Patent Application
20230398079
The present invention relates to a new formulation (a tablet) comprising Human Milk Oligosaccharides (HMOs), which dissolves or can be dispersed in water (or water based liquids) fast. The tablets are when dissolved can be consumed easily by a human.
HMOs are often used in infant formula. There are many other known formulations for HMOs (powders, tablets, capsules etc).
The present invention relates to new way to deliver HMOs. The form is a specific non-effervescent fast dissolvable tablet.
Effervescent or carbon tablets are tablets which dissolve in water (or water based liquids) and release carbon dioxide. Such tablets are products of compression of component ingredients in the form of powders into a dense mass, which is packaged in blister pack, or with a hermetically sealed package with incorporated desiccant in the cap. To use them, they are dropped into water (or water-based liquids) to make a solution.
Effervescent tablets have some advantages over regular tablets, such as the following:
Pleasant Taste Compared to Regular Tablets
Distributed More Evenly
Increased Liquid Intake
Easy Alternative to Regular Tablets
Simple and Easy to Measure
All these factors combine to make effervescent tablets a very popular choice for those taking tablets for either dietary supplementation or medicinal reasons.
Besides these advantages, there are also some major disadvantages of effervescent tablets, such as a complex production process and, very often, the need for special packaging materials for achieving a good storage stability.
The primary material used in the manufacture of effervescent tablets is relatively hygroscopic, that is, it absorbs moisture from the air. However, this must be prevented because it will initiate the effervescent reaction. One of the principle strategies used to overcome this problem is a completely closed material handling system during production,
Furthermore, the tablets need to be packed in such a way that it that moisture cannot harm the tablet during storage before use.
Therefore, the present invention relates to a non-effervescent (water) fast dissolvable tablet (DS), which comprises
All percentages are always added up to 100 in total (in one embodiment of a tablet according to the present invention).
The dissolution rate of the tablet according to the present invention is excellent. The tablet according to the present invention dissolves in a water-based liquid in similar rate as an effervescent tablet. No additional vigorous shaking, stirring or other means are necessary to achieve a complete dissolution in an acceptable time.
The size of the tablet according to the present invention can vary.
The size is more or less the same as a conventional effervescent tablet. The typical and preferred size is usually chosen that the amount of the HMOs and of any other used physiologically active ingredient is enough to cover the daily recommended or any desired amount.
The shape of the tablet according to the present invention is not an essential feature. But usually it has a disc-like shape having a diameter of up to 3 cm (preferably 1.5-2.5 cm) and a thickness of up to 0.8 cm (preferably 0.3-0.6 cm) and it has a weight of up to 5 g (preferably 0.2-5 g).
Therefore the present invention relates to a fast dissolvable tablet DS1, which is fast dissolvable tablet DS, wherein the tablet has a disc-like shape.
Therefore the present invention relates to a fast dissolvable tablet DS1′, which is fast dissolvable tablet DS1, wherein the tablet has a diameter of up to 3 cm (preferably 1.5-2.5 cm) and a thickness of up to 0.8 cm (preferably 0.3-0.6 cm).
Therefore the present invention relates to a fast dissolvable tablet DS2, which is fast dissolvable tablet DS, DS1 or DS1′, wherein the tablet has a weight of up to 5 g (preferably 0.2-5 g).
Usually the tablet according to the present invention is dissolved or dispersed in a glass of water (or water based liquid), which is usually between 0.1-0.4 liter.
The tablets according to the present invention dissolved rapidly. It has similar dissolving properties as a usual effervescent tablets.
The dissolving time is less than 4 minutes (or even less than 2 minutes).
The tablet according to the present invention is soluble in pure water as well as in water-based solvents. This means the tablet according to the present invention can also be dissolved in any water based liquid (such as fruit juices, milk, smoothies, etc). The liquid can be cold or hot. The liquid can be carbonated or non-carbonated.
Preferred embodiments according to the present inventions are fast dissolvable tablets comprises 0.1-40 wt-%, based on the total weight of the fast dissolvable tablet, of at least one HMO.
More preferred embodiments according to the present inventions are fast dissolvable tablets comprises 5-35 wt-%, based on the total weight of the fast dissolvable tablet, of at least one HMO.
Especially preferred embodiments according to the present inventions are fast dissolvable tablets comprises 10-35 wt-%, based on the total weight of the fast dissolvable tablet, of at least one HMO.
Therefore the present invention relates to a fast dissolvable tablet DS3, which is fast dissolvable tablet DS, DS1, DS1′ or DS2, wherein the tablet comprises 0.1-50 wt-%, based on the total weight of the fast dissolvable tablet, of at least one HMO.
Therefore the present invention relates to a fast dissolvable tablet DS3′, which is fast dissolvable tablet DS, DS1, DS1′ or DS2, wherein the tablet comprises 5-35 wt-%, based on the total weight of the fast dissolvable tablet, of at least one HMO.
Therefore the present invention relates to a fast dissolvable tablet DS3″, which is fast dissolvable tablet DS, DS1, DS1′ or DS2, wherein the tablet comprises 10-35 wt-%, based on the total weight of the fast dissolvable tablet, of at least one HMO.
Human milk oligosaccharides (HMOs) are a family of structurally diverse unconjugated glycans that are highly abundant in and unique to human milk. Originally, HMOs were proposed to be prebiotic “bifidus factors,” or human milk glycans found to promote growth in Bifidobacterial species of the gut and found uniquely in the stool of breast fed infants compared to formula fed infants.
HMOs are composed of the five monosaccharides glucose (Glc), galactose (Gal), N-acetylglucosamine (GlcNAc), fucose (Fuc) and sialic acid (Sia), with N-acetylneuraminic acid (Neu5Ac) as the predominant if not only form of Sia. More than two hundred different HMOs have been identified so far. The most important ones are 2′-fucosyllactose (2′ FL), lacto-N-neotetraose (LNnT), 3-fucosyllactose (3FL), difucosyllactose (DFL), Lacto-N-fucopentaose I (LNFP I), 3″Sialyllactose Sodium Salt (3′SL), 6″Sialyllactose Sodium Salt (6′SL), and Lacto-N-Tetraose (LNT).
HMOs can be isolated from breast milk or they can be produced chemically or biochemically. HMOs are available commercially from a variety of producers.
For the purpose of the present invention the source of the HMO is not essential. It is clear that HMOs from different sources can be used.
Therefore the present invention relates to a fast dissolvable tablet DS4, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, or D53″, wherein the at least one HMO is chosen from the group consisting of 2′-fucosyllactose (2′ FL), lacto-N-neotetraose (LNnT), 3-fucosyllactose (3FL), difucosyl-lactose (DFL), Lacto-N-fucopentaose I (LNFP I), 3″Sialyllactose Sodium Salt (3′SL), 6″Sialyllactose Sodium Salt (6′SL), and Lacto-N-Tetraose (LNT).
It is also possible to add other active ingredient to the tablet according to the present invention. Such active ingredients are usually used in common effervescent tablets.
Such suitable additional active ingredients are vitamins, carotenoids, minerals, and any other dietary ingredient.
Therefore the present invention relates to a fast dissolvable tablet DS5, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, or D53″ or DS4, wherein the tablet according to the present invention can also comprise at least one additional active ingredient.
Therefore the present invention relates to a fast dissolvable tablet DS5′, which is fast dissolvable tablet DS5, wherein the additional active ingredient is chosen from the group consisting of vitamins, carotenoids, minerals, and any other dietary ingredient.
The amount of the additional active ingredient can be up to 25 wt-%, based on the total weight of the fast dissolvable tablet (usually up to 15 wt-%).
The active ingredients used in the tablet according to the present invention can be used in pure form as well as in preformulated form (which means that one or more active ingredient is formulated before used in the production of the tablet according to the present invention).
The vitamins according to the present invention can be fat-soluble as well as water-soluble.
The fat-soluble vitamins are selected from the group consisting of vitamin A, D, E and K. These vitamins are usually used as preformulated form in the tablet.
The water-soluble vitamins are selected from the group consisting of vitamin B1 (thia-mine), vitamin B2 (riboflavin), vitamin B3 (niacin, niacinamide), vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine, pyridoxamine, pyridoxal), vitamin B7 (biotin), vitamin B9 (folic acid, folinic acid), vitamin B12 (cyanocobalamin, hydroxycobalamin, methylcobalamin), and vitamin C (ascorbic acid).
Carotenoids are chosen form the group consisting of beta-carotene, lycopene, lutein, bixin, astaxanthin, apocarotenol, beta-apo-8′-carotenal, beta-apo-12′-carotenal, canthaxanthin, cryptoxanthin, citranaxanthin and zeaxanthin. These carotenoids are usually used as preformulated form in the tablet.
The minerals are chosen from the group consisting of minerals, which are added to the formulation are Sodium, Potassium, Calcium, Iron, Zinc, and Magnesium.
A suitable trace element is for example iodine.
Therefore the present invention relates to a fast dissolvable tablet DS6, which is the fast dissolvable tablet DS5 or DS5′, wherein the at least active ingredient is chosen from the group consisting of vitamins chosen from the group consisting of vitamin A, vitamin D (vitamin D3), vitamin E, vitamin K1, vitamin K2, vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, vitamin B12, and vitamin C;
A preferred embodiment of the present invention is as fast dissolvable tablet comprising 25-90 wt-%, based on the total weight of the fast dissolvable tablet, of at least one diluent.
A more preferred embodiment of the present invention is as fast dissolvable tablet comprising 30-80 wt-%, based on the total weight of the fast dissolvable tablet, of at least one diluent.
Suitable diluents are sugar alcohols such as mannitol, sorbitol, xylitol and disaccharides such as sucrose or lactose.
Therefore the present invention relates to a fast dissolvable tablet DS7, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS5′ or DS6, wherein the tablet comprises 25-90 wt-%, based on the total weight of the fast dissolvable tablet, of at least one diluent.
Therefore the present invention relates to a fast dissolvable tablet DS7′, which is fast dissolvable tablet DS7, wherein the tablet comprises 30-80 wt-%, based on the total weight of the fast dissolvable tablet, of at least one diluent.
Suitable diluents are sugar alcohols such as mannitol, sorbitol, xylitol and disaccharides such as sucrose or lactose.
Therefore the present invention relates to a fast dissolvable tablet DS8, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS5′, DS6, DS7 or DS7′, wherein the least one diluent is chosen from the group consisting of sugar alcohols (such as mannitol, sorbitol and xylitol) and disaccharides (such as sucrose and lactose).
A preferred embodiment of the present invention is as fast dissolvable tablet comprising 3-45 wt-%, based on the total weight of the fast dissolvable tablet, of at least one disintegrant.
A more preferred embodiment of the present invention is as fast dissolvable tablet comprising 15-40 wt-%, based on the total weight of the fast dissolvable tablet, of at least one disintegrant.
Suitable disintegrant are starch, crospovidone (cross linked polyvinyl N-pyrrolidone), co-processed sugar alcohol with starch, croscarmellose Sodium, and sodium starch glycolate.
Therefore the present invention relates to a fast dissolvable tablet DS9, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS5′, DS6, DS7, DS7′, or DS8, wherein the tablet comprises 10-45 wt-%, based on the total weight of the fast dissolvable tablet, of at least one disintegrant.
Therefore the present invention relates to a fast dissolvable tablet DS9′, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS5′, DS6, DS7, DS7′ or DS8, wherein the tablet comprises 15-40 wt-%, based on the total weight of the fast dissolvable tablet, of at least one disintegrant.
Therefore the present invention relates to a fast dissolvable tablet DS10, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS5′, DS6, DS7, DS7′, DS8, DS9 or DS9′, wherein the at least one disintegrant is chosen from the group consisting of starches, crospovidone (cross linked polyvinyl N-pyrrolidone), co-processed sugar alcohol with starch, croscarmellose Sodium, and sodium starch glycolate.
Furthermore the tablet according to the present invention can comprise further ingredients (auxiliary agents), such as flavours, colours, fillers, lubricants, and sweeteners. These ingredients are not essential for the invention, but they are useful to design a tablet, which is useful for the desired aim of the tablet.
Such ingredients can be present in the tablets according to the present invention in amount of up to 15 wt-%, based on the total weight of the tablet.
Usually when they are used they are present in an amount of 2-15 wt-% (preferably 3-12 wt-%), based on the total weight of the tablet.
Therefore the present invention relates to a fast dissolvable tablet DS11, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS5′, DS6, DS7, DS7′, DS8, DS9, DS9′ or DS10, wherein the tablet comprises at least one auxiliary agent chosen from the group consisting of, flavours, colours, fillers, lubricants and sweetener.
Therefore the present invention relates to a fast dissolvable tablet DS11′, which is fast dissolvable tablet DS11, wherein the tablet comprises 2-15 wt-% (preferably 3-12 wt-%), based on the total weight of the tablet, of at least one auxiliary agent.
Furthermore a preferred embodiment of the present invention is a tablet, wherein the carbonate content is below 0.5 wt-%, based on the total weight of the tablet.
A more preferred embodiment of the present invention is a tablet, wherein the carbonate content is below 0.3 wt-%, based on the total weight of the tablet.
Especially preferred embodiment of the present invention is a tablet which is essentially free of any carbonate. This means that the tablet does not comprise any carbonate. This means that no carbonate is added to the tablet.
Therefore the present invention relates to a fast dissolvable tablet DS12, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS6, DS6′, DS7, DS8, DS8′, DS9, DS10, DS10′ or DS11, wherein the tablet comprises less than 0.5 wt-%, based on the total weight of the tablet, of carbonate.
Therefore the present invention relates to a fast dissolvable tablet DS12′, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, D53″, DS4, DS5, DS6, DS6′, DS7, DS8, DS8′, DS9, DS10, DS10′ or DS11, wherein the tablet comprises less than 0.3 wt-%, based on the total weight of the tablet, of carbonate.
Therefore the present invention relates to a fast dissolvable tablet DS12″, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, DS3″, DS4, DS5, DS6, DS6′, DS7, DS8, DS8′, DS9, DS10, DS10′ or DS11, wherein the tablet is essentially free of any carbonate.
The tablets according to the present invention can be produced by using commonly known processes.
Usually the following process steps are used
The pressing can be done by commonly known and used equipment, such as a “D” type rotary press.
A suitable and ideal tablet according to the present invention has a hardness of around 5 kp to 20 kp, preferably 5 kp-15 kp.
Therefore the present invention relates to a fast dissolvable tablet DS13, which is fast dissolvable tablet DS, DS1, DS1′, DS2, DS3, DS3′, DS3″, DS4, DS5, DS6, DS6′, DS7, DS8, DS8′, DS9, DS10, DS10′ or DS11, DS12, DS12′ or DS12″, wherein the tablet is essentially free of any carbonate.
The tablet (depending on the choice of active ingredients) can be used as dietary supplements.
The tablets can be packed and sold in any commonly used container for tablet, due to the good storage stability.
The following examples serve to illustrate the invention.
Tablets of the following compositions (table 1 and Table 2) has been produced:
The tablets with the composition of table 1 and table 2 and has been produced by the following procedure:
Compression force 2000-3500 PSI, Tablet hardness 6-9 kp
This tablet has been dropped in about 236 ml (8 oz) of water and was shaken gently.
The tablet was dissolved rapidly and completely within 2 mins.
Tablets of the following compositions (table 3 and table 4) have been produced:
The tablets with the composition of table 3 and table 4 and has been produced by the following procedure:
Table 3 example: Compression force 6000 Lbs, Tablet hardness ˜8 kp, 48 rpm
Table 4 example: Compression force 4000 Lbs, Tablet hardness ˜6 kp, 48 rpm
This tablet has been dropped in about 236 ml (8 oz) of water and was shaken gently.
The tablet was dissolved rapidly and completely within 2 mins.
| Number | Date | Country | Kind |
|---|---|---|---|
| 01434/20 | Nov 2020 | CH | national |
| Filing Document | Filing Date | Country | Kind |
|---|---|---|---|
| PCT/EP2021/079454 | 10/25/2021 | WO |
| Number | Date | Country | |
|---|---|---|---|
| 63107650 | Oct 2020 | US |
