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    Glp-1 derivatives and transmicosal absorption preparations thereof
    1.
    发明申请
    Glp-1 derivatives and transmicosal absorption preparations thereof 失效
    Glp-1衍生物及其经半吸收制剂

    公开(公告)号：US20060194720A1

    公开(公告)日：2006-08-31

    申请号：US10530125

    申请日：2003-10-10

    申请人： Yuji Hayashi ,  Mitsuhiro Makino ,  Toshiyuki Kouzaki ,  Motohiro Takeda ,  Takahito Jomori

    发明人： Yuji Hayashi ,  Mitsuhiro Makino ,  Toshiyuki Kouzaki ,  Motohiro Takeda ,  Takahito Jomori

    IPC分类号： C07K14/605 ,  A61K38/22

    CPC分类号： C07K14/605 ,  A61K38/26 ,  Y10S514/866

    摘要： The invention relates to a GLP-1 derivative including an amino acid sequence of GLP-1 (7-35) having deletion, substitution and/or addition of one or more amino acids and having Waa-(Xaa)n-Yaa (in which Waa is Arg or Lys, Xaa is Arg or Lys, n is an integer of 0 to 14, and Yaa is Arg, Arg-NH2, Lys, Lys-NH2 or Hse) added to the C-terminus of the peptide having a GLP-1 activity. These derivatives are derivatives highly absorbable via a mucous membrane. In the invention, the GLP-1 derivative can be conferred with resistance to dipeptidyl peptidase IV by substituting amino acid 8 in its GLP-1 amino acid sequence with Ser, or with resistance to trypsin by substituting amino acids 26 and 34 with Gln and Asn, respectively. The efficiency of absorption of the GLP-1 derivatives of the invention via mucous membranes can be further improved by preparing a composition using a charge-regulated fat emulsion regulated to be negatively charged thereon.

    摘要翻译： 本发明涉及包含具有缺失，取代和/或添加一个或多个氨基酸并具有Waa-（Xaa）n-Yaa）的GLP-1（7-35）氨基酸序列的GLP-1衍生物（其中 Waa为Arg或Lys，Xaa为Arg或Lys，n为0〜14的整数，Yaa为Arg，Arg-NH 2 Lys，Lys-NH 2 >或Hse）加入具有GLP-1活性的肽的C末端。 这些衍生物是通过粘膜高度吸收的衍生物。 在本发明中，通过用Ser取代其GLP-1氨基酸序列中的氨基酸8或通过用Gln和Asn取代氨基酸26和34对胰蛋白酶具有抗性，GLP-1衍生物可赋予对二肽基肽酶IV的抗性 ， 分别。 本发明的GLP-1衍生物通过粘膜吸收的效率可以通过使用调节为带负电荷的电荷调节脂肪乳剂制备组合物而进一步改善。

    GLP-1 derivative and preparation thereof absorbable via mucous membrane
    2.
    发明授权
    GLP-1 derivative and preparation thereof absorbable via mucous membrane 失效
    GLP-1衍生物及其可通过粘膜吸收的制剂

    公开(公告)号：US07291594B2

    公开(公告)日：2007-11-06

    申请号：US10530125

    申请日：2003-10-10

    申请人： Yuji Hayashi ,  Mitsuhiro Makino ,  Toshiyuki Kouzaki ,  Motohiro Takeda ,  Takahito Jomori

    发明人： Yuji Hayashi ,  Mitsuhiro Makino ,  Toshiyuki Kouzaki ,  Motohiro Takeda ,  Takahito Jomori

    IPC分类号： A61K38/26 ,  C07K14/605

    CPC分类号： C07K14/605 ,  A61K38/26 ,  Y10S514/866

    摘要： A GLP-1 derivative is provided including an amino acid sequence of GLP-1 (7-35) having deletion, substitution and/or addition of one or more amino acids and having Waa-(Xaa)n-Yaa (in which Waa is Arg or Lys, Xaa is Arg or Lys, n is an integer of 0 to 14, and Yaa is Arg, Arg-NH2, Lys, Lys-NH2 or Hse) added to the C-terminus of the peptide having a GLP-1 activity. These derivatives are highly absorbable via a mucous membrane. The GLP-1 derivative can be conferred with resistance to dipeptidyl peptidase IV by substituting amino acid 8 in its GLP-1 amino acid sequence with Ser, or with resistance to trypsin by substituting amino acids 26 and 34 with Gln and Asn, respectively.The absorption efficiency of the GLP-1 derivatives via mucous membranes can be further improved by preparing a composition using a charge-regulated fat emulsion regulated to be negatively charged thereon.

    摘要翻译： 提供GLP-1衍生物，其包含具有缺失，取代和/或添加一个或多个氨基酸并具有Waa-（Xaa）n-Yaa的GLP-1（7-35）的氨基酸序列（其中Waa为 Arg或Lys，Xaa是Arg或Lys，n是0-14的整数，Yaa是Arg，Arg-NH 2，Lys，Lys-NH 2或 Hse）加入具有GLP-1活性的肽的C末端。 这些衍生物通过粘膜是高度可吸收的。 通过用Ser取代其GLP-1氨基酸序列中的氨基酸8，或分别用Gln和Asn取代氨基酸26和34，对胰蛋白酶具有抗性，GLP-1衍生物可赋予对二肽基肽酶IV的抗性。 通过使用调节为带负电荷的电荷调节脂肪乳液制备组合物，可以进一步提高通过粘膜的GLP-1衍生物的吸收效率。

    Polystyrene sulfonate-containing gel preparation
    4.
    发明授权
    Polystyrene sulfonate-containing gel preparation 失效
    含聚苯乙烯磺酸盐的凝胶制剂

    公开(公告)号：US06703013B1

    公开(公告)日：2004-03-09

    申请号：US09508539

    申请日：2000-04-05

    申请人： Hideaki Ninomiya ,  Masahiro Nakajima ,  Toshiyuki Kouzaki ,  Masaki Ando ,  Fumio Higuchi

    发明人： Hideaki Ninomiya ,  Masahiro Nakajima ,  Toshiyuki Kouzaki ,  Masaki Ando ,  Fumio Higuchi

    IPC分类号： A61K3774

    CPC分类号： A61K9/006 ,  A61K9/06 ,  A61K31/795 ,  Y10S514/944

    摘要： The invention relates to a polystyrene sulfonate-containing gel preparation for therapy of hyperpotassemia, wherein the particle size of polystyrene sulfonate is controlled within the range of at least 5-100 &mgr;m, the viscosity of its solution before gelation is adjusted depending on the particle size by adding a thickening agent, and the polystyrene sulfonate particles after gelation is uniformly dispersed therein. More preferably, a water-displacing agent is contained, whereby the amount of water in the preparation is reduced. This gel preparation does not cause a sense of foreign matter or a sense of roughness in the oral cavity upon ingestion and intake, thus making it unnecessary to drink water for ingestion, and further its water content is low, so that control of water intake is made easy, even in the case of a patient with renal insufficiency who is subjecting to restriction in intake of water to significant improve the quality of life of the patient.

    摘要翻译： 本发明涉及一种用于治疗高钾血症的聚苯乙烯磺酸盐凝胶制剂，其中聚苯乙烯磺酸盐的粒径控制在至少5-100μm的范围内，凝胶化前溶液的粘度根据粒径 通过添加增稠剂，凝胶化后的聚苯乙烯磺酸酯粒子均匀分散。 更优选含有取代剂，由此减少制剂中的水量。 这种凝胶制剂在摄入和摄入时不会引起口腔感和异味，因此不必饮用水摄取，进一步其含水量低，从而控制摄入水量 即使在患有肾功能不全的患者进行限制摄入水以显着改善患者的生活质量的情况下也是容易的。