Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10- hydroxydecy l)-1,4-benzoquinone

A technique for mucosal administration of idebenone, applied in the field of mucosal administration of 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1,4-benzoquinone

Active Publication Date: 2009-09-23
SANTHERA PHARMA SCHWEIZ
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dermal route of administration has strong limitations regarding dosing, patient compliance, and dose accuracy for systemic applications

Method used

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  • Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10- hydroxydecy l)-1,4-benzoquinone
  • Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10- hydroxydecy l)-1,4-benzoquinone
  • Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10- hydroxydecy l)-1,4-benzoquinone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] microemulsion

[0035] Table 1

[0036] Element

[0037] Preparation: Preheat TPGS (tocopherol-polyethylene glycol-400-succinate) to about 60°C. Miglyol 812N and idebenone were mixed and sonicated for approximately 10 minutes until the material was completely dissolved (clear orange solution). Molten TPGS was added to the Miglyol / idebenone solution and stirred. The mixture is diluted and homogenized until a homogeneous emulsion is obtained.

Embodiment 2

[0039] sublingual lozenge

[0040] Table 2

[0041] Element

[0042] Preparation: Idebenone, lactose monohydrate, flavor and aspartame were mixed in a high shear mixer until a homogeneous mixture was obtained. Povidone was dissolved in water (approximately 8-10% solution) and added to the dry mix and granulated. The wet granulation is dried in a fluid bed drier, sieved and added to a premix of microcrystalline cellulose, magnesium stearate and talc. The final blend is compressed into tablets.

Embodiment 3

[0044] spray preparation

[0045] table 3

[0046] Element

[0047] Preparation: 10 g of idebenone was dissolved in 500 ml of ethanol (96%) and mixed with 400 ml of pure water. Methylparaben, propylparaben and aspartame were dissolved in the mixture. Adjust the final volume to 1000ml with purified water. The solution is filtered and filled into a suitable spray device.

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Abstract

Use of idebenone for the preparation of a medicament for transmucosal administration.

Description

technical field [0001] The present invention relates to medicaments for the mucosal administration of 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1,4-benzoquinone (idebenone). Background technique [0002] Idebenone is a synthetic analogue of coenzyme Q10 (CoQ10), an important cell membrane antioxidant and an essential component of adenosine triphosphate (ATP) generating the mitochondrial electron transport chain (ETC). To date, idebenone has been used in various medical applications. Similar to coenzyme Q10, idebenone undergoes a reduction / oxidation cycle in living organisms, and reduced idebenone is an antioxidant and free radical scavenger (A.Mordente, G.E.Martorana, G.Minotti, B.Giardina, Chem. Res. Toxicol. 11 (1998), 54-63). Idebenone is known to protect cell membranes and mitochondria from oxidative damage due to its ability to inhibit lipid peroxidation (M.Suno, M.Shibota, A.Nagaoka, Arch.Gerontol.Geriatr.8(1989), 307 -311). Idebenone also reacts with ETC, preserv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P25/00A61P25/16A61P25/28A61P21/00
CPCA61K31/122A61P21/00A61P21/04A61P25/00A61P25/16A61P25/28A61P27/02A61P3/00A61P3/12A61P39/06A61P43/00A61P9/00A61P9/10
Inventor 朱迪斯·杜巴赫-鲍威尔鲁道夫·豪斯曼皮埃尔·万坎
Owner SANTHERA PHARMA SCHWEIZ
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