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    Synthesis of insulin derivatives
    1.
    发明授权
    Synthesis of insulin derivatives 有权
    胰岛素衍生物的合成

    公开(公告)号：US06323311B1

    公开(公告)日：2001-11-27

    申请号：US09400942

    申请日：1999-09-22

    申请人： Feng Liu ,  Sung Wan Kim ,  Miroslav Baudys

    发明人： Feng Liu ,  Sung Wan Kim ,  Miroslav Baudys

    IPC分类号： A61K3828

    CPC分类号： C07K14/62 ,  A61K38/00 ,  A61K47/60 ,  Y02P20/55

    摘要： A method for the “one-pot” synthesis of insulin derivatives wherein insulin is modified at the &agr;-amino group of the PheB1 residue is described. The method comprises protecting the &agr;-amino group of the GlyA1 residue and the &egr;-amino group of the LysB29 residue by reaction of insulin with a cyclic anhydride of a dicarboxylic acid in the presence of a tertiary amine. The protected insulin is then reacted with an activated hydrophilic compound, preferably an activated polyethylene glycol, resulting in a conjugate of the hydrophilic compound coupled to the PheB1 residue of insulin. The protecting groups are then removed from the conjugate under mild acidic conditions, and the resulting insulin derivative can be purified by conventional methods. Monosubstituted insulin derivatives wherein polyethylene glycol or derivatives thereof or glycosides are coupled to the PheB1 residue of insulin are also described.

    摘要翻译： 描述了在PheB1残基的α-氨基处修饰胰岛素的“一锅”合成胰岛素衍生物的方法。 该方法包括在叔胺存在下，通过胰岛素与二羧酸的环状酸酐的反应来保护GlyA1残基的α-氨基和LysB29残基的ε-氨基。 然后将受保护的胰岛素与活化的亲水化合物，优选活化的聚乙二醇反应，得到与胰岛素的PheB1残基偶联的亲水性化合物的缀合物。 然后在温和的酸性条件下将保护基团从缀合物中除去，所得到的胰岛素衍生物可以通过常规方法纯化。 还描述了其中聚乙二醇或其衍生物或糖苷偶联至胰岛素的PheB1残基的单取代胰岛素衍生物。

    Stabilization and oral delivery of calcitonin
    3.
    发明授权
    Stabilization and oral delivery of calcitonin 失效
    降钙素的稳定和口服递送

    公开(公告)号：US5726154A

    公开(公告)日：1998-03-10

    申请号：US671870

    申请日：1996-06-28

    申请人： Miroslav Baudys ,  Sung Wan Kim

    发明人： Miroslav Baudys ,  Sung Wan Kim

    IPC分类号： A61K38/23 ,  A61K38/00 ,  A61K38/02 ,  A61K38/30 ,  C07K5/00

    CPC分类号： A61K38/23

    摘要： Compositions and methods for stabilization and oral delivery of human calcitonin are described. An aqueous liquid composition for stable storage of human calcitonin comprises an aqueous mixture of SDS and an organic acid. An nonaqueous liquid composition for stable storage of human calcitonin comprises about 90-100% by volume of a mixture of C.sub.8 /C.sub.10 mono- and di-glycerides and about 0-10% by volume of a polar, nonaqueous solvent. Both of these stabilized human calcitonin formulations provided significant intestinal absorption of calcitonin.

    摘要翻译： 描述了人类降钙素稳定和口服递送的组合物和方法。 用于稳定储存人降钙素的水性液体组合物包括SDS和有机酸的水性混合物。 用于稳定储存人降钙素的非水液体组合物包含约90-100体积％的C8 / C10单甘油酯和二甘油酯的混合物和约0-10体积％的极性非水溶剂。 这两种稳定的降钙素制剂都能提供显着的降钙素吸收。