公开(公告)号：US20080045447A1

公开(公告)日：2008-02-21

申请号：US11811170

申请日：2007-06-08

Applicant: Robert Gyurik ,  Carl Reppucci ,  Zhengmao Li

Inventor： Robert Gyurik ,  Carl Reppucci ,  Zhengmao Li

IPC: A61K38/28 ,  A61M11/00 ,  A61P3/08

CPC classification number: A61K38/28 ,  A61K9/0043 ,  A61K9/107 ,  A61K9/1075 ,  A61K47/02 ,  A61K47/08 ,  A61K47/12 ,  A61K47/22 ,  A61K47/26

Abstract: Compositions and methods are disclosed for treating a patient with insulin, wherein a composition in a form suitable for nasal delivery to a patient comprises a therapeutically effective amount of insulin, a permeation enhancer, a liquid carrier, and an acid present in said composition in an amount sufficient to provide an acidic pH, but not greater than a pH of 4.5, said acid being selected from the group consisting of: monovalent inorganic acid(s), sulfuric acid, and acetic acid. Preferably the composition is essentially-free of citrate(s) and essentially-free of phosphate(s). The composition being thus designed with the intent to provide a composition that is essentially-free of fibrilliform (or beta-sheet) insulin polymorphs.

Abstract translation: 公开了用于治疗患有胰岛素的患者的组合物和方法，其中适于鼻输给患者的形式的组合物包含治疗有效量的胰岛素，渗透增强剂，液体载体和存在于所述组合物中的酸 足以提供酸性pH但不大于pH 4.5的量，所述酸选自：一价无机酸，硫酸和乙酸。 优选地，组合物基本上不含柠檬酸盐，并且基本上不含磷酸盐。 这样设计的组合物旨在提供基本上不含原纤维状（或β-片）胰岛素多晶型物的组合物。

公开(公告)号：US20140128379A1

公开(公告)日：2014-05-08

申请号：US14007153

申请日：2012-03-29

Applicant: Nils Bergenhem ,  Carl Reppucci ,  Zhengmao Li

Inventor： Nils Bergenhem ,  Carl Reppucci ,  Zhengmao Li

IPC: A61K31/5513 ,  A61K9/00

CPC classification number: A61K31/5513 ,  A61K9/0043 ,  A61K31/365 ,  A61K31/551 ,  A61K31/5517 ,  A61K47/08 ,  A61K47/10

Abstract: The present invention provides pharmaceutical compositions for intranasal delivery of a benzodiazepine. The composition may contain a therapeutically effective amount of a benzodiazepine or a pharmaceutically acceptable salt thereof, and a permeation enhancer. The permeation enhancer may be propylene glycol or a Hsieh permeation enhancer. The present compositions have excellent bioavailability. After administration of the present compositions, therapeutically effective plasma levels of the benzodiazepine may be achieved rapidly. The present pharmaceutical composition may be used to treat a patient suffering from anxiety, epilepsy, insomnia, agitation, seizures, muscular disorders, alcohol dependence, and drug withdrawal.

Abstract translation: 本发明提供了用于鼻内递送苯二氮卓类药物的药物组合物。 组合物可以含有治疗有效量的苯并二氮杂或其药学上可接受的盐和渗透促进剂。 渗透促进剂可以是丙二醇或Hsieh渗透促进剂。 本发明的组合物具有优异的生物利用度。 在给予本发明组合物后，可以快速实现苯二氮卓类药物的治疗有效血浆水平。 本发明的药物组合物可用于治疗患有焦虑，癫痫，失眠，激动，癫痫发作，肌肉障碍，酒精依赖和药物戒断的患者。

公开(公告)号：US20110097363A1

公开(公告)日：2011-04-28

申请号：US12902397

申请日：2010-10-12

Applicant: Fred Feldman ,  Zhengmao Li ,  Jeffrey Banas ,  Carl Reppucci

Inventor： Fred Feldman ,  Zhengmao Li ,  Jeffrey Banas ,  Carl Reppucci

IPC: A61K38/28 ,  A61K9/107 ,  A61P3/10

CPC classification number: A61K9/0043 ,  A61K9/107 ,  A61K47/22

Abstract: The present invention provides a preparation of a therapeutically effective amount of insulin with a concentration of A21 desamido insulin greater than about 2% (w/w).

Abstract translation: 本发明提供治疗有效量的胰岛素的制剂，其胰岛素浓度高于约2％（w / w）。

公开(公告)号：US20080305174A1

公开(公告)日：2008-12-11

申请号：US11760083

申请日：2007-06-08

Applicant: Robert J. Gyurik ,  Zhengmao Li

Inventor： Robert J. Gyurik ,  Zhengmao Li

IPC: A61K9/51 ,  A61K38/02 ,  A61K38/16 ,  A61K38/28 ,  A61P3/10 ,  A61K47/30 ,  A61K47/32 ,  A61K47/34

CPC classification number: A61K9/5153 ,  A61K9/1075 ,  A61K9/1273 ,  A61K38/28

Abstract: The present invention relates to drug delivery formulations that utilize nanocapsules, such as nanovesicles, micelles, lamellae particles, polymersomes, dendrimers, and other nano-size particles of various other fabrications, including those that are known in the art. The invention employs diblock copolymers or single block polymers that hold, adhere to, absorb or encapsulate drug molecules, including, but not limited to, those that heretofore have not been successfully formulated for oral drug delivery, e.g., insulin. Nanocapsule holding, adherence, absorption or encapsulation of such drugs or other molecules enables their delivery via oral or mucosal means.

Abstract translation: 本发明涉及使用纳米胶囊的药物递送制剂，例如纳米囊，胶束，薄片颗粒，聚合物囊泡，树枝状大分子和其它各种制造的纳米尺寸颗粒，包括本领域已知的纳米尺寸颗粒。 本发明使用保持，粘附，吸收或包封药物分子的二嵌段共聚物或单嵌段聚合物，包括但不限于迄今尚未成功配制用于口服药物递送的那些，例如胰岛素。 这些药物或其他分子的纳米胶囊保持，粘附，吸收或包封使其能够通过口腔或粘膜手段递送。