EP3645119A1

EP3645119A1 - Veterinary granules composition containing hemp extract

Info

Publication number: EP3645119A1
Application number: EP18746743.6A
Authority: EP
Inventors: Miriam HALPERIN WERNLI; Jorge WERNLI; Gian Batista TREPP; Silvia Huber; Franco MADEA
Original assignee: Creso Pharma Switzerland GmbH
Current assignee: Creso Pharma Switzerland GmbH
Priority date: 2017-06-30
Filing date: 2018-06-25
Publication date: 2020-05-06
Also published as: WO2019002933A1; CO2020000111A2; MX2019015673A; BR112019026635A2

Abstract

Cette invention concerne des compositions vétérinaires ou des compléments diététiques ou alimentaires utiles dans la prévention ou le traitement des troubles du comportement, respectivement liés à l'âge, et de la douleur chez les mammifères. Ils sont également destinés à soutenir ou à renforcer le système immunitaire, le bilan comportemental des mammifères et à soutenir la réponse inflammatoire naturelle. Ces compositions ou compléments se présentent sous la forme de granulés hydrosolubles à base de polysaccharides qui contiennent à titre de source de cannabinoïdes une huile normalisée ou un extrait de chanvre (Cannabis sativa L.) sensiblement dépourvu de substances psychotropes.This invention relates to veterinary compositions or dietary or dietary supplements useful in the prevention or treatment of age-related behavioral disorders and mammalian pain. They are also intended to support or strengthen the immune system, the behavioral balance of mammals and to support the natural inflammatory response. These compositions or supplements are in the form of water-soluble granules based on polysaccharides which contain as a source of cannabinoids a standardized oil or hemp extract (Cannabis sativa L.) substantially free of psychotropic substances.

Description

Veterinary granules composition containing hemp extract

The invention pertains to veterinary compositions or dietary or feed supplements for use in the prevention or the treatment of behavioral, respectively age-related disorders or troubles in mammals, or for supporting or strengthening the immune system, the behavioral balance of mammals and for supporting the natural inflammatory response of mammals, in particular of companion animals.

Background of the invention

There exist already a few veterinary products comprising cannabinoids and which have been proposed for preventing or treating behavioral troubles affecting pets or companion animals, mainly dogs, cats and horses.

They are provided in various forms like treats, croquettes or biscuits comprising hemp or cannabis plant material intimately mixed with a suitable carrier. Although the relevant plant material can be controlled more or less efficiently in terms of concentration of active substances, i.e. the cannabinoids, administration of same can be problematic if dosage is not duly monitored.

This is particularly true if minor quantities of psychotropic substances like e.g. THC or are still present: THC toxicity can be serious and prevent the pet from standing and eating , so overdosage can be counterproductive if not dangerous.

There also exist veterinary compositions making use of hemp or cannabis oils or extracts used as the source of cannabinoids wherein the amount of active substances is easier to control. Such compositions are frequently provided in their liquid, in particular oily form or as capsules which, however, necessitates a very cautious administration.

For instance, a few more drops only per body weight, can lead to undesired effects due to their high concentration of cannabinoids and namely psychotropic THC even when the latter is only present as traces. In that context too, THC toxicity can be serious and prevent the pet from standing and eating.

Oils or capsules do not dissolve in the pet mouth and consequently are furthermore subject to significant liver first-pass metabolism as the oral bioavailability of cannabinoids is below In certain cases, an adequate mixing to the pet diet is also of concern, especially when off flavors are too intense and then cause rejection of the diet provided to the pet.

There is today an imperious need to obviate and to overcome efficiently all the above-mentioned drawbacks when providing to the pets in need thereof new and easily absorbed veterinary compositions comprising hemp extracts. This goal is achieved by means of the invention defined below.

The invention

The composition according to the invention consist in a veterinary composition or dietary supplement or complementary feed which is in the form of water soluble polysaccharide-based granules comprising as the source of cannabinoids as a standardized oil or a standardized extract of hemp (Cannabis sativa L.) essentially devoid of psychotropic substances.

The latter is designed for a wide scope of uses and in particular in:

- the prevention or the treatment of behavioral disorders or troubles in mammals

- the prevention or the treatment of age related disorders or troubles in mammals

- supporting or strengthening the behavioral balance of mammals

- the prevention or the treatment of pain or inflammation in mammals

- supporting and strengthening the immune system and the natural anti-inflammatory response in mammals

and even more, in fact almost any troubles and disorders that can be therapeutically addressed in animals by means of the administration of cannabis- or hemp derived extracts with non-psychotropic cannabinoids and terpenes.

Definitions

The term "mammals" define here companion animals like dogs, cats, horses, donkeys and mules and camels or zoo animals where behavioral disorders like anxiety, stress or seizures are frequently of concern.

The term "granules" defines here edible particles in their granulated form, e.g. such as spherical or similar particles consisting essentially of a water soluble biodegradable matrix containing the selected active substances, wherein the cannabinoids providing from hemp or cannabis extract are dispersed inside or sprayed or coated on the surface. In certain cases, these granules can further comprise additives like stabilizers, binding or disintegrating agents or even flavors. The granules of the invention can be prepared according to the techniques conventional in the art such as extrusion, nebulization or fluid-bed granulation. The term "polysaccharides" defines substances commonly used in veterinary or human medicine as carriers and more particularly water-soluble polysaccharides selected among starch, soluble starch, microcrystalline cellulose, dextrin, dextrose, sucrose, isomaltose, oligosaccharides such as fructo-oligosaccharides (FOS) or gluco-oligosaccharides (GOS), mixtures of same and any other water-soluble representatives of this class of compounds. This enumeration, however, is not limitative.

The term "essentially devoid of" defines here cannabis or hemp (Cannabis sativa L.) oils or extracts wherein the content of psychotropic substances, namely THC is significantly below the applicable regulatory provisions according to EFSA and EU regulatory bodies

recommendation to be equal to or lower than 10 ppm (mg per kg), usually below 0.2 % if not below 0.05 % (weight). Some of such oils or extracts are commercially available whereas others can be obtained when subjecting the adequate raw plant material i.e. buds, leaves, flowers, etc. or their oils or their extracts to specific extraction and purification techniques.

The terms "standardized oil" and "standardized extract" apply to compositions of matter that are either already commercially available or manufactured on request by dedicated companies that are mastering current extraction, e.g. solvent or C02 extraction, and purification techniques and that can deliver oils or extracts with a precisely defined and characterized content in active substances, cannabinoids in the instant case.

Standardized hemp (Cannabis sativa L.) extracts used according to the invention present furthermore a high content in non-psychotropic cannabinoids and in particular CBD, namely up to ca. 25 to 50 or even 80 % CBD and with THC less than 0.05 % (weight).

An example of a preferred standardized hemp extract comprises 23.6 % CBD, 0.25 % of a mix of CBDV, CBDA & CBG and less than 0.05 % THC (weight).

According to an optional embodiment of the invention the selected hemp extract is defined as "full spectrum" extract, meaning that it contains a blend of other cannabinoids, terpenes, flavonoids and phytonutrients that boost its bioavailability.

Embodiments of the invention

The granule composition according to the invention has been conceived to be delivered through a delivery system which maximizes the absorption and the bioavailability to optimize the benefits of the hemp oils extract, in particular the cannabinoids contained therein, essentially CBD and any additional active ingredients.

The active ingredients are delivered through granules, which are highly soluble in saliva of the mouth and in water. While oils or capsules do not dissolve in saliva or water and have to go through the gastro-intestinal tract, the active ingredients, namely the cannabinoids, are diffused directly into the blood vessels in the mouth through buccal diffusion.

Within the frame of the invention, it was observed that such a buccal diffusion allows 3 to 4 times higher bioavailability that comparable oral products delivered in an oil or in a capsule.

The granule composition according to the invention absorbs straight into the pet's blood through the mucosal membrane in the mouth, allowing the hemp components, i.e. the cannabinoids, mainly CBD here, to bypass the gastrointestinal system and the first pass liver metabolism. The effect is likely as high as 30 % versus 4 to 6 % of that observed when cannabinoids are administered by means of oils.

Eventually, besides being better absorbed, fast and reliable, buccal absorption provides a more precise dosing.

Veterinary compositions or dietary supplements according to the invention are conveniently used by simple addition or mixing with the regular diet of the selected mammal, e.g. the selected companion animal (pet). The administration follows usually the same feeding pattern as that applied for healthy pets, e.g. once or twice a day. Although this way of administration is preferred, pouring directly granules according to the invention into the pet's mouth is also accepted and even common practice.

For preventing or treating the various troubles or disorders which are addressed within the frame of the invention the dosage of CBD, i.e. the main active cannabinoid, extends conveniently from ca. 0.2 to 10, preferably from 0.2 to 5 mg per day per kg body weight. The prevention of said troubles or disorders requires low 0.2 to 0.5 mg CBD per day per kg body weight. The advice is to start low and increase slowly. Due to the lack of THC negative side effects or even drug addiction are definitely avoided.

Severe troubles may require significantly higher dosages over a shortened period, e.g. ca. 10 to 25 mg CBD per day per kg body weight or even more. But even at these doses no negative side effects are predicted as well as any addiction.

The veterinary composition or dietary supplement according to the invention can be provided in the form of unit doses each corresponding to one serving as follows: for dogs, sachets, pouches or bags or capsules containing 5 g of granules comprising 10 mg of the hemp (Cannabis sativa L.) extract mentioned here above or, expressed differently 2.0 to 3.0 mg CBD;

for horses or camels or zoo animals, pouches or bags or capsules containing 16 g of granules comprising 320 mg of the hemp (Cannabis sativa L.) extract mentioned here above or, expressed differently 80 mg CBD;

dogs weighing from 5 to 20 kg are conveniently treated by means of one portion of 5 g granules per day whereas dogs with body weight over that 20 kg are conveniently treated with 3 portions of 5 g per day or even more if ever necessary. Alternatively, sachets containing granules providing up to 8 mg CBD par dose can be used within that frame.

horses weighing less than 500 kg are usually provided with one 16 g portion of granules per day which is most frequently administered directly into the mouth, whereas horses weighing more than 500 kg are usually provided with two 16 g doses of granules per day or even more if ever necessary.

Adding the said portions to the daily diet of the horses at stake, nevertheless, is also possible. It was observed that treatments ranging for or even over 20 days did not reveal any negative side effects.

Camels or zoo animals can be subject to similar dosages as long as the above ratio CBD per day per kg body weight is duly monitored.

Examples

Example 1

Predefined portions of sucrose (41 % weight), dextrose (D-glucose monohydrate 58 %) and glucose syrup (1.4 % weight) were intimately mixed with minute amounts of a commercially available, standardized hemp extract** and eventually processed according to a standard granulation technique to afford dried spherical granules containing 0.23 g of the said hemp extract** per lOOg granules.

**containing 23.6 % weight CBD; 0.25 % weight (CBDV + CBDA + CBG) and less that 0.05 % weight THC

Micronutrients like Vitamin B6, Niacin and zinc acetate dihydrate can be added to the above formulation if ever desired; the latter can further comprise a stabilizer like gum Arabic or similar. Portions of 5 g granules were then packed individually to afford dose units providing each ca. 10.5 mg hemp extract** corresponding to ca. 2.5 mg CBD per 5 g portion.

These portions are designed for small mammals like dogs and cats and provide the recommended daily serving for an animal subject to behavioral disorders. Depending on the animal or the severity of the disorder, one observes first signs of relaxing within 30 minutes to 2 hours already.

Example 2

Portions of 16 granules each manufactured according to the method of Example 1 have been prepared in such a way to comprise 360 to 370 mg of the above hemp extract** or, expressed differently ca. 80 mg CBD per 16 portions. The latter are designed for large mammals like horses, camel and zoo animals.

^♦♦containing 23.6 % weight CBD; 0.25 % weight (CBDV + CBDA + CBG) and less that 0.05 % weight THC.

Example 3

A sugar-free granule composition was prepared according to Example 1 when substituting the 41 % weight of sucrose by 20 % weight of GOS/FOS and the necessary increase of weight % of dextrose to balance.

Such a granule formulation has the advantage to be less caloric and consequently better suited to dogs suffering from age related disorders or diseases like diabetes.

This granule formulation is also better suited for treating chronic pain over an extended period.

Example 4

Referring to the recipe disclosed in Example 1 the proportions of dextrose can vary from 30 to 90 % of weight without affecting substantially the delivery of the cannabinoids provided by the hemp extract.

The same applies concerning sucrose the proportions of which can vary from 10 to 70 % weight whereas those of GOS/FOS are kept between 10 and 20 % weight.

Claims

1. A veterinary composition or dietary supplement for use in the prevention or the treatment of behavioral disorders or troubles in mammals which is in the form of water soluble polysaccharide-based granules comprising as the source of

cannabinoids an oil or an extract of hemp (Cannabis sativa L.) essentially devoid of psychotropic substances.

2. A veterinary composition or dietary supplement for use in the prevention or the treatment of age related disorders or troubles in mammals which is in the form of water soluble polysaccharide-based granules comprising as the source of

3. A veterinary composition or dietary supplement for use in supporting or

strengthening the behavioral balance of mammals which is in the form of water soluble polysaccharide-based granules comprising as source of cannabinoids an oil or an extract of hemp (Cannabis sativa L.) essentially devoid of psychotropic substances.

4. A veterinary composition or dietary supplement for use in the prevention or the treatment of pain or inflammation or nauseas in mammals which is in the form of water soluble polysaccharide-based granules comprising as source of cannabinoids an oil or an extract of hemp (Cannabis sativa L.) essentially devoid of psychotropic substances.

5. A veterinary composition or dietary supplement for use in supporting and

strengthening the immune system and the natural anti-inflammatory response in mammals which is in the form of water soluble polysaccharide-based granules comprising as source of cannabinoids an oil or an extract of hemp (Cannabis sativa L.) essentially devoid of psychotropic substances.

6. A veterinary composition or dietary supplement according to any of the preceding claims wherein the granules consist of a matrix of water soluble polysaccharides selected among starch, soluble starch, microcrystalline cellulose, dextrin, dextrose, sucrose, isomaltose, oligosaccharides such as fructo-oligosaccharides (FOS) or gluco- oligosaccharides (GOS) and mixtures of same.

7. A veterinary composition or dietary supplement according to any of the preceding claims wherein the source of cannabinoids is a C02 or solvent extract of hemp (cannabis sativa L.) essentially devoid of psychotropic substances and namely devoid of THC.

8. A veterinary composition or dietary supplement according to any of the preceding claims wherein the source of cannabinoids is a standardized solvent extract of hemp (cannabis sativa L.) comprising ca. 25 % (weight) of CBD.

9. A veterinary composition or dietary supplement according to any of the preceding claims wherein the granules comprise ca. 0.01 to 0.25 %, preferably 0.05 to 0.15 % (weight) of CBD.

10. A veterinary composition or dietary supplement according to any of the preceding claims wherein the mammals are zoo animals or companion animals and in particular dogs, cats, horses and camels.

11. A veterinary composition or dietary supplement according to any of the preceding claims which is administered in such a way to provide to the mammals in need thereof a daily dose of ca. 0.1 to 10 mg, preferably ca. 0.5 to 5.0 mg CBD per kg body weight.