FR2620619A1 - Novel pharmaceutical process for obtaining a unique formula for novel and improved therapeutic applications and safety - Google Patents
Novel pharmaceutical process for obtaining a unique formula for novel and improved therapeutic applications and safety Download PDFInfo
- Publication number
- FR2620619A1 FR2620619A1 FR8808828A FR8808828A FR2620619A1 FR 2620619 A1 FR2620619 A1 FR 2620619A1 FR 8808828 A FR8808828 A FR 8808828A FR 8808828 A FR8808828 A FR 8808828A FR 2620619 A1 FR2620619 A1 FR 2620619A1
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- FR
- France
- Prior art keywords
- novel
- safety
- obtaining
- therapeutic applications
- improved therapeutic
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Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
Abstract
Description
Nouveau procédé pharmaceutique pour obtenir une formule
unique pour des usagers et une sécurité thérapeutiques
nouveaux et meilleurs
La présente invention concerne une nouvelle composition pharmaceutique contenant, comme substances actives, du 6-pipéridino-2,4-diamino-pyridine-3-oxyde et de l'acide 15-apo ss-carotène-15-oïque, et un procédé pour la préparer.New pharmaceutical process to obtain a formula
unique for therapeutic users and safety
new and better
The present invention relates to a new pharmaceutical composition containing, as active substances, 6-piperidino-2,4-diamino-pyridine-3-oxide and 15-apo ss-carotene-15-oic acid, and a process for prepare it.
Le but de la présente invention est de produire une efficacité thérapeutique nouvelle et/ou meilleure d'une substance médicamenteuse classique, à l'aide d'une nouvelle composition pharmaceutique qui permet de modifier les propriétés pharmacologiques de chacune de ces substances actives. The aim of the present invention is to produce a new and / or better therapeutic efficacy of a conventional medicinal substance, using a new pharmaceutical composition which makes it possible to modify the pharmacological properties of each of these active substances.
La composition pharmaceutique de cette invention comprend du 6-pipéridino-2,4-diamino-pyridine-3-oxyde que l'on a utilisé couramment dans les formes posologiques orales telles que comprimés, capsules ou solutions, pour traiter l'hypertension grave, ou que l'on a utilisé dans des formes topiques comme des solutions ou des lotions, à raison de 2 à 5%, pour traiter l'alopécie, et de l'acide 15-apo-ss-caro- tène-15-oïque que l'on a également utilisé couramment dans des formes topiques telles que crèmes, gels ou solutions, en différentes concentrations allant de 0,025 à 0,1%, pour traiter principalement l'acné vulgaire. The pharmaceutical composition of this invention comprises 6-piperidino-2,4-diamino-pyridine-3-oxide which has been commonly used in oral dosage forms such as tablets, capsules or solutions, to treat severe hypertension, or that have been used in topical forms like solutions or lotions, at a rate of 2 to 5%, to treat alopecia, and 15-apo-ss-carotene-15-oic acid which has also been commonly used in topical forms such as creams, gels or solutions, in different concentrations ranging from 0.025 to 0.1%, to treat mainly acne vulgaris.
Les modes d'action pharmacologiques de l'acide 15-apo ss-carotène-15-oïque, utilisé localement comme ci-dessus, semblent stimuler l'épithélium pour produire des cellules cornées à une vitesse plus élevée et pour réduire leur cohésion, peut-être en altérant la synthèse ou la qualité de la substance cémentaire qui lie la couche cornée en enclavements, lesquels sont bénéfiques dans le traitement de l'acné vulgaire, dans lequel les comédons, les papules et les pustules prédominent. Les modes d'action du 6-pipéridino-2,4- diamino-pyridine-3-oxyde semblent, quant à eux, agir princi palement en provoquant une vasodilatation périphérique directe dans le traitement de l'hypertension réfractaire lorsqu'on l'utilise oralement, et de l'alopécie lorsqu'on l'utilise localement. The pharmacological modes of action of 15-apo ss-carotene-15-oic acid, used locally as above, appear to stimulate the epithelium to produce horny cells at a higher rate and to reduce their cohesion, may -being by altering the synthesis or the quality of the cementitious substance which binds the horny layer in enclosures, which are beneficial in the treatment of acne vulgaris, in which comedones, papules and pustules predominate. The modes of action of 6-piperidino-2,4-diamino-pyridine-3-oxide seem to act mainly by causing direct peripheral vasodilation in the treatment of refractory hypertension when used orally, and alopecia when used locally.
Le but principal de la présente invention est de développer une nouvelle composition médicamenteuse topique combinant deux ou plusieurs composés de médicaments classiques, qui-peut être plus efficace et présenter moins de danger que l'un ou l'autre des composés seuls, dans le traitement de l'alopécie et de l'acné vulgaire. The main object of the present invention is to develop a new topical drug composition combining two or more compounds of conventional drugs, which may be more effective and present less danger than one or the other of the compounds alone, in the treatment alopecia and acne vulgaris.
Les arrière-plans théoriques de la présente invention sont fondés sur une synergie thérapeutique entre les composés combinés lorsqu'ils sont formulés par l'invention et utilises localement. The theoretical backgrounds of the present invention are based on a therapeutic synergy between the combined compounds when they are formulated by the invention and used locally.
Les avantages précis de la présente invention semblent provenir de la synergie thérapeutique qui exerce des effets plus profonds, même en concentration inférieure, que l'un ou, l'autre des composés seuls, avec des avantages additionnels dans la prophylaxie de l'alopécie et de l'acné vulgaire. The precise advantages of the present invention seem to come from the therapeutic synergy which exerts deeper effects, even at a lower concentration, than one or the other of the compounds alone, with additional advantages in the prophylaxis of alopecia and vulgar acne.
Un autre avantage de cette invention est la meilleure sécurité qu'offre une formulation en concentration 4 à 10 fois moins élevée que la formulation topique à 2-5% classique, lors de l'utilisation prolongée, parfois à vie, du 6 pipéridino-2,4-diamino-pyridine-3-oxyde, qui est un médicament hypertenseur très puissant pouvant causer de sérieux problèmes cardiaques, même en utilisation topique pendant des périodes prolongées. Another advantage of this invention is the better safety offered by a formulation at a concentration 4 to 10 times lower than the conventional topical formulation at 2-5%, during the prolonged use, sometimes for life, of 6 piperidino-2. , 4-diamino-pyridine-3-oxide, which is a very potent hypertensive drug that can cause serious heart problems, even when used topically for extended periods of time.
En outre, l'avantage de cette invention est l'économie des coûts de fabrication due à la concentration de 4 à 10 fois plus faible que la composition classique de 6-pipéridino-2,4-diamino-pyridine-3-oxyde qui est un composé très coûteux, coté actuellement à 2 500-9 000 dollars/kg sur le marché international. In addition, the advantage of this invention is the saving in manufacturing costs due to the concentration of 4 to 10 times lower than the conventional composition of 6-piperidino-2,4-diamino-pyridine-3-oxide which is a very expensive compound, currently quoted at 2,500-9,000 dollars / kg on the international market.
La composition de cette invention peut également contenir, outre les deux composés actifs seuls, du dexpanthénol, du sulfomucopolysaccharide, pour hydrater et nourrir les cheveux, et divers ingrédients pharmaceutiques non actifs, pour donner un système véhicule unique servant à optimiser la stabilité de la composition selon l'invention et l'absorption percutanée de la formulation synergique, afin de garantir un maximum de sécurité et la meilleure efficacité clinique, même lors d'une utilisation prolongée. The composition of this invention may also contain, in addition to the two active compounds alone, dexpanthenol, sulfomucopolysaccharide, to hydrate and nourish the hair, and various non-active pharmaceutical ingredients, to give a unique vehicle system serving to optimize the stability of the composition. according to the invention and the percutaneous absorption of the synergistic formulation, in order to guarantee maximum safety and the best clinical efficacy, even during prolonged use.
Une formulation représentative constituant un mode de réalisation de la présente invention contient, pour des solutions topiques, de 0,02 à 0,1% d'acide 15-apo-ss-carotène- 15-oïque, de 0,2 à 0,1% de 6-pipéridino-2,4-diamino-pyridine-3-oxyde, dans un système véhicule de tonique pour cheveux spécialement conçu, constitué de 1 à 5% de polyvinylpyrrolydone et de copolymères, de 40 à 70% d'alcool isopropylique ou d'éthanol, de 10 à 20% de propylène-glycol ou de glycérine, de 0,5 à 1,0% d'émulsifiant/solubilisant, de 0,5 à 3% de dexpanthénol, de sulfomucopolysaccharide-et de l'eau purifiée en quantité suffisante. A representative formulation constituting an embodiment of the present invention contains, for topical solutions, from 0.02 to 0.1% of 15-apo-ss-carotene-15-oic acid, from 0.2 to 0, 1% 6-piperidino-2,4-diamino-pyridine-3-oxide, in a specially designed vehicle hair tonic system, consisting of 1 to 5% polyvinylpyrrolydone and copolymers, from 40 to 70% alcohol isopropyl or ethanol, 10 to 20% propylene glycol or glycerin, 0.5 to 1.0% emulsifier / solubilizer, 0.5 to 3% dexpanthenol, sulfomucopolysaccharide - and l purified water in sufficient quantity.
Pour une meilleure acceptabilité cosmétique, on peut ajouter des agents colorants, parfums, anti-oxydants ou de l'adipate de diisopropyle de qualité cosmétique. For better cosmetic acceptability, coloring agents, perfumes, antioxidants or diisopropyl adipate of cosmetic quality can be added.
La composition de cette invention destinée à l'utilisation topique a été testée cliniquement dans une clinique dermatologique avec des patients volontaires de 20 alopécies et de 16 acnés vulgaires, comparée à un nombre non identifié de patients souffrant d'alopécie ou d'acné vulgaire traités avec un produit placebo contenant la même proportion de l'un ou l'autre des composés actifs dans le même système véhicule que la composition de l'invention.Les résultats de cet essai clinique montrent que la réponse clinique bonne et excellente à la composition produite par cette invention est de 66 à 90%, en comparaison de O à 58% pour les produits placebo, comme on s'y attendait. I1 n'a pas été possible de comparer le profil de sécurité de la composition produite par l'invention directement aux compositions classiques de l'un ou l'autre des composés seuls. Cependant, personne ne peut contester le fait qu'une concentration de 4 à 10 fois inférieure du médicament cardio-vasculaire puissant, dans la composition de l'invention, peut être une bonne preuve scientifique d'une meilleure sécurité par rapport aux compositions classiques, lors d'une utilisation prolongée. The composition of this invention for topical use has been clinically tested in a dermatological clinic with voluntary patients with 20 alopecia and 16 acne vulgaris, compared to an unidentified number of patients suffering from alopecia or acne vulgaris treated with a placebo product containing the same proportion of one or the other of the active compounds in the same vehicle system as the composition of the invention. The results of this clinical trial show that the good and excellent clinical response to the composition produced by this invention is 66 to 90%, compared to 0 to 58% for placebo products, as expected. It was not possible to compare the safety profile of the composition produced by the invention directly with the conventional compositions of one or the other of the compounds alone. However, no one can dispute the fact that a concentration of 4 to 10 times lower than the powerful cardiovascular drug, in the composition of the invention, can be good scientific proof of better safety compared to conventional compositions, during prolonged use.
Les exemples suivants illustrent plus en détail la présente invention, sans limiter sa portee. The following examples illustrate the present invention in more detail, without limiting its scope.
Exemple 1 a) On dissout 1 g de polymère PVP et 0,5 g de dexpanthénol dans 30 g d'eau purifiée.Example 1 a) 1 g of PVP polymer and 0.5 g of dexpanthenol are dissolved in 30 g of purified water.
b) Séparément, on mélange 50 g d'alcooi éthylique, 1 g d'adipate de diisopropyle et 1 g de solubilisant non ionique, puis on réchauffe le mélange à 40-60 C pour former une solution limpide. On ajoute à la solution limpide ainsi produite 0,5 g de 6-pipéridino-2,4-diamino-pyridine-3-oxyde et 0,025 g d'acide 15-apo-ss-carotène-15-oïque, tout en agitant lentement jusqu'à ce qu'ils se dissolvent complètement. Acette solution alcoolique, maintenue à la température ci-dessus, on ajoute la solution aqueuse obtenue dans la partie (a), préchauffée à 40-600C, puis on ajuste le pH mélange de 5 à 6 en ajoutant des solutions de NaOH ou d'acide citrique, pour compléter le volume de la solution à 100 ml, et on laisse la solution refroidir à la température ambiante pendant une nuit.b) Separately, 50 g of ethyl alcohol, 1 g of diisopropyl adipate and 1 g of nonionic solubilizer are mixed, then the mixture is warmed to 40-60 C to form a clear solution. 0.5 g of 6-piperidino-2,4-diamino-pyridine-3-oxide and 0.025 g of 15-apo-ss-carotene-15-oic acid are added to the clear solution thus produced. until they completely dissolve. This alcoholic solution, maintained at the above temperature, the aqueous solution obtained in part (a) is added, preheated to 40-600C, then the pH mixture is adjusted from 5 to 6 by adding solutions of NaOH or citric acid, to make up the volume of the solution to 100 ml, and the solution is allowed to cool to room temperature overnight.
Enfin, on vérifie la qualité de la composition ainsi obtenue avant de la conditionner en emballages individuels. Finally, the quality of the composition thus obtained is checked before being packaged in individual packages.
Exemple 2
On reprend le mode opératoire de l'exemple 1, sauf qu'on enlève le dexpanthénol.Example 2
The procedure of Example 1 is repeated, except that the dexpanthenol is removed.
Exemple 3
On reprend le mode opératoire de l'exemple 1, sauf qu'on peut en outre ajouter, dans la préparation de la solution aqueuse de la partie (a), 500 à 1 000 unités lipasiques de sulfomucopolysaccharide pancréatique de boeuf. Example 3
The procedure of Example 1 is repeated, except that it is also possible to add, in the preparation of the aqueous solution of part (a), 500 to 1,000 lipase units of pancreatic sulfomucopolysaccharide of beef.
Claims (3)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1019870006990A KR890001556A (en) | 1987-07-01 | 1987-07-01 | Pharmaceutical composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| FR2620619A1 true FR2620619A1 (en) | 1989-03-24 |
| FR2620619B1 FR2620619B1 (en) | 1992-06-05 |
Family
ID=19262648
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FR888808828A Expired - Fee Related FR2620619B1 (en) | 1987-07-01 | 1988-06-30 | NEW PHARMACEUTICAL PROCESS FOR OBTAINING A SINGLE FORMULA FOR NEW AND BETTER THERAPEUTIC USES AND SAFETY |
Country Status (3)
| Country | Link |
|---|---|
| KR (1) | KR890001556A (en) |
| FR (1) | FR2620619B1 (en) |
| IT (1) | IT1219666B (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0717627A1 (en) * | 1993-08-06 | 1996-06-26 | The Procter & Gamble Company | Cosmetic compositions |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100382412B1 (en) * | 2000-05-31 | 2003-05-01 | 김정혜 | Device for and method of cabbage or tumip dried radish leaves |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1983002558A1 (en) * | 1981-11-09 | 1983-08-04 | Gail Sansone Bazzano | The use of retinoids and minoxidil (2,4,-diamino-6-piperidino-pyrimidine-3-oxide) to increase the rate of growth of human scalp hair and to treat certain types of alopecias |
| WO1985003226A1 (en) * | 1984-01-25 | 1985-08-01 | L'oreal | Medicinal composition for the treatment or prevention of acne by oral administration |
| WO1988005653A1 (en) * | 1987-01-28 | 1988-08-11 | Proctor Peter H | Topical composition for stimulating hair growth with stable free radicals |
-
1987
- 1987-07-01 KR KR1019870006990A patent/KR890001556A/en not_active Application Discontinuation
-
1988
- 1988-06-21 IT IT48116/88A patent/IT1219666B/en active
- 1988-06-30 FR FR888808828A patent/FR2620619B1/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1983002558A1 (en) * | 1981-11-09 | 1983-08-04 | Gail Sansone Bazzano | The use of retinoids and minoxidil (2,4,-diamino-6-piperidino-pyrimidine-3-oxide) to increase the rate of growth of human scalp hair and to treat certain types of alopecias |
| WO1985003226A1 (en) * | 1984-01-25 | 1985-08-01 | L'oreal | Medicinal composition for the treatment or prevention of acne by oral administration |
| WO1988005653A1 (en) * | 1987-01-28 | 1988-08-11 | Proctor Peter H | Topical composition for stimulating hair growth with stable free radicals |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0717627A1 (en) * | 1993-08-06 | 1996-06-26 | The Procter & Gamble Company | Cosmetic compositions |
| EP0717627A4 (en) * | 1993-08-06 | 1997-09-10 | Procter & Gamble | Cosmetic compositions |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2620619B1 (en) | 1992-06-05 |
| IT8848116A0 (en) | 1988-06-21 |
| KR890001556A (en) | 1989-03-27 |
| IT1219666B (en) | 1990-05-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| ST | Notification of lapse |