANCE PERCUTANEOUS DELIVERY AND METHODS FOR DISCOVERY THEREFOR 审中-公开
公开(公告)号：WO2006091297A3
公开(公告)日：2006-08-31
申请号：PCT/US2006/001964
申请日：2006-01-17
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , MITRAGOTRI, Samir , KARANDE, Pankaj , JAIN, Amit, K.
发明人： MITRAGOTRI, Samir , KARANDE, Pankaj , JAIN, Amit, K.
IPC分类号： G01N33/48 , G06G7/48
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.

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