WO2004009105A1 - Phytotherapic composition based on vegetable extracts, process for obtainment of said composition and use of vegetable extracts for preparation of a phytotherapic composition - Google Patents

Abstract

The present invention refers to a phytotherapic composition containing extracts of selected medical plants useful for the neutralization/minimization of the harm effects caused by the mad habits of oral hygiene. The composition for oral hygiene may be in liquid, gel or solid form, such as a cream or a paste.

Description

"PHYTOTHERAPIC COMPOSITION BASED ON VEGETABLE EXTRACTS, PROCESS FOR OBTAINMENT OF SAID COMPOSITION AND USE OF VEGETABLE EXTRACTS FOR PREPARATION OF A PHYTOTHERAPIC COMPOSITION".

The present invention refers to a phytotherapic composition containing extracts based on certain vegetables that, in the aggregate form, grants a conjugated effect to the composition, providing it with a specific function in relation to the neutralization/minimization of the harm effects caused by the mad habits of oral hygiene. The composition for oral hygiene of this invention may be presented in gel, liquid, solid or chewing gum form.

On a second aspect, the invention comprises the process for obtainment of such composition, which technical parameters, selection of the compounds involved and the presentation of the conjugated effect between each other, grants to the said composition, the innovative and unexpected character in relation to that known in the art, referring to this matter. In a particular character, it deals with a composition for night use, immersion bath.

A third aspect of the invention refers to a dentifrice composition based on the referred composition made in cream or gel, or liquid or paste form, which allows the easy application in the oral cavity, preferably for night use only.

The fourth aspect is related to the use of vegetable extracts selected for preparing the referred composition.

Several preparations for the hygiene and prophylaxis of the oral cavity are known. The active ingredients thereof maintain the effective control of the etiologic factors that cause the diseases in the oral cavity. It also controls the micro-flora of the oral cavity, inflammations, and other oral factors that help the person to improve its conditions when they are suffering of dental and oral diseases.

The solutions of dentifrice compositions and/or medical, or that contain vegetable extracts are also known by the art, such as: Patent US 5,376,374, which describes an oral composition with good taste, which contains, among other elements, bee glue (propolis) , Cayenne pepper, calendula and vinegar. The PI 9605706-8, the document JP 58,121,218 and the article KOHDA, Et al, Med. Plant Apr. (2) : 119-20, are incorporated herein as reference. For example, PI 9605706-8 describes a dentifrice composition where a synergic effect between Jujube and specific emulsifying agents is alleged, specially the sodium lauryl sulfate. Although it is not mentioned by the art, the dentifrice containing Jujube and Propolis, launched in the market by beginning-2002, is known.

However, none of these references mentioned the use of the set of components, originating from vegetable extracts, as preparations for the hygiene and prophylaxis of the oral cavity, controlling/removing the offensive breath, according to the present invention.

The human body is constituted of a perfect balance ecosystem, where several types of lives harmoniously coexists among each other, through a consortium of mutual functions, existing therein, all possible and conceivable ecologic models, such as commensalisms, symbiosis, parasitism, etc. Two important communities, biologically active representatives of this process are found in the mouth and intestines. In addition to the mutual and reciprocal cooperation existing between the species of such communities, there is a complete relation of integration with the host organism. Those integrating such communities are considered as natives, with important functions for the maintenance of their health, that its functions deals with material related to the immune-stimulation, balance and maintenance of the physiologic pH, antagonism to the pathogenic alien bacteria, transformation of the food bolus into fecal, enabling, among others, a digestive transit proper to the perfect absorption of nutrients.

The harmonious and passive coexistence exercised by such communities, are many times interrupted by factors such as the improper hygiene from the part of the hosts, thus, causing an over-population in the medium, with several consequences, among which, the odor.

In the cranium-caudal sense, from the mouth to the intestines, this unbalance, if any, may bring the offensive breath as a consequence thereof. In this context, this process should be understood and interpreted as a congenital incapacity of the individual to neutralize these odors that originate from the anaerobic metabolism - fermentation. The mouth, with its oral basic functions and of food grinding organ, constitutes in the most significant and important organ in relation to the offensive breath, either due to local factors, which are considered as critical, or also on account of being bonded to other organs directly involved with the offensive breath. Among the most important factors, we may specify the presence of focus such as dental, tonsillitis, as many others, all of them constituting in a concentration of pain generator organisms.

The tongue, with its anatomy in the form of "carpet", the tonsil scarves and crypts, favor the retention of food substrates in the odor bacteria in this process.

With regard to "satellite" factors, i.e., those that are discharged in the mouth through its direct communication, we may mention the pharyngitis and sinusitis carriers.

Continuing downwards, we have the esophagus with its pathologies such as hernias, diverticulitis, and reflux exophagitis, all of them favoring the permanence of food substrates for the fermentative bacteria, achieving the mouth either by exhalation or the return of fermented food material, by eructation/regurgitation.

The stomach that has the basic digestive/liquefying function of the food bolus, recently ground in the mouth, should be efficient to the point of preventing the long permanence of the same in its interior, otherwise it would cause its fermentation, generation of odors, by eructation/regurgitation. There is a consensus in the scientific class regarding the theory, which considers the digestion as an auto-stimulating process, where its initiation occurs under the visual contact with food, giving rise to a series of organic events that the objective is to transform the complex chemical structures present in food, in simply structures, by hydrolysis means. Several factors may hamper, or even hinder this transformation, as the pathologies that may endanger or not the stomach performance, causing dyspepsia, translated by the proper indigestion. This picture may be caused by emotional gastritis, improper food habits, and some intestinal parasitosis among others.

The food bolus now ground and duly liquefied, continues the course to the intestines, so that the digestive process is concluded with the absorption of nutrients and water and the transformation of the food bolus into fecal. The fermentative bacteria that digest and metabolize the food residues, which escaped from the digestive process, develop such process. Particular parasitosis such as amebas may cause a picture of dyspepsia, therefore, favoring the bacterial fermentation by the stagnation of the food bolus in the stomach.

Returning to the oral cavity as the main repercussion place of all this picture in the generation of odors, factors as the tissue sensibility should always be taken into account; bonding with noble organs as lung and stomach; the possibility of systemic sublingual absorption and, the presence of a microbial community ecologically balanced, which constitutes principles that should be respected and exhaustively analyzed in order to serve as guidelines for taking the decision on which therapeutic modality for controlling the halitosis should be adopted.

The extreme complexity of the microbial physic- pathogenesis in the generation of odors is recognized, where practically nothing can be done without taking into account the consequences before a disastrous therapeutic.

The bacteria present therein are organized in several communities, all of them compatible with the requirements of its constituents as luminosity, presence or absence of oxygen, among others. This event is carried out by an efficient enzymatic system (protein) , which basic objectives are the acquisition and feasibility of food substrates, and the physical structuring of the plaque skeleton, its "home".

In order to understand this process, we may separate these bacteria into two large groups: those that are fed by carbohydrates producing corrosive acids, mainly attacking the hard tissues of the teeth, promoting the decalcification, cavity and another group which uses proteins (amino acids) as food substrates, producing destructive soluble enzymes, swelling/destructing mainly the soft tissues of tooth upholding, periodontal. Both groups act in the generation of odor, the latter being the most critical one.

The ecologically correct solution would be the use of a product would contemplate, preserve and respect all factors previously mentioned in relation to the oral ecosystem. The astringency, the quality of a substance of conjugating with structures of protean nature, by partial molecular hydrolysis, forming new compounds would be opportune, added together with some other therapeutic properties to counterbalance the possible undesirable effects of such quality. Particularly, the astringency, duly dosed and balanced, with the use thereof indicated and controlled by a professional, through a simple chemical conjugation, would "neutralize" the harmful, stench and electrically instable (free radicals) bacterial protean catabolytes, in this way, preserving the flora so necessary for the oral health. This product would have the properties of neutralization/minimization of offensive odors, tissue cicatrisation, the reduction of plaques/cavities and the integration, from the viewpoint of lack of undesired side effects.

The preparation of the phytotherapic compound in fixing gel form, constitutes an innovative inventive concept, either by its use during sleep, with slow, continuous and prolonged effect, either by the set of phytotherapic properties, which attend all requirements of the oral medium, constituting of an "ecologically correct" therapeutic method.

There is a consensus in the scientific class about the necessity of the host strengthen, detrimental to the elimination of the invading microorganism.

It is in the maintenance and strict control of the oral native flora, with its interactive functions so necessary for the health and also with the minimization of its undesired side effects such as odor, which rests the concept of complete oral health.

The tonic of this patent claim is the neutralization/minimization of offensive odors, with preservation of the ecosystem and maintenance of the health of the oral structures, through a consortium of functions present in the referred to phytotherapic compound, interacting in a joint form, with the maximum efficiency and minimum side effects to the hosts, when properly used.

The statistical data proves that from 20% to 30% of the persons suffering from chronic halitosis. The causes are related with lack of oral activity, caused by long fasting periods that is typical of those under inordinate diet, may increase the number of bacteria in the mouth. The emotional stress may generate the disturb, negligence in relation to the correct hygiene originating from infectious sinusitis, nasal secretion at the base of the tongue, poor oral hygiene, gingival diseases, incorrect cleaning of the denture and removable apparatus, and respiratory problems with the accumulation of secretions.

The oral cavity of each individual has particular characteristics. Certain areas in the oral cavity are more susceptible to the accumulation of material and food residues. These places are favorable for the development of the bacterial plaque, and the same is the main responsible for the disease called cavity and other periodontal diseases. The correct brushing is the most efficient manner for the prevention of the cavity disease and other periodontal diseases.

The maintenance of the oral health and, consequently, the prevention of cavity and diseases of systemic risks, derive from the absolute control of the bacterial plaque (biofilm) . Habits of hygiene and systematic brushing should be created and adopted by all.

There is the necessity of establishing habits that may favor a better oral health. However, it is difficult to make the persons aware of the importance of the brushing, and of the proper "presence" of bacterial plaque, since it is not visible without the use of particular dies. The systematic application of fluorine and the maintenance thereof, at proper levels on teeth surface and in the underlying regions, results in a more intense control of the microbial populations that inhabit the oral cavity.

Many attempts were made for the control and prevention of the formation of the dental plaque. Such treatments are typically made in a dentist's office, at periodic intervals, however, not frequently. However, such treatments do not result in the control of the plaque during a prolonged period.

With such problems being possible from the plaque/gingivitis, it is not surprising that the external efforts have been made trying to find efficient compositions that may equate the existing problems, either in the sphere of prevention, prophylaxis and treatment, either in the sphere of the discovery and control of the presence of dental plaque.

Despite the several descriptions in the area of anti-plaque, anti-gingivitis, etc., did not yet reveal an anti-bacterial oral composition that, at the same time, reveals the presence of dental plaque in the oral cavity, and is of free application, with total access, including the domestic sphere.

Although the compositions of topic oral hygiene already existing in the market, present in the composition thereof, compounds with anti-bacterial action associated with wetting agents, surfactants, abrasives, etc, did not reveal, up to the present moment, compositions typically based on vegetable extracts, that associated would present the surprising effects found by the present invention, which proposal deals with the control of halitosis by an unique form.

With the aim and purpose to fight all these inconvenient, is the reason for developing the composition of the present invention that contains the desired active principles. The correct use of this compound, which may be available in the form of gel, liquid, solid and chewing gum, or any other form, and should always be taken into consideration the medium where it will be applied, which medium should be considered as extremely delicate.

The plaque existing in the medium, may in no way be completely eliminated, in a continuous form and without the agreement of a professional of the area, since its necessity and functional importance, should indeed, and this is the main function of the composition object of the patent application in question, neutralize/minimize the effects thereof, i.e., give a solution to the gingival inflammation of the tissues and prevent the generation of odors.

The composition object of the patent application in question, presents the following ingredients listed hereunder, which functions in the isolated form, do not solve the aforementioned problems. Such problems may only be solved in the form herein proposed.

The composition of the present invention is composed of the following ingredients: a) Brazil peppertree (Schinnus Terebinthi Folius) leaf. b) Calendula (Calendula Officinalis) leaf and flower . c) Chamomile (Matricaria Chamomile) flowers. d) Common Witch Hazel (Hamamelis Virgiana) leaves. e) Jujube (Zizupphus Joazeiro) peels. f) Bee Glue (Propolis) resin. g) Garden Sage (Ξalvia Officinalis) leaves, h) Carbomer. i) Deionized water. j) Triethanolamine. k) Aromatizing and/or Flavoring.

The composition of the present invention, if compared with that already existing in the state of the art, presents the advantages to: reduce or eliminate the offensive breath, fight the inflammation and infections, promote the cicatrisation, the hygiene of the oral cavity, reduce the plaque action, and consequently, the incidence of cavities, and eliminate the bleeding, however, without killing the bacteria that compose the oral ecosystem.

The present invention also refers to gel, cream or paste dentifrices, containing the composition of this invention associated with other substances such as abrasives, deodorants and others.

Now, it was surprisingly verified that the extracts used, in proportions established to develop this composition, present particular characteristics, that in association represent the new technical, unexpected and desired effect of the invention. a) Brazil peppertree acts as an astringent in the compound. b) Calendula presents the antiallergenic, anti- inflammatory, antiseptic, cicatrizing and soothing functions to the gingival, and the necessary objective functions required from it, are to reduce inflammation, promote the cicatrisation and act as soother. c) Chamomile presents in its leaves, the chemical composition that contain organic acids, salicylic acid, apigenin, borneol, camphor, choline, coumarine, flavonoid, burstwort, saponin, mucilage, pro-camazulene, azulene terpene and umbelifer. Chamomile is used on account of its astringent, analgesic, antiallergenic, anti- inflammatory, cicatrizing and refreshing properties . d) Common Witch Hazel is rich in gallic-tannin and also contains phenol acids. Such different constituents are equally important to the gingival since it presents astringent, antioxidant and vasoconstrictor. e) Jujube is rich in saponin, the substances that produce soap, promoting the dilution of the components. In this case, it will react against the plaque, solving it in a small proportion, and will also act as moderator, carrier of another important substance, which is Brazil peppertree. Jujube has the basic function of being the mediator, abbreviator of Brazil peppertree actions, which in this case has an equally important function in the compound, acting as antioxidant - eliminator of free radicals. Although its characteristics are natural Jujube saponifies, makes the substances remain not too long in contact with the medium. It is an astringency dosimeter, accelerating the action and permanence of the other substances in the medium, by the reduction of the superficial stress of the compound providing interaction, functional binding and action in the medium. f) Propolis, in the concentration proposed, acts as a cicatrizing factor, in addition to a buffering function, due to the presence of mineral elements and proteins that will conjoin with the end products of the bacteria final products, with the catabolytes, forming new products, therefor, neutralizing its odor. It has the anti- inflammatory character, g) Garden sage contains essential oils, such as thujones, cineol and borneol, saponin, tannin, among others, and has anti-inflammatory, antioxidants and astringent properties, h) Carbomer is an C10-30 acrylate copolymer, which purpose is to give thickness to the compound that hydrates, forming a transparent gel, when in contact with water, i) The Deionized Water will be the carrier used in the compound, it is ion free in order to prevent incompatibilities with the other components of the compound. j) Triethanolamine is a weak alkali used as pH adjusting agent, k) Aromatizing and/or flavoring will have the function to give odor and/or a more pleasant taste to the compound. It should be emphasized that in the state of the art, specifically in PI 9605706-8 the use of Brazil peppertree as a saponifying element in synergic effect with sodium lauryl sulfate in known dentifrices and, as already mention, by beginning-2002, was launched a dentifrice containing propolis and Brazil peppertree, in addition to the usual ingredients. However, these references do not mention the possibility of joint use of the other phytotherapic components present in the invention and the other benefits originating therefrom.

Moreover, the state of the art was far from describing or forecasting the composition of the present invention, since it would not care to achieve the desired effects of the invention. The composition of the present invention does not have the purpose of blotting out the bacteria that are found in the oral cavity, but indeed promote the balance of the oral ecosystem. The composition of the invention, although not being used as usual dentifrice, has the purpose of promoting an environment in which the bacteria do not proliferate in a disorderly form and harmful to the organism. The effects achieved by the combination of the elements differ from what would be expected for the individual effects of its components, however, without eliminating or restricting it.

Therefore, it is completely unexpected that the joint action of the active elements of the composition would neutralize/minimize the effects of the offensive breath. Moreover, it was easily found that the composition of the invention also provides the relief of aphthae, among other oral affections.

In this respect, the developments of the researches showed that, with the exception of the use in the oral cavity, the composition might also have topic use on other parts of the human body. For example: helps in promoting the cicatrisation of cold spell and neutralizing/minimizing its offensive odor, and also helps in the cicatrisation of ordinary wounds.

As carrier and/or coadjuvant agents, it is understood that the compounds common of the state of the art for compositions of hygiene and oral cleaning, including those that are used as dentifrices (paste, cream or gel), hygiene liquids, chewing gum and others. Or even in a more comprehensive aspect, with carrier common of the state of the art for skin topic use ointments .

With no restricting intention, in relation to the carriers, is common the use of anionic surfactants, flavorings, preserves, wetting and thickening agents, and others .

The inventors have associated the aforementioned elements with the referred to vegetable extracts, obtaining a phytotherapic composition for oral application through the joint effect obtained therefrom.

In the invention practice, the composition presents from 0.2% to 4.0% of Brazil peppertree extract, preferably, 0.5% to 2.5%; from 0.2% to 4.0% of Calendula extract, preferably 0.5% to 2.5%; from 0.2% to 4.0% of Chamomile extract, preferably 0.5% to 2.5%; from 0.2% to 4.0% of Common Witch Hazel extract, preferably 0.5% to 2.5%; from 0.2% to 4.0% of Jujube extract, preferably 0.5% to 2.5%; from 0.2% to 4.0% of Propolis extract, preferably 0.5% to 2.5%; from 0.2% to 4.0% of Garden Sage extract, preferably 0.5% to 2.5%; from 0.1% to 2.0% of Carbomer extract, preferably 0.5% to 1.5%; from 98.39% to 68.8% of deionized water, preferably 95.78% to 80.05%; from 0.1% to 1.0% of Triethanolamine, preferably 0.2% to 0.8% and from 0.01% to 0.2% of Aromatizing and Flavoring, preferably 0.02% to 0.15%.

The compositions of the invention should contain at least four out of seven vegetable extracts presented and may be used separately, or jointly, i.e., making part of the composition of dentifrices, chewing gums, sweets and spray, usual of the technique. The percentage may range out of a long rate. The selection of the percentages should be made case by case, since it will be natural not to substantially alter the characteristics of the products already existing.

Another modality of the invention relates with the process of preparation of the phythoterapic composition for oral use. With no intention to restrict the description of the processes for obtainment of the composition of the invention, describes hereunder, a preferred preparation method.

In a stainless steel mixer, duly sterilized, from 98.39% to 68.8% of deionized water is poured, and then, from 0.1% to 2.0% of carbomer is slowly and gradually added, maintaining a slow and constant stirring until complete hydration of the carbomer, forming the 1^st preparation. To the preparation, is added from 0.2% to 4.0% of each extract of Brazil peppertree, calendula, chamomile, common witch hazel, jujube, propolis and garden sage, under permanent stirring until the complete homogenization of the medium, forming the 2^nd preparation. To the 2^nd preparation, add from 0.01% to 0.2% of aromatizing and/or flavoring, also stirring until the complete homogenization, thus, forming the 3^rd preparation. To the 3^rd preparation and continuing in the same mixer, the medium pH adjustment is made, to a range of 6.5 to 7.5, by adding from 0.1% to 1.0% of triethanolamine, with permanent stirring until homogenization and achieving the pH desired, thus forming the phytotherapic gel compound, object of the invention in question.

We consider some of the examples hereunder as proper for use, maintaining the process for preparation of the phytotherapic composition, following the same steps described above, and the quantity of vegetable extracts may be altered to at least four, maintaining its percentage participation, within the rate proposed, therefore, altering the quantity of deionized water in the medium, also maintaining the participation rate of the other ingredients, as follows:

Example 1 - The composition as originally described, with seven vegetables extracts.

Example 2 - The composition as originally described, with at least four extracts, ranging between the seven existing extracts, altering the percentage variation of deionized water, to the rate of 98.99% to 84.8%, preferably 97.28% to 87.55%.

Example 3 - The composition as originally described, with five extracts, ranging between the seven existing extracts, altering the percentage variation of deionized water to the rate of 98.79% to 80.8%, preferably 96.78% to 85.05%.

Example 4 - The composition as originally described, with six extracts, ranging between the seven existing extracts, altering the percentage variation of deionized water to the rate of 98.59% to 76.8%, preferably from 96.28% to 82.55%.

The composition of the invention was tested in a substantial number of chronic halitosis carriers. In all cases treated, complete elimination and/or minimization of the offensive breath was obtained. The prolonged use of the composition of the invention, with a professional follow-up and supervision, did not cause any disturbance or unpleasant secondary effect. It was inclusive observed that, even the non-carriers of chronic halitosis could benefit of the effects of the composition of the invention; are, for example, the cases of the individuals that used food with strong condiments or have ingested alcoholic beverages.

In these cases, the use of the composition of the invention reduces efficiently the odor caused by the ingestion of food with strong condiments and alcohol.

Although not being the main objective of the researches, the topic use of the composition has also proved to be quite efficient, as mentioned above.

During the tests, there was no case in which the compositions presented and tested herein, would present any side effect in the persons; however, it is advisable to immediately suspend the use, consult a physician and inform a dentist, in case of occurring any dysfunction upon the use thereof.

The proposal of the present invention starts from a simple, opportune and wise measure. Upon applying the composition object of the letter patent, during a few seconds in the mouth, of night use preferably, and without washing, it will form an immersion bath and, no doubt, through its components, will promote the ideal conditions for the oral environment to be ecologically

Claims

correct, making the mouth healthy and with pleasant odor.

1 - Phytotherapic composition based on vegetable extracts for topic or oral use to fight halitosis and other affections, characterized by constituting the elements: Brazil peppertree, Calendula, Chamomile, Common Witch Hazel, Jujube, Propolis and Garden Sage, and excipients, preserves, flavorings and/or coadjuvant carriers of therapeutic and/or oral hygiene formulations.

2 - Phytotherapic composition based on vegetable extracts, in accordance with Claim 1, characterized by containing from 0.2% to 4.0% of Brazil peppertree extract; from 0.2% to 4.0% of Calendula extract; from 0.2% to 4.0% of Chamomile extract; from 0.2% to 4.0% of Common Witch Hazel extract; from 0.2% to 4.0% of Jujube extract; from 0.2% to 4.0% of Propolis extract, and from 0.2% to 4.0% of Garden Sage extract.

3 - Phytotherapic composition based on vegetable extracts, in accordance with Claim 2, characterized by each extract containing preferably from 0.5% to 2.5% in volume .

4 - Phytotherapic composition based on vegetable extracts, in accordance with one of the Claims 1, 2 or 3, characterized by containing at least four types of the seven vegetable extracts that compose the compound.

5 - Phytotherapic composition based on vegetable extracts, in accordance with one of the Claims 1, 2 or 3, characterized by being in the form of dentifrice gels, chewing gum, sweet or confetti, liquid or spray.

6 - Phytotherapic composition based on vegetable extracts, in accordance with one of the Claims 1, 2 or 3, characterized by being in the form of topic use formulations .

7 - Process for preparation of a phytotherapic composition based on vegetable extracts, as described in one of the Claims 1, 2 or 3, characterized for containing the phases of: a) In a stainless steel mixer, duly sterilized, deionized water is poured, and then, slowly and gradually, add carbomer maintaining a slow and constant stirring, until the complete hydration of the same, forming preparation 1; b) Add to the preparation, one of the vegetable extracts, as described in Claims 1, 2 and 3, and stir until total homogenization, forming preparation 2; c) Add the aromatizing and/or flavoring to preparation 2, and stir until total homogenization of the medium, forming preparation 3; d) Adjust the pH in preparation 3, to a range of 6,5 and 7,5 with the addition and homogenization of triethalonamine, forming the end-compound.

8 - Use of a phytotherapic composition based on vegetable extracts, as described in one of the Claims 1, 2 and 3, characterized for being used to prepare a gel, cream, paste, chewing gum, sweet or confetti, liquid or spray for oral use.

9 - Use of a phytotherapic composition based on vegetable extracts, as described in one of the Claims 1, 2 or 3, characterized for being used to prepare a medicinal composition for topic use.