CA2362575A1 - Spray containing ubiquinone qn - Google Patents
Spray containing ubiquinone qn Download PDFInfo
- Publication number
- CA2362575A1 CA2362575A1 CA002362575A CA2362575A CA2362575A1 CA 2362575 A1 CA2362575 A1 CA 2362575A1 CA 002362575 A CA002362575 A CA 002362575A CA 2362575 A CA2362575 A CA 2362575A CA 2362575 A1 CA2362575 A1 CA 2362575A1
- Authority
- CA
- Canada
- Prior art keywords
- ubiquinone
- spray
- treatment
- spray according
- spray containing
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 title claims abstract description 18
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 title claims abstract description 15
- 239000007921 spray Substances 0.000 title claims abstract description 10
- 235000017471 coenzyme Q10 Nutrition 0.000 title abstract description 19
- NPCOQXAVBJJZBQ-UHFFFAOYSA-N reduced coenzyme Q9 Natural products COC1=C(O)C(C)=C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)C(O)=C1OC NPCOQXAVBJJZBQ-UHFFFAOYSA-N 0.000 title abstract description 12
- 229940035936 ubiquinone Drugs 0.000 title abstract description 12
- 208000002193 Pain Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 208000019695 Migraine disease Diseases 0.000 claims description 3
- 239000007922 nasal spray Substances 0.000 claims description 3
- 229940097496 nasal spray Drugs 0.000 claims description 3
- 230000001537 neural effect Effects 0.000 claims description 3
- 239000000668 oral spray Substances 0.000 claims description 3
- 229940041678 oral spray Drugs 0.000 claims description 3
- 208000007542 Paresis Diseases 0.000 claims description 2
- 208000028017 Psychotic disease Diseases 0.000 claims description 2
- 230000002490 cerebral effect Effects 0.000 claims description 2
- 238000001246 colloidal dispersion Methods 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 abstract 1
- 150000003669 ubiquinones Chemical class 0.000 description 7
- 239000002243 precursor Substances 0.000 description 6
- RRHGJUQNOFWUDK-UHFFFAOYSA-N Isoprene Chemical group CC(=C)C=C RRHGJUQNOFWUDK-UHFFFAOYSA-N 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 210000000653 nervous system Anatomy 0.000 description 2
- 229940005561 1,4-benzoquinone Drugs 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 108091006149 Electron carriers Proteins 0.000 description 1
- 102000004310 Ion Channels Human genes 0.000 description 1
- 108090000862 Ion Channels Proteins 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 206010027603 Migraine headaches Diseases 0.000 description 1
- 102000003797 Neuropeptides Human genes 0.000 description 1
- 108090000189 Neuropeptides Proteins 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
- 206010043269 Tension headache Diseases 0.000 description 1
- 208000008548 Tension-Type Headache Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 150000004648 butanoic acid derivatives Chemical class 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000003412 degenerative effect Effects 0.000 description 1
- 230000000037 effect on migraine Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 210000003470 mitochondria Anatomy 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 230000036542 oxidative stress Effects 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 150000004053 quinones Chemical class 0.000 description 1
- 230000035806 respiratory chain Effects 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000004102 tricarboxylic acid cycle Effects 0.000 description 1
- UIXPTCZPFCVOQF-UHFFFAOYSA-N ubiquinone-0 Chemical class COC1=C(OC)C(=O)C(C)=CC1=O UIXPTCZPFCVOQF-UHFFFAOYSA-N 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 230000007332 vesicle formation Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to the utilization of ubiquinone Qn together with comm on adjuvants as a spray.
Description
SMB
S~ray Containing Ubiquinone Q
Ubiquinones are prenylated quinones which are wide-spread in the animal and vegetable kingdoms. They are derivatives of 2,3-dimethoxy-5-methyl-1,4-benzoquinone having linearly linked isoprene units in the 6-position.
Depending on the number of isoprene units, the ubiquinones are designated as Q-1, Q-2, Q-3 etc. In most mammals including humans, Q-10 (2,3-dimethoxy-5-methyl-6-deca-prenyl-1,4-benzoquinone) is prevailing. Ubiquinones serve as electron carriers in the respiratory chain, and they participate in the cyclic oxidation and reduction of substrates in the citric acid cycle. Ubiquinones Q~ represent a precondition of the energy supply to all cells. The oxidative stress which arises, inter alia, from a high oxygen consumption causes damage to the membranes of mitochondria and cells which result in acute or degenerative disorders of the nervous system. The nervous system has a very high energy demand for the signal transduction by membrane potential build-up, ion-channel control, as well as by neuropeptide and neurotransmitter vesicle formation.
Ubiquinone Q-10 (also referred to as coenzyme Q-10) has previously been used in the therapy of heart diseases.
The subject matter of the invention is a spray containing ubiquinone Q~ or ubiquinone Q~ precursors together with usual auxiliaries.
The term "ubiquinone Q" precursors" refers to compounds which are converted to ubiquinone Q~ in the body. These include, on the one hand, the ubihydroquinones, which are in an equilibrium with the ubiquinones, as well as simple esters of the ubihydroquinones with short-chained carboxylic acids having from 1 to 10 carbon _2_ atoms, for example, acetate, propionate or butyrate esters. These precursors are converted to the corresponding ubiquinones after the application thereof.
Ubiquinone Q-10 is preferably used because this is the main ubiquinone in humans.
The spray according to the invention is preferably an oral or nasal spray, so that the administration of ubiquinone Q~ or ubiquinone Q" precursors can be effected on an inhalative or intranasal route. The spray according to the invention is useful, in particular, for the treatment of pain conditions as encountered in migraine and neuropathy, in neural disorders, such as depressions, psychoses, lack of concen-tration, and in neurodegenerative diseases, such as Alzheimer's, Parkinson's, Huntington's, multiple sclerosis and cerebral paresis. The application as an oral or nasal spray seems to accelerate the transport of ubiquinone Qn or its precursors through the blood-brain barrier. It was found that the oral administration of from 600 to 800 mg of Q-10 in the form of capsules exhibited virtually no effect on migraine, whereas a nasal formulation could effectively alleviate pain from migraine and tension headaches already at a low amount. Thus, doses of about 20 mg were sufFcient for a significant alleviation of pain. In principle, however, doses of as high as 1000 mg can be employed.
Ubiquinones are lipophilic substances which are virtually insoluble in water.
However, a particularly high effectiveness was found when the ubiquinone Q~ or its precursors are in aqueous dispersion. Aqueous colloidal dispersions are particularly preferred. The preparation of the corresponding dispersions is described in WO
95/05164 and in the related DE-A-43 27 063.
S~ray Containing Ubiquinone Q
Ubiquinones are prenylated quinones which are wide-spread in the animal and vegetable kingdoms. They are derivatives of 2,3-dimethoxy-5-methyl-1,4-benzoquinone having linearly linked isoprene units in the 6-position.
Depending on the number of isoprene units, the ubiquinones are designated as Q-1, Q-2, Q-3 etc. In most mammals including humans, Q-10 (2,3-dimethoxy-5-methyl-6-deca-prenyl-1,4-benzoquinone) is prevailing. Ubiquinones serve as electron carriers in the respiratory chain, and they participate in the cyclic oxidation and reduction of substrates in the citric acid cycle. Ubiquinones Q~ represent a precondition of the energy supply to all cells. The oxidative stress which arises, inter alia, from a high oxygen consumption causes damage to the membranes of mitochondria and cells which result in acute or degenerative disorders of the nervous system. The nervous system has a very high energy demand for the signal transduction by membrane potential build-up, ion-channel control, as well as by neuropeptide and neurotransmitter vesicle formation.
Ubiquinone Q-10 (also referred to as coenzyme Q-10) has previously been used in the therapy of heart diseases.
The subject matter of the invention is a spray containing ubiquinone Q~ or ubiquinone Q~ precursors together with usual auxiliaries.
The term "ubiquinone Q" precursors" refers to compounds which are converted to ubiquinone Q~ in the body. These include, on the one hand, the ubihydroquinones, which are in an equilibrium with the ubiquinones, as well as simple esters of the ubihydroquinones with short-chained carboxylic acids having from 1 to 10 carbon _2_ atoms, for example, acetate, propionate or butyrate esters. These precursors are converted to the corresponding ubiquinones after the application thereof.
Ubiquinone Q-10 is preferably used because this is the main ubiquinone in humans.
The spray according to the invention is preferably an oral or nasal spray, so that the administration of ubiquinone Q~ or ubiquinone Q" precursors can be effected on an inhalative or intranasal route. The spray according to the invention is useful, in particular, for the treatment of pain conditions as encountered in migraine and neuropathy, in neural disorders, such as depressions, psychoses, lack of concen-tration, and in neurodegenerative diseases, such as Alzheimer's, Parkinson's, Huntington's, multiple sclerosis and cerebral paresis. The application as an oral or nasal spray seems to accelerate the transport of ubiquinone Qn or its precursors through the blood-brain barrier. It was found that the oral administration of from 600 to 800 mg of Q-10 in the form of capsules exhibited virtually no effect on migraine, whereas a nasal formulation could effectively alleviate pain from migraine and tension headaches already at a low amount. Thus, doses of about 20 mg were sufFcient for a significant alleviation of pain. In principle, however, doses of as high as 1000 mg can be employed.
Ubiquinones are lipophilic substances which are virtually insoluble in water.
However, a particularly high effectiveness was found when the ubiquinone Q~ or its precursors are in aqueous dispersion. Aqueous colloidal dispersions are particularly preferred. The preparation of the corresponding dispersions is described in WO
95/05164 and in the related DE-A-43 27 063.
Claims (5)
1. A spray containing ubiquinone Q-10 as an aqueous colloidal dispersion together with usual auxiliaries.
2. The spray according to claim 1, characterized by being an oral or nasal spray.
3. Use of the spray according to any of claims 1 or 2 for the treatment of pain conditions from neural disorders, especially in migraine and neuropathy.
4. Use of the spray according to any of claims 1 or 2 for the treatment of neural disorders such as depressions, psychoses, lack of concentration.
5. Use of the spray according to any of claims 1 or 2 for the treatment of neurodegenerative diseases, such as Alzheimer's, Parkinson's, Huntington's, multiple sclerosis and cerebral paresis.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19905880A DE19905880A1 (en) | 1999-02-11 | 1999-02-11 | Spray containing ubiquinone Qn |
| DE19905880.6 | 1999-02-11 | ||
| PCT/EP2000/001012 WO2000047185A1 (en) | 1999-02-11 | 2000-02-09 | SPRAY CONTAINING UBIQUINONE Q¿n? |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2362575A1 true CA2362575A1 (en) | 2000-08-17 |
Family
ID=7897296
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002362575A Abandoned CA2362575A1 (en) | 1999-02-11 | 2000-02-09 | Spray containing ubiquinone qn |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP1150657B1 (en) |
| AT (1) | ATE249204T1 (en) |
| CA (1) | CA2362575A1 (en) |
| DE (2) | DE19905880A1 (en) |
| ES (1) | ES2206196T3 (en) |
| WO (1) | WO2000047185A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7754205B2 (en) | 2001-05-10 | 2010-07-13 | Kaneka Corporation | Composition for transmucosal administration containing conenzyme Q as the active ingredient |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19905879A1 (en) * | 1999-02-11 | 2000-08-17 | Mse Pharmazeutika Gmbh | Ubiquinon Qn used to treat pain |
| JP2003026567A (en) * | 2001-05-10 | 2003-01-29 | Kanegafuchi Chem Ind Co Ltd | Composition for mucosal administration containing coenzyme Q as active ingredient |
| US6747090B2 (en) | 2001-07-16 | 2004-06-08 | Pharmacia Groningen Bv | Compositions capable of forming hydrogels in the eye |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5938203B2 (en) * | 1976-04-26 | 1984-09-14 | エーザイ株式会社 | A therapeutic agent for cerebral circulation disorders whose main ingredient is coenzyme Q. |
| FR2703591B1 (en) * | 1993-04-06 | 1995-06-02 | Sederma Sa | Cosmetic and dermopharmaceutical and / or dietetic compositions containing coenzyme A associated with coenzyme Q10. |
| DE4327063A1 (en) * | 1993-08-12 | 1995-02-16 | Kirsten Dr Westesen | Ubidecarenone particles with modified physicochemical properties |
| AU4510596A (en) * | 1994-12-06 | 1996-06-26 | National Research Council Of Canada | Water soluble ubiquinone compositions, prodrugs, and methods relating thereto |
| US5660835A (en) * | 1995-02-24 | 1997-08-26 | East Carolina University | Method of treating adenosine depletion |
| GB9601398D0 (en) * | 1996-01-24 | 1996-03-27 | Piper Edwina M | Composition |
| US5891465A (en) * | 1996-05-14 | 1999-04-06 | Biozone Laboratories, Inc. | Delivery of biologically active material in a liposomal formulation for administration into the mouth |
-
1999
- 1999-02-11 DE DE19905880A patent/DE19905880A1/en not_active Withdrawn
-
2000
- 2000-02-09 DE DE50003634T patent/DE50003634D1/en not_active Expired - Fee Related
- 2000-02-09 CA CA002362575A patent/CA2362575A1/en not_active Abandoned
- 2000-02-09 WO PCT/EP2000/001012 patent/WO2000047185A1/en not_active Ceased
- 2000-02-09 ES ES00907522T patent/ES2206196T3/en not_active Expired - Lifetime
- 2000-02-09 AT AT00907522T patent/ATE249204T1/en not_active IP Right Cessation
- 2000-02-09 EP EP00907522A patent/EP1150657B1/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7754205B2 (en) | 2001-05-10 | 2010-07-13 | Kaneka Corporation | Composition for transmucosal administration containing conenzyme Q as the active ingredient |
Also Published As
| Publication number | Publication date |
|---|---|
| ATE249204T1 (en) | 2003-09-15 |
| DE50003634D1 (en) | 2003-10-16 |
| WO2000047185A1 (en) | 2000-08-17 |
| ES2206196T3 (en) | 2004-05-16 |
| EP1150657B1 (en) | 2003-09-10 |
| EP1150657A1 (en) | 2001-11-07 |
| DE19905880A1 (en) | 2000-08-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |