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    • 5. 发明申请
    • STABLE NON-ALCOHOLIC FOAMABLE PHARMACEUTICAL EMULSION COMPOSITIONS WITH AN UNCTUOUS EMOLLIENT AND THEIR USES
    • 稳定的非酒精泡沫药物组合物与联合动物及其用途
    • US20110097279A1
    • 2011-04-28
    • US12974857
    • 2010-12-21
    • Dov TAMARKINMeir EINIDoron FRIEDMANDavid SCHUZTal BERMAN
    • Dov TAMARKINMeir EINIDoron FRIEDMANDavid SCHUZTal BERMAN
    • A61K9/12A61P17/00A61K8/06A61Q19/00
    • A61K9/0014A61K8/046A61K8/39A61K8/731A61K8/86A61K9/1075A61K9/122A61Q7/00A61Q19/00
    • A stable non-alcoholic foamable pharmaceutical emulsion composition includes an unctuous emollient, at a concentration of about 0.5% to about 49% by weight; at least one multi-active agent; at a concentration of about 0.5% to about 15% by weight; water; an effective amount of an active pharmaceutical agent having a degree of solubility in the emulsion composition; and at least one liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition; wherein the unctuous emollient comprises a petrolatum alone or in combination with other unctuous agents; wherein the multi active agent is selected from the group consisting of (a) two or more complex emulgators wherein there is a difference of about 4 or more units between the HLB values of two of the emulgators or there is a significant difference in the chemical nature or structure of two of the emulgators; (b) a surfactant and a foam adjuvant or co surfactant, wherein the surfactant has a HLB close to the required HLB of the oil phase; (c) a surfactant and a liquid wax, wherein the surfactant has a HLB close to the required HLB of the oil phase; (d) a surfactant and a polymeric agent other than starch or a modified starch ester, wherein the surfactant has a HLB close to the required HLB of the oil phase; (e) a polymeric agent and a foam adjuvant or co surfactant, which can cooperate to stabilize the emulsion; (f) a single surfactant without a long polymeric side chain that is composed of a mixture of esters having a HLB close to the required HLB of the oil phase; combinations of any of the above, and wherein the composition is substantially flowable is stored in an pressurized container and upon release expands to form a breakable foam.
    • 稳定的非醇可发泡药物乳液组合物包含浓度为约0.5%至约49%(重量)的单一润肤剂; 至少一种多活性剂; 浓度为约0.5%至约15%重量; 水; 有效量的在乳液组合物中具有溶解度的活性药剂; 和至少一种浓度为总组合物重量的约3%至约25%的液化或压缩气体推进剂; 其中所述柔性润肤剂单独包含凡士林或与其它浮游剂组合; 其中所述多活性剂选自(a)两种或更多种复合乳化剂,其中在两个所述乳化剂的HLB值之间存在约4个或更多个单元的差异,或者化学性质存在显着差异 或结构的两个emulgators; (b)表面活性剂和泡沫助剂或助表面活性剂,其中表面活性剂具有接近油相所需HLB的HLB; (c)表面活性剂和液体蜡,其中所述表面活性剂具有接近所述油相所需HLB的HLB; (d)除淀粉或改性淀粉酯以外的表面活性剂和聚合物,其中所述表面活性剂具有接近油相所需HLB的HLB; (e)聚合剂和泡沫助剂或助表面活性剂,其可以配合以稳定乳液; (f)不含长聚合物侧链的单一表面活性剂,其由具有接近油相所需HLB的HLB的酯的混合物组成; 并且其中组合物基本可流动的组合物储存在加压容器中并且当释放时膨胀以形成可破裂的泡沫。
    • 6. 发明申请
    • STABLE NON-ALCOHOLIC FOAMABLE PHARMACEUTICAL EMULSION COMPOSITIONS WITH AN UNCTUOUS EMOLLIENT AND THEIR USES
    • 稳定的非酒精泡沫药物组合物与联合动物及其用途
    • US20080206155A1
    • 2008-08-28
    • US11940290
    • 2007-11-14
    • Dov TAMARKINMeir EINIDoron FRIEDMANDavid SCHUZTal BERMAN
    • Dov TAMARKINMeir EINIDoron FRIEDMANDavid SCHUZTal BERMAN
    • A61K9/12
    • A61K9/0014A61K8/046A61K8/39A61K8/731A61K8/86A61K9/1075A61K9/122A61Q7/00A61Q19/00
    • A stable non-alcoholic foamable pharmaceutical emulsion composition includes an unctuous emollient, at a concentration of about 0.5% to about 49% by weight; at least one multi-active agent; at a concentration of about 0.5% to about 15% by weight; water; an effective amount of an active pharmaceutical agent having a degree of solubility in the emulsion composition; and at least one liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition; wherein the unctuous emollient comprises a petrolatum alone or in combination with other unctuous agents; wherein the multi active agent is selected from the group consisting of (a) two or more complex emulgators wherein there is a difference of about 4 or more units between the HLB values of two of the emulgators or there is a significant difference in the chemical nature or structure of two of the emulgators; (b) a surfactant and a foam adjuvant or co surfactant, wherein the surfactant has a HLB close to the required HLB of the oil phase; (c) a surfactant and a liquid wax, wherein the surfactant has a HLB close to the required HLB of the oil phase; (d) a surfactant and a polymeric agent other than starch or a modified starch ester, wherein the surfactant has a HLB close to the required HLB of the oil phase; (e) a polymeric agent and a foam adjuvant or co surfactant, which can cooperate to stabilize the emulsion; (f) a single surfactant without a long polymeric side chain that is composed of a mixture of esters having a HLB close to the required HLB of the oil phase; combinations of any of the above, and wherein the composition is substantially flowable is stored in an pressurized container and upon release expands to form a breakable foam.
    • 稳定的非醇可发泡药物乳液组合物包含浓度为约0.5%至约49%(重量)的单一润肤剂; 至少一种多活性剂; 浓度为约0.5%至约15%重量; 水; 有效量的在乳液组合物中具有溶解度的活性药剂; 和至少一种浓度为总组合物重量的约3%至约25%的液化或压缩气体推进剂; 其中所述柔性润肤剂单独包含凡士林或与其它浮游剂组合; 其中所述多活性剂选自(a)两种或更多种复合乳化剂,其中在两个所述乳化剂的HLB值之间存在约4个或更多个单元的差异,或者化学性质存在显着差异 或结构的两个emulgators; (b)表面活性剂和泡沫助剂或助表面活性剂,其中表面活性剂具有接近油相所需HLB的HLB; (c)表面活性剂和液体蜡,其中所述表面活性剂具有接近所述油相所需HLB的HLB; (d)除淀粉或改性淀粉酯以外的表面活性剂和聚合物,其中所述表面活性剂具有接近油相所需HLB的HLB; (e)聚合剂和泡沫助剂或助表面活性剂,其可以配合以稳定乳液; (f)不含长聚合物侧链的单一表面活性剂,其由具有接近所述油相所需HLB的HLB的酯的混合物组成; 并且其中组合物基本可流动的组合物储存在加压容器中并且当释放时膨胀以形成可破裂的泡沫。
    • 9. 发明申请
    • FOAMABLE COMPOSITIONS AND KITS COMPRISING ONE OR MORE OF A CHANNEL AGENT, A CHOLINERGIC AGENT, A NITRIC OXIDE DONOR, AND RELATED AGENTS AND THEIR USES
    • 包含一个或多个通道代理,化学试剂,氮氧化物和相关试剂及其用途的可燃组合物和试剂盒
    • US20080317679A1
    • 2008-12-25
    • US11767442
    • 2007-06-22
    • Dov TAMARKINMeir EINIDoron FRIEDMANTal BERMANAlex BESONOV
    • Dov TAMARKINMeir EINIDoron FRIEDMANTal BERMANAlex BESONOV
    • A61K9/00A61P17/14A61P17/02A61P17/06
    • A61K31/554A01N25/16A61K9/1075A61K9/12A61K31/4422A61K31/505A61K47/10
    • The present invention relates to a foamable therapeutic composition comprising: (a) a therapeutically effective concentration of at least one active agent selected from the group consisting of a channel agent, a cholinergic agent, and a nitric oxide donor; and (b) a foamable carrier comprising: i. about 50% to about 98% of a solvent selected from the group consisting of water; a hydrophilic solvent; a hydrophobic solvent; a potent solvent; a polar solvent, a silicone, an emollient, and mixtures thereof; ii. 0% to about 48% of a secondary solvent selected from the group consisting of water; a hydrophilic solvent; a hydrophobic solvent; a potent solvent; a polar solvent, a silicone, an emollient, a co-solvent, a penetration enhancer and mixtures thereof; iii. a surface-active agent; iv. about 0% to about 5% by weight of at least one polymeric agent; and v. a liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition; wherein the composition is housed in a container and is substantially flowable, and which upon release expands to form a breakable foam; and wherein the foamable carrier is selected to generate a foam of good to excellent quality. The invention further provides a method of treating, alleviating or preventing a disorder of mammalian subject, comprising administering such a composition to an afflicted target site.
    • 本发明涉及可发泡治疗组合物,其包含:(a)治疗有效浓度的至少一种选自通道剂,胆碱能药和一氧化氮供体的活性剂; 和(b)可发泡载体,包括:i。 约50%至约98%的选自水的溶剂; 亲水性溶剂; 疏水溶剂; 有效溶剂; 极性溶剂,硅氧烷,软化剂及其混合物; ii。 0%至约48%的选自水的第二溶剂; 亲水性溶剂; 疏水溶剂; 有效溶剂; 极性溶剂,硅氧烷,软化剂,​​助溶剂,渗透增强剂及其混合物; iii。 表面活性剂; iv。 约0重量%至约5重量%的至少一种聚合物; 和v。浓度为总组合物重量的约3%至约25%的液化或压缩气体推进剂; 其中所述组合物容纳在容器中并且基本上是可流动的,并且其在释放时膨胀以形成可破坏的泡沫; 并且其中所述可发泡载体被选择以产生良好至优异质量的泡沫。 本发明进一步提供治疗,减轻或预防哺乳动物受试者病症的方法,包括将所述组合物施用于受影响的靶位点。