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    • 4. 发明申请
    • INSULIN FORMULATIONS FOR RAPID UPTAKE
    • 胰岛素制剂用于快速摄取
    • US20100227795A1
    • 2010-09-09
    • US12397219
    • 2009-03-03
    • Solomon S. SteinerRoderike PohlMing LiRobert Hauser
    • Solomon S. SteinerRoderike PohlMing LiRobert Hauser
    • A61K38/28A61P3/10
    • A61K9/0019A61K38/00A61K38/28A61K47/12A61K47/183C07K14/62
    • Injectable insulin formulations with improved stability and rapid onset of action are described herein. The formulations may be for subcutaneous, intradermal or intramuscular administration. In the preferred embodiment, the formulations are administered via subcutaneous injection. The formulations contain insulin in combination with a chelator and dissolution agent, and optionally additional excipients. In the preferred embodiment, the formulation contains human insulin, a zinc chelator such as EDTA and a dissolution agent such as citric acid or sodium citrate. These formulations are rapidly absorbed into the blood stream when administered by subcutaneous injection. In the preferred embodiment, the insulin is provided as a clear liquid, neutral pH, in a multi-use sterile vial. In an alternative embodiment, the insulin is provided as a powder in a sterile vial. This is mixed with a diluent containing a pharmaceutically acceptable carrier, such as water, a zinc chelator such as EDTA and a dissolution agent such as citric acid shortly before or at the time of administration. In another embodiment, the insulin is stored as a frozen mixture, ready for use upon thawing.
    • 本文描述了具有改善的稳定性和快速起效的可注射的胰岛素制剂。 制剂可用于皮下,皮内或肌内给药。 在优选的实施方案中,通过皮下注射施用制剂。 制剂含有与螯合剂和溶解剂以及任选的其它赋形剂组合的胰岛素。 在优选的实施方案中,制剂含有人胰岛素,锌螯合剂如EDTA和溶解剂如柠檬酸或柠檬酸钠。 当通过皮下注射给药时,这些制剂被快速地吸收到血流中。 在优选的实施方案中,胰岛素以多用途无菌小瓶中的透明液体中性pH提供。 在替代实施方案中,胰岛素以无菌小瓶中的粉末形式提供。 将其与包含药学上可接受的载体如水,锌螯合剂如EDTA的稀释剂和不久之前或给药时的溶解剂如柠檬酸混合。 在另一个实施方案中,将胰岛素作为冷冻混合物储存,准备在解冻时使用。
    • 5. 发明授权
    • Insulin formulations for rapid uptake
    • 胰岛素配方快速吸收
    • US09060927B2
    • 2015-06-23
    • US12397219
    • 2009-03-03
    • Solomon S. SteinerRoderike PohlMing LiRobert Hauser
    • Solomon S. SteinerRoderike PohlMing LiRobert Hauser
    • A61K38/28C07K14/62A61K9/00A61K38/00
    • A61K9/0019A61K38/00A61K38/28A61K47/12A61K47/183C07K14/62
    • Injectable insulin formulations with improved stability and rapid onset of action are described herein. The formulations may be for subcutaneous, intradermal or intramuscular administration. In the preferred embodiment, the formulations are administered via subcutaneous injection. The formulations contain insulin in combination with a chelator and dissolution agent, and optionally additional excipients. In the preferred embodiment, the formulation contains human insulin, a zinc chelator such as EDTA and a dissolution agent such as citric acid or sodium citrate. These formulations are rapidly absorbed into the blood stream when administered by subcutaneous injection. In the preferred embodiment, the insulin is provided as a clear liquid, neutral pH, in a multi-use sterile vial. In an alternative embodiment, the insulin is provided as a powder in a sterile vial. This is mixed with a diluent containing a pharmaceutically acceptable carrier, such as water, a zinc chelator such as EDTA and a dissolution agent such as citric acid shortly before or at the time of administration. In another embodiment, the insulin is stored as a frozen mixture, ready for use upon thawing.
    • 本文描述了具有改善的稳定性和快速起效的可注射的胰岛素制剂。 制剂可用于皮下,皮内或肌内给药。 在优选的实施方案中,通过皮下注射施用制剂。 制剂含有与螯合剂和溶解剂以及任选的其它赋形剂组合的胰岛素。 在优选的实施方案中,制剂含有人胰岛素,锌螯合剂如EDTA和溶解剂如柠檬酸或柠檬酸钠。 当通过皮下注射给药时,这些制剂被快速地吸收到血流中。 在优选的实施方案中,胰岛素以多用途无菌小瓶中的透明液体中性pH提供。 在替代实施方案中,胰岛素以无菌小瓶中的粉末形式提供。 将其与包含药学上可接受的载体如水,锌螯合剂如EDTA的稀释剂和不久之前或给药时的溶解剂如柠檬酸混合。 在另一个实施方案中,将胰岛素作为冷冻混合物储存,准备在解冻时使用。
    • 6. 发明申请
    • Compositions And Methods For Modulating The Pharmacokinetics and Pharmacodynamics of Insulin
    • 用于调节胰岛素的药代动力学和药效学的组合物和方法
    • US20120178675A1
    • 2012-07-12
    • US13176435
    • 2011-07-05
    • Roderike PohlSolomon SteinerRobert HauserRichard SeibertMing Li
    • Roderike PohlSolomon SteinerRobert HauserRichard SeibertMing Li
    • A61K38/28A61P25/00A61P3/10
    • C07K14/62A61K9/0019A61K38/28A61K47/183
    • Compositions and methods for modulating the pharmacokinetics and pharmacodynamics of rapid acting injectable insulin formulations are described herein. In the preferred embodiment, the formulations are administered via subcutaneous injection. The formulations contain insulin in combination with a zinc chelator such as ethylenediaminetetraacetic acid (“EDTA”) and a dissolution/stabilization agent, and optionally additional excipients. Calcium disodium EDTA is less likely to remove calcium from the body, and typically has less pain on injection in the subcutaneous tissue. Modulating the type and quantity of EDTA can change the insulin absorption profile. Increasing the quantity of citrate can further enhance absorption and chemically stabilize the formulation. In the preferred embodiment, the formulation contains human insulin, calcium disodium EDTA and a dissolution/stabilization agent such as citric acid or sodium citrate. These formulations are rapidly absorbed into the blood stream when administered by subcutaneous injection.
    • 本文描述了用于调节快速作用的可注射胰岛素制剂的药代动力学和药效学的组合物和方法。 在优选的实施方案中,通过皮下注射施用制剂。 制剂含有与锌螯合剂如乙二胺四乙酸(“EDTA”)和溶解/稳定剂以及任选的其它赋形剂组合的胰岛素。 EDTA二钠不太可能从体内去除钙,并且通常在皮下组织中注射时疼痛较少。 调节EDTA的类型和数量可以改变胰岛素吸收特征。 增加柠檬酸盐的量可以进一步增强吸收和化学稳定制剂。 在优选的实施方案中,制剂含有人胰岛素,EDTA二钠钙和溶解/稳定剂如柠檬酸或柠檬酸钠。 当通过皮下注射给药时,这些制剂被快速地吸收到血流中。