WO2007045407A2 - Nutraceutical and pharmaceutical compositions containing choline as adiuvants for the prevention and treatment of retinopathies and glaucoma - Google Patents
Nutraceutical and pharmaceutical compositions containing choline as adiuvants for the prevention and treatment of retinopathies and glaucoma Download PDFInfo
- Publication number
- WO2007045407A2 WO2007045407A2 PCT/EP2006/009926 EP2006009926W WO2007045407A2 WO 2007045407 A2 WO2007045407 A2 WO 2007045407A2 EP 2006009926 W EP2006009926 W EP 2006009926W WO 2007045407 A2 WO2007045407 A2 WO 2007045407A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- choline
- compositions according
- treatment
- nutraceutical
- prevention
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 19
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 title claims abstract description 15
- 229960001231 choline Drugs 0.000 title claims abstract description 15
- 208000010412 Glaucoma Diseases 0.000 title claims abstract description 14
- 230000002265 prevention Effects 0.000 title claims abstract description 14
- 206010038923 Retinopathy Diseases 0.000 title claims abstract description 10
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 9
- 239000002417 nutraceutical Substances 0.000 title claims abstract description 8
- 235000021436 nutraceutical agent Nutrition 0.000 title claims abstract description 8
- 235000021122 unsaturated fatty acids Nutrition 0.000 claims abstract description 10
- 150000004670 unsaturated fatty acids Chemical class 0.000 claims abstract description 10
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 9
- 239000000203 mixture Substances 0.000 claims description 25
- 235000006708 antioxidants Nutrition 0.000 claims description 8
- REFJWTPEDVJJIY-UHFFFAOYSA-N Quercetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 REFJWTPEDVJJIY-UHFFFAOYSA-N 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 229920002770 condensed tannin Polymers 0.000 claims description 5
- 150000003248 quinolines Chemical class 0.000 claims description 5
- OHCQJHSOBUTRHG-KGGHGJDLSA-N FORSKOLIN Chemical compound O=C([C@@]12O)C[C@](C)(C=C)O[C@]1(C)[C@@H](OC(=O)C)[C@@H](O)[C@@H]1[C@]2(C)[C@@H](O)CCC1(C)C OHCQJHSOBUTRHG-KGGHGJDLSA-N 0.000 claims description 4
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims description 4
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 claims description 4
- QWJSAWXRUVVRLH-UHFFFAOYSA-M choline bitartrate Chemical compound C[N+](C)(C)CCO.OC(=O)C(O)C(O)C([O-])=O QWJSAWXRUVVRLH-UHFFFAOYSA-M 0.000 claims description 4
- 229960004874 choline bitartrate Drugs 0.000 claims description 4
- 229960001284 citicoline Drugs 0.000 claims description 4
- 229930003935 flavonoid Natural products 0.000 claims description 4
- 235000017173 flavonoids Nutrition 0.000 claims description 4
- 150000002215 flavonoids Chemical class 0.000 claims description 4
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims description 4
- 235000005875 quercetin Nutrition 0.000 claims description 4
- 229960001285 quercetin Drugs 0.000 claims description 4
- 239000004381 Choline salt Substances 0.000 claims description 3
- JAZBEHYOTPTENJ-JLNKQSITSA-N all-cis-5,8,11,14,17-icosapentaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O JAZBEHYOTPTENJ-JLNKQSITSA-N 0.000 claims description 3
- 235000019417 choline salt Nutrition 0.000 claims description 3
- 235000020669 docosahexaenoic acid Nutrition 0.000 claims description 3
- 235000020673 eicosapentaenoic acid Nutrition 0.000 claims description 3
- 229960005135 eicosapentaenoic acid Drugs 0.000 claims description 3
- JAZBEHYOTPTENJ-UHFFFAOYSA-N eicosapentaenoic acid Natural products CCC=CCC=CCC=CCC=CCC=CCCCC(O)=O JAZBEHYOTPTENJ-UHFFFAOYSA-N 0.000 claims description 3
- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 claims description 2
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims description 2
- SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 claims description 2
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 claims description 2
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims description 2
- ZVOLCUVKHLEPEV-UHFFFAOYSA-N Quercetagetin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=C(O)C(O)=C(O)C=C2O1 ZVOLCUVKHLEPEV-UHFFFAOYSA-N 0.000 claims description 2
- HWTZYBCRDDUBJY-UHFFFAOYSA-N Rhynchosin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=CC(O)=C(O)C=C2O1 HWTZYBCRDDUBJY-UHFFFAOYSA-N 0.000 claims description 2
- 235000014787 Vitis vinifera Nutrition 0.000 claims description 2
- 240000006365 Vitis vinifera Species 0.000 claims description 2
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 2
- 229940114079 arachidonic acid Drugs 0.000 claims description 2
- 235000021342 arachidonic acid Nutrition 0.000 claims description 2
- 239000011324 bead Substances 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- SGMZJAMFUVOLNK-UHFFFAOYSA-M choline chloride Chemical group [Cl-].C[N+](C)(C)CCO SGMZJAMFUVOLNK-UHFFFAOYSA-M 0.000 claims description 2
- AGVAZMGAQJOSFJ-WZHZPDAFSA-M cobalt(2+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+2].N#[C-].[N-]([C@@H]1[C@H](CC(N)=O)[C@@]2(C)CCC(=O)NC[C@@H](C)OP(O)(=O)O[C@H]3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)\C2=C(C)/C([C@H](C\2(C)C)CCC(N)=O)=N/C/2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O AGVAZMGAQJOSFJ-WZHZPDAFSA-M 0.000 claims description 2
- OHCQJHSOBUTRHG-UHFFFAOYSA-N colforsin Natural products OC12C(=O)CC(C)(C=C)OC1(C)C(OC(=O)C)C(O)C1C2(C)C(O)CCC1(C)C OHCQJHSOBUTRHG-UHFFFAOYSA-N 0.000 claims description 2
- 229910052802 copper Inorganic materials 0.000 claims description 2
- 239000010949 copper Substances 0.000 claims description 2
- 229940090949 docosahexaenoic acid Drugs 0.000 claims description 2
- 229960000304 folic acid Drugs 0.000 claims description 2
- 235000019152 folic acid Nutrition 0.000 claims description 2
- 239000011724 folic acid Substances 0.000 claims description 2
- 239000000499 gel Substances 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 235000002532 grape seed extract Nutrition 0.000 claims description 2
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 claims description 2
- 229960000367 inositol Drugs 0.000 claims description 2
- MWDZOUNAPSSOEL-UHFFFAOYSA-N kaempferol Natural products OC1=C(C(=O)c2cc(O)cc(O)c2O1)c3ccc(O)cc3 MWDZOUNAPSSOEL-UHFFFAOYSA-N 0.000 claims description 2
- AGBQKNBQESQNJD-UHFFFAOYSA-M lipoate Chemical compound [O-]C(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-M 0.000 claims description 2
- 235000019136 lipoic acid Nutrition 0.000 claims description 2
- 235000012680 lutein Nutrition 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims description 2
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 claims description 2
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims description 2
- 235000003687 soy isoflavones Nutrition 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 239000000725 suspension Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 229960002663 thioctic acid Drugs 0.000 claims description 2
- KBPHJBAIARWVSC-XQIHNALSSA-N trans-lutein Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C(=CC(O)CC2(C)C)C KBPHJBAIARWVSC-XQIHNALSSA-N 0.000 claims description 2
- 239000011715 vitamin B12 Substances 0.000 claims description 2
- 239000011726 vitamin B6 Substances 0.000 claims description 2
- 229910052725 zinc Inorganic materials 0.000 claims description 2
- 239000011701 zinc Substances 0.000 claims description 2
- 235000016804 zinc Nutrition 0.000 claims description 2
- RZZPDXZPRHQOCG-OJAKKHQRSA-M CDP-choline(1-) Chemical group O[C@@H]1[C@H](O)[C@@H](COP([O-])(=O)OP([O-])(=O)OCC[N+](C)(C)C)O[C@H]1N1C(=O)N=C(N)C=C1 RZZPDXZPRHQOCG-OJAKKHQRSA-M 0.000 claims 1
- 235000010208 anthocyanin Nutrition 0.000 claims 1
- 239000004410 anthocyanin Substances 0.000 claims 1
- 229930002877 anthocyanin Natural products 0.000 claims 1
- 150000004636 anthocyanins Chemical class 0.000 claims 1
- 239000001656 lutein Substances 0.000 claims 1
- 229960005375 lutein Drugs 0.000 claims 1
- KBPHJBAIARWVSC-RGZFRNHPSA-N lutein Chemical compound C([C@H](O)CC=1C)C(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\[C@H]1C(C)=C[C@H](O)CC1(C)C KBPHJBAIARWVSC-RGZFRNHPSA-N 0.000 claims 1
- ORAKUVXRZWMARG-WZLJTJAWSA-N lutein Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C)C=CC=C(/C)C=CC2C(=CC(O)CC2(C)C)C ORAKUVXRZWMARG-WZLJTJAWSA-N 0.000 claims 1
- FJHBOVDFOQMZRV-XQIHNALSSA-N xanthophyll Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C=C(C)C(O)CC2(C)C FJHBOVDFOQMZRV-XQIHNALSSA-N 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 abstract description 11
- 206010012689 Diabetic retinopathy Diseases 0.000 abstract description 7
- 239000002671 adjuvant Substances 0.000 abstract description 4
- 208000002780 macular degeneration Diseases 0.000 description 12
- 238000009472 formulation Methods 0.000 description 5
- RZZPDXZPRHQOCG-OJAKKHQRSA-O CDP-choline(1+) Chemical compound O[C@@H]1[C@H](O)[C@@H](COP(O)(=O)OP(O)(=O)OCC[N+](C)(C)C)O[C@H]1N1C(=O)N=C(N)C=C1 RZZPDXZPRHQOCG-OJAKKHQRSA-O 0.000 description 3
- 235000005911 diet Nutrition 0.000 description 3
- 230000037213 diet Effects 0.000 description 3
- 230000004410 intraocular pressure Effects 0.000 description 3
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 description 2
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 235000010755 mineral Nutrition 0.000 description 2
- 230000000324 neuroprotective effect Effects 0.000 description 2
- 235000016709 nutrition Nutrition 0.000 description 2
- 210000001328 optic nerve Anatomy 0.000 description 2
- 238000011422 pharmacological therapy Methods 0.000 description 2
- 150000003904 phospholipids Chemical class 0.000 description 2
- 210000001525 retina Anatomy 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 description 1
- DVSZKTAMJJTWFG-SKCDLICFSA-N (2e,4e,6e,8e,10e,12e)-docosa-2,4,6,8,10,12-hexaenoic acid Chemical compound CCCCCCCCC\C=C\C=C\C=C\C=C\C=C\C=C\C(O)=O DVSZKTAMJJTWFG-SKCDLICFSA-N 0.000 description 1
- GZJLLYHBALOKEX-UHFFFAOYSA-N 6-Ketone, O18-Me-Ussuriedine Natural products CC=CCC=CCC=CCC=CCC=CCC=CCCCC(O)=O GZJLLYHBALOKEX-UHFFFAOYSA-N 0.000 description 1
- 201000009487 Amblyopia Diseases 0.000 description 1
- 229940123413 Angiotensin II antagonist Drugs 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- 101000579300 Homo sapiens Prostaglandin F2-alpha receptor Proteins 0.000 description 1
- FKUISVKPMQSWTN-UHFFFAOYSA-N Kesselringine Natural products C1CC(C2=C34)N(C)CCC2=CC(O)=C4OC2(OC)C(O)CCC31C2 FKUISVKPMQSWTN-UHFFFAOYSA-N 0.000 description 1
- 206010025421 Macule Diseases 0.000 description 1
- 206010061323 Optic neuropathy Diseases 0.000 description 1
- 102100028248 Prostaglandin F2-alpha receptor Human genes 0.000 description 1
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000004509 aqueous humor production Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 235000021028 berry Nutrition 0.000 description 1
- 239000002876 beta blocker Substances 0.000 description 1
- 229940097320 beta blocking agent Drugs 0.000 description 1
- 230000008827 biological function Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- KAUVQQXNCKESLC-UHFFFAOYSA-N docosahexaenoic acid (DHA) Natural products COC(=O)C(C)NOCC1=CC=CC=C1 KAUVQQXNCKESLC-UHFFFAOYSA-N 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 235000012055 fruits and vegetables Nutrition 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 208000018769 loss of vision Diseases 0.000 description 1
- 231100000864 loss of vision Toxicity 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 208000020911 optic nerve disease Diseases 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 description 1
- 229960001416 pilocarpine Drugs 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- PXGPLTODNUVGFL-YNNPMVKQSA-N prostaglandin F2alpha Chemical class CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)C[C@H](O)[C@@H]1C\C=C/CCCC(O)=O PXGPLTODNUVGFL-YNNPMVKQSA-N 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 210000003994 retinal ganglion cell Anatomy 0.000 description 1
- 230000009897 systematic effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 230000004393 visual impairment Effects 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/16—Inorganic salts, minerals or trace elements
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/115—Fatty acids or derivatives thereof; Fats or oils
- A23L33/12—Fatty acids or derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Definitions
- the present invention relates to nutraceutical and pharmaceutical compositions useful as adjuvant for the prevention and treatment of retinopathies (macular degeneration, diabetic retinopathy, etc.) and glaucoma, in particular to compositions containing choline.
- retinopathies molecular degeneration, diabetic retinopathy, etc.
- glaucoma compositions containing choline.
- Age-Related Macular Degeneration is a degenerative disease of the macula (the central portion of the retina). This pathology is the most common cause of sight loss in persons generally over 50. The incidence statistically increase with age. ARMD is caused by several and different factors. Defective arterial circulation, whereby capillary perfusion and supply of oxygen and other nutrients essential for correct functioning of the retina are reduced, determine the typical macular damage with consequent loss of central vision.
- Several systematic clinical studies have shown a close relationship between the diet and ARMD development: it has been demonstrated that a diet rich in fruit and vegetables (in particular green-leaf vegetables and berries) remarkably lowers ARMD incidence. Clinical studies recently carried out in the USA have shown that in patients whose diet was enriched in minerals and specific antioxidants, ARMD incidence was reduced by 25%.
- Glaucoma is an optic neuropathy characterized by rise in intraocular pressure and loss of visual field, causing slight or severe loss of vision, as the increased intraocular pressure damages the optic nerve and retinal ganglion cells death by apoptosis.
- the pharmacological therapy depends of the type of glaucoma, that can be primary (chronic or acute) or secondary.
- Treatments can be either topical (administration of eye-drops containing, e.g., pilocarpine, beta-blockers, prostaglandin F2 analogues selective, alpha-agonists ff FP prostanoid receptor, carbonic anhydrase inhibitors) or systemic (administration of carbonic anhydrase inhibitors) which reduce intraocular pressure by decreasing aqueous humor production or increasing its drainage.
- eye-drops containing, e.g., pilocarpine, beta-blockers, prostaglandin F2 analogues selective, alpha-agonists ff FP prostanoid receptor, carbonic anhydrase inhibitors
- systemic administration of carbonic anhydrase inhibitors
- compositions comprising biologically active compounds exerting protective action on the optic nerve.
- WO 93/18028 claims compositions containing phospholipids and antioxidants for the treatment of macular degeneration.
- GB 1431841 discloses ophthalmic-nutritional compositions containing vitamins and choline.
- Choline has several biological functions, for example it's a precursor of phosphatidylcholine and sphingomyelin, which are components of the cell membranes, nervous cells membranes included; as a consequence, choline administration can facilitate the biosynthesis of membrane phospholipids and exert a neuro-protective function.
- WO 93/15717 discloses the use of a choline salt for the treatment of diabetic retinopathy. It would be therefore advantageous to provide nutritional compositions which can be used as adjuvants for the prevention and/or treatment of retinopathies (ARMD, diabetic retinopathy, etc.).
- WO 05/37262 discloses oral compositions containing citicholine as a choline donor, in combination with Vitamins A e B 6 for the treatment of eye disorders such as glaucoma and amblyopia.
- WO 9315717 discloses the use of angiotensin II antagonists choline salts for the treatment of glaucoma.
- compositions useful as adjutants in the prevention and/or treatment of retinopathies would therefore be advantageous. Disclosure of the invention
- compositions containing choline or salts or derivatives thereof, unsaturated fatty acids and antioxidants are particularly effective as adjuvants for the prevention and/or treatment of retinopathies (ARMD, diabetic retinopathy, etc.), as well as for the prevention and/or treatment of glaucoma.
- the invention relates to nutritional or pharmaceutical compositions containing a combination of choline, or biologically acceptable salts or derivatives thereof, unsaturated fatty acids and optionally antioxidants.
- salts or derivatives thereof means biologically acceptable salts or derivatives, such as choline hydrochloride or choline bitartrate, preferably choline bitartrate.
- the preferred choline derivative is cytidine-diphosphocholine, commonly known as citicholine.
- the amount of choline in the formulations is comprised between 100 and 1000 mg.
- saturated fatty acids indicates preferably linoleic acid, arachidonic acid, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA).
- the formulations intended for use in the prevention and/or treatment of retinopathies will contain antioxidants selected from lipoic acid, luteine, flavonoids and minerals such as zinc and copper.
- flavonoids quercetine, anthocyanes, proanthocyanidins and soy isoflavones are preferred.
- the proanthocyanidins will derive from Vitis vinifera.
- the formulations intended for use in the prevention and/or treatment of glaucoma will contain docosahexaenoic acid as the unsaturated fatty acid.
- the formulations intended for use in the prevention and/or treatment of glaucoma will further contain biologically active substances exerting neuro-protective action, particularly vitamins of the B group.
- said formulations will further contain one or more substances selected from inositol, forskolin, folic acid, vitamin B 12 , vitamin B 6 and quercetin.
- compositions of the invention can be prepared according to conventional techniques and with excipients well known to those skilled in the art and disclosed, for example, in Remington's Pharmaceutical Sciences Handbook, XVII ed. Mack Pub., N.Y., U.S.A..
- the compositions of the invention can be in the form of tablets, capsules, powders, granules, beads, gels, solutions or suspensions, whose posology will be determined according to the patient's needs and age.
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Abstract
The invention relates to nutraceutical and pharmaceutical compositions containing choline, unsaturated fatty acids and optionally antioxidants useful as adjuvants in the prevention and treatment of retinopathies (ARMD, diabetic retinopathy, etc.) and glaucoma.
Description
NUTRACEUTICAL AND PHARMACEUTICAL COMPOSITIONS CONTAINING CHOLINE AS ADIUVANTS FOR THE PREVENTION AND TREATMENT OF RETINOPATHIES AND GLAUCOMA
Field of the invention
The present invention relates to nutraceutical and pharmaceutical compositions useful as adjuvant for the prevention and treatment of retinopathies (macular degeneration, diabetic retinopathy, etc.) and glaucoma, in particular to compositions containing choline. State of the art
Age-Related Macular Degeneration (ARMD) is a degenerative disease of the macula (the central portion of the retina). This pathology is the most common cause of sight loss in persons generally over 50. The incidence statistically increase with age. ARMD is caused by several and different factors. Defective arterial circulation, whereby capillary perfusion and supply of oxygen and other nutrients essential for correct functioning of the retina are reduced, determine the typical macular damage with consequent loss of central vision. Several systematic clinical studies have shown a close relationship between the diet and ARMD development: it has been demonstrated that a diet rich in fruit and vegetables (in particular green-leaf vegetables and berries) remarkably lowers ARMD incidence. Clinical studies recently carried out in the USA have shown that in patients whose diet was enriched in minerals and specific antioxidants, ARMD incidence was reduced by 25%.
Glaucoma is an optic neuropathy characterized by rise in intraocular pressure and loss of visual field, causing slight or severe loss of vision, as the increased intraocular pressure damages the optic nerve and retinal ganglion cells death by apoptosis. The pharmacological therapy depends of the type of glaucoma, that can be primary (chronic or acute) or secondary. Treatments can
be either topical (administration of eye-drops containing, e.g., pilocarpine, beta-blockers, prostaglandin F2 analogues selective, alpha-agonists ff FP prostanoid receptor, carbonic anhydrase inhibitors) or systemic (administration of carbonic anhydrase inhibitors) which reduce intraocular pressure by decreasing aqueous humor production or increasing its drainage.
Recently, efforts have been made to support pharmacological therapy with compositions comprising biologically active compounds exerting protective action on the optic nerve. WO 93/18028 claims compositions containing phospholipids and antioxidants for the treatment of macular degeneration.
GB 1431841 discloses ophthalmic-nutritional compositions containing vitamins and choline. Choline has several biological functions, for example it's a precursor of phosphatidylcholine and sphingomyelin, which are components of the cell membranes, nervous cells membranes included; as a consequence, choline administration can facilitate the biosynthesis of membrane phospholipids and exert a neuro-protective function.
WO 93/15717 discloses the use of a choline salt for the treatment of diabetic retinopathy. It would be therefore advantageous to provide nutritional compositions which can be used as adjuvants for the prevention and/or treatment of retinopathies (ARMD, diabetic retinopathy, etc.).
WO 05/37262 discloses oral compositions containing citicholine as a choline donor, in combination with Vitamins A e B 6 for the treatment of eye disorders such as glaucoma and amblyopia.
WO 9315717 discloses the use of angiotensin II antagonists choline salts for the treatment of glaucoma.
Some compositions useful as adjutants in the prevention and/or treatment of retinopathies (ARMD, diabetic retinopathy, etc.) and glaucoma, would therefore be advantageous.
Disclosure of the invention
It has now been found that compositions containing choline or salts or derivatives thereof, unsaturated fatty acids and antioxidants, are particularly effective as adjuvants for the prevention and/or treatment of retinopathies (ARMD, diabetic retinopathy, etc.), as well as for the prevention and/or treatment of glaucoma. Accordingly, the invention relates to nutritional or pharmaceutical compositions containing a combination of choline, or biologically acceptable salts or derivatives thereof, unsaturated fatty acids and optionally antioxidants. The expression "salts or derivatives thereof means biologically acceptable salts or derivatives, such as choline hydrochloride or choline bitartrate, preferably choline bitartrate. The preferred choline derivative is cytidine-diphosphocholine, commonly known as citicholine.
The amount of choline in the formulations is comprised between 100 and 1000 mg.
The term "unsaturated fatty acids" indicates preferably linoleic acid, arachidonic acid, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA).
According to a preferred aspect of the invention, the formulations intended for use in the prevention and/or treatment of retinopathies (ARMD, diabetic retinopathy, etc.), will contain antioxidants selected from lipoic acid, luteine, flavonoids and minerals such as zinc and copper. Among flavonoids, quercetine, anthocyanes, proanthocyanidins and soy isoflavones are preferred. Preferably, the proanthocyanidins will derive from Vitis vinifera. According to a preferred aspect of the invention, the formulations intended for use in the prevention and/or treatment of glaucoma will contain docosahexaenoic acid as the unsaturated fatty acid.
According to a preferred aspect of the invention, the formulations
intended for use in the prevention and/or treatment of glaucoma will further contain biologically active substances exerting neuro-protective action, particularly vitamins of the B group. According to a more preferred aspect of the invention, said formulations will further contain one or more substances selected from inositol, forskolin, folic acid, vitamin B12, vitamin B6 and quercetin.
The compositions of the invention can be prepared according to conventional techniques and with excipients well known to those skilled in the art and disclosed, for example, in Remington's Pharmaceutical Sciences Handbook, XVII ed. Mack Pub., N.Y., U.S.A.. The compositions of the invention can be in the form of tablets, capsules, powders, granules, beads, gels, solutions or suspensions, whose posology will be determined according to the patient's needs and age.
The following examples illustrate the invention in greater detail:
EXAMPLE 1
Claims
1. Nutraceutical and pharmaceutical compositions containing choline or a salt or a biologically acceptable derivative thereof in combination with unsaturated fatty acids in admixture with suitable excipients and/or vehicles.
2. Compositions according to claim 1 wherein the salt is choline hydrochloride or choline bitartrate.
3. Compositions according to claim 2 wherein the choline salt is choline bitartrate.
4 Compositions according to claim 1 wherein the choline derivative is citicholine.
5. Compositions according to any one of claims 1-4 wherein the unsaturated fatty acid is selected from linoleic acid, arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid.
6. Compositions according to any one of claims 1-5, further containing antioxidants.
7. Compositions according to claim 6 wherein the antioxidants are selected from: lipoic acid, lutein, flavonoids, zinc and copper.
8. Compositions according to claim 7 wherein the flavonoids are selected from quercetine, anthocyanin, proanthocyanidins and soy isoflavones.
9. Compositions according to claim 8 wherein the proanthocyanidins are Vitis Vinifera proanthocyanidins.
10. Compositions according to any one of claims 1-5 further contain one or more substances selected from inositol, forskolin, folic acid, vitamin B12, vitamin B6 e quercetin.
11. Compositions according to any one of claims 1-10 in the form of tablets, capsules, powders, granules, beads, gels, solutions or suspensions.
12. The use of a combination of choline or a pharmacologically acceptable derivative thereof with unsaturated fatty acids, for the preparation of nutraceutical and pharmaceutical compositions for the prevention and/or treatment of retinopathies and glaucoma.
13. The use of a combination of choline or a pharmacologically acceptable derivative thereof with unsaturated fatty acids and antioxidants, for the preparation of nutraceutical and pharmaceutical compositions for the prevention and/or treatment of retinopathies.
14. The use of a combination of choline or a pharmacologically acceptable derivative thereof with unsaturated fatty acids, for the preparation of nutraceutical and pharmaceutical compositions for the prevention and/or treatment of glaucoma.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06806269A EP1951071A2 (en) | 2005-10-18 | 2006-10-13 | Nutraceutical and pharmaceutical compositions containing choline as adiuvants for the prevention and treatment of retinopathies and glaucoma |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITMI2005A001968 | 2005-10-18 | ||
| ITMI20051968 ITMI20051968A1 (en) | 2005-10-18 | 2005-10-18 | COLINA-BASED NEUTRACEUTICAL COMPOSITIONS IN THE PREVENTION AND TREATMENT OF GLAUCOMA |
| IT001969A ITMI20051969A1 (en) | 2005-10-18 | 2005-10-18 | CHINA-BASED NEUTRACEUTICAL COMPOSITIONS GIVEN IN THE PREVENTION AND TREATMENT OF MACULAR DEGENERATION AND RETINOPATHIES |
| ITMI2005A001969 | 2005-10-18 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2007045407A2 true WO2007045407A2 (en) | 2007-04-26 |
| WO2007045407A3 WO2007045407A3 (en) | 2007-07-26 |
Family
ID=37806145
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2006/009926 WO2007045407A2 (en) | 2005-10-18 | 2006-10-13 | Nutraceutical and pharmaceutical compositions containing choline as adiuvants for the prevention and treatment of retinopathies and glaucoma |
Country Status (2)
| Country | Link |
|---|---|
| EP (1) | EP1951071A2 (en) |
| WO (1) | WO2007045407A2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITRM20120284A1 (en) * | 2012-06-18 | 2013-12-19 | Omikron Italia S R L | CITICOLINE FOR THE TREATMENT OF DIABETIC RETINOPATHY. |
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| WO1993015717A1 (en) * | 1992-02-17 | 1993-08-19 | Ciba-Geigy Ag | Compositions for the treatment of glaucoma |
| US5626849A (en) * | 1995-06-07 | 1997-05-06 | Reliv International, Inc. | Weight loss composition for burning and reducing synthesis of fats |
| WO2001084961A2 (en) * | 2000-05-08 | 2001-11-15 | N.V. Nutricia | Preparation for the prevention and/or treatment of vascular disorders |
| WO2002102394A2 (en) * | 2001-06-18 | 2002-12-27 | Neptune Technologies & Bioressources Inc. | Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases, arthritis, skin cancer, diabetes, premenstrual syndrome and transdermal transport |
| EP1275399A2 (en) * | 2001-07-09 | 2003-01-15 | N.V. Nutricia | Method and preparation for preventing and/or treating vascular disorders and secondary disorders associated therewith |
| WO2003003981A2 (en) * | 2001-07-05 | 2003-01-16 | Vital Basics, Inc. | Compositions for improving mental performance |
| US20030044472A1 (en) * | 2001-08-28 | 2003-03-06 | Dexgen-Intellectual Property, Homocysteine, Inc. | Method and synergistic composition for treating attention deficit/hyperactivity disorder |
| WO2004082402A1 (en) * | 2003-03-18 | 2004-09-30 | Novartis Ag | Compositions comprising fatty acids and amino acids |
| WO2005037262A1 (en) * | 2003-10-22 | 2005-04-28 | Tubilux Pharma S.P.A. | Citicoline-based composition in combination with vitamins for the prevention and treatment of eye pathologies |
| US20050163873A1 (en) * | 2004-01-14 | 2005-07-28 | Robert Ritch | Methods and formulations for treating glaucoma |
| US20050180990A1 (en) * | 2004-02-12 | 2005-08-18 | Kenichi Matsunaga | Antidiabetic agent and food |
| US20050180989A1 (en) * | 2004-02-12 | 2005-08-18 | Kenichi Matsunaga | Antihyperlipidemic agent and food |
-
2006
- 2006-10-13 EP EP06806269A patent/EP1951071A2/en not_active Withdrawn
- 2006-10-13 WO PCT/EP2006/009926 patent/WO2007045407A2/en active Application Filing
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993015717A1 (en) * | 1992-02-17 | 1993-08-19 | Ciba-Geigy Ag | Compositions for the treatment of glaucoma |
| US5626849A (en) * | 1995-06-07 | 1997-05-06 | Reliv International, Inc. | Weight loss composition for burning and reducing synthesis of fats |
| WO2001084961A2 (en) * | 2000-05-08 | 2001-11-15 | N.V. Nutricia | Preparation for the prevention and/or treatment of vascular disorders |
| WO2002102394A2 (en) * | 2001-06-18 | 2002-12-27 | Neptune Technologies & Bioressources Inc. | Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases, arthritis, skin cancer, diabetes, premenstrual syndrome and transdermal transport |
| WO2003003981A2 (en) * | 2001-07-05 | 2003-01-16 | Vital Basics, Inc. | Compositions for improving mental performance |
| EP1275399A2 (en) * | 2001-07-09 | 2003-01-15 | N.V. Nutricia | Method and preparation for preventing and/or treating vascular disorders and secondary disorders associated therewith |
| US20030044472A1 (en) * | 2001-08-28 | 2003-03-06 | Dexgen-Intellectual Property, Homocysteine, Inc. | Method and synergistic composition for treating attention deficit/hyperactivity disorder |
| WO2004082402A1 (en) * | 2003-03-18 | 2004-09-30 | Novartis Ag | Compositions comprising fatty acids and amino acids |
| WO2005037262A1 (en) * | 2003-10-22 | 2005-04-28 | Tubilux Pharma S.P.A. | Citicoline-based composition in combination with vitamins for the prevention and treatment of eye pathologies |
| US20050163873A1 (en) * | 2004-01-14 | 2005-07-28 | Robert Ritch | Methods and formulations for treating glaucoma |
| US20050180990A1 (en) * | 2004-02-12 | 2005-08-18 | Kenichi Matsunaga | Antidiabetic agent and food |
| US20050180989A1 (en) * | 2004-02-12 | 2005-08-18 | Kenichi Matsunaga | Antihyperlipidemic agent and food |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITRM20120284A1 (en) * | 2012-06-18 | 2013-12-19 | Omikron Italia S R L | CITICOLINE FOR THE TREATMENT OF DIABETIC RETINOPATHY. |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1951071A2 (en) | 2008-08-06 |
| WO2007045407A3 (en) | 2007-07-26 |
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