阅读说明：本技术 用于局部使用的包含精油的组合物 (Composition for topical use comprising essential oils ) 是由 E·邦巴尔代利 于 2018-04-09 设计创作，主要内容包括：本发明涉及包含一种或多种精油的组合物,所述精油选自来自柑橘属水果、薰衣草或肉桂的油。所述组合物可以优选地局部施用。本发明的组合物可用于预防和/或治疗失眠和焦虑,以及用于降低食欲和刺激代谢。(The present invention relates to a composition comprising one or more essential oils selected from oils from citrus fruit, lavender or cinnamon. The composition may preferably be administered topically. The composition of the present invention is useful for preventing and/or treating insomnia and anxiety, and for reducing appetite and stimulating metabolism.)

1. a composition comprises one or more essential oils from citrus fruit, lavender (Lavandula officinalis) or cinnamon (Cinnamomum cassia).

2. The composition of claim 1, comprising the combination of essential oils of bergamot (Citrus bergamia) and lavender.

3. The composition of claim 2, wherein the weight ratio of essential oil of bergamot to essential oil of lavender is 10: 1.

4. A composition as claimed in claim 1, which comprises essential oils of grapefruit (Citrus paradisi) and cinnamon.

5. a composition as claimed in claims 1-4, wherein the essential oil is replaced by one or more active ingredients contained in the essential oil, selected from linalool, linalyl acetate and/or limonene.

6. The composition as claimed in claims 1-5, wherein the composition is administered via topical route.

7. The composition of claim 6, wherein the composition is administered in the nasal and/or perinasal and/or labial area.

8. A composition as claimed in claims 1-7 for use in the treatment of insomnia.

9. A composition as claimed in claims 1-7 for use in the treatment of anxiety.

10. A composition as claimed in claims 1-7 for use in reducing appetite and/or stimulating metabolism.

11. A composition as claimed in claims 1-7 for use in the treatment of overweight and obesity.

12. Use of a composition as claimed in claims 1-7 for weight loss.

Prior Art

Anxiety, depression and obesity are the most common diseases in modern times affecting a large proportion of people from infancy to adulthood.

Dysfunctions such as insomnia, anxiety states and mild depression are often caused by stress, competition and metabolic disorders, and their treatment requires the use of specific effective drugs, which are not recommended because of their side effects and possible risk of dependence.

Sleep disorders are highly prevalent in oncology and pre-operative fields and can increase problems that can lead to a reduction in the quality of life of the patient.

Anxiety and depression are often directly or indirectly related to metabolic disorders, leading to interpersonal problems.

Overweight before and after puberty and obesity in general cause major depression problems due to contact with the opposite sex or failure to follow a predetermined diet.

Overweight is also one of the major health problems, as it is positively associated with an increased risk of many serious diseases such as cardiovascular disease, diabetes and cancer.

Anxiety, depression and insomnia are interrelated in the absence of a specific mental disorder.

Insomnia is a very common problem in adults, both male and female, and it affects more and more individuals at the working age of 30 to 50 years, due to stress-induced anxiety, causing the individual to become tired and irritable; thus, there is a need for non-sedating tranquilizers having a calming, sleep-inducing function which should act in the most physiological manner possible.

sleep, and in particular good sleep quality, is one of the essential elements of good quality of life to maintain an individual's physical, social, emotional, and functional well-being.

Sleep is one of the major sources of energy in individuals, particularly in patients with severe illness, who have become exhausted from the illness.

Insomnia is a sleep disorder characterized by the inability to fall asleep even if the body is physically demanding sleep. Insomnia can be defined as a subjective feeling of difficulty with the initiation, duration and consolidation of sleep, leading to a reduction in sleep quality, which occurs despite adequate opportunities for rest, and leads to damage throughout the day.

This is associated with poor daytime quality of life, including symptoms of fatigue, learning and memory difficulties, and lack of interest in daily activities. The psychological effects are a great influence on the interpersonal relationships and the resulting irritability worsens the situation.

Unless otherwise indicated, "insomnia" means that there has been chronic insomnia for at least one month; otherwise, the condition is called acute or transient insomnia, which can vary in duration from days to weeks.

symptoms of insomnia can be found in approximately 33% to 50% of the adult population; when associated with stress or weakness, their incidence is between 10% and 15% of cases, while insomnia associated with a particular disease affects between 5% and 10% of cases.

Risk factors causing insomnia include aging, women, the presence of complications (medical, psychiatric, etc.), shift work, and the occurrence of devastating socioeconomic conditions.

The main disease features of insomnia relate to difficulty falling asleep, long nocturnal awakenings, no restorative or poor sleep quality, with individual variables related to the onset, duration, frequency and duration of triggers, the type of treatment currently and used in the past, and its efficacy.

Common problems associated with insomnia are a mean sleep onset latency >30 minutes, a night wake time with a total duration of more than 30 minutes, and a sleep time of less than 6 hours per night.

to ensure treatment success, it is necessary to confirm whether the patient suffers from true insomnia or insufficient sleep due to abnormal behavior or conditions associated with respiratory problems, restless leg syndrome, parasomnia, gastroesophageal reflux disease, and the like.

Some individuals suffering from hypersomnia, i.e. individuals who are abnormally asleep during the day, complain that they are unable to fall asleep and sleep for only a few minutes, with accompanying anxiety, which becomes chronic over time.

Hypersomnia is not a common condition, while chronic insomnia is common and can alter the natural sleep cycle, which is difficult to recover, in part because the patient attempts to fall asleep when he can sleep during the day and then stays awake at night, disrupting the circadian rhythm. In this regard, sleep deprivation can lead to physical and mental problems that are so severe that corrective medications are required; however, like all drugs that act on the central nervous system, they are not without side effects.

the risk of long-term insomnia is associated with cardiovascular, metabolic and immune deficiencies. Various forms of insomnia are a known problem since ancient times. In traditional medicine, a number of plants have been identified which, taken alone or even in a complex, mixture, appear to improve physical and mental status. Indeed, as with all symptoms related to the nervous system, the placebo effect is also evident.

The extract with mental metabolism effect can also be used for regulating appetite and body weight, and generating psychosomatic reaction.

Widely used products for oral administration are plants from the Papaveraceae (Papaveraceae) and Valerianaceae (Valerianaceae) families with hypnotic effects, or plant families containing sedative flavonoids, such as passion flower, hawthorn, chamomile, or plants rich in essential oils, lavender, citrus, etc.

The field patrinia family is widely used, although it has no clinically supported activity of many other commonly used plants. Recently, some essential oils, either orally administered at high doses, or designed for aromatherapy at the time of use, have entered into pharmaceutical and nutraceutical formulations.

Lavender essential oil was recently marketed as an anxiolytic in capsules at a dose of 80 mg/unit and its efficacy compared to the well-known benzodiazepines (Woelk. phytomedine 2010,12, 94-99; Kasper, European neuropsycosopharmalogy, 2015,25, 1960-67).

However, given the considerable antibacterial activity and the considerable irritancy of these active ingredients, high doses of essential oils are not without gastrointestinal side effects and may lead to e.g. gastroesophageal reflux. In the long run, continuous oral administration of large amounts of essential oils causes problems with renal clearance, so that treatment must be stopped.

Classical aromatherapy of anxiety and sleep disorders is known in traditional medicine, wherein its use is left to the user, who applies oil to various parts of the body, such as the temples or feet, or sprays drops in boiling water and inhales steam. However, these uses are not standardized and are not particularly easy to apply. For these reasons, the methods used in traditional medicine have not yet been clearly concluded with respect to their efficacy and use. High-dose oral administration was introduced to eliminate these drawbacks, but this involves the above-mentioned adverse effects.

The use of essential oil of bergamot (Citrus bergamia) in aromatherapy is disclosed in Frontiers in Pharmacology, 3 months and 2 days 2015, volume 6, clause 36, and its ability to improve mood and alleviate mild symptoms of stress disorder is mentioned.

The use of linalool-induced sedation in mice by vapor inhalation is disclosed in phytomedicin, 16(2009)303-307 by Link, v.m.

De Sousa, D.P. et al, in Molecules 2015,20,18620-18660 disclose sedative and anxiolytic activity of linalool and limonene when administered by inhalation.

Cheng, Bing-Ho et al, Journal of Traditional and Complementary Medicine, Vol.5, pp.1 (2014), 27-34, disclose anxiolytic activity of linalool from cinnamon cortex cinnamomi (Cinnamomum osmophorum) when administered orally to mice.

The effects of olfactory stimulation of grapefruit and lavender oils on Autonomic nervous activity and physiological function and their effect on appetite reduction are reviewed in Autonomic neuroscience, Basic and Clinical 185(2014)29-35 by Katsuya N.

However, none of the above documents specifically teach the use of essential oils in compositions for nasal, perinasal or labial administration.

CN 106266963a discloses the use of cinnamon and lime (Citrus aurantium) in a composition in the form of a lotion, ointment or powder for the treatment of fatty liver and hyperlipidemia. The document is silent about essential oils and their use in treating anxiety disorders or reducing appetite.

Thus, there remains a need to identify alternative products that can be used to prevent and/or treat insomnia and anxiety, as well as reduce appetite and metabolic stimulation.

Brief description of the invention

The present invention relates to compositions comprising one or more essential oils from citrus fruit, lavender (Lavandula officinalis) or cinnamon (Cinnamomum cassia).

The invention also relates to the use of said composition for the prevention and/or treatment of insomnia and anxiety, for reducing appetite and metabolic stimulation, for the treatment of overweight and obesity, and for weight loss.

Detailed Description

It has been surprisingly found that compositions comprising one or more essential oils selected from essential oils from citrus fruit, lavender, or cinnamon can be used to treat insomnia and anxiety, reduce appetite, and metabolic stimulation.

The essential oils are preferably obtained from the fruits of bergamot (Citrus bergamia), lemon (Citrus limon), grapefruit (Citrus paradisi) and lavender (Lavandula officinalis). The oil may be conventionally obtained by steam distillation or extraction with supercritical gases. The essential oil is preferably obtained from bergamot (Citrus bergamia).

Essential oils of bergamot (Citrus bergamia) can be prepared by compression and preferably contain 35% linalool, 30% linalyl acetate and 20% limonene and small amounts of other terpenes.

Grapefruit (Citrus paradisi) essential oil may be prepared by pressing and distillation.

The essential oil of lavender (Lavandula officinalis) preferably contains linalool and linalyl acetate in about the same ratio, as well as a small fraction of other monoterpenes.

The composition may comprise a single essential oil or a mixture of said essential oils.

Alternatively, the composition may comprise active ingredients contained in said essential oils, such as linalool, linalyl acetate and limonene. For example, the composition may comprise linalool, linalyl acetate and limonene, preferably in a 1:1:1 weight ratio.

According to a preferred aspect, the composition comprises only essential oils of bergamot (Citrus bergamia) as essential oils.

According to another preferred aspect, the composition comprises essential oils of bergamot (Citrus bergamia) in combination with essential oils of lavender (Lavandula officinalis), preferably in a weight ratio of 10: 1.

According to another preferred aspect, the composition comprises only essential oil of grapefruit (Citrus paradisi) as essential oil.

According to another preferred aspect, the composition comprises an essential oil of grapefruit (Citrus paradisi) and an essential oil of cinnamon (cinnamon cassia).

In another further preferred aspect, the composition comprises an essential oil from citrus fruit, an essential oil of lavender (Lavandula officinalis) and an essential oil of cinnamon (Cinnamomum cassia).

In the composition of the invention, the essential oil or oils may range from 2% to 25% w/w, and preferably 15% or 20% w/w, relative to the total weight of the composition.

In compositions where the essential oil of bergamot (Citrus bergamia) is the only essential oil, the amount may be from 5% to 25% w/w, and preferably 10% or 15% w/w.

In compositions where the grapefruit (Citrus paradisi) essential oil is the only essential oil, the amount may be from 10% to 25% w/w, and preferably 18% or 20% w/w.

The composition of the present invention may be administered 1 to 3 times per day, preferably 10 to 50mg of the composition is administered to the nose and the perinasal area.

According to another aspect, the composition may be administered topically, e.g., nasally, perinasally, labially, or other suitable site of the body.

The compositions may be incorporated into a semi-solid formulation, such as an ointment, gel or cream. Such formulations include, in addition to one or more of the aforementioned essential oils, other ingredients or excipients suitable for diluting the oil to the desired concentration and allowing topical application. Such other ingredients include vegetable oils and/or fats, such as castor (Ricinus communis) seed oil, avocado oil, sweet almond (Prunus amygdalus dulcis) oil, shea butter (shea butter); a thickener; surfactants and antioxidants.

The compositions of the present invention may be formulated according to conventional techniques, such as those described in Remington's Pharmaceutical Handbook, Mack Publishing co.

The compositions of the present invention are useful for treating insomnia and anxiety, reducing appetite, and stimulating metabolism.

Thus, the compositions of the present invention that reduce appetite and/or stimulate metabolism are useful for weight loss in general, and for the treatment of overweight and obesity in particular.

It was surprisingly found that the composition of the invention, applied topically on the lips, around the nose and in the nasal region, induces sleep in a short time and in a comfortable way in patients with insomnia (which is usually anxiety-dependent), without any side effects due to the low amount of essential oil applied.

Furthermore, the composition is characterized by easy use, even on nights where the patient wakes up and has difficulty falling asleep again.

The compositions of the present invention are particularly useful in pediatrics, as wake/sleep problems are particularly pronounced in growing children.

essential oils also have analgesic activity characteristics, which can be used in anxiety and insomnia states, especially in the case of chronic pain in elderly and long-term tumor patients, followed by appropriate analgesic treatment. The active principle is targeted mainly to the limbic system of the hypothalamus, from which biochemical and neuronal information is transmitted to specific sites. The hypothalamic-pituitary-adrenal axis is involved in metabolic regulation and insomnia.

The combination to be administered to humans is first tested on a rat basis, the electroencephalogram is monitored before and during treatment, and the experimental animals are placed in a controlled atmosphere of the active ingredient, as reported in the literature, to assess their efficacy in aromatherapy.

Thus, the present invention also relates to a method for treating insomnia and anxiety, in particular insomnia associated with anxiety, said method comprising administering to a subject in need thereof an effective amount of a composition, preferably in the form of an ointment, gel or cream, said composition comprising one or more essential oils selected from essential oils from citrus fruit, lavender or cinnamon.

In a preferred aspect, the method is a method for treating insomnia associated with anxiety, the method comprising administering to an individual in need thereof an effective amount of a composition comprising only bergamot (Citrus bergamia) essential oil as an essential oil. Preferably, the composition further comprises castor (Ricinus communis) seed oil, avocado oil and sweet almond (Prunus amygdalus dulcis) oil.

The invention also relates to a method for reducing appetite and stimulating metabolism, for treating overweight and obesity, and for reducing body weight, comprising administering to an individual in need thereof an effective amount of a composition, preferably in the form of an ointment, gel or cream, comprising one or more essential oils selected from oils from citrus fruit, lavender or cinnamon.

In a preferred aspect, the method is a method for reducing appetite, stimulating metabolism, and reducing weight, comprising administering to an individual in need thereof an effective amount of a composition comprising only grapefruit (Citrus paradisi) essential oil as an essential oil. Preferably, the composition further comprises castor (Ricinus communis) oil, avocado oil and sweet almond (Prunus amygdalus dulcis) oil.

The following examples further illustrate the invention.

Example 1 perinasal ointment based on essential oil of bergamot (Citrus bergamia)

Preparing a composition comprising (% w/w):