ITMI20081862A1 - COMPOSITION FOR TOPIC USE FOR THE TREATMENT OF LOCALIZED ADIPOSITIES AND RELATED IMAGINATIONS - Google Patents

COMPOSITION FOR TOPIC USE FOR THE TREATMENT OF LOCALIZED ADIPOSITIES AND RELATED IMAGINATIONS Download PDF

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Publication number
ITMI20081862A1
ITMI20081862A1 IT001862A ITMI20081862A ITMI20081862A1 IT MI20081862 A1 ITMI20081862 A1 IT MI20081862A1 IT 001862 A IT001862 A IT 001862A IT MI20081862 A ITMI20081862 A IT MI20081862A IT MI20081862 A1 ITMI20081862 A1 IT MI20081862A1
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IT
Italy
Prior art keywords
treatment
localized
imaginations
composition
phosphatidiicoline
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IT001862A
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Italian (it)
Inventor
Prima Gian Mario Di
Giovanni Lissi
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Funziona Srl
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Priority to IT001862A priority Critical patent/ITMI20081862A1/en
Publication of ITMI20081862A1 publication Critical patent/ITMI20081862A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/06Preparations for care of the skin for countering cellulitis

Description

DESCRIZIONE DEL BREVETTO DI INVENZIONE INDUSTRIALE AVENTE COME DESCRIPTION OF THE INDUSTRIAL INVENTION PATENT HAVING AS

TITOLO : TITLE :

Composizioni ad uso topico per il trattamento delle adiposità localizzate e dei relativi inestetismi . Topical compositions for the treatment of localized adiposity and related imperfections.

DESCRIZIONE DESCRIPTION

Parte 1 : introduzione Part 1: introduction

Per adiposità localizzate si intende l accumulo di grasso (=cellule adipose), specialmente in alcune parti del corpo come parete addominale, glutei e cosce, con danno estetico anche notevole. Localized adiposity means the accumulation of fat (= fat cells), especially in some parts of the body such as the abdominal wall, buttocks and thighs, with even considerable aesthetic damage.

Ciò avviene a seguito di_ abitudini alimentari errate ( dieta ipercalorica, con_ conseguente tendenza all’ obesità ), sedentarietà e carenza di attività fisica, ma anche in seguito ad un intervento chirurgico, oppure ad una gravidanza. This occurs as a result of incorrect eating habits (high-calorie diet, resulting in a tendency to obesity), a sedentary lifestyle and lack of physical activity, but also following surgery, or a pregnancy.

La tendenza ad_accumulare grasso aumenta, comunque, in funzione dell’ età, disquilibri ormonali ( iperandrogenismo nella donna ), di alterazioni metaboliche { sindrome metabolica, iperinsulinismo, diabete di tipo 2 ). The tendency to accumulate fat increases, however, as a function of age, hormonal imbalances (hyperandrogenism in women), metabolic alterations (metabolic syndrome, hyperinsulinism, type 2 diabetes).

Parte 2 : le tecniche precedenti Part 2: the previous techniques

I trattamenti di comune impiego per la rimozione delle adiposità localizzate sono : The treatments commonly used for the removal of localized adiposity are:

- L’ intervento chirurgico o liposuzione. Avviene in anestesia locale e consiste in una vera e propria aspirazione mediante cannula del grasso in eccesso, - Surgery or liposuction. It takes place under local anesthesia and consists of a real aspiration through a cannula of excess fat,

- La mesoterapia. Somministrazione intradermica di principi attivi omeopatici e non, comunque in dosi molto basse,grazie all’ uso di appositi aghi. - Mesotherapy. Intradermal administration of homeopathic and non-homeopathic active ingredients, in any case in very low doses, thanks to the use of special needles.

- L’ intralipoterapia, Si tratta della somministrazione localizzata, per via iniettiva, di principi attivi lipolitici. Nello specifico : fosfatidilcolina e sodio desossicolato. - Intralipotherapy, This is the localized administration, by injection, of lipolytic active ingredients. Specifically: phosphatidylcholine and sodium deoxycholate.

- L' uso di prodotti cosmetici a base di fosfatidilcolina o, molto più spesso, di fosfatidilcolina idrogenata. - The use of cosmetic products based on phosphatidylcholine or, much more often, hydrogenated phosphatidylcholine.

In ogni caso possono costituire un utile complemento massaggi e attività fisica, unitamente ad una dieta appropriata. In any case, massages and physical activity can be a useful complement, together with an appropriate diet.

Parte 3 inconvenienti delie tecniche precedenti. Part 3 drawbacks of previous techniques.

La liposuzione comporta tutti i rischi di un vero e proprio intervento chirurgico, anche se questi possono e.ssere minimizzati ricorrendo a professionisti qualificati e_ a strutture idonee debitamente atrezzate. Le precauzioni da adottare e gli strumenti da impiegare rendono comunque il trattamento piuttosto costoso. Liposuction involves all the risks of a real surgery, even if these can be minimized by resorting to qualified professionals and suitable structures duly equipped. However, the precautions to be taken and the tools to be used make the treatment rather expensive.

La mesoterapia può causare edemi e irritazioni locali. Mesotherapy can cause local edema and irritation.

Inoltre Γ assorbimento di farmaci per via intradermica è lento, specie se i dosaggi sono bassi. Se il preparato utilizzato è infine di natura omeopatica, non esiste Γ avallo della medicina ufficiale. Furthermore, intradermal absorption of drugs is slow, especially if the dosages are low. If the preparation used is finally of a homeopathic nature, there is no Γ endorsement of official medicine.

L’ intralipoterapia non è pure priva di effetti indesiderati : oltre a fenomeni transitori dì gonfiore e arrossamento locale, alcuni autori rilevano vere e proprie alterazioni istologiche, riconducibili a fibrosi_e necrosi sia del tessuto adiposo che di quello vascolare.. In caso di trattamento a lungo termine si può anche determinare la formazione di cisti, con ovvie conseguenze di tipo estetico. Intralipotherapy is also not without undesirable effects: in addition to transient phenomena of local swelling and redness, some authors detect real histological alterations, attributable to fibrosis and necrosis of both adipose and vascular tissue. In case of long-term treatment term can also determine the formation of cysts, with obvious consequences of an aesthetic nature.

Schuller- Petrovic.S e coll. Schuller- Petrovic.S and coll.

Tissue toxic effects of phosphatidylcholine/deoxycholate after subcutaneous injection for fat dissolution in rats and human volunteers. Tissue toxic effects of phosphatidylcholine / deoxycholate after subcutaneous injection for fat dissolution in rats and human volunteers.

Derm Surg.2008 Apr; 34(4): 529-42. Derm Surg. 2008 Apr; 34 (4): 529-42.

L’ impiego di preparazioni cosmetiche è, grazie alle modalità applicative (=uso esterno), praticamente privo di effetti collaterali significativi. The use of cosmetic preparations is, thanks to the application methods (= external use), practically free of significant side effects.

Il frequente ricorso, tuttavia, alla sola fosfatidilcolina idrogenata, che risulta cosmetologicamente più accettabile perché .protegge il mantello idrolipidico cutaneo, solleva dubbi sulla reale efficacia di questi prodotti. Solo la fosfatidilcolina NON idrogenata sembrerebbe in grado di penetrare attraverso la cute e di raggiungere così i depositi di grasso. Questa azione, d’ altro canto, danneggerebbe lo strato superficiale dell’ epidermide, aumentando la perdita di acqua per evaporazione. Frequent use, however, of hydrogenated phosphatidylcholine alone, which is cosmetologically more acceptable because it protects the skin's hydrolipidic mantle, raises doubts about the real effectiveness of these products. Only NON-hydrogenated phosphatidylcholine would appear to be able to penetrate through the skin and thus reach fat deposits. This action, on the other hand, would damage the surface layer of the epidermis, increasing the loss of water by evaporation.

Handbook of Cosmetic Science and Technology, p. 155-163 Edited by A.O. Borei, M. Paye and H.l. Maibach Handbook of Cosmetic Science and Technology, p. 155-163 Edited by A.O. Borei, M. Paye and H.l. Maibach

CRC Press Taylor & Francis Group, Boca Raion 2006 Kosmetic International 1999(1), 104-106. CRC Press Taylor & Francis Group, Boca Raion 2006 Kosmetic International 1999 (1), 104-106.

Anche la fosfatidilcolina NON idrogenata, se non combinata col desossicolato, non garantirebbe comunque una sufficiente attività lipolitica, al fine di dissolvere le adiposità localizzate. Even NON-hydrogenated phosphatidylcholine, if not combined with deoxycholate, would still not guarantee sufficient lipolytic activity, in order to dissolve localized adiposities.

Salti G. e coll. Salti G. and coll.

Phosphatidylchoijne and Sodium Deoxycholate in thè treatment of localized fat_: a double-blind, randomized study. Dermatol Surg 2008 Jan;34{1 ):60-66. Phosphatidylchoijne and Sodium Deoxycholate in the treatment of localized fat_: a double-blind, randomized study. Dermatol Surg 2008 Jan; 34 {1): 60-66.

In conclusione : mentre le tecniche invasive ( chirurgiche ed iniettive ) pongono più che altro problemi di reazioni avverse, quelle non invasive { cosmetiche ) rischiano di non garantire una sufficiente efficacia. In conclusion: while invasive techniques (surgical and injection) pose more problems of adverse reactions, non-invasive ones (cosmetic) risk not guaranteeing sufficient efficacy.

Parte 4 : vantaggi dell’ invenzione Part 4: advantages of the invention

Scopo della presente invenzione.è quello di mettere a disposizione delle utilizzatrici e degli utilizzatori un trattamento non invasivo per le adiposità localizzate ed i relativi in estetismi. Tale trattamento è basato su preparazioni dermatologiche per uso topico, che abbinino in maniera ottimale tollerabilità ed efficacia. Si vogliono in particolare minimizzare gli effetti indesiderati della fosfatidilcolina NON idrogenata sul mantello idrolipidico che protegge fisiologicamente Γ epidermide. The purpose of the present invention is to provide users with a non-invasive treatment for localized adiposity and related aesthetic problems. This treatment is based on dermatological preparations for topical use, which optimally combine tolerability and efficacy. In particular, we want to minimize the undesirable effects of NON-hydrogenated phosphatidylcholine on the hydrolipidic mantle which physiologically protects the epidermis.

Come già accennato, la fosfatidilcolina NON idrogenata deteriora questo sistema di protezione naturale,aumentando sensibilmente le perdite d’ acqua per evaporazione e determinando così secchezza cutanea. As already mentioned, NON-hydrogenated phosphatidylcholine deteriorates this natural protection system, significantly increasing water losses due to evaporation and thus causing skin dryness.

Parte 5 : il concetto inventivo Part 5: the inventive concept

Si è trovato che l associazione di fosfatidilcolina _NON idrogenata, acido desossicolico e/o suoi sali e fosfatidilcolina idrogenata è risultata particolarmente efficace nel trattamento topico delle adiposità localizzate e degli in estetismi ad esse riconducibili. It has been found that the combination of NON-hydrogenated phosphatidylcholine, deoxycholic acid and / or its salts and hydrogenated phosphatidylcholine was found to be particularly effective in the topical treatment of localized adiposities and of the imperfections attributable to them.

Le composizioni oggetto_della presente invenzioni mostrano risultati non spiegabili con la semplice sommatoria degli effetti registrati con la somministrazione separata dei singoli componenti. Questo sembra apparentemente dovuto alla azione idratante indiretta della fosfatidilcolina idrogenata. Tale sostanza, al contrario della fosfatidilcolina NON idrogenata, preserva, stabilizzandolo, il mantello idrolipidico superficiale della pelle, In questo modo si minimizza la perdita d’ acqua per evaporazione, garantendo alla cute un livello di idratazione ottimale, evitando così uno stato di sofferenza da secchezza. Di conseguenza, risulterebbe facilitata la penetrazione in profondità della fosfatidilcolina NON idrogenata e del desossicolato, e quindi la loro azione lipolitica per la dissoluzione delle adiposità localizzate. The compositions object of the present invention show results that cannot be explained with the simple sum of the effects recorded with the separate administration of the single components. This appears apparently due to the indirect moisturizing action of hydrogenated phosphatidylcholine. This substance, unlike NON-hydrogenated phosphatidylcholine, preserves and stabilizes the surface hydrolipidic mantle of the skin, thus minimizing the loss of water by evaporation, guaranteeing the skin an optimal level of hydration, thus avoiding a state of suffering from dryness. Consequently, the deep penetration of NON-hydrogenated phosphatidylcholine and deoxycholate, and therefore their lipolytic action for the dissolution of localized adiposities, would be facilitated.

La migliore sinergia sembra ottenersi quando : The best synergy seems to be obtained when:

- la fosfatidilcolina NON idrogenata ha una - NON-hydrogenated phosphatidylcholine has a

concentrazione tra lo 0.3 ed il 3%, preferibilmente dell' 1% concentration between 0.3 and 3%, preferably 1%

- la fosfatidilcolina idrogenata ha una concentrazione tra lo 0.1 ed il 10%, preferibilmente dello 0.5% - hydrogenated phosphatidylcholine has a concentration between 0.1 and 10%, preferably 0.5%

- il desossicolato. ha una concentrazione non inferiore allo 0.2%, preferibilmente dello 0.5%. - the deoxycholate. it has a concentration of not less than 0.2%, preferably 0.5%.

Parte 6 ; il dettaglio dell’ invenzione Part 6; the detail of the invention

Le composizioni della presente invenzione saranno formulate in modo. da essere adatte ad una applicazione topica sulla cute. The compositions of the present invention will be formulated in a manner. to be suitable for topical application on the skin.

Si presenteranno in forma di gel creme, soluzioni o sospensioni, utilizzando tecniche ed eccipienti convenzionali e comunque compatibili con l uso. Creams, solutions or suspensions will be presented in gel form, using conventional techniques and excipients and in any case compatible with use.

Si riporta qui di seguito un esempio di formulazione secondo , l invenzione. An example of the formulation according to the invention is reported below.

ESEMPIO EXAMPLE

Formulazione in crema Cream formulation

INGREDIENTE QUANTITÀ % IN PESO Liporeductyl 5 Fosfatidilcolina _ 1 Fosfatidilcolina idrogenata 0.5 INGREDIENT AMOUNT% BY WEIGHT Liporeductyl 5 Phosphatidylcholine _ 1 Hydrogenated Phosphatidylcholine 0.5

Sodio desossicolato 0.5 Sodium deoxycholate 0.5

Eccipienti cosmetici q.b. Cosmetic excipients q.s.

Acqua q b. a 100 Water q b. to 100

Parte 7 : il funzionamento dell ’ invenzione Part 7: the operation of the invention

Applicare sulla pelle e massaggiare energicamente fino a totale assorbimento, preferibilmente al mattino, prima di iniziare fa giornata, e.la sera, immediatamente prima di coricarsi. Apply to the skin and massage vigorously until completely absorbed, preferably in the morning, before starting the day, and in the evening, immediately before going to bed.

Il trattamento va continuato fino al raggiungimento di un risultato soddisfacente The treatment should be continued until a satisfactory result is achieved

Parte 8 : chiusura Part 8: closing

Il trovato così concepito è suscettibile di modifiche e varianti, purché rientranti nell ambiti del concetto inventivo. Tutti i dettagli sono infine sostituibili con altri tecnicamente equivalenti. The invention thus conceived is susceptible of modifications and variations, provided they fall within the scope of the inventive concept. Finally, all the details can be replaced with other technically equivalent ones.

Claims (1)

RIVENDICAZIONI 1 ) Composizioni farmaceutiche, medicali, cosmeceutiche e cosmetiche ad uso topico, per il trattamento delle adiposità localizzate e dei relativi inestetismì, contenenti fosfatidiicolina, fosfatidiicolina idrogenata, acido desossicolico e/o suoi sali 2) Composizioni secondo la rivendicazione 1 } contenenti tra lo 0.3 ed il 3% di, fosfatidiicolina in peso, preferibilmente. l’ 1% 3) Composizioni secondo le rivendicazioni 1 ) e 2) contenenti tra lo 0.1 ed il 10% di fosfatidiicolina in peso, preferibilmente l’1% 4) Composizioni secondo le rivendicazioni 1 ), 2) e 3), con un contenuto_dì sodio desossicolato superiore allo 0.2% in peso, preferibilmente lo 0.5% 5) Composizioni. secondo le rivendicazioni 1 ), 2), 3) e 4), in forma di gel, creme, soluzioni o sospensioni.CLAIMS 1) Pharmaceutical, medical, cosmeceutical and cosmetic compositions for topical use, for the treatment of localized adiposity and related imperfections, containing phosphatidiicoline, hydrogenated phosphatidiicoline, deoxycholic acid and / or its salts 2) Compositions according to claim 1, preferably containing between 0.3 and 3% of phosphatidiicoline by weight. 1% 3) Compositions according to claims 1) and 2) containing between 0.1 and 10% of phosphatidiicoline by weight, preferably 1% 4) Compositions according to claims 1), 2) and 3), with a sodium deoxycholate content higher than 0.2% by weight, preferably 0.5% 5) Compositions. according to claims 1), 2), 3) and 4), in the form of gels, creams, solutions or suspensions.
IT001862A 2008-10-21 2008-10-21 COMPOSITION FOR TOPIC USE FOR THE TREATMENT OF LOCALIZED ADIPOSITIES AND RELATED IMAGINATIONS ITMI20081862A1 (en)

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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0739623A1 (en) * 1994-01-19 1996-10-30 Taisho Pharmaceutical Co. Ltd Dermatologic composition
WO2000045774A1 (en) * 1999-02-04 2000-08-10 Phares Pharmaceutical Research Nv Membrane lipid compositions
CA2381571A1 (en) * 1999-08-25 2001-03-01 Merckle Gmbh Phospholipid gel
WO2004108140A1 (en) * 2003-06-05 2004-12-16 Doosan Corporation Composition for inhibiting differentiation or growth of fat cells
US20060127468A1 (en) * 2004-05-19 2006-06-15 Kolodney Michael S Methods and related compositions for reduction of fat and skin tightening
WO2006116486A2 (en) * 2005-04-26 2006-11-02 P.A. Holdings Llc Composition and method for reducing the appearance for cellulite
WO2007135703A2 (en) * 2006-05-18 2007-11-29 Vitrupharma S.R.L. Patch for the treatment of the cellulite and localized adiposity

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0739623A1 (en) * 1994-01-19 1996-10-30 Taisho Pharmaceutical Co. Ltd Dermatologic composition
WO2000045774A1 (en) * 1999-02-04 2000-08-10 Phares Pharmaceutical Research Nv Membrane lipid compositions
CA2381571A1 (en) * 1999-08-25 2001-03-01 Merckle Gmbh Phospholipid gel
WO2004108140A1 (en) * 2003-06-05 2004-12-16 Doosan Corporation Composition for inhibiting differentiation or growth of fat cells
US20060127468A1 (en) * 2004-05-19 2006-06-15 Kolodney Michael S Methods and related compositions for reduction of fat and skin tightening
WO2006116486A2 (en) * 2005-04-26 2006-11-02 P.A. Holdings Llc Composition and method for reducing the appearance for cellulite
WO2007135703A2 (en) * 2006-05-18 2007-11-29 Vitrupharma S.R.L. Patch for the treatment of the cellulite and localized adiposity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ROTUNDA A M ET AL: "Detergent effects of sodium deoxycholate are a major feature of an injectable phosphatidylcholine formulation used for localized fat dissolution", DERMATOLOGIC SURGERY, ELSEVIER SCIENCE, NEW YORK, NY, US, vol. 30, no. 7, 1 July 2004 (2004-07-01), pages 1001 - 1008, XP002331643, ISSN: 1076-0512 *

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