Novel fast-dissolving tablets
The novel fast-dissolving tablet formulation addresses manufacturing and storage issues of effervescent tablets by using a specific composition that ensures rapid dissolution and uniform dispersion, enhancing usability and stability without special packaging.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- DSM IP ASSETS BV
- Filing Date
- 2021-07-13
- Publication Date
- 2026-07-29
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Effervescent tablets face manufacturing complexity and storage stability issues due to hygroscopic materials, requiring special packaging and handling to prevent moisture absorption, which complicates their production and storage.
A novel fast-dissolving tablet formulation with a composition of 1-40% active ingredient, 20-95% diluent, 2-50% disintegrant, and less than 1% carbonate, designed to dissolve completely in under 4 minutes without special packaging, using common manufacturing processes.
The tablets provide rapid dissolution in aqueous liquids, ensuring complete and uniform dispersion without the need for shaking, improving taste and hydration, and are suitable for individuals with swallowing difficulties, while avoiding the drawbacks of traditional effervescent tablets.
Smart Images

Figure 0007897157000001
Abstract
Description
Detailed Description of the Invention
[0001] The present invention relates to a novel preparation (tablet) containing a physiologically active ingredient that can be rapidly dissolved or dispersed in water (or an aqueous liquid). When this tablet is dissolved, it becomes easily ingestible by humans.
[0002] Numerous preparations for physiologically active ingredients (such as vitamins, minerals, carotenoids, etc.) are known.
[0003] An important and commonly used one is the effervescent tablet (also called a carbon tablet).
[0004] An effervescent tablet or carbon tablet is a tablet that dissolves in water (or an aqueous liquid) and releases carbon dioxide. This type of tablet is a high-density mass produced by compressing the constituent components in powder form and is packaged in a blister pack or using a sealed package in which a desiccant is incorporated in the lid. When in use, it is put into water (or an aqueous liquid) to form a solution.
[0005] Effervescent tablets have several advantages compared to ordinary tablets, such as the following: · Tastes better than ordinary tablets Effervescent tablets can be dissolved in liquids such as water and fruit juice, that is, they often taste better than ordinary tablets, so they are preferred. Conventional tablets dissolve slowly, and as a result, the absorption rate may decrease. On the other hand, effervescent tablets dissolve rapidly and completely, that is, the benefits from the components can be fully enjoyed. · Disperses more uniformly Conventional tablets gradually dissolve in the stomach after ingestion, but may remain undissolved, and in some cases, this may lead to irritation. The advantage of effervescent tablets is that they dissolve completely and uniformly. That is, there is no risk of local deviation of the component concentration. This not only improves the taste but also reduces the possibility of irritation and also means that it is a more efficient means for ingesting the components. · Increases the water intake In addition to providing intended nutritional benefits, effervescent tablets also increase fluid intake. This can be particularly advantageous if you are dehydrated or ill and not drinking as much fluid as usual. Beyond hydration, effervescent tablets can be an excellent way to reap the benefits of any tablet you take, whether it is a dietary supplement or not. • Easily replaces regular tablets. These can be excellent alternatives for individuals who experience difficulty swallowing due to illness or aging. Elderly individuals may have swallowing problems but still need to take medication or nutritional supplements regularly, and in this regard, effervescent tablets may be far easier than swallowing tablets. • Measurement is simple and easy. Effervescent tablets dissolve easily in water or your preferred liquid, and after a short wait, they mix thoroughly and are ready to drink. On the other hand, conventional tablets or powders require measuring and mixing, and repeated stirring to avoid a drink with many granular clumps and an uneven consistency.
[0006] Effervescent tablets, which combine all of these elements, are a very popular choice for people who take tablets for nutritional supplementation or medicinal purposes.
[0007] While effervescent tablets offer these advantages, they also have several significant drawbacks, including a complex manufacturing process (using very low relative humidity) and, in many cases, the need for special packaging materials to achieve good storage stability.
[0008] The main materials used in the manufacture of effervescent tablets are relatively hygroscopic, meaning they easily absorb moisture from the air. However, this moisture triggers the effervescence reaction, which must be prevented. One basic strategy to overcome this problem is to use a completely sealed material handling system during manufacturing.
[0009] Furthermore, the tablets must be packaged in a way that prevents them from being damaged by moisture during storage before use.
[0010] Therefore, the objective of the present invention was to find a soluble formulation that has all the advantages of well-known typical effervescent tablets but without their disadvantages.
[0011] Therefore, the present invention relates to a novel type of effervescent tablet, a fast (water) dissolvable effervescent beverage tablet (DS), which is: (a) At least one active ingredient is present in an amount of 1 to 40% by weight (wt%) based on the total weight of the rapid-dissolving tablets. (b) At least one diluent is added in an amount of 20-95 wt% based on the total weight of the fast-dissolving tablets, (c) At least one disintegrant, in an amount of 2-50 wt% based on the total weight of the rapid-dissolving tablet, This relates to tablets containing [specific ingredient], where the content of any carbonate is less than 1 wt% based on the total weight of the fast-dissolving tablet.
[0012] The rapidly dissolving tablets according to the present invention must be dissolved in water (or an aqueous liquid) before ingestion. This means that the tablets are not swallowed in their raw state.
[0013] All percentages (in one embodiment of the tablet according to the present invention) always add up to 100.
[0014] The tablets according to the present invention exhibit excellent dissolution rate. They dissolve in aqueous liquids at the same rate as effervescent tablets. There is no need to add shaking, stirring, or other means to ensure complete dissolution within an acceptable time.
[0015] The tablets according to the present invention can have various sizes.
[0016] This size is approximately the same as that of conventional effervescent tablets. A typical and preferred size is usually selected so that the amount of the bioactive ingredient is sufficient to meet the recommended daily dose or any desired dose.
[0017] The shape of the tablet according to the present invention is not an essential feature. However, it typically has a disc-like shape with a diameter of 3 cm or less (preferably 1.5 to 2.5 cm) and a thickness of 0.8 cm or less (preferably 0.3 to 0.6 cm), and a weight of 5 g or less (preferably 0.2 to 5 g).
[0018] Therefore, the present invention relates to a fast-dissolving tablet DS1 having a disc-shaped fast-dissolving tablet.
[0019] Therefore, the present invention relates to a rapid-dissolving tablet DS1', which is a rapid-dissolving tablet DS1 having a diameter of 3 cm or less (preferably 1.5 to 2.5 cm) and a thickness of 0.8 cm or less (preferably 0.3 to 0.6 cm).
[0020] Therefore, the present invention relates to a rapid-dissolving tablet DS2, which is a rapid-dissolving tablet DS, DS1, or DS1' having a weight of 5g or less (preferably 0.2 to 5g).
[0021] Typically, the tablets according to the present invention are dissolved or dispersed in a glass of water (or an aqueous liquid), usually 0.1 to 0.4 liters.
[0022] The tablets according to the present invention dissolved rapidly. Their dissolution characteristics were the same as those of ordinary effervescent tablets.
[0023] The dissolution time is less than 4 minutes (or even less than 2 minutes).
[0024] The tablets according to the present invention are soluble in both pure water and aqueous solvents. In other words, the tablets according to the present invention can be dissolved in any aqueous liquid (fruit juice, milk, smoothie, etc.). The liquid may be at low or high temperatures. The liquid may be carbonated or non-carbonated.
[0025] According to a preferred embodiment of the present invention, the instant dissolving tablet contains at least one active ingredient at 5 to 30 wt% based on the total weight of the instant dissolving tablet.
[0026] According to a more preferred embodiment of the present invention, the instant dissolving tablet contains at least one active ingredient at 5 to 20 wt% based on the total weight of the instant dissolving tablet.
[0027] According to a particularly preferred embodiment of the present invention, the instant dissolving tablet contains at least one active ingredient at 7 to 15 wt% based on the total weight of the instant dissolving tablet.
[0028] Therefore, the present invention relates to an instant dissolving tablet DS3, which is instant dissolving tablet DS, DS1, DS1' or DS2 containing at least one active ingredient at 5 to 30 wt% based on the total weight of the instant dissolving tablet.
[0029] Therefore, the present invention relates to an instant dissolving tablet DS3', which is instant dissolving tablet DS, DS1, DS1' or DS2 containing at least one active ingredient at 5 to 20 wt% based on the total weight of the instant dissolving tablet.
[0030] Therefore, the present invention relates to an instant dissolving tablet DS3'', which is instant dissolving tablet DS, DS1, DS1' or DS2 containing at least one active ingredient at 7 to 15 wt% based on the total weight of the instant dissolving tablet.
[0031] The active ingredients used in the tablets according to the present invention are those commonly used in general effervescent tablets.
[0032] Suitable active ingredients are vitamins, prebiotics, probiotics, carotenoids, minerals and any other dietary ingredients.
[0033] Therefore, the present invention relates to an instant dissolving tablet DS4, which is instant dissolving tablet DS, DS1, DS1', DS2, DS3, DS3' or DS3'' wherein the at least one active ingredient is selected from the group consisting of vitamins, prebiotics, probiotics, carotenoids, minerals and any other food ingredients.
[0034] The active ingredients used in the tablets according to the present invention may be used in their pure form or in a preformulated form (meaning that one or more active ingredients are combined before being used in the manufacture of the tablets according to the present invention).
[0035] The vitamins according to the present invention may be fat-soluble or water-soluble.
[0036] Fat-soluble vitamins are selected from the group consisting of vitamins A, D, E, and K. These vitamins are usually used in a pre-formulated state in tablets so that they can be dispersed in water in a pre-formulated state.
[0037] Water-soluble vitamins are selected from the group consisting of vitamin B1 (thiamine), vitamin B2 (riboflavin), vitamin B3 (niacin, niacinamide), vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine, pyridoxamine, pyridoxal), vitamin B7 (biotin), vitamin B9 (folic acid, folic acid), vitamin B12 (cyanocobalamin, hydroxycobalamin, methylcobalamin), and vitamin C (ascorbic acid).
[0038] Prebiotics are typically any commonly used dietary fiber (such as inulin).
[0039] Probiotics are, in other words, bacteria of the Lactobacillus or Bifidobacterium genera.
[0040] Carotenoids are selected from the group consisting of β-carotene, lycopene, lutein, bixin, astaxanthin, apocarotenal, β-apo-8'-carotenal, β-apo-12'-carotenal, canthaxanthin, cryptoxanthin, citranaxanthin, and zeaxanthin. These carotenoids are usually used in tablets in a pre-formulated state.
[0041] The minerals are selected from the group consisting of sodium, potassium, calcium, iron, zinc, and magnesium, which are added to the preparation.
[0042] A suitable trace element is, for example, iodine.
[0043] Therefore, the present invention provides that at least the active ingredient is a vitamin selected 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; and / or carotenoids selected from the group consisting of β-carotene, lycopene, lutein, bixin, astaxanthin, apocarotenal, β-apo-8'-carotenal, β-apo-12'-carotenal, canthaxanthin, cryptoxanthin, citranaxanthin and zeaxanthin; and / or Inulin; and / or Probiotics selected from the group consisting of Lactobacillus and Bifidobacterium; and / or Minerals selected from the group consisting of sodium, potassium, calcium, iron, zinc, and magnesium; The present invention relates to a rapid-dissolving tablet DS5, which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', or DS4, selected from the group consisting of and / or any other food component (such as trace elements or plant extracts).
[0044] A preferred embodiment of the present invention is a fast-dissolving tablet containing at least one diluent in an amount of 25 to 90 wt% based on the total weight of the fast-dissolving tablet.
[0045] A more preferred embodiment of the present invention is a fast-dissolving tablet containing at least one diluent in an amount of 30-80 wt% based on the total weight of the fast-dissolving tablet.
[0046] Suitable diluents include sugar alcohols such as mannitol, sorbitol, and xylitol, and disaccharides such as sucrose or lactose.
[0047] Accordingly, the present invention relates to a rapid-dissolving tablet DS6, which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, or DS5, containing at least one diluent in an amount of 25 to 90 wt% based on the total weight of the rapid-dissolving tablet.
[0048] Therefore, the present invention relates to a rapid-dissolving tablet DS6', which is a rapid-dissolving tablet DS6 containing at least one diluent in an amount of 30 to 80 wt% based on the total weight of the rapid-dissolving tablet.
[0049] Suitable diluents include sugar alcohols such as mannitol, sorbitol, and xylitol, and disaccharides such as sucrose or lactose.
[0050] Accordingly, the present invention relates to a rapid-dissolving tablet DS7, wherein at least one diluent is selected from the group consisting of sugar alcohols (such as mannitol, sorbitol, and xylitol) and disaccharides (such as sucrose and lactose), and is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, or DS6'.
[0051] A preferred embodiment of the present invention is a fast-dissolving tablet containing at least one disintegrant in an amount of 3 to 45 wt% based on the total weight of the fast-dissolving tablet.
[0052] A more preferred embodiment of the present invention is a fast-dissolving tablet containing at least one disintegrant in an amount of 15 to 40 wt% based on the total weight of the fast-dissolving tablet.
[0053] Suitable disintegrants include starch, crospovidone (cross-linked polyvinyl N-pyrrolidone), sugar alcohols co-treated with starch, and sodium starch glycolate.
[0054] Accordingly, the present invention relates to a rapid-dissolving tablet DS8, which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', or DS7, containing at least one disintegrant in an amount of 10 to 45 wt% based on the total weight of the rapid-dissolving tablet.
[0055] Accordingly, the present invention relates to a rapid-dissolving tablet DS8' which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', or DS7, containing at least one disintegrant in an amount of 15 to 40 wt% based on the total weight of the rapid-dissolving tablet.
[0056] Accordingly, the present invention relates to a rapid-dissolving tablet DS9, wherein at least one disintegrant is selected from the group consisting of starch, crospovidone (cross-linked polyvinyl N-pyrrolidone), sugar alcohols co-treated with starch, and sodium starch glycolate, and is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', DS7, DS8, or DS8'.
[0057] Furthermore, the tablets according to the present invention may contain additional ingredients (auxiliaries) such as flavorings, colorings, excipients (fillers), lubricants, and sweeteners. While these ingredients are not essential to the present invention, they are useful in the design of the tablets and in achieving the desired purpose of the tablets.
[0058] This type of component can be present in the tablet according to the present invention in an amount of up to 20 wt% based on the total weight of the tablet.
[0059] When these are used, they are typically present in an amount of 2-20 wt% (preferably 3-15 wt%) based on the total weight of the tablet.
[0060] Accordingly, the present invention relates to a rapid-dissolving tablet DS10, which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', DS7, DS8, DS8', or DS9, comprising at least one excipient selected from the group consisting of fragrances, colorants, excipients, lubricants, and sweeteners.
[0061] Therefore, the present invention relates to a rapid-dissolving tablet DS10', which is a rapid-dissolving tablet DS10 containing at least one excipient in an amount of 2 to 20 wt% (preferably 3 to 15 wt%) based on the total weight of the tablet.
[0062] Furthermore, a preferred embodiment of the present invention is a tablet in which the carbonate content is less than 0.5 wt% based on the total weight of the tablet.
[0063] A more preferred embodiment of the present invention is a tablet in which the carbonate content is less than 0.3 wt% based on the total weight of the tablet.
[0064] A particularly preferred embodiment of the present invention is a tablet that is essentially free of carbonates. This means that the tablet does not contain carbonates. This means that no carbonates are added to the tablet.
[0065] Accordingly, the present invention relates to a rapid-dissolving tablet DS11, which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', DS7, DS8, DS8', DS9, DS10, or DS10', containing less than 0.5 wt% of carbonate based on the total weight of the tablet.
[0066] Accordingly, the present invention relates to a rapid-dissolving tablet DS11', which is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', DS7, DS8, DS8', DS9, DS10, or DS10', containing less than 0.3 wt% of carbonate based on the total weight of the tablet.
[0067] Accordingly, the present invention relates to a rapid-dissolving tablet DS11'' which is essentially carbonate-free, and is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', DS7, DS8, DS8', DS9, DS10, or DS10'.
[0068] The tablets according to the present invention can be manufactured using a generally known process.
[0069] Typically, the following steps are used: (i) Mix all ingredients (except lubricant) and blend them together. (ii) Add the lubricant and mix all the ingredients together. (iii) Compress the mixture into the desired tablet form.
[0070] This compression molding can be carried out using commonly known and commonly used equipment, such as a "D" type rotary compression molding machine.
[0071] The preferred and ideal hardness of the tablet according to the present invention is approximately 5 kp to 20 kp, preferably 6 kp to 15 kp.
[0072] Accordingly, the present invention relates to a rapid-dissolving tablet DS12, which is essentially carbonate-free, and is a rapid-dissolving tablet DS, DS1, DS1', DS2, DS3, DS3', DS3'', DS4, DS5, DS6, DS6', DS7, DS8, DS8', DS9, DS10, DS10', DS11, DS11', or DS11''.
[0073] The tablets can be used as a dietary supplement (depending on the selection of the active ingredient).
[0074] The tablets can be packaged and sold in any commonly used tablet container to ensure good storage stability.
[0075] The tablets according to the present invention are dissolved or dispersed in water or an aqueous liquid before being ingested.
[0076] The following examples are helpful in illustrating the present invention.
[0077] [Examples] [Example 1] Tablets with the following composition (Table 1) were manufactured.
[0078] [Table 1]
[0079] Tablets having the composition shown in Table 1 were manufactured according to the following procedure: 1. Sieve all components using a 20-mesh sieve. 2. Mix all ingredients except the lubricant in a V-type blender for 10 minutes. 3. Add the sieved lubricant to step 2 and mix for 5 minutes. 4. Tablets are manufactured using a "D" type rotary compression molding machine fitted with a 0.875-inch corner-plane pestle. Compression force: 6000 lbs, compression speed: 55 rpm, tablet hardness: approximately 7 kp.
[0080] The tablet was placed in approximately 236 ml (8 ounces) of water and gently shaken. The tablet dissolved rapidly and completely within 2 minutes. Further embodiments are as follows: [Embodiment 1] A rapidly dissolving effervescent tablet for beverages, (a) At least one active ingredient, in an amount of 1 to 40% by weight (wt%) based on the total weight of the rapid-dissolving tablets, (b) At least one diluent is added in an amount of 20-95 wt% based on the total weight of the rapid-dissolving tablets, (c) At least one disintegrant, in an amount of 2 to 50 wt% based on the total weight of the rapid-dissolving tablet, Includes, A tablet in which the content of any carbonate is less than 1 wt% based on the total weight of the rapid-dissolving tablet. [Embodiment 2] The tablet is the tablet according to Embodiment 1, having a disc shape. [Embodiment 3] A tablet according to Embodiment 1 or 2, comprising at least one active ingredient in an amount of 5 to 30 wt% based on the total weight of the rapid-dissolving tablet. [Embodiment 4] The tablet according to any one of Embodiments 1 to 3, wherein the at least one active ingredient is selected from the group consisting of vitamins, prebiotics, probiotics, carotenoids, minerals, and other arbitrary food components. [Embodiment 5] A tablet according to any one of Embodiments 1 to 4, comprising at least one diluent in an amount of 25 to 90 wt% based on the total weight of the rapid-dissolving tablet. [Embodiment 6] The tablet according to any one of Embodiments 1 to 5, wherein the at least one diluent is selected from the group consisting of sugar alcohols (such as mannitol, sorbitol, and xylitol) and disaccharides (such as sucrose and lactose). [Embodiment 7] A tablet according to any one of Embodiments 1 to 6, comprising at least one disintegrant in an amount of 10 to 45 wt% based on the total weight of the rapid-dissolving tablet. [Embodiment 8] The tablet according to any one of Embodiments 1 to 7, wherein the at least one disintegrant is selected from the group consisting of starch, crospovidone (cross-linked polyvinyl N-pyrrolidone), sugar alcohols co-treated with starch, and sodium starch glycolate. [Embodiment 9] The tablet according to any one of Embodiments 1 to 8, wherein the tablet contains at least one excipient selected from the group consisting of flavorings, colorings, excipients, lubricants, and sweeteners. [Embodiment 10] The tablet according to any one of Embodiments 1 to 9, wherein the carbonate content is less than 0.5 wt% based on the total weight of the tablet. [Embodiment 11] The tablet is a tablet according to any one of embodiments 1 to 10, which is essentially free of carbonates. [Embodiment 12] The tablet is the tablet according to any one of Embodiments 1 to 11, wherein the hardness is approximately 5 to 20 kp.
Claims
1. A fast-dissolving tablet for drinking, (a) At least one active ingredient selected from the group consisting of vitamins, dietary fiber, probiotics, carotenoids, minerals, trace elements, and plant extracts, in an amount of 7 to 30% by weight (wt%) based on the total weight of the rapid-dissolving tablets. (b) At least one diluent selected from the group consisting of sugar alcohols and disaccharides, in an amount of 20 to 95 wt% based on the total weight of the rapid-dissolving tablets, (c) At least one disintegrant selected from the group consisting of starch, crospovidone (cross-linked polyvinyl N-pyrrolidone), sugar alcohols co-treated with starch, and sodium starch glycolate, in an amount of 10 to 45 wt% based on the total weight of the rapid-dissolving tablet. Includes, The content of any carbonate is less than 0.5 wt% based on the total weight of the rapid-dissolving tablets. The aforementioned rapid-dissolving tablets are dissolved or dispersed in water or an aqueous liquid before being ingested. The hardness of the aforementioned fast-dissolving tablets is 6 kp to 15 kp. The rapid-dissolving tablet has a diameter of 1.5 cm to 2.5 cm and a thickness of 0.8 cm or less.
2. The rapid-dissolving tablet according to claim 1, wherein the rapid-dissolving tablet has a disc-shaped form.
3. The rapid-dissolving tablet according to claim 1 or 2, wherein the diameter of the rapid-dissolving tablet is 2.2225 cm to 2.5 cm.
4. The rapid-dissolving tablet according to any one of claims 1 to 3, wherein the time it takes for the rapid-dissolving tablet to dissolve or disperse in water or an aqueous liquid is less than 4 minutes.
5. The rapid-dissolving tablet according to any one of claims 1 to 4, comprising 25 to 90 wt% of the above-mentioned diluent based on the total weight of the rapid-dissolving tablet.