EXPANDABLE MICROCAPSULE
20220079885 · 2022-03-17
Inventors
Cpc classification
A61K9/50
HUMAN NECESSITIES
International classification
Abstract
An expandable microcapsule, which includes a core layer consisting of 300 parts by weight of foaming agent, 250 parts by weight of polymer water-absorbing material and 60 parts by weight of core layer lubricant, wherein the foaming agent has characteristics of reacting with water to generate gas; and a coating layer covering the surface of the core layer to form a granular structure, wherein the coating layer is consisting of 10% to 40% by weight of edible water-absorbent colloid, 5% to 40% by weight of functional health food additives, 2% to 30% by weight of emulsifier, 4% to 15% by weight of coating layer lubricant and 5% to 40% by weight of film coating composition, and wherein the film coating composition has characteristics of resistance to gastric acid decomposition and being decomposed only in the intestinal tract.
Claims
1. An expandable microcapsule, comprising: a core layer consisting of 300 parts by weight of foaming agent, 250 parts by weight of polymer water-absorbing material and 60 parts by weight of core layer lubricant, wherein the foaming agent has characteristics of reacting with water to generate gas; and a coating layer covering the surface of the core layer to form a granular structure, wherein the coating layer is consisting of 10% to 40% by weight of edible water-absorbent colloid, 5% to 40% by weight of functional health food additives, 2% to 30% by weight of emulsifier, 4% to 15% by weight of coating layer lubricant and 5% to 40% by weight of film coating composition, and wherein the film coating composition has characteristics of resistance to gastric acid decomposition and being decomposed only in the intestinal tract.
2. The expandable microcapsule according to claim 1, wherein the foaming agent is consisting of 100 to 300 parts by weight of an acidic compound and 130 to 410 parts by weight of a basic compound, wherein the acidic compound is composed of at least one of citric acid or tartaric acid, and the basic compound is composed of at least one of sodium carbonate, sodium bicarbonate, potassium carbonate, and potassium bicarbonate.
3. The expandable microcapsule according to claim 1, wherein the polymer water-absorbing material is sodium polyacrylate, wherein the polymer water-absorbing material is superfinely pulverized to a size of 300 mesh or more, and dried at 40° C. to 80° C. for 5 hours.
4. The expandable microcapsule according to claim 1, wherein the core layer lubricant is consisting of 20 to 60 parts by weight of an internal lubricant and 2 to 6 parts by weight of an external lubricant, wherein the internal lubricant is composed of one or a combination of polyethylene glycol 4000 and polyethylene glycol 6000, and the external lubricant is composed of magnesium stearate, talc, or one or a combination of L-leucine and DL-leucine.
5. The expandable microcapsule according to claim 4, wherein the core layer is made by mixing with a foaming agent, a polymer water-absorbing material and an internal lubricant, then adding 240 parts by weight of a soft material made of anhydrous ethanol, granulated by sieving, and dried at 40° C. to 80° C. to make the water content of the mixture particles below 3%, and then adding an external lubricant and mixing.
6. The expandable microcapsule according to claim 1, wherein the edible water-absorbing colloid is composed of pectin, konjac powder, arabic gum, carrageenan, alginate, agar, guargum, xanthan gum, locust bean gum, gelatin, gellan gum, galactomannan, tragacanth gum, karaya gum, curdlan gum, chitosan, xyloglucan, β-glucan, furcellaran, Ghattigum, tamarin, bacterial gum, propylene glycol alginate, carboxymethyl locust bean gum, low methoxy pectin, mixture of emulsified calcium and pectin, modified microcrystalline cellulose, modified carboxymethyl cellulose (CMC), modified methyl cellulose (MC), modified hydroxypropyl methyl cellulose (HPMC), modified hydroxypropyl cellulose (HPC), or any combination thereof.
7. The expandable microcapsule according to claim 1, wherein the film coating composition is consisting of one of 1% to 25% by weight of film-forming agent, 0.5% to 15% by weight of anti-sticking agent, and 60% to 95% by weight of solvent, and the film-forming agent is composed of shellac methyl cellulose, ethyl cellulose, propyl methyl cellulose, hydroxypropyl methyl cellulose phthalate (HPMCP), pectin, seaweed gum, sodium alginate, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, polyvinylpyrrolidone, polyethylene glycol, aminoalkyl methacrylate copolymer, maltodextrin and polydextrose or any combination thereof.
8. The expandable microcapsule according to claim 1, wherein the emulsifier is selected from one of lecithin, fatty ester of glycerol, sucrose and sorbitol.
9. The expandable microcapsule according to claim 1, wherein the coating layer lubricant is composed of one of polyethylene glycol 4000, polyethylene glycol 6000, sodium lauryl sulfate, magnesium lauryl sulfate, L-leucine, sodium benzoate, sodium oleate, sodium chloride, sodium acetate, boric acid, magnesium stearate, talc, micronized silica gel, sucrose fatty acid ester, sodium stearyl fumarate, L-leucine and DL-leucine, or any combination thereof.
Description
BRIEF DESCRIPTION OF THE DRAWINGS
[0009]
[0010]
[0011]
[0012]
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0013] First, please refer to
[0014] the core layer 11 consists of 300 parts by weight of foaming agent, 250 parts by weight of polymer water-absorbing material and 60 parts by weight of core layer lubricant, and the foaming agent has the characteristics of reacting with water to generate gas; and
[0015] the coating layer 21 covering the surface of the core layer 11 to form a granular structure, the coating layer 21 is consisting of 10% to 40% by weight of edible water-absorbent colloid, 5% to 40% by weight of functional health food additives, 2% to 30% by weight of emulsifier, 4% to 15% by weight of coating layer lubricant and 5% to 40% by weight of film coating composition, and wherein the film coating composition has the characteristics of resistance to gastric acid decomposition and being decomposed only in the intestinal tract.
[0016] In actual production, the foaming agent of the present disclosure is composed of 100 to 300 parts by weight of acidic compounds and 130 to 410 parts by weight of basic compounds, and the foaming agent is dried for 2 to 4 hours at 40° C. to 80° C. before use, and passed through a 40 to 100 mesh sieve. The acidic compound and the basic compound are preferably: 200 parts by weight of the acidic compounds and 270 parts by weight of the basic compounds; or 240 parts by weight of the acidic compounds and 400 parts by weight of the basic compounds; or 160 parts by weight of the acidic compounds and 140 parts by weight of the basic compounds.
[0017] Preferably, the above-mentioned basic compound may be one of sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate, calcium carbonate, sodium glycine carbonate, potassium glycine carbonate, or any combination thereof. In addition, all edible alkali metal or alkaline earth metal carbonates, percarbonates, bicarbonates and their mixed carbonates can be used as basic compounds that can generate carbon dioxide gas. Among the basic compounds, at least one of sodium carbonate, sodium bicarbonate, potassium carbonate, and potassium bicarbonate is preferred. In addition, considering that taking sodium-containing foaming agents multiple times a day will cause adverse consequences for eaters who are not suitable to eat more sodium, it can be taken into account that using less sodium carbonate and sodium bicarbonate but using potassium bicarbonate, potassium carbonate, calcium carbonate, zinc carbonate and other non-sodium or low-sodium carbon dioxide sources used as a substitute.
[0018] Preferably, the polymer water-absorbing material of the present disclosure is sodium polyacrylate, and the polymer water-absorbing material is superfinely pulverized to a size of 300 mesh or more, and dried at 40° C. to 80° C. for 2 to 5 hours.
[0019] The core layer lubricant of the present disclosure mainly consists of 20 to 60 parts by weight of internal lubricant and 2 to 6 parts by weight of external lubricant. Preferably, the internal lubricant is polyethylene glycol 4000 or polyethylene glycol 6000, and the external lubricant is magnesium stearate, talc, or L-leucine or DL-leucine, or any combination thereof. The internal lubricant and the external lubricant are preferably: 40 parts by weight of the internal lubricant and 4 parts by weight of the external lubricant, or 25 parts by weight of the internal lubricant and 5 parts by weight of the external lubricant, or 57 parts by weight of the internal lubricant and 3 parts by weight of the external lubricant.
[0020] The core layer 11 of the present disclosure is prepared by mixing the foaming agent, the polymer water-absorbing material, and the internal lubricant according to the above formula ratio, sieving (according to product requirements), mixing homogeneously, and adding 240 parts by weight of a soft material made of anhydrous ethanol. After granulation by sieving (according to product requirements), drying at 40° C. to 80° C. to make the water content of the mixture particles below 3 then sieving and finishing (according to product requirements), and then adding the external lubricant, mixing homogeneously, and the granular core layer 11 of the present disclosure can be obtained.
[0021] Next, each composition of the coating layer 21 of the present disclosure is described as follows, wherein:
[0022] the coating layer is consisting of 10% to 40% by weight of edible water-absorbent colloid, 5% to 40% by weight of functional health food additives, 2% to 30% by weight of emulsifier, 4% to 15% by weight of coating layer lubricant and 5% to 40% by weight of film coating composition. The edible water-absorbent colloid in the coating layer 21 includes naturally occurring materials, such as plant secretions, seed gums and seaweed extracts, or can also be chemically modified materials, such as modified cellulose, starch or natural rubber derivatives. In a feasible embodiment, the edible water-absorbing colloid is composed of pectin, konjac powder, arabic gum, carrageenan, alginate, agar, guargum, xanthan gum, locust bean gum, gelatin, gellan gum, galactomannan, tragacanth gum, karaya gum, curdlan gum, chitosan, xyloglucan, β-glucan, furcellaran, Ghattigum, tamarin, bacterial gum, propylene glycol alginate, carboxymethyl locust bean gum, low methoxy pectin, mixture of emulsified calcium and pectin, modified microcrystalline cellulose, modified carboxymethyl cellulose (CMC), modified methyl cellulose (MC), modified hydroxypropyl methyl cellulose (HPMC), modified hydroxypropyl cellulose (HPC), or any combination thereof.
[0023] The functional health food additives in the coating layer 21 include, but are not limited to, cellulose, probiotics or vitamins that are beneficial to the human body, as well as all that can help digestion, improve metabolism, promote fat burning, help smooth bowel movements, inhibit sugars and fat absorption and other beneficial additives to the human body.
[0024] The film coating composition in the coating layer 21 is designed to remain intact and not digested in the acidic environment of the stomach and can absorb the water in the stomach, but it can be dissolved in the more alkaline environment of the intestine. In some embodiments, the film-forming agent includes shellac methyl cellulose, ethyl cellulose, propyl methyl cellulose, hydroxypropyl methyl cellulose phthalate, pectin, seaweed gum, sodium alginate, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, polyvinylpyrrolidone, polyethylene glycol aminoalkyl methacrylate copolymer, maltodextrin and polydextrose, or any combination thereof. Preferably, the film-forming agent with stomach insolubility is sodium alginate. In addition, based on 100% by weight of the film coating composition, the film coating composition includes 1% to 25% of the film-forming agent, 0.5% to 15% of the anti-sticking agent, and 60% to 95% of the solvent. In addition, an emulsifier can be further added to the coating layer 21, the mass ratio of the edible water-absorbant colloid to the emulsifier can be 7:1, and the emulsifier can be particularly selected from lecithin, fatty esters of glycerol, sucrose or sorbitol, in order to be used in the environment where there is a high content of protein or oil. Furthermore, according to production needs, add a coating layer lubricant that is convenient for granulation, the coating layer lubricant is composed of one of polyethylene glycol 4000, polyethylene glycol 6000, sodium lauryl sulfate, magnesium lauryl sulfate, L-leucine, sodium benzoate, sodium oleate, sodium chloride, sodium acetate, boric acid, magnesium stearate, talc, micronized silica gel, sucrose fatty acid ester, sodium stearyl fumarate, L-leucine and DL-leucine, or any combination thereof.
[0025] Preferably, the method for coating the surface of the core layer with the coating layer 21 of the present disclosure can be made into a granular structure by conventional pharmacological techniques. Conventional pharmacological techniques include, for example, one or a combination of the following methods: (1) dry mixing, (2) direct compression, (3) grinding, (4) dry or non-aqueous granulation, (5) wet granulation, (6) melting, or (7) extrusion/spheronization. Other methods such as commonly used solvent evaporation methods (e.g. spray drying, stratification or fluidized bed granulation, rotating disk, three-phase emulsification technology, etc.). Suitable solvents for solvent evaporation include alcohols (e.g. methanol, ethanol, n-propanol, isopropanol and butanol), ketones (e.g. acetone, methyl ethyl ketone and methyl isobutyl ketone), esters (e.g. ethyl acetate and propyl acetate) and various other solvents such as isopropyl ether, acetonitrile, dichloromethane, chloroform, hexane, toluene, tetrahydrofuran, cyclic ethers, and 1,1,1-trichloroethane; low volatility solvent can also be used, such as dimethyl acetamide or dimethyl sulfide. Mixtures of solvents can also be used, such as 20% ethanol, 80% acetone, and their mixtures with water.
[0026] The expandable microcapsule 10 of the present disclosure made of the above-mentioned components can remove water generated by the inevitable acid-base reaction in time by adding a polymer water-absorbing material to the core layer 11, so that the particle surface of the foaming agent in the core layer can be isolated, and kept in a dry state to prevent the acid-base reaction, thereby solving the problem that the foaming agent is unstable due to easily absorbing moisture and flatulence. Also, under actual action, it can be ensured that the effect of the foaming agent at a fast foaming speed after absorbing water. On the other hand, absorbing water through the polymer water-absorbing material is beneficial to stabilize the colloidal shape of the coating layer and have an excellent molding effect.
[0027] When the expandable microcapsule 10 of the present disclosure enters the human stomach after being eaten, the edible water-absorbent colloid of the coating layer 21 will be softened after absorbing water, and the core layer 11 will also swell due to the absorption of water. Since the foaming agent in the core layer 11 reacts with water to generate carbon dioxide, the coating layer 21 covering the core layer 11 can be blown by the continuous carbon dioxide generated by the foaming agent and rapidly expand and become larger (as shown in
[0028] In addition, in practical applications of the expandable microcapsules provided by the present disclosure, the eater not only directly eat a predetermined amount of the expandable microcapsules 10 to make them physically expand in the human stomach to increase satiety and suppress appetite, but also according to needs tablets as shown in
[0029] In another embodiment of the present disclosure shown in