WO2014012156A1

WO2014012156A1 - Prolonged-action intimate hygiene composition, method for producing same and use thereof

Info

Publication number: WO2014012156A1
Application number: PCT/BR2013/000088
Authority: WO
Inventors: Priscila RAMOS RODRIGUES GUIMARÃES
Original assignee: Sanofi Aventis Farmacêutica Ltda.
Priority date: 2012-07-16
Filing date: 2013-03-22
Publication date: 2014-01-23
Also published as: AR091330A1; PE20150768A1; CR20140570A; MX2014014896A; ECSP15001584A; DOP2014000276A; UY34910A; CL2015000101A1; CO7160048A2; GT201500008A; BR102012017571A2

Abstract

The present invention provides a liquid, prolonged-action intimate hygiene composition comprising: a pH regulator for the mucous membranes; a moisturiser; and a component that stimulates the grow of (resident and beneficial) saprophyte flora. This prolonged-action combination maintains a balanced pH in the mucous membrane to which it is applied, regulating skin acidity, preventing or minimising the proliferation of undesirable microbial or bacterial flora; and is tissue-moisturising and regenerating. Also disclosed are methods for producing this composition.

Description

Patent Invention Descriptive Report

COMPOSITION FOR EXTENDED INTIMATE HYGIENE PROCESS

PRODUCTION AND USE

Field of the Invention

The present invention relates to the field of personal care compositions. More particularly, the invention discloses a composition for promoting an individual's prolonged intimate personal hygiene, as well as its process of obtaining and use.

Background of the Invention

Today, people are subject to many social and professional commitments throughout the day that are usually long and do not offer adequate conditions for performing intimate hygiene. This fact creates insecurity in the face of the concrete possibility of the release of odors and the production of secretions that may stain your clothes.

Genital hygiene, especially for women, is of particular importance, either because it is an anatomical region that is difficult to access, lack of knowledge about it, or even because it accumulates different secretions and substances.

Studies on the behavior of the vaginal ecosystem have brought new insights into the magnificent and perfect interplay between the millions of bacteria that colonize the light of this cavity. The vaginal ecosystem is known to be unstable and subject to many variations that depend on diet, sexual activity, hormone production, medication use and also on genital hygiene. Despite this, unfortunately the knowledge is not the same for the vulvar region. It is reasonable to suppose, however, that hygiene probably plays a much stronger role.

According to the FEBRASGO intimate hygiene guide, proper (vulvar) intimate hygiene is essential to help maintain cleanliness and acid pH balance of the region, greatly affected by the daily life of the modern woman who spends a lot of time outside the home and wears clothes that promote lack of aeration and exaggerated compression. Thus, proper hygiene of the female intimate region is a great ally in helping to protect women. The cleaning of the female intimate region is best done with liquid soap, as most bar soaps have neutral or alkaline pH, and can be shared by others in the same house. Preferably the products should have mild detergency (high detergency rate may dry out vulvar skin), be hypoallergenic and with physiological pH (slightly acidic and not neutral or alkaline).

Body hygiene is undoubtedly a necessity for all, and especially women, for their genital area. Although this practice is usual and daily, many women still have doubts about the form, frequency and the correct occasion to perform it.

Under normal conditions, there is a constant and significant scaling of skin cells and semimucosa of the vulvar region, as well as perspiration and natural physiological vaginal discharge. For the skin cells to function perfectly it is necessary to keep the pH between 4.6 and 5.9 (acid). The vulva's skin behaves the same way and works more properly when its pH is acidic. Therefore, all physicochemical substances and conditions that alter the pH of the vulva's skin may cause disorders to its proper functioning.

The female external genitalia is formed by numerous skin folds and is located in a region that makes aeration very difficult. Both features favor humidity, increased temperature and the difficulty of removing debris. In addition, the skin of the intimate region as well as the rest of the body due to the disposition of its cells (keratinocytes) and the production of substances (ceramides, fatty acids, triglycerides, free steroids, cholesterol, fat esters, squalene) form a "Skin barrier" that prevents the loss of water and other elements. This barrier is as much a physical barrier as it is antimicrobial with immunological function, establishes a sensory interface and promotes the maintenance of physiological pH (Cutaneous Acid Cloak).

The cutaneous acid mantle is one of the main responsible for the balance of the microbiological ecosystem and the perfect functioning of the skin cells. Like other parts of our body, maintaining pH in restricted ranges is critical for biochemical reactions to proceed smoothly. The disruption of the skin barrier and acid mantle may favor tissue damage and compromise the balance of the vulvar ecosystem triggering irritative and infectious processes. There are several factors that can compromise genital and skin homeostasis by activating the production of pro-inflammatory cytokines, cell adhesion molecules, DNA synthesis, among others. Factors such as family history of dry skin, conditions such as eczema and psoriasis, use of dry skin medications, aging, sun exposure, wind and low humidity, inadequate soap and cleanser promote skin dryness and ease skin lesions. by the formation of continuity solution between the keratinocytes. In addition, a chronic inflammatory process is established that will increase the risk of infections.

Genital hygiene is necessary to prevent accumulation of secretions, dead cells and debris. It is natural to assume that poor hygiene can cause foul smell, itching, secretion buildup, and vulvar and vaginal infection. The female genital region, besides being more sensitive, is subject to more intense bacterial colonization, occlusions and compressions due to dress habits and greater friction by the anatomical location, that is, it is more susceptible to maladjustments of its ecosystem. Prolonged use of occlusive pads and clothing that promotes lack of aeration and excessive compression should be avoided.

In the vulvar region, because of the many folds of skin, aggressions tend to be more frequent. The chronic and continued use of inappropriate soaps in the sanitation of female genitalia has the potential to promote maladjustment in the microenvironment and promote irritative and infectious processes.

Although the problems are known, few concrete initiatives have actually achieved satisfactory solutions. In the patent field, some partially relevant approaches are known in the context of the present invention and are described below.

EP 2236127 (Rottapharm S.p.A.) describes an intimate hygiene composition comprising one or more active substances in conjunction with xanthan gum, where it is an agent capable of favoring bioadhesion of the active substances to the skin and mucous membranes. Examples of such active substances include, without limitation, lactic acid, which contributes to maintaining the physiological pH of the slightly acidic vulva surface, preventing the development of pathogens, and also pasteurized and atomized whey, which together with lactic acid have buffering action and ensures continued acidity of the vulva surface. The present invention differs from said document, among other reasons in that it is directed to other problems rather than adherence of the formulation by the use of xanthan gum. Furthermore, xanthan gum is not used in the present invention, being a polysaccharide very distinct from oligosaccharides. Polysaccharides are made up of a large amount of monosaccharides, while oligosaccharides are made up of only 2 to 10 monosaccharides. In the present invention, the lasting effect for longer periods is provided by the combination of the oligosaccharide, whey and lactic acid ingredients, and adhesion of the product by the addition of a polysaccharide such as xanthan gum is not required.

US 6,706,941 discloses an absorbent article where microorganisms of a saprophytic flora of the skin or non-pathogenic microorganisms to the skin may proliferate, thereby suppressing the growth of possibly pathogenic microorganisms around the area of application of the article and reducing odor. and dermatitis. That document is, It is therefore related to the incorporation of a compound containing an alpha 1-2 skeleton, such as glycooligosaccharide which can act as a substrate for enzymes present only in certain bacteria. Said document differs from the knowledge disclosed by the present invention, among other reasons, in that it does not provide a liquid composition that prevents the proliferation of a pathogenic flora, and promotes a prolonged hydration and freshness effect in the sanitized regions.

WO 2010/004005 (Alliospharma) describes pharmaceutical and dermatological compositions comprising a probiotic chosen from oligosaccharides, such as gluco-oligosaccharides (GOS), fructooligosaccharides (FOS), galactooligosaccharides, and an extract. of plant containing isoflavones selected from soybean extracts (Glycine max) and clover extracts (Trifolium sp.), for use in the treatment of bacterial vaginosis and / or for the treatment of the vaginal mucosa. The present invention differs from said document, among other reasons, in that it presents in its composition the association of oligosaccharides not with plant extracts (which may present problems of stability and / or compositional variability due to seasonality), but with lactic acid and whey, which act as a moisturizer and tissue recovery ingredient, thus providing some of the desirable effects mentioned above. The said document neither presents or even suggests a moisturizing effect on the composition of the intimate soap, which promotes an extension of its duration, differing from the present invention.

Thus, the need persists to develop products in the form of stable liquid composition that provide, especially with prolonged action: the maintenance of a balanced pH in the mucous region where it is applied, regulating the skin acidity; prevent or minimize the proliferation of undesirable microbial / bacterial flora; and provide hydration, aiding tissue recovery.

From the research literature, no documents were found anticipating or suggesting the teachings of the present invention, so that the solution proposed here, in the eyes of the inventors, has all the patentability requirements before the state of the art.

Summary of the Invention

The present invention provides a prolonged intimate hygiene liquid composition comprising: pH regulator for the mucosal region; moisturizer; and a component that stimulates the growth of saprophytic flora (resident and beneficial). This combination provides, with prolonged action, the maintenance of a balanced pH in the mucous region where it is applied, regulating the skin acidity; prevents or minimizes proliferation of undesirable microbial / bacterial flora; and provides hydration, aiding tissue recovery. Processes for obtaining them are also disclosed.

In a preferred embodiment, the growth stimulating component of saprophytic flora is alpha-glucan oligosaccharide.

In a preferred embodiment, therefore being one of the objects of the invention, there is provided an intimate hygiene composition comprising: at least one oligosaccharide; whey; and at least one pH regulator. The composition of the invention provides effects on the intimate region over prolonged periods, with considerable reduction of the proliferation of pathogenic microorganisms in the product application region and, consequently, a healthier intimate region.

In a preferred embodiment, the composition comprises from 0.1% to 10% by weight of oligosaccharide, from 0.1% to 20%; by weight of whey and from 0.1% to 20% by weight of pH regulator.

Another object of the present invention is a process for producing an intimate hygiene composition. The process of the invention comprises the steps of mixing an oligosaccharide in whey and adding a pH regulator and one or more cosmetically acceptable carriers until the pH is in the range of 4.2 to 4.8. It is also an object of the present invention to use a combination of: oligosaccharide; whey; and a pH regulator for the preparation of an intimate hygiene composition. These and other objects of the invention will be immediately appreciated by those skilled in the art and companies having an interest in the segment, and will be described in sufficient detail for their reproduction in the following description.

Description of the figures

Figure 1 shows the growth of Micrococcus kristinae and Corynebacterium xerosis. Inoculation of 10 ⁵ cells / ml in the presence of the composition of the present invention.

Figure 2 shows the growth of Micrococcus kristinae and Corynebacterium xerosis. Inoculation of 10 ⁶ cells / ml in the presence of the composition of the present invention.

Detailed Description of the Invention

The present invention provides a prolonged intimate hygiene liquid composition comprising: pH regulator for the mucosal region; moisturizer; and a component that stimulates the growth of saprophytic flora (resident and beneficial). This combination provides, with prolonged action, the maintenance of a balanced pH in the mucous region where it is applied, regulating the skin acidity; prevents or minimizes proliferation of undesirable microbial / bacterial flora; and provides hydration, aiding tissue recovery.

The present invention provides an intimate hygiene composition comprising at least one oligosaccharide, whey and at least one pH regulator.

The following are some definitions of terms that are presented throughout the patent application.

Personal and intimate hygiene

Body cleansing habits are essential to ensure the health of the whole body against external stimuli such as the proliferation of unwanted and disease causing microorganisms. The set of body cleansing habits characterizes an individual's personal hygiene. Hygiene Personal care is critical in the face of inability to perceive the onslaught of pathogens, which gives hygiene a key role in bodily well-being. In the context of the present invention, intimate hygiene is defined as the use of products that do not harm an individual's external genital regions.

The composition of the present invention inhibits the growth of non-saprophytic flora, stimulates beneficial flora and prevents opportunistic colonization and is therefore a cosmetic and functional personal hygiene composition.

Oligosaccharide

For the purposes of the present invention, "oligosaccharide" means saccharides of up to 10 saccharide monomers, obtained from natural or synthetic sugars, such as by enzymatic synthesis involving the transferase enzyme. Can be used as sugars originating sucrose and maltose.

Alpha-glucan is a preferred oligosaccharide of the present invention having the following formula: 1-6)

Said oligosaccharide is a powder with a white appearance and a slight and characteristic odor. It is soluble in water, polyethylene glycol and glycerol, insoluble in ethanol 50 ° GL and not miscible with vegetable and / or mineral oils. Your CAS number is 27707-45-5.

The preferred oligosaccharide of the present invention is a component that selectively stimulates the growth of an individual's (resident and beneficial) saprophyte flora over a pathogenic flora. The alpha1-6 and alpha1-2 bonds of their polymeric structure provide a better hydrolysis. difficult to cause bioselectivity since this substrate restricts the growth of a pathogenic flora. Thus, in a competitive environment, saprophytic flora will prevail. Alpha-glucan is an oligosaccharide that protects the skin's ecosystem by keeping the ecosystem constant or balancing it in such a way as to revert it to its previous or natural state. It acts selectively, eliminating the use of antibiotics to prevent the emergence of unwanted flora. Whey

Whey (whey or lactose) is the product derived from the hydromineral fraction of milk. Its main function in composition is to maintain the effect of lactic acid for a longer time as well as moisturize and maintain the hydroelectric balance of the skin, acting as a moisturizing and tissue recovery factor. In a preferred embodiment, the whey used in the present invention is atomized (whey) whey.

PH regulator

PH regulator is a component that ensures skin acidity, hindering microbial proliferation, as well as maintaining the pH of the skin surface on which the intimate hygiene product will be applied. In a preferred embodiment, the pH regulator used in the present invention is lactic acid (or 2-hydroxypropanoic acid).

Preferred Embodiments

The examples shown herein are intended solely to exemplify some of the numerous ways of carrying out the invention, but should not limit the scope thereof.

In a preferred embodiment of the invention, an intimate hygiene composition has been prepared and its beneficial effects tested.

Example 1

Table 1 - Qualitative and quantitative formula

Components Composition Composition (INCI nomenclature) ³ percent unit (mg / mL)

Lactosoro (powder) 1.050% 10.500 mg

Lactic acid 1,020% 10,200 mg

Alpha glucan 0.500% 5,000 mg oligosaccharide

Acrylate Copolymers 2,000% 20,000 mg

Sodium Lauryl Sulphate 18.360% 183.600 mg

Sodium lauryl sulfate

Glycol distearate

5,100% 51,000 mg

Cocamide MEA

Lauril 10

Hydroxyethylcellulose 0.714% 7, 140 mg

Methylparaben 0.153% 1,530 mg

Perfume ¹³ 0.4% 4.000 mg

q.s.p. pH

Sodium hydroxide ⁰ -

4.2 - 4.8

q.s.p. pH

Phosphoric acid -

4.2 - 4.8

Water q.s.p. 100,000% qsp 1,000 mL

Example 2

Physicochemical tests

The above composition was analyzed for their physicochemical characteristics. The results can be seen in table 2:

- Aerobic Bacteria

<5 X 10 ² CFU / g

totals + fungi

Pathogens ^(t1) T-MB-0009

Staphylococcus aureus Absent / g

Pseudomonas aeruginosa Absent / g

Total coliforms and

Missing / g faecal T-MB-0009 ^(E1)

Subtitle:

^L = Tests performed for batch release to market

^E = Tests performed on stability studies

^E1 = Tests performed at the beginning and end of stability studies

^M = Non-routine tests (POP P0368)

^F = Test performed by manufacturer only

The physicochemical test proves the maintenance of a stable acidic pH (4.2 to 4.8) at room temperature, which is an essential feature in a composition that can be used in the female external genital region. Another important data about the physicochemical test is the amount of total aerobic bacteria and fungi, which remain within acceptable limits, as well as the absence of pathogenic microorganisms and fecal and total coliforms.

Characteristics such as density, foam, fill volume and viscosity were also qualitatively analyzed, remaining at desired values for a liquid composition intended for intimate cleaning.

Example 3

Stability test

The stability study was carried out with the product in its commercial packaging, stored in an oven at 40 ± 2 ° C / 75% ± 5% RH, and at 30 ± 2 ° C / 75% ± 5% RH for 3 months.

The results can be seen in the following tables: Table 3 - Stability Study

Table 4 - Stability Study

24 months 30 ° C 75% RH

01 month 40 ° C 75% RH - - - -

02 months 40 ° C 75% RH - - - -

03 months 40 ° C 75% RH <10 CFU / g Away Away Away

06 months 40 ° C 75% RH

The stability test aims to verify, within 24 months, the maintenance of the desirable characteristics of the composition of said composition. The composition maintained its characteristics and microbiological contamination remained below 10 CFU (Colony Forming Units) / g, with no growth of pathogenic bacteria detected. The pH remained acidic (between 4.2 and 4.8), an essential characteristic in a composition for use in the female external genital region.

The results of the tests allow us to conclude that the product is stable under the conditions under which it was submitted, maintains its physical and chemical characteristics according to predetermined specifications and quality attributes and has a proposed shelf life of 24 months.

Example 4

Efficacy of Alpha-Qlucan Oligosaccharide

Alpha glucan oligosaccharide favors the growth of saprophytic flora over pathogenic because it has bonds (a1-6) and (a1-2) which are more difficult to hydrolyze, restricting their growth by bioselectivity. In a study to investigate the metabolism of alpha glucan oligosaccharide by microbial strains of the skin and vaginal mucosa, a comparison was made of the use of alpha glucan oligosaccharide and glucose as a carbon source. The results are in the tables below.

Table 5: Classification used for the scores.

Sugar level consumed Reference signal

0 to 20% -

20 to 40% +

40 to 60% ++

60 to 100% +++ Table 6: Results of the use of alpha glucan oligosaccharide and glucose by saprophyte flora as carbon source.

Table 7: Results of the use of alpha glucan oligosaccharide and glucose by pathogenic flora as carbon source.

Table 8: Results of alpha glucan oligosaccharide and glucose utilization by saprophytic flora not established as carbon source.

Therefore, it was found that alpha glucan oligosaccharide is a carbon source for most saprophytic microorganisms tested, and not for the pathogenic microorganisms tested. Thus, alpha glucan oligosaccharide provides a selective carbon source for desirable plant growth, indirectly acting as a growth inhibitor of these undesirable bacteria. Additionally, a test was conducted to investigate the inhibitory potential of alpha glucan oligosaccharide by competition by analyzing the growth of a combination of pathogenic or undesirable saprophytic bacteria. Bacteria were inoculated into culture medium (USP tryptone) containing 0.5% alpha glucan oligosaccharide. After 24h of growth, the bacteria was counted. The PCA, Chapman and BHI methods were used for total flora, Staphylococcus aureus and Corynebacterium xerosis, respectively. In a first culture combination, Staphylococcus aureus and Micrococcus kristinae were inoculated at a concentration of 10 ⁶ cells / ml. Bioselective development of Micrococcus kristinae was observed to the detriment of Staphylococcus aureus. The results are in the table below.

Table 9: Growth of Staphylococcus aureus and Micrococcus kristinae.

In a second co-culture was inoculated Micrococcus kristinae and Corynebacterium xerosis 0 at a concentration of ⁵ cells / ml.

Table 10: Bacterial inoculation time related development. Inoculation of 10 ⁵ cells / ml.

Figure 1 shows growth data for Micrococcus kristinae and Corynebacterium xerosis. Inoculation of 10 ⁵ cells / ml. A culture combination was performed by inoculating Micrococcus kristinae and Corynebacterium xerosis at a concentration of 10 ⁶ cells / ml. Table 1 1: Time of inoculation of bacteria related development. Inoculation of 10 ⁶ cells / ml.

Figure 2 shows the growth of Micrococcus kristinae and Corynebacterium xerosis. Inoculation of 10 ⁶ cells / ml.

The graphs indicate that alpha glucan oligosaccharide preferentially promotes Micrococcus kristinae growth over Corynebacterium xerosis. This competitive inhibition occurs due to a bioselective assimilation of alpha glucan oligosaccharide by Micrococcus kristinae. Therefore, there is a faster and more beneficial metabolism of alpha glucan oligosaccharide by saprophytic flora, favoring its growth over pathogens, inhibiting opportunistic colonization.

Those skilled in the art will appreciate the knowledge presented herein and may reproduce the invention in the embodiments presented and in other embodiments within the scope of the appended claims.

Claims

COMPOSITION FOR EXTENDED INTIMATE HYGIENE, PRODUCTION AND USE PROCESS

1. Composition for intimate hygiene characterized by:

- pH regulator for the mucous region;

- moisturizing component; and

- a selective component for growth of saprophytic flora.

Composition according to Claim 1, characterized in that said selective component is alpha-glucan oligosaccharide.

Composition according to Claim 1 or 2, characterized in that it comprises oligosaccharide, whey and a pH regulator.

Composition according to Claim 1, 2 or 3, characterized in that it comprises atomized whey.

Composition according to any one of claims 1-4, characterized in that it comprises from 0.1% to 10% by weight of oligosaccharide, from 0.1% to 20%; by weight of whey and from 0.1% to 20% by weight of pH regulator.

Composition according to Claim 5, characterized in that the percentage of oligosaccharide is from 0.1% to 1%.

Composition according to Claim 5, characterized in that the whey content is from 0.5% to 1.5%.

Composition according to Claim 5, characterized in that the percentage of pH regulator is from 0.5% to 1.5%.

9. Use of a combination of: pH regulator for mucous region; moisturizing component; and a selective component for the growth of saprophytic flora characterized in that it is for the preparation of an intimate hygiene composition.

Use according to claim 9, characterized in that it is for the preparation of a composition which promotes the growth of Micrococcus kristinae over Corynebacterium xerosis.

Process for producing an intimate hygiene composition comprising the steps of mixing a moisturizing component with a selective component for saprophytic flora growth and adding a pH regulator to the mucosal region and / or one or more cosmetically acceptable carriers up to pH is in the range of 4.2 to 4.8.