STABLE SUSTAINED RELEASE THERAPEUTIC COMPOSITIONS IN APROTIC POLAR SOLVENTS AND METHODS OF MANUFACTURING THE SAME

    公开(公告)号:US20210401945A1

    公开(公告)日:2021-12-30

    申请号:US17359202

    申请日:2021-06-25

    摘要: The present invention relates to the use of aprotic polar solvents and an ionization stabilizing agent to prepare storage stable sustained release therapeutic formulations by dissolving a therapeutic agent (active ingredient) in an aprotic polar solvent system that can then be administered to patients suffering from or predisposed to a variety of physical conditions or disorders, notably hypoglycemia. In certain embodiments, the invention is directed to formulations comprising one or more therapeutic agents, as well as methods of making such formulations, comprising at least one therapeutic agent dissolved in an aprotic polar solvent such as DMSO, comprising at least one ionization stabilizing excipient (suitably, a mineral acid) and at least one sustained release modifier (suitably, a divalent cation-donating compound such as a zinc salt and/or a polymer such as a PLGA) in concentrations sufficient to impart physical and chemical stability to the therapeutic agent and to produce a formulation that results in a sustained release of the therapeutic agent into the bloodstream of an animal to which the formulation has been administered. The invention also relates to methods of producing such storage stable sustained release therapeutic formulations and to methods of treating, preventing and diagnosing certain physical conditions and disorders, notably hypoglycemia, by administering such storage stable sustained release therapeutic formulations to a patient.

    Methods for rapidly treating severe hypoglycemia
    9.
    发明授权
    Methods for rapidly treating severe hypoglycemia 有权
    快速治疗严重低血糖症的方法

    公开(公告)号:US09018162B2

    公开(公告)日:2015-04-28

    申请号:US13826662

    申请日:2013-03-14

    CPC分类号: A61K38/26 A61K9/0019 A61K9/19

    摘要: Disclosed is a method for treating or preventing hypoglycemia in a patient comprising administering an effective amount of a composition comprising a glucagon peptide which has been dried in a non-volatile buffer, and wherein the glucagon peptide has a pH memory that is about equal to the pH of the glucagon peptide in the non-volatile buffer, and an aprotic polar solvent, wherein the moisture content of the formulation is less than 5%, and wherein the dried glucagon peptide maintains the pH memory that is about equal to the pH of the glucagon peptide in the non-volatile buffer when the dried glucagon peptide is reconstituted in the aprotic polar solvent, wherein the patient has been diagnosed as having a blood glucose level between 0 mg/dL and less than 50 mg/dL or has an indication of impending hypoglycemia based on a blood glucose monitoring device before administration of the composition, and wherein the patient has a blood glucose level greater than 50 mg/dL to 180 mg/dL within 1 to 20 minutes after administration of the composition.

    摘要翻译: 公开了一种用于治疗或预防患者中的低血糖的方法,包括给予有效量的包含已在非挥发性缓冲液中干燥的胰高血糖素肽的组合物,并且其中所述胰高血糖素肽具有约等于 胰高血糖素肽在非挥发性缓冲液中的pH以及非质子极性溶剂,其中制剂的水分含量小于5%,并且其中干燥的胰高血糖素肽保持pH记忆大约等于 当干性胰高血糖素肽在非质子极性溶剂中重构时,在非挥发性缓冲液中的胰高血糖素肽,其中所述患者被诊断为具有0mg / dL至小于50mg / dL的血糖水平或具有 在施用组合物之前基于血糖监测装置的即将发生的低血糖,并且其中所述患者的血糖水平在1t以内大于50mg / dL至180mg / dL ○给予组合物20分钟。

    FORMULATIONS FOR THE TREATMENT OF DIABETES
    10.
    发明申请
    FORMULATIONS FOR THE TREATMENT OF DIABETES 有权
    治疗糖尿病的配方

    公开(公告)号:US20140349926A1

    公开(公告)日:2014-11-27

    申请号:US14354848

    申请日:2012-10-31

    IPC分类号: A61K47/20 A61K38/22 A61K38/28

    摘要: Disclosed is a formulation for parenteral administration comprising insulin that comprises a pH memory between 1 to 4 or between 6 to 8 and an aprotic polar solvent, wherein the insulin is solubilized in the aprotic polar solvent, wherein the solubilized insulin comprises stable monomeric or dimeric forms of insulin or mixtures thereof, and wherein the water content of the formulation is equal to or less than 15% w/v.

    摘要翻译: 公开了一种用于肠胃外给药的制剂,其包含含有1至4或6至8之间的pH记忆和非质子极性溶剂的胰岛素,其中所述胰岛素溶解在非质子极性溶剂中,其中所述溶解的胰岛素包含稳定的单体或二聚体形式 的胰岛素或其混合物,并且其中制剂的水含量等于或小于15%w / v。