IES59992B2 - Preparations for treating mucous membrane conditions - Google Patents

Description

PREPARATIONS FOR TREATING MUCOUS MEMBRANE CONDITIONS J The present invention relates to oral preparations for treating conditions of the mucous membrane, such as irritation or inflammation thereof. In particular, the invention relates to preparations which may be used to alleviate symptoms caused by the common cold or by sinus problems or by allergies such as hay fever. More generally, the invention relates to preparations which may be used to alleviate conditions of the mucous membrane caused by such agents as viruses, bacteria, dust or pollen, and also conditions which occur in post-operative patients and in patients undergoing chemotherapy for example.

The mucous membrane in the nose normally provides mucus which acts as a barrier against invasion by foreign bodies such as bacteria, viruses, dust and pollen, which are trapped by the mucus in the nose and throat and are subsequently either expelled or brought into the oesophagus for swallowing. Infectious material which is swallowed is subsequently destroyed in the digestive tract. A large number of viruses are capable of infecting the mucous membrane and by replicating themselves can temporarily overwhelm the natural defence mechanism provided, resulting in the well-known symptoms of the common cold, when a virus is present in a body, it can attach itself only to a cell whose surface matches the virus surface chemically. In the case of a common cold, the virus attaches itself to a mucous membrane cell. The virus then injects its genetic ·? 30 material into the cell, the cell reproduces the virus, and the viral progeny attack other surrounding cells. Pollen and/or dust are also capable of causing mucous membrane inflammation, vaccines have been developed to counteract the action of many viruses but under normal circumstances - 2 the virus must be identified so that the correct vaccine can be administered. A single vaccine is not available to counteract the action of all known viruses which attack the mucous membrane. vaccines have no action against dust or pollen irritation.

Antibiotics, ascorbic acid, pharmaceutical compositions and herbal remedies are also used to attempt to alleviate symptoms caused by the above sources but many provide, at best, only partial relief. Additionally, some vaccines, antibiotics and pharmaceutical products can have serious adverse side-effects. In these cases the treatment of the symptoms cannot be prolonged and these products must be administered with caution.

The most obvious initial symptom brought on by the common cold is what is generally known as a runny nose. This occurs when the mucous membrane starts to be affected by a foreign body. Mucus produced by irritated mucous membranes has a lower than normal solids content, so that when the mucous membrane is infected or aggravated the usual relatively high viscosity of the mucus is quickly reduced. The viscosity of the mucus decreases and subsequently does not provide the protection normally provided. This leaves a sufferer vulnerable to reinfection or secondary infection.

Dry mouth and sore throat conditions are typical symptoms in those suffering the common cold or an allergy attack. These conditions are often also present post-operatively and in patients undergoing extreme medication regimes, for example chemotherapy.

It is an object of the present invention to provide preparations which may afford protection, against reinfection or secondary infection and additionally to alleviate some of the discomfort and misery associated with the common cold and similar symptoms induced in other ways.

Accordingly, the present invention provides an oral preparation for treating irritation or inflammation of the mucous membranes and/or the naso-buccal region, characterised in that the preparation comprises at least one component selected from the group comprising sugars, sugar syrups, carbohydrates, gelling agents, gums or colloids, provided that when the at least one component comprises a sugar or sugar syrup, the preparation further comprises at least one other component from the group, further provided that where said at least one other component is a sugar or sugar syrup, the sugars and/or sugar syrups are different, the preparation being effective to alleviate dry and/or sore throat and mouth.

Advantageously, the preparation contains a viscous, high-solids content sugar syrup comprising one or more of glucose, fructose, corn or malt syrup or syrups and/or molasses.

Preferably, the carbohydrate comprises a dextrin and/or the gelling agent comprises gelatine, gelatinised starch, an alginate or a pectin and optionally at least one of the components has nutritional value.

The invention further provides a use of a material which comprises at least one component selected from the group comprising sugars, sugar syrups, carbohydrates, gelling agents, gums or colloids, provided that when the at least one component comprises a sugar or sugar syrup, the preparation further comprises at least one other component r from the group, further provided that where said at least one other component is a sugar or sugar syrup, the sugars t and/or sugar syrups are different, for the manufacture of a preparation for treating irritation or inflammation of the mucous membranes and/or the naso-buccal region and/or for treating the common cold or allergic conditions which affect the mucous membrane.

The present invention provides yet further an oral preparation for treating irritation or inflammation of the mucous membranes and/or the naso-buccal region, characterised in that the preparation comprises at least two components selected from the group comprising sugars, sugar syrups, carbohydrates, gelling agents, gums or colloids, provided that when the said at least two components each comprises a sugar or sugar syrup, the sugars and/or sugar syrups are different, the preparation being effective to alleviate dry and/or sore throat and mouth.

Preferably, the preparation contains a viscous, high-solids content sugar syrup. The sugar syrup may comprise one or more of glucose, fructose, corn or malt syrup or syrups and/or molasses. The preparation may be pharmaceutically inert and at least one of the components may have nutritional value.

Conveniently, the carbohydrate comprises a dextrin and. the gelling agent comprises gelatine, gelatinised starch, an alginate or a pectin.

The invention also provides the use of a material which comprises at least two components selected from the group comprising sugars, sugar syrups, carbohydrates, gelling agents, gums or colloids, and in which when the said at least two components each comprises a sugar or sugar syrup, the sugars and/or sugar syrups are different, for the manufacture of a preparation for treating irritation or inflammation of the mucous membranes and/or the naso-buccal region. The preparation is particularly useful for treating the common cold or allergic conditions which affect the mucous membrane, for example hay fever or house dust 0 allergy.

The preparations provided by the invention support the natural viscosity of mucus in the mucous membrane, whereby viruses, bacteria, dust and pollen, which normally deleteriously affect the action of mucus, are trapped by the mucous membrane as before, thereby eliminating or decreasing reaction to further attacks.

The preparations of the present invention may increase the 20 inherent viscosity of mucus such that under viral and/or bacterial attack and in cases of dust and/or pollen aggravation, where mucus loses its viscosity and does not provide the protection normally provided by said mucous membrane, the sufferer takes the preparation orally as soon 25 as the symptoms are noticed.

The components of the preparations are chosen so that high doses of them do not cause any harmful or hazardous side-effects.

The preparations are conveniently provided in the form of syrups, jellies, lozenges or tablets.

The preparations of the present invention may also be used for alleviating dry mouth conditions associated with illness such as cancer, extreme medical procedures such as chemotherapy and post operative dry mouth sensation.

The mucus produced normally in a healthy individual has a solids content of about 1%, whereas one constituent of a preparation according to the invention (such as malt syrup for example) will have a solids content of approximately 80%. The body has a far greater opportunity of expelling the viral infection with the support of the syrup than with the mucus alone. Additionally, preparations having highly viscous sugar contents have a well known ability to retard growth of micro-organisms.

Dextrins, gums, colloids and syrups of various types when taken as part of a preparation according to the invention have the ability to act as supportive and or protective agents for the mucous membranes. These components function with remarkable speed in alleviating the typical symptoms of the common cold and similarly distressing effects from other causes such as sinus problems and allergies.

Dextrins, gums, colloids and syrups are available either from natural or synthetic sources. Many have no deleterious side effects and a large percentage have nutritional qualities. Each of the above components have differing viscosities and differing amounts of solid matter content, all of which effect the characteristics of the final composition. a> The present invention utilises many dextrins, gums, colloids and syrups including what are generally known as > glucose syrups, corn syrups, dextrose syrups, fructose syrups, malt syrups, brewers and distillers syrups, sugar beet and sugar cane syrups, all prepared by means well known in the art from cereal, starch and carbohydrate sources, together with gel preparations thereof. In this specification, the term carbohydrate includes oligosaccharides and polysaccharides.

Such materials may be used in quantities ranging from a fraction of a gram to any convenient amount which is to be administered orally by placing on the tongue to dissolve and preferably by spreading over the gums and palate.

The actual soluble solids (predominantly sugar) content of sugar syrups such as glucose syrup, malt syrup, corn syrup and fructose syrup, may vary according to the methods of preparation. The methods of manufacture of these syrups is well known in the art. These syrups may have higher or lower conversion rates (starch to sugar ratios) depending on specific commercial requirements. Many of these syrups are freely available commercially.

For instance, commercially available malt syrups may have a total solid matter content of 80% in solution, containing approximately 75% maltose and maltotriose on dry matter. However, the proteins and non-fermentable sugars (dextrins etc.) may vary in content according to the processing temperatures.

In the case of commercially available glucose syrups, dextrose syrups and corn syrups, these are normally supplied as 42% dextrose equivalent, with approximately 16-20% dextrose, 25-29% maltose/maltotriose, 51-59% of higher sugars and dextrins. The individual materials content may vary according to the method of production, whether by the acid or enzyme processes, and temperature conditions. f All of the preparations described can be flavoured and/or coloured as required. 9 The physical and chemical compositions of these syrups as supplied commercially appears to be eminently suitable for use in the Examples of the present invention.

The fructose syrup types would be preferentially used for diabetic cases.

The following are examples of preparations within the scope of the invention: Example 1: 40% corn syrup mixed with 60% malt syrup.

This preparation allows easy dispersion of corn syrup in the mouth but retains the more pleasant flavour of the malt.

In this Example, glucose syrup may be substituted for the corn syrup.

Example 2: 90% corn syrup mixed with 10% of a solution of high solids content sodium alginate, prepared by dissolving 10 grams sodium alginate in 90 grams water.

This preparation provides greater adherence of the i components of the preparation to the throat and mouth and delays dilution by saliva.

Q _ A malt syrup may be used to provide a more pleasant J tasting preparation than that provided by the corn syrup preparation.

Example 3: 88% corn syrup mixed with 10% honey, 1% lemon extract and 1% glycerine.

This preparation provides relief in the case of an already established infection involving a sore throat.

Example 4: 49.5% corn syrup, 49.5% malt syrup plus 1% oil of garlic.

This preparation acts in a manner similar to the above preparations but additionally provides oil of garlic which 20 is know to impede many viruses.

Example 5: 97.5% fructose syrup, 2% gelatine and 0.5% oil of garlic.

Fructose syrup is provided for diabetic use and is combined with components to ensure longer useful life in the throat and mouth. , 30 Example 6: ,· 97.5% fructose syrup mixed with 2% locust bean gum, together with 0.5% oil of garlic.

This preparation provides an alternative to Example 5 for diabetics together with longer presence in the throat and mouth.

Example 7: 80% corn syrup mixed with 20% molasses.

This provides an alternative to corn syrup alone while enhancing flavour.

Example 8: 150 gms malt syrup with up to 6 gms gelatine melted in 40 ml warm water.

This preparation sets well and may be cut into cubes of suitable size for sucking in the mouth. The preparation may also be stoved to produce a hardened sweet or lozenge, which has a longer life in the mouth.

Example 9: Satisfactory pectin jellies are made using varying proportions of glucose syrup and/or malt syrup as described in the above Examples together with different proportions of sucrose, prepared using standard industrial procedures.

A typical formula which gives good results is as follows: 2.5 grams pectin in powder form pre-mixed with between 2 to 3 times its weight of sugar to aid dissolution; the pectin/sugar admixture is added to 30 ml water at ‘70°C with strong agitation. gms malt syrup and 30 gms sucrose are mixed and heated to 95-100°C. The solution of pectin/sugar and water above is then added and heated with agitation until approximately 76 to 80% solids in solution are reached as measured by a sugar refractometer. gm 50% w/v citric acid is added with agitation and the mixture immediately poured into moulds. Full setting takes place in approximately 24 hours.

Example 10: Extra strong jellies are obtained by adding up to 10 gms starch to the preparation of Example 9. In this case, pregelatinised starch is much more easy to use than native starch, as lumping is eliminated.

Example 11: 100 gms malt syrup to which up to 1% sodium alginate is dissolved.

This preparation shows good mouth retention.

A similar preparation may be made using glucose syrup and propylene glycol alginate in like proportions.

Example 12: An improved preparation of malt syrup with up to 1% sodium alginate as described in Example 11 is produced by adding various quantities of sodium hexametaphosphate. Quantities ranging from 0.05 to 25% sodium hexametaphosphate based on the dry weight of sodium alginate produce improved . l preparation texture.

Example 13: Preparations similar to the pectin jellies of Example 9 are prepared by adding starch to the malt and alginate mixtures, as follows: 100 gms malt syrup; up to 10 gms starch; and up to 1% sodium alginate.

An addition of from 20 to 50% sucrose adds to the body and flavour of the above.

Starch dispersal is facilitated by the addition of sodium hexametaphosphate in amounts preferably ranging from 0.05 to 25% based on the dry weight of sodium alginate.

Native starch may be substituted by pregelatinised starch and propylene glycol alginate may be used in place of the sodium alginate.

Example 14: Boilings based on malt syrup with a substantial proportion of sucrose are boiled down to give a suckable lozenge with lasting effect in the mouth, comprising: gms malt syrup and 50 gms sucrose, mixed and gradually heated until the sucrose is dissolved, then cooked at a higher temperature until ready to pour into moulds. Lower temperatures are necessary than for sugar cooking to prevent charring.

J Example 15: The addition of gums and starches to the preparations described in Example 14 adds considerably to mouth retention when boiled down to high solids content. They also aid against inadvertent moisture pick-up from the atmosphere. gms malt syrup; up to 10 gms pregelatinised starch dispersed in water; and gms sucrose, are boiled together to suitable solids content. In this case it is more necessary to control the cooking to prevent charring.

Example 16: Dried glucose powder and dried malt powder may also be used as bases either singly or in admixture with various thickeners, as for examples 48% dried glucose powder , 30 48% dried malt powder 4% gelatine powder, acacia powder and/or tragacanth x powder.

Example 17: Γ A further thickener comprises 42% dried glucose powder 44% dried malt powder 4% gelatine powder, acacia powder and/or tragacanth powder % pregelatinised starch and/or starch derivative.

Example 18: The preparations of Examples 16 and 17 are suitable for tabletting by adding products such as cellulose ethers, polymers of vinyl and acrylic acids, and their salts.

These preparations also contribute viscosity and mouth retention on their own or in admixture.

Binders and lubricants can contribute substantial viscosities to the preparations. Such binders and lubricants are selected from the group comprising cellulose ethers, cellulose esters, polyvinyl compounds, polyethylene and polyethylene glycols, acrylic compounds, microcrystalline cellulose and polyvinylpyrrolidone.

Example 19: Preparations similar to those of Example 10, tabletted using preparations as described in Example 18, are prepared in the following proportions: 44% dried glucose powder 42% dried malt powder * % pregelatinised starch or starch derivative 4% cellulose ether, cellulose ester, polyvinyl alcohol, polyethelene glycol derivative, acrylic derivative, microcrystalline cellulose, polyvinyl pyrrolidone, either singly or in combination.

The following preparations according to the invention illustrate the use of unitary hydrocolloids which are dissolved or dispersed by techniques well known in the art.

Example 20: 0.1 to 10 gms sodium alginate and gm sodium hexametaphosphate are mixed in water to 100 gms.

Example 21: to 3 gms locust bean gum in water to 100 gms.

Example 22: 0.1 to 4 gms guar gum in water to 100 gms.

Example 23: 0.1 to 2 gms. carrageenan in water to 100 gms.

Example 24: 0.1 to 2 gms pectin in water to 100 gms.

Example 25: Γ 0.1 to 2 gms propylene glycol alginate in water to 100 gms.

Example 26: 0.1 to 5 gms sodium carboxymethylcellulose in water to 100 gms.

Example 27: 0.1 to 5 gms methyl cellulose in water to 100 gms.

Example 28: 0.1 to 5 gms microcrystalline cellulose in water to 100 gms.

Example 29: 0.1 to 5 gms xanthan gum in water to 100 gms.

Example 30: 0.5 to δ gms gelatine in water to 100 gms. (5* Example 31: i to 10 gms starch, starch derivative, starch dextrins and/or flour in water to 100 gms.

Example 32: to 10 gms linseed in water to 100 gms.

The following examples which are similar to Examples 3 and 6, respectively, illustrate the use of citric and tartaric acids.

Example 33: 87.75% malt syrup % honey 2% locust bean gum 0.25% citric acid or tartaric acid.

Example 34: 97.25% fructose syrup 2% locust bean gum 0.5% oil of garlic 0.25% citric acid or tartaric acid.

It will of course be understood that for commercial use, permitted preservatives as specified by national legislation may be added to the above preparations. Suitable colourings and/or flavourings may also be added as desired.

The materials and compositions act on the mucus in a manner contrary to the normal reaction to a viral attack or an allergic reaction, that is the viscosity of the mucus is 18maintained and/or increased which alleviates discomfort but also supports and protects the mucous membrane so that it may fight further attacks.

The protective and supportive effects may last for up to some hours, while in the case of a strong attack, further doses of the materials may be taken ad lib until the distressing symptoms pass away altogether.

The following are some reasons why the materials and compositions cited apart from the many possibilities make an excellent choice for general application: they are cheap; are widely available in bulk; are pleasant to take; are harmless; have the correct consistency for rapid effect; do not conflict with many other medicaments added to or taken in conjunction with them; have good heat stability; need little extra preservation; have long shelf life; and, as well as by direct intake, are capable of being prepared in many different ways for application such as in tablets, in capsules, in various forms of suga.r confectionery, and many other feasible means while still maintaining their effectiveness.

As well as the materials cited as being suitable, starch preparations, alginates, collagens, gelatines, carrageens, and carrageenates, agars, natural gums such as tragcanth, guar, acacia., karaya, pectins, locust bean gum, and all their acceptable derivatives as well as the mucilaginous e extracts of plants and seeds, carboxy methyl cellulose, microcrystalline cellulose, carob, honey, molasses, « cellulose and derivatives, xanthans, milk proteins, mucoproteins, lipoproteins, isinglass, in suitable condition and formulation and products possessing the desired characteristics have capabilities of being supportive of and protective to the mucous membrane.

It is also possible to formulate variations of the most effective types by combining various saccharides with the various raw materials cited above. It should be noted that the application of simple sugars alone, such as sucrose and dextrose, do not have significant effect.

Specific pharmaceutical products such as vitamins and antibiotics, aspirin or paracetamol may be added to the preferred preparations. Prolonged local action of some pharmaceutical products in the throat and mouth may be non-benefical. The preparations of the present invention are usually quick and effective such that pharmaceutical additives are most unlikely to be needed. It is therefore recommended that pharmaceutical remedies should be taken, separately from the preparations of the present invention.

The preparations of the present invention are also suitable for use in alleviating unpleasant conditions of sore and dry mouth which occur after anaesthesia, or to those suffering distressing conditions such as cancer, undergoing 25 chemotherapy or similar procedures. Known remedies often fail to give the required relief, while examples of the preparations above give immediate and lasting relief.

It will of course be understood that the present invention 30 is not limited to the specific details described herein, which are given by way of example only and that various modifications and alterations are possible within the scope of the appended claims.

Claims (5)

CLAIMS :

1. An oral preparation for treating irritation or L inflammation of the mucous membranes and/or the naso-buccal region, characterised in that the preparation comprises at least one component selected from the group comprising sugars, sugar syrups, carbohydrates, gelling agents, gums or colloids, provided that when the at least one component comprises a sugar or sugar syrup, the preparation further comprises at least one other component from the group, further provided that where said at least one other component is a sugar or sugar syrup, the sugars and/or sugar syrups are different, the preparation being effective to alleviate dry and/or sore throat and mouth.

2. A preparation according to claim 1, characterised in that the preparation contains a viscous, high-solids content sugar syrup comprising one or more of glucose, fructose, corn or malt syrup or syrups and/or molasses.

3. A preparation according to any preceding claim, characterised in that the carbohydrate comprises a dextrin and/or the gelling agent comprises gelatine, gelatinised starch, an alginate or a pectin and optionally at least one of the components has nutritional value.

4. Use of a material which comprises at least one component selected from the group comprising sugars, sugar syrups, carbohydrates, gelling agents, gums or colloids, provided that when the at least one component comprises a * sugar or sugar syrup, the preparation further comprises at least one other component from the group, further provided that where said at least one other component is a sugar or sugar syrup, the sugars and/or sugar syrups are different, for the manufacture of a preparation for treating irritation or inf lamination of the mucous membranes and/or the naso-buccal region and/or for treating the common cold or allergic conditions which affect the mucous membrane.

5. A preparation for treating irritation or inflammation of the mucous membranes and/or the naso-buccal region and/or for treating common cold or allergic conditions which affect the mucous membrane substantially as herein