EP-4739284-A1 - AN ADHESIVE ORAL DISC FOR SUSTAINED RELEASE OF CANNABINOIDS

Abstract

The present invention relates to an adhesive oral disc for sustained release of cannabinoids. The disc comprises one or more cannabinoids and being composed of at least a mucosal contacting layer having a mucosal contacting surface operable to be fixed to the gingiva of a person in need of alleviation or treatment of a medical condition, where the mucosal contacting layer comprising one or more mucoadhesive polymers allowing the adhesive oral disc to adhere to the gingiva for an extended period of time. Further, the disc comprises a non-mucoadhesive module fused to the mucosal contacting layer, where the non-mucoadhesive module comprising a solid tablet composition allowing the non-mucoadhesive module to dissolve within an extended period of time upon adhesion of the adhesive oral disc to the gingiva. The invention is particularly useful for alleviation or treatment of ulcers.

Inventors

• WITTORFF, HELLE
• JENSEN, SANNE SKOV
• NIKOLAJSEN, Gitte Nykjær
• DAWSON, GORDON FINDLAY

Assignees

• Fertin Pharma A/S

Dates

Publication Date

20260513

Application Date

20240708

Claims (20)

1. 1. An adhesive oral disc for sustained release of cannabinoids, the disc comprising one or more cannabinoids and being composed of at least: a mucosal contacting layer having a mucosal contacting surface operable to be fixed to the gingiva of a person in need of alleviation or treatment of a medical condition, the mucosal contacting layer comprising one or more mucoadhesive polymers allowing the adhesive oral disc to adhere to the gingiva for an extended period of time; and a non-mucoadhesive module fused to the mucosal contacting layer, the non- mucoadhesive module comprising a solid tablet composition allowing the non- mucoadhesive module to dissolve within an extended period of time upon adhesion of the adhesive oral disc to the gingiva.
2. 2. The adhesive oral disc according to claim 1, wherein the solid tablet composition comprises one or more separate binders, such as one or more separate cellulose derivative binders.
3. 3. The adhesive oral disc according to any one of claims 1-2, wherein the solid tablet composition comprises one or more separate binders in an amount of 1 to 15% by weight of the non-mucoadhesive module.
4. 4. The adhesive oral disc according to any one of claims 1-3, wherein the solid tablet composition comprises one or more separate binders in an amount of 2 to 10% by weight of the non-mucoadhesive module.
5. 5. The adhesive oral disc according to any one of claims 1-4, wherein the solid tablet composition comprises one or more separate binders in an amount of 4 to 8% by weight of the non-mucoadhesive module.
6. 6. The adhesive oral disc according to any one of claims 1-5, wherein the solid tablet composition comprises one or more separate binders selected from the group consisting of cellulose, carboxymethylcellulose, ethylcellulose, hydroxyethyl cellulose, hydroxyethyl methyl cellulose, hydroxypropyl cellulose, methylcellulose, hydroxypropyl methylcellulose, microcrystalline cellulose, and any combination thereof.
7. 7. The adhesive oral disc according to any one of claims 1-6, wherein the solid tablet composition comprises one or more separate cellulose derivative binders selected from the group consisting of carboxymethylcellulose, ethylcellulose, hydroxyethyl cellulose, hydroxyethyl methyl cellulose, hydroxypropyl cellulose, methylcellulose, hydroxypropyl methylcellulose, microcrystalline cellulose, and any combination thereof.
8. 8. The adhesive oral disc according to any one of claims 1-7, wherein the solid tablet composition comprises one or more separate binders selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose, and any combination thereof.
9. 9. The adhesive oral disc according to any one of claims 1-8, wherein the solid tablet composition comprises hydroxypropyl cellulose.
10. 10. The adhesive oral disc according to any one of claims 1-8, wherein the solid tablet composition comprises hydroxypropyl methylcellulose.
11. 11. The adhesive oral disc according to any one of claims 1-10, wherein the solid tablet composition comprises one or more sugar alcohol particles.
12. 12. The adhesive oral disc according to any one of claims 1-11, wherein the solid tablet composition comprises one or more sugar alcohol particles in an amount of at least 40% by weight of the non-mucoadhesive module.
13. 13. The adhesive oral disc according to any one of claims 1-12, wherein the solid tablet composition comprises one or more sugar alcohol particles in an amount of at least 60% by weight of the non-mucoadhesive module.
14. 14. The adhesive oral disc according to any one of claims 1-13, wherein the solid tablet composition comprises one or more sugar alcohol particles in an amount of at least 80% by weight of the non-mucoadhesive module.
15. 15. The adhesive oral disc according to any one of claims 1-14, wherein the solid tablet composition comprises one or more sugar alcohol particles selected from the group consisting of xylitol, maltitol, mannitol, erythritol, isomalt, sorbitol, lactitol, and any combination thereof.
16. 16. The adhesive oral disc according to any one of claims 1-15, wherein the solid tablet composition does not comprise a flavoring agent.
17. 17. The adhesive oral disc according to any one of claims 1-16, wherein the solid tablet does not comprise an edible alcohol, such as not comprising an edible alcohol in the non-mucoadhesive module.
18. 18. The adhesive oral disc according to any one of claims 1-17, wherein the solid tablet composition comprises one or more cannabinoids.
19. 19. The adhesive oral disc according to any one of claims 1-18, wherein the solid tablet composition comprises one or more cannabinoids in an amount of 1 to 100 mg.
20. 20. The adhesive oral disc according to any one of claims 1-19, wherein the solid tablet composition comprises one or more cannabinoids in an amount of 2 to 50 mg.

Description

AN ADHESIVE ORAL DISC FOR SUSTAINED RELEASE OF CANNABINOIDS FIELD OF INVENTION The present invention relates to an adhesive oral disc suitable for oral administration of cannabinoids. Particularly, the invention is useful for sustained release of cannabinoids and for alleviation or treatment of medical indications, such as oral medical indications. BACKGROUND Cannabinoids are a group of chemicals found in Cannabis sativa, Cannabis indica, Cannabis ruderalis, Marijuana plant and related plant species. They are known to activate cannabinoid receptors (CB1 and CB2). These chemicals are also produced endogenously in humans and other animals. Cannabinoids are cyclic molecules exhibiting particular properties such as being lipophilic, have the ability to easily cross the blood-brain barrier, and having low toxicity. Cannabis sativa contains more than 400 chemicals and approximately 120 cannabinoids, the active constituents of cannabis, including tetrahydrocannabinol (THC), cannabidiol (CBD), cannabinol (CBN), tetrahydrocannabivarin (THCV) and cannabigerol (CBG). Pharmacologically, the principal psychoactive constituent of cannabis is tetrahydrocannabinol (THC), which is used for treating a wide range of medical conditions, including glaucoma, AIDS wasting, neuropathic pain, treatment of spasticity associated with multiple sclerosis, fibromyalgia, and chemotherapy- induced nausea. THC is also effective in the treatment of allergies, inflammation, infection, depression, migraine, bipolar disorders, anxiety disorder, drug dependency and drug withdrawal syndromes. Various attempts have been made to formulate tablets for oral delivery of cannabinoids, such as cannabidiol (CBD). However, various challenges are associated with providing prolonged delivery of the active and at the same time keep a safe and convenient delivery. This is particularly important when the medical indication is present as a local medical indication in the oral cavity, such as ulcers, gingivitis, and the like. In these cases, it may be advantageous to provide a local delivery of cannabinoids, such as cannabidiol, with a sustained release of the active that is targeted to the medical indication. Various conventional tablets have been provided in the art that serve to release cannabinoids to the oral cavity in a broad sense. However, these tablets generally fail to deliver cannabinoids to local targets in the oral cavity with an improved release time, such as a sustained release time, to obtain optimal conditions for alleviation or treatment of medical indications, such as ulcers. In some cases, various oral disorders may be found as local disorders in the oral cavity, such as ulcers. By targeting alleviation or treatment to these places in the oral cavity, the active may be applied in an increased concentration and/or applied with a higher precision in terms of release time suitable for alleviation or treatment of the condition. Furthermore, it is important that a formulation is provided that may also help in obtaining increased convenience and effectiveness. In general, less attention is given in the prior art on the impact of the formulation of the oral delivery platform for the sensorics properties of oral cannabinoid delivery. These properties are both relevant from a convenience perspective for oral administration, but certainly also in order to support an appropriate delivery of cannabinoids and avoid adverse side effects of cannabinoids. Hence, there is a need in the prior art for improved delivery vehicles that solve the above-referenced challenges and problems of the prior art. In particular, there is a need in the prior art for new delivery vehicles that support appropriate sustained delivery of cannabinoids combined with beneficial sensorics properties. Also, there is a need in the prior art for new delivery vehicles that support local administration of cannabinoids combined with optimized release time of the actives. SUMMARY Accordingly, in a first aspect of the invention, there is provided an adhesive oral disc for sustained release of cannabinoids, the disc comprising one or more cannabinoids and being composed of at least: a mucosal contacting layer having a mucosal contacting surface operable to be fixed to the gingiva of a person in need of alleviation or treatment of a medical condition, the mucosal contacting layer comprising one or more mucoadhesive polymers allowing the adhesive oral disc to adhere to the gingiva for an extended period of time; and a non-mucoadhesive module fused to the mucosal contacting layer, the non-mucoadhesive module comprising a solid tablet composition allowing the non-mucoadhesive module to dissolve within an extended period of time upon adhesion of the adhesive oral disc to the gingiva. In a second aspect, there is provided an adhesive oral disc for sustained release of cannabinoids, the disc comprising one or more cannabinoids and being composed of at least: a mucosal contacting layer having a