GB2613695A - Lollipop for the administration of pharmaceuticals, food supplements and nutraceuticals - Google Patents

Abstract

A dosage form is disclosed comprising i) a gel forming hydrocolloid which is gelatine, ii) a pharmaceutical, food supplement or nutraceuticals and iii) a fruit concentrate, characterised in that the said dosage form has an available water content of less than 8% by weight. The dosage form can be used as a carrier for pharmaceuticals, food supplements and nutraceuticals and is suitable for use with young children and the elderly. The dosage form takes the form of a jelly pop or lollipop. The fruit concentrate in the dosage form controls the available water and free water in the formulation. Honey may be used to further control the available water and free water in the said dosage form.

Description

Lollipop for the administration of pharmaceuticals, food supplements and nutraceuticals Field of the Invention The present invention relates to a dosage form which can be used as a carrier for pharmaceuticals, food supplements and nutraceuticals and which is suitable for use with young children, and a jelly pop or lollipop which comprises the dosage form. Background to the Invention It is difficult to administer medication of any kind to young children.

There are very few solutions available to parents to allow them to soothe their children's sore scratchy throat when they are suffering from a cough, cold or virus, specifically children between the ages of 1-6 years of age. Due to restrictions placed on the sale of over the counter medicines by regulatory bodies, to children under 6, most medicinal based products were removed for sale for this vulnerable age group The only option they can offer their children is Calpol or Nurofen which are essential to reduce pain and inflammation/temperature, or Glycerine, Lemon & Honey Syrups to act as soothers. However these Glycerine & Honey Syrups are for the most part, ineffective. Glassy lozenges are unsafe for children under 4 as they present a substantial choking hazard.

This vulnerable age group can easily pick up viruses and infections which can cause them to have coughs and irritable, sore throats. Medication isn't always required but a soothing medicament containing calming ingredients can make a happier child. Children are born with an immune system that has not fully developed, and as a result children up to about eight years of age can get up to 8 coughs and colds per year. No other product on the market currently delivers the ability to provide comfort to sore throats and coughs in young children. Natural syrups lack long enough contact with the throat making its effectiveness questionable. Hard glass lollipops, sweets or lozenges pose a choke hazard, and they oflen also contain additives and preservatives that parents and caregivers don't want to administer to children Pain relieving syrups although essential do not act locally at the site of irritation.

There are also particular health challenges for some children which can result in failure to thrive (FTT), faltering growth (FO) or micronutrient deficiencies (MNDs), some of which can have serious long term effects. Once such example is children who receive a diagnosis of Avoidant Restrictive Food Intake Disorder (ARFID), which mainly appears in children with anxiety disorders or who have Autism Spectrum Disorder (ASD). ARFID is characterized by a lack of interest in eating, or avoiding specific types of foods, because of their sensory characteristics. This avoidance results in decreased nutritional intake, eventually causing nutritional deficiencies. In severe cases, ARFID can lead to dependence on oral nutritional supplements, which interferes with psychosocial functioning. A product such as that of the present invention, formulated to address the specific nutritional deficits of this patient cohort, could be a very useful tool in their overall care plan.

Furthermore in the Pharmaceutical, Functional foods and Supplements sectors, dosage forms for the paediatric populations remain a challenge. Traditional dosage forms designed for adult use, such as tablets and capsules, are often not considered appropriate for young children. Crushing tablets, splitting capsules, and mixing with a food (solid or liquid) are well reported as common practices in medical settings, and viewed as a suitable dosage form for Paediatric treatments but not ideal. These practices can create problems for paediatric dosage and the likelihood that the young child may not receive the appropriate dosage.

Object of the Invention It is thus an object of the present invention to provide a jelly based medicament carrier that removes the choke hazard for young children. A further object is to provide a cough and sore throat soother suitable for paediatric personalised patient treatment that does not present a choke hazard. A still further object is to provide a jelly based lollipop for the administration of pharmaceuticals, food supplements or nutraceuticals which is palatable for young children and encourages them to take the medicaments, supplements or the like. Yet another object of the invention is to provide a dosage form which is free of artificial additives or preservatives and which still has unacceptable shelf life.

Summary of the Invention

According to the present invention there is provided a paediatric dosage form suitable to deliver pharmaceuticals, nutraceuticals or food supplements to young children comprising a gel-forming hydrocolloid which has a melting temperature of below about 38 degrees centigrade, and a pharmaceutical, nutraceutical or food supplement, the dosage form having an available water content of less than of less than 2 to 8% by weight at room temperature (20-23°c).

Preferably the available water content is less than 5% at room temperature (20-23°c Or more preferably less than 3% or less than 2% at room temperature (20-23°c).

er activity (or available water) (aw) is the aniCralli of water available to support n (bacteria; yeast and mould) growth. Water activity indicates the amount of water in die total -water content \Old) is a,..,,ailableko microsorganisms. Each species of microorganism (bacteria, yeast and mould) has its own minimum aw value below which growth is no longer possible, oven when the other environmental parameters "e. temperature, nutrient content) are optimal. in this invention the water activity is reduced by making, it unavailable by binding it with the hydroccolid gelatine. Typically Water Activity is measured using an Aw or water activity probe which are commercially available from a variety of suppliers.

The gel-forming hydrocolloid preferably has a melting temperature of below 37 °C. More preferably the melting temperature melting (Tm) temperature is less than 35°c. Preferably the dosage form further comprises a flavouring agent Preferably the hydrocolloid is selected from alginate, pectin, carrageenan, gellan, gelatine, agar, modified starch, methylcellulose, and hydroxypropyl methylcellulose. Particularly preferred is gelatine. The bloom rate of the gelatine is suitably in the range of 170 to 220. Gelatine is sold by its strength, also known as its Bloom value. The Bloom value is a measure of the strength of a gel or gelatin. The Bloom test determines the weight in grams needed by a specified plunger (normally with a diameter of 0.5 inch) to depress the surface of the gel by 4mm 'without breaking it at a specified temperature. Thc. Dumber of grams is called the Bloom value, Gelatin is normally sold at values starting at about 90 Bloom (the weakest) to about 300 Bloom (the strongest). Gelatine is an important industrial gelling biopolymer because of to its ability to form thermally reversible gels when heated with water. Unlike other gels it is thermoreversible at low temperatures, close to body temperature. Gelatine is widely utilized in the food industry to increase the viscosity of aqueous systems such as in dessert formulations and confectionary. Melting points of all Gelatines are in the temperature range of 31.7-34.2 °C. The gel melting (Tm) temperature (<35°C) of Gelatine based products, provide unique organoleptic properties and flavour release at body temperature as the gel begins to melt. Hence Gelatine has unique "melt in the mouth" characteristics, which make it very suitable for use in a lick-able lollipop for young children.

Though all hydrocolloids thicken aqueous dispersions, only a comparatively few gums or hydrocolloids form gels. The important gums that find application in food as gelling agents include alginate, pectin, carrageenan, gellan, gelatine, agar, modified starch, methylcellulose, and hydroxypropyl methylcellulose. The textural properties (e.g., elastic or brittle, long or spreadable, chewy or creamy) of a gel vary widely with the type of hydrocolloid used. The other sensory properties such as opacity, mouth feel and taste also depend on the hydrocolloid employed.

Gelatine offers particularly advantageous properties including the following.

* "Melt-in-mouth" perception that leads to intensive flavour and aroma release * Thermally reversible gel. Some plant hydrocolloids, such as carrageenan and agar, form thermally reversible gels, but melting points are higher than gelatine.

* Surface activity. Although gelatine does not perform as well as gum Arabic, in regard to emulsifying/stabilizing properties, it still has an appropriate surfactant activity.

* Customisation ability. Gelatine is available in different gel strengths and particle sizes.

* Easy to use. Gelatine gels within the pH range typical of foods and does not require salts, sugars or food acid additions to set.

If you heat a gelatine derived gel by putting it in the microwave or into your mouth, the water molecules get excited, and the weak bond is broken. The water molecules float away, and you get liquid water, and therefore the flavour becomes available on the tongue, as is the case in the Soothing Solution pops. The same happens with the bonds between the gelatine chains, breaking down the 3D matrix to form a liquid. So, the gel melts in the mouth at 35-37°c.

Sodium Alginate maybe used as an alternative to Gelatine. However, while Gelatine is considered to have excellent flavour release mainly because it melts in the mouth, Alginate is said to have poor flavour release because it tends to lock up flavours. There are other potential hydrocolloids that could have bene used to form gels, such as Carrageenan, made from seaweed, and Pectin derived from fruit, however they do not melt at such a low temperature and do not provide for the same flavour release or texture. One of the most important features in the invention is the ability to melt on application of the tongue, to ensure that the product is safe for paediatric and infant patients. A solid gel formed by a gelatine complex that will melt at body temperature is less likely to cause immovable obstruction of the windpipe or blockage of the upper airway.

The dosage form of the invention melts safely in the mouth whilst having a firmness that allows a child to work at it long enough to coat the throat and provide the desired soothing relief Suitably the available and free water is reduced by using Fruit concentrates and/or Honey. The Fruit concentrates and the Honey compete for any available water and will bind to the water to form a syrup. The hydrocolloid then serves to lock up remaining available water and form a gel on setting.

A fruit concentrate is made by removing the water from the fruit which effectively concentrates the naturally occurring sugars present in the fruit, including Fructose and Sucrose. The concentration of solids or sugars is measured in Degrees Brix. One degree Brix is 1 gram of sucrose in 100 grams of solution and represents the strength of the solution as a percentage by mass. The concentrates used in the invention have a Brix of 60 to 70%, more suitably about 65 or 65% by weight so that about 65% of the concentrate is made up of sugar solids. In using concentrated fruits, the water added to the recipe is reduced which contributes to the low overall available water. If flavoured water only was used, this would not achieve the same low water availability result, and the texture and shelf-life stability would not be as effective.

Concentrated flavorings could be used or the level of flavorings added could be increased, instead of adding fruit concentrates, however this would provide a dosage form with a softer texture because of the lack the levels of sugar solids provided by the fruit concentrates. This would also affect the overall sensory acceptability of the product, and the Ph., which is important for the acidic fruit flavours and for shelf-life stability. Omitting fruit concentrates for flavorings only, would provide for a loser gel that would not be as manageable to process or pack, and the shelf life would be reduced as the final pH of the product would also be higher. By using fruit concentrates, the dosage form have a higher level of solids and therefore less water content, have a lower Ph., and provide for a more indulgent mouth feel and texture.

Preferably the honey has a Brix of 80 to 82%.

The liquid honey provides for the natural remedy and antibacterial properties of the lollipops. Honey is one the oldest known antibiotics. It is known to contain hydrogen peroxide which accounts for some of its antibacterial properties, hence it is a good remedy for bacterial infections of the throat, for example a Streptococcus throat infection.

The combination of the Honey, Gelatin and Fruit concentrates provides a blend that ensures the lollipops are robust for manufacturing, have good flavor release at body temperature, have a naturally low Ph., contain natural honey remedy properties, and provide for good shelf-life and mouth feel.

The dosage form may also comprise zinc and/or vitamin C, chamomile and/or vitamin A. A dosage form containing honey, fruit concentrate, zinc and vitamin C is desirable because these are important weapons in the fight against infection and actively support immune function.

The invention also provides a lollipop comprising a paediatric dosage form as claimed in any preceding claim.

One of the most important features in the design of the jelly pops formula, is their ability to melt at body temperature thus removing a choke hazard.

The product was formulated for use as an appropriate and safe carrier and dosage delivery system for immune supporting nutraceuticals, whilst providing a naturally soothing remedy for sore throats and coughs for young children.

Brief Description of the Drawings

Figure 1 shows a lollipop of the invention with the paediatric dosage form loaded onto the head region Figure 2 shows the lollipop stick, in the form of a human stick figure before loading with the paediatric dosage form.

Detailed Description of the Drawings

As discussed above an objective of the invention was to add no artificial additives or preservatives into the product Our unique approach to achieve shelf life without preservatives was accomplished by reducing the available water (AW) in the formulation.

The food safety and shelf life of the pops is based around the principles of available water or water activity. Water in food is an important parameter in the field of food science and safety. Due to its unique role in various chemical and biochemical reactions in a food matrix an understanding of water is crucial. One of the oldest forms of preserving foods is drying or desiccation. However, the water content is less important than the specific behaviour of the water or Water Activity (AW).

The free or available water (aw) in a food supports microbial growth, and participates in and supports chemical and enzymatic reactions and spoilage processes. It is this amount of free water which is called water activity or "aw", and it is more important for food stability, chemical and microbial, than the overall total water content. The factors that reduce the mobility of water in a food also reduce its tendency to evaporate and its availability to spoilage microorganisms and enzymes. The rate of certain chemical and biochemical processes are also affected by the amount of available water. One of the effects of reducing the AW in a food product is to reduce the rate of these spoilage reactions. By adding concentrated sugars such as honey and fruit concentrates and by binding the whole mix together with a hydrocolloid such as gelatine, the invention has reduced the available water in the lollipops so much as to limit the growth of spoilage microorganisms and enzyme activity. This approach to reducing the Available Water in the product gives a specific microbiology inside the packaging, extends the shelf life and safety of the product without compromising the product with the addition of artificial additives or preservatives.

The pediatric dosage form was developed with safety in mind. The jelly based carrier is mounted on a stick which is shaped like a human stick figure. The jelly based carrier is loaded onto the head of the figure, the arms of the figure prevent the stick going too far into the child's mouth or being pushed to the back of the throat, and the legs provide a handle for a child to hold. The shape makes it safe for children to use and removes the choke hazard associated with conventional lollipop sticks whilst at the same time providing a fun element for a child. The dimensions and shape of the head are exact in assuring the jelly remains firmly in place.

Example 1

Jelly Lollipop Composition The jelly lollipops can be made in a number of flavours, but the following is a representative base recipe.

Table 1.0 Typical Ingredients present in Jelly Pops NN* 'S\ 'S\ % Leaf Gelatine Honey Water Dry We Wet We Wet Dry

-

Nattiral Apfile Flavour Apple Fruit Concentrate NtrUirtibrie Zinc ":"TotalsH* Table 2 Composition of representative lollipop 0.04 eight.

All % are by * *%**-*'* ........ *'**-*%**%*-*'* ..... ... . .. . . . . .... .... ...... .. . . . . . . . . . . . " ...... . . . . . ... ... .. .. .. ..

Leaf Gelatine Honey Water Raspberry Flavour Raspberry Concentrate Vitamin C Ascorbic acid 99% Vitamin C Totals Zinc Citrate DihYd1rate Nutrition Gracie 3% zinc 100.00 wet 46.71 8.76 Shelf life: Shelf life is defined as the time frame in which a food will remain safe, maintain its quality and comply with food safety and labelling regulations. Samples were analysed from a microbiological and sensory perspective.

The main factors which influence food shelf life include product formulation, the production environment and barrier packaging. Food properties that affect shelf life include such properties as pH, total acidity, water activity, and the presence of natural occurring or added preservatives. The production environmental factors include factors relating to temperature, relative humidity, gaseous atmosphere, and contamination risk. Including any process designed to kill or retard growth of microorganisms such as thermal processing, freezing.

The formulation of the invention contains a high level of soluble solids, attributable mainly to the added fruit concentrates and honey. The Degree Brix is a useful measure employed in the food industry to provide a measure of the level of solids suspended in solution and is an important quality control measure.

The Degree Brix of the kitchen concept jelly pops was typically 52°.

* The honey used in the product development had a typical degree Brix of 82°.

* The fruit juice concentrates had a degree Brix in the range 65 -68°Brix.

* The added water in the formulation was 25%, with a 10-15% cook off.

* The Typical Ph. value for the products was in the range of 3.5-4.0 * The product was fully set by hydrocolloid, there was no unbound or free water available. (Bound water is not available for biological fiinctions) Microbiological Analysis Samples of the Apple flavoured Jelly pops were hot filled into plastic shot glasses and bagged in clear food grade Polythene bags, with no vacuum, and were not hermetically sealed. The samples were incubated at 30 °c to accelerate potential spoilage systems, and stored at 30°c for 1 month. The samples were analysed microbiologically and for sensory analysis after 1 month's incubation at 30°c (crudely equivalent to 3 months ambient storage).

Laboratory Results of Microbiological Analysis on sample Sample Sample Total Count Presumptive Coagulase Positive Mould Yeast Salmonella Listeria D/ Description and no 3000 48hr glucuranidas Enterbaceria Staphylococci cfu / cfu g Cfu / g spp D /ND in ND M23 Codes &Lig M1 e positive ceae du /g g ML M7 M7 The M22 E col' cfu / g M10 M14 Refrigerated, 352 <10 <10 <10 <20 <20 <20 ND ND Incubated 1 month Apple S avoured jelly Popsicle Microbiological Results (after 1 Months incubation summary of results) CMU, W:NAMk\AkaN.a.\\" * \"\.*:"k.,skk\- , To al Viable Counts: 13-glucuronidase positive E.coli Presumptive Enterobacteria Coagulase Positive Staphyloccous IVIoulti Yeast Salinotiella spp D / ND in 25g 11122 Listeria spp 9*' ND in 25g N123 The microbiological analysis conducted after 1 month's incubation demonstrated extremely low microbial counts indicting very minimum microbiological activity. One month's incubation at 30 °c is considered crudely equivalent to 3 months ambient storage.

Sensory Analysis results on Samples: In conjunction with the Microbiological Analysis conducted, Sensory analysis was undertaken on incubated samples. The incubated jelly pops were allowed to temper down to room temperature overnight and then reviewed by a food sensory panel for overall acceptability in terms of Appearance, Aroma, Odours, Taste, and Mouthfeel. The panellists felt the products had not changed and remained stable and remained very acceptable with no detectable off flavours' odours or issues with appearance. Hydrocolloids are widely used in the Food Industry for their theological properties They are most widely employed as thickeners, gelling agents, emulsifiers, stabilisers, fat replacers, and whipping agents. Though all hydrocolloids thicken aqueous dispersions, Ii O. <10 <-20 <20 <20 ND

ND

only a comparatively few gums form gels. The gels thus formed vary widely in gel character and texture. One the most important features in design of the jelly lollipops was their ability to melt on application of the tongue, and to ensure product safety for paediatric and infant patients.

Hydrocolloids including carrageenan, xanthan, guar gum, and pectin could be used in the invention. The use of a gelatine hydrocolloid system in the jelly pops was based on its ability to modify the Theology of the formulations ensuring a fully set jelled product that was suitable and functional for fixing and securing a lollipop stick. Notwithstanding this another important feature in design was the effective reduction of water activity while providing an appropriate and pleasant sensory experience for young children. However, the most important feature of gelatine considered fundamental and critical to design, was Gelatine's low melt temperature. Gelatine melts at much lower temperature than other hydrocolloids and was therefore considered more suitable for use as lollipop designed for consumption by young children, where choking is a possible risk. A solid gel formed by gelatine complex that will melt at body temperature is less likely to cause immovable obstruction of the windpipe or blockage of the upper airway.

Samples of the lollipops that have been frozen were found to be freeze thaw stable. The words "comprises/comprising" and the words "having/including' when used herein with reference to the present invention are used to specify the presence of stated features, integers, steps or components but does not preclude the presence or addition of one or more other features, integers, steps, components or groups thereof.

It is appreciated that certain features of the invention, which are, for clarity, described in the context of separate embodiments, may also be provided in combination in a single embodiment. Conversely, various features of the invention which are, for brevity, described in the context of a single embodiment, may also be provided separately or in any suitable sub-combination.

Claims (3)

1. Claims A a paediatric dosage form in the form of a lollipop, the dosage form being suitable to deliver pharmaceuticals, nutraceuticals or food supplements to young children, the paediatric dosage form comprising a gel-forming hydrocolloid which has a melting temperature of below about 38 degrees centigrade, wherein the hydrocolloid is gelatine, and a pharmaceutical, nutraceutical or food supplement, the dosage form having an available water content of less than 8% by weight at room temperature (20-23°c), and wherein the available and free water is controlled by the addition of fruit concentrates.
2. A paediatric dosage form as claimed in claim 1 wherein the available water content is less than 5% at room temperature (20-23°c).
3. 3. A paediatric dosage form as claimed in claim 1 or 2 wherein the available water content is less than 3% at room temperature (20-23°c).A paediatric dosage form as claimed in any preceding claim wherein the available water content is less than 2% at room temperature (20-23°c) A paediatric dosage form as claimed in any preceding claim wherein the gel-forming hydrocolloid has a melting temperature of below 37 °C, more preferably the melting temperature is less than 35°c.A paediatric dosage form as claimed any preceding claim wherein the melting temperature of the gelatine is in the temperature range of 31.7-34.2 °C.A paediatric dosage form as claimed in any preceding claim wherein the bloom rate of the gelatine is in the range of 1.70 to 2.20.A paediatric dosage form as claimed in any preceding claim further comprising a flavouring agent.A paediatric dosage form as claimed in any preceding claim wherein the available and free water is further controlled by the addition of honey.A paediatric dosage form as claimed in claim 9 wherein the fruit concentrates have a Brix of 60 to 70%.11. A paediatric dosage form as claimed in claim 9 or 10 wherein the honey has a Brix of 80 to 82% 12. A paediatric dosage form as claimed in any preceding claim further comprising zinc and/or vitamin C. 13. A paediatric dosage form as claimed in any preceding claim further comprising chamomile and/or vitamin A.