Transmucosal delivery system for idebenone

Patent metadata

Field	Value
Publication number	US-11547677-B2
Application number	US-201816490684-A
Country	US
Kind code	B2
Filing date	Feb 28, 2018
Priority date	Mar 1, 2017
Publication date	Jan 10, 2023
Grant date	Jan 10, 2023

Abstract

The invention relates to a transmucosal delivery system for idebenone, comprising an external phase, which contains at least one hydrophilic polymer, and an inner hydrophobic phase, which contains idebenone and at least one hydrophobic substance, wherein the inner hydrophobic phase is emulsified in the form of droplets in the external phase. The invention is characterized in that the inner hydrophobic phase is stabilized by at least one emulsifier in the external phase. The invention also relates to a method for producing the same and its use as a medicament.

First claim

The invention claimed is:

1. A transmucosal delivery system for idebenone, comprising an outer, hydrophilic, phase that makes up 20 to 70 wt. % of the total weight of the transmucosal delivery system for idebenone and which contains at least one hydrophilic polymer, and an inner, hydrophobic, phase which contains idebenone and at least one hydrophobic substance, wherein the at least one hydrophobic substance in the inner, hydrophobic, phase comprises methyl salicylate, tributyl citrate, triethyl citrate, eucalyptol, methyl salicylate, linoleic acid, oleic acid and/or mixtures thereof, wherein the inner, hydrophobic, phase is emulsified in the form of droplets in the outer phase, characterised in that the inner, hydrophobic, phase is stabilised by at least one emulsifier in the outer phase, wherein the at least one emulsifier comprises polysorbate, sorbitan esters, polyoxyethylene fatty acid ethers and/or mixtures thereof, and wherein the transmucosal delivery system for idebenone further comprises a vitamin E free-radical scavenger.

2. The transmucosal delivery system for idebenone according to claim 1 , characterised in that idebenone is present substantially in the inner, hydrophobic, phase.

3. The transmucosal delivery system for idebenone according to claim 1 , characterised in that idebenone is present dissolved in non-crystalline form.

4. The transmucosal delivery system for idebenone according to claim 1 , characterised in that idebenone is present in a pharmaceutically effective concentration below its saturation concentration.

5. The transmucosal delivery system for idebenone according to claim 1 , characterised in that the at least one hydrophilic polymer comprises polyvinyl alcohol, polyvinylpyrrolidone, a cellulose derivative and/or copolymers thereof.

6. The transmucosal delivery system for idebenone according to claim 1 , characterised in that the at least one hydrophobic substance in the inner, hydrophobic, phase has a logP value of greater than about 1.

7. The transmucosal delivery system for idebenone according to claim 1 , characterised in that the at least one emulsifier has an HLB value of 3 to 15.

8. The transmucosal delivery system for idebenone according to claim 1 , characterised in that the inner phase makes up 30 to 60 wt. %, relative to the total weight of the transmucosal delivery system for idebenone.

9. The transmucosal delivery system for idebenone according to claim 1 , characterised in that the emulsifier makes up 2 to 7 wt. %, relative to the total weight of the transmucosal delivery system for idebenone.

10. The transmucosal delivery system for idebenone according to claim 3 , characterised in that idebenone is substantially in the inner, hydrophobic, phase.

11. The transmucosal delivery system for idebenone according to claim 4 , characterised by a idebenone concentration which corresponds to 90% of the saturation concentration of idebenone in the at least one hydrophobic substance.

12. The transmucosal delivery system for idebenone according to claim 1 , wherein the at least one hydrophobic substance comprises at least one of methyl salicylate and eucalyptol.

Assignees

• Lts Lohmann Therapie Systeme Ag
• Santhera Pharmaceuticals Schweiz Ag

Inventors

• Linn Michael
• Muller Markus
• Bauer Marius

Classifications

• A61K9/113

  Multiple emulsions, e.g. oil-in-water-in-oil {(A61K9/0026 takes precedence)} · CPC title

• A61K31/122 Primary

  having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin · CPC title

• A61K9/006 Primary

  Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title