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    • 51. 发明授权
    • Mixed solvent mutually enhanced transdermal therapeutic system
    • 混合溶剂相互增强透皮治疗系统
    • US5925372A
    • 1999-07-20
    • US725222
    • 1991-06-26
    • Bret BernerCharles EbertGerard C. MazzengaJohn H. Otte
    • Bret BernerCharles EbertGerard C. MazzengaJohn H. Otte
    • A61K9/70A61F13/02
    • A61K9/7069A61K9/7084
    • A transdermal drug delivery system comprising(i) an occlusive, impermeable polymeric backing layer;(ii) a drug depot on one side thereof;(iii) a removable, occlusive covering layer over said drug depot; and(iv) an adhesive means by which said delivery system, absent said removable covering layer may be affixed to an intended patient;said drug depot containing a drug formulation comprising a transdermally administrable pharmaceutically acceptable pharmaceutically active agent or a precursor thereof, water and lower alkanol; said active agent or precursor thereof being present in a pharmaceutically effective amount; said lower alkanol and said water being present in a volume:volume ratio of from 30:70 up to less than 95:5 such that said lower alkanol, water and drug are delivered to a patient's skin, which patient has applied said system absent said removable covering layer to said patient's skin, in amounts that said drug is delivered in a transdermally administrable efficacious amount, said water has an activity at said patient's skin of about 0.4 to about 0.95 and said lower alkanol, at said patient's skin, has an activity of 0.3 to about 0.9, and wherein, once applied to said patient's skin, said lower alkanol has a flux from said system to said skin of at least 1500 mcg/cm.sup.2 /hr and through said skin of at least 1500 mcg/cm.sup.2 /hr.
    • 一种透皮药物递送系统,其包括(i)封闭的,不可渗透的聚合物背衬层; (ii)其一侧的药剂库; (iii)所述药物库上的可移除的封闭覆盖层; 和(iv)粘合剂装置,其中没有所述可移除覆盖层的所述递送系统可以被固定到预期的患者身上; 所述药物贮库含有药物制剂,其包含透皮给药的药学上可接受的药物活性剂或其前体,水和低级链烷醇; 所述活性剂或其前体以药学上有效的量存在; 所述低级链烷醇和所述水以体积比为30:70至小于95:5存在,使得所述低级链烷醇,水和药物被递送至患者的皮肤,该患者应用所述系统不存在所述 所述药物以经皮可施用的有效量递送的量,所述水在所述患者皮肤上具有约0.4至约0.95的活性,并且所述低级烷醇在所述患者皮肤处具有活性 0.3至约0.9,并且其中一旦施用于所述患者皮肤,所述低级链烷醇具有从所述系统到所述皮肤的通量至少为1500mcg / cm 2 /小时,并且通过所述皮肤至少为1500mcg / cm 2 /小时 。
    • 52. 发明授权
    • Copolymer of (meth)acryloxy-alkyl-siloxysilane and alkyl(meth)acrylates
and the use thereof as pressure sensitive adhesives
    • (甲基)丙烯酰氧基 - 烷基 - 硅氧烷硅烷和(甲基)丙烯酸烷基酯的共聚物及其作为压敏粘合剂的用途
    • US5288827A
    • 1994-02-22
    • US18667
    • 1993-02-17
    • Xiaoling LiBret Berner
    • Xiaoling LiBret Berner
    • C08F220/18C08F30/08C08F220/10C08F230/08
    • C08F230/08Y10S526/931
    • A new polymer, the feed monomers and molar percents of which, exclusive of a polymerization initiator and crosslinker, are:A.(I) 42 mole % to 58 mole % of a siloxy silane of formula I,(II) 42 mole % to 58 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 16 mole % of an additional vinylic copolymerizable monomer;B.(I) 42 mole % to 58 mole % of a siloxy silane of formula I,(II) 21 mole % up to less than 42 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 29 mole % of an additional vinylic copolymerizable monomer, orC.(I) 16 mole % up to less than 42 mole % of a siloxy silane of formula I,(II) 42 mole % of 58 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 36 mole % of an additional vinylic copolymerizable monomer,where formula I is ##STR1## where formula II is ##STR2## where Group A is a vinylic acid or a (meth)acrylate as defined herein. Methods of manufacture of the polymer and the use thereof as a pressure adhesive, especially a transdermal and/or transmucosal delivery system pressure sensitive adhesive, are also claimed.
    • 一种新的聚合物,不包括聚合引发剂和交联剂的进料单体和摩尔百分数为:A.(I)42摩尔%至58摩尔%的式I的(甲氧基)硅烷,(II)为42摩尔% 58摩尔%的式II,(III)的未取代的(甲基)丙烯酸烷基酯,(III)0-5摩尔%的A组单体,和(Ⅳ)0-16摩尔%的另外的乙烯基可共聚单体; B.(I)42摩尔%至58摩尔%的式I,(II)的甲硅烷氧基硅烷,21摩尔%至至少少于42摩尔%的式II,(III)的未取代的(甲基)丙烯酸烷基酯, 5摩尔%的A组单体,和(IV)0-29摩尔%的另外的乙烯基可共聚单体,或C.(I)16摩尔%至多至少于42摩尔%的式I的甲硅烷氧基硅烷,( II)42摩尔%的58摩尔%的式II,(III)的未取代的(甲基)丙烯酸烷基酯,0-5摩尔%的A组单体,和(Ⅳ)0-36摩尔%的另外的乙烯基可共聚单体 其中式I是(*化学结构*)(I),其中式II是(*化学结构*)(II),其中A组是本文定义的乙烯基酸或(甲基)丙烯酸酯。 还要求保护聚合物的制造方法及其作为压力粘合剂,特别是透皮和/或经粘膜递送系统压敏粘合剂的用途。
    • 54. 发明授权
    • Article useful for administration of pharmacologically-active substances
transdermally, orally, or by means of implant
    • 用于透皮,口服或通过植入物施用药理活性物质的制品
    • US4758434A
    • 1988-07-19
    • US847635
    • 1986-04-03
    • Agis KydonieusKishore R. ShahBret Berner
    • Agis KydonieusKishore R. ShahBret Berner
    • A61K9/70A61K31/21A61M31/00A61L15/03A61F13/00
    • A61K9/703A61K31/21A61K9/7084A61M31/002
    • Described is an article of manufacture useful for administration of pharmacologically-active substances, transdermally, orally or by means of subdermal implant comprising a solid vinyl plastisol layer for contacting a patient's tissue, internally or externally, the layer containing from about 20 up to about 70% by weight of a polyvinyl chloride resin or a polyvinyl chloride-polyvinyl acetate copolymer containing a minor proportion of vinyl acetate; from about 20-70% plasticizer composition; from abotu 0.5 up to 35% of pharmacologically-active substance such as isosorbide dinitrate, nicotine, clonidine, guanfacine, indomethacin, glyceryl trinitrate and prostaglandin and optionally excipients. Also described is the novel plasticizer-polyvinyl chloride composition of matter comprising 1-dodecylhexahydro-2H-azepin-2-one and polyvinyl chloride resin taken together with a pharmacologically-active substance whereint he 1-dodecylhexahydro-2H-azepin-2-one not only acts as a plasticizer but also acts as a penetration enhancer (through tissue) for the pharmacologically-active substance.
    • 描述了可用于施用药理学活性物质,经皮,口服或通过皮下植入的制剂,其包括固体乙烯基增塑溶胶层,用于在内部或外部将患者组织接触含有约20至约70的层 重量百分比的聚氯乙烯树脂或含有少量醋酸乙烯酯的聚氯乙烯 - 聚乙酸乙烯酯共聚物; 约20-70%的增塑剂组成; 来自abotu 0.5至35%的药理活性物质如硝酸异山梨酯,尼古丁,可乐定,胍法西林,吲哚美辛,三硝酸甘油酯和前列腺素以及任选的赋形剂。 还描述了包含1-十二烷基六氢-2H-氮杂-2-酮和聚氯乙烯树脂与药物活性物质一起的新型增塑剂 - 聚氯乙烯组合物,其中1-十二烷基六氢-2H-氮杂-2-酮不包括 仅用作增塑剂,但也用作药理活性物质的渗透促进剂(通过组织)。