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    INSULIN FORMULATIONS FOR INSULIN RELEASE AS A FUNCTION OF TISSUE GLUCOSE LEVELS
    21.
    发明申请
    INSULIN FORMULATIONS FOR INSULIN RELEASE AS A FUNCTION OF TISSUE GLUCOSE LEVELS 审中-公开
    胰岛素释放作为组织葡萄糖水平的功能的胰岛素制剂

    公开(公告)号：US20090175840A1

    公开(公告)日：2009-07-09

    申请号：US12348839

    申请日：2009-01-05

    Applicant: Nandini Kashyap ,  Solomon S. Steiner ,  Roderike Pohl

    Inventor： Nandini Kashyap ,  Solomon S. Steiner ,  Roderike Pohl

    IPC: A61K38/44 ,  A61K38/28 ,  A61K38/43 ,  A61P3/10

    CPC classification number: A61K9/0019 ,  A61K38/28 ,  A61K47/46

    Abstract: Injectable insulin formulations that are capable of modifying the amount of insulin released based on the patient's tissue glucose levels, methods for making and using these formulations are described herein. The formulation may be administered via subcutaneous, intradermal or intramuscular administration. In one preferred embodiment, the formulations are administered via subcutaneous injection. The formulations contain insulin, an oxidizing agent or enzyme and a reducing agent or enzyme, a diluent and optionally one or more thickening agents. If a thickening agent is present in the formulation, the thickening agent increases the viscosity of the formulation following administration. Preferably the formulation contains an insulin, a diluent, glucose oxidase and peroxidase. Following administration to a patient, the insulin is released from the formulations as a function of the patient's tissue glucose level, which in turn maintains the patient's blood glucose level within an optimum range. The formulation is often referred to as a “smart” formulation since it modifies its release rate of insulin according to the patient's needs at a particular time. In a preferred embodiment, the formulation is designed to release insulin into the systemic circulation over time with a basal release profile following injection in a patient. In another embodiment, the formulation is designed to release insulin into the systemic circulation over time with a non-basal release profile following injection in a patient, such as a regular human insulin release profile or a prandial release profile.

    Abstract translation: 本文描述了能够改变基于患者组织葡萄糖水平释放的胰岛素量的可注射胰岛素制剂，制备和使用这些制剂的方法。 制剂可以通过皮下，皮内或肌肉内施用来施用。 在一个优选的实施方案中，通过皮下注射施用制剂。 制剂含有胰岛素，氧化剂或酶，还原剂或酶，稀释剂和任选的一种或多种增稠剂。 如果制剂中存在增稠剂，则增稠剂在给药后增加制剂的粘度。 优选地，制剂含有胰岛素，稀释剂，葡萄糖氧化酶和过氧化物酶。 在给予患者之后，胰岛素作为患者组织葡萄糖水平的函数从制剂中释放，其又将患者的血糖水平维持在最佳范围内。 该制剂通常被称为“智能”制剂，因为其在特定时间根据患者的需要改变其胰岛素的释放速率。 在优选的实施方案中，所述制剂被设计为在患者中注射后具有基础释放曲线随时间将胰岛素释放到全身循环中。 在另一个实施方案中，所述制剂被设计成在患者注射后，例如常规人胰岛素释放曲线或餐时释放曲线，随着时间推移胰岛素进入体循环随着非基础释放曲线。

    RAPID ACTING AND LONG ACTING INSULIN COMBINATION FORMULATIONS
    23.
    发明申请
    RAPID ACTING AND LONG ACTING INSULIN COMBINATION FORMULATIONS 有权
    快速行动和长期行动胰岛素组合制剂

    公开(公告)号：US20080039368A1

    公开(公告)日：2008-02-14

    申请号：US11734161

    申请日：2007-04-11

    Applicant: Solomon S. Steiner ,  Roderike Pohl

    Inventor： Solomon S. Steiner ,  Roderike Pohl

    IPC: A61K38/28 ,  A61P3/10

    CPC classification number: A61K38/28 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0034 ,  A61K9/0043 ,  A61K9/006 ,  A61K47/12 ,  A61K47/183

    Abstract: A combined rapid acting-long acting insulin formulation has been developed wherein the pH of the rapid acting insulin is adjusted so that the long acting glargine remains soluble when they are mixed together. In the preferred embodiment, this injectable basal bolus insulin is administered before breakfast, provides adequate bolus insulin levels to cover the meal, does not produce hypoglycemia after the meal and provides adequate basal insulin for 24 hours. Lunch and dinner can be covered by two bolus injections of a fast acting, or a rapid acting or a very rapid acting insulin. As a result, a patient using intensive insulin therapy should only inject three, rather than four, times a day. Experiments have been performed to demonstrate, the importance of the addition of specific acids to hexameric insulin to enhance speed and amount of absorption and preserve bioactivity following dissociation into the monomeric form by addition of a chelator such as EDTA. As shown by the examples, the preferred acids are aspartic, maleic, succinic, glutamic and citric acid. These are added in addition to a chelator, preferably ethylenediaminetetraacetic acid (EDTA). The results show that the citric acid formulation was more effective at dropping the blood glucose rapidly than the identical rapid acting formulation prepared with HCl in swine. Charge masking by the polyacid appears to be responsible for rapid insulin absorption. EDTA was not effective when used with adipic acid, oxalic acid or HCl at hastening the absorption of insulin. These results confirm the results seen in clinical subjects and patients with diabetes treated with the rapid acting insulin in combination with citric acid and EDTA.

    Abstract translation: 已经开发了组合的快速作用长效胰岛素制剂，其中调节快速作用的胰岛素的pH，使得长效甘精灵在它们混合在一起时仍然是可溶的。 在优选的实施方案中，这种可注射的基础推注胰岛素在早餐前施用，提供足够的推注胰岛素水平以覆盖膳食，在餐后不产生低血糖并提供足够的基础胰岛素24小时。 午餐和晚餐可以通过快速作用或快速作用或非常快速作用的胰岛素的两次快速注射来覆盖。 因此，使用强化胰岛素治疗的患者每天只能注射三次，而不是四次。 已经进行了实验以证明，通过加入螯合剂如EDTA，将特异性酸加入到六聚胰岛素中以增加速度和吸收量并保持生物活性，并将其解离成单体形式。 如实施例所示，优选的酸是天冬氨酸，马来酸，琥珀酸，谷氨酸和柠檬酸。 除了螯合剂，优选乙二胺四乙酸（EDTA）之外还加入它们。 结果表明，柠檬酸配方比在猪中​​用HCl制备的相同的快速作用制剂快速降低血糖。 多酸的电荷掩蔽似乎是快速胰岛素吸收的原因。 当与己二酸，草酸或HCl一起使用以加速胰岛素的吸收时，EDTA无效。 这些结果证实了临床受试者和用快速作用胰岛素与柠檬酸和EDTA组合治疗的糖尿病患者的结果。

    Insulin formulations for rapid uptake
    24.
    发明授权
    Insulin formulations for rapid uptake 有权
    胰岛素配方快速吸收

    公开(公告)号：US09060927B2

    公开(公告)日：2015-06-23

    申请号：US12397219

    申请日：2009-03-03

    Applicant: Solomon S. Steiner ,  Roderike Pohl ,  Ming Li ,  Robert Hauser

    Inventor： Solomon S. Steiner ,  Roderike Pohl ,  Ming Li ,  Robert Hauser

    IPC: A61K38/28 ,  C07K14/62 ,  A61K9/00 ,  A61K38/00

    CPC classification number: A61K9/0019 ,  A61K38/00 ,  A61K38/28 ,  A61K47/12 ,  A61K47/183 ,  C07K14/62

    Abstract: 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.

    Abstract translation: 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。

    Compositions And Methods For Modulating The Pharmacokinetics and Pharmacodynamics of Insulin
    25.
    发明申请
    Compositions And Methods For Modulating The Pharmacokinetics and Pharmacodynamics of Insulin 审中-公开
    用于调节胰岛素的药代动力学和药效学的组合物和方法

    公开(公告)号：US20120178675A1

    公开(公告)日：2012-07-12

    申请号：US13176435

    申请日：2011-07-05

    Applicant: Roderike Pohl ,  Solomon Steiner ,  Robert Hauser ,  Richard Seibert ,  Ming Li

    Inventor： Roderike Pohl ,  Solomon Steiner ,  Robert Hauser ,  Richard Seibert ,  Ming Li

    IPC: A61K38/28 ,  A61P25/00 ,  A61P3/10

    CPC classification number: C07K14/62 ,  A61K9/0019 ,  A61K38/28 ,  A61K47/183

    Abstract: 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.

    Abstract translation: 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。

    STABILIZED GLUCAGON SOLUTIONS
    28.
    发明申请
    STABILIZED GLUCAGON SOLUTIONS 审中-公开
    稳定的GLUCAGON解决方案

    公开(公告)号：US20110097386A1

    公开(公告)日：2011-04-28

    申请号：US12715203

    申请日：2010-03-01

    Applicant: Solomon S. Steiner ,  Robert Hauser ,  Ming Li ,  Robert Feldstein ,  Roderike Pohl

    Inventor： Solomon S. Steiner ,  Robert Hauser ,  Ming Li ,  Robert Feldstein ,  Roderike Pohl

    IPC: A61K38/26 ,  A61K9/127 ,  A61P3/08

    CPC classification number: A61K38/26 ,  A61K9/0019 ,  A61K9/1075 ,  A61K9/127 ,  A61K9/19 ,  A61K47/24

    Abstract: A formulation composed of a sugar such as glucose and a surfactant such as myristoyl lysophosphocholine (LMPC) has been designed to stabilize both hydrophilic and hydrophobic portions of the glucagon molecule, under prolonged physiological conditions, in a formulation that is sufficiently similar to the pH and osmolarity of plasma so as not to induce or to minimize site irritation. The combination of a simple sugar and an surfactant stabilizes the glucagon molecule in an aqueous solution for seven days at 37° C.

    Abstract translation: 已经设计了由糖如葡萄糖和表面活性剂如肉豆蔻酰溶血磷脂酰胆碱（LMPC）组成的制剂，以在长时间的生理条件下稳定胰高血糖素分子的亲水部分和疏水部分，其浓度与pH和pH足够相似， 血浆的渗透压，以免诱发或最小化部位刺激。 单糖和表面活性剂的组合使得胰高血糖素分子在37℃下在水溶液中稳定7天。

    Rapid acting and long acting insulin combination formulations
    29.
    发明授权
    Rapid acting and long acting insulin combination formulations 有权
    快速作用和长效胰岛素组合配方

    公开(公告)号：US07713929B2

    公开(公告)日：2010-05-11

    申请号：US11695562

    申请日：2007-04-02

    Applicant: Solomon S. Steiner ,  Roderike Pohl

    Inventor： Solomon S. Steiner ,  Roderike Pohl

    IPC: A61K38/28 ,  A61K38/16 ,  A61K31/185 ,  C07K14/62

    CPC classification number: A61K38/28 ,  A61K31/185 ,  A61K31/19 ,  A61K31/385 ,  A61K2300/00

    Abstract: A combined rapid acting-long acting insulin formulation has been developed in which the pH of the rapid acting insulin is decreased so that the long acting glargine remains soluble when they are mixed together. In the preferred embodiment, this injectable basal bolus insulin is administered before breakfast, provides adequate bolus insulin levels to cover the meal, does not produce hypoglycemia after the meal and provides adequate basal insulin for 24 hours. Lunch and dinner can be covered by two bolus injections of a fast acting, or a rapid acting or a very rapid acting insulin. As a result, a patient using intensive insulin therapy should only inject three, rather than four, times a day.

    Abstract translation: 已经开发了组合的快速作用长效胰岛素制剂，其中快速作用的胰岛素的pH降低，使得长效甘精氨酸在混合在一起时仍然是可溶的。 在优选的实施方案中，这种可注射的基础推注胰岛素在早餐前施用，提供足够的推注胰岛素水平以覆盖膳食，在餐后不产生低血糖并提供足够的基础胰岛素24小时。 午餐和晚餐可以通过快速作用或快速作用或非常快速作用的胰岛素的两次快速注射来覆盖。 因此，使用强化胰岛素治疗的患者每天只能注射三次，而不是四次。

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