Compositions and methods for non-parenteral delivery of oligonucleotides
    7.
    发明授权
    Compositions and methods for non-parenteral delivery of oligonucleotides 失效
    用于非肠胃外递送寡核苷酸的组合物和方法

    公开(公告)号:US06747014B2

    公开(公告)日:2004-06-08

    申请号:US10029598

    申请日:2001-12-21

    IPC分类号: A61K3170

    摘要: The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.

    摘要翻译: 本发明涉及通过非肠胃外给药途径增强寡核苷酸和核酸的局部和全身摄取和递送的组合物和方法。 包含本文公开的寡核苷酸的药物组合物包括用于全身递送的乳液和微乳液制剂用于各种应用和口服剂型。 还令人惊讶地发现,可以用简单的溶液,例如纯的或盐水,通过直肠灌肠剂和栓剂将寡核苷酸局部递送至结肠部位。 寡核苷酸的这种药物组合物可以进一步包括一种或多种用于将寡核苷酸和其它核酸转移穿过粘膜的渗透增强剂。 本发明的组合物和方法用于对动物进行口服,口腔,直肠或阴道施用反义寡核苷酸,以调节动物中基因在调查,治疗,姑息或预防目的中的表达。

    Pulsatile release compositions and methods for enhanced intestinal oligonucleotide drug absorption
    8.
    发明授权
    Pulsatile release compositions and methods for enhanced intestinal oligonucleotide drug absorption 有权
    脉冲释放组合物和增强肠道寡核苷酸药物吸收的方法

    公开(公告)号:US07576067B2

    公开(公告)日:2009-08-18

    申请号:US11000814

    申请日:2004-12-01

    CPC分类号: A61K9/4808 A61K9/4891

    摘要: Delayed release oral pharmaceutical formulations and methods for enhanced intestinal drug absorption. The formulation comprises a first population of carrier particles comprising a drug and a penetration enhancer which are released at a first location in the intestine, and a second population of carrier particles comprising a penetration enhancer and a delayed release coating or matrix. This penetration enhancer is released at a second location in the intestine downstream from the first location and enhances absorption of the drug when it reaches the second location.

    摘要翻译: 延迟口服药物制剂和增强肠吸收药物的方法。 所述制剂包含第一载体颗粒群,其包含在肠中的第一位置释放的药物和渗透增强剂,以及包含渗透促进剂和延迟释放包衣或基质的第二种载体颗粒。 该渗透促进剂在第一位置下游的肠道的第二位置释放,并且当药物到达第二位置时增强药物的吸收。