pastilles

Abstract

The lozenge comprises 1.4-1.8 wt% pectin; 78-88 wt% sweetener; 0.1-1.5% organic acid; and 10-19 wt% water. A method of treating sore throat, comprising administering the lozenge of claim 1 to the oral cavity of a patient in need thereof; and dissolving the lozenge over a period of at least 5 minutes.

Description

TECHNICAL FIELD

[0001] The present invention relates to a sweet lozenge for delivering pectin to treat sore throat. The lozenge of the present invention utilizes pectin as the sole active to treat the ailment. The present invention provides an optimized formulation to achieve superior soothing performance over existing products. BACKGROUND

[0002] Therapeutic methods for sore throat are very popular among consumers. They are a treatment that does not require the investment of a health care worker and thus can be used as needed quickly when needed.

[0003] Many different products are available to treat sore throat in consumers. They include different dosage forms and a variety of different active agents and mechanisms of action to achieve treatment of the pain.

[0004] The present invention relates generally to throat lozenges and more specifically to HCl lozenges using pectin as the active ingredient.

[0005] Pectin acts as a demulcent. A demulcent is an agent that forms a soothing film over a mucous membrane that can reduce mild pain and mucosal inflammation.

[0006] However, demulcents typically last for about 30 minutes or so as the normal action of the throat (swallowing or breathing or any eating or drinking of water) gradually removes the protective layer. This means that effective relief requires a continuous replenishment of the film. This has favored the delivery of these active agents ("active substances") in the form of sweet lozenges that can be taken steadily throughout the day.

[0007] Demulcents are sometimes referred to as mucoprotective agents. In addition to pectin, natural demulcents include glycerin, honey, and syrup. Methyl cellulose, propylene glycol, and glycerin are good examples of synthetic demulcents.

[0008] Such demulcents are typically used in over-the-counter (OTC) medications to treat sore throat.

[0009] Pectin is a commercial heteropolysaccharide derived from higher plant cell walls. It consists of 1-4 linked partially methylated polygalacturonic acid units.

[0010] The carboxyl groups of the pectin component can exist as esters, free acids, ammonium, potassium, or sodium salts, or amides.

[0011] According to the United States Food and Drug Administration ("FDA"), pectin is a GRAS (Generally Recognized as Safe) food substance.

[0012] Lozenges are a popular oral active agent delivery vehicle. They are typically very sweet to encourage and maintain consumption. Lozenges range from soft jellies like gummies to hard solids, sugar-based confections.

[0013] Many commercial lozenges contain pectin. Examples include Extra Lozenges, Breezers and Smith Soother Lozenges.

[0014] The amount and timing of pectin delivery can be a consideration when using a lozenge treatment product to effectively relieve sore throat.

[0015] To effectively soothe and treat a sore throat, a layer of pectin needs to be formed on the painful tissue. This requires a balance in the amount of pectin available, the ease of release from the lozenge, and the delivery time frame.

[0016] Gummies are easy to load with pectin, but they are generally intended to encourage chewing and rapid consumption. This is a good form for delivering active materials (e.g. vitamins and drugs / actives) that need to reach the body systemically quickly.

[0017] However, since gummies are generally consumed in less than a minute, they are not generally a good form for the local delivery of active materials to the throat / mouth, since any pectin (or other active) contained will not be fully released from the rest of the gummy before it is swallowed.

[0018] Most of the pectin or other active in a gummy will go directly to the stomach and not coat the mucosal tissue as desired.

[0019] Hard lozenges are better suited for the slow release of active materials for the mouth and throat. A hard lozenge can take many minutes to dissolve in the mouth. It allows for a steady release of active materials. The hard body also discourages early swallowing.

[0020] However, the hardness sometimes encourages some consumers to chew the lozenge. This is a consideration since it also means that, like a gummy, most of the pectin contained will be lost to the stomach.

[0021] Unfortunately, it is also difficult for a hard lozenge to reach the levels of pectin needed to treat a sore throat. Pectin has low solubility / mixing in a hard lozenge form.

[0022] This can be seen from the fact that commercial hard lozenge soother lozenges generally contain very low levels of pectin. It is common for commercial hard lozenge soother lozenges to contain between 2 and 7 mg of pectin per lozenge.

[0023] This level of pectin is too low for effective soothing capabilities. Since soothing performance requires a physical coating of the tissue to provide relief, more soothing agent material is needed to provide a satisfactory coating of the inflamed throat tissue.

[0024] It is an object of the present invention to provide a more effective lozenge for treating sore throat. SUMMARY

[0025] In its broadest form, the first aspect of the present invention comprises a lozenge comprising:

[0026] a) 1.4-1.8% by weight of pectin;

[0027] b) 78-88% by weight of a sweetener;

[0028] c) 0.1-1.5% of an organic acid; and

[0029] d) 10-19% by weight of water.

[0030] Further, preferably the lozenge does not contain gelatin, starch or any other gelling agent or rheology modifier.

[0031] In another aspect, the total weight of the lozenge is 2-6 grams.

[0032] In another aspect, the lozenge comprises at least 40 mg of pectin.

[0033] In another aspect, the sweetener comprises 82-86% by weight of the lozenge.

[0034] In another aspect, the sweetener is an artificial sweetener.

[0035] In another aspect, the sweetener comprises one or more of fructose, sucrose, lactose, glucose and mixtures thereof.

[0036] In another aspect, the sweetener is a combination of sucrose and corn syrup, and the sucrose and corn syrup can be present in a weight ratio of 20:80 to 80:20.

[0037] In another aspect, the organic acid comprises 0.5-1% by weight of the lozenge.

[0038] In another aspect, the organic acid comprises citric acid, citrate salts and mixtures thereof.

[0039] In another aspect, the water comprises 12-17% by weight.

[0040] In another aspect, the lozenge further comprises one or more of a flavoring agent, a dye, a preservative or mixtures thereof.

[0041] In another aspect, the lozenge has a hardness of between 8000 and 20,000 grams as measured by TPA test.

[0042] In another aspect, the lozenge further comprises at least one other active selected from menthol, guaifenesin, acetaminophen, benzocaine, phenylephrine hydrochloride, dextromethorphan hydrobromide and mixtures thereof.

[0043] In another aspect of the present invention, the lozenge consists essentially of:

[0044] 1.6% by weight of pectin;

[0045] 81-83% by weight of sucrose and glucose;

[0046] 14-17% by weight of water;

[0047] 0.9-1.10% by weight of citric acid and / or citrate and / or mixtures thereof; and

[0048] 0.1-0.5% by weight of flavoring agent.

[0049] And in another aspect, the lozenge has a weight ratio of sucrose and glucose of 60:40 to 40:60. Further, the lozenge has a total weight of between 3-4 grams.

[0050] The present invention also includes a method of treating sore throat comprising applying the lozenge of the first aspect of the present invention to the oral cavity of a patient in need thereof, and further dissolving said lozenge over a period of at least 5 minutes.

[0051] In another aspect, the method of treatment dissolves said lozenge over a period of at least 10 minutes.

[0052] Definitions

[0053] All percentages are weight percentages based on the total weight of the composition, unless otherwise stated.

[0054] For the purposes of the present specification, the term "comprising" means including the following features, but is not limited to them. An open-ended structure.

[0055] For the purposes of the present specification, the term "consisting of means including only the following. A closed-ended structure.

[0056] For the purposes of the present invention, the term "consisting essentially of is equivalent to "consisting of, but with the additional possibility of containing minor amounts of non-essential ingredients. For the purposes of the present invention, "consisting essentially of means that less than 5% by weight of the composition can be an undefined, non-essential ingredient. These can include dyes, flavoring agents, preservatives, and the like, minor ingredients.

[0057] For the purposes of the present specification, any disclosure of a composition or formulation including the following features can be assumed to disclose the same composition or formulation consisting of or consisting essentially of the same features. DETAILED DESCRIPTION

[0058] Applicants have surprisingly found that by careful control of the levels of pectin, sweetener, acid and water, an optimum balance can be achieved to provide a lozenge with a high level of pectin and just the right hardness so that the lozenge has the ideal release profile in the mouth.

[0059] This ideal level of hardness naturally encourages the lozenge to be consumed by sucking rather than chewing. It is not too soft nor too hard to prevent crunching.

[0060] The composition of the lozenge also contains sufficient moisture to maintain a high enough level of pectin to very effectively soothe the throat.

[0061] The lozenges of the present invention have been optimised to use pectin as the only active and soothing agent.

[0062] The pectin used for the purposes of the present invention can be used in a variety of purities and grades. Pectin is a natural product and inevitably contains small amounts of natural contaminants. For the purposes of the present invention, it is preferred to use the highest purity grade of pectin.

[0063] For example, gelatin is commonly used in lozenge confections to control texture, providing elasticity to the soft candy. Starch and other gelling agents are also often used to achieve similar functions.

[0064] The lozenges of the present invention do not include gelatin or starch or any other gelling or rheology modifying agents. By careful control of the proportions of the defined ingredients used, the present invention provides a confectionery lozenge which is completely free of other modifying agents.

[0065] The lozenges of the present invention are therefore very suitable for vegetarians.

[0066] However, in some cases, it can still be desirable to include secondary ingredients such as colourings, preservatives and flavourings.

[0067] In its broadest scope, the lozenges of the present invention comprise or consist essentially of:

[0068] Table 1

[0069] Ingredients wt.% Pectin 1.4-1.8％ Sweetener 78-88％ Acid 0.1-1.5％ Water 10-19％

[0070] There is in principle no reason to limit the upper limit of the pectin content in the finished lozenges to this range. However, due to the pectin acting as a gelling and binding agent, in order to achieve a suitable level of hardness in the lozenges while maintaining effective conditions in manufacture, there is a practical upper limit of less than 2% pectin in the optimised formulation of the present invention to achieve a lozenge with the required properties.

[0071] Using pectin levels greater than 2% by weight means that the formulation is both difficult to handle and produces a non-uniform final product. Higher levels of pectin also increase the gelling temperature and require excessive amounts of energy (heat) to remain in a liquid state. Uniform mixing is also extremely difficult and there is a risk of the formulation setting prematurely and blocking the production line.

[0072] The preferred range of pectin for use in the present application is 1.4 to 1.8% by weight of the lozenge, more preferably 1.5 to 1.7% by weight, most preferably about 1.6% by weight.

[0073] The amount of pectin required in the lozenge to effectively relieve pain depends on a number of factors. The area of the painful or inflamed tissue, the rate of release of the pectin in the lozenge, the rate of reduction of the mucous protective layer (coughing or swallowing), the rate of consumption of the lozenge in the mouth (dissolution time) and the amount of pectin in the lozenge.

[0074] These factors obviously vary from person to person. However, the applicants have found that for most adults, in order to effectively treat inflamed throat tissue, at least 30-40mg of pectin per lozenge is required. Preferably at least 45mg of pectin per lozenge, more preferably at least 50mg of pectin per lozenge, most preferably at least 55mg of pectin per lozenge can provide the required performance.

[0075] There is a clear relationship between the concentration of pectin in the mix and the amount of pectin in each final lozenge. Given the inherent difficulties of increasing the concentration of pectin in a batch, any increase in the amount of pectin required per lozenge would need to be achieved by increasing the size of the lozenge.

[0076] The sweetener in the lozenges of the present application comprises 78-88% by weight of the lozenge, more preferably 80-86% by weight, most preferably 81-84% by weight of the lozenge.

[0077] The sweetener can comprise any sweetener known in the art. The sweetener helps to encourage consumption of the lozenge by making it taste pleasant.

[0078] The sweetener of the present application can be a natural or artificial "sugar". Artificial sugars can be beneficial for those seeking relief from throat pain while maintaining control over their calorie intake.

[0079] Preferably, the sweetener comprises one or more sugars.

[0080] The sugar can be selected from the list comprising fructose, mannose, lactose, galactose, sucrose, glucose, dextrose and mixtures thereof.

[0081] The sugar can be in their natural or non-natural form, or mixtures thereof.

[0082] It is particularly preferred that the sweetener of the present application comprises a mixture of glucose and sucrose.

[0083] Glucose and sucrose can be present in any weight ratio. Preferably, both sugars can be used in a weight ratio of 80:20 to 20:80, more preferably in a ratio of 60:40 to 40:60 and most preferably in a ratio of 55:45 to 45:55.

[0084] In a preferred lozenge composition, sucrose and glucose are used in a weight ratio of about 1 :1.

[0085] The sugar can be used in any form. From crystalline sugar particles, aqueous solutions to natural syrups.

[0086] A particularly preferred source of glucose in the present application is corn syrup. Particularly preferred sources of sucrose are granulated sucrose and aqueous solutions of sucrose.

[0087] An acid is used in the formulation to adjust the pH to aid the setting process. Any suitable acid can be used for this purpose.

[0088] A particularly preferred source of acid is citric acid or a citrate or mixtures thereof.

[0089] The acid is used in an amount of 0.1 to 1.5% by weight of the lozenge, more preferably 0.05% to 1.0% and most preferably about 1% by weight.

[0090] The amount of water present in the lozenge can be in the range of 10% to 19% by weight. More preferably the water content is 11 to 16% by weight and most preferably 14 to 16% by weight.

[0091] A more preferred lozenge of the present application comprises or consists essentially of:

[0092] Table 2

[0093]

[0094]

[0095] Other optional minor ingredients include flavourings and colourings if necessary. The optional minor ingredients will comprise less than 1% by weight of the lozenge. More preferably the minor ingredients will comprise less than 0.75% by weight and most preferably less than 0.5% by weight.

[0096] The flavourings used can be natural or artificial or a mixture of both. There is no restriction on the choice of flavourings for the present application.

[0097] It is preferred that natural flavourings are used. A particularly preferred flavouring is a natural product such as honey or a mint extract.

[0098] The lozenges of the present application are formulated to relieve sore throat as described using pectin as the sole active ingredient. However, it can be desirable to enhance the performance of the lozenges by the addition of at least one further active ingredient.

[0099] Any other active ingredient can be used. It is particularly preferred that the additional active agent can include anesthetic, antitussive and decongestant agents and mixtures thereof as desired.

[0100] Particular APIs of particular relevance to the present application include menthol, benzocaine, guaifenesin, acetaminophen, phenylephrine hydrochloride, dextromethorphan hydrobromide and mixtures thereof.

[0101] The present application is not limited to these active ingredients and the skilled person can consider other examples.

[0102] Particular APIs of particular relevance to the present application include menthol, benzocaine, guaifenesin, acetaminophen, phenylephrine hydrochloride, dextromethorphan hydrobromide and mixtures thereof.

[0103] Table 3

[0104]

[0105] Method of Manufacture

[0106] The manufacturing process is not critical to the present application. The skilled person will be familiar with the general process of preparing lozenges.

[0107] US 5,932,273 and US 2010 / 0226904 Al (both incorporated herein by reference) disclose exemplary manufacturing processes for manufacturing lozenges.

[0108] The gist of the process is to mix all the ingredients in solution (water) at high temperature and then remove the excess water until the formulation reaches the desired moisture content. Finally, the formulation is allowed to cool in a mould until it solidifies.

[0109] The precise order of addition of the ingredients to the initial solution is not critical to the present application. Although it is common to add the acid ingredients last as they will promote the gelation of the pectin. The precise batch temperature will vary depending on the manufacturing equipment used.

[0110] The applicant has found that a temperature of 110°C for the mixing and moisture optimization process, a temperature of 90°C for the transfer to the mould and a drying temperature of room temperature are optimal.

[0111] Hardness Test

[0112] The hardness of the lozenges of the present application is intermediate between classic hard candy lozenges and soft candies. The applicant has found that this particular hardness range optimizes the consumption time in the mouth by preventing the mastication of the lozenges.

[0113] The following texture profile analysis (TPA) hardness test is used to test the lozenges and obtain the correct hardness level.

[0114] The TPA method is a very commonly used method to characterise food properties. For more details see https: / / texturetechnologies.com / resources / texture-profile-analysis#settings-and-standards, which is incorporated herein by reference.

[0115] This method compresses the sample twice and measures properties such as hardness, stickiness, springiness etc. For the purposes of this invention, the test is used to test hardness.

[0116] The test has several defined steps. The key set points for the hardness test used herein are:

[0117] Probe: A 40mm flat probe and it is much larger than the sample area being tested. This leaves a lot of room for human error in sample positioning (i.e. as long as the sample is fully under the probe it will repeat the test).

[0118] Compression and withdrawal speed: 2mm / s is used as a suitable test speed. Various speeds can be used. However, too fast and the resolution of the peak can not be clear due to the sampling rate. Slower sampling speeds are possible but these tests are usually carried out on a large number of samples so the overall test time would increase. 2mm / s achieves a balance between resolution and test time.

[0119] Compression distance: The compression distance is set as a strain %. Strain measurement requires a high degree of calibration. The probe moves down at 3mm / s “finding” the sample. Once the load cell receives a force of 10g the test starts.

[0120] The probe calculates the sample height from the height calibration and then proceeds to compress the sample to 50% of its total height. A higher strain percentage is used to simulate sample mastication. 50% strain is chosen as it provides accurate and repeatable hardness readings without exceeding the capacity of the load cell.

[0121] Repeatability - all results shown are the average of at least 10 tests.

[0122] Results of Hardness Test

[0123] The lozenge of the invention (Table 3 formulation) was tested for comparison against 3 commercially available pectin containing (low content) lozenges.

[0124] The results in Table 4 clearly show that the hardness of the lozenges of the invention is intermediate between soft and hard (the Ludens sample was too hard to get a result in this test, the actual hardness value was out of range).

[0125] Table 4

[0126]

[0127]

[0128] Preferably the lozenge of the application has a hardness value (with 50% strain according to the TPA test described above) of 8,000 to 20,000 g, more preferably 9,000 to 15,000 g, most preferably 10,000 to 13,000 g.

[0129] A particularly preferred hardness for the lozenge of the application is about 12,000 g.

[0130] This balance allows for a high pectin content and encourages the right consumer behaviour to optimise the soothing effect.

[0131] For optimal performance, the lozenge of the application can dissolve slowly in the mouth and release pectin in the mouth over a period of only 5 minutes. Preferably, the lozenge should dissolve over a period of at least 10 minutes, most preferably at least 12 minutes.

Claims

1. A tablet comprising: 1.4-1.8% by weight of pectin; 78-88% by weight of sweetener; 0.1-1.5% organic acids; and 10-19% by weight of water.

2. The tablets of claim 1, wherein (i) the tablets are free of gelling agents and rheology modifiers; or (ii) the tablets are free of gelatin and starch.

3. The tablets according to claim 1, wherein the total weight of the tablets is between 2 and 6 grams.

4. The tablet of claim 1, wherein the tablet contains at least 40 mg of pectin.

5. The tablet of claim 1, wherein (i) the sweetener comprises 82-86% by weight of the tablet; or (ii) the sweetener is an artificial sweetener; or (iii) the sweetener comprises one or more of fructose, sucrose, lactose, glucose, and mixtures thereof.

6. The tablet of claim 1, wherein the sweetener is a combination of sucrose and corn syrup.

7. The tablet of claim 1, wherein the organic acid accounts for 0.5-1% by weight of the tablet.

8. The tablet of claim 1, wherein the organic acid comprises citric acid, citrate, and mixtures thereof.

9. The tablets of claim 1, wherein the water comprises 12-17% by weight.

10. The tablets of claim 1, further comprising flavoring agents, dyes, preservatives, or mixtures thereof.

11. The tablet of claim 1, wherein the tablet has a hardness between 8,000 and 20,000 grams as measured by a TPA test.

12. The tablet of claim 1, further comprising an additional active ingredient selected from menthol, guaiacyl ether, acetaminophen, benzocaine, phenylephrine HCl, dextromethorphan HBr, and mixtures thereof.

13. The tablet according to claim 1, which is substantially composed of: 1.4-1.8% by weight of pectin; 81-83% by weight of sucrose and glucose; 14-17% by weight of water; 0.9-1.10% by weight of citric acid and / or citrate and / or mixtures thereof; and 0.1-0.5% by weight of flavoring agent, wherein the total amount of all components is 100% by weight.

14. The tablet of claim 13, wherein the weight ratio of sucrose to glucose is between 60:40 and 40:

60.

15. The tablet of claim 13, wherein the total weight of the tablet is between 3 and 4 grams.

16. The tablet of claim 6, wherein the weight ratio of sucrose to corn syrup is 20:80 to 80:

20.

17. Use of the tablet of claim 1 in a method for preparing a product for treating a sore throat, wherein the method comprises: Apply the tablets of claim 1 to the oral cavity of patients in need; as well as The tablets are dissolved over a period of at least 5 minutes.

18. The use of claim 17, wherein the tablet dissolves over a period of at least 10 minutes.

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