ES2464692A1 - Composition for the improvement of female sexual response (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

The present invention relates to a dermopharmaceutical and/or cosmetic composition for the improvement of the female sexual response comprising an effective amount of: oil of prunus amygdalus dulcis, oil of simmondsia chinensis, essential oil of lavandula angustifolia, oil of santalum album and of essential oil from pogostemon cablin. The present invention also relates to the use thereof for the preparation of a dermocosmetic and/or dermopharmaceutical composition for improving the female sexual response. (Machine-translation by Google Translate, not legally binding)

Description

FIELD OF THE INVENTION

The present invention is part of the field of cosmetic and dermopharmaceutical industry.

In particular, the present invention falls within the technical sector of compositions for topical use for the improvement of the welfare state of women by improving their sexuality.

The present invention relates to a topical composition in the form of a gel based on natural ingredients, thanks to which the sensitivity of the female erogenous zones is stimulated or improved by acting as a natural lubricant and moisturizing, nourishing and balancing the skin, as well as, stimulating with its aroma the olfactory nerve terminals, an effect that is enhanced by encapsulation of one of its components.

The present invention is formulated based on Prunus amygdalus dulcis oil, Simmondsia chinensis oil, Santalum album essential oil, Pogostemon cablin essential oil and Lavandula angustifolia essential oil. In the latter, its majority compound, linalool, is encapsulated with cyclodextrins.

STATE OF THE TECHNIQUE

The present invention relates to the stimulation or improvement of the sensitivity of the female erogenous zones by helping to stimulate the female sexual response and improving the sexuality of women.

Sexuality is one of the most important aspects of a woman's quality of life and is an indicator of the level of physical, psychological and social well-being. Different studies on

Female sexuality disorders conclude that these disorders primarily compromise desire and arousal.

In 1994, the American Psychiatric Association (APA) grouped normal sexual response disorders into four types: 1. Desire disorders; 2. Disorders of arousal; 3. Orgasmic failure and 4. Sexual pain. This classification refers only to psychological aspects. Later in 2000, the International Consensus Development Conferences on Female Sexual Dysfunctions added two more areas to the APA classification: lubrication and satisfaction. This fact resulted in the development of a test called "Female Sexual Function Index" (IFSF) for the evaluation of female sexual function through the scores obtained in six domains: desire, excitement, lubrication, orgasm, satisfaction and pain.

Different studies have demonstrated the usefulness of IFSF to evaluate sexuality at different stages of life and in different situations. A recent study conducted with 179 sexually active Spanish women, aged between 40 and 65, who completed the IFSF test concluded that there is a positive relationship between lower sexual function and menopause as well as the emotional states of women (Assessment of sexual function and related factors in mid-aged sexually active Spanish women with the six-item Female Sex Function Index. Pérez-López FR, Fernández-Alonso AM, Trabalón-Pastor M, Vara C, Chedraui P; MenopAuse Risk Assessment (MARIA) Research Group, Menopause, 2012 Nov; 19 (11): 1224-30)

Pregnancy is another factor associated with the reduction in the frequency of sexual activity as shown in a study conducted in 2012 by Corbacioglu et al. (The role of pregnancy awareness on female sexual function in early gestation. Corbacioglu A, Bakir VL, Akbayir O, Cilesiz Goksedef BP, Akca A. J Sex Med. 2012 Jul; 9 (7): 1897-903).

In this study, pregnant women at different gestational ages completed the IFSF test, obtaining lower results (P <0.001) for those women who were in the last trimester of pregnancy.

On the other hand, there are numerous studies that correlate the development of diseases with reduced sexual function.

The image that each woman has of her body can significantly affect the female sexual response, as shown in a study by Yasisca et al. in 2010 (The Association Between Sexual Satisfaction and Body Image in Women. Yasisca Pujols, BA, Cindy M. Meston, PhD, and Brooke N. Seal, PhD. J Sex Med. 2010 February; 7 (2 Pt 2): 905– 916). These authors studied 159 women between 18 and 49 years old with the objective of evaluating which aspects of body image influence female sexual satisfaction. To do this, different scales were used to measure the body image that each participant had of themselves and the IFSF test was used to measure sexual function. The results revealed that sexual satisfaction is related to a high concept of body image and a low frequency of distraction during sexual experience through thoughts related to appearance.

Therefore, the female sexual response is the set of psychophysiological changes associated with the performance of sexual acts.

The sexual response is characterized by the cyclic sequence of the phases of desire, excitement and orgasm, and finally the resolution phase (Mas, 2007) Physiology of the female sexual response: update Rev. Int Androl. 2007; 5 (1): 11-21

It is called desire or livid to the mental state of attention to erotic stimuli and psychological motivation that precedes or accompanies the performance of sexual acts. It can occur spontaneously or in response to various sensory stimuli and is mediated by hormones such as testosterone, some neuropeptides and pheromones. The factors that negatively affect desire are diet, stress, depression and diseases, both chronic and acute. It is important to highlight that the perception of desire presents a great interindividual variation and that psychological motivation can be affected by taboos and phobias.

Sexual arousal is a sensation that includes physical and psychological aspects of sexuality and is a response to stimuli. It may include a sensation of heat or beat in the genitals, vaginal lubrication or vaginal contractions.

The female sexual response can be increased when both desire and arousal increase. There are currently different products that are marketed as sexual stimulants ranging from drugs, capsules made from natural compounds and food supplements.

However, the female sexual response is characterized by being of great complexity due to the type of physical and psychological factors that can condition it and the enormous interindividual variability. This fact creates the need for topical products made from natural compounds aimed at the improvement of female sexuality through the senses, avoiding the side effects attributed to the intake of drugs or certain products made from natural extracts in the context of a more or less prolonged treatment.

Additionally, vaginal lubrication and hydration play a fundamental role in the female sexual response. Therefore, the application of a product that lubricates and moisturizes the vaginal area can help improve this response. However, the process of sexual excitement of women has a psychological and emotional component related to the so-called preparation period in which caresses have a very important role in obtaining the feelings of affection, safety and relaxation that precede desire sexual.

A large variety of products that hydrate or lubricate when applied in the vaginal area are currently marketed. However, it is necessary to have a product that in addition to providing the effects of hydration and lubrication, nourishes and balances the skin, sensitizes and stimulates not only in the vaginal area but can be applied in other erogenous areas of the female body and perform a aroma-therapeutic effect on female sexual response.

This fact is significant for the purpose of the present invention, because smell has a great relevance and importance in the context of today's world since the olfactory system is very present and linked to human relations in a very special way. The functioning of the physiological system that makes the sensation of smell possible has striking physical, rational, emotional and psychic effects in man. Smell, through the odoriferous signals of brain centers, is involved in sexuality, food, moods, character and basic behavioral impulses. Thus, there are numerous publications related to the use of odors to modify mood, attitude and sexual arousal (Relationship between mood change, odor and its physiological effects in humans while inhaling the fragrances of essential oils as well as linalool and its enantiomers. Sugawara Y, Shigetho A, Yoneda M, Tuchiya T, Matumura T, Hirano M. Molecules. 2013 Mar 13; 18 (3): 3312-38 Morris, ET Fragrance; Scribners: New York, NY, USA, 1984). Aromatherapy is the use of essential oils extracted from plants for the treatment of physical and physiological health. In the literature, the therapeutic properties of plants are widely described, both for the ingestion of the extracted compounds and for the inhalation of their aromas.

Thus, for example, the aroma of Sandalwood is sedative and relaxing and is beneficial for the treatment of anxiety, depression and insomnia. Lavender lifts your spirits, reassures and helps reduce stress, anxiety, depression and insomnia (Price, S. (1991) Aromatherapy for common ailments, p. 66. London: Gaia)

Today, aromatherapy is practiced together with massage and one of the most important allegations of aromatherapy is the reduction of anxiety (Why aromatherapy works (even if it doesn't) and why we need less research. A Vickers. Br J Gen Pract. 2000 June; 50 (455): 444-445).

In 2009, a systematic review was published to evaluate scientific experimentation aimed at demonstrating the effects of aromas on mood, psychology and behavior (Herz, 2009) Aromatherapy facts and fictions: a scientific analysis of olfactory effects on mood, physiology and behavior. Rachel S. Herz International Journal of Neuroscience, 119: 263-290, 2009. Of all the studies published between 1999 and 2009, only 18 met the necessary methodological requirements. An analysis of the two mechanisms proposed to explain these effects (pharmacological mechanisms or psychological mechanisms) concluded that the psychological one better explained the results obtained. Only one of the studies evaluated studied the effects of linalool after absorption through the skin (Transdermal absorption of (-) - linalool induces autonomic deactivation but has no impact on ratings of well-being in humans. Heuberger E, Redhammer S, Buchbauer G. Neuropsychopharmacology 2004 Oct; 29 (10): 1925-32) with effects on the deactivation of the autonomic central nervous system after 20 minutes of application on the skin of the abdomen.

In general, the aforementioned literature review concludes that the results indicate that various odors can significantly affect mood, consciousness, psychology and behavior. Among these, lavender stands out along with its majority component, linalool (Diego, MA, Jones, NA, Field, T., Hernandez-Reif, M., Schanberg, S., Kuhn, C., et al. (1998) Aromatherapy positively affects mood, EEG patterns of alertness and math computations, International Journal of Neuroscience, 96, 217-224, Moss, M., Cook, J., Wesnes, K., & Duckett, P. (2003). of rosemary andlavender essential oils differentially affect cognition and mood in healthy adults.International Journal of Neuroscience, 113, 15–38. Motomura, N, Sakurai, A., & Yotsuya, Y. (2001). Reduction of mental stress with lavender odorant Perceptual and Motor Skills, 93, 713-718. Campenni,

C. E., Crawley, E. J., & Meier, M. E. (2004). Role of suggestion in odor- induced mood change. Psychological Reports, 94, 1127-1136. Burnett, K. M., Solterbeck, L. A., & Strapp,

C. M. (2004). Scent and mood state following an anxiety provoking task. Psychological Reports, 95, 707-722).

Reviewing patent literature, we find patent document MXPA02003388A which refers to a facilitating gel for the female sexual response composed of a formula based on Papaverine, Atropine, Levomepromazine, Alprostadil, Pentoxifylline and physiological solution. The objective to be achieved after the topical application of the gel directly on the clitoris is a genital vasocongestive response, generating greater vaginal lubrication, increased sexual desire and a greater feeling of vaginal fullness. However, this composition has the problem that it can only be applied in the area of the clitoris without being able to be used in any other way.

US2011245345 refers to a topical composition for application in the genitals to improve the human sexual response. Said composition includes L-arginine and trans-resveratrol. However, this composition has the problem that it can only be applied in the area of the female genitals without being able to be used in other parts of the body.

WO03047610 describes a composition and method for increasing female sexual desire and satisfaction. The patent argues that it is a natural composition for topical use that is applied to the clitoris of women with and without sexual dysfunction 30 minutes before sexual activity. This composition contains L-Arginine, L-Histidine, Damiana leaves powder, Black Cohosh root powder, pregnelone, Maca extract and Progesterone. However, this composition has the problem that it can only be applied in the area of the clitoris without being able to be used in any other way.

The US8128972 patent refers to a composition and its intravaginal application to modulate all aspects related to the female sexual response including female sexual dysfunction. This composition is formulated with botanical extracts such as Angelica pubescens root and Coleus forskohlii extract. Specifically, it is argued that this composition improves vaginal lubrication, provides warmth, sensitivity, improves arousal and orgasm and accelerates them. However, this patent is an intravaginal application, having a fundamentally lubricating action, so it has limitations and cannot be used in other parts of the body.

Patent ES2291333 describes an invention that relates to all aspects that modulate the sexual response in women, including female sexual dysfunction, such as disorders of female sexual arousal, orgasmic disorders and sexual pain disorders, and increased sexual experience. of the woman. It refers to topical local compositions comprising one or more of the following ingredients: borage seed oil and other sources of gamma linolenic acid (GLA), Angelica pubescens root, Coleus forskohlii extract. According to said invention, these effects are achieved by the increase in localized nitric oxide, production and / or elevation of cAMP, production and / or elevation of cGMP, production of prostaglandin E1, inhibition of the degradation of prostaglandin E1, channel antagonism. calcium, phosphodiesterase inhibition, anti oxidation, vasodilation, smooth muscle relaxation, etc. In this case, it happens as with the aforementioned documents of the state of the art, which is a local application, without being able to be used as an essence of massage or of application in other parts of the body, outside the environment of the female genital area .

In the field of cosmetics, Procter & Gamble have a large number of patents (more than 300 patents) that describe the use of cyclodextrins to form inclusion complexes with different aromas and essential oils. These patents provide information on the characteristics that these complexes give to cosmetic products to which they are added: they prevent the destruction of aromas during processing and storage, increase the water solubility of lipophilic materials, convert liquid or oily products powder, increases the physical and chemical stability of complexed molecules, provides controlled emission of active ingredients, reduces or prevents skin irritation, prevents interaction with other ingredients in the formulation, increases or reduces the absorption of various compounds on the skin, stabilize emulsions and suspensions and reduce or eliminate undesirable odors. In any case, the formation of cyclodextrins is known to one skilled in the art for the complexation of essential oils and other lipophilic substances.

However, there is still a need in the state of the art for a natural product capable of stimulating and improving the sensitivity of the woman's erogenous zones acting through the dermis, while moisturizing, nourishing and balancing the skin, naturally achieving a lubricating effect and acting through its aroma by stimulating olfactory receptors. This aspect has been achieved by the inventors of the present invention by providing the composition object thereof

It has effects from the early stages of sexual stimulation (desire and arousal) improving the development of each stage of the female sexual response.

Another advantage of the present invention with respect to the state of the art is that there is no topical composition to this date in the state of the art comprising natural substances that meet the stability requirement necessary to exert its effect in a longer period of time or less long and that depends on the individual use that is given to the product. This is achieved by means of the formulation object of the present invention that favors a sustained release system thanks to the fact that the essential oils are complexed with cyclodextrins that help retain the aroma and achieve its controlled release after topical application.

There is therefore a need to find a non-invasive, safe, effective, sustained release and versatile composition in terms of the different areas of application while being effective in improving the female sexual response.

In this way the present invention solves the drawbacks of the state of the art by referring to a dermopharmaceutical and / or cosmetic composition of topical (non-invasive) administration in a plurality of areas of the body that allows a sustained release of the natural compounds included in the same. Additionally, the present invention has solved the problem presented by the formulations used for this purpose based on essential oils in terms of their instability as a result of the volatility of their compounds. These volatile compounds are responsible for the effects attributed to these substances. Therefore, in the present invention linalool has been encapsulated by complexing it with 2HP�-cyclodextrin (2-HP�-CD).

DETAILED DESCRIPTION OF THE INVENTION

Essential oils are complex mixtures that can have between 20 and 60 compounds of different chemical structure found in varying concentrations. Most of them are characterized by their volatility and their low solubility or insolubility in water. These characteristics make it difficult to manipulate the essential oils for the formulation of cosmetic products as they can affect the stability of the final product during storage due to the reduction in the amount of active compounds.

Volatile compounds can be stabilized by forming inclusion complexes with cyclodextrins (CDs) increasing their solubility and reducing or preventing evaporation. Furthermore, by complexing with CDs it is possible to achieve controlled emission of aromas by reducing their volatility and achieving a lasting aroma (Loftsson et al., 2000).

The CDs are natural cyclic oligosaccharides of six (a-CDs), seven (-CDs) or eight (V-CDs) glucose units linked by a- (1,4) bonds and having a hydrophobic central cavity and an outer surface lipophilic (Motwani M, Zatz JL. Applications of cyclodextrins in skin products. Cosmet Toilet. 1997; 112: 39Y47).

In aqueous solutions, the CDs are capable of forming inclusion complexes with various types of lipophilic materials when they are introduced into the hydrophobic cavity and a dimensional adjustment occurs between both molecules (Másson, M., Loftsson, T., Jónsdóttir, S., Fridriksdóttir, H., Petersen, DS Stabilization of drugs through complexation with non-ionic and ionic cyclodextrins. Int. J. Pharm. 1998, 164, 45–55).

There are numerous techniques for the formation of complexes with CDs. These include co-precipitation, complexing by the slurry method (or suspension complexation), paste complexing, wet mixing and heating, extrusion and dry mixing (Loftsson, T., Brewster, ME Pharmaceutical applications of cyclodextrins. 1. Drug solubilization and stabilization J. Pharm. Sci. 1996, 85, 1017-1025). Once the complexes have formed and dried they become very stable compounds. Thus, in the case of cosmetic formulations related to our invention, CDs are used to increase the water solubility of lipophilic compounds, convert the oily material into powder and facilitate its handling, increase the physical and chemical stability of the molecules of interest to protect them from decomposition, oxidation, hydrolysis and loss by evaporation, provide a controlled emission of the active ingredients allowing, for example, the more lasting perception of aroma and reducing skin irritation, among others (Buschmann, HJ, Schollmayer, E. Application of ciclodextrins in cosmetic products: a review J. Cosmet. Sci. 2002, 53, 185-191.

Among the natural compounds that are part of the composition of the present invention, the most important is lavender (Lavandula aungustifolia), considered as one of the most commercially used medicinal plants, since it provides several essential oils important for the food industry. fragrances, soaps, colognes, perfumes, skin lotions and other cosmetics (Inclusion interactions of cyclodextrins and crosslinked cyclodextrin polymers with linalool and camphor in Lavandula angustifolia essential oil. A. Ciobanua, b, c, I. Mallarda, b, D. Landya, b, G. Brabiec, D. Nistorc, S. Fourmentina Carbohydrate Polymers 87 (2012) 1963–1970 Lavender has been used in medicine as an antispasmodic, sedative, antihypertensive, antiseptic, healing and anti-inflammatory (Biological activities of lavender essential oil, Cavanagh HM, Wilkinson JM, Phytother Res. 2002 Jun; 16 (4): 301-8).

Recently, its potential to reduce stress has also been demonstrated in different clinical and preclinical studies (Takahashi M, Satou T, Ohashi M, Hayashi S, Sadamoto K, et al. (2011) Interspecies comparison of chemical composition and anxiolytic-like effects of lavender oils upon inhalation. Nat Prod Commun 6: 1769-1774). Attributing linalol responsibility for the anxiolytic effect (Linck VM, da Silva AL, et al. (2010). Effects of inhaled Linalool in anxiety, social interaction and aggressive behavior in mice. Phytomedicine 17 (89): 679-83. Tsang, HW, Ho, TY, 2010. A systematic review on the anxiolytic effects of aromatherapy on rodents under experimentally induced anxiety models. Reviews in the Neurosciences 21, 141–152. Umezu, T., Nagano, K., Ito, H., Kosakai, K., Sakaniwa, M., Morita, M., 2006. Anti-conflict effects of lavender oil and identification of its active constituents Pharmacology Biochemistry and Behavior 85, 713-721 Woronuk, G., Demissie, Z. , Rheault, M., Mahmoud, S., 2011. Biosynthesis and therapeutic properties of Lavandula essential oil constituents. Planta Medica. 77, 7–15).

One of the major compounds of lavender is linalool, present in different concentrations in more than 200 plants. Linalool is a monoterpene synthesized by the isopentyl pyrophosphate pathway, from the universal intermediate geranyl pyrophosphate, through the enzyme linalool synthetase.

Linalool is used as an aroma in a large number of cosmetic products, giving them a characteristic odor easily detectable and identifiable as "harmonizing" as shown in a very recent review on the relationship between mood swings, smell and physiological effects while essential oil fragrances such as linalool (Relationship between Mood Change, Odor and Its Physiological Effects in Humans While Inhaling the Fragrances of Essential Oils as well as Linalool and Its Enantiomers Yoshiaki Sugawara *, Asami Shigetho, Mai Yoneda, Tomoko Tuchiya , Tomomi Matumura and Miki Hirano. Molecules 2013, 18, 3312).

However, even the research that supports the present invention has not determined the beneficial properties it has as a stimulant of the female sexual response.

For the present invention, research has focused on developing a controlled release system of one of the major components of the essential oil of lavender (Lavandula Angustifolia), linalool (9.68%). For this, different experiments were carried out using cyclodextrins to form inclusion compounds, obtaining higher formation constants when -CD was used as well as greater capacity to retain the aroma in the aqueous phase. In addition, in consecutive extractions of the aroma complexed with -CD, linalool was quantified and the results were compared with those obtained from this same compound without complexing, obtaining that the period of time that lasted the emission and consequent release of linalool was longer when it was part of the inclusion compounds.

Among the natural compounds that are part of the composition of the present invention, they stand out for their properties:

 Prunus amygdalus dulcis (Sweet almond oil). It contains 62% oleic acid (a w9 fatty acid), 29% linoleic acid (polyunsaturated fatty acid w6), 6% palmitic acid (saturated fatty acid) according to the USDA (National Reference Database for Standard reference) ) and the "oleum amygdalae" which is a glyceryl oleate that gives it the soft smell and taste of almonds. Almond oil also contains other fatty acids, such as myristic acid, palmitoleic acid, heptadecanoic acid, 9heptadecanoic acid, stearic acid, arachidic acid and eicosanoic acid. The widespread cosmetic use of almond oil is as a base oil for massages because, due to its hypoallergenicity, it can be used on sensitive skin. It is a good skin softener while giving it a radiant and healthy appearance. It nourishes the skin since almond oil contains antioxidants, compounds that protect the skin from damage caused by environmental agents and stimulate the skin's natural repair mechanism. Almond oil contains natural fatty acids that maintain the skin's hydration levels, creating a barrier that limits moisture loss and restores natural protection to skin cells while allowing skin to absorb moisture.

 Simmondsia chinensis oil. The chemical constituents of jojoba oil have surprisingly similarities with human fat. This makes jojoba oil have a very important role in the development of cosmetics and other topically applied products. Jojoba oil contains nutrients, phospholipids, vitamins E and B and minerals such as silicon, copper, zinc and iodine. It contains fatty acids such as palmitic, palmitoleic, oleic acid (10-113%), linoleic, linolenic, arachidic, eicosanoic (66-71%), behemic, erucic, docosaenoic (14-20%), lignoceric and nervous. The oil is a mixture of wax esters with a length of 36-46 Carbon atoms. Each molecule consists of fatty acids and fatty alcohols linked by an ester bond. 98% of the fatty acids are polyunsaturated w9. The cosmetic use of jojoba oil, applied to the skin, is balancing. Therefore, it is an excellent moisturizer for all skin types. It has absorption properties in the skin, it is emollient and softening. It forms a non-greasy or sticky layer on the skin that prevents excessive loss of water keeping the skin healthy and hydrated. Jojoba oil balances the natural pH of the skin. It also has antibacterial properties.

Lavandula Angustifolia Essential Oil (lavender). The main compounds of the 150 constituents of Lavender are linalool (20-46%) and terpene esters, mainly linalyl acetate (36-51%). The main chemical constituents of Lavender are esters (45%), Alcohols (36%) and Ketones (4%). Lavender essential oil contains about 40 compounds that include linalyl acetate, cineole, linalool, nerol, borneol, Falvonoids and Tannins. The generalized cosmetic use of lavender is due to its antiseptic, antibacterial, anti-toxic, anti-inflammatory, bactericidal, healing and restorative properties. It also performs tonic and therapeutic effects when applied to the skin. In external use it is a good essence to add to the bathroom and get a gentle relaxing effect. It is a cell regenerator, skin rejuvenator, anti-cellulite, reduces anxiety, depression and general weakness.

 Santalum album (Sandalwood). Its oil extracted from wood contains terpenic, santálicos, teresantálicos and hydrocarbon alcohols. Externally it gives off a very characteristic smell that helps to reach very interesting mystical and relaxing states. Also in aromatherapy has effects such as skin anti-aging.

Pogostemon cablin essential oil (Pachouli). The main component of the essential oil of Pachouli is pachulol (17.5-54.31%). Among its effects, appetite reduction, anti-inflammatory, efficacy in the treatment of acne, insomnia, tranquilizer, sedative and hypotensive are known.

Therefore, the present invention relates to a composition for topical use in a plurality of parts of the human body in the form of an emulsion based on natural ingredients, thanks to which the sensitivity of female erogenous zones is stimulated or improved by acting as a natural lubricant and moisturizing, nourishing and balancing the skin as well as stimulating with its aroma the olfactory nerve terminals, an effect that is enhanced by encapsulating one of its components.

Taking into account the aforementioned components, the invention object of the present invention is considered highly novel, because thanks to the inventive effort of the researchers it has been possible to obtain a combination of elements with beneficial properties for the improvement of the female sexual response, since there are no state-of-the-art documents that disclose a composition for the improvement of the female sexual response formulated based on Prunus amygdalus dulcis oil, Simmondsia chinensis oil, Santalum album essential oil, Pogostemon cablin essential oil and Lavandula essential oil angustifolia

Additionally, the composition object of the present invention contains linalool conjugated with -cyclodextrin, which improves its stability during formulation and in the product's shelf life. The complex formed by linalool-cyclodextrin fulfills the function of releasing the active agent in a controlled manner during the topical application of the product.

Preferably, the application of the composition for topical use is in the form of a gel, cream or lotion. The preferred form is a cremigel, that is to say, a topical pharmaceutical form composed in turn of two: emulsion and gel, generally defined as an emulsion (generally of external aqueous phase) whose aqueous phase is gelled.

The present invention relates to a dermopharmaceutical and / or cosmetic composition for the improvement of the female sexual response comprising the following components in the following proportions, so that the sum thereof does not exceed 100% of the composition:

Prunus amygdalus dulcis oil

at least 20%

Simmondsia chinensis oil

at least 1%

Essential oil of Lavandula angustifolia

at least 1%

Santalum album oil

at least 1%

Pogostemon cablin essential oil

at least 1%

Preferably, the essential oil of Lavandula angustifolia is encapsulated in cyclodextrins.

The present invention relates to a dermopharmaceutical and / or cosmetic composition for the improvement of the female sexual response comprising at least 1% of linalool. Preferably, linalool is within an inclusion complex with 2-HP-CD.

The amount of linalool conjugated with HP-CDs in the composition is 12% linalool and 88% HP-CDs; such that the ratio between linalool and cyclodextrin in the linalool conjugated with HP-CDs is 1: 1.

To calculate the efficiency of linalool conjugated with HP-CDs, an aqueous solution with HP-CDs was placed to which a saturating amount of linalool was added and kept in an ultrasonic bath for 60 minutes at 20 ° C until reaching the Balance. The solution was then filtered through a 0.45 µm pore size nylon filter to remove excess undissolved linalool. A complexation constant (Kc) of 2471 M-1 and a complexation efficiency of 93502 were obtained.

The inclusion complex of Lavender essential oil with HP-CDs with a 1: 1 molar ratio was prepared by modifying the method of de Matsuda et al., 1991. Matsuda H, Ito K, Fujiwara Y, et al. Complexation of various fragrance materials with 2-hydroxypropyl-cyclodextrin. Chem Pharm Bull (Tokyo). 1991; 39: 827Y830.

2.5 g of HP-CDs were dissolved in 47 ml of distilled water to prepare the aqueous CD solution. 0.28 g of linalool and 0.272 g of benzyl acetate were gradually added to the aqueous CD solution and mixed for 12 hours at 300 rpm with magnetic stirrer being maintained at a constant temperature of 25 ° C ± 2 ° C. The solution was filtered through a 0.45 µm cellulose acetate membrane filter pore size. Finally, the aqueous solution of the inclusion complex was transformed into a powder compound by the lyophilization method.

The topical composition object of the present invention also contains a series of ingredients that act as thickeners, emulsifiers and stabilizers necessary to make the composition with the active ingredients, improve stability and facilitate its dispensing. The use of these ingredients is well known for formulating topical compositions on the skin such as emulsions, gels, creams or lotions.

The topical form of the present invention is a cremigel formed by an oil phase composed of fats and / or oils and emulsifiers w / o and a gelled aqueous phase composed of water, humectants, o / w emulsifiers and gelling agent. The cremigeles are very evanescent, have high extensibility, excellent cosmetic appearance (high gloss), tend to have high consistency (the higher the concentration of gelling agent, the greater consistency) and have a great cooling effect.

The composition object of the present invention may also contain ingredients and

5 additives that are widely used for the elaboration of topical application formulations. For example, moisturizers such as glycerin; antioxidants such as tocopherol acetate; emulsifiers and stabilizers such as polysorbate 60, polymers based on sodium acrylate, acryloyl dimethyl restaurant and dimethylacrylamide; emollient agents such as isohexadecane, tocopheryl acetate as an antioxidant and antimicrobials such as methylchloroisothiazolinone and

10 methylisothiazolinone.

On the other hand, the invention relates to a method for improving the female sexual response administered topically in the vaginal area and in other erogenous areas of the female body such as the breasts, behind the ears and the neck being able to be applied along the spine vertebral and other areas of the body.

In addition, the invention relates to a product formed by the topical solution in a container for instant dispensing.

EXAMPLES OF REALIZATION

The following specific examples provided herein serve to illustrate the nature of the present invention. These examples are included for purposes only.

20 illustrative and should not be construed as limitations on the invention claimed herein.

Example 1: Formulation of a cremigel for topical use in women.

In this example, a composition with the following components is formulated:

Ingredient Weight percentage

Glycerin

15-25

Prunus amygdalus dulcis oil

20-25

Sodium acrylate / acryloylmethyl restaurant / dimethyl acrylamide

1.00-1.50

Simmondsia chinensis oil

1.00-1.50

Essential oil of Lavandula angustifolia

1.00-1.50

Santalum album essential oil

1.00-1.50

Isohexadecane

0.5-1.00

Tocopheryl acetate

0.5-1.50

Pogostemon cablin essential oil

1.00-1.50

Polysorbate 60

0.15-0.30

Methylchloroisothiazolinone

0.05-0.15

Methylisothiazolinone

0.05-0.15

Water

 q.s.

Example 2: Evaluation of effect on female sexual response

To determine the effectiveness of the formulation of Example 1 in the female sexual response, a study was conducted with 10 women aged between 18 and 45 years who had a stable partner. This efficacy was assessed using the female sexual function index index (FSFI) based on the clinical interpretation of the analysis of the 6 main components of sexual function: desire, excitement, lubrication, orgasm, satisfaction and pain ( The Female Sexual Function Index (FSFI): A Multidimensional Self-Report Instrument for the Assessment of Female Sexual Function R. ROSEN et al. Journal of Sex & Marital Therapy, 26: 191–208, 2000).

To establish the effectiveness of the product, a comparison was made between the score obtained in the test before the use of the product and the score obtained after one month of use of the product. This comparison was made by T-Student test for related samples.

The score obtained by this group of women in the female sexual function index before using the product was 15.8 ± 4.2 while after a month of use, the score was 25.6 ± 8.4 obtaining statistically significant differences between both scores (p <0.002). Therefore, the use of this product produced a significant improvement in female sexual functionality.

Table 1 shows the results obtained for each of the components of the Female Sexual Function Index Test before and after the use of the formulation of Example 1.

Wish

Lubrication Orgasm Satisfaction Pain

Baseline result (Mean ± standard deviation)

2.4 ± 0.8 2.5 ± 0.8 2.6 ± 1.0 2.6 ± 6 3.0 ± 1.2

Final result (Mean ± standard deviation)

4.0 ± 1.2 4.0 ± 1.7 4.3 ± 1.4 4.4 ± 1.4 4.4 ± 1.5

Table 1

Table 1 represents the mean and standard deviation of the results obtained for the components of the FSFI test, desire, lubrication, orgasm, satisfaction and pain.

During the use of the formulation of Example 1, no adverse events were recorded.

According to an important aspect, the present invention relates to a dermopharmaceutical and / or cosmetic composition for the improvement of the female sexual response comprising an effective amount of: Prunus amygdalus dulcis oil, Simmondsia chinensis oil, Lavandula essential oil angustifolia, Santalum album oil

15 and essential oil of Pogostemon cablin.

According to another aspect, the dermopharmaceutical and / or cosmetic composition comprises the following components in the following proportions by weight, so that the sum thereof does not exceed 100% of the composition:

Prunus amygdalus dulcis oil at least 20% Simmondsia chinensis oil at least 1% 20 Essential oil of Lavandula angustifolia at least 1% Santalum album oil at least 1% Pogostemon cablin essential oil at least 1%

According to another aspect, the dermopharmaceutical and / or cosmetic composition comprises at least 1% linalool. Preferably, linalool is within an inclusion complex with 2-HP-CD.

According to another aspect, the ratio between linalool and 2-HP-CD in the complex formed is 5 of 1: 1.

According to another aspect, the dermopharmaceutical and / or cosmetic composition additionally has moisturizing agents, antioxidant agents, emulsifying agents, stabilizing agents, emollient agents and antimicrobial agents.

According to another aspect, the dermopharmaceutical and / or cosmetic composition comprises the following components in the following proportions by weight, so that the sum thereof does not exceed 100% of the composition:

Ingredient Weight percentage

Glycerin 15-25 Prunus amygdalus dulcis oil 20-25 Sodium acrylate / acryloylmethyl restaurant / dimethyl acrylamide 1.00-1.50 Simmondsia chinensis oil 1.00-1.50

Lavandula angustifolia essential oil 1.00-1.50 Santalum album essential oil 1.00-1.50 Isohexadecane 0.5-1.00 Tocopheryl acetate 0.5-1.50 Pogostemon cablin essential oil 1.00- 1.50 Polysorbate 60 0.15-0.30 Methylchloroisothiazolinone 0.05-0.15 Methylisothiazolinone 0.05-0.15 Water qs

In accordance with another important aspect, the present invention relates to the use of the aforementioned composition for the preparation of a dermocosmetic and / or dermopharmaceutical composition for improving the female sexual response. Preferably, the use is topical in emulsion form. Preferably, the use is topical in liquid form, in foam form, in gel form, in cremigel form or in spray form. Preferably, the composition object of the present invention is applied topically in the vaginal area, in the breasts, behind the ears, in the neck and / or in the back.

Claims (12)

1. Dermopharmaceutical and / or cosmetic composition for the improvement of the female sexual response characterized in that it comprises an effective amount of Prunus amygdalus dulcis oil, Simmondsia chinensis oil, Lavandula angustifolia essential oil, Santalum album oil and essential oil of Pogostemon cablin. 2. Composition according to claim 1 characterized in that it comprises the following components in the following proportions by weight, so that the sum thereof does not exceed 100% of the composition:

Prunus amygdalus dulcis oil

at least 20%

Simmondsia chinensis oil

at least 1%

Essential oil of Lavandula angustifolia

at least 1%

Santalum album oil

at least 1%

Pogostemon cablin essential oil

at least 1%

3. Composition according to any of claims 1 and 2 characterized in that the essential oil of Lavandula angustifolia is encapsulated in cyclodextrins. 4. Composition according to claim 1 characterized in that it comprises at least 1% linalool. 5. Composition according to claim 4 characterized in that the linalool is within an inclusion complex with 2-HP-CD. 6. Composition according to claim 5 characterized in that the ratio between linalool and 2-HP-CD in the complex formed is 1: 1. 7. Composition according to any of claims 1 to 6, characterized in that it additionally has moisturizing agents, antioxidant agents, emulsifying agents, stabilizing agents, emollient agents and antimicrobial agents. 8. Composition according to claim 1 characterized in that it comprises the following components in the following proportions by weight, so that the sum thereof does not exceed 100% of the composition: Ingredient Weight percentage Glycerin 15-25 Prunus amygdalus dulcis oil 20-25 Sodium acrylate / acryloylmethyl restaurant / dimethyl acrylamide 1.00-1.50 Simmondsia chinensis oil 1.00-1.50 Lavandula angustifolia essential oil 1.00-1.50 Oil essential of Santalum album 1.00-1.50 Isohexadecane 0.5-1.00 Tocopheryl acetate 0.5-1.50 Pogostemon cablin essential oil 1.00-1.50 Polysorbate 60 0.15-0.30 Methylchloroisothiazolinone 0.05-0.15 Methylisothiazolinone 0.05-0.15 Water q.s. 9. Use of the composition as defined in any of claims 1 to 8 for 10 the preparation of a dermocosmetic and / or dermopharmaceutical composition to improve the female sexual response. 10. Use of the composition as defined in any of claims 1 to 8 for the preparation of a dermocosmetic and / or dermopharmaceutical composition for topical use in the form of emulsion. 11. Use of the composition as defined in any one of claims 1 to 8 for the preparation of a dermocosmetic and / or dermopharmaceutical composition for topical use in liquid form, in foam form, in gel form, in cremigel form. or in the form of a spray. 12. Use of the composition as defined in any of claims 1 to 8 20 applied topically on the vaginal area, on the breasts, behind the ears, on the neck and / or on the back. SPANISH OFFICE OF THE PATENTS AND BRAND Application no .: 201430090 SPAIN Date of submission of the application: 27.01.2014 Priority Date: REPORT ON THE STATE OF THE TECHNIQUE 51 Int. Cl.: See Additional Sheet RELEVANT DOCUMENTS

Category

56 Documents cited Claims Affected

Y

WO 2006101409 A1 (PRO-PERSPIRANT LIMITED) 28.09.2006, page 1, lines 9-17; page 6, line 32 - page 7; page 17, lines 7-8; page 18, lines 19-23; page 20, line 35 - page 21; pages 24-28. 1-7,10.11

Y

US 6579543 B1 (McCLUNG, J. H.) 06.17.2003, column 17, lines 40-65. one

Y

WO 2005062730 A2 (KIM, N. H.) 07.07.2005, pages 1.2; page 4, line 13 - page 5; page 6, lines 2-15; page 10; page 11, line 22 - page 12, line 15; page 21. 2,7,10.11

Y

CIOBANU, A., MALLARD, I., LANDY, D., BRABIE, G., NISTOR, D., FOURMENTIN, S. Inclusion interactions of cyclodextrins and crosslinked cyclodextrin polymers with linalool and camphor in Lavandula angustifolia essential oil. Carbohydrate Polymers, 2012, vol. 87, No. 3, pages 1963-1970. ISSN: 0144-8617. Doi: 10.1016 / j.carbpol. 2011.10.005. 3-6

TO

FR 2973706 A1 (N GUYEN GERARD DUC) 12.10.2012, page 3; claim 1. one

Category of the documents cited X: of particular relevance Y: of particular relevance combined with other / s of the same category A: reflects the state of the art O: refers to unwritten disclosure P: published between the priority date and the date of priority submission of the application E: previous document, but published after the date of submission of the application

This report has been prepared • for all claims • for claims no:

Date of realization of the report 05.26.2014

Examiner A. Sukhwani Page 1/5

REPORT OF THE STATE OF THE TECHNIQUE Application number: 201430090 CLASSIFICATION OBJECT OF THE APPLICATION A61K36 / 736 (2006.01) A61K36 / 53 (2006.01) A61K36 / 185 (2006.01) A61K8 / 92 (2006.01) A61P15 / 00 (2006.01) A61Q19 / 00 (2006.01) Minimum documentation sought (classification system followed by classification symbols) A61K, A61P, A61Q Electronic databases consulted during the search (name of the database and, if possible, search terms used) INVENES, EPODOC, WPI, X-FULL, NPL State of the Art Report Page 2/5  WRITTEN OPINION Application number: 201430090 Date of Completion of Written Opinion: 05.26.2014 Statement

Novelty (Art. 6.1 LP 11/1986)

Claims Claims 1 -12 IF NOT

Inventive activity (Art. 8.1 LP11 / 1986)

Claims Claims 8, 9, 12 1 -7, 10, 11 IF NOT

The application is considered to comply with the industrial application requirement. This requirement was evaluated during the formal and technical examination phase of the application (Article 31.2 Law 11/1986).  Opinion Base.- This opinion has been made on the basis of the patent application as published.  Considerations: A subject of the present invention is a dermopharmaceutical and / or cosmetic composition comprising Prunus amygdalus dulcis oil (sweet almonds), Simmondsia chinensis oil (jojoba), Lavandula angustifolia essential oil (lavender), Santalum album oil (sandalwood) and essential oil of Pogostemon cablin (patchouli) (claim 1), wherein the proportions are at least 20% of Prunus amygdalus dulcis and at least 1% of the other four oils, so that the sum does not exceed 100% of the composition (reiv. 2). The essential oil of Lavandula angustifolia is encapsulated in cyclodextrins (reiv. 3) and comprises at least 1% of linalool (reiv. 4), within an inclusion complex with 2-HP -CD, in the 1: 1 ratio ( reivs. 5, 6). The composition additionally contains moisturizing agents, stabilizing emulsifying antioxidants, emollients and antimicrobial agents (reiv. 7) so that the sum of these and the claimed oils does not exceed 100% (reiv. 8). Finally, the use of the composition for the preparation of a dermocosmetic and / or dermopharmaceutical composition for the improvement of the female sexual response (reiv. 9), for topical use in the form of emulsion (reiv. 10), is protected. or in liquid form, foam, gel, cremigel or spray (reiv. 11), applied in the vaginal area, breasts, ears, in the neck and / or in the back (reiv. 12). State of the Art Report Page 3/5  WRITTEN OPINION Application number: 201430090 1. Documents considered.- The documents belonging to the state of the art taken into consideration for the realization of this opinion are listed below.

Document

Publication or Identification Number publication date

D01

WO 2006101409 A1 (PRO-PERSPIRANT LIMITED) 28.09.2006

D02

US 6579543 B1 (McCLUNG, J. H.) 06.17.2003

D03

WO 2005062730 A2 (KIM, N. H.) 07/14/2005

D04

CIOBANU, A., MALLARD, I., LANDY, D., BRABIE, G., NISTOR, D., FOURMENTIN, S. Inclusion interactions of cyclodextrins and crosslinked cyclodextrin polymers with linalool and camphor in Lavandula angustifolia essential oil. Carbohydrate Polymers, 2012, vol. 87, No. 3, pages 1963-1970. 2012

D05

FR 2973706 A1 (N GUYEN GERARD DUC) 12.10.2012

2. Statement motivated according to articles 29.6 and 29.7 of the Regulations for the execution of Law 11/1986, of March 20, on Patents on novelty and inventive activity; quotes and explanations in support of this statement  NOVELTY  The documents cited D01 to D03, D05 refer to topical compositions for the skin with oils, while D04 refers to the inclusion of essential oils in cyclodextrins. So:

-

D01 discloses the use of vegetable oils to stabilize essential oils and promote their absorption through the skin. Essential oils have therapeutic effect and improve mood such as anxiety and stress, among the oils used are lavender (Lavandula angustifolia), patchouli and sandalwood (page 28) and as carrier oils among other sweet almond oil or Jojoba oil (page 1, lines 9-17; page 6, line 32-page 7; page 17, lines 7-8; page 18, lines 19-23; page 20, line 35-page 21; pages 24-28 ), although, it does not disclose that the five oils are in the same composition and therefore do not anticipate the invention.

-

D02 refers to a topical skin composition that incorporates essential oils and lists the five oils of claim 1 (column 17, lines 40-65) although, not necessarily all five at the same time.

-

D03 refers to a cosmetic composition for mental stability, depression, insomnia, stress (page 1) with lavender and sandalwood essential oils in almond oil that can reach up to 50% (page 2; page 4, line 13 page 5; page 6, lines 2-15; page 10; page 11, line 22-page 12, line 15; page 21).

-

D04 discloses the inclusion in linalool cyclodextrins of Lavandula angustifolia (pages 1963-1970).

-

D05 refers to a concentrated composition of essential oils for external use to improve muscle tissue contractures comprising oils such as Lavandula angustifolia, Pogostemon cablin (patchouli) in oils such as sweet almonds (page 3; claim 1).

 These cited documents do not disclose compositions with the five claimed oils. Therefore, in view of documents D01 to D05, it can be concluded that claims 1-12 are new in accordance with Article 6 LP 11/86.  INVENTIVE ACTIVITY The composition object of the invention is evident to those skilled in the art in view of documents D01 to D04, the most relevant being D01. Indeed,

-

D01 discloses compositions of three of the minor oils lavender, patchouli and sandalwood in sweet almond oil or jojoba oil. That is, two alternatives with four of the oils (page 6, line 32-page 7; page 17, lines 7-8; page 18, lines 19-23; page 20, line 35-page 21; pages 24-28), affecting the inventive activity of claims 1-7, 10, 11.

-

D02 discloses the five oils in a list (column 17, lines 40-65).

For the expert in view of these two documents it would not be any technical problem to arrive at the composition of the three oils of D01 with sweet almond oil, adding jojoba oil, cited in D01 and listed in D02 with the other claimed oils. State of the Art Report Page 4/5  WRITTEN OPINION Application number: 201430090

-

D03 reports that the majority component is almond oil that is at least 20% (page 2; page 4, line 13-page 5; page 6, lines 2-15; page 10; page 11, line 22-page 12, line 15; page 21).

-

D04 refers to Lavandula angustifolia linalool within an inclusion complex with 2-HP-CD (page 1965, column 1; page 1966; column 1).

With these disclosures of the state of the art for the expert the composition of the five oils is evident, the majority being sweet almond oil, in which linalool is in inclusion complexes, which additionally carries agents and is of topical use , either in the form of emulsion, liquid, foam, gel, cremigel or spray. Therefore, in view of documents D01 to D04, it can be concluded that claims 1-7, 10, 11 lack inventive activity according to Article 8 LP 11/86. State of the Art Report Page 5/5