GB2519965A

GB2519965A - Formulation

Info

Publication number: GB2519965A
Application number: GB1319352.9A
Authority: GB
Inventors: Katherine Coleman; Didi Verdina
Original assignee: READYSUPP Ltd
Current assignee: READYSUPP Ltd
Priority date: 2013-11-01
Filing date: 2013-11-01
Publication date: 2015-05-13
Also published as: GB201319352D0; HK1209981A1

Abstract

A composition for use in delaying the onset of muscle fatigue in horses comprises L-carnitine, creatine and beta-alanine. Also claimed is a composition comprising 10g/kg to 500g/kg of L-carnitine, 10g/kg to 600g/kg of creatine and 10g/kg to 600g/kg of beta-alanine. The composition may comprise a flavouring selected from mint, apple and garlic, and be administered as an equine feed supplement.

Description

Formulation

Field of Invention

The present invention relates to compositions comprising ingredients such as L-carnitine, creatine and beta-alanine and equine feed supplements comprising the same.

The invention additionally provides methods fin delaying onset of muscle fatigue in horses.

Background to the Invention

Horses in disciplines such as three day eventin& endurance, and racing must be very fit in order to compete successfully. To attain this peak level of fitness they must adhere to a rigorous daily training program. Many horses suffer thm undesirable muscle conditions related to the intense training schedules necessary fin top-level performance. These conditions can become severe enough to prevent a horse fitm competing or decrease their perlbrmance during competition. Pulled muscles, fittigued muscles, back soreness, and an equine specific condition called equine exertional rhabdomyolysis or tying-up' are just a lèw common muscle disorders related to intense training. Tying-up is when a horse develops muscle dysfunction that may involve pain and stiffliess in its large limb muscles (especially the hindlimb muscles in the hindquarters) and/or its back muscles. The muscle cells are ruptured to varying degrees. The condition can very from mild cramping to a very severe ease in which the horse cannot move and may even have to be euthanized.

Any of the aibrementioned muscle conditions could cause a racehorse to miss a race or run poorly costing the owner millions; or cause a three day event horse to not jump properly, which could endanger the rider's life; or cause the horse to compensate in other areas of its body. which puts undue strain on ligaments and tendons and commonly leads to injuries such as a tear of the superficial digital flexor tendon (known as a bowed tendon' tendon) or a torn suspensory ligament. Both of these injuries are extremely costly. An injured tendon or ligament dramatically affects the resale value of a horse and could potentially end the horse's career. In a best-case scenario ofaninjurylikeoneofthesethehorse willbeoffworkfbratleast9to 12 months.

Fitness training is undertaken in order to maximise the potential performance of a horse during competition, and delaying onset of muscle fatigue is one of the benefits of a physically trained horse. Delaying the onset of muscle fatigue by a fraction could make the difference between a win or not. If muscle function can be manipulated during training to fatigue later, then this will allow training gains over and above what can be attained normally. The result will be a higher level of fitness and a resulting higher potential for performance during competition.

It is an object of the prcscnt invention to providc a supplement to delay onset of muscle fatigue in horses, thereby enabling horses to work harder for longer and attain a higher level of peak fitness with a decreased risk of injury.

Description

In a first aspect the present invention provides a composition comprising L-camitine, creatine and beta-alanine.

Camitine is an amino acid that is considered non-essential. It is made in the liver and kidneys from lysine and methionine. The majority of carnitine is located in the muscle. Low levels are found in plant materials, although horses naturally have high muscle levels. Carnitine is a component of the enzymes that transport fatty acids into the mitochondria where they are used for energy production. Camitine is important for heart and brain function, muscle movement, and many other body processes.

Compositions of thc invention can comprise carnitinc at a conccntration of about lOg/Kg to about SOOg'Kg, preferably about 50g/Kg to about 300g/Kg, more preferably about 150g/Kg to about 250g/Kg. In preferred embodiments of the invention the composition comprises carnitine at a concentration of about 200g'T'Cg.

Creatine (also known as methylguanidine-acetic acid) is naturally produced in the body from amino acids, primarily in the kidneys and liver, and transported in the blood for use by the muscles. In humans and animals, approximately half of stored creatine originates from food. Burke et al (2003) showed that vegetarians had significantly lower lcvcls of crcatinc than non-vegetarians. Since vegetables are not thc primary source of creatine, vcgetarians can bc cxpected to show lowcr lcvcls of directly derived muscle creatine. However, the subjects happened to show the same levels after using supplements.

Many athletes, body-builders and sprinters use creatine to help build muscle mass.

Creatine is also under investigation as a possible therapeutic approach for the treatment of muscular, neuromuscular, neurological and neurodegenerativc diseases.

The conccntration of ATP (adenosinc triphosphate) in skeletal muscic is usually 2-5 mM, which would result in a muscle contraction of only a few seconds. Fortunately, during times of increased energy demands, the phosphagen (or ATP/PCr) system rapidly rcsynthcsizcs ATP from ADP with the usc of phosphocrcatinc (PCr) through a rcvcrsible rcaction with the cnzyme creatine kinasc (CK). In skelctal musclc, PCr concentrations may reach 20-35 mM or more. Additionally, in most muscles, the ATP regeneration capacity of CK is very high and is therefore not a limiting factor.

Although the cellular concentrations of ATP are small, changes are difficult to detect because ATP is continuously and efficiently replenished from the large pools of PCr and CK. Supplemental creatine has the ability to increase muscle stores of PCr, potentially increasing the muscle's ability to resynthesize ATP from ADP to meet increased energy demands.

Creatine can also buffer hydrogen ions (H') produced durthg intense, anaerobic exercise and transport ATP produced by aerobic metabolism from the muscle cell mitochondria to the cytoplasm, where it can be used for muscle contractioll.

Compositions of the invention can comprise creatine at a concentration of about lOg/Kg to about 600gIKg, prcferably about lOOg/Kg to about 400gIKg, more preferably about 300gIKg to about 400g!Kg. In preferred embodiments of the invention the composition comprises creatine at a concentration of about 360g/Kg.

Beta-alanine (also known as 3-aminopropionic acid) is a naturally-occurring beta- amino acid that in combination with histidine makes up the dipeptide carnosine. Beta-alaninc is also a component of anserine and as well as vitamin B5, or pantothenic acid.

Carnosine is found in large amounts in the brain and muscle, and especially in fast twitch muscle fibres. Camosine is degraded in the gastrointestinal tract, and production is beloved to be limited by the availability of beta-alanine.

Carnosine is a potent antioxidant. It also contributes to the buffering ability of the muscle to the acidity caused as a result of high intensity exercise (lactic acid). The reduction in pU within muscle calls as a result of lactic acid production is a major contributor to fatigue, due to disturbed enzyme ffinction and excitation-contraction coupling.

Beta-alanine assists performance in short duration, high intensity exercise lasting 1-2 minutes by allowing the muscles to contract and produce force for longer before a drop in pH causes fatigue.

Compositions of the invention can comprise beta-alanine at a concentration of about lOg/Kg to about (iOOg'Kg, preferably about lOOg/kg to about 400g/Kg, more preferably about 25OgIKg to about 350g/Kg. In preferred embodiments of the invention the composition comprises beta-alanine at a concentration of about 300g/Kg.

In embodiments of the invention the composition may comprise one or more of beta-hydroxy-beta-methylbutyrate (HMB), sodium bicarbonate and sodium citrate.

Bcta-hydroxy-bcta-methylbutyratc (HMB) is a metabolite of leucinc that has anti-catabolic activity, while sodium bicarbonate and sodium citrate buffer muscle acidity.

Compositions of the invention may be administered as dietary supplement or a feed supplement, such as an equine feed supplement. Preferably the composition is administered at least once per day. Ahematively, the composition may be administered twice per day or three times per day or more.

It is especially preferred that the composition is an equine formulation, i.e. in a formulation suitable for administration to equines.

The present invention additionally comprises an equine feed supplement comprising a composition as herein described.

The present invention additionally provides a method for delaying onset of muscle fatigue in horses comprising administering a combination of L-carnitine, creatine and beta-alanine.

In embodiments of the invention L-camitine is administered at a dosage of about 0.005g/Kg of body weight/day to about 0.1 g/Kg of body weight/day, preferably about 0.01 g/Kg of body weight/day to about 0.05g/Kg of body weight/day, most preferably L-carnitine is administered at a dosage of about 0.02g/Kg of body weight/day.

Creatine may be administered at a dosage of about 0.OOSg/Kg of body weight/day to about 0.5g/Kg of body weight/day, preferably about 0.02g/Kg of body weight/day to about 0.lg/Kg of body weight/day, most preferably creatine is administered at a dosage of about 0.05g/Kg of body weight/day.

Beta-alanine may be administered at a dosage of about 0.005g/Kg of body weight/day to about 0.3g/Kg of body weight/day, preferably about 0.Olg/Kg of body weight/day to about 0.OSg/Kg of body weight/day, most preferably beta-alanine is administered at a dosage of about 0.04g/Kg of body weight/day.

Compositions of the present invention may additionally comprise mint or mint flavour to aid in palatability for the horse and provide a pleasant aroma to the supplement.

Suitable mints include peppermint. Similarly, palatability can be improved by including one or more of apple, apple flavouring or garlic. Additionally or ahernatively, compositions of the invention can include wheat flour and/or wheat feed used as a mixing additive and binder. Wheat feed or wheat flour also aids palatability.

The composition may also comprise one or more suitable carriers or exeipients. In embodiments of the invention the composition may comprise one or more of a colour retention agent, salt, preservatives, flavouring, sweetener or colouring.

In embodiments of the invention the composition may comprise one or more additional active ingredients selected from vitamins, minerals, herbs, and natural compounds such as fruit or vegetable extracts.

Compositions of the present invention may be formulated as pills, powders, lozenges, sachets, cachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols, ointments or capsules. Preferably the composition is in the form of a powder.

Examples

A composition according to one embodiment of the invention was prepared as an equine feed supplement as follows:-Product Version 1 bag_wt 6.6 batch_size 1000 no_bags 152 inci_IvI 70 bag 0.7 LITRE TUB + LIDS JET 107-P Ingredient Active Ingredient per Formula inclusion Qty (Kg) L-CARNITINE t0000.0000 g 284.714 PEPPERMINT FLAVOUR 350.0000 g 5.000 CREATIINE 25000.0000 g 357.142 BETA ALANINE 20000.0000 g 285.714 WHEATFEEDWflEATFLOUR g/kg 66.4300 g 66.430 Analysis: Ca % 0.449 Na % 0.007 AlA % 14.663 Lys % 0.033 Cu mg 0.000 Ph % 5.390 Ash % 18.387 Mag 0.023 Meth 0.013 CI % 0.007 % VitA VitD3 VitE in 0.000 miii miii L-Camitine, creatine and beta-alanine have been uniquely combined to create an equine muscle performance supplement. As far as the inventors are aware, this is the first time this combination of compounds or any variation there-of has been used in horses to support muscles during training.

References Burke DG, Chilibeck PD, Parise G, Candow DG, Mahoney D, Tamopoisky M (2003).

"Effect of creatine and weight training on muscle creatine and performance in vegetarians" Medicine and science in sportc and exercise 35 (11): 1946-55

Claims

Claims 1. A composition comprising about lOg/Kg to about 500g'Kg of L-carnitine, about lOgtKg to about 600g/Kg of crcatinc and about 10g./Kg to about 600g/Kg of bcta-alanine.
2. A composition according to claim 1, wherein the concentration of L-camitine is about 50g./Kg to about 300g/Kg, the concentration of creatine is about bOg/Kg to about 400g/Kg and the concentration of beta-alanine is about I 00g/kg to about 400g/Kg.
3. A composition according to claim I or claim 2, wherein the concentration of L-camitine is about 200g/Kg, the concentration of creatine is about 360g/Kg and the concentration ofbcta-alaninc is about 300g/Kg.
4. A composition according to any of claims Ito 3, further comprising one or more of flavourings selected from mint, apple and garlic.
5. A composition according to any of claims Ito 4, further comprising wheat flour.
6. A composition according any of claims 1 to 5, wherein the composition is an equine formulation.
7. A composition for use in delaying onset of muscle fatigue in horses, wherein the composition comprises L-canitine, creatine and beta-alanine.
8. A composition for use according to claim 7, wherein the composition comprises about log/Kg to about 500g/Kg of L-carnitine, about lOg/Kg to about 600g/Kg of creatine and about I Og/Kg to about 600g/Kg of beta-alanine.
9. A composition for use according to claim 7 or claim 8, wherein the concentration of L-carnitine is about 50g/Kg to about 300g/Kg, the concentration of creatine is about 100g./Kg to about 400g/Kg and the concentration of beta-alaninc is about lOOg/kg to about 400g/Kg.
10. A composition for use according to any of claims 7 to 9, wherein the concentration of L-carnitinc is about 200g/Kg, the concentration of creatine is about 360g/Kg and the concentration ofbeta-alanine is about 300g/Kg.
11 A composition for use according to any of claims 7 to 10, fUrther comprising one or more of flavourings selected from mint, apple and garlic.
12. A composition for use according to any of claims 7 to 11, further comprising wheat flour.
13. A composition for use according any of claims? to 12, wherein the composition is an equine formulation.
14. An equine feed supplement comprising a composition according to any of claims Ito 6.
15. A method for delaying onset of muscle fatigue in horses comprising administering a combination of L-camitine, creatine and beta-alanine.
16. A method according to claim 15, wherein L-carnitine is administered at a dosage of about 0.OOSg/Kg of body weight/day to about 0.lg/Kg of body weight/day.
17. A method according to claim 15 or claim 16 wherein L-camitine is administered at a dosage of about 0.01 g/Kg of body weight/day to about 0.05g/Kg of body weight/day.
18. A method according to any of claims 15 to 17 wherein L-camitine is administered at a dosage of about O.02g/Kg of body weight/day.
19. A method according to any of claims 15 to 18, wherein creatine is administered at a dosage of about 0.OO5gIKg of body weight/day to about 0.5g/Kg of body weight/day.
20. A method according to any of claims 15 to 19, wherein creatine is administered at a dose of about 0.02g/Kg of body weight/day to about 0.lg/Kg of body weight/day.
21. A method according to any of claims 15 to 20, wherein creatine is administered at a dosage of about 0.05g/Kg of body weight/day.
22. A method according to any of claims 15 to 21, wherein beta-alanine is administered at a dosage of about 0.005g/Kg of body weight/day to about 0.3g/Kg of body weight/day.
23. A method according to any of claims 15 to 22, wherein beta-alanine is delivered at a dosage of about preferably about 0.Olg/Kg of body weight/day to about 0.OSg/Kg of body weight/day.
24. A method according to any of claims 15 to 23, wherein beta-alanine is administered at a dosage of about 0.04g/Kg of body weight/day.