CH651209A5 - Medicament consisting of an aqueous extract of red grape marc - Google Patents
Medicament consisting of an aqueous extract of red grape marc Download PDFInfo
- Publication number
- CH651209A5 CH651209A5 CH7527/80A CH752780A CH651209A5 CH 651209 A5 CH651209 A5 CH 651209A5 CH 7527/80 A CH7527/80 A CH 7527/80A CH 752780 A CH752780 A CH 752780A CH 651209 A5 CH651209 A5 CH 651209A5
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- Switzerland
- Prior art keywords
- aqueous extract
- red grape
- grape marc
- marc
- medicament according
- Prior art date
Links
- 241001593968 Vitis palmata Species 0.000 title claims description 14
- 239000006286 aqueous extract Substances 0.000 title claims description 13
- 239000003814 drug Substances 0.000 title claims description 13
- 230000004856 capillary permeability Effects 0.000 claims description 6
- 239000002775 capsule Substances 0.000 claims description 4
- 239000007924 injection Substances 0.000 claims description 4
- 238000002347 injection Methods 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 239000000243 solution Substances 0.000 claims description 3
- 240000006365 Vitis vinifera Species 0.000 claims description 2
- 239000003889 eye drop Substances 0.000 claims description 2
- 229940012356 eye drops Drugs 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 239000002674 ointment Substances 0.000 claims description 2
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000000047 product Substances 0.000 description 11
- 101800004538 Bradykinin Proteins 0.000 description 6
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 description 6
- 102100035792 Kininogen-1 Human genes 0.000 description 6
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 description 6
- 239000000284 extract Substances 0.000 description 6
- 241000700159 Rattus Species 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 230000000144 pharmacologic effect Effects 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 230000001476 alcoholic effect Effects 0.000 description 2
- 239000000975 dye Substances 0.000 description 2
- 238000010828 elution Methods 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 239000002504 physiological saline solution Substances 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 244000215068 Acacia senegal Species 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 1
- COXVTLYNGOIATD-HVMBLDELSA-N CC1=C(C=CC(=C1)C1=CC(C)=C(C=C1)\N=N\C1=C(O)C2=C(N)C(=CC(=C2C=C1)S(O)(=O)=O)S(O)(=O)=O)\N=N\C1=CC=C2C(=CC(=C(N)C2=C1O)S(O)(=O)=O)S(O)(=O)=O Chemical compound CC1=C(C=CC(=C1)C1=CC(C)=C(C=C1)\N=N\C1=C(O)C2=C(N)C(=CC(=C2C=C1)S(O)(=O)=O)S(O)(=O)=O)\N=N\C1=CC=C2C(=CC(=C(N)C2=C1O)S(O)(=O)=O)S(O)(=O)=O COXVTLYNGOIATD-HVMBLDELSA-N 0.000 description 1
- 206010007191 Capillary fragility Diseases 0.000 description 1
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- JOYRKODLDBILNP-UHFFFAOYSA-N Ethyl urethane Chemical compound CCOC(N)=O JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- YYVIFBVXJYYHCW-UHFFFAOYSA-N Malvin Natural products COc1cc(cc(OC)c1O)C2=C(Cc3c(OC4OC(CO)C(O)C(O)C4O)cc(O)cc3O2)OC5OC(CO)C(O)C(O)C5O YYVIFBVXJYYHCW-UHFFFAOYSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229930182559 Natural dye Natural products 0.000 description 1
- 241000219094 Vitaceae Species 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000003463 adsorbent Substances 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000003125 aqueous solvent Substances 0.000 description 1
- 239000008135 aqueous vehicle Substances 0.000 description 1
- 238000000429 assembly Methods 0.000 description 1
- 230000000712 assembly Effects 0.000 description 1
- 235000011089 carbon dioxide Nutrition 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 210000001715 carotid artery Anatomy 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 229960003699 evans blue Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000007710 freezing Methods 0.000 description 1
- 230000008014 freezing Effects 0.000 description 1
- 235000015203 fruit juice Nutrition 0.000 description 1
- 239000002223 garnet Substances 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 230000001631 hypertensive effect Effects 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- CILLXFBAACIQNS-BTXJZROQSA-O malvin Chemical compound COC1=C(O)C(OC)=CC(C=2C(=CC=3C(O[C@H]4[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O4)O)=CC(O)=CC=3[O+]=2)O[C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=C1 CILLXFBAACIQNS-BTXJZROQSA-O 0.000 description 1
- 229940117886 malvin Drugs 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- QSHDDOUJBYECFT-UHFFFAOYSA-N mercury Chemical compound [Hg] QSHDDOUJBYECFT-UHFFFAOYSA-N 0.000 description 1
- 229910052753 mercury Inorganic materials 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000000978 natural dye Substances 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 208000001297 phlebitis Diseases 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 201000002282 venous insufficiency Diseases 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
Landscapes
- Health & Medical Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Medicinal Chemistry (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Description
La présente invention concerne un médicament consistant en un extrait aqueux de marcs de raisins rouges. The present invention relates to a medicament consisting of an aqueous extract of red grape marc.
Le brevet français N° 2378070 a déjà décrit un procédé d'extraction d'un colorant naturel sous forme concentrée à partir des marcs de raisins rouges, de lies ou de vin. Ce produit semble destiné à la coloration de substances dans l'industrie alimentaire, cosmétologi-que ou pharmaceutique; le brevet n'indique pour ce produit ni propriété pharmacologique, ni application thérapeutique. French Patent No. 2378070 has already described a process for extracting a natural dye in concentrated form from the marcs of red grapes, lees or wine. This product seems intended for coloring substances in the food, cosmetology or pharmaceutical industry; the patent does not indicate for this product either pharmacological property or therapeutic application.
Il est par ailleurs connu par le Brevet Spécial de Médicament N° 1369 d'utiliser des anthocyanosides extraits de végétaux ou de jus de fruits dans des buts thérapeutiques, notamment pour améliorer l'acuité visuelle. It is also known from the Special Medicines Patent No. 1369 to use anthocyanosides extracted from plants or fruit juices for therapeutic purposes, in particular to improve visual acuity.
Mais il n'avait encore jamais été décrit de médicaments extraits de marcs de raisins rouges. Or, la titulaire a découvert que ces extraits étaient doués de propriétés pharmacologiques intéressantes, notamment de remarquables propriétés de réduction de la perméabilité capillaire. But there had never before been described drugs extracted from red grape marc. However, the licensee discovered that these extracts were endowed with interesting pharmacological properties, in particular remarkable properties for reducing capillary permeability.
La présente invention a donc pour objet, à titre de médicaments, des extraits aqueux de marcs de raisins rouges. The present invention therefore relates, as medicaments, aqueous extracts of marc of red grapes.
Parmi les médicaments, objet de l'invention, on retient notamment les extraits aqueux de marcs de raisins rouges appartenant à l'espèce Vitis vinifera (famille des vitacées). Among the drugs which are the subject of the invention, there are in particular the aqueous extracts of red grape marc belonging to the species Vitis vinifera (family of vitaceae).
On retient aussi, notamment, les extraits aqueux lyophilisés des marcs de raisins rouges; parmi ceux-ci, on retient particulièrement les lyophilisats obtenus à partir d'extraits aqueux de marcs de raisins rouges concentrés à un poids de matière sèche compris entre 10 et 20%. We also retain, in particular, the lyophilized aqueous extracts of the red grape marc; among these, the lyophilisates obtained especially are obtained from aqueous extracts of red grape marc concentrated to a weight of dry matter of between 10 and 20%.
Les extraits aqueux préférés selon l'invention sont préparés selon le procédé décrit dans le brevet français Roussillon Alimentaire N° 2378070, à savoir: extraction à chaud de marcs de raisins rouges à l'aide d'un solvant aqueux, détartrage de l'extrait obtenu, filtration sur une ou plusieurs colonnes adsorbantes, élution de l'extrait adsorbé, concentration puis, si désiré, lyophilisation. The preferred aqueous extracts according to the invention are prepared according to the method described in French patent Roussillon Alimentaire N ° 2378070, namely: hot extraction of red grape marc using an aqueous solvent, descaling of the extract obtained, filtration through one or more adsorbent columns, elution of the adsorbed extract, concentration then, if desired, lyophilization.
Parmi ceux-ci, on retient notamment ceux caractérisés en ce que l'élution est effectuée à l'aide d'un solvant ou d'un mélange de solvants alcooliques, et parmi ces derniers on retient en particulier ceux pour lesquels le solvant alcoolique utilisé est l'éthanol. Among these, there are in particular those characterized in that the elution is carried out using a solvent or a mixture of alcoholic solvents, and among the latter there are in particular those for which the alcoholic solvent used is ethanol.
Les extraits aqueux tout particulièrement préférés selon l'invention sont obtenus selon le procédé décrit à l'exemple 4 du brevet Roussillon Alimentaire cité. Ces produits obtenus dans cet exemple sont concentrés à environ 30% de poids sec. The aqueous extracts very particularly preferred according to the invention are obtained according to the process described in Example 4 of the Roussillon Alimentaire patent cited. These products obtained in this example are concentrated to around 30% by dry weight.
Lorsque l'on veut lyophiliser l'extrait obtenu, on se contente de concentrations de 10 à 20% en matière sèche, et de préférence 12 à 15%. When it is desired to lyophilize the extract obtained, one is satisfied with concentrations of 10 to 20% in dry matter, and preferably 12 to 15%.
La lyophilisation est effectuée de façon classique, par exemple dans des ensembles congélateur-sublimeur de taille moyenne comme les modèles SMU ou SMRG commercialisés par la Société Usifroid, Lyophilization is carried out in a conventional manner, for example in medium-sized freezer-sublimator assemblies such as the SMU or SMRG models sold by the Company Usifroid,
des lyophilisateurs de grande taille comme, par exemple, l'ensemble formé par un congélateur CAI et un sublimeur SMIRS, tous deux commercialisés par Usifroid. Des modèles plus petits, de laboratoire, peuvent aussi être utilisés, ainsi que ceux commercialisés par d'autres sociétés, telle la Société Sérail. large freeze-dryers such as, for example, the assembly formed by a CAI freezer and a SMIRS sublimator, both marketed by Usifroid. Smaller, laboratory models can also be used, as well as those sold by other companies, such as Société Sérail.
Il a été trouvé que les extraits aqueux des marcs de raisins rouges possèdent de très intéressantes propriétés pharmacologiques. Ils sont doués, notamment, d'un remarquable pouvoir de réduction de l'hy-perperméabilité capillaire, illustré plus loin dans la partie expérimentale. It has been found that the aqueous extracts of red grape marc have very interesting pharmacological properties. They are endowed, in particular, with a remarkable power to reduce capillary water permeability, illustrated later in the experimental part.
En raison de ces propriétés, les médicaments, objet de la présente invention, trouvent par exemple leur emploi dans le traitement et la prévention de la fragilité capillaire, comme dans les insuffisances veineuses de la grossesse, les séquelles de phlébites, les troubles vascu-laires rétiniens. Ces médicaments trouvent notamment leur emploi chez les hypertendus. Because of these properties, the drugs which are the subject of the present invention find, for example, their use in the treatment and prevention of capillary fragility, such as in venous insufficiency in pregnancy, the after-effects of phlebitis, vascular disorders. retinas. These drugs find their use especially in hypertensive patients.
La dose usuelle, variable selon le sujet traité et l'affection en cause, peut être par exemple de 0,25 à 5 g/d, par voie orale, chez l'homme, d'un lyophilisât d'extrait concentré à 15% de matière sèche. The usual dose, which varies according to the subject treated and the condition in question, can be for example from 0.25 to 5 g / d, orally, in humans, of a lyophilisate of concentrated extract at 15%. dry matter.
Les extraits aqueux de marcs de raisins rouges, tels que définis ci-dessus, peuvent constituer les principes actifs de nombreuses formes pharmaceutiques destinées à la voie digestive, parentérale ou locale, telles que les capsules, les gélules, les comprimés simples ou dragéifiés, les granulés, les solutions buvables, les préparations injectables, les collyres ou les pommades. The aqueous extracts of red grape marc, as defined above, can constitute the active principles of numerous pharmaceutical forms intended for the digestive, parenteral or local route, such as capsules, capsules, simple or coated tablets, granules, oral solutions, injections, eye drops or ointments.
L'invention a donc aussi pour objet les compositions pharmaceutiques renfermant, à titre de principe actif, l'un au moins des médicaments tels que définis ci-dessus. Le ou les principes actifs peuvent y être incorporés à des excipients habituellement employés dans ces compositions pharmaceutiques, tels que le talc, la gomme arabique, le lactose, l'amidon, le stéarate de magnésium, le beurre de cacao, les véhicules aqueux ou non, les corps gras d'origine animale ou végétale, les dérivés paraffiniques, les glycols, les divers agents mouillants, dispersants ou émulsifiants, les conservateurs. The invention therefore also relates to pharmaceutical compositions containing, as active principle, at least one of the medicaments as defined above. The active ingredient (s) can be incorporated therein into excipients usually used in these pharmaceutical compositions, such as talc, gum arabic, lactose, starch, magnesium stearate, cocoa butter, aqueous vehicles or not , fatty substances of animal or vegetable origin, paraffinic derivatives, glycols, various wetting agents, dispersants or emulsifiers, preservatives.
Les exemples suivants illustrent l'invention. The following examples illustrate the invention.
Exemple 1 : Example 1:
On dilue de moitié, par de l'eau distillée, 20 ml d'un concentré d'extrait de marcs de raisins rouges, tel qu'obtenu à l'exemple 4 du brevet français N° 2378070, et concentré à 27% de matière sèche. Les 40 ml de solution obtenus sont congelés dans un bain réfrigérant de carboglace/méthanol et lyophilisés immédiatement après dans un lyophilisateur muni d'un piège refroidi par de l'azote liquide, sous vide de 0,01 mm de mercure. Après une nuit, on obtient 5,5 g d'un résidu sec, friable, de couleur rouge grenat. Diluted by half, with distilled water, 20 ml of a concentrate of red grape marc extract, as obtained in Example 4 of French patent N ° 2378070, and concentrated to 27% of material dried. The 40 ml of solution obtained are frozen in a freezing bath of dry ice / methanol and lyophilized immediately afterwards in a lyophilizer fitted with a trap cooled by liquid nitrogen, under a vacuum of 0.01 mm of mercury. After one night, 5.5 g of a dry, crumbly residue, garnet red in color, is obtained.
Analyse: Analysis:
Titre spectrométrique en anthocyanosides Spectrometric titer in anthocyanosides
(méthode au bisulfite) 13,6% Titre spectrométrique direct (bisulfite method) 13.6% Direct spectrometric titer
(exprimé en malvin) 11,3% (expressed in Malvin) 11.3%
Azote 1,2% Nitrogen 1.2%
Cendres 2,6% Ash 2.6%
Exemple 2: Example 2:
On a préparé des comprimés répondant à la formule: Tablets corresponding to the formula have been prepared:
Lyophilisat de l'exemple 1 200 mg Lyophilisate from Example 1 200 mg
Excipient q.s. pour un comprimé terminé à 600 mg Excipient q.s. for a tablet finished at 600 mg
Détail de l'excipient: lactose, talc, amidon, stéarate de magnésium. Details of the excipient: lactose, talc, starch, magnesium stearate.
Etude pharmacologique: Pharmacological study:
Action sur la perméabilité capillaire Action on capillary permeability
Le test est pratiqué sur la peau abdominale de rats mâles de 200 g environ, mis à jeun 16 h avant l'expérience. L'augmentation de la perméabilité capillaire est induite par 3 injections intradermiques de bradykinine (2 [ig dans 0,1 ml de sérum physiologique); le traite5 The test is performed on the abdominal skin of male rats weighing approximately 200 g, fasted 16 h before the experiment. The increase in capillary permeability is induced by 3 intradermal injections of bradykinin (2 μg in 0.1 ml of physiological saline); the treaty5
10 10
15 15
20 20
25 25
30 30
35 35
40 40
45 45
50 50
55 55
60 60
65 65
3 3
651 209 651,209
ment est administré 30 ou 60 min avant la bradykinine selon la voie d'administration. Les rats sont anesthésiés à l'uréthanne immédiatement avant les injections de bradykinine. Le bleu d'Evans, révélateur de l'augmentation de la perméabilité capillaire, est injecté par voie intraveineuse (50 mg/kg dans 2 ml/kg de sérum physiologique) immédiatement après la bradykinine. ment is administered 30 or 60 min before bradykinin depending on the route of administration. The rats are anesthetized with urethane immediately before the bradykinin injections. Evans blue, indicative of the increase in capillary permeability, is injected intravenously (50 mg / kg in 2 ml / kg of physiological saline) immediately after bradykinin.
30 min après, les rats sont sacrifiés par section de la carotide et les zones colorées sont prélevées. Le colorant est extrait par le form- 30 min later, the rats are sacrificed by section of the carotid artery and the colored zones are removed. The dye is extracted by the form-
amide dans des tubes mis à l'étuve pendant 24 h à 45° C. Les surnageants sont décantés et leur densité optique est lue à 620 m|i au spec-trophotomètre Gilford 240. Les résultats sont exprimés en quantité de colorant par spot. amide in tubes placed in an oven for 24 h at 45 ° C. The supernatants are decanted and their optical density is read at 620 m 3 with the Gilford 240 spec-trophotometer. The results are expressed in quantity of dye per spot.
Le produit de l'exemple 1 a été administré en suspension dans une solution aqueuse de carboxyméthylcellulose (0,25%) et polysor-bate 80 (0,2%) soit par voie intrapéritonéale, soit par voie orale. The product of Example 1 was administered in suspension in an aqueous solution of carboxymethylcellulose (0.25%) and polysor-bate 80 (0.2%) either intraperitoneally or orally.
Résultats Voie intrapéritonéale Results Intraperitoneal route
Traitement 30 min avant bradykinine Treatment 30 min before bradykinin
Doses mg/kg Doses mg / kg
Nombre de rats Number of rats
Bleu Evans Hg/spot Blue Evans Hg / spot
% %
inhibition inhibition
Témoins Witnesses
Produit de l'exemple 1 Product of Example 1
50 50
12 12 12 12
9,6 + 2,1 5,8 ± 1,1 9.6 + 2.1 5.8 ± 1.1
39 39
Témoins Witnesses
Produit de l'exemple 1 Product of Example 1
100 100
12 ~~1 12 ~~ 1
12 12
10,1 + 2,0 4,6 ± 0,8 10.1 + 2.0 4.6 ± 0.8
54 54
Témoins Witnesses
Produit de l'exemple 1 Product of Example 1
200 200
12 1 12 12 1 12
10,5 + 0,9 5,7 ± 0,5 10.5 + 0.9 5.7 ± 0.5
46 46
Traitement 60 min avant bradykinine Treatment 60 min before bradykinin
Doses mg/kg Doses mg / kg
Nombre de rats Number of rats
Bleu Evans p.g/spot Evans Blue p.g / spot
% %
inhibition inhibition
Témoins Witnesses
Produit de l'exemple 1 Product of Example 1
200 200
6 6 6 6
12.0 + 0,7 12.0 + 0.7
13.1 + 1,6 13.1 + 1.6
0 0
Témoins Witnesses
Produit de l'exemple 1 Product of Example 1
500 500
6 6 6 6
19.1 + 1,9 19.1 + 1.9
16.2 + 1,9 16.2 + 1.9
15 15
Témoins Witnesses
Produit de l'exemple 1 Product of Example 1
1000 1000
6 6 6 6
13,7 + 2,3 11,1 ± 0,7 13.7 + 2.3 11.1 ± 0.7
19 19
Le produit de l'exemple 1 diminue la perméabilité capillaire. Son effet est beaucoup plus marqué par voie intrapéritonéale que par voie orale. The product of Example 1 decreases the capillary permeability. Its effect is much more marked intraperitoneally than orally.
R R
Claims (5)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR7925065A FR2466989A1 (en) | 1979-10-09 | 1979-10-09 | APPLICATION AS MEDICINES OF AQUEOUS EXTRACTS OF MARCS OF RED GRAPES, AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAID EXTRACTS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CH651209A5 true CH651209A5 (en) | 1985-09-13 |
Family
ID=9230478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CH7527/80A CH651209A5 (en) | 1979-10-09 | 1980-10-08 | Medicament consisting of an aqueous extract of red grape marc |
Country Status (7)
| Country | Link |
|---|---|
| BE (1) | BE885574A (en) |
| CH (1) | CH651209A5 (en) |
| DE (1) | DE3038198A1 (en) |
| FR (1) | FR2466989A1 (en) |
| GR (1) | GR70759B (en) |
| IT (1) | IT1144015B (en) |
| PT (1) | PT71883B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AUPO830197A0 (en) * | 1997-07-29 | 1997-08-21 | Tarac Distillers Pty Ltd | Process for the recovery and improvement of wine extract and derivatives from grape marc |
| CN104958372A (en) * | 2015-06-28 | 2015-10-07 | 四川金堂海纳生物医药技术研究所 | External used drug for treating thrombophlebitis and preparation method thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2378070A1 (en) * | 1977-01-25 | 1978-08-18 | Roussillon Alimentaire La Cata | Extracting anthocyanin colourants from grape residues - using hot water, for use in food and cosmetics etc. |
-
1979
- 1979-10-09 FR FR7925065A patent/FR2466989A1/en active Granted
-
1980
- 1980-10-07 GR GR63073A patent/GR70759B/el unknown
- 1980-10-07 PT PT71883A patent/PT71883B/en unknown
- 1980-10-08 IT IT49848/80A patent/IT1144015B/en active
- 1980-10-08 BE BE0/202362A patent/BE885574A/en not_active IP Right Cessation
- 1980-10-08 CH CH7527/80A patent/CH651209A5/en not_active IP Right Cessation
- 1980-10-09 DE DE19803038198 patent/DE3038198A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| GR70759B (en) | 1983-03-16 |
| BE885574A (en) | 1981-04-08 |
| PT71883A (en) | 1980-11-01 |
| FR2466989A1 (en) | 1981-04-17 |
| FR2466989B1 (en) | 1982-10-08 |
| PT71883B (en) | 1982-04-02 |
| IT1144015B (en) | 1986-10-29 |
| DE3038198A1 (en) | 1981-05-07 |
| IT8049848A0 (en) | 1980-10-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PL | Patent ceased |