公开(公告)号：US20080096800A1

公开(公告)日：2008-04-24

申请号：US11923591

申请日：2007-10-24

Applicant: Roderike Pohl ,  Solomon Steiner

Inventor： Roderike Pohl ,  Solomon Steiner

IPC: A61K38/28 ,  A61P3/10

CPC classification number: A61K9/0056 ,  A61K9/006 ,  A61K9/06 ,  A61K9/107 ,  A61K38/28 ,  A61K47/12 ,  A61K47/18 ,  A61K47/183

Abstract: Gel, powder, suspension, emulsions or film formulations for systemic delivery of insulin with improved stability and rapid onset of action are described herein. The formulations are preferably absorbed to a mucosal surface, most preferably via buccal or sublingual administration, although rectal, vaginal, nasal or ocular administration is possible. 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. Following administration, these formulations are rapidly absorbed into the blood stream. The formulation is preferably a polymeric gel, powder or film which adheres to the mucosal surface, thereby enhancing uptake of the incorporated drug. In the preferred embodiment, this formulation is administered sublingually, most preferably before a meal or after a meal.

Abstract translation: 本文描述了具有改善的稳定性和快速起效的胰岛素全身递送的凝胶，粉末，悬浮液，乳剂或膜制剂。 制剂优选被吸收到粘膜表面，最优选通过颊或舌下施用，尽管可以进行直肠，阴道，鼻或眼睛给药。 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。 给药后，这些制剂被快速吸收到血液中。 制剂优选是粘附到粘膜表面的聚合物凝胶，粉末或膜，从而增强所掺入的药物的摄取。 在优选的实施方案中，该制剂是舌下给药，最优选在饭前或​​饭后服用的。

公开(公告)号：US20070235365A1

公开(公告)日：2007-10-11

申请号：US11767698

申请日：2007-06-25

Applicant: Roderike Pohl ,  Solomon Steiner

Inventor： Roderike Pohl ,  Solomon Steiner

IPC: A61K38/28 ,  A61K9/70 ,  B65D83/06

CPC classification number: A61K9/006 ,  A61K9/0019 ,  A61K9/0056 ,  A61K38/28 ,  Y10S514/866 ,  Y10S514/951 ,  Y10S514/953 ,  Y10S514/959

Abstract: Drug formulations for systemic drug delivery with improved stability and rapid onset of action are described herein. The formulations may be administered via buccal administration, sublingual administration, pulmonary delivery, nasal administration, subcutaneous administration, rectal administration, vaginal administration, or ocular administration. In the preferred embodiments, the formulations are administered sublingually or via subcutaneous injection. The formulations contain an active agent and one or more excipients, selected to increase the rate of dissolution. In the preferred embodiment, the drug is insulin, and the excipients include a metal chelator such as EDTA and an acid such as citric acid. Following administration, these formulations are rapidly absorbed by the oral mucosa when administered sublingually and are rapidly absorbed into the blood stream when administered by subcutaneous injection. In one embodiment, the composition is in the form of a dry powder. In another embodiment, the composition is in the form of a film, wafer, lozenge, capsule, or tablet. In a third embodiment, a dry powdered insulin is mixed with a diluent containing a pharmaceutically acceptable carrier, such as water or saline, a metal chelator such as EDTA and an acid such as citric acid. Devices for storing and mixing these formulations are also described.

Abstract translation: 本文描述了具有改善的稳定性和快速起效的全身药物递送的药物制剂。 制剂可以通过口腔给药，舌下给药，肺部输送，鼻内给药，皮下给药，直肠给药，阴道给药或眼部给药来施用。 在优选的实施方案中，制剂是舌下给药或通过皮下注射给药。 制剂含有活性剂和一种或多种赋形剂，其被选择以增加溶解速率。 在优选的实施方案中，药物是胰岛素，赋形剂包括金属螯合剂如EDTA和酸如柠檬酸。 给药后，这些制剂在舌下施用时被口腔粘膜快速吸收，并且当通过皮下注射给药时，其迅速地被吸收到血液流中。 在一个实施方案中，组合物为干粉的形式。 在另一个实施方案中，组合物为薄膜，晶片，锭剂，胶囊或片剂的形式。 在第三个实施方案中，将干粉状胰岛素与含有药学上可接受的载体如水或盐水，金属螯合剂如EDTA和酸如柠檬酸的稀释剂混合。 还描述了用于储存和混合这些制剂的装置。

公开(公告)号：US20070086952A1

公开(公告)日：2007-04-19

申请号：US11537335

申请日：2006-09-29

Applicant: Solomon Steiner ,  Roderike Pohl

Inventor： Solomon Steiner ,  Roderike Pohl

IPC: A61K38/28 ,  A61K9/12

CPC classification number: A61K38/28 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0034 ,  A61K9/006 ,  A61K9/0075 ,  A61K9/0078 ,  A61K47/12 ,  A61K47/183

Abstract: It has been discovered that by combining a chelator, such as ethylenediaminetetraacetic acid, with an acidifier, such as citric acid, the insulin is absorbed much more rapidly than in the absence of the chelator and acidifier, with a commercially available rapid, intermediate or long lasting insulin such as glargine, one can increase and/or prolong the bioavailability of the insulin mixture. The formulations are suitable for administration by injection or to a mucosal surface such as the pulmonary or oral regions, although subcutaneous injection is preferred.

Abstract translation: 已经发现，通过将诸如乙二胺四乙酸的螯合剂与酸化剂如柠檬酸组合，胰岛素比不含螯合剂和酸化剂的吸收要快得多，可商购的快速，中间或长期 持久的胰岛素如甘精胰岛素，可以增加和/或延长胰岛素混合物的生物利用度。 制剂适合于通过注射施用或粘膜表面如肺部或口腔区域，尽管皮下注射是优选的。