FR2714292A1 - Medicaments contg. lysine acetyl-salicylate and vitamin E - Google Patents

Medicaments contg. lysine acetyl-salicylate and vitamin E Download PDF

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Publication number
FR2714292A1
FR2714292A1 FR9315554A FR9315554A FR2714292A1 FR 2714292 A1 FR2714292 A1 FR 2714292A1 FR 9315554 A FR9315554 A FR 9315554A FR 9315554 A FR9315554 A FR 9315554A FR 2714292 A1 FR2714292 A1 FR 2714292A1
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France
Prior art keywords
vitamin
pharmaceutical composition
composition according
carotene
lysine acetylsalicylate
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FR9315554A
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French (fr)
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FR2714292B1 (en
Inventor
Scheldewaert Rudy
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Synthelabo SA
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Synthelabo SA
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/618—Salicylic acid; Derivatives thereof having the carboxyl group in position 1 esterified, e.g. salsalate
    • A61K31/621—Salicylic acid; Derivatives thereof having the carboxyl group in position 1 esterified, e.g. salsalate having the hydroxy group in position 2 esterified, e.g. benorylate

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Pharmaceutical compsns. comprising DL-lysine acetylsalicylate (I), vitamin E (II) and excipients are new, where (II) is selected from d- and dl- alpha -tocopherols and their salts (esters may be intended). Also claimed is a compsn. as above also contg. beta -carotene (III).

Description

La présente invention a pour objet une association d'acétylsalicylate de DL-lysine et de vitamine E, contenant éventuellement du ss-carotène. The subject of the present invention is a combination of DL-lysine acetylsalicylate and vitamin E, optionally containing ss-carotene.

La source de vitamine E utilisée est l'a-tocophérol racémique ou dextrogyre, naturel ou synthétique, sous forme de base ou d'un sel tel que l'acétate, le palmitate ou le succinate.The source of vitamin E used is racemic or dextrorotatory a-tocopherol, natural or synthetic, in the form of a base or a salt such as acetate, palmitate or succinate.

L'acide acétylsalicylique est un agent antiagrégant plaquettaire connu, dont l'utilisation dans la prévention secondaire des événements cardio- et cérébro-vasculaires a été décrite par exemple dans B. M. J., 436-440 (1974),
J.A.M.A., vol. 260, nO 14, 2088-2093 (1988) et Circulation, vol. 87, nO 2, 659-675 (1993).Acetylsalicylic acid is a known platelet aggregation agent, the use of which in the secondary prevention of cardio- and cerebrovascular events has been described for example in BMJ, 436-440 (1974),
JAMA, vol. 260, no. 14, 2088-2093 (1988) and Circulation, vol. 87, No. 2, 659-675 (1993).

L'acétylsalicylate de lysine, forme soluble dans l'eau et stable, améliore considérablement la tolérance digestive locale de l'acide acétylsalicylique.Lysine acetylsalicylate, a water-soluble and stable form, significantly improves the local digestive tolerance of acetylsalicylic acid.

La vitamine E a également un effet antiagrégant plaquettaire.Vitamin E also has an anti-platelet aggregation effect.

De plus, elle a un effet vasodilatateur de la paroi artérielle.In addition, it has a vasodilating effect on the arterial wall.

La vitamine E et le B-carotène sont connus par ailleurs comme agents antioxydants et piégeurs de radicaux libres.Vitamin E and B-carotene are also known as antioxidants and free radical scavengers.

Or, on sait que les radicaux libres provoquent des altérations des acides nucléiques, des protéines et des lipides cellulaires et jouent donc un rôle dans la cancérogénèse, l'athérogénèse et l'ischémie.However, it is known that free radicals cause alterations in nucleic acids, proteins and cellular lipids and therefore play a role in carcinogenesis, atherogenesis and ischemia.

On sait que la formation d'athéromes est favorisée par le LDL cholestérol oxydé, du fait de son action inhibitrice de la motilité des macrophages tissulaires, de son incorporation aux monocytes dans la paroi artérielle, de son action cytotoxique vis à vis des cellules endothéliales et de son effet vasoconstricteur artériel et par les radicaux libres libérés lors de traumatismes de l'endothélium.It is known that the formation of atheromas is favored by oxidized LDL cholesterol, due to its inhibiting action on the motility of tissue macrophages, its incorporation into monocytes in the arterial wall, its cytotoxic action with respect to endothelial cells and of its arterial vasoconstrictor effect and by free radicals released during trauma to the endothelium.

La vitamine E et le 8-carotène, en s'opposant à l'oxydation du LDL cholestérol et en inactivant les radicaux libres libérés par l'endothélium, préviennent ou réduisent la formation d'athéromes et diminuent ainsi les risques de maladies cardio- et cérébro-vasculaires.Vitamin E and 8-carotene, by opposing the oxidation of LDL cholesterol and by inactivating the free radicals released by the endothelium, prevent or reduce the formation of atheromas and thus reduce the risks of cardio- and cerebrovascular.

D'autre part, la vitamine E et le 8-carotène, en tant qu'antioxydants et piégeurs de radicaux libres, régulateurs de la différenciation cellulaire et stimulants de l'immunité, et la vitamine E, par son effet bloquant de la transformation des nitrosamines en nitrosamides cancérigènes, ont une activité antinéoplasique.On the other hand, vitamin E and 8-carotene, as antioxidants and scavengers of free radicals, regulators of cell differentiation and stimulants of immunity, and vitamin E, by its blocking effect of the transformation of nitrosamines into carcinogenic nitrosamides, have antineoplastic activity.

L'association de l'invention est donc destinée à la prévention primaire des maladies cardio- et cérébrovasculaires, à la prévention secondaire d'événements cardioet cérébro-vasculaires, à la prévention de la resténose après angioplastie coronarienne, à la prévention de l'apparition et/ou de la progression de lésions athéromateuses, à la prévention de l'athéromatose coronarienne et de la sténose des greffons après pontage coronarien et à la prévention des cancers de tous types.The combination of the invention is therefore intended for the primary prevention of cardio- and cerebrovascular diseases, for the secondary prevention of cardio-cerebrovascular events, for the prevention of restenosis after coronary angioplasty, for the prevention of the appearance and / or the progression of atherosclerotic lesions, the prevention of coronary atheromatosis and graft stenosis after bypass surgery and the prevention of cancers of all types.

L'association de l'invention peut être utilisée, en combinaison avec des excipients appropriés, pour la préparation de compositions pharmaceutiques destinées à l'administration par voie orale.The combination of the invention can be used, in combination with suitable excipients, for the preparation of pharmaceutical compositions intended for oral administration.

Les excipients sont choisis parmi les composants utilisés habituellement lors de la formulation et de la fabrication des médicaments, tels que diluants, substances tampons, agents de glissement, aromatisants, édulcorants.The excipients are chosen from the components usually used during the formulation and manufacture of drugs, such as diluents, buffering substances, slip agents, flavorings, sweeteners.

Les compositions pharmaceutiques de l'invention peuvent être présentées sous forme de comprimés, de gélules, de capsules ou de poudre, en particulier de poudre pour solution buvable.The pharmaceutical compositions of the invention can be presented in the form of tablets, capsules, capsules or powder, in particular powder for oral solution.

Elles peuvent contenir de 54 & 540 mg d'acétylsalicylate de
DL-lysine, soit l'équivalent de 30 à 300 mg d'acide acétylsalicylique, de 10 à 1000 UI de vitamine E et, éventuellement, de 5 à 50 mg de B-carotène par dose unitaire.They may contain 54 & 540 mg of acetylsalicylate
DL-lysine, the equivalent of 30 to 300 mg of acetylsalicylic acid, 10 to 1000 IU of vitamin E and, optionally, 5 to 50 mg of B-carotene per unit dose.

Les compositions de l'invention sous forme de poudre sont obtenues par mélanges successifs des différents constituants à sec dans un mélangeur à poudre.The compositions of the invention in powder form are obtained by successive mixtures of the various constituents dry in a powder mixer.

La poudre peut ensuite être transformée en comprimés ou introduite dans des gélules, des capsules ou des sachets dose unitaire selon des méthodes connues en soi.The powder can then be transformed into tablets or introduced into capsules, capsules or sachets unit dose according to methods known per se.

Les exemples suivants illustrent l'invention
Exemple 1 : poudre pour solution buvable acétylsalicylate de DL-lysine 320 mg acétate de DL-a-tocophérol 250 UI
Glycine 35,5 mg
Arome 30 mg
pour 1 sachet
Exemple 2 : poudre pour solution buvable acétylsalicylate de DL-lysine 320 mg acétate de DL-a-tocophérol 250 UI ss-carotène 25 mg
Glycine 35,5 mg
Arome 30 mg
pour un sachet
La posologie journalière est de 54 à 540 mg d'acétylsalicylate de DL-lysine, soit l'équivalent de 30 à 300 mg d'acide acétylsalicylique, de 10 à 1000 UI de vitamine E et de 5 à 50 mg de 8-carotène. The following examples illustrate the invention
Example 1: powder for oral solution DL-lysine acetylsalicylate 320 mg DL-a-tocopherol acetate 250 IU
Glycine 35.5 mg
Aroma 30 mg
for 1 sachet
Example 2: powder for oral solution DL-lysine acetylsalicylate 320 mg DL-a-tocopherol acetate 250 IU ss-carotene 25 mg
Glycine 35.5 mg
Aroma 30 mg
for a sachet
The daily dosage is 54 to 540 mg of DL-lysine acetylsalicylate, the equivalent of 30 to 300 mg of acetylsalicylic acid, 10 to 1000 IU of vitamin E and 5 to 50 mg of 8-carotene.

Claims (7)

RevendicationsClaims 1. Composition pharmaceutique caractérisée en ce qu'elle est constituée d'un mélange d'acétylsalicylate de D,L-lysine et d'a-tocophérol racémique ou dextrogyre, sous forme de base ou d'un sel, en association avec des excipients appropriés.1. Pharmaceutical composition characterized in that it consists of a mixture of D, L-lysine acetylsalicylate and racemic or dextrorotatory α-tocopherol, in the form of a base or of a salt, in association with excipients appropriate. 2. Composition pharmaceutique caractérisée en ce qu'elle est constituée d'un mélange d'acétylsalicylate de D,L-lysine, d'a-tocophérol racémique ou dextrogyre, sous forme de base ou d'un sel, et de ss-carotène, en association avec des excipients appropriés.2. Pharmaceutical composition characterized in that it consists of a mixture of D, L-lysine acetylsalicylate, racemic or dextrorotatory a-tocopherol, in the form of a base or a salt, and ss-carotene , in combination with suitable excipients. 3. Composition pharmaceutique selon l'une des revendications 1 ou 2, caractérisée en ce que l'a-tocophérol est utilisé sous forme d'acétate, de palmitate ou de succinate.3. Pharmaceutical composition according to one of claims 1 or 2, characterized in that the a-tocopherol is used in the form of acetate, palmitate or succinate. 4. Composition pharmaceutique selon l'une des revendications 1 ou 3, caractérisée en ce qu'elle contient 54 à 540 mg d'acétylsalicylate de DL-lysine et 10 à 1000 UI de vitamine E par dose unitaire.4. Pharmaceutical composition according to one of claims 1 or 3, characterized in that it contains 54 to 540 mg of DL-lysine acetylsalicylate and 10 to 1000 IU of vitamin E per unit dose. 5. Composition pharmaceutique selon l'une des revendications 2 ou 3, caractérisée en ce qu'elle contient 54 à 540 mg d'acétylsalicylate de DL-lysine, 10 à 1000 UI de vitamine E et 5 à 50 mg de S-carotène par dose unitaire.5. Pharmaceutical composition according to one of claims 2 or 3, characterized in that it contains 54 to 540 mg of DL-lysine acetylsalicylate, 10 to 1000 IU of vitamin E and 5 to 50 mg of S-carotene per unit dose. 6. Composition pharmaceutique selon l'une quelconque des revendications 1 à 5, caractérisée en ce qu'elle est sous forme de poudre, de comprimés, de gélules ou de capsules.6. Pharmaceutical composition according to any one of claims 1 to 5, characterized in that it is in the form of powder, tablets, capsules or capsules. 7. Composition pharmaceutique selon la revendication 6, caractérisée en ce qu'elle est sous forme de poudre pour solution buvable en sachet dose unitaire. 7. Pharmaceutical composition according to claim 6, characterized in that it is in the form of powder for oral solution in unit dose sachet.
FR9315554A 1993-12-23 1993-12-23 Combination of DL-lysine acetylsalicylate and vitamin E. Expired - Lifetime FR2714292B1 (en)

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FR9315554A FR2714292B1 (en) 1993-12-23 1993-12-23 Combination of DL-lysine acetylsalicylate and vitamin E.

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FR9315554A FR2714292B1 (en) 1993-12-23 1993-12-23 Combination of DL-lysine acetylsalicylate and vitamin E.

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FR2714292A1 true FR2714292A1 (en) 1995-06-30
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0736301A1 (en) * 1995-04-07 1996-10-09 Synthelabo Pharmaceutical composition containing lysine acetylsalicylate and vitamin E
EP0793490A1 (en) * 1994-12-22 1997-09-10 Henkel Corporation Compositions of tocopherol and beta-carotene

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2115060A1 (en) * 1970-11-26 1972-07-07 Metabio Freeze-dried acetylsalicylates of lysine and arginine - easily prepd derivs of aspirin

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2115060A1 (en) * 1970-11-26 1972-07-07 Metabio Freeze-dried acetylsalicylates of lysine and arginine - easily prepd derivs of aspirin

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
STEINER M.: "Vitamin E: More than an antioxidant", CLIN. CARDIOL. (USA), VOL. 16, NO. 4 SUPPL. I PAGE(S) I16-I18, April 1993 (1993-04-01) *
STEINER M: "EFFECT OF ALPHA TOCOPHEROL ADMINISTRATION ON PLATELET FUNCTION IN MAN", THROMB HAEMOSTASIS,, VOL. 49, NO. 2, PAGE(S) 73-77, 1983 *
VIOLI F ET AL: "INHIBITION OF CYCLOOXYGENASE-INDEPENDENT PLATELET AGGREGATION BY LOW VITAMIN E CONCENTRATION", ATHEROSCLEROSIS,, VOL. 82, NO. 3, PAGE(S) 247-252, 1990 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0793490A1 (en) * 1994-12-22 1997-09-10 Henkel Corporation Compositions of tocopherol and beta-carotene
EP0793490A4 (en) * 1994-12-22 1999-12-15 Henkel Corp Compositions of tocopherol and beta-carotene
EP0736301A1 (en) * 1995-04-07 1996-10-09 Synthelabo Pharmaceutical composition containing lysine acetylsalicylate and vitamin E

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FR2714292B1 (en) 1996-02-02

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