公开(公告)号：US11471406B2

公开(公告)日：2022-10-18

申请号：US17063644

申请日：2020-10-05

Applicant: INTELGENX CORP.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Justin Conway ,  Billal Tir

IPC: A61K9/00 ,  A61K47/38 ,  A61K31/4985

Abstract: An oral film dosage form includes a high viscosity polymer in an amount of from 1% to 5% by dry weight to reduce, modulate and/or control Cmax of an active agent. The high viscosity polymer has a viscosity of from 100 cps to 500 cps as determined at 2% concentration in water by weight at 25° C. using a Brookfield LVF viscometer with spindle no. 2 at 60 rpm.

公开(公告)号：US20160324773A1

公开(公告)日：2016-11-10

申请号：US15216903

申请日：2016-07-22

Applicant: IntelGenx Corp.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Billal Tir

IPC: A61K9/00 ,  A61K31/4985 ,  A61K47/38 ,  A61K31/5513

CPC classification number: A61K47/10 ,  A61K9/006 ,  A61K9/7007 ,  A61K31/196 ,  A61K31/216 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4985 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/573 ,  A61K31/58 ,  A61K31/60 ,  A61K31/704 ,  A61K31/7076 ,  A61K38/00

Abstract: Oral thin film dosage form of a stable dispersion of non-solubilized amorphous or partially amorphous active agent(s), having a mean particle size diameter D50 equal or less than 250 μm, that remains uniformly distributed within a film matrix and contains at least one film forming polymer, and optional pharmaceutically-acceptable excipients, such as diluents, plasticizers, surfactants, sweeteners, and taste-masking agent(s), are prepared by a process including first providing the active agent in an amorphous particle form having a mean particle size diameter D50 equal or less than 250 μm. Next, the active agent is suspended in a liquid film-forming formulation without dissolving the active agent. Therefore, the solvent is removed to form a film.

Abstract translation: 具有平均粒度直径D50等于或小于250μm的未溶解的无定形或部分无定形活性剂的稳定分散体的口服薄膜剂型保持均匀分布在膜基质内并含有至少一种 成膜聚合物和任选的药学上可接受的赋形剂，例如稀释剂，增塑剂，表面活性剂，甜味剂和掩味剂，通过包括首先提供具有平均颗粒的无定形颗粒形式的活性剂的方法制备 尺寸直径D50等于或小于250μm。 接下来，将活性剂悬浮在液体成膜剂中而不溶解活性剂。 因此，除去溶剂以形成膜。

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：US20190247505A1

公开(公告)日：2019-08-15

申请号：US16391430

申请日：2019-04-23

Applicant: Intelgenx Corp.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Billal Tir

IPC: A61K47/10 ,  A61K9/70 ,  A61K31/196 ,  A61K31/5513 ,  A61K9/00 ,  A61K31/4985 ,  A61K31/7076 ,  A61K31/704 ,  A61K31/60 ,  A61K31/58 ,  A61K31/573 ,  A61K31/5517 ,  A61K31/415 ,  A61K31/40 ,  A61K31/216

CPC classification number: A61K47/10 ,  A61K9/006 ,  A61K9/7007 ,  A61K31/196 ,  A61K31/216 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4985 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/573 ,  A61K31/58 ,  A61K31/60 ,  A61K31/704 ,  A61K31/7076 ,  A61K38/00

Abstract: Oral thin film dosage form of a stable dispersion of non-solubilized amorphous or partially amorphous active agent(s), having a mean particle size diameter D50 equal or less than 250 μm, that remains uniformly distributed within a film matrix and contains at least one film forming polymer, and optional pharmaceutically-acceptable excipients, such as diluents, plasticizers, surfactants, sweeteners, and taste-masking agent(s), are prepared by a process including first providing the active agent in an amorphous particle form having a mean particle size diameter D50 equal or less than 250 μm. Next, the active agent is suspended in a liquid film-forming formulation without dissolving the active agent. Therefore, the solvent is removed to form a film.

公开(公告)号：US20160243036A1

公开(公告)日：2016-08-25

申请号：US14630699

申请日：2015-02-25

Applicant: IntelGenx Corp.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Billal Tir

IPC: A61K9/00 ,  A61K31/4985 ,  A61K47/38 ,  A61K47/36 ,  A61K47/10 ,  A61K31/5513 ,  A61K9/70

CPC classification number: A61K47/10 ,  A61K9/006 ,  A61K9/7007 ,  A61K31/196 ,  A61K31/216 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4985 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/573 ,  A61K31/58 ,  A61K31/60 ,  A61K31/704 ,  A61K31/7076 ,  A61K38/00

Abstract: Oral thin film dosage form of a stable dispersion of non-solubilized amorphous or partially amorphous active agent(s), having a mean particle size diameter D50 equal or lower than 250 μm, that remains uniformly distributed within a film matrix and contains at least one film former polymer, and optional pharmaceutically-acceptable excipients, such as diluents, plasticizers, surfactants, sweeteners, and taste-masking agent(s). The oral thin film dosage exhibits increased solubility or rate of dissolution and enhanced bioavailability compared to a crystalline form of the active agent(s). The oral dosage form also exhibits long term stability confirmed by no changes in the dissolution profile over time.

Abstract translation: 平均粒度直径D50等于或低于250μm的非溶解无定形或部分无定形活性剂的稳定分散体的口服薄膜剂型，其保持均匀分布在膜基质内并含有至少一种 成膜剂聚合物和任选的药学上可接受的赋形剂，例如稀释剂，增塑剂，表面活性剂，甜味剂和掩味剂。 与活性剂的结晶形式相比，口服薄膜剂量显示增加的溶解度或溶解速率和增强的生物利用度。 口服剂型还显示长期稳定性，通过随时间的溶出曲线没有变化而证实。

公开(公告)号：US10828254B2

公开(公告)日：2020-11-10

申请号：US16146516

申请日：2018-09-28

Applicant: Intelgenx Corp.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Justin W. Conway ,  Billal Tir

IPC: A61K9/00 ,  A61K47/38 ,  A61K31/4985

Abstract: An oral film dosage form includes a high viscosity polymer in an amount of from 1% to 5% by dry weight to reduce, modulate and/or control Cmax of an active agent. The high viscosity polymer has a viscosity of from 100 cps to 500 cps as determined at 2% concentration in water by weight at 25° C. using a Brookfield LVF viscometer with spindle no. 2 at 60 rpm.

公开(公告)号：US20200101008A1

公开(公告)日：2020-04-02

申请号：US16146516

申请日：2018-09-28

Applicant: Intelgenx Corp.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Justin W. Conway ,  Billal Tir

IPC: A61K9/00 ,  A61K31/4985 ,  A61K47/38

Abstract: An oral film dosage form includes a high viscosity polymer in an amount of from 1% to 5% by dry weight to reduce, modulate and/or control Cmax of an active agent. The high viscosity polymer has a viscosity of from 100 cps to 500 cps as determined at 2% concentration in water by weight at 25° C. using a Brookfield LVF viscometer with spindle no. 2 at 60 rpm

公开(公告)号：US12156937B2

公开(公告)日：2024-12-03

申请号：US17952300

申请日：2022-09-25

Applicant: INTELGENX CORP.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Justin Conway ,  Billal Tir

IPC: A61K9/00 ,  A61K31/4985 ,  A61K47/38

Abstract: An oral film dosage form includes a high viscosity polymer in an amount of from 1% to 5% by dry weight to reduce, modulate and/or control Cmax of an active agent. The high viscosity polymer has a viscosity of from 100 cps to 500 cps as determined at 2% concentration in water by weight at 25° C. using a Brookfield LVF viscometer with spindle no. 2 at 60 rpm.

公开(公告)号：US20190231685A1

公开(公告)日：2019-08-01

申请号：US16261284

申请日：2019-01-29

Applicant: Intelgenx Corp.

Inventor： Nadine Paiement ,  Rodolphe Obeid ,  Billal Tir

IPC: A61K9/00 ,  A61K31/4402 ,  A61K31/138 ,  A61K47/12 ,  A61K47/38 ,  A61K47/32

CPC classification number: A61K9/0056 ,  A61K31/138 ,  A61K31/4402 ,  A61K47/12 ,  A61K47/32 ,  A61K47/38

Abstract: An oral film dosage form for administration in the buccal cavity includes a film layer containing a safe and effective amount of an antihistamine and 3% to 12% (w/w) of a numbness mitigating agent.