CAPSAICINOIDS AND USES THEREOF AS MEDICAMENTS

20170239198 ยท 2017-08-24

    Inventors

    Cpc classification

    International classification

    Abstract

    The present invention is directed towards a medicament comprising a capsaicinoid possessing antiviral activity and useful in the treatment of viral infections and in the treatment of HIV/AIDS. The medicament also possesses neuroplasticity-enhancing activity and is useful in the treatment of stress and other psychological conditions. Further, the medicament possesses anti-inflammatory activity and is useful in the treatment of arthritis. The medicament has also been shown to possess antibacterial activity.

    Claims

    1-12. (canceled)

    13. A medicament comprising a capsaicinoid possessing antiviral activity, when used in the treatment of viral infections and in the treatment of HIV/AIDS, characterised in that the medicament is consumed orally.

    14. A medicament according to claim 13, characterised in that the medicament possesses neuroplasticity-enhancing activity, and is useful in the treatment of stress and other psychological conditions.

    15. A medicament according to claim 13, characterised in that the medicament possesses anti-inflammatory activity, and is useful in the treatment of arthritis.

    16. A medicament according to claim 13, characterised in that the capsaicinoid is capsaicin.

    17. A medicament according to claim 16, characterised in that a source of the capsaicin is Capsicum annuum Bird's Eye.

    18. A medicament according to claim 13, characterised in that the medicament possesses wound healing, anti-fungal, antibacterial, pain relief, cellular regeneration, metabolic enhancement and skin condition activity as well as immune system activity by acting as an immuno-activator.

    19. A medicament according to claim 13, characterised in that the medicament is useful in the treatment of malaria, stomach ulcers, tuberculosis, bronchitis, constipation and eczema.

    20. A treatment comprising the use of the medicament of claim 13, characterised in that a dose of the medicament is 550 mg.

    21. A treatment according to claim 20, characterised in that the dose of the medicament comprises consumption of one capsule.

    22. A treatment according to claim 20, characterised in that a dosage regimen comprises one dose per day.

    23. A treatment according to claim 20, characterised in that the dose is consumed during a meal.

    24. A treatment according to claim 20, characterised in that the dosage regimen may be 90 days in length.

    Description

    DESCRIPTION OF PREFERRED EMBODIMENTS

    [0025] The present invention relates to a medicament comprising a capsaicinoid. The medicament possesses antiviral activity and is useful in the treatment of viral infections and in the treatment of HIV/AIDS. The medicament of the present invention exerts a strong antiviral activity on human immunodeficiency virus (HIV). The activity of the medicament results in a dramatic increase in the CD4 count of HIV infected patients, either in conjunction with its antiviral activity, or as a result of their activity against the virus.

    [0026] Moreover, the medicament of the present invention possesses neuroplasticity-enhancing activity and is useful in the treatment of stress and other psychological conditions. Due to the capability of the hippocampus in suppressing stress response and even independently generating responses, the present medicament has been found to be effective in influencing one's stress perception by enhancing the ability of the hippocampus to suppress stress response. Neuropeptide Y, a protein synthesised in the hypothalamus, acts as a chemical messenger in the brain and is implicated in anxiety and stress, specifically, stress resilience. The present medicament acts on the hypothalamus to enhance stimulation for the abundant production of Neuropeptide Y protein thereby enhancing stress resilience.

    [0027] The present medicament effectively enhances neuroplasticity greatly. It has been advantageously found that when good concentration levels of capsaicinoids (those of the present invention) in the body are maintained, the result is that neuroplasticity and neurogenesis is greatly improved. The creation of new pathways for the purpose of re-establishing lost functionality is also speeded up and enhanced. The rejuvenating effects of capsaicin on the central nervous system is unprecedented.

    [0028] Additionally, the release of the messenger cortisol by the adrenal gland into the bloodstream is for the purpose of instructing the body to redistribute energy to areas where it is needed most as the body deals with a stressor or stressors. The medicament of the present invention works to improve the efficiency of the body's metabolism, mainly because of its anti-inflammatory effect which greatly reduces stress (which may be caused by chronic inflammation). There are threshold levels of capsaicinoids that need to be in the bloodstream to achieve this. The present medicament achieves or exceeds those levels.

    [0029] The medicament also possesses anti-inflammatory activity and is useful in the treatment of arthritis.

    [0030] The capsaicinoid is obtained from their natural source, being the fruit of the Capsicum genus of plants, for example chillies. In accordance with a preferred embodiment of the present invention, bird's eye chillies (100,000 SHU) are used. The relative low cost of bird's eye chillies results in the added advantage of a relatively inexpensive method of treatment.

    [0031] The preferred capsaicinoid of the medicament of the present invention is capsaicin, the chemical structure of which is shown below.

    ##STR00001##

    [0032] The chillies are ground into a very fine powder and are then encapsulated for ingestion, in order to avoid contact with the mouth during ingestion. Preferably, each capsule is as small as is conveniently possible for manufacture. The small size of the capsule results in achieving the required amount of capsaicin to be administered, by varying the number of capsules ingested at each dosage point. It has been found that wider distribution in the stomach upon ingestion is achieved with a higher number of a smaller sized capsule. In turn, it has been found that this ensures a wider distribution of the active substance.

    [0033] Following ingestion of the capsules, levels of capsaicin and/or other capsaicinoids in the bloodstream are found to be raised and those raised levels are sustained. The sustained levels of blood capsaicinoids are preferably those that are optimum for the antiviral or other therapeutic treatment according to the present invention.

    [0034] The present medicament has been found to result in unprecedented relief and even recovery to patients infected with HIV. Patient trials have demonstrated that most participants who underwent this therapy tested negative for HIV after taking the medicament for a period of between three months and twelve months. Cases where patients' have gained an increase in CD4 count in excess of 400 cells/mm.sup.3, in just one month, have been recorded.

    [0035] It is well known that capsaicin binds to the TRPV1 receptor, resulting in the signalling of heat and pain to the brain. This signalling is a result of merely the activation of TRPV1 and not any physical damage to cells. However, the sensation and discomfort that results, requires management for patients receiving capsaicinoid therapy.

    [0036] The medicament of the present invention is preferably never consumed on an empty stomach. It is preferred that the medicament never be consumed without a meal, including not even shortly following a meal. More preferably, the medicament of the present invention is consumed at substantially the same time as a full meal. Most preferably, the medicament is consumed at approximately one quarter of the way through consumption of the full meal. In a preferred embodiment of the present invention, the full meal is an evening meal as drowsiness may occur, although the dosage may be consumed at any time of the day.

    [0037] In use, each capsule preferably comprises 550 mg of finely ground bird's eye chillies. For the treatment of patients, one dose comprises one capsule. Each dose is taken with a meal once every day for 90 days. Preferably, the outer of the capsule disintegrates or dissolves at least 90 minutes following ingestion, allowing the contents of the capsule to be released in the lower parts of the stomach for easier management of the chilli heat.

    [0038] In a preferred embodiment of the present invention, a minimum of 500 ml of water (preferably lukewarm, or according to a patient's preference), is consumed early each morning. This assists in both keeping hydrated and avoiding overly dry mucous membranes of the digestive tract. Greater volumes, above 500 ml, provide better effects.

    [0039] After the 90 day regimen, the patient undergoes testing for the presence of their condition in a manner which would be understood by the skilled person. If a positive result is obtained, the same dosage regimen is continued. The patient undergoes similar testing every 30 days thereafter until a negative result is obtained.

    [0040] It is preferred that, as large amounts of chillies are not harmful, patients continue taking the present medicament, even after testing negative for their condition. The continuing dosage may comprise a reduced quantity and frequency of capsules.

    [0041] Other embodiment medicaments are also contemplated in accordance with the present invention. For instance, the aforementioned encapsulating of the plant material may, instead of forming a capsule, be provided as a coated table or, in fact, any method suited to the relevant function of providing a vehicle for delivery of the active ingredient while preventing discomfort to the patient. Likewise, instead of capsaicin, any suitable capsaicinoid, such as for example, dihydrocapsaicin or Nonivamide, to provide a favourable result, may be used. Both the size and volume of the capsule and the amount, frequency and length of the dosage regimen may be varied according to the optimal needs for the patient and the treatment. Further, while the preferred embodiment of the present medicament comprises bird's eye chillies, any appropriate source of capsaicinoid, which provides the desired treatment effect, may be used. It has been found that the higher the SHU rating of the capsaicinoid source (for example, a chilli with a higher SHU rating that bird's eye chillies), the greater effect achieved.

    [0042] Modifications and variations as would be apparent to a skilled addressee are deemed to be within the scope of the present invention.