ITMI20110954A1 - COMBINATIONS FOR THE TREATMENT OF VAGINAL OR RECTAL MUCOSITES - Google Patents

COMBINATIONS FOR THE TREATMENT OF VAGINAL OR RECTAL MUCOSITES Download PDF

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ITMI20110954A1
ITMI20110954A1 IT000954A ITMI20110954A ITMI20110954A1 IT MI20110954 A1 ITMI20110954 A1 IT MI20110954A1 IT 000954 A IT000954 A IT 000954A IT MI20110954 A ITMI20110954 A IT MI20110954A IT MI20110954 A1 ITMI20110954 A1 IT MI20110954A1
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vaginal
rectal
treatment
gel
composition according
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IT000954A
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Italian (it)
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Edoardo Conti
Paolo Giorgetti
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Professional Dietetics Srl
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Priority to IT000954A priority Critical patent/ITMI20110954A1/en
Priority to PCT/EP2012/059018 priority patent/WO2012159937A1/en
Publication of ITMI20110954A1 publication Critical patent/ITMI20110954A1/en

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Reproductive Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gynecology & Obstetrics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Description

Descrizione Description

“COMPOSIZIONI PER IL TRATTAMENTO DELLE MUCOSITI VAGINALI O RETTALI†⠀ œCOMPOSITIONS FOR THE TREATMENT OF VAGINAL OR RECTAL MUCOSITESâ €

La presente invenzione ha per oggetto l’uso di una combinazione di glicina, prolina, ed eventualmente un polimero filmogeno naturale o sintetico, e/o lisina e/o leucina, per la preparazione di composizioni per l’uso nel trattamento delle mucositi vaginali o rettali. The present invention relates to the use of a combination of glycine, proline, and possibly a natural or synthetic film-forming polymer, and / or lysine and / or leucine, for the preparation of compositions for use in the treatment of mucositis vaginal or rectal.

Background tecnico Technical background

Le mucositi sono condizioni patologiche per lo più su base infiammatoria a carico delle mucose. Le mucositi possono interessare ad esempio le mucose orali, rettali o vaginali. Mucositis are pathological conditions mostly on an inflammatory basis affecting the mucous membranes. Mucositis can affect, for example, the oral, rectal or vaginal mucous membranes.

Sono state descritte composizioni utili in particolare per il trattamento di mucositi orali che comprendono agenti antiinfiammatori associati ad agenti filmogeni capaci di formare un rivestimento protettivo sulla mucosa. Compositions useful in particular for the treatment of oral mucositis have been described which comprise anti-inflammatory agents associated with film-forming agents capable of forming a protective coating on the mucosa.

Le mucositi a carico di altre mucose, in particolare quella rettale e quella vaginale, presentano problematiche diverse sia per le diverse caratteristiche istologiche delle mucose sia per le diverse cause patogenetiche. The mucositis of other mucous membranes, in particular the rectal and vaginal ones, present different problems both for the different histological characteristics of the mucous membranes and for the different pathogenetic causes.

Se infatti le mucositi orali sono per lo più causate da un sistema immunitario alterato, ad esempio in seguito a trattamenti chemioterapici o radioterapici, le mucositi vaginali (vaginiti o vaginosi) e le mucositi rettali (proctiti) possono essere determinate anche da infezioni batteriche, virali micotiche, parassiti, da allergie da contatto o alimentari, da interventi chirurgici e simili. La flora batterica vaginale e quella rettale sono inoltre diverse dalla flora batterica che alberga nella mucosa orale. In fact, if oral mucositis are mostly caused by an impaired immune system, for example following chemotherapy or radiotherapy treatments, vaginal mucositis (vaginitis or vaginosis) and rectal mucositis (proctitis) can also be caused by bacterial, viral infections fungi, parasites, contact or food allergies, surgery and the like. The vaginal and rectal bacterial flora are also different from the bacterial flora that resides in the oral mucosa.

Sono noti diversi prodotti, per lo più a base di antibattericiantimicotici, utili nel trattamento di vaginiti e proctiti ma esiste ancora l’esigenza di prodotti ben tollerati che possano agire non solo sull’agente eziologico (batteri, virus o funghi) ma che siano in grado di esercitare un’azione trofica a livello mucosale e di diminuire rapidamente i fenomeni legati all’infiammazione a gli stati dolorosi tipici di queste affezioni. Several products are known, mostly based on anti-bacterial and anti-fungal, useful in the treatment of vaginitis and proctitis but there is still a need for well-tolerated products that can act not only on the etiological agent (bacteria, viruses or fungi) but which are able to exert a trophic action at the mucosal level and to rapidly decrease the phenomena related to inflammation and the painful states typical of these diseases.

È noto che un’associazione di glicina, lisina, leucina e prolina e sodio ialuronato à ̈ particolarmente efficace nell’agevolazione del processo di reintegrazione cellulare alla base di una veloce cicatrizzazione delle ferite cutanee. I processi di cicatrizzazione cutanea non sono assimilabili tuttavia alle condizioni di infiammazione cronica che caratterizzano le mucositi vaginali e rettali. It is known that an association of glycine, lysine, leucine and proline and sodium hyaluronate is particularly effective in facilitating the cellular reintegration process at the base of a fast healing of skin wounds. However, skin healing processes cannot be assimilated to the conditions of chronic inflammation that characterize vaginal and rectal mucositis.

Descrizione dell’invenzione Description of the invention

Si à ̈ ora trovato che combinazioni comprendenti glicina, prolina eventualmente associati a un polimero filmogeno naturale o sintetico, ed eventualmente anche a lisina e/o leucina, sono efficaci nel trattamento delle mucositi rettali o vaginali di varia origine. It has now been found that combinations comprising glycine, proline optionally associated with a natural or synthetic film-forming polymer, and possibly also with lysine and / or leucine, are effective in the treatment of rectal or vaginal mucositis of various origins.

Le composizioni dell’invenzione sono risultate particolarmente efficaci sotto il profilo della gestione del dolore nei pazienti. The compositions of the invention have been found to be particularly effective in terms of pain management in patients.

Infatti, le composizioni della presente invenzione mostrano un notevole effetto di accelerazione della cicatrizzazione delle lesioni, ma soprattutto un sorprendente effetto sulla gestione del dolore, in termini di riduzione del dolore e di sollievo immediato (già 2 ore dopo la somministrazione). In fact, the compositions of the present invention show a notable effect of accelerating wound healing, but above all a surprising effect on pain management, in terms of pain reduction and immediate relief (already 2 hours after administration).

Di conseguenza l’uso delle composizioni secondo l’invenzione costituisce un aiuto concreto nella gestione del dolore, offrendo un effetto analgesico rapido ed efficace. Consequently, the use of the compositions according to the invention constitutes a concrete aid in the management of pain, offering a rapid and effective analgesic effect.

Pertanto, la presente invenzione ha per oggetto l’uso di una composizione comprendente: Therefore, the present invention relates to the use of a composition comprising:

a) glicina, a) glycine,

b) prolina, b) proline,

ed eventualmente and eventually

c) un polimero filmogeno naturale o sintetico, e/o c) a natural or synthetic film-forming polymer, and / or

d) lisina, e/o d) lysine, and / or

e) leucina, e) leucine,

per la preparazione di una composizione per il trattamento delle mucositi rettali o vaginali. for the preparation of a composition for the treatment of rectal or vaginal mucositis.

Secondo l’invenzione, il polimero filmogeno naturale o sintetico à ̈ scelto tra acido ialuronico o un suo sale, polivinilpirrolidone e derivati di cellulosa. According to the invention, the natural or synthetic film-forming polymer is chosen from hyaluronic acid or one of its salt, polyvinylpyrrolidone and cellulose derivatives.

Secondo un aspetto preferito, il polimero filmogeno naturale o sintetico à ̈ l’acido ialuronico o un suo sale, tipicamente sodio ialuronato. Gli amminoacidi sono preferibilmente presenti nella forma L. According to a preferred aspect, the natural or synthetic film-forming polymer is hyaluronic acid or a salt thereof, typically sodium hyaluronate. The amino acids are preferably present in the L form.

Secondo un aspetto preferito, le composizioni secondo l’invenzione conterranno i vari componenti attivi nei seguenti intervalli di composizione in peso: According to a preferred aspect, the compositions according to the invention will contain the various active components in the following composition ranges by weight:

a) da 0,5 a 20% di glicina, a) 0.5 to 20% glycine,

b) da 0,2 a 15% di prolina, b) 0.2 to 15% proline,

ed eventualmente and eventually

c) da 0,5 a 5% di acido ialuronico o un suo sale, e/o c) from 0.5 to 5% of hyaluronic acid or a salt thereof, and / or

d) da 0,05 a 10% di lisina, e/o d) 0.05 to 10% lysine, and / or

e) da 0,05% a 3% di leucina. e) from 0.05% to 3% of leucine.

Le composizioni della presente invenzione potranno essere formulate in modo adatto alla somministrazione per via topica orale sotto forma di spray, crema, unguento o gel, e saranno preparate secondo metodi convenzionali ben noti in tecnica farmaceutica, come quelli descritti in “Remington’s Pharmaceutical Handbook†, Mack Publishing Co., N.Y., USA, utilizzando eccipienti, solubilizzanti, emollienti, stabilizzanti, emulsionanti, regolatori di pH, conservanti accettabili per il loro uso finale. The compositions of the present invention can be formulated in a manner suitable for oral topical administration in the form of spray, cream, ointment or gel, and will be prepared according to conventional methods well known in the pharmaceutical technique, such as those described in â € œRemingtonâ € ™ s Pharmaceutical Handbookâ €, Mack Publishing Co., N.Y., USA, using excipients, solubilizers, emollients, stabilizers, emulsifiers, pH regulators, preservatives that are acceptable for their final use.

Si riportano di seguito esempi di formulazioni preferite secondo l’invenzione. Examples of preferred formulations according to the invention are reported below.

ESEMPIO 1: GEL RETTALE EXAMPLE 1: RECTAL GEL

INGREDIENTI Composizione % INGREDIENTS Composition%

ACQUA DEPURATA 88,67 PURIFIED WATER 88.67

SODIO JALURONATO 2,00 SODIUM HYALURONATE 2.00

GLICINA 2,00 GLYCINE 2.00

L PROLINA 1,50 L PROLINA 1.50

L LEUCINA 0,30 L LEUCINE 0.30

L LISINA Hcl 0,20 L LYSINE Hcl 0.20

METILPARAOSSIBENZOATO 0,30 METHYL PARAOXYBENZOATE 0.30

PROPILPARAOSSIBENZOATO 0,03 PROPYLPARAOXYBENZOATE 0.03

GLICOLE PROPILENICO 5,00 PROPYLENE GLYCOL 5,00

ESEMPIO 2: CREMA PER APPLICAZIONE VAGINALE EXAMPLE 2: CREAM FOR VAGINAL APPLICATION

Composizione INGREDIENTI Composition INGREDIENTS

% Acqua purificata 82,27 Jaluronato sodico 1,33 Glicina 1.00 % Purified water 82.27 Sodium hyaluronate 1.33 Glycine 1.00

L-Prolina 0,75 L-Proline 0.75

L-Leucina 0,15 L-Leucine 0.15

L-Lisina HCl 0,10 Cetil stearil ottanoato (Saboderm CSO) 6,00 Acrylic acid and vinyl ester copolymer (Stabylen30) 0,30 Cetil stearil alcol (Lanette O) 4,00 Potassio cetil fosfato (Amphisol K) 3,00 Imidazolidinil urea 0,30 Fenossietanol-parabens (Sepicide Hb2) 0,60 L-Lysine HCl 0.10 Cetyl stearyl octanoate (Saboderm CSO) 6.00 Acrylic acid and vinyl ester copolymer (Stabylen30) 0.30 Cetyl stearyl alcohol (Lanette O) 4.00 Potassium cetyl phosphate (Amphisol K) 3.00 Imidazolidinyl urea 0.30 Phenoxyethanol-parabens (Sepicide Hb2) 0.60

32% Idrossido di sodio 0,20 32% Sodium hydroxide 0.20

SPERIMENTAZIONE CLINICA CLINICAL TRIAL

Gel rettale Rectal gel

Le mucositi rettali, idiopatiche, aspecifiche o iatrogene (stipsi ostinata, radioterapia, o altro) risentono favorevolmente dell’uso del gel rettale dell’invenzione. Rectal mucositis, idiopathic, non-specific or iatrogenic (obstinate constipation, radiotherapy, or other) are favorably affected by the use of the rectal gel of the invention.

I noti effetti della attivazione delle pompe energetiche mitocondriali, e della inibizione di iNOS portano ad una diminuzione della flogosi, e alla disattivazione di tutti quei meccanismi che la stessa genera. The known effects of the activation of the mitochondrial energy pumps, and of the inhibition of iNOS lead to a decrease in inflammation, and to the deactivation of all those mechanisms that it generates.

È stato condotto uno studio osservazionale su un campione di 20 pazienti, 10 trattati con 3 ml di gel rettale dell’invenzione, e 10 con placebo. An observational study was conducted on a sample of 20 patients, 10 treated with 3 ml of the rectal gel of the invention, and 10 with placebo.

L’applicazione del gel e del placebo à ̈ stata effettuata due volte al giorno, la mattina e la sera. Sono stati presi in considerazione i seguenti parametri: dolore (valutato in accordo con la scala VAS 1-10), flogosi, stato del Pattern Vascolare Mucoso (PVM), tenesmo rettale, ematochezia (l’emissione di feci di un colore anomalo, rosso o marrone), e discomfort evacuativo. Lo studio ha evidenziato come l’uso del gel rettale dell’invenzione abbia clinicamente migliorato la Quality of Life (QoL) dei pazienti trattati, agendo positivamente su due fondamentali meccanismi, ovvero: riduzione della flogosi e diminuzione del dolore. The application of the gel and the placebo was carried out twice a day, in the morning and in the evening. The following parameters were taken into consideration: pain (evaluated according to the VAS 1-10 scale), inflammation, state of the mucous vascular pattern (PVM), rectal tenesmus, hematochezia (the emission of faeces of an abnormal color, red or brown), and evacuative discomfort. The study highlighted how the use of the invented rectal gel has clinically improved the Quality of Life (QoL) of the patients treated, acting positively on two fundamental mechanisms, namely: reduction of inflammation and reduction of pain.

I risultati ottenuti sono riportati nella Tabella 1 seguente. The results obtained are reported in the following Table 1.

Tabella 1 Table 1

PARAMETRO PLACEBO GEL RETTALE RECTAL PLACEBO GEL PARAMETER

1 DOLORE 1 PAIN

6 2 (scala VAS 1-10) 6 2 (scale VAS 1-10)

2 FLOGOSI 2 FLOGOSIS

Moderata Lieve (Lieve-Moderata-Severa) Moderate Mild (Mild-Moderate-Severe)

3 STATO PVM Moderato Lieve (Pattern Vascolare Mucoso) (Anoscopia) (Anoscopia) 4 TENESMO RETTALE 3 PVM STATUS Moderate Mild (Mucosal Vascular Pattern) (Anoscopy) (Anoscopy) 4 RECTAL TENESMUS

Presente Presente (Presente-Assente) Present Present (Present-Absent)

5 EMATOCHEZIA 5 HEMATOCHEZIA

Presente Assente (Presente-Assente) Present Absent (Present-Absent)

6 DISCOMFORT 6 DISCOMFORT

EVACUATIVO Presente Assente (Presente-Assente) EVACUATIVE Present Absent (Present-Absent)

Gel vaginale Vaginal gel

Le mucositi vaginali, idiopatiche, aspecifiche o iatrogene (da trattamenti con antibiotici, radioterapia, o altro) risentono favorevolmente dell’uso del gel vaginale dell’invenzione. Vaginal mucositis, idiopathic, non-specific or iatrogenic (from treatments with antibiotics, radiotherapy, or other) are favorably affected by the use of the vaginal gel of the invention.

È stato condotto uno studio osservazionale su un campione di 20 pazienti, 10 trattate con 2 ml di gel vaginale dell’invenzione, e 10 con placebo. L’applicazione del gel e del placebo à ̈ stata effettuata due volte al giorno, la mattina e la sera. Sono stati presi in considerazione i seguenti parametri: eritema della mucosa, soluzione di continuità della mucosa, dolore (valutata in accordo con la scala vas 1-10), edema, edema perilesionale, secchezza /distrofia della mucosa e dispareunia (dolore avvertito nell'area della vagina o della pelvi durante un rapporto sessuale). An observational study was conducted on a sample of 20 patients, 10 treated with 2 ml of the vaginal gel of the invention, and 10 with placebo. The application of the gel and the placebo was carried out twice a day, in the morning and in the evening. The following parameters were considered: mucosal erythema, mucosal continuity solution, pain (assessed according to the vas scale 1-10), edema, periwound edema, mucosal dryness / dystrophy and dyspareunia (pain felt in the area of the vagina or pelvis during intercourse).

Lo studio ha evidenziato come l’uso del gel vaginale dell’invenzione abbia clinicamente migliorato la Quality of Life (QoL) delle pazienti trattate, agendo positivamente sia a livello del dolore, sia a livello dell’edema e della distrofia della mucosa vaginale, e di conseguenza esercitando anche un effetto benefico sulla dispareunia. The study showed that the use of the vaginal gel of the invention has clinically improved the Quality of Life (QoL) of the treated patients, acting positively both in terms of pain and in terms of edema and mucosal dystrophy. vaginal, and consequently also exerting a beneficial effect on dyspareunia.

I risultati ottenuti sono riportati nella Tabella 2 seguente. The results obtained are reported in the following Table 2.

Tabella 2 Table 2

PARAMETRO PLACEBO<GEL>PLACEBO <GEL> PARAMETER

VAGINALEVAGINAL

1 ERITEMA della MUCOSA 1 ERITEMA of the MUCOSA

Moderato Assente (Lieve - Moderato - Severo) Moderate Absent (Mild - Moderate - Severe)

2 SOLUZIONE DI CONTINUITÀ 2 CONTINUITY SOLUTION

(Puntiforme - Ragadiforme - Puntiforme Assente Confluente (Point-like - Ragadiform - Point-like Absent Confluent

3 DOLORE 3 PAIN

8 4 (Scala VAS 1-10) 8 4 (Scale VAS 1-10)

4 EDEMA 4 EDEMA

Moderato Assente (Lieve - Moderato - Severo) Moderate Absent (Mild - Moderate - Severe)

5 EDEMA PERILESIONALE 5 PERILESIONAL EDEMA

Presente > 1 cm Assente (Presente-Assente) Present> 1 cm Absent (Present-Absent)

6 SECCHEZZA/DISTROFIA 6 DRYNESS / DYSTROPHY

DELLA MUCOSA Moderata Assente (Lieve-Moderata-Severa) MUCOSA Moderate Absent (Mild-Moderate-Severe)

7 DISPAREUNIA 7 DISPAREUNIA

Presente Assente (Presente-Assente) Present Absent (Present-Absent)

Claims (6)

RIVENDICAZIONI 1. Composizione comprendente: a) glicina, b) prolina, ed eventualmente c) un polimero filmogeno naturale o sintetico, e/o d) lisina, e/o e) leucina, per l’uso nel trattamento delle mucositi vaginali o rettali. CLAIMS 1. Composition comprising: a) glycine, b) proline, and eventually c) a natural or synthetic film-forming polymer, and / or d) lysine, and / or e) leucine, for use in the treatment of vaginal or rectal mucositis. 2. Composizione secondo la rivendicazione 1, in cui il polimero filmogeno naturale o sintetico à ̈ scelto tra acido ialuronico o un suo sale, polivinilpirrolidone e derivati di cellulosa. 2. Composition according to claim 1, wherein the natural or synthetic film-forming polymer is selected from hyaluronic acid or a salt thereof, polyvinylpyrrolidone and cellulose derivatives. 3. Composizione secondo la rivendicazione 2, in cui il polimero filmogeno naturale o sintetico à ̈ l’acido ialuronico o un suo sale. 3. Composition according to claim 2, wherein the natural or synthetic film-forming polymer is hyaluronic acid or a salt thereof. 4. Composizione secondo la rivendicazione 1, in cui gli amminoacidi sono nella forma L. 4. Composition according to claim 1, wherein the amino acids are in the L form. 5. Composizione secondo la rivendicazione 1 e 2, in cui i vari componenti sono presenti nei seguenti intervalli di composizione in peso: a) da 0,5 a 20% di glicina, b) da 0,2 a 15% di prolina, ed eventualmente c) da 0,5 a 5% di acido ialuronico o un suo sale, e/o d) da 0,05 a 10% di lisina, e/o e) da 0,05% a 3% di leucina. 5. Composition according to claim 1 and 2, wherein the various components are present in the following composition ranges by weight: a) 0.5 to 20% glycine, b) 0.2 to 15% proline, and eventually c) from 0.5 to 5% of hyaluronic acid or a salt thereof, and / or d) 0.05 to 10% lysine, and / or e) from 0.05% to 3% of leucine. 6. Composizione secondo la rivendicazione 1 e 2, in cui sotto forma di spray, crema, unguento o gel.6. Composition according to claims 1 and 2, wherein in the form of a spray, cream, ointment or gel.
IT000954A 2011-05-26 2011-05-26 COMBINATIONS FOR THE TREATMENT OF VAGINAL OR RECTAL MUCOSITES ITMI20110954A1 (en)

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