CROSS REFERENCE TO RELATED APPLICATIONS

This application is the US National Phase of and claims the benefit of and priority on International Application No. PCT/BR2019/050040 having a filing date of 11 Feb. 2019, which claims priority on and the benefit of Brazilian Patent Application No. 102018002843-0 having a filing date of 9 Feb. 2018.

FIELD OF THE INVENTION

The present invention discloses a composition and its use as a medicament for the treatment of neurological disorders to be administered preferably in humans and can also be used for treating animals. The present invention is in the field of Pharmacy and Medicine.

BACKGROUND OF THE INVENTION

Parkinson's disease is a chronic, progressive disease affecting one in every thousand people and directly affecting the patients' life quality. It is a pathology resulting from the death of dopamine-producing neurons from the substantia nigra, having an idiopathic etiology. It is believed its appearance comes from environmental and genetic factors, being able to interact and contribute to the development of neurodegeneration.

When signs and symptoms are detected, the loss of approximately 60% dopaminergic neurons has probably already occurred, and the dopamine content in the striatum is already about 80% lower than normal. Given this, the development of drugs and more in-depth research for the treatment of Parkinson's disease are relevant

The main symptoms of this disease are slowness, stiffness, resistance to passive movement, difficulty in postural balance and tremor. In advanced stages, dementia, cognitive impairment, and extension of the brain morbid process can occur. The treatments available on the market treat the symptoms, but do not change the degenerative process. Over time, as the patient's clinical condition worsens, there is greater difficulty in controlling symptoms.

The main drugs currently indicated for Parkinson's disease are: triexiphenidyl hydrochloride, levodopa+benserazide hydrochloride, rasagiline mesylate, levodopa+carbidopa, among others.

Cannabidiol has shown to be a promising alternative for several neurological disorders, highly effective and devoid of psychotoxicity and other side effects. The neuroprotective action proposed in this invention, which slows down the progression of Parkinson's disease and other neurological diseases and minimizes the worsening of the patient's clinical condition, decreasing the extent of the morbid process related to the dopaminergic system to other brain areas, being unprecedented.

In the last 10 years there has been a notable increase in scientific publications on Cannabidiol, mainly stimulated by the discovery of its anti-inflammatory, antioxidative and neuroprotective effects. These studies have suggested a wide range of possible therapeutic effects of the asset in various therapeutic indications.

There are data from preclinical studies that used the striatal lesion model of rats with the 6-hydroxy dopamine toxin and the active decreased the degeneration of dopaminergic neurons and the activation of microglial cells. However, the mechanisms responsible for these effects are not elucidated.

Considering there are not enough pre-clinical studies to characterize the therapeutic potential of Cannabidiol in the treatment of Parkinson's disease, nor the pharmaceutical formulation for such indication, the present invention goes beyond these generic and preliminary teachings, describing and proving the feasibility of formulation of such indication.

Functional motor analysis and comorbidities usually accompanying Parkinson's disease need to be proven with synthetic Cannabidiol, Cannabidiol of plant origin and/or association.

In the search for the state of the art in scientific and patent literature, the following documents dealing with the subject matter were found:

The document WO 2009/020666, entitled “ORAL CANNABINOID LIQUID FORMULATIONS AND METHODS OF TREATMENT”, discloses a liquid oral composition of cannabinoids, wherein the solvent is aqueous, and has a more efficient in vivo absorption profile than commercial gelatin capsules.

The document U.S. Pat. No. 7,025,992, entitled “Pharmaceutical formulations”, discloses a formulation of powder cannabinoids, which when hydrated, has its absorption facilitated by means of an emulsifier.

The document WO 2015/068052, entitled “TERPENE AND CANNABINOID FORMULATIONS”, discloses liposomes comprising cannabinoids and terpenes.

The document BR 10 2015 024165 8, entitled “ORAL PHARMACEUTICAL COMPOSITION UNDERSTANDING CANABINOID, PROCESS FOR ITS PREPARATION AND USE”, discloses an oral pharmaceutical composition comprising cannabinoids, a process for its preparation and use.

Thus, what depends on the researched literature, no documents were found anticipating or suggesting the teachings of the present invention, so that the formulation proposed herein has novelty and inventive activity in view of the state of the art.

Briefly, there are noted several formulations for the treatment of neurological disorders.

SUMMARY OF THE INVENTION

Thus, the present invention describes two new formulations comprising cannabidiol (CBD) of synthetic and vegetal origin, respectively, and which has surprising neuroprotective activity, as well as for the treatment of several neurological disorders.

In a first object, the present invention discloses a pharmaceutical composition containing the active ingredient Cannabidiol of synthetic origin, and with: up to 0.06% cannabinol, up to 0.06% Delta-8-tetrahydrocannabinol, up to 0.06% Delta-9-tetrahydrocannabinol, up to 0.06% cannabidiolic acid methyl ester, up to 0.06% menthadienol and up to 0.06% methyl olivetolate.

In a second object, the present invention discloses an excipient for composition comprising oil of vegetable, animal or mineral origin or a combination thereof.

In a third object, the present invention discloses the use of the pharmaceutical composition with neuroprotective action.

In a fourth aspect, the present invention discloses the use of the pharmaceutical composition for the preparation of a medicament for the treatment of neurological disorders.

These and other objects of the invention will be immediately appreciated by those skilled in the art and will be described in detail below.

