Herbal preparation and its application for colds and flu

Abstract

A herbal preparation consisting of raw plant material, whose active components are herbal extracts (Pelargonium root, Sambucus nigra fruit, acerola and rosehip, Salix alba bark), vitamin D, zinc, and copper, and which has a synergistic effect in the prevention and / or treatment of symptoms of cold and flu, such as cough, sore throat, and inflammatory processes of the upper respiratory tract.

Description

[0001] HERBAL PREPARATION AND ITS APPLICATION FOR COLDS AND FLU

[0002] FIELD OF INVENTION

[0003] The subject invention relates to the field of pharmacy, specifically to viral therapy. More precisely, it refers to a herbal preparation consisting of plant material whose active components are plant extracts ( Pelargonium root, blackberry fruit, acerola and rosehip, white willow bark), vitamin D, zinc and copper, and their pharmaceutical use for the prevention and / or treatment of cold and flu symptoms such as cough, sore throat and inflammatory processes of the upper respiratory tract. According to the International Patent Classification (IPC, 2025.01), the subject invention is classified under A61K 31 / 00, A61K 31 / 191 , A61K 36 / 00, A61K 36 / 35, A61K 36 / 738, A61K 125 / 00 (2006.01), A61K 131 / 00 (2006.01).

[0004] TECHNICAL PROBLEM

[0005] The subject invention solves the technical problem of how to provide a herbal preparation with pronounced pharmacological properties through the use of appropriate amount of plant extracts (pelargonium root, blackberry fruit, acerola and rosehip, white willow root), vitamin D, zinc and copper, intended for the prevention and / or treatment of symptoms of cold, flu, sore throat, cough and respiratory problems in individuals with weakened immunity.

[0006] STATE OF THE ART

[0007] Acute respiratory infections (ARIs) are the most common infections in modern humans. Adults typically get sick from these infections 3-5 times per year on average, while children are affected even more frequently. With a drop in temperature, the body’s natural resistance significantly decreases, increasing tendency to acute respiratory infections. Full work activity and prolonged stays in enclosed spaces with insufficient fresh air contribute to a higher frequency of illness. This group of diseases includes infections of the respiratory tract caused by various microorganisms, but mostly viral infections. Viruses, the most common causes of acute respiratory infections, include rhinoviruses, influenza and parainfluenza viruses, respiratory syncytial virus, coronaviruses, adenoviruses, and others. The symptoms of infection differ depending on whether the infection affects the upper or lower respiratory tract and usually include: congestion and blockage (of the sinuses, lungs, or nose), runny nose, cough, sore throat, muscle pain, fatigue, exhaustion, and malaise. The common cold is the most frequent viral respiratory infection. It usually occurs during the autumn and spring months, as well as in winter. The common cold is caused by viruses from several different virus families. More than 100 different viral subtypes of the common cold are known, which is why the incidence of colds is high. In most cases, it lasts about a week unnles it is complicated by a bacterial infection. A cold usually begins gradually, characterized by normal or slightly elevated temperature, nasal congestion, rhinorrhea, sneezing, and increased tearing of the eyes. Headache, sore throat, and cough may also occur, but they are milder in intensity compared to the flu.

[0008] Sore throat is so common because the nose and throat are the first passages through which pathogens enter the body. The mucous membrane has one of the mechanisms responsible for removing pathogens. Cold weather, for example during the winter months, causes the blood vessels in this area to constrict due to the cold air. They also tend to dry out more frequently. Reduced circulation, and the associated decreased mucus production, make it easier for viruses to infect the throat and build up there. Difficulty swallowing also occasionally occurs along with a sore throat. A potential cause could be inflammation of the esophagus or mucous membrane.

[0009] Cough is one of the most common symptoms for which patients visit a doctor in primary health care, as well as a pulmonologist, because cough can strongly and negatively affect patients’ quality of life. By definition, cough represents a significant defensive reflex mechanism by which secretions and foreign bodies are removed from the tracheobronchial tree through explosive expiration. Cough has several functions. Most often, it is an indicator of an existing disease, but also an important defensive mechanism for “cleaning” the airways. However, if it becomes ineffective, excessive, or persistent, it can greatly and adversely affect patients’ quality of life and lead to complications.

[0010] Influenza is an acute respiratory disease in humans caused by influenza viruses type A and type B. Based on the surface antigens hemagglutinin (H) and neuraminidase (N), further classification of influenza type A into subtypes has been made. Over the past four decades, in addition to influenza type B, the H3N2 and H1N1 subtypes of influenza A are mostly encountered. Influenza viruses belong to highly variable viruses, and the result of these changes is a new antigenic variant of the virus, which can cause an epidemic in the population. Influenza epidemics occur suddenly, usually in winter, and last for several weeks. Unlike the common cold, the flu has a very pronounced seasonal character. Seasonal flu occurs suddenly and is always accompanied by high fever, chills, headache, muscle and joint pains, a sense of fatigue and exhaustion, and a dry, unpleasant cough. Unlike the common cold, nasal congestion (stuffy nose) and sneezing occur less frequently in influenza. Additionally, the common cold usually does not lead to serious health problems, while influenza can cause pneumonia, bronchitis, sinusitis, and other serious respiratory complications. In individuals over 65 years of age, influenza is associated with high rates of hospitalization and mortality.

[0011] The therapy applied so far for all acute respiratory viral infections involves so-called symptomatic therapy, that is, therapy that will relieve the present symptoms. Primarily, these are medicines against elevated body temperature and pain (antipyretics - analgesics), as well as medicines for relieving cough or facilitating expectoration. The development of a vaccine has also proven to be very demanding, due to the large number of rapidly mutating viral agents, which complicate the whole process. The most important preventive measures for preventing acute respiratory diseases are in the domain of maintaining personal hygiene measures and improving human immunity.

[0012] Antiviral agents, such as vaccines, drugs, and virucides, help reduce virus transmission. Although vaccines are an effective weapon against viral infection, it is not feasible to develop a vaccine against all enteroviruses. In addition, the process of developing and approving a vaccine also requires time. Therefore, there is a great need to find broad-spectrum antiviral agents that would reduce the infectivity of viruses and could complement vaccines and drugs in the fight against viruses.

[0013] Today, medicinal plants play an important role in the prevention and treatment of viral infections. They are increasingly being studied for their potential benefits in the fight against various diseases, including viral infections. Namely, medicinal herbs can act through different mechanisms, including direct antiviral activity, strengthening the immune system, or reducing inflammation. Compared to standard drugs used in the treatment of viral infections, herbal preparations and medicinal plants are cheaper, more accessible, and culturally more acceptable. Herbal preparations can stimulate or modulate the immune system, helping the body fight infections more effectively.

[0014] Herbal preparations are a rich source of bioactive compounds. Out of 1,881 approved drugs from the beginning of January 1981 to the end of September 2019, a total of 41.8% are either biological macromolecules, unmodified natural products, herbal medicines, or derivatives of natural products. If synthetic products that mimic natural compounds are also considered, the share increases to 64.3% (Nevman and Gragg, 2020). It has been reported that various natural products exhibit antiviral activity, and they are an interesting source of new antiviral drugs due to their availability, tolerability, and expected low side effects (Kumar and Pandei, 2013; Goh et al., 2020). For example, flavonoids are a diverse group of plant secondary metabolites known for their antioxidant, anti-inflammatory, anticancer, and other therapeutic properties (Kumar and Pandei, 2013; Panche et al., 2016). Although the mechanism of antiviral action often remains unknown, it is reported that natural products interact with the viral life cycle or target viral entry, replication, assembly, or release (Lin et al., 2014; Linnakoski et al., 2018).

[0015] There are various herbal preparations containing plant extracts that are used in the prevention and / or treatment of symptoms of acute respiratory infection. One of the preparations is described in patent application WO 2007 / 083123, where the purpose of the invention is the use of elderberry (Sambucus nigra) extract in the fight against the influenza virus NIBRG-16 (H5N1). Compared to the present invention, the key difference is precisely in the content of the herbal preparation and the amount of elderberry extract, which in this invention is 380 mg of dry elderberry fruit extract and, in addition to elderberry, also contains extracts of pelargonium root, white willow bark, elderberry fruit, acerola, and rosehip, with the addition of vitamin D, zinc, and copper, which enhancing the action and effectiveness of the herbal preparation itself in the prevention and / or treatment of symptoms of acute respiratory infection.

[0016] Considering the above, it can be seen that there is still a need for the development of herbal preparations that are safer, more effective, and easier to use.

[0017] A SUMMARY OF THE INVENTION

[0018] It has been found that a herbal preparation containing material in the form of plant extracts (pelargonium root, white willow bark, elderberry fruit, acerola, and rosehip) with the addition of vitamin D, zinc, and copper simultaneously acts on the cause of cold and flu, as well as on the symptoms of inflammatory processes of the upper respiratory tract such as cough, sore throat, and weakened immunity. Due to this synergy, the amount of active components required to achieve the desired pharmacological effect is such that it manages to address both the cause and the symptoms, acting analgesically and antivirally, making the herbal preparation easy to use and providing a unique therapy based on natural ingredients.

[0019] DETAILED DESCRIPTION OF THE INVENTION

[0020] The present invention provides a herbal preparation which contains as active components pelargonium root (Pelargonium sidoides), white willow bark (Salix cortex), elderberry fruit (Sambucus nigra), acerola (Malpighia punicifolia L.), rosehip (Rosa canina), vitamin D, zinc, and copper. The herbal preparation itself can be in the form of oral preparations, in liquid and semi-solid forms, such as concentrate, drops, syrup, emulsion, suspension, powder, capsule, tablet, lozenge, pastille, spray, which is administered to children and adults with the first symptoms of a cold. As used herein, “effective amount” refers to the amount of the given substance or active component that is effective to provide relief of symptoms caused by the innate immune response when administered over a certain period of time according with predetermined dosing regimens.

[0021] Pelargonium (Pelargonium sidoides) is a medicinal evergreen plant originating from South Africa. It belongs to traditional medicinal plants that have been used for centuries for colds and influenza. The medicinal part of the plant is the root, from which an extract is commonly obtained and used to relief symptoms of bronchitis, acute rhinosinusitis, colds, and to stimulate the immune system. The extract itself can neutralize certain types of bacteria and viruses. Pelargonium extract contains several bioactive components that contribute to its medicinal properties, including flavonoids, coumarin, phenolic acids, and purine, which exhibit antiviral, antibacterial, and antioxidant activity, as well as beneficial effects on the immune system.

[0022] Pharmacological studies suggest that the mechanism of action of Pelargonium is multifactorial, i.e., it acts cytoprotectively against virus-induced cell destruction and also increases the release of antimicrobial peptides, known as defensins, from neutrophilic granulocytes, which improves the body’s ability to fight infections. It can directly inhibit the growth of bacteria and viruses by preventing pathogens from binding to host cells, making it more difficult for bacteria and viruses to colonize and infect the respiratory tract. Its bioactive components can interfere with viral replication, which helps reduce viral load. It has also been found to act as an immunostimulant. These actions are mainly mediated by the release of tumor necrosis factor (TNF-α) and nitric oxide, stimulation of interferon-β synthesis, and increased natural killer cell activity. Pelargonium extract modulates the production of secretory immunoglobulin A in saliva, interleukin-15 (IL-15) and interleukin-6 (IL-6) in serum, and interleukin-15 in nasal mucosa, such that immunoglobulin A levels are increased while IL-15 and IL-6 levels are decreased. In view of this, it can be seen that the mentioned plant can exert a strong modulatory effect on the immune response associated with the mucosa of the upper respiratory tract.

[0023] Pelargonium extract has been shown to be effective in fighting viruses by inhibiting an early stage of influenza infection through weakening the virus. It is known that hemagglutinin from the virus is a protein spike on the surface of the virus. It is the key of the virus that penetrates the cell. Once inside, the viral genetic material penetrates the cell nucleus and turns it into a factory for thousands of new viral clones. Using Pelargonium, it has been observed that it weakens viral hemagglutination as well as neuraminidase activity, reducing the risk of bacterial superinfection, enabling faster functional recovery, and decreasing the use of other drugs such as paracetamol or antibiotics. The antiviral effect of Pelargonium is also associated with interferon 9 production, although a recent study highlighted a direct antiviral effect on several viruses (influenza, parainfluenza, respiratory syncytial virus, rhinoviruses, coxsackieviruses, and coronaviruses).

[0024] Considering the above, it can be seen that Pelargonium is an effective herbal preparation for the treatment of symptoms of respiratory infections. Its antimicrobial, immunomodulatory, and mucolytic effects make it useful for reducing symptoms and accelerating recovery in colds, bronchitis, and other respiratory infections.

[0025] According to the present invention, an extract of Pelargonium sidoides, DER 3-7:1 or DER 4-25:1, was used. The effective amount ranges from 14.00 mg to 85.0 mg of Pelargonium root extract if the DER 3-7:1 extract is used, or from 4.0 mg to 35.0 mg if the DER 4-25:1 extract is used.

[0026] White willow (Salix alba) is a perennial woody plant, and its herbal drug is obtained from the bark (Salicis cortex). Its main ingredients, in concentrations of 1-11%, are phenolcarboxylic acid heterosides (salicin, populin, and alicortin), flavonoid heterosides, and oligomeric proanthocyanidins. The most interesting and most frequently used component is salicin, which gradually hydrolyzes in the digestive tract, releasing sallicyl alcohol, which further oxidized into the active pharmacological form, salicylic acid, which has anti-inflammatory, antiviral, and antirheumatic effects. Salicin from white willow inhibits cyclooxygenase- 1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes, which are key for the production of prostaglandins, substances that cause pain and inflammation. It reduces the production of proinflammatory cytokines and other inflammatory mediators, decreasing inflammation in tissues, and also acts on the temperature regulation center in the hypothalamus, helping to reduce elevated body temperature.

[0027] According to the present invention, an extract of Salicis cortex, DER 25:1, standardized to 25% salicin, was used. The effective amount ranges from 95.00 mg to 105.00 mg of dry white willow bark extract, i.e., from 20.00 mg to 30.00 mg of salicin.

[0028] Elderberry, black elder (Sambucus nigra), is a shrub or low tree originating from Europe and North America, whose lifespan is up to about 60 years. In Central European countries, it is cultivated as a fruit. It grows in bright and warm places, around settlements and along roads. The bark is gray-brown and cracked, while the young green branches have oval buds. Elderberry is a hermaphroditic plant, meaning that male and female flowers are found on the same inflorescence. The medicinal properties are shown by the flower, fruit, and root. The flower contains B-group vitamins and vitamin C, as well as minerals iron and selenium, and essential oil whose most important active component is sambunigrin. The fruit is a berry, shiny dark red-purple to black in color, which can be used after cooking. It has been shown to contain flavonoid heterosides (rutin, isoquercetin, and hyperoside), 3% tannins, 15% anthocyanidins (sambucin, sambucianin, chrysanthemin), as well as traces of essential oil. It is rich in sugars, fruit acids, and vitamin C. Traditionally, it is used to alleviate early symptoms of colds and to strengthen immunity. It is used as a warm, sweetened drink, infusion, or in the form of liquid dosed products. Elderberry contributes to immune system function by reducing the duration and severity of cold and flu symptoms, including cough, sore throat, and nasal congestion. It can also relief symptoms such as fever and muscle pain associated with flu. Regular consumption of black elder may improve overall immune system health and reduce the frequency of respiratory infections.

[0029] Elderberry berries describe its potential mechanisms of action. It has been reported that elderberry berries “modulate inflammatory cytokines IL-1 and TNF-alpha in vitro, increase the secretion of human basophils IL-4, IL-13, and histamine, inhibit the release of proinflammatory cytokines from macrophages, and contain flavonoids reported to possess antioxidant activity.” It has been identified that elderberry solution stimulates cells to release certain cytokines, which are chemical messengers that the immune system uses to communicate between different types of cells to coordinate a more efficient response against an invasive pathogen. The antiviral activity of elderberry can also be attributed to its anthocyanidin compounds - phytonutrients responsible for giving the fruit its vivid purple color. These phytochemicals have been shown to be effective in stopping viruses that infect cells and in suppressing viral spread in the later stages of the flu cycle when cells have already been infected. Elderberry has been found to contain a flavonoid called cyanidin-3- sambubioside that acts as a neuraminidase inhibitor. A neuraminidase inhibitor is any molecule that can inhibit the production of the viral neuraminidase enzyme. Viruses such as coronaviruses use the neuraminidase enzyme to replicate in the human body, and its inhibition can stop the infection.

[0030] According to the present invention, an extract of Sambucus nigra, DER 10:1, was used, and extracts DER 30-50:1 or DER 20-40:1 may also be used. Standardized to more than 9% polyphenols. The effective amount ranges from 370.00 mg to 1140.00 mg of dry black elderberry fruit extract with a DER 10:1 ratio. If a dry extract with a DER 30-50:1 ratio is used, the effective amount ranges from 70.00 mg to 225.00 mg, and for a dry extract DER 20-40:1 , the effective amount is 90.00 mg to 285.00 mg.

[0031] Acerola, Barbados cherry (Malpighia punicifolia L.), is a wild tropical shrub that grows in South Mexico and Central America. Today, it is also cultivated in slightly more northern areas, such as Texas in the USA. The fruit is bright red in color and visually resembles the fruit of a cherry. These fruits are known as very rich sources of vitamin C, which is absorbed significantly better than the synthetic form of vitamin C. Acerola fruit can contain 3.00 to 46.00 g of vitamin C per kilogram of pulp, making it one of the most important natural sources of vitamin C. It contains up to 20 times more vitamin C than a lemon. Acerola fruit is also rich in other vitamins (A and B vitamins), antioxidant substances such as carotenoids and polyphenols (biflavonoids), and minerals such as calcium, iron, magnesium, phosphorus, copper, sodium, zinc, and selenium. It is considered a powerful antioxidant. In traditional medicine, acerola fruit is used for the treatment of dysentery, diarrhea, anemia, urinary infections, liver diseases, sore throat, flu, and colds. Acerola, as a natural source of vitamin C, contributes to increased production of white blood cells, which are key in fighting infections. Also, the antioxidant properties of the vitamin C present in acerola help neutralize free radicals and maintain healthy tissues.

[0032] According to the present invention, the effective amount is 200.00 mg of dry acerola fruit extract, standardized to 25% vitamin C, i.e., 50.00 mg of natural vitamin C.

[0033] Rosehip (Rosa canina) is a widely distributed polymorphic plant. The genus Rosa (roses) contains 120 to 6,000 plant species that are distributed throughted the northern hemisphere. Wild rose is a deciduous shrub reaching a height of 2-3 m with branches covered in thorns. Its pseudo-fruit is an aggregate nut of orange-red color, which ripens in September or October and is called Rosehip (hip, wild hip). The ripe fruit is most commonly used in the food industry to obtain exceptionally tasty marmalade. The use of Rosa species plants in medicine in Europe dates back to around 500 BCE, as its fruit contains various bioactive substances. The most important are vitamin C, carotenoids, vitamin K and B-complex vitamins, flavonoid heterosides, fruit acids, sugars, pectins, minerals, and tannins. Rosehip represents a significant natural source of vitamin C. Dried rosehip is used for making teas, as a stimulant and tonic, and as a potential diuretic. Raw rosehip fruit is used in the food industry. Traditionally, in folk medicine, rosehip is used preventively for colds, flu, and infectious diseases. Vitamin C and other antioxidants in rosehip help neutralize free radicals, reducing oxidative stress and cell damage, which may help prevent chronic diseases and slow the aging process. Also, vitamin C from rosehip helps improve immune system function, which can help increase resistance to respiratory infections and colds.

[0034] According to the present invention, the effective amount is 143.00 mg of dry rosehip fruit extract, standardized to 70% vitamin C, i.e. , 100.00 mg of natural vitamin C. Zinc is an essential trace element that is part of more than 70 different enzymatic systems in the body. It is particularly important for immunity and the synthesis of DNA and RNA. It has an immunomodulatory role, acts protectively on the macula, and act as an antiviral and antioxidant within the superoxide dismutase enzyme system.

[0035] According to the present invention, the effective amount ranges from 5.00 mg to 15.00 mg of zinc, and zinc gluconate is used as the source of zinc.

[0036] Copper is an essential trace element that is included in the compositioin of a large number of enzymes and proteins, within which it plays a role in cellular respiration, melanin synthesis, connective tissue formation, and protection of cells from the effects of free radicals. It is also important for collagen formation, maturation of erythrocytes and leukocytes, glucose and cholesterol metabolism, immune functions, and bone health.

[0037] According to the present invention, the effective amount is 1,000.00 μg of copper, and copper gluconate is used as the source of copper.

[0038] Vitamin D belongs to the group of liposoluble vitamins, the most important of which are vitamin D2 - ergocalciferol and vitamin D3 - cholecalciferol. In the present invention, vitamin D3 is used. It is an essential vitamin substance that plays a key role in various biological processes and is important for maintaining health and preventing various health problems. It plays an important role in regulating the immune system and inflammatory processes by helping the body defend against infections and inflammation and may support the function of immune cells such as T-lymphocytes.

[0039] According to the present invention, the effective amount is 10.00 μg of vitamin D.

[0040] The combination of plant extracts according to the present invention has a synergistic effect, which means that in combination they have a stronger and better effect than when taken separately. Accordingly, the herbal preparation according to the present invention, due to the synergistic effect of the herbal extracts, has surprising efficacy against acute respiratory infections, such as cough, sore throat, and inflammatory processes of the upper respiratory tract. The herbal preparation according to the present invention, depending on its form and whether it is administered to children or adults, i.e., whether it is in the form of a concentrate, drops, syrup, emulsion, suspension, powder, capsule, tablet, lozenge, pastille, or spray, can be administered once daily, twice daily, or four times daily at the first symptoms of a cold. For example, when it is a syrup, it is administered to children once daily at 5 ml, while for adults it is administered twice daily at 7.5 ml. Capsules are administered to children over 12 years once daily at 1 capsule, while for adults they are administered twice daily at 1 capsule. Lozenges are administered to adults four times daily at 1 lozenge. When the herbal preparation is in powder form, it is administered to adults twice daily at 1 sachet.

Claims

Patent claims1. The herbal preparation consisting of plant material, characterized in that it contains herbal extracts, vitamin D, zinc, and copper.

2. The herbal preparation according to claim 1 , characterized in that the plant extracts consist of Pelargonium sidoides root, white willow bark (Salix cortex), black elderberry fruit (Sambucus nigra), Acerola (Malpighia punicifolia L.), and rosehip (Rosa canina).

3. The herbal preparation according to claim 1 or 2, characterized in that acerola and rosehip fruit are used as a natural source of vitamin C, in an amount of 50.00 mg to 100.00 mg of natural vitamin C.

4. The herbal preparation according to claim 2, characterized in that the amount of Pelargonium root is from 14.00 mg to 85.0 mg of Pelargonium root extract if a DER 3-7:1 extract is used, and from 4.0 mg to 35.0 mg if a DER 4-25:1 extract is used.

5. The herbal preparation according to claim 2, characterized in that the amount of white willow bark is from 95.00 mg to 105.00 mg of dry bark extract.

6. The herbal preparation according to claim 2, characterized in that the amount of blackberry fruit is from 370.00 mg to 1,140.00 mg of dry fruit extract if a DER 10:1 extract is used, from 70.00 mg to 225.00 mg if a DER 30-50:1 extract is used, and from 90.00 mg to 285.00 mg if a DER 20-40:1 extract is used.

7. The herbal preparation for use in the treatment and / or prevention of cold and flu symptoms.

8. The herbal preparation according to claim 7, characterized in that it is administered as an oral formulation.

9. The herbal preparation according to any of claims 7 to 8, characterized in that it is in the form of a concentrate, drops, syrup, emulsion, suspension, powder, capsule, tablet, lozenge, pastille, or spray.

10. The herbal preparation according to any of claims 7 to 9, characterized in that the preparation is administered orally once, twice, or four times daily at the first symptoms of a cold.