Oral thin film with high active agent loading

Patent metadata

Field	Value
Publication number	US-12527751-B2
Application number	US-201816770501-A
Country	US
Kind code	B2
Filing date	Dec 6, 2018
Priority date	Dec 6, 2017
Publication date	Jan 20, 2026
Grant date	Jan 20, 2026

Abstract

The present invention relates to an oral thin film comprising at least one cellulose derivative and at least one pharmaceutically active agent, the at least one pharmaceutically active agent having a water solubility of at most 50 g/L at 20° C. and a pH of 6 to 7 and being contained in the oral thin film in an amount of at least 20 wt. % in relation to the total weight of the oral thin film, and to a method for production of said oral thin film, and use thereof as a medicament.

First claim

The invention claimed is:

1 . An oral thin film comprising at least one cellulose derivative and at least one pharmaceutically active agent, characterised in that the at least one pharmaceutically active agent comprises ketamine or a pharmaceutically acceptable salt thereof and is contained in the oral thin film in an amount of at least approximately 20 wt. % in relation to the total weight of the oral thin film and wherein the oral thin film has a disintegration time of less than 41 seconds and wherein the at least one cellulose derivative comprises a mixture of two hydroxypropyl methylcelluloses having different viscosities.

2 . The oral thin film according to claim 1 , characterised in that the at least one cellulose derivative is contained in the oral thin film in an amount of approximately 5 to 80 wt. % in relation to the total weight of the oral thin film.

3 . The oral thin film according to claim 1 , characterised in that the at least one cellulose derivative comprises a water-soluble and/or water-swellable cellulose derivative.

4 . The oral thin film according to claim 1 , characterised in that the at least one pharmaceutically active agent has a molecular weight of at most approximately 1000 g/mol.

5 . The oral thin film according to claim 1 , characterised in that the at least one pharmaceutically active agent comprises(S) ketamine or a pharmaceutically acceptable salt thereof.

6 . The oral thin film according to claim 1 , characterised in that the oral thin film further comprises at least one auxiliary selected from the group comprising colouring agents, flavourings, sweeteners, taste-masking agents, emulsifiers, enhancers, pH regulators, humectants, preservatives and/or antioxidants.

7 . The oral thin film according to claim 1 , characterised in that the mass per unit area of the oral thin film is approximately 50 to 300 g/m 2 .

8 . A medicament for reducing a risk of suicide comprising the oral thin film of claim 1 .

9 . The oral thin film according to claim 1 , characterised in that the at least one pharmaceutically active agent has a molecular weight of at most approximately 500 g/mol.

10 . The oral thin film according to claim 1 wherein the ratio of a lower viscosity hydroxypropyl methylcellulose to a higher viscosity hydroxypropyl methylcellulose is approximately 1:5 to 5:1.

11 . The oral thin film according to claim 1 wherein the pharmaceutically active agent is contained in an amount of at least 40 wt. %.

12 . The oral thin film according to claim 1 wherein the at least one cellulose derivative is contained in the oral thin film in an amount of approximately 20 to 60 wt. %.

13 . The oral thin film according to claim 6 wherein the auxiliary is contained in the oral thin film in an amount of approximately 0.1 to 10 wt. %.

14 . The oral thin film according to claim 1 wherein the at least one hydroxypropyl methylcellulose has a viscosity of approximately 1 to 5 mPas.

15 . The oral thin film according to claim 14 wherein the other at least one hydroxypropyl methylcellulose has a viscosity of approximately 40 to 60 mPas.

16 . The oral thin film according to claim 15 wherein the at least one hydroxypropyl methylcellulose comprises about 35 to 40 wt. %.

17 . The oral thin film according to claim 16 wherein the other at least one hydroxypropyl methylcellulose comprises about 5 to 15 wt. %.

18 . The oral thin film according to claim 17 including about 40 to 45 wt. %. (S) Ketamine.

Assignees

• Lts Lohmann Therapie Systeme Ag

Inventors

• Schmitz Christoph
• Müller Markus
• Bauer Marius
• Linn Michael

Classifications

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K9/7007

  Drug-containing films, membranes or sheets (A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence) · CPC title

• A61K9/0056

  Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61K31/135 Primary

  having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} · CPC title