GB2390303A

GB2390303A - Coated compositions for birds

Info

Publication number: GB2390303A
Application number: GB0312280A
Authority: GB
Inventors: William Raymond Bruce
Original assignee: Individual
Current assignee: Individual
Priority date: 2002-06-08
Filing date: 2003-05-29
Publication date: 2004-01-07
Anticipated expiration: 2023-05-29
Also published as: GB2390303B; GB0312280D0; GB0213192D0

Abstract

A coated pharmaceutical compositions suitable for orally administering anthelmintics to birds comprises a core (12) coated with an active ingredient (14) over which are provided two further layers of water insoluble material (16, 18). The core is limestone or quartz grit which is white which is attractive to game birds. The active ingredient is especially an anthelmintic. The first (inner) further layer is an oil or fat and the second (outer) further layer is a fatty acid.

Description

r '. ORAL COMPOSITIONS

FIELD OF THE INVENTION

This invention relates to compositions suitable for 5 administering medicaments. In particular, this invention relates to coated pharmaceutical compositions suitable for orally administering anthelmintics to birds.

BACKGROUND OF THE INVENTION

10 The administration of medicaments to animals such as birds can involve considerable logistical problems, especially where relatively large numbers are involved in free-range conditions.

A convenient way in which to administer pharmaceutical 15 compositions to animals, such as birds, is to combine the pharmaceutical compositions with the animal's food.

However, the pharmaceutical and food must be combined in such a way so that the resulting product will still be eaten by the animals. Many animals have a keen sense of 20 smell and any adverse smell will therefore deter an animal from eating the food.

In the treatment of birds, such as game birds (e.g. grouse), racing pigeons, free-range poultry (e.g. hens) anthelmintics may be required to prevent and/or cure 25 parasitic infections (e.g worm infections, such as Trichostrongylus or Capillaria, tick-borne infections,

i -2- Trichomanas or Coccidiosis). The anthelmintics become activated in the birds gut and destroy any worms.

Game birds such as grouse normally eat only heather, insects, cotton grass and grit. Grit is required for the 5 game birds digestion. Game birds therefore pose a particular problem as they are very selective about what they will eat. Furthermore, as the grit eaten by game birds is generally white, any material which alters the grit to be non-white may deter a game bird from eating the 10 grit.

Although it is known to coat grit particles with pharmaceutical compositions and then use a single waterproof coating such as fat (e.g. palm fat) or a relatively high melting point oil, previous attempts have 15 been relatively unsuccessful as the waterproof coating has the tendency to be washed off over a relatively short period of time. On removal of the waterproof coating the pharmaceutical composition on the coated grit particle is exposed whereupon the grit will no longer contain the 20 correct dose of the pharmaceutical agent.

Furthermore, grit particles with an outer coating of fat or relatively high melting point oil are found not to store very well as they tend to stick to one another. This makes it difficult to distribute the grit and for the 25 target recipients to eat the grit. The coated grit particles are also not very white with the result that the

l grit may not be eaten by the required recipient. J It is an object of embodiments of the present invention to obviate or at least mitigate at least one or more of the aforementioned problems.

5 It is a further object of embodiments of the present invention to provide a coated pharmaceutical composition suitable for orally administering medicaments to birds.

It is a yet further object of embodiments of the present invention to provide a coated pharmaceutical I 10 composition which is resistant to weathering.

SUMMARY OF THE INVENTION

According to a first aspect of the present invention there is provided an oral composition for ingestion by a 15 bird, said composition comprising: a core particle coated with a pharmaceutical material comprising a pharmaceutically active ingredient; wherein said coated particle further comprises at least two further layers of water insoluble material coated 20 thereon.] The pharmaceutically active ingredient may be medicinally active.

The core particle may be quartz or limestone grit. It should be noted that both quartz and limestone grit are I 25 white. If the coated core particle is non-white it may not be eaten by a recipient. The core particle may have an

l -4- average particle cross-section of about 0.1 to 5mm and preferably of about 1 to 3mm.

The pharmaceutically active ingredient is usually mixed with a suitable carrier such as starch and, in 5 particular, corn starch to form the pharmaceutical material. The pharmaceutically active ingredient may be selected from any of the following: anthelmintics; parasitic fungi; and/or neutraceuticals such as dietary supplements.

10 A suitable anthelmintic is, for example, fenbendazole which prevents or destroys worms in egg, larvae or adult stages of a helminth.

Parasitic fungi may be used in the control of free living infective worm larvae or to destroy worm eggs in 15 faeces. Suitable dietary supplements are selected from any of the following: vitamins; minerals; trace elements; antioxidants; and the like.

The pharmaceutical material may also comprise, for 20 example, flavourings and/or scent which are attractive to the recipient in order to maximise uptake of the oral composition. For example, in the case of grouse the pharmaceutical coating may also comprise aniseed oil which is known to attract grouse.

25 The pharmaceutical coating may form in the region of 0.1 to 10 we% and preferably 2.5 to 4 wit of the total oral composition.

r. -5- The first layer of water insoluble material may be a water insoluble fat or oil. Suitable oils are mineral oils such as petroleum and/or hydrocarbon oils. Alternatively, vegetable and/or animal oils may be used.

5 Preferably, the mineral oil is SILKOLENE GRADE T85 (Registered Trade Mark). SILKOLENE GRADE T85 is a saturated mineral oil with an average chain length of C24 and a range of about C12 - C32. The average molecular weight is about 285g. (SILKOLENE GRADE T85 is available from Fuchs 10 Lubricants (UK) PLC, Silkolene Oil Refinery, Belper, Derbyshire, UK).: Suitable water insoluble fats and oils may also be selected from any of the following: corn oil, coconut oil, cottonseed oil, palm oil, bacon fat and butter fat.

15 A first further layer of water insoluble material may form in the region of 0.1 to 5 we% and preferably about 1.0 wt% of the total oral composition.

A second further layer of water insoluble material may be formed from or derived from saturated or unsaturated 20 fatty acids or mixtures thereof. Typically, metal salts of saturated or unsaturated fatty acids are used. Suitable salts are sodium, potassium, calcium, copper, aluminium and lithium salts. Metal salts of fatty acids are commonly known as soaps. The saturated or unsaturated fatty acids 25 may be of Coo to C24 and preferably C12 to C18 The saturated or unsaturated fatty acids may be selected from any of the

l: -6- following: lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid and linolenic acid.

Preferably, the second further layer of water insoluble material is calcium stearate.

5 Alternatively, the second further layer of water insoluble material may be any suitable water insoluble material such as a water insoluble fat which forms a waterproof outer coating which is different to that of the first layer of water insoluble material.

10 The second layer of water insoluble material may form in the region of 0.1 to 5 wt% and preferably about 0.75 to 1.25 wit of the total oral composition.

Preferably, the oral composition is in the form of a coated particle.

15 Typically, the recipient is intended to be a bird such as a game bird, racing pigeon, free-range poultry such as hens and the like. In particular, the recipient is a grouse. The oral composition may be waterproof and may be 20 resistant to weathering.

Typically, on digestion of the oral composition the first and second further water insoluble layers are dissolved in the recipients gut thus exposing the medicinal material. 25 According to a second aspect of the present invention there is provided a method of forming an oral composition

according to the first aspect comprising: mixing a core particle with a pharmaceutical material comprising a pharmaceutically active ingredient to form a first coating on the core particle; and then 5 mixing the pharmaceutically coated core particle with a first water insoluble ingredient, followed by a second water insoluble ingredient to form second and third coating layers on the particle.

A barrel type open-top mixer/coaler may be used for 10 the mixing. The mixing may be performed in large quantities. Typically, core particles and pharmaceutically active ingredients are mixed in a ratio of about 97. 5 wt% to 2.5 wt% and then mixed with about 1 wt% of a first water 15 insoluble ingredient and then about 1 wt% of a second water insoluble ingredient.

According to a third aspect of the present invention there is provided a method of treating a medical disorder using an oral composition according to the first aspect.

20 The medical disorder may be the presence of worms and/or worm eggs within a recipient.

According to a fourth aspect of the present invention there is provided an oral composition according to the first aspect for use as a medicament.

25 According to a fifth aspect of the present invention there is provided an oral composition according to the

> l l i first aspect wherein the oral composition comprises an anthelmintic for use as an anthelmintic.

BRIEF DESCRIPTION OF THE DRAWINGS

Embodiments of the present invention will now be 5 described, by way of example only, with reference to the accompanying drawing in which: Figure 1 is a sectional view of a coated grit particle according to a first embodiment of the present convention.

10 DETAILED DESCRIPTION

Shown in Figure 1, there is an oral composition in the form of a coated grit particle generally designated 10 according to a first embodiment of the present invention.

The coated grit particle 10 comprises: a grit core 12; a 15 pharmaceutical coating 14 on the grit core 12; a first layer of water insoluble material 16; and a second layer of water insoluble material 18.

The grit core 12 may be any type of suitable grit particle. In the case of grouse where quartz or limestone 20 grit is a normal part of their intake diet, the grit core 12 is conveniently quartz or limestone grit. Usually, the grit core 12 has substantially sharp edges to assist in the normal digestive activity of the recipient bird. The grit core 12 is of about 1 to 3mm in cross-section.

25 The pharmaceutical coating 14 is a mixture of corn starch and fenbendazole.

- 9 - The thickness of the coating may be varied according e to the species of the recipient and the dosage. The pharmaceutical coating 14 is a thin layer and forms in the region of about 2.5 to 4 wit of the total coated grit 5 particle 10.

The first layer of water insoluble material 16, interposed between the pharmaceutical coating 14 and the second layer of water insoluble material 18, is SILKOLENE GRADE T85 which is a saturated mineral oil with an average 10 chain length of C24 and a range of about C12 - C32.

SILKOLENE GRADE T85 has an average molecular weight of about 285g. (SILKOLENE GRADE T85 is obtained from Fuchs Lubricants (UK) PLC, Silkolene Oil Refinery, Belper, UK).

SILKOLENE GRADE T85 is a colourless clear liquid.

15 The first layer of water insoluble material 16 forms about 2 we% of the total coated grit particle 10. The first layer of water insoluble material 16 has the effect of sealing the pharmaceutical coating 14.

The second layer of water insoluble material 18 forms -

20 an outer waterproof coating and is formed from calcium stearate. The second layer of water insoluble material 18 forms 0.75 to 1.25 we% of the coated grit particle 10.

To form the coated grit particles 10 simple mixing 25 techniques may be used. For example, about 25kg of a pharmaceutical composition comprising fenbendazole and corn

-10- starch is initially mixed with about 955kg grit of approximately 1 to 3mm in cross-section to form a pharmaceutical coating 14 on a grit core 12. Any type of barrel type open-top mixer/coaler may be used. About 10kg 5 of a first coating ingredient of SILKOLENE GRADE T85 (Registered Trade Mark) is then added under mixing to form the first layer of water insoluble material 16. 10kg of a second coating ingredient of calcium stearate is then added under mixing to form the second layer of water insoluble 10 material 18.

The formed coated grit particles 10 are found to store well and do not adhere to other particles. The coated grit particles 10 are therefore easy to distribute.

Furthermore, the coated grit particles 10 may be 15 placed in outdoor conditions and remain fundamentally unaffected. The particles 10 are therefore resistant to weathering from rain and retain their waterproof coating.

Additionally, the coated grit particles 10 are generally white in nature and will therefore be freely 20 eaten along with any uncoated grit which is also white. If the coated grit particles were not white this is likely to deter a recipient, such as a grouse, from eating them.

On digestion of the coated grit particles 10, the second layer of water insoluble material 18 and then the 25 first layer of water insoluble material 16 will be dissolved in the recipients gut allowing the

: l -11 pharmaceutically active ingredients to be delivered to the recipients. EXAMPLES

5 EXAMPLE 1

The coated grit particles 10 were compared with coated grit according to the prior art.

Coated grit particles, according to the prior art were

prepared by mixing 2.5kg of palm fat with 2.5kg 4% 10 fenbendazole and adding this to 95kg of quartz grit with an average particle cross-section of 1 - 3mm. These particles with a single water insoluble layer are called Sample A below. Coated grit particles 10 were then prepared as 15 previously described. These coated particles 10 with two water insoluble layers are called Sample B. A further sample according to the present invention was then prepared wherein the outer coating of calcium sterate is doubled. This is achieved by doubling the 20 amount of calcium stearate to 2% during mixing.

Three separate trays of Samples A, B and C were set out on separate perforated aluminium trays and left outside for three months. At the end of 1, 2 and 3 months, one tray of each formulation was removed for analysis.

25 The amount of fenbendazole retained after 1, 2 and 3 months for Samples A, B and C is shown in the table below.

-12 _ % Retention of Fenbendazole l Sample I 1 Month 2 Months l 3 Months | A 52.3 58.7 56.4

B 83.1 82.8 82.9

C 76.4 93.4 I 77.9 1

The results illustrate that Sample B is more effective 5 than Sample A at retaining the fenbendazole. The coated grit particles 10 according to Sample B therefore provide the best waterproofing for the pharmaceutically active fenbendazole. Sample C shows that if an excess amount of calcium 10 stearate is used the calcium stearate powder does not all adhere to the grit 12 and variable results are obtained.

Sample C was seen to be more (dusty) and this could be seen during manufacture.

15:

Claims

- 13 CLAINS

1. An oral composition for ingestion by a bird, said composition comprising: a core particle coated with a pharmaceutical 5 material comprising a pharmaceutically active ingredient; wherein said coated particle further comprises at least two further layers of water insoluble material coated thereon.

10 2. An oral composition according to claim 1, wherein the pharmaceutically active ingredient is medicinally active. 3. An oral composition according to any of claims 1 15 or 2 wherein the core particle is quartz or limestone grit. 4. An oral composition according to any preceding claim wherein the core particle is substantially white.

5. An oral composition according to any preceding claim wherein the core particle has an average particle cross-section of about 0.1 to 5mm.

25 6. An oral composition according to any of claims l to 4 wherein the core particle has an average particle cross-section of about 1 to 3mm.

- 14 7. An oral composition according to any preceding claim wherein the pharmaceutically active ingredient is mixed with a suitable carrier to form the pharmaceutical material. s 8. An oral composition according to claim 7 wherein the carrier is starch or corn starch.

9. An oral composition according to any preceding 10 claim wherein the pharmaceutically active ingredient is selected from any combination of anthelmintics, parasitic fungi, and/or neutracouticals such as dietary supplements. 15 10. An oral composition according to claim 9 wherein the anthelmintic is fenbendazole which prevents or destroys worms in egg, larvae or adult stages of a helminth. 20 11. An oral composition according to any of claims 9 or 10 wherein dietary supplements are selected from any combination of vitamins, minerals, trace elements and antioxidants. 25 12. An oral composition according to any preceding claim wherein the pharmaceutical material also comprises flavourings and/or scent which are attractive to the recipient in order to maximise uptake of the oral composition. ,

l l 13. An oral composition according to any preceding claim wherein the pharmaceutical coating comprises aniseed oil.

s 14. An oral composition according to any preceding claim wherein the pharmaceutical coating forms about 0.1 to 10 wt% of the total oral composition.

10 15. An oral composition according to any of claims 1 to 13 wherein the pharmaceutical composition forms about 2.5 to 4 wt% of the total oral composition.

16. An oral composition according to any preceding IS claim wherein the first layer of water insoluble material is a water insoluble fat or oil.

17. An oral composition according to claim 16 wherein the oil is a mineral oil.

18. An oral composition according to claim 17 wherein the mineral oil is any combination of petroleum, hydrocarbon, vegetable and/or animal oils.

25 19. An oral composition according to any of claims 17 and 18 wherein the mineral oil is a saturated mineral oil with an average chain length of C2 and a range of about C12 - C32 and an average molecular weight of about 285g.

l - 16 20. An oral composition according to any of claims 16 to 19 wherein the water insoluble fats and oils also comprise any of the following: corn oil, coconut oil, cottonseed oil, palm oil, bacon fat and butter fat.

21. An oral composition according to any preceding claim wherein a first further layer of water insoluble material forms in the region of about 0. 1 to 5 wt% of the total oral composition.

22. An oral composition according to any of claims 1 to 20 wherein a first further layer of water insoluble material forms about 1.0 wt% of the total oral composition. 23. An oral composition according to any preceding claim wherein a second further layer of water insoluble material is formed from or derived from saturated or unsaturated fatty acids or mixtures thereof.

24. An oral composition according to claim 23 wherein metal salts of saturated or unsaturated fatty acids are used. 25 25. An oral composition according to claim 24 wherein the salts are any combination of sodium, potassium, calcium, copper, aluminium and lithium salts.

- 17 26. An oral composition according to any of claims 23 to 25 wherein the saturated or unsaturated fatty acids are ClO to C2,.

S 27. An oral composition according to any of claims 23 to 25 wherein the saturated or unsaturated fatty acids are Cl2 to C1&.

28. An oral composition according to any of claims 23 10 to 25 wherein the saturated or unsaturated fatty acids are selected from any combination of the following: lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid and linolenic acid.

15 29. An oral composition according to any of claims 1 to 22 wherein a second further layer of water insoluble material is calcium stearate.

30. An oral composition according to any preceding 20 claim wherein a second further layer of water insoluble material is a water insoluble fat which forms a waterproof outer coating which is different to that of the first layer of water insoluble material.

25 31. An oral composition according to any of claims 1, 29 or 30 wherein a second layer of water insoluble material forms about 0.1 to 5 wti of the total oral composition.

i - 18 32. An oral composition according to any of claims 1, 29 or 30 wherein a second layer of water insoluble material forms about 0.75 to 1. 25 wt% of the total oral composition. s 33. An oral composition according to any proceeding claim wherein the oral composition is in the form of a coated particle.

10 34. An oral composition according to any preceding claim wherein the oral composition is intended to be ingested by a game bird, racing pigeon, free-range poultry such as hens and the like.

IS 35. An oral composition according to claim 34 wherein the recipient is a grouse.

36. An oral composition according to any preceding claim wherein the oral composition is waterproof and is 20 resistant to weathering.

37. An oral composition according to any preceding claim wherein on digestion of the oral composition, first and second further water insoluble layers are 25 dissolved in a recipients gut thus exposing the medicinal material. 38. A method of forming an oral composition comprising:

- 19 mixing a core particle with a pharmaceutical material comprising a pharmaceutically active ingredient to form a first coating on the core particle; and then mixing the pharmaceutically coated core particle 5 with a first water insoluble ingredient, followed by a second water insoluble ingredient to form second and third coating layers on the particle.

39. A method of forming an oral composition according 10 to claim 38 wherein a barrel type open-top mixer/coaler is used for the mixing.

40. A method of forming an oral composition according to any of claims 38 or 39 wherein core particles and IS pharmaceutically active ingredients are mixed in a ratio of about 97.5 wt% to 2.5 wt% and then mixed with about 1 wt% of a first water insoluble ingredient and then about 1 wt% of a second water insoluble ingredient.

20 41. An oral composition according to any of claims 1 to 36 for use as a medicament.

42. An oral composition according to claim 41 wherein the medicament is used to treat the presence of worms 25 and/or worm eggs within a recipient.

43. An oral composition according to any of claims 1 to 37 wherein the oral composition is used as an anthelmintic.