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    Testosterone prodrugs for improved drug delivery
    29.
    发明授权
    Testosterone prodrugs for improved drug delivery 失效
    用于改善药物递送的睾酮前药

    公开(公告)号：US5622944A

    公开(公告)日：1997-04-22

    申请号：US434892

    申请日：1995-05-04

    申请人： Ron L. Hale ,  Amy T. Lu ,  Dennis W. Solas ,  Michel J. N. Cormier

    发明人： Ron L. Hale ,  Amy T. Lu ,  Dennis W. Solas ,  Michel J. N. Cormier

    IPC分类号： A61K9/00 ,  A61K47/48 ,  A61K31/575

    CPC分类号： A61K31/568 ,  A61K47/4803 ,  A61K47/48992 ,  A61K9/0009 ,  B82Y5/00

    摘要： Compositions and methods are provided for enhanced transdermal electrotransport of 17-hydroxy sterol compounds, including testosterone. The parent sterols are modified at the 17-hydroxy position by covalent attachment of a charged chemical modifier. The chemical modifier provides the parent sterol with enhanced transport properties and is hydrolyzed under physiological conditions to release the active parent compound.The composition comprises a 17-hydroxy sterol/chemical modifier complex, more generally represented by the formula (sterol--O--)C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+. The portion of the complex derived from the chemical modifier is indicated by "C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ ", where N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ represents a quaternary ammonium group and R.sup.1, R.sup.2, and R.sup.3 are independently selected from the group consisting of lower alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroalkyl, and heteroarylalkyl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached form a substituted heterocycle and R.sup.3 is lower alkyl, and R is a linking moiety, linking the (sterol--O)--C(O)-- to the nitrogen atom.

    摘要翻译： 提供组合物和方法用于增强17-羟基甾醇化合物（包括睾酮）的透皮电转运。 母体甾醇通过带电化学改性剂的共价连接在17-羟基位置被修饰。 化学改性剂提供具有增强的转运性质的亲本甾醇，并在生理条件下水解以释放活性母体化合物。 该组合物包含17-羟基甾醇/化学改性剂复合物，更通常由式（甾醇-O-）C（O）-R-N（R1）（R2）（R3）+表示。 衍生自化学改性剂的复合物部分由“C（O）-RN（R1）（R2）（R3）+”表示，其中N（R1）（R2）（R3）+代表季铵基团， R 1，R 2和R 3独立地选自低级烷基，烷基，芳基，芳基烷基，环烷基，杂烷基和杂芳基烷基; 或R 1和R 2与它们所连接的氮一起形成取代的杂环，并且R 3是低级烷基，R是将（甾醇-O）-C（O） - 与氮原子连接的连接部分。

    Aerosol Drug Delivery Device Incorporating Percussively Activated Heat Packages
    30.
    发明申请
    Aerosol Drug Delivery Device Incorporating Percussively Activated Heat Packages 审中-公开
    气溶胶药物输送装置包含冲击式活化热包装

    公开(公告)号：US20100006092A1

    公开(公告)日：2010-01-14

    申请号：US12550209

    申请日：2009-08-28

    申请人： Ron L. Hale ,  Mingzu Lei ,  Peter M. Lloyd ,  Patrik Munzar ,  C.V. Krishnamohan Sharma ,  Dennis W. Solas ,  Matthew D. Stracker

    发明人： Ron L. Hale ,  Mingzu Lei ,  Peter M. Lloyd ,  Patrik Munzar ,  C.V. Krishnamohan Sharma ,  Dennis W. Solas ,  Matthew D. Stracker

    IPC分类号： A61M15/06 ,  F23Q1/06

    CPC分类号： A61M11/041 ,  A61M11/047 ,  A61M15/0031 ,  A61M15/0045

    摘要： Aerosol drug delivery devices incorporating percussively activated heat packages are disclosed. The heat packages include a percussive igniter and a fuel capable of undergoing an exothermic oxidation-reduction reaction when ignited by the percussive igniter. The drug delivery devices disclosed can be activated by an actuation mechanism to vaporize a thin solid film comprising a drug disposed on the exterior of a hat package. Metal coordination complexes of volatile drugs, and in particular nicotine, from which the drug can be selectively vaporized when heated are also disclosed. The use of aerosol drug delivery devices comprising thin films of nicotine metal salt complexes for the treatment of nicotine craving and for effecting smoking cessation are also disclosed.

    摘要翻译： 公开了包含冲击活化热包装的气溶胶药物递送装置。 热包装包括打击式点火器和能够在被打击式点火器点燃时经历放热氧化还原反应的燃料。 所公开的药物输送装置可以由致动机构激活，以蒸发包括设置在帽子包装的外部上的药物的薄的固体膜。 还公开了挥发性药物的金属配位络合物，特别是加热时药物可以从其中选择性蒸发的尼古丁。 还公开了包括尼古丁金属盐络合物的薄膜用于治疗尼古丁渴望和用于戒烟的气溶胶药物递送装置的使用。