FR2577803A1 - Pharmaceutical compositions based on nifedipine and alfuzosin - Google Patents

Pharmaceutical compositions based on nifedipine and alfuzosin Download PDF

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Publication number
FR2577803A1
FR2577803A1 FR8502725A FR8502725A FR2577803A1 FR 2577803 A1 FR2577803 A1 FR 2577803A1 FR 8502725 A FR8502725 A FR 8502725A FR 8502725 A FR8502725 A FR 8502725A FR 2577803 A1 FR2577803 A1 FR 2577803A1
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Prior art keywords
sep
alfuzosin
nifedipine
pharmaceutical compositions
compositions based
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FR8502725A
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French (fr)
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FR2577803B1 (en
Inventor
Icilio Cavero
Peter Hicks
Salomon Langer
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Synthelabo SA
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Synthelabo SA
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Priority to FR8502725A priority Critical patent/FR2577803B1/en
Priority to EP86400015A priority patent/EP0189336A1/en
Priority to AU52456/86A priority patent/AU5245686A/en
Priority to HU24386A priority patent/HUT39604A/en
Priority to DK22386A priority patent/DK22386A/en
Publication of FR2577803A1 publication Critical patent/FR2577803A1/en
Application granted granted Critical
Publication of FR2577803B1 publication Critical patent/FR2577803B1/en
Priority to US07/106,968 priority patent/US4925837A/en
Expired legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

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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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Pharmaceutical composition containing a combination of nifedipine and alfuzosin.

Description

La présente invention a pour objet des compositions pharmaceutiques a base de nifédipine et d'alfuzosine5 destinées au traitement de maladies cardiovasculaires, plus particulièrement de l'hypertension quelle que soi son origine.The present invention relates to pharmaceutical compositions based on nifedipine and alfuzosine 5 for the treatment of cardiovascular diseases, more particularly hypertension regardless of its origin.

La nifédipine, de formule

Figure img00010001

est connue pour ses propriétés antihypertensives, antiangineuses et antagonistes du calcium
L'alfuzosine, de formule
Figure img00010002

possède également des propriétés antihypartensives.Nifedipine, of formula
Figure img00010001

is known for its antihypertensive, antianginal and calcium antagonist properties
Alfuzosin, of formula
Figure img00010002

also has antihypertensive properties.

La demanderesse a constaté que, de manière surprenante, il existe un effet de synergie important entre les propriétés antihypertensives des deux composés lorsqu'on les associe
Les compositions pharmaceutiques de l'invention ont été soumises à une série d'essais pharmacologiques qui révèlent leurs intéressantes propriétés dans le domaine cardiovasculaire.The Applicant has found that, surprisingly, there is a significant synergistic effect between the antihypertensive properties of the two compounds when they are combined
The pharmaceutical compositions of the invention have been subjected to a series of pharmacological tests which reveal their interesting properties in the cardiovascular field.

Le test utilisé est le suivant : des rats spontanément hypertendus âgés de plus de 5 mois, sont placés pendant 30~mon, dans une cage à air conditionné maintenue à 280C. La pression systolique des rats est mesurée- selon la méthode décrite par Gerold et Tschirky (Arzneim. Forsch. 1968, 18, 1285).The test used is as follows: spontaneously hypertensive rats older than 5 months, are placed for 30 ~ mon, in an air conditioned cage maintained at 280C. The systolic pressure of the rats is measured according to the method described by Gerold and Tschirky (Arzneim, Forsch, 1968, 18, 1285).

On administre à un groupe de 6 rats spontanément hypertendus
0,3 mg/kg ou 1 mg/kg d'alfuzosine séparément ou l'association de nifédipine et d'alfuzosine.A group of 6 spontaneously hypertensive rats is given
0.3 mg / kg or 1 mg / kg of alfuzosin separately or the combination of nifedipine and alfuzosin.

La pression systolique est mesurée avant l'administration des agents thérapeutiques puis 1, 2 ou 3 heures après l'administration d'un des composés ou de l'association de nifédipine et d'alfuzosine.Systolic pressure is measured prior to administration of the therapeutic agents and then 1, 2 or 3 hours after administration of one of the compounds or combination of nifedipine and alfuzosin.

Les résultats sont donnés sous forme de diminutions de la pression sanguine par rapport à la pression de base.The results are given as decreases in blood pressure relative to the basal pressure.

Dans le tableau suivant sont donnés les résultats obtenus, et pour les composés administrés seuls, et pour les associations de nifédipine et d'alfuzosine. In the following table are given the results obtained, and for the compounds administered alone, and for the combinations of nifedipine and alfuzosin.

Tableau

Figure img00030001
Board
Figure img00030001

<tb> <SEP> dose <SEP> pression <SEP> Diminution <SEP> de <SEP> la
<tb> Composé <SEP> mg/kg <SEP> p.o. <SEP> de <SEP> base <SEP> pression <SEP> systolique
<tb> <SEP> (mm <SEP> Hg) <SEP> (mm <SEP> Hg) <SEP>
<tb> <SEP> 1h <SEP> 2h <SEP> 3h <SEP>
<tb> nifédipine <SEP> 10 <SEP> 219 <SEP> + <SEP> 4 <SEP> -23+4 <SEP> -6+9 <SEP> -5+4
<tb> alfuzosine <SEP> 0,3 <SEP> 213 <SEP> + <SEP> 2 <SEP> 45 <SEP> -1+4 <SEP> 13+4
<tb> alfuzosine <SEP> 1 <SEP> 216 <SEP> + <SEP> 2 <SEP> -2+6 <SEP> 5+7 <SEP> 18+7 <SEP>
<tb> nifédipine <SEP> 10+0,3 <SEP> 211 <SEP> + <SEP> 3 <SEP> 474* <SEP> -355* <SEP> -322* <SEP>
<tb> +alfuzosine
<tb> nifédipine <SEP> 10+1 <SEP> 219 <SEP> 3 <SEP> -668* <SEP> -596* <SEP> -555* <SEP>
<tb> + <SEP> alfuzosine
<tb> * Effet significativement supérieur à une simple addition des effets de chacun des composés. <tb><SEP> dose <SEP> pressure <SEP> Decrease <SEP> of <SEP> la
<tb> Compound <SEP> mg / kg <SEP> po <SEP> of <SEP> base <SEP> systolic pressure <SEP>
<tb><SEP> (mm <SEP> Hg) <SEP> (mm <SEP> Hg) <SEP>
<tb><SEP> 1h <SEP> 2h <SEP> 3h <SEP>
<tb> nifedipine <SEP> 10 <SEP> 219 <SEP> + <SEP> 4 <SEP> -23 + 4 <SEP> -6 + 9 <SEP> -5 + 4
<tb> alfuzosin <SEP> 0.3 <SEP> 213 <SEP> + <SEP> 2 <SEP> 45 <SEP> -1 + 4 <SEP> 13 + 4
<tb> alfuzosin <SEP> 1 <SEP> 216 <SEP> + <SEP> 2 <SEP> -2 + 6 <SEP> 5 + 7 <SEP> 18 + 7 <SEP>
<tb> nifedipine <SEP> 10 + 0.3 <SEP> 211 <SEP> + <SEP> 3 <SEP> 474 * <SEP> -355 * <SEP> -322 * <SEP>
<tb> + alfuzosin
<tb> nifedipine <SEP> 10 + 1 <SEP> 219 <SEP> 3 <SEP> -668 * <SEP> -596 * <SEP> -555 * <SEP>
<tb> + <SEP> alfuzosin
<tb> * Significantly greater effect than a simple addition of the effects of each of the compounds.

Ces résultats montrent que l'association de nifédipine avec l'alfuzosine produit un effet antihypertenseur significativement plus important que la somme des effets engendrés par chacun des composés administrés isolément.These results show that the combination of nifedipine with alfuzosin produces a significantly greater antihypertensive effect than the sum of the effects generated by each of the compounds administered alone.

Il existe donc une synergie entre.les effets antihypertenseurs de la -nifédipine et de l'alfuzosine.There is therefore a synergy between the antihypertensive effects of nifedipine and alfuzosin.

Les compositions pharmaceutiques de l'invention peuvent contenir de 5 à 20 mg de nifédipine et de 0,5 à 10 mg d'alfuzosine par unité de prise.The pharmaceutical compositions of the invention may contain from 5 to 20 mg of nifedipine and from 0.5 to 10 mg of alfuzosin per unit dose.

Les compositions pharmaceutiques de l'invention peuvent être présentées sous toute forme appropriée pour l'administration par voie orale ou parentérale, en association avec tout excipient approprié.The pharmaceutical compositions of the invention may be presented in any form suitable for oral or parenteral administration, in combination with any suitable excipient.

Les compositions pharmaceutiques de l'invention peuvent être utilisées pour le traitement de l'hypertension et pour le traitement d'autres maladies telles que l'asthme, l'angine de poitrine, l'athérosclérose et les affections urologiques.The pharmaceutical compositions of the invention can be used for the treatment of hypertension and for the treatment of other diseases such as asthma, angina pectoris, atherosclerosis and urological diseases.

La posologie quotidienne est telle que l'on administre de 10 à 30 mg de nifédipine et de 0,5 à 20 mg d'alfuzosine. The daily dosage is such that 10 to 30 mg of nifedipine and 0.5 to 20 mg of alfuzosin are administered.

Claims (2)

Revendicationsclaims 1. Composition pharmaceutique contenant une association de nifédipine et d'alfuzosine.1. A pharmaceutical composition containing a combination of nifedipine and alfuzosin. 2. Composition selon la revendication 1 caractérisée en ce qu'elle contient de 5 à 20 mg de nifédipine et de 0,5 à 10 mg d'alfuzosine par unité de prise. 2. Composition according to claim 1 characterized in that it contains 5 to 20 mg of nifedipine and 0.5 to 10 mg of alfuzosin per unit setting.
FR8502725A 1984-09-14 1985-02-26 PHARMACEUTICAL COMPOSITIONS BASED ON NIFEDIPINE AND ALFUZOSINE Expired FR2577803B1 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
FR8502725A FR2577803B1 (en) 1985-02-26 1985-02-26 PHARMACEUTICAL COMPOSITIONS BASED ON NIFEDIPINE AND ALFUZOSINE
EP86400015A EP0189336A1 (en) 1985-01-18 1986-01-07 Pharmaceutical compositions containing an alpha-blocker and a calcium antagonist
AU52456/86A AU5245686A (en) 1985-01-18 1986-01-17 Compositions of alpha blocking and calcium-antagonistic compounds
HU24386A HUT39604A (en) 1985-01-18 1986-01-17 Process for producing pharmaceutical compositions containing alpha-blocking agents and calcium-antagonistic agents
DK22386A DK22386A (en) 1985-01-18 1986-01-17 MEDICINE CONTAINING A COMBINATION OF AN ALFA BLOCKER AND A CALCIUM ANTAGONIST
US07/106,968 US4925837A (en) 1984-09-14 1987-10-13 Pharmaceutical compositions

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR8502725A FR2577803B1 (en) 1985-02-26 1985-02-26 PHARMACEUTICAL COMPOSITIONS BASED ON NIFEDIPINE AND ALFUZOSINE

Publications (2)

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FR2577803A1 true FR2577803A1 (en) 1986-08-29
FR2577803B1 FR2577803B1 (en) 1987-04-03

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FR8502725A Expired FR2577803B1 (en) 1984-09-14 1985-02-26 PHARMACEUTICAL COMPOSITIONS BASED ON NIFEDIPINE AND ALFUZOSINE

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2421888A1 (en) * 1978-02-06 1979-11-02 Synthelabo ALKYLENE DIAMINE AMIDES AND THEIR APPLICATION IN THERAPEUTICS
FR2466462A2 (en) * 1978-02-06 1981-04-10 Synthelabo Antihypertensive quinazoline derivs. - substd. by 2-acylamino: alkylamino group

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2421888A1 (en) * 1978-02-06 1979-11-02 Synthelabo ALKYLENE DIAMINE AMIDES AND THEIR APPLICATION IN THERAPEUTICS
FR2445323A2 (en) * 1978-02-06 1980-07-25 Synthelabo ALKYLENEDIAMINE AMIDES AND THEIR THERAPEUTIC APPLICATION
FR2466462A2 (en) * 1978-02-06 1981-04-10 Synthelabo Antihypertensive quinazoline derivs. - substd. by 2-acylamino: alkylamino group

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