DESCRIPTION

FIELD OF INVENTION

This invention relates to compositions for appetite suppression and reducing weight in humans and/or other species that can tolerate cocoa and/or theobromine, and more particularly to compositions that contain chocolate which has been enhanced in natural theobromine or synthetic theobromine.

BACKGROUND TO THE INVENTION

Chocolate bars normally contains in the order of 29 - 45% of fat by weight. With chocolate formulations of less than this it becomes increasingly difficult to mould and/or use the chocolate as a coating. Chocolate chips usually contain between 24 - 30 % fat by weight. This invention relates not to theobromine consumption alone but in the presence of chocolate, which has a synergistic effect on appetite suppression over and above the two separate components. The active ingredients therefore are chocolate or chocolate extract or cocoa or cocoa extract together with enhanced concentrations of theobromine over and above the quantities normally present in standard cocoa commodities such are cocoa bean, cocoa liquor, cocoa powder and chocolate.

Theobromine is a known alkaloid and stimulant and it has been widely reported to have a food suppressant effect and it has been proposed in weight loss formulations, but never in formulations comprising of cocoa without the addition of over non cocoa related functional ingredients and or in formulations of chocolate without the addition of other non cocoa related functional ingredients. This patent is about the synergistic effect of the individual components, namely of theobromine together with reduced fat chocolate and / or reduced fat cocoa.

The naturally occurring theobromine content of cocoa powder ( 10-12 % total fat ) is in the range of between 1- 2.5% by weight. In plain chocolate there is usually in the order of 0.5 - 1.5% by weight. Theobromine is a mild diuretic, a mind stimulant ( on the cardiovascular system, the muscular system and the central nervous system ), it can lower the blood pressure because it can dilute the blood vessels, and also has relaxing effects creating a feeling of well being.. It has a long lasting effect in that it is broken down to about 50% in the blood stream after 6 to 10 hours. It increases the metabolic rate and stimulate the breakdown of fat ( lipolysis).

BRIEF DESCRIPTION OF THE INVENTION.

It is a well established fact that overweight and obesity is not a healthy condition. Obesity is highly prevalent and of increasing concern to the population atiarge. It follov/s that products that aid and result in appetite suppression or resulting in weight loss would ^" He 'highly beneficial to a society where millions suffer from obesity, as long as the dosage is safe and effective, when taken as directed.

Overweight and obesity are chronic conditions not only associated with the social stigma of being unattractive and undesirable, but it is also associated with decreased longevity and many pathological conditions such as diabetes, varicose veins, arthritis, heart disease and cancer to name but a few.

Over weight and obesity is characterised by the excessive accumulation of fat in the body and as a consequence of a caloric intake that surpasses the energy expenditure. The excessive fat is not metabolised and there is a gradual deposition of fat in the body; and when this is above 20% of the ideal weight ( as described for example in the Metropolitan Height and Weight tables in Jama, 260, 2547-48, 1988 ) the person concerned is described as obese.

The availability therefore of a dietary supplement which will suppress appetite and lead to weight loss in overweight and obese persons is highly desirable.

OBJECTIVE OF THE INVENTION

The objective of this invention is to provide a composition and regimen that is useful in helping persons not only to reduce body weight but also not to put in on in the first place. Such an invention as proposed will result in maintenance of a lowered body weight over a long period with the unpleasant side effects that are commonly experienced with prescription drugs.

DETAILED DESCRIPTION OF THE INVENTION AND PREFERRED EMBODIMENTS THEREOF

The present invention is directed to a composition comprising chocolate which is enhanced with theobromine to a level that is higher that that normally inherently present in cocoa liquor or cocoa powder. We are stating that there is synergistic effect of theobromine and other substances present in chocolate, which when consumed together on a regular basis create a stronger appetite suppression that leads to weight loss than if theobromine is consumed alone.

Cocoa contains a number of chemical substances whose influence on human and/or animal physiology is not fully understood. These include but is not limited to for example biogenic amines such as phenylethylamine and tyramine which act as neurotransmitters. Phenylethylamine stimulates the brain in much the same way as amphetamine. Tyramine has a similar effect of epinephrine These substances effect mood swing by causing an emotional high , which can be associated with a feeling of alertness and contentment. Another class of substances are the flavenoids, and include catechin, epicatechin and proanthocyadins and are all powerful antioxidants and there role may also be implicated in the synergistic effect.

It should also be mentioned that cocoa dies contain some caffeine. Cocoa powder usually contains about 0.1 % caffeine by weight and plain chocolate about 0.05% caffeine by weight. Caffeine is a well known stimulant although the amounts present are indeed quite small.

Chocolate also contains some sugar and the rapid absorption of sugar into the blood stream will lead to a rush of glucose to the brain this may contribute to a feeling of contentment. In contract cocoa contains virtually no sugar and is considered to be a low digestible carbohydrate food.

More importantly, in the conching of the chocolate the cocoa reacts with the sugar in what is described as Maillard reactions which creates pleasant flavours and aromas usually associated with chocolate. The conching also removes the acidic volatiles normally associated with cocoa. There may also be some caramelisation reactions. It is no wonder then that chocolate has a much more pleasant taste than cocoa which is acid, bitter and somewhat astringent. For this very reason cocoa is virtually always sweetened with sugar prior to consumption.

We do not really understand the chemistry behind chocolate craving and many hypotheses have been presented in the scientific literature but there is something in the chocolate which may be associated to the smell and/ or taste of chocolate including cocoa, as well as the pleasure-causing anandamines in the presence of carbohydrate consumption ( i.e the sugar content of chocolate and complex carbohydrate in the cocoa), which increases the availability of the amino acid typtophan, the presursor of seratonin. Our hypothesis is that for the synergistic effect claimed in this invention the presence of one or more of these substances is important in combination of enhanced quantities of theobromine over and about the levels normally found in standard cocoa powder and chocolate.

Of course one could consume large quantities of cocoa and theobromine by eating chocolate or drinking chocolate beverages, but this would mean consuming large amounts of sugar and fat which would defeat the object as the caloric intake would increase. The compositions in this invention contain much less calories because the formulations are presented principally as dietary supplements for example capsules or tablet or gum in which over a few grams need be consumed.

These compositions are safe and effective when used as directed and side effects are minor or none.

Excellent results were obtained demonstrating appetite suppression in a clinical trial study according to the present invention in which product was administered orally either in capsules or tablets ( pills). This was a cross over study in which each participant acted as his/her own control; participants were administered the test product daily over a seven day period after which there was a seven day wash out period and seven days on a placebo. AU products were allocated blind so that the participant was unaware of whether which was the test product or placebo.

The appropriate active components may be formulated for administration by any conventional route such as rectal, nasal, topical ( dermal) or parental. The composition may be in the form

of tablets, capsules, suspensions, chewing gum, emulsions, solutions, suppositories, sprays or preparations that can be injected. Tablets for oral use contain the active ingredients that are usually present in inert admixtures necessary for manufacturing the table for example inert diluents such as calcium carbonate, calcium phosphate, lactose sodium phosphate etc; granulating and disintegration agents such as starches, maltodextrins; and lubricating agents for example magnesium stearate or talc. Other acceptable excipients include colouring agents, plasticisers, humecatants etc. The tablets may optionally be coated.

The active ingredients of the appetite suppression compositions can also be incorporated into slow release formulations by delaying disintegration and absorption in the gastrointestinal tract. Glycerol monosterate or glycerol distearate are such know substances, although many techniques are known in the art.

The inactive excipients in a tablet may include for example calcium carbonate, dicalcium phosphate, macrocrystalline cellulose, stearic acid, silica or magnesium stearate. The active ingredients may also be incorporated into a soft or hard gel capsule either by themselves or by mixing the active ingredients with water or an oil medium such as liquid paraffin or edible oil and enclosing it within the capsule or gel capsule.

The active ingredients can also be administered as an oral liquid form by suspending the active ingredients in an aqueous solution in a mixture with dispersion agents, wetting agents suspension agents and preservation agents or thickening agents. These agents are when known in the art.

The active ingredients may also be delivered parenterally in dosage forms consistent with conventional pharmaceutically acceptable carriers and adjuvants. For this form of administration the chocolate and cocoa components are limited soluble to extracts and synthetic theobromine or other soluble theobromine containin -gσ h ^• erbal extracts.

In rectal preparations, suitable dosage forms for the active ingredients according to the present invention include suppositories ( emulsion or suspension types ), and rectal gelatins capsules ( either in solution or suspension ) . A typical suppository formulation the active principles would mixed into pharmaceutical grade cocoa butter, esterified acids, glycerinated gelatin, and acceptable water soluble or dispersible bases such as polyethylene glycols and polyethylene glycols and polyoxyehtylene sorbitan fatty acid esters.

Other formulations include for example the incorporation of theobromine ( either synthetic, or solvent extracts of chocolate or cocoa which are enriched in natural theobromine or other herbal extracts rich in theobromine ) into chocolate mass , chocolate or cocoa powder, and / or chocolate or cocoa beverage preparations incorporated in dry mixes or ready to drink beverages.

This invention also includes sugar confectionery of all descriptions into which both of the appropriate active ingredients are incorporated into the formulation. This includes, candies of all description including for example hard boiled candy, toffee, jellies, gums, chewing gum, bubble gum and fondant.

EXAMPLES

Example 1

Normal healthy adult individuals were given tablets containing plain chocolate powder with 65 % cocoa solids and standardised with 10% theobromine. Each tablet contained the following active ingredients, namely 30mg of theobromine and 270 mg of reduced fat chocolate. Participants were instructed to consume one tablets was about thirty minutes prior to their habitual meal times, repetitively on a daily basis. No instructions were given asking the individuals to purposely change their diet and/or modify their eating habits.

A feeling of appetite suppression and satiety was reported by individuals after a few days. The majority of individuals cut down on the amount they ate and did not feel the need to snack in between meals

Example 2

Normal healthy adult individuals were given capsules containing cocoa extract which contained 8% of theobromine and 400mg total weight ( excluding the gelatin capsule) and asked to consume two capsules before breakfast on a daily basis. No instructions were given asking individuals to purposely change their diet and/or to modify their eating habits.

A feeling of appetite suppression and satiety was reported by individuals after a few days. The majority of individuals cut down on the amount they ate and did not feel the same need to snack in between meals.

Example 3

Normal healthy adult individuals were given tablets containing cocoa powder standardised with 20% theobromine and each tablet contained 300 mg , that is 240 mg of fat free cocoa powder and 60 mg of theobromine. Individuals were asked to consume one tablet before each meal on a daily basis. No instructions were given to individuals to purposely change ihe diet and/or to modify their eating habits.

A feeling of appetite suppression and satiety was reported by individuals after a few days. The majority of individuals cut down on the amount they ate and did not feel the same need to snack in between meals.

This feeling of appetite suppression disappeared when individuals stopped consuming the tablets. ' ^:

Example 4.

10 grams of plain chocolate powder with 65% cocoa solids and standardised 10% theobromine was prepared and administered into sachets. Healthy adult individuals were instructed to mix the contents into 150 ml of skimmed milk or water and to consume every day at breakfast.

Individuals reported that they simply lost their appetite and reported that were struggling to eat as much as they used to.