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Idebenone composition for the treatment of neurological disorders

A technique for neurological disorders and compositions, applied in the field of stable preparations of idebenone, capable of solving problems such as low solubility

Inactive Publication Date: 2010-06-16
ALPHARX
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solubility of idebenone in fixed oils (soybean oil, corn oil, almond oil, etc.) is low and the drug precipitates from these emulsions during storage, which limits their use in the preparation of said drug. Use in an emulsion based injectable form

Method used

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  • Idebenone composition for the treatment of neurological disorders
  • Idebenone composition for the treatment of neurological disorders
  • Idebenone composition for the treatment of neurological disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-10

[0031] Examples 1-10: Oil-in-Water Emulsions of Idebenone

Embodiment 1

[0032] Example 1. Preparation of injectable idebenone o / w (oil-in-water) emulsion

[0033] The oil components of the formulation (Capric / caprylic triglyceride, acetylated monoglyceride and D-alpha-tocopherol USP) were combined with lecithin and ethoxylated castor oil and mixed for 1 hour at 40°C. Idebenone was dissolved in a warm oil and surfactant mixture and then mixed with water, Aqueous blend of EDTA and glycerin. The resulting emulsion is subjected to a high-pressure homogenizer (eg Avestin TM Emulsiflex C5) was treated 3-5 times. After cooling to room temperature, the emulsion was aseptically filtered through a sterile microporous membrane filter (0.2 μm or 0.45 μm) and dispensed into sterile glass vials. Store the sealed vial in the refrigerator or at room temperature protected from light.

[0034] The HPLC method was used to test the content of idebenone in the preparation.

[0035] The o / w emulsions loaded with idebenone of Examples 2-10 were prepared in a simil...

Embodiment 11

[0040] The idebenone-loaded emulsions of Examples 11-16 with increased oil phase content were prepared by high pressure homogenization, or by idebenone in a mixture of oil, surfactant and stabilizer after addition to the aqueous phase The solution was prepared by spontaneous emulsification without a homogenization step. For Example 11, idebenone was dissolved in acetylated monoglycerides (Myvacet TM 9-45K) and slightly heated (50-55°C) in an oily mixture of D-alpha-tocopheryl polyethylene glycol 1000 succinate (D-alpha tocopheryl polyethyleneglycol 1000succinate, vitamin E (TPGS) surfactant and soy lecithin. Add propylene glycol to the warm solution, then add the water phase heated to 65-70°C and mix with the oily composition at low speed using a propeller mixer to avoid foaming. Examples 13 and 15 were prepared in the same manner as Example 11, while Examples 12, 14 and 16 were treated with a high pressure homogenizer. The formed oil-in-water emulsion was passed through a...

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Abstract

The invention describes the use of an injectable form of Idebenone to induce protect from neuronal damage, improve recovery after brain trauma; stroke, intoxication, neurodegenerative diseases, memory loss or neuropathology associated with neuroinflammation or infection damage and to restore cognitive function, suppress disorientation, alcoholic and drug abuse associated syndromes and other signs of neuronal damage.

Description

technical field [0001] The present invention relates to the field of preparing stable formulations of idebenone suitable for parenteral administration. Existing oral dosage forms of idebenone, which are associated with hypermetabolism occurring in the liver ("first-pass effect"), cannot be administered in acute situations or while the patient is unconscious. An injectable form of idebenone is therefore highly desirable. Background technique [0002] Neuronal damage, neurodegenerative diseases and syndromes (Alzheimer's disease, multiple sclerosis, Friedrich's ataxia, brain and spinal cord injuries and neurotrauma, stroke, Parkinson's disease, alcoholism and narcolepsy, postoperative recovery syndrome, and postanesthesia recovery syndrome) and many other conditions require effective treatment and prevention [1]. [0003] Postoperative stroke and cognitive deficit (POSCD) syndrome is common, especially in older adults who have undergone extensive surgical procedures such as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P25/00A61P9/10A61P25/28A61P25/32A61P25/30
CPCA61K9/0019A61K47/14A61K31/122A61K47/44A61K9/1075A61P25/00A61P25/28A61P25/30A61P25/32A61P31/00A61P9/10
Inventor 约瑟夫·施瓦茨迈克尔·韦斯帕皮尔
Owner ALPHARX
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