FR2683455A1 - Composition for stimulating the localised synthesis of connective tissue - Google Patents
Composition for stimulating the localised synthesis of connective tissue Download PDFInfo
- Publication number
- FR2683455A1 FR2683455A1 FR9113838A FR9113838A FR2683455A1 FR 2683455 A1 FR2683455 A1 FR 2683455A1 FR 9113838 A FR9113838 A FR 9113838A FR 9113838 A FR9113838 A FR 9113838A FR 2683455 A1 FR2683455 A1 FR 2683455A1
- Authority
- FR
- France
- Prior art keywords
- procaine
- weight
- parts
- composition
- composition according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims description 12
- 210000002808 connective tissue Anatomy 0.000 title description 4
- 230000015572 biosynthetic process Effects 0.000 title description 2
- 238000003786 synthesis reaction Methods 0.000 title description 2
- 230000004936 stimulating effect Effects 0.000 title 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229960004919 procaine Drugs 0.000 claims abstract description 11
- ANPFKWRGHBBICV-UHFFFAOYSA-N C[SiH](O)[SiH2][SiH3].OC(=O)c1ccccc1O Chemical compound C[SiH](O)[SiH2][SiH3].OC(=O)c1ccccc1O ANPFKWRGHBBICV-UHFFFAOYSA-N 0.000 claims abstract description 8
- 239000003814 drug Substances 0.000 claims abstract description 5
- 206010003694 Atrophy Diseases 0.000 claims abstract description 3
- 230000037444 atrophy Effects 0.000 claims abstract description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 230000004048 modification Effects 0.000 claims description 4
- 238000012986 modification Methods 0.000 claims description 4
- 230000000638 stimulation Effects 0.000 claims description 3
- 238000007920 subcutaneous administration Methods 0.000 claims description 3
- VSTDKEWSKBIOMX-UHFFFAOYSA-N CC[SiH](O)[SiH2][SiH3] Chemical compound CC[SiH](O)[SiH2][SiH3] VSTDKEWSKBIOMX-UHFFFAOYSA-N 0.000 claims 2
- 210000001519 tissue Anatomy 0.000 description 5
- 230000008929 regeneration Effects 0.000 description 4
- 238000011069 regeneration method Methods 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 210000004400 mucous membrane Anatomy 0.000 description 3
- 238000011282 treatment Methods 0.000 description 3
- 0 CCC(C)(*)*(C)(CC)c1ccccc1C Chemical compound CCC(C)(*)*(C)(CC)c1ccccc1C 0.000 description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 2
- 230000018109 developmental process Effects 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 102000016942 Elastin Human genes 0.000 description 1
- 108010014258 Elastin Proteins 0.000 description 1
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 1
- 208000034189 Sclerosis Diseases 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229920002549 elastin Polymers 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 229940102223 injectable solution Drugs 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000003589 local anesthetic agent Substances 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 238000006068 polycondensation reaction Methods 0.000 description 1
- 201000003068 rheumatic fever Diseases 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 150000004819 silanols Chemical class 0.000 description 1
- -1 sodium monomethyltrisilanol Chemical compound 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/695—Silicon compounds
Landscapes
- 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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
COXPOSITION POUR LA STIMULATION DE LA
SYNTHESE LOCALISEE DES TISSUS CONJONCTIFS
L'invention concerne une nouvelle composition à caractère pharmaceutique utilisable pour la reconstitution de régions du corps ayant subi des atrophies, voire même la modification localisée et contrôlée de régions choisies du corps par stimulation du développement des tissus concernés.COXPOSITION FOR STIMULATION OF
LOCALIZED SYNTHESIS OF CONNECTIVE TISSUES
The invention relates to a new composition of pharmaceutical nature which can be used for the reconstitution of regions of the body having undergone atrophies, or even the localized and controlled modification of selected regions of the body by stimulation of the development of the tissues concerned.
Dans l'une de ses applications préférées, la composition selon l'invention est destinée à la modification contrôlée du galbe des visages. La régénération ou reconstitution des gencives constituent une autre application importante de l'invention. In one of its preferred applications, the composition according to the invention is intended for the controlled modification of the curve of the faces. Another important application of the invention is the regeneration or reconstitution of the gums.
L'invention met en oeuvre un mélange de deux principes actifs
- de la procaïne de formule
- formula procaine
et, un alcoxysilane ou aryloxysilane pharmaceutiquement acceptable et, plus particulièrement, le salicylate de monométhyltrisilanol de formule
dans laquelle les liaisons hydrogènes qui unissent les fonctions OH des silanols aux fonctions phénol de l'acide salicylique sont suffisamment fortes pour empêcher, même à haute température, la polycondensation et donc l'insolubilisation du salicylate de monométhytrisilanol (principe actif d'un médicament commercialisé sous la marque CONJONCTYL).and, a pharmaceutically acceptable alkoxysilane or aryloxysilane and, more particularly, the monomethyltrisilanol salicylate of formula
in which the hydrogen bonds which unite the OH functions of the silanols with the phenol functions of the salicylic acid are sufficiently strong to prevent, even at high temperature, the polycondensation and therefore the insolubilization of the monomethytrisilanol salicylate (active principle of a marketed drug under the brand CONJONCTYL).
Pris individuellement, ces principes actifs de médicaments sont bien connus. Taken individually, these active drug ingredients are well known.
La procaïne a souvent été utilisée comme anesthésique local. Son utilisation en gérontologie a été envisagée. Procaine has often been used as a local anesthetic. Its use in gerontology has been considered.
De même, la salicylate de monométhyltrisilanol constitue le principe actif d'un médicament qui, (notamment par voie intraveineuse ou orale), permet une régénération du tissu conjonctif et, plus particulièrement, de l'élastine et du collagène, lorsqu'ils ont été détériorés sous l'effet de causes pathologiques. Likewise, monomethyltrisilanol salicylate constitutes the active principle of a medicament which, (in particular by intravenous or oral route), allows a regeneration of the connective tissue and, more particularly, of elastin and collagen, when they have been deteriorated under the effect of pathological causes.
Son utilisation a été recommandée pour le traitement des troubles de l'état général, plus particulièrement dans le domaine rhumatologique (arthroses, rhumatismes inflammatoires et dégénératifs, scléroses des tissus conjonctifs). Its use has been recommended for the treatment of disorders of the general condition, more particularly in the rheumatological field (arthritis, inflammatory and degenerative rheumatism, sclerosis of connective tissues).
De même conduit-il, dans un certain nombre de cas, à un meilleur contrôle du taux sanguin de cholestérol, des lipides et des triglycérides, d'où l'application qui en a également été envisagée en cardiologie. Likewise it leads, in a certain number of cases, to better control of the blood level of cholesterol, lipids and triglycerides, hence the application which has also been considered in cardiology.
L'invention résulte donc de la découverte que l'administration du salicylate de monométhyltrisilanol, dans des conditions permettant sa diffusion localisée dans les tissus, et cela en présence de procaïne, permettait non seulement une régénération, mais une véritable reconstruction des tissus intéressés : d'où la possibilité, par traitements répétés, de développer, voire modifier, le modelé même de ces tissus. The invention therefore results from the discovery that the administration of the monomethyltrisilanol salicylate, under conditions allowing its localized diffusion in the tissues, and this in the presence of procaine, allowed not only a regeneration, but a true reconstruction of the tissues concerned: d '' where the possibility, by repeated treatments, to develop, even modify, the very shape of these tissues.
Afin d'aboutir à cette administration localisée, on a recours principalement à l'administration du mélange des deux principes actifs par voie souscutanée ou hypodermique. In order to achieve this localized administration, recourse is mainly had to the administration of the mixture of the two active principles by subcutaneous or hypodermic route.
Ainsi peut-on, de façon contrôlée, reconstituer, voire développer, localement une modification du galbe d'un visage, voire de la silhouette, d'une personne. Thus we can, in a controlled manner, reconstitute, even develop, locally a modification of the curve of a face, even of the silhouette, of a person.
Dans une application préférée, l'invention - on l'a déjà dit - s'applique de façon avantageuse au traitement des muqueuses gingivales. I1 est non seulement possible d'interrompre une rétraction gingivale en cours, mais aussi de les redévelopper ou reconstituer au volume souhaité. In a preferred application, the invention - as has already been said - is applied advantageously to the treatment of the gingival mucous membranes. It is not only possible to interrupt a gingival retraction in progress, but also to redevelop or reconstitute it at the desired volume.
De préférence les proportions des deux principes actifs au sein de la composition administrable par voie sous-cutanée ou hypodermique, varient de 40 à 49,5 parties en poids de salicylate de monométhyltrisilanol pour 10 à 0,5 parties en poids de procaïne. De façon préférée, ces proportions varient de 45 à 49 parties en poids de salicylate de monométhyltrisilanol pour de 5 à I parties en poids de procaine. Preferably, the proportions of the two active ingredients in the composition which can be administered by the subcutaneous or hypodermic route vary from 40 to 49.5 parts by weight of monomethyltrisilanol salicylate per 10 to 0.5 parts by weight of procaine. Preferably, these proportions vary from 45 to 49 parts by weight of monomethyltrisilanol salicylate for from 5 to I parts by weight of procaine.
Il appartint au praticien de choisir les sites et, à la fois le nombre des injections et les espacements de ces points d'injection, au regard des surfaces de tissus (en particulier dans le cas des muqueuses gingivales) dont la régénération et le développement sont souhaites. Il va sans dire que le protocole d'administration ne peut également que dépendre de la localisation (visage, autres parsies du corps, muqueuses, notamment gencives). It was up to the practitioner to choose the sites and, at the same time the number of injections and the spacings of these injection points, with regard to the tissue surfaces (in particular in the case of the gingival mucous membranes) whose regeneration and development are wishes. It goes without saying that the administration protocol can also only depend on the location (face, other parsies of the body, mucous membranes, especially the gums).
Sans que les indications qui suivent aient le moindre caractère limitatif, il peut être admis que les points d'injection seront espacés les uns des autres de façon à couvrir toute ia surface à traiter à des distances mutuelles de l'ordre de 0,1 à plusieurs centimètres, par exemple 5 cm, la quantité de l'association administrable en chaque site étant de l'ordre de 0,1 à 5 mg (calculée par rapport au salicylate de monométhyltrisilanol) dans la composition administrée. Without the indications which follow having the least limiting character, it can be admitted that the injection points will be spaced from each other so as to cover any ia surface to be treated at mutual distances of the order of 0.1 to several centimeters, for example 5 cm, the amount of the association which can be administered at each site being of the order of 0.1 to 5 mg (calculated relative to the monomethyltrisilanol salicylate) in the composition administered.
A titre d'exemple, une proportion galénique appropriée est une solution à 1 % de monométhyltrisilanol orthohydroxybenzoate de sodium (4,5 ml), une solution à 1 % ae procaïne (0,5 ml) et de l'eau pour soluté injectable (q.s.p.) (100 ml). By way of example, a suitable dosage proportion is a 1% solution of sodium monomethyltrisilanol orthohydroxybenzoate (4.5 ml), a 1% solution of procaine (0.5 ml) and water for injectable solution ( qs) (100 ml).
I1 va de soi que les deux principes actifs peuvent être utilisés sous des formes différentes, par exemple sous -orme de seis pharmaceutiquement acceptables. It goes without saying that the two active ingredients can be used in different forms, for example in the form of pharmaceutically acceptable salts.
De même es compositions mettant en jeu des analogues de I 'un ou de l'autre des deux constituants principaux mentlnnés ci-dessus, ou des deux à la fois, entrent-elles dans le cadre de la protection demandée, par l'intermédiaire des revendications qui suivent : par exemple chlorhydrate de diéthyl-(2,6- xylidil)-acétamide (XYLOCAINER) ou chlorhydrate de diéthylamino-2,6-diméthyl-acétanilide (LIGNOCAINER) en lieu et place de la procaïne. Likewise, the compositions bringing into play analogues of one or the other of the two main constituents mentioned above, or of both at the same time, come within the framework of the protection requested, via Claims which follow: for example diethyl- (2,6-xylidil) -acetamide hydrochloride (XYLOCAINER) or diethylamino-2,6-dimethylacetanilide hydrochloride (LIGNOCAINER) in place of procaine.
Claims (5)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9113838A FR2683455B1 (en) | 1991-11-08 | 1991-11-08 | COMPOSITION FOR STIMULATION OF LOCALIZED SYNTHESIS OF CONNECTIVE TISSUES. |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9113838A FR2683455B1 (en) | 1991-11-08 | 1991-11-08 | COMPOSITION FOR STIMULATION OF LOCALIZED SYNTHESIS OF CONNECTIVE TISSUES. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| FR2683455A1 true FR2683455A1 (en) | 1993-05-14 |
| FR2683455B1 FR2683455B1 (en) | 1994-02-11 |
Family
ID=9418781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FR9113838A Expired - Lifetime FR2683455B1 (en) | 1991-11-08 | 1991-11-08 | COMPOSITION FOR STIMULATION OF LOCALIZED SYNTHESIS OF CONNECTIVE TISSUES. |
Country Status (1)
| Country | Link |
|---|---|
| FR (1) | FR2683455B1 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2725207A1 (en) * | 1994-09-30 | 1996-04-05 | Exsymol Sa | BIOLOGICALLY ACTIVE SILICON-BASED COMPOUNDS, THEIR THERAPEUTIC AND COSMETIC APPLICATIONS |
| EP0796861A1 (en) * | 1996-03-22 | 1997-09-24 | L'oreal | Silated derivatives of salicilic acid with desquamative properties |
| FR2938438A1 (en) * | 2008-11-17 | 2010-05-21 | Guenoun Gilbert | Composition, useful for the elimination of e.g. atheromatous plaques, circulatory ischemia, gerontology and aging disorder, comprises combination of procaine and alkoxysilane or aryloxysilane, preferably monomethytrisilanol salicylate |
| WO2011144248A1 (en) * | 2010-05-20 | 2011-11-24 | Gilbert Guenoun | Composition for removing atheromatous plaque |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0281435A1 (en) * | 1987-02-06 | 1988-09-07 | Jean Gueyne | Therapeutical product based on organic silicon compounds |
| EP0391769A1 (en) * | 1989-04-07 | 1990-10-10 | Jean Gueyne | Therapeutical product based on an organic silicon compound and polycarboxylated poly-amine, particularly useful for treatment of atherome |
-
1991
- 1991-11-08 FR FR9113838A patent/FR2683455B1/en not_active Expired - Lifetime
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0281435A1 (en) * | 1987-02-06 | 1988-09-07 | Jean Gueyne | Therapeutical product based on organic silicon compounds |
| EP0391769A1 (en) * | 1989-04-07 | 1990-10-10 | Jean Gueyne | Therapeutical product based on an organic silicon compound and polycarboxylated poly-amine, particularly useful for treatment of atherome |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2725207A1 (en) * | 1994-09-30 | 1996-04-05 | Exsymol Sa | BIOLOGICALLY ACTIVE SILICON-BASED COMPOUNDS, THEIR THERAPEUTIC AND COSMETIC APPLICATIONS |
| EP0796861A1 (en) * | 1996-03-22 | 1997-09-24 | L'oreal | Silated derivatives of salicilic acid with desquamative properties |
| FR2746397A1 (en) * | 1996-03-22 | 1997-09-26 | Oreal | NOVEL SILICY DERIVATIVES OF SALICYLIC ACID WITH DESQUAMANT PROPERTIES |
| US5756485A (en) * | 1996-03-22 | 1998-05-26 | L'oreal | Silicone-containing derivatives of salicylic acid which have desquamating properties |
| US5900231A (en) * | 1996-03-22 | 1999-05-04 | L'oreal | Silicone-containing derivatives of salicylic acid which have desquamating properties |
| US5906812A (en) * | 1996-03-22 | 1999-05-25 | L'oreal | Silicone-containing derivatives of salicylic acid which have desquamating properties |
| FR2938438A1 (en) * | 2008-11-17 | 2010-05-21 | Guenoun Gilbert | Composition, useful for the elimination of e.g. atheromatous plaques, circulatory ischemia, gerontology and aging disorder, comprises combination of procaine and alkoxysilane or aryloxysilane, preferably monomethytrisilanol salicylate |
| WO2011144248A1 (en) * | 2010-05-20 | 2011-11-24 | Gilbert Guenoun | Composition for removing atheromatous plaque |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2683455B1 (en) | 1994-02-11 |
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