公开(公告)号：US20200215063A1

公开(公告)日：2020-07-09

申请号：US16820794

申请日：2020-03-17

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Nadine Paiement ,  Angela Angusti ,  Cormac Long ,  Rodolphe Obeid ,  Laetitia Rodes ,  Billal Tir

IPC: A61K31/4985 ,  A61K9/00 ,  A61K9/70

Abstract: Oral film dosage forms that provide improved solubilization and stabilization of an active ingredient in particle form include at least one primary crystallization inhibitor in an amount that inhibits growth and/or agglomeration of the active ingredient, a polyoxyethylated fatty acid glycerides in an amount that further enhances inhibition of crystallization, growth and agglomeration of the particles of the pharmaceutically active ingredient; and at least one plasticizer present in an amount that is effective to increase flexibility and elasticity of the film dosage form.

公开(公告)号：US20150038540A1

公开(公告)日：2015-02-05

申请号：US14447071

申请日：2014-07-30

Applicant: IntelGenx Corp.

Inventor： Horst G. Zerbe ,  Angela Angusti ,  Nadine Paiement

IPC: A61K31/4196 ,  A61K47/32 ,  A61K47/02 ,  A61K47/38

CPC classification number: A61K31/4196 ,  A61K9/0056 ,  A61K9/006 ,  A61K31/422 ,  A61K31/473 ,  A61K31/5513 ,  A61K31/5517 ,  A61K47/02 ,  A61K47/32 ,  A61K47/38

Abstract: An instantly wettable and rapidly disintegrating oral film dosage form without a surfactant and without a polyalcohol was achieved by combining at least one water soluble polymer that is not a copolymer of vinylpyrrolidone, at least one active agent, a copolymer of vinylpyrrolidone and titanium dioxide. In certain embodiments, the film comprises hydroxypropyl cellulose or a combination of hydroxypropyl cellulose and a polymer or copolymer of vinylpyrrolidone or a substituted vinylpyrrolidone as the water soluble polymer(s). A plasticizer, and optional additives selected from synthetic sweeteners, natural sweeteners, flavorants, antioxidants, colorants, and opacifiers, can be added to the disclosed film oral dosage forms.

Abstract translation: 通过组合不是乙烯基吡咯烷酮，至少一种活性剂，乙烯基吡咯烷酮和二氧化钛的共聚物的共聚物的至少一种水溶性聚合物，实现了无表面活性剂和不含多元醇的立即可湿性和快速崩解的口腔膜剂型。 在某些实施方案中，该膜包含羟丙基纤维素或羟丙基纤维素与乙烯基吡咯烷酮或取代的乙烯基吡咯烷酮的聚合物或共聚物作为水溶性聚合物的组合。 可以向所公开的膜口服剂型中加入增塑剂和选自合成甜味剂，天然甜味剂，调味剂，抗氧化剂，着色剂和遮光剂的任选添加剂。

公开(公告)号：US20190290595A1

公开(公告)日：2019-09-26

申请号：US16441872

申请日：2019-06-14

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Rodolphe Obeid ,  Justin W. Conway ,  Nadine Paiement ,  Ludwig Aigner

IPC: A61K9/70 ,  A61K9/00 ,  A61K31/381 ,  A61K31/404 ,  A61K31/47

Abstract: Disclosed is a device and method for treating a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having a film layer and a safe and effective amount of a leukotriene receptor antagonist or leukotriene synthesis inhibitor. The device is configured and formulated to achieve transmucosal and/or enteral delivery of the leukotriene receptor antagonist or leukotriene synthesis inhibitor. The method includes transmucosally and/or enterally delivering to an animal in need of treatment, a safe and effective amount of a leukotriene blocker capable of crossing the blood-brain barrier.

公开(公告)号：US20180228738A1

公开(公告)日：2018-08-16

申请号：US15912103

申请日：2018-03-05

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Rodolphe Obeid ,  Justin W. Conway ,  Nadine Paiement ,  Ludwig Aigner

IPC: A61K9/70 ,  A61K31/47 ,  A61K31/381 ,  A61K31/404

Abstract: Disclosed is a device and method for treating a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having a film layer and a safe and effective amount of a leukotriene receptor antagonist or leukotriene synthesis inhibitor. The device is configured and formulated to achieve transmucosal and/or enteral delivery of the leukotriene receptor antagonist or leukotriene synthesis inhibitor. The method includes transmucosally and/or enterally delivering to an animal in need of treatment, a safe and effective amount of a leukotriene blocker capable of crossing the blood-brain barrier.

公开(公告)号：US20180250240A1

公开(公告)日：2018-09-06

申请号：US15940288

申请日：2018-03-29

Applicant: Intelgenx Corp.

Inventor： Nadine Paiement ,  Horst G. Zerbe ,  Justin W. Conway ,  Rodolphe Obeid

IPC: A61K9/70 ,  A61K31/47 ,  A61K9/00 ,  A61K47/14 ,  A61K47/18 ,  A61K47/10

CPC classification number: A61K9/7007 ,  A61K9/006 ,  A61K31/47 ,  A61K47/10 ,  A61K47/14 ,  A61K47/183 ,  A61K47/36 ,  A61K47/38

Abstract: Disclosed is a method of administration and device for the improved bioavailability of leukotriene receptor antagonists. This method and device involve an alkaline surface pH oral film dosage form designed to deliver leukotriene receptor antagonists, such as Montelukast, to the stomach in an amorphous precipitate suspended in aqueous medium. Also disclosed is a device and method for treating a disease, such as a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having an alkaline surface pH film layer and a safe and effective amount of Montelukast. The device is configured and formulated to predominantly achieve enteral delivery of the Montelukast. The method includes enterally delivering to a human or an animal in need of treatment, a safe and effective amount of Montelukast capable of crossing the blood-brain barrier.

公开(公告)号：US09949934B1

公开(公告)日：2018-04-24

申请号：US15299054

申请日：2016-10-20

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Rodolphe Obeid ,  Justin W. Conway ,  Nadine Paiement ,  Ludwig Aigner

IPC: A61K9/70 ,  A61K31/4704 ,  C07D215/18 ,  A61K31/404 ,  A61K31/381 ,  A61K31/47

CPC classification number: A61K9/7007 ,  A61K9/006 ,  A61K31/381 ,  A61K31/404 ,  A61K31/47

Abstract: Disclosed is a device and method for treating a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having a film layer and a safe and effective amount of a leukotriene receptor antagonist or leukotriene synthesis inhibitor. The device is configured and formulated to achieve transmucosal and/or enteral delivery of the leukotriene receptor antagonist or leukotriene synthesis inhibitor. The method includes transmucosally and/or enterally delivering to an animal in need of treatment, a safe and effective amount of a leukotriene blocker capable of crossing the blood-brain barrier.

公开(公告)号：US20190133925A1

公开(公告)日：2019-05-09

申请号：US16131995

申请日：2018-09-14

Applicant: Intelgenx Corp.

Inventor： Nadine Paiement ,  Horst G. Zerbe ,  Justin W. Conway ,  Rodolphe Obeid ,  Ludwig Aigner ,  Johanna Michael

IPC: A61K9/00 ,  A61K31/47

Abstract: Disclosed is a method of administration and device for the improved bioavailability of leukotriene receptor antagonists. This method and device involve an alkaline surface pH oral film dosage form designed to deliver leukotriene receptor antagonists, such as Montelukast, to the stomach in an amorphous precipitate suspended in aqueous medium. Also disclosed is a device and method for treating a disease, such as a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having an alkaline surface pH film layer and a safe and effective amount of Montelukast. The device is configured and formulated to predominantly achieve enteral delivery of the Montelukast. The method includes enterally delivering to a human or an animal in need of treatment, a safe and effective amount of Montelukast capable of crossing the blood-brain barrier.

公开(公告)号：US20180110724A1

公开(公告)日：2018-04-26

申请号：US15848819

申请日：2017-12-20

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Nadine Paiement ,  Cormac Long ,  Rodolphe Obeid

IPC: A61K9/00 ,  A61K9/14 ,  A61K9/70 ,  A61K31/4985 ,  A61K31/4709 ,  A61K31/58 ,  A61K31/19 ,  A61K31/40 ,  A61K31/34 ,  A61K31/496 ,  A61K31/439 ,  A61K31/553 ,  A61K31/353 ,  A61K47/14

CPC classification number: A61K9/006 ,  A61K9/14 ,  A61K9/145 ,  A61K9/1635 ,  A61K9/7007 ,  A61K31/19 ,  A61K31/34 ,  A61K31/353 ,  A61K31/40 ,  A61K31/439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/553 ,  A61K31/58 ,  A61K47/14

Abstract: Oral film dosage forms that provide improved solubilization and stabilization of an active ingredient in particle form include at least one primary crystallization inhibitor in an amount that inhibits growth and/or agglomeration of the active ingredient, a polyoxyethylated fatty acid glycerides in an amount that further enhances inhibition of crystallization, growth and agglomeration of the particles of the pharmaceutically active ingredient; and at least one plasticizer present in an amount that is effective to increase flexibility and elasticity of the film dosage form.

公开(公告)号：US20170157119A1

公开(公告)日：2017-06-08

申请号：US15426149

申请日：2017-02-07

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Nadine Paiement ,  Angela Angusti ,  Cormac Long ,  Rodolphe Obeid

IPC: A61K31/4985 ,  A61K47/14 ,  A61K47/44 ,  A61K47/12 ,  A61K47/10 ,  A61K9/00 ,  A61K47/26

CPC classification number: A61K31/4985 ,  A61K9/006 ,  A61K9/7007

Abstract: Oral film dosage forms that provide improved solubilization and stabilization of an active ingredient in particle form include at least one primary crystallization inhibitor in an amount that inhibits growth and/or agglomeration of the active ingredient, a polyoxyethylated fatty acid glycerides in an amount that further enhances inhibition of crystallization, growth and agglomeration of the particles of the pharmaceutically active ingredient; and at least one plasticizer present in an amount that is effective to increase flexibility and elasticity of the film dosage form.

公开(公告)号：US10722476B2

公开(公告)日：2020-07-28

申请号：US15912103

申请日：2018-03-05

Applicant: Intelgenx Corp.

Inventor： Horst G. Zerbe ,  Rodolphe Obeid ,  Justin W. Conway ,  Nadine Paiement ,  Ludwig Aigner

IPC: A61K9/70 ,  A61K9/00 ,  A61K31/381 ,  A61K31/404 ,  A61K31/47

Abstract: Disclosed is a device and method for treating a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having a film layer and a safe and effective amount of a leukotriene receptor antagonist or leukotriene synthesis inhibitor. The device is configured and formulated to achieve transmucosal and/or enteral delivery of the leukotriene receptor antagonist or leukotriene synthesis inhibitor. The method includes transmucosally and/or enterally delivering to an animal in need of treatment, a safe and effective amount of a leukotriene blocker capable of crossing the blood-brain barrier.