WO2023008567A1 - Composition de coque de capsule et capsule obtenue à l'aide de celle-ci - Google Patents

Composition de coque de capsule et capsule obtenue à l'aide de celle-ci Download PDF

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Publication number
WO2023008567A1
WO2023008567A1 PCT/JP2022/029330 JP2022029330W WO2023008567A1 WO 2023008567 A1 WO2023008567 A1 WO 2023008567A1 JP 2022029330 W JP2022029330 W JP 2022029330W WO 2023008567 A1 WO2023008567 A1 WO 2023008567A1
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Prior art keywords
mass
capsule shell
content
capsule
starch
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PCT/JP2022/029330
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English (en)
Japanese (ja)
Inventor
真司 矢野
昌史 野津
雄斗 望月
明広 幡野
憲一 小山
崇典 小林
徹 風岡
広樹 小林
貴広 脇田
裕司 藤田
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三生医薬株式会社
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Priority to JP2023538643A priority Critical patent/JPWO2023008567A1/ja
Publication of WO2023008567A1 publication Critical patent/WO2023008567A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate

Definitions

  • the present invention relates to a capsule shell composition and capsules using the same.
  • gelatin is suitably used for the capsule shell composition used in the production of capsule shells.
  • Gelatin exhibits suitable physical properties such as the viscosity and fluidity of the capsule shell composition, the strength of the formed capsule shell, heat-sealing properties, and resistance to cracking.
  • gelatin is mostly derived from animal collagen, and in recent years, from the viewpoint of religion, vegetarianism, allergies, mad cow disease, etc., there has been a demand for a capsule shell composition that uses a raw material that replaces gelatin as a main component. ing.
  • Patent Document 1 discloses a dry film composition suitable for soft capsules containing a mixture of iota carrageenan and modified starch, water, a plasticizer, and a buffer ( An invention relating to a capsule shell composition) is described.
  • Patent Document 1 describes that the capsule shell composition forms a film that is mechanically tough and has sufficient elasticity to stretch the film during filling (blow molding).
  • Patent Document 1 describes that a buffer (phosphate buffer) is added for the purpose of preventing destruction (decomposition) of carrageenan.
  • the capsule shell composition described in Patent Document 1 has high viscosity and is sometimes inferior in handleability. Therefore, there is a demand for a capsule shell composition that is easy to handle.
  • the present invention includes, for example, the following aspects.
  • a capsule shell composition comprising starches, iota carrageenan, and gums, The content of the iota carrageenan is 2% by mass or more with respect to 100% by mass of the capsule shell composition, A capsule shell composition, wherein the gum content is 0.3 to 14% by mass with respect to 100% by mass of the capsule shell composition.
  • the capsule shell composition according to [1] above which does not contain gelatin.
  • gum is one or more selected from the group consisting of gum arabic, guar gum, locust bean gum, gellan gum, xanthan gum, and tamarind gum. capsule shell composition.
  • the content ratio of starch to iota carrageenan (starch content (% by mass)/iota carrageenan content (% by mass)) is 1.2 to 10,
  • the content ratio of starches to gums (starch content (mass%) / gum content (mass%)) is 1 to 50, Any of the above [1] to [4], wherein the content ratio of iota carrageenan to gums (content of iota carrageenan (% by mass) / content of gums (% by mass)) is 0.5 to 15 2.
  • the capsule shell composition according to 1.
  • the starch content is 10 to 30% by mass with respect to 100% by mass of the capsule shell composition;
  • the starch contains at least one selected from the group consisting of natural starch and modified starch.
  • the content ratio of starch to iota carrageenan in the capsule shell (starch content (% by mass) / iota carrageenan content (% by mass)) is 1.2 to 10
  • the content ratio of starches to gums in the capsule shell (starch content (mass%) / gum content (mass%)) is 1 to 50, [10] or The capsule of [11].
  • the content ratio of starch to iota carrageenan in the capsule shell (starch content (mass%) / iota carrageenan content (mass%)) is 1.2 to 10,
  • the content ratio of starches to gums in the capsule shell (starch content (mass%) / gum content (mass%)) is 1 to 50,
  • the content ratio of iota carrageenan to gums in the capsule shell (content of iota carrageenan (% by mass) / content of gums (% by mass)) is 0.5 to 15 [13] to [16], and the capsule of any one of [13-1].
  • a capsule shell composition and the like with excellent handleability are provided.
  • the capsule shell composition of one aspect of the present invention comprises starches, iota carrageenan, and gums.
  • the iota-carrageenan content is 2% by mass or more with respect to 100% by mass of the capsule shell composition.
  • the content of the gums is 0.3 to 14% by mass with respect to 100% by mass of the capsule shell composition.
  • the capsule shell composition has excellent handleability. Specifically, the capsule shell composition has a suitable viscosity. As a result, for example, the obtained capsules are excellent in formability of a film (wet film) that can be formed during production of the capsules, so that filling suitability is high (for example, high-speed filling is possible) and heat-sealability is excellent. At least one of the effects of high blocking resistance, good appearance, and the like can be obtained.
  • the capsule shell composition may have jelly strength and flexibility suitable for a film (wet coating) formed during production of the capsule. Therefore, at least one of the effects of high strength of the film formed during production of the capsule and high hardness of the resulting capsule can be achieved. Furthermore, in one embodiment, since the capsule shell composition contains starches, high disintegrability can be obtained.
  • the capsule shell composition of the present invention does not contain gelatin. As a result, even those who cannot take gelatin due to religious reasons, vegetarianism, allergies, etc., can take the capsules. Also, safety issues such as mad cow disease are less likely to occur.
  • the capsule shell composition of the present invention does not contain a phosphate buffer.
  • Patent Document 1 it was necessary to adjust the pH with a phosphate buffer in order to prevent destruction (decomposition) of carrageenan, but the capsule shell composition of the present invention does not require such pH adjustment. can be. As a result, the amount of chemical substances such as phosphate buffers can be reduced, so that even health-conscious people can take the capsules.
  • Starch has a film-forming property and functions as a base agent for capsule shells. Since the capsule shell composition uses starches as a base agent, the obtained capsules can have excellent disintegration properties.
  • the starches are not particularly limited, but include natural starch and processed starch.
  • the natural starch is not particularly limited, but includes potato starch, tapioca starch, glutinous corn starch, glutinous rice starch, sago starch, sweet potato starch, mung bean starch, wheat starch and the like.
  • the modified starch is obtained by physically, chemically and enzymatically processing natural starch.
  • Said processing includes, for example, esterification, etherification, oxidation, cross-linking, hydrolysis, and combinations thereof.
  • modified starch examples include esterified starch such as acetylated starch, phosphated starch and octenyl succinic acid starch; etherified starch such as hydroxypropylated starch and sodium starch glycolate; oxidized starch; Esterified crosslinked starch such as phosphate monoesterified phosphate crosslinked starch and starch phosphate sodium; etherified crosslinked starch such as hydroxypropylated starch for phosphorylation; esterified oxidized starch such as acetylated oxidized starch; glucose, starch syrup , maltodextrin, dextrin, and starch hydrolyzate such as roasted dextrin.
  • esterified starch such as acetylated starch, phosphated starch and octenyl succinic acid starch
  • etherified starch such as hydroxypropylated starch and sodium starch glycolate
  • oxidized starch Esterified crosslinked starch
  • the dextrose equivalent (DE) of the starch hydrolyzate is preferably 20 or less, more preferably 15 or less, even more preferably 10 or less, and particularly preferably 5 or less. , more than 0 and less than or equal to 5.
  • DE dextrose equivalent
  • the starch hydrolyzate has a dextrose equivalent of 20 or less, deterioration over time is less likely to occur, which is preferable.
  • the physical properties (filling suitability, heat-sealing property, jelly strength, flexibility, etc.) of a film (wet film) formed during the production of capsules and the physical properties of capsules (hardness, blocking resistance, appearance) are high.
  • D.E. glucose equivalent
  • the amount of reducing sugars in the starch hydrolyzate is measured by the Reine Einone method, the Willstetter-Schudel method, the Bertrand method, or the HPLC method (for example, "Starch Sugar Related Industrial Analysis Method” (Starch Sugar Technical Committee Ed., published by Shokuhin Kagaku Shimbunsha (published on November 1, 1991))).
  • pure glucose D.I. E. is 100, the D.O.D. of undegraded starch (native starch). E. becomes 0.
  • the starch preferably contains at least one selected from the group consisting of natural starch and modified starch, and at least one selected from the group consisting of natural starch, etherified starch, and starch hydrolyzate. More preferably, it contains at least one selected from the group consisting of native starch and etherified starch, and at least one selected from the group consisting of native starch and hydroxypropylated starch. Especially preferred.
  • the above-mentioned starches may be used alone or in combination of two or more.
  • the viscosity of the starch is preferably 200 mPa s or less, more preferably 100 mPa s or less, even more preferably 50 mPa s or less, and particularly preferably 1 to 50 mPa s. Most preferably, it is 20 to 50 mPa ⁇ s. It is preferable that the viscosity of the starch is 200 mPa ⁇ s or less, since the viscosity of the capsule shell composition can be reduced.
  • the "viscosity of starches" means the average value measured by the method described in the Examples.
  • the starch content is preferably 3% by mass or more, more preferably 8% by mass or more, and even more preferably 10% by mass or more, relative to the total mass of the capsule shell composition. , is particularly preferably 15% by mass or more, and most preferably 19% by mass or more.
  • the starch content is preferably 40% by mass or less, more preferably 30% by mass or less, and 22% by mass or less, relative to the total mass of the capsule shell composition. More preferably, yes.
  • the starch content is preferably 3 to 40% by mass, preferably 10 to 30% by mass, and 10 to 25% by mass, based on the total mass of the capsule shell composition. More preferably, 15 to 25% by mass is even more preferable.
  • a starch content of 3% by mass or more is preferable because the capsule shell can be suitably formed.
  • the starch content is 40% by mass or less, it is preferable because the physical properties can be easily adjusted by adding other components (for example, iota carrageenan) to the capsule shell composition.
  • Iota carrageenan Iota ( ⁇ ) carrageenan can form soft, elastic, highly transparent gels with low syneresis. Therefore, iota-carrageenan has the function of improving at least one of jelly strength and flexibility of a film (wet film) formed during production of capsules, hardness and appearance of capsules, and the like.
  • Iota carrageenan has a main chain with a linear structure represented by the following structural formula.
  • iota carrageenan has a linear main chain composed of glasstose having one sulfate group and 3,6-anhydrogalactose having one sulfate group.
  • iota carrageenan may have galactose having two sulfate ester groups, 3,6-anhydrogalactose having no sulfate ester groups, or branched chains in a part of the main chain. may be
  • the viscosity of iota carrageenan is preferably 5000 mPa s or less, more preferably 4000 mPa s or less, still more preferably 500 to 4000 mPa s, particularly preferably 1000 to 3500 mPa s. .
  • Iota-carrageenan having a viscosity of 5000 mPa ⁇ s or less is preferable because the viscosity of the capsule shell composition can be reduced.
  • the "viscosity of iota carrageenan" means the average value measured by the method described in Examples.
  • the content of iota carrageenan is 2% by mass or more, preferably 3% by mass or more, more preferably 4% by mass or more, and 6% by mass, relative to the total mass of the capsule shell composition. It is particularly preferable that it is above.
  • the content of iota carrageenan is preferably 20% by mass or less, more preferably 15% by mass or less, and preferably 10% by mass or less, relative to the total mass of the capsule shell composition. More preferred.
  • the content of iota carrageenan is preferably 2 to 20% by mass, more preferably 3 to 20% by mass, more preferably 4 to 20% by mass, based on the total mass of the capsule shell composition.
  • % by mass is more preferred, 4 to 15% by mass is particularly preferred, 4 to 10% by mass is more preferred, and 6 to 10% by mass is most preferred.
  • content of iota carrageenan is 2% by mass or more, at least one of the jelly strength and flexibility of the film (wet film) formed during production of the capsule, and the hardness and appearance of the capsule can be improved. preferable.
  • content of iota carrageenan is 20% by mass or less, the viscosity of the capsule shell composition can be lowered, which is preferable.
  • iota carrageenan can be obtained by extracting Eucheuma Spinosum, etc.
  • Eucheuma Spinosum is washed with water, pulverized, and boiled to extract iota carrageenan, filtered, isolated, purified, dehydrated, dried, pulverized, and if necessary, sugar or the like is used to obtain iota carrageenan. be able to.
  • isolation, purification and dehydration of iota carrageenan are preferably carried out by a gel press method.
  • the gel press method is a method in which the iota carrageenan extract is cooled to gel the iota carrageenan, and then pressurized and dehydrated.
  • a metal salt such as potassium chloride may be added before cooling and gelling.
  • the gel press method does not allow amino acids, proteins, and relatively low-molecular-weight carbohydrates to be extracted during purification. It is difficult for impurities such as Therefore, the gel press method is less likely to cause the Maillard reaction and accompanying pH reduction, and thus less likely to cause the decomposition of iota carrageenan, so that high-quality iota carrageenan can be obtained.
  • Gums have a function of reducing the viscosity of the capsule shell composition, a function of improving the flexibility of the film (wet film) formed during the manufacture of the capsule, and the like. Gums may exhibit a synergistic effect with the iota carrageenan. For example, gums and iota carrageenan form a double helix structure.
  • the double helix structure is a rigid skeleton having crystalline and amorphous regions, and can stably exist in the wet film and the capsule shell of the capsule.
  • iota carrageenan enhances the jelly strength and flexibility of the wet film, the hardness and appearance of the capsule, suppresses the increase in viscosity of the capsule shell composition due to the addition of iota carrageenan, and prevents the decomposition of iota carrageenan. At least one effect of performing, etc. can be further exhibited.
  • the gums are preferably one or more selected from the group consisting of gum arabic, guar gum, locust bean gum, gellan gum, xanthan gum, and tamarind gum, and are selected from the group consisting of gum arabic, guar gum, and gellan gum. It is more preferably one or more, and one or more selected from the group consisting of gum arabic and gellan gum from the viewpoint of improving the jelly strength and flexibility of the resulting wet film and the hardness of the resulting capsule. More preferably, it contains gum arabic. In addition, gums may be used individually or may be used in combination of 2 or more types.
  • Gum arabic is mainly composed of polysaccharides and includes arabinogalactan, arabinogalactan protein, glycoprotein, and the like.
  • Guar gum is a polysaccharide having two molecules of mannose linked in a linear chain and one molecule of galactose as a side chain.
  • the guar gum may be a guar gum derivative, and examples of the guar gum derivative include hydroxypropyl guar gum, cationized guar gum, and guar gum enzymatic decomposition products.
  • Locust bean gum is a polysaccharide having 4 molecules of mannose linked in a straight chain and a side chain of 1 molecule of galactose.
  • Gellan gum includes high acyl gellan gum and low acyl gellan gum.
  • the high-acyl gellan gum is also called native gellan gum, and has a structure in which acyl groups are bound to constituent sugars (mainly glucose).
  • the low acyl gellan gum is also called deacylated gellan gum, and is obtained by deacylating high acyl gellan gum.
  • gellan gum is preferably low acyl gellan gum from the viewpoint of its low gelation temperature and suitability for capsule production.
  • Xanthan gum has a repeating unit structure of two molecules of glucose, two molecules of mannose, and glucuronic acid.
  • Tamarind gum is a polysaccharide with a structure called xyloglucan, which contains glucose in the main chain and xylose and galactose in the side chains.
  • the content of gums is 0.3 to 14% by mass, preferably 0.3 to 7.5% by mass, and 1 to 7.5% by mass, relative to the total mass of the capsule shell composition. %, more preferably 1 to 4% by mass. It is preferable that the content of the gums is within the above range, since the viscosity of the capsule shell composition can be lowered.
  • at least one of the physical properties of the film (wet film) formed during capsule production (filling suitability, heat-sealing property, jelly strength, flexibility, etc.) and the physical properties of the capsule (hardness, blocking resistance, appearance) It is preferable because it can be improved.
  • the content ratio of starches to iota carrageenan is preferably 1 to 20, preferably 1.2 to 10 is more preferred, 1.2 to 5 is even more preferred, and 2 to 5 is particularly preferred.
  • the content ratio of starches to gums is preferably 1 to 75, preferably 1 to 50. It is more preferably 1, more preferably 2 to 50, particularly preferably 2 to 40, and most preferably 5 to 30.
  • the content ratio of iota carrageenan to gums is preferably 0.1 to 30. It is more preferably from 5 to 15, even more preferably from 1 to 25, particularly preferably from 2 to 25, and most preferably from 2 to 12.
  • the total content of starches and iota carrageenan is preferably 5 to 40% by mass, more preferably 10 to 40% by mass, based on the total mass of the capsule shell composition. , more preferably 22 to 40% by mass, particularly preferably 26 to 40% by mass.
  • the total content of starches and gums is preferably 3.5 to 40% by mass, preferably 5 to 35% by mass, based on the total mass of the capsule shell composition. It is more preferably 15 to 30% by mass, particularly preferably 15 to 25% by mass, and most preferably 21 to 25% by mass.
  • the total content of iota carrageenan and gums is preferably 2.5 to 30% by weight, preferably 2.5 to 20% by weight, based on the total weight of the capsule shell composition. is more preferable, 2.5 to 15% by mass is more preferable, and 2.5 to 10% by mass is particularly preferable.
  • the capsule shell composition preferably further comprises alginate.
  • the alginate can improve the jelly strength of the film (wet film) formed during capsule production and the hardness of the physical properties of the capsule while suppressing the increase in the viscosity of the capsule shell composition.
  • a synergistic effect between alginic acid ester and gums is considered.
  • the action of alginate on proteins, which are constituents of gums will further improve the effect of suppressing increases in the viscosity of capsule shell compositions due to the addition of iota-carrageenan contained in gums.
  • Alginic acid ester is a linear polysaccharide polymerized from two types of uronic acid ( ⁇ -D-mannuronic acid (M) and ⁇ -L-guluronic acid (G)). has an ester-bonded structure.
  • Alginate has a surface active effect because it has a hydrophilic alginic acid portion and a lipophilic propylene glycol portion.
  • the alginate content is 0.001% by mass or more, preferably 0.01% by mass or more, and preferably 0.03% by mass or more, relative to the total mass of the capsule shell composition. More preferably, it is particularly preferably 0.3% by mass or more.
  • the alginate content is preferably 10% by mass or less, more preferably 5% by mass or less, and 0.75% by mass or less, relative to the total mass of the capsule shell composition. is particularly preferred.
  • the alginate content is preferably 0.001 to 10% by mass, more preferably 0.001 to 5% by mass, relative to the total mass of the capsule shell composition. , more preferably 0.01 to 5% by mass, and particularly preferably 0.03 to 0.75% by mass.
  • the jelly strength of the film (wet film) formed during the production of the capsules and the hardness of the physical properties of the capsules are improved while suppressing an increase in the viscosity of the capsule shell composition. can be improved.
  • the content ratio of gums to alginate is preferably 0.01 to 100, and 0.1 to 50. is more preferred, 0.5 to 20 is even more preferred, and 3 to 20 is particularly preferred.
  • the capsule shell composition preferably further comprises a plasticizer.
  • a plasticizer has the function of imparting flexibility to the film (wet film) formed during the production of capsules.
  • Plasticizers include, but are not limited to, polyhydric alcohols such as glycerin, sorbitol, maltitol, ethylene glycol, propylene glycol; hydroxymethylcellulose (HPMC), hydroxypropylcellulose (HPC), methylcellulose (MC), carboxymethylcellulose (CMC); ) and other cellulose derivatives.
  • the plasticizer preferably contains a polyhydric alcohol, and more preferably contains glycerin. These plasticizers may be used alone or in combination of two or more.
  • the content of the plasticizer is preferably 1 to 50% by mass, more preferably 5 to 30% by mass, and 5 to 25% by mass, relative to the total mass of the capsule shell composition. is more preferred. It is preferable that the content of the plasticizer is within the above range, since the flexibility of the wet film becomes suitable.
  • the capsule shell composition may further comprise gelatin.
  • gelatin By including gelatin in the capsule shell composition, it is possible to improve the viscosity and flowability of the capsule shell composition, the strength of the formed capsule shell, the heat-sealing property, the resistance to cracking, and the like.
  • gelatin examples include, but are not limited to, pig gelatin, bovine gelatin, fish gelatin, gelatin derivatives, and the like.
  • gelatin derivatives include succinated gelatin, gelatin hydrolysates, and crosslinked gelatin. These gelatins may be used alone or in combination of two or more. For example, by using fish gelatin or a derivative thereof, it may be possible to ingest animal collagen even in cases where it is difficult to ingest animal collagen from the viewpoint of religion, vegetarianism, allergies, or the like.
  • the gelatin content is preferably 40% by mass or less, more preferably 30% by mass or less, and even more preferably 1 to 20% by mass, relative to the total mass of the capsule shell composition. .
  • the capsule shell composition preferably contains a solvent.
  • a solvent in the capsule shell composition, the viscosity of the capsule shell composition can be adjusted.
  • solvents include water and organic solvents.
  • the organic solvent is not particularly limited, but includes ethanol, isopropyl alcohol, acetone, ethyl butyrate, and the like.
  • the solvent preferably contains water.
  • the above-mentioned solvent may be used independently or may be used in combination of 2 or more types.
  • the content of the solvent is preferably 20 to 90% by mass, more preferably 30 to 80% by mass, and 40 to 70% by mass, based on the total mass of the capsule shell composition. More preferably, it is particularly preferably 50 to 60% by mass.
  • the capsule shell composition may contain additives.
  • Such additives include other thickeners, pH adjusters, sequestering agents, film coloring agents, corrigents, sweeteners, preservatives, flavoring agents, and the like.
  • Olether thickeners means thickeners other than iota carrageenan, gums, gelatin, and alginate.
  • the other thickening agents include, but are not limited to, kappa ( ⁇ ) carrageenan, lambda ( ⁇ ) carrageenan, pullulan, agar, alginic acid, sodium alginate, and the like. These other thickening agents may be used alone or in combination of two or more.
  • Kappa-carrageenan has a linear main chain composed of galactose having one sulfate ester group and 3,6-anhydrogalactose having no sulfate ester group.
  • kappa carrageenan may have galactose having two sulfate ester groups, 3,6-anhydrogalactose having sulfate ester groups in part of the main chain, or may have a branched chain. good too.
  • lambda carrageenan has a main chain with a linear structure composed of galactose with two sulfate ester groups and galactose with one sulfate ester group.
  • Lambda carrageenan may have 3,6-anhydrogalactose having a sulfate ester group, 3,6-anhydrogalactose having no sulfate ester group, or branched It may have chains.
  • the pH adjuster is not particularly limited, but includes acids such as hydrochloric acid, sulfuric acid, and nitric acid; bases such as sodium hydroxide and potassium hydroxide; buffers such as phosphate buffers and Tris buffers. These pH adjusters may be used alone or in combination of two or more.
  • the capsule shell composition preferably does not contain a buffering agent, and more preferably does not contain a phosphate buffering agent.
  • sequestering agents include citric acid, tartaric acid, lactic acid, phosphoric acid, acetic acid, gluconic acid, ethylenediaminetetraacetic acid, metaphosphoric acid, salts thereof; glycine, and the like.
  • additives may be used alone or in combination of two or more.
  • the method for producing the capsule shell composition is not particularly limited, and it can be produced by a known method.
  • starch, iota carrageenan, gums, and if necessary, alginate, plasticizer, gelatin, and additives are added to a solvent, and the resulting suspension is heated and dissolved to form a capsule shell composition. can manufacture things.
  • capsules are provided.
  • the capsule includes contents and a capsule shell.
  • a capsule shell is formed using the capsule shell composition described above.
  • a capsule containing contents and a capsule shell containing starches, iota carrageenan, and gums.
  • the capsule has a hardness of 15 kg or more.
  • the capsule shell may further contain at least one of alginate, plasticizer, gelatin, solvent and additive.
  • Contents are not particularly limited, and include active ingredients and additives.
  • Examples of the active ingredient include, but are not limited to, hypnotics, psychotropic drugs, antiepileptic drugs, antiparkinsonian drugs, analgesics, therapeutic drugs for Alzheimer's disease, antiallergic drugs, cardiotonic drugs, antiarrhythmic drugs, and antianginal drugs.
  • Anticancer drugs Antifungal drugs Immunosuppressive drugs Crude drugs such as senega, clove, angelica gentian, gentian, ryutan, assembly, rhubarb, digitalis, valerian, bellflower, aloe, hange, turmeric, ginger; Herbal medicines such as shakuyakusan and maoto; vitamins, minerals, collagen, coenzyme Q10, DHA, EPA, lutein, blueberry, placenta, soybean isoflavone, lactic acid bacteria, bifidobacteria, and other health-promoting ingredients; caryophyllene, menthol, limonene, Aroma components such as sesquiterpene and vanill
  • the additives include, but are not particularly limited to, excipients, coloring agents, masking agents, sweeteners, antioxidants, preservatives, lubricants, flavoring agents, and the like. These additives may be used alone or in combination of two or more.
  • the total mass of the contents is preferably 40-90% by mass, more preferably 50-80% by mass, relative to the total mass of the capsule.
  • a capsule shell is formed using a capsule shell composition.
  • the capsule shell comprises starches, iota carrageenan, and gums.
  • the capsule shell may further contain at least one of alginate, plasticizer, gelatin, solvent, and additives.
  • the capsule shell does not contain gelatin. Moreover, it is preferable that the capsule shell does not contain a phosphate buffer.
  • the film thickness of the capsule shell is preferably 200 ⁇ m or more, more preferably 250 to 800 ⁇ m, even more preferably 250 to 500 ⁇ m.
  • the film thickness of the capsule film can be measured using a digital microscope (for example, trade name VHX-900 manufactured by Keyence Corporation, using a 10 ⁇ m calibration scale). can.
  • the total mass of the capsule shell is preferably 10-60% by mass, more preferably 20-50% by mass, relative to the total mass of the capsule.
  • the content ratio of starch to iota carrageenan in the capsule shell is preferably 1 to 20, It is more preferably from 1.2 to 10, even more preferably from 1.2 to 5, and particularly preferably from 2 to 5.
  • the content ratio of starches to gums in the capsule shell is preferably 1 to 75, It is more preferably from 1 to 50, even more preferably from 2 to 50, particularly preferably from 2 to 30, and most preferably from 5 to 30.
  • the content ratio of iota-carrageenan to gums in the capsule shell is 0.1 to 30. It is preferably from 0.5 to 15, even more preferably from 1 to 25, particularly preferably from 2 to 25, and most preferably from 2 to 12.
  • the starch content (% by mass), the iota carrageenan content (% by mass), and the gum content (% by mass) in the capsule shell are the contents of each component with respect to 100% by mass of the capsule shell. means.
  • each content ratio can correspond to each content ratio in the capsule shell composition.
  • the shape of the capsule is not particularly limited, but may be spherical, ellipsoidal, triangular, rhomboidal, rectangular parallelepiped, rectangular parallelepiped, or the like.
  • the capsule is preferably a soft capsule.
  • a soft capsule By being a soft capsule, it is possible to obtain effects such as the ability to formulate a liquid active ingredient with a large amount of oil, a high degree of freedom in the shape of the capsule, and the ability to print the product name on the capsule surface.
  • the hardness of the capsule is preferably 10 kg or more, more preferably 15 kg or more, still more preferably 20 kg or more, particularly preferably 22 kg or more, and preferably 24 kg or more and 25 kg or more. Most preferred.
  • the upper limit of hardness of the capsule is, for example, preferably 40 kg or less, more preferably 35 kg or less, and even more preferably 30 kg or less. Due to the high hardness of the capsule, deformation of the capsule can be suppressed during storage and distribution.
  • a method for producing capsules is provided.
  • the method for producing capsules is not particularly limited, but includes a filling step of filling the capsule shell composition described above with a content liquid containing an active ingredient, and a drying step of drying the resulting filling.
  • the filling step is a step of filling the capsule shell composition described above with a content liquid containing an active ingredient.
  • the content liquid contains active ingredients.
  • additives may be further included. Said active ingredients and additives are as described above.
  • capsule shell composition is as described above.
  • the filling method is not particularly limited, but it is preferably a random punching method.
  • the stamping process is usually performed using rotary manufacturing equipment. More specifically, the punching method involves sandwiching two skin sheets obtained from a capsule shell composition between a pair of cylindrical molds so as to overlap each other, and injecting the liquid content between the two skin sheets. In this method, pressure cutting and crimping are performed simultaneously using a mold.
  • the capsule shell composition according to the present invention has a low viscosity and is excellent in handleability.
  • excellent filling suitability for example, high-speed filling is possible
  • excellent moldability of a film (wet film) that can be formed during the production of capsules
  • excellent heat sealability There are two effects.
  • the capsule shell composition may have a jelly strength and flexibility suitable for the film formed during production of the capsule. Therefore, it is possible to obtain effects such as high strength of the film formed during production of the capsule.
  • a drying process is a process of drying the obtained filling.
  • the resulting filling has a structure in which the content liquid is filled in the wet film.
  • the capsule shell can be obtained by removing mainly the moisture contained in the wet coating.
  • the temperature and relative humidity during drying are not particularly limited, it is performed in an environment with a temperature of 25-45°C and a relative humidity of 30% RH or less.
  • the drying process is preferably carried out until the water content of the capsule shell falls below 15%.
  • Example 1 Starch (viscosity: 46 ⁇ 5 mPa s), iota carrageenan (viscosity: 2,600 ⁇ 800 mPa s), gum arabic gum (viscosity: 260 ⁇ 80 mPa s), and glycerin as a plasticizer , was mixed with water at the compounding ratio shown in Table 1, and the resulting suspension was stirred and dissolved under heating at 90°C or higher for 3 hours to prepare a capsule shell composition.
  • the viscosity of starches, the viscosity of iota carrageenan, and the viscosity of gums were measured by the following methods.
  • Viscosity of gums 25 g of gums and 75 g of purified water were placed in a beaker and mixed well with a stirrer. The prepared mixed solution is No. After transferring to a 12 standard bottle and adjusting the mixture to 25° C., the viscosity was measured. The viscosity was measured with a Brookfield viscometer (Brookfield DV-E, liquid temperature 25° C., rotor No. 2, value after rotating at 60 rpm for 1 minute) using the obtained 25% mixture. . In addition, in this example, the viscosity of gums was measured 3 times, and was described as the average value ⁇ SD (standard deviation).
  • Examples 2 to 15, Comparative Examples 1 to 6 A capsule shell composition was produced in the same manner as in Example 1, except that the compounding ratios shown in Tables 1 and 2 were changed.
  • the raw materials used are as follows.
  • Guar gum was manufactured by Unitech Foods Co., Ltd., and gellan gum was manufactured by Sumitomo Pharma Food & Chemical Co., Ltd., respectively.
  • Viscosity was evaluated for the capsule shell compositions produced in Examples 1-15 and Comparative Examples 1-6. Also, the wet film formed from the capsule shell composition was evaluated for jelly strength, flexibility, and filling suitability. Furthermore, hardness, blocking resistance, appearance, and disintegrability were evaluated for soft capsules produced using the capsule shell composition.
  • Capsule composition (viscosity) The viscosities of the capsule shell compositions produced in Examples 1 to 15 and Comparative Examples 1 to 6 were measured using a Brookfield viscometer (TVB-15 manufactured by Toki Sangyo Co., Ltd., liquid temperature 95° C., rotor No. H7, 12 rpm. value after rotating for 1 minute). In addition, in this example, the viscosity of the capsule shell composition was measured three times, and was described as the mean ⁇ SD (standard deviation).
  • Brookfield viscometer Brookfield viscometer
  • Soft capsules production of soft capsules
  • the capsule shell compositions produced in Examples 1 to 15 and Comparative Examples 1 to 6 were filled with medium-chain fatty acid triglycerides using a rotary die capsule filling machine to obtain football-shaped wet capsules. .
  • the resulting wet capsules were dried in a dryer set at 40 ⁇ 2° C. and a humidity of less than 20% to produce soft capsules.
  • the moisture content of the capsule shell of the soft capsule after drying was set to 10 ⁇ 1% by weight.
  • the water content was calculated by the following method.
  • the hardness of the soft capsule prepared above was evaluated using a Monsanto type tablet hardness tester (B type 30 kg) 208-0219-B manufactured by Ohiwa Pharmaceutical Machinery Co., Ltd. Specifically, pressure was applied to the soft capsule using the tablet hardness tester, and the load (hardness) applied when the soft capsule was broken was measured. In this example, the hardness was measured three times, and the average value ⁇ SD (standard deviation) was described.
  • the inner stopper and metal cap of the bottle were removed, and the following conditions A to E were operated in order starting from A, and the evaluation result was the condition when all 20 soft capsules fell out of the bottle.
  • the blocking resistance is high, that is, the surface of the soft capsules is less sticky and the soft capsules are less likely to adhere to each other.
  • the capsule shell compositions of Examples 1-15 had low viscosities. Also, although the viscosity of the capsule shell composition was low, the jelly strength and flexibility of the wet coating were high. For this reason, it is considered that filling suitability is good and, for example, high-speed filling becomes possible. Also, the hardness of the soft capsule was high. In addition, the soft capsules were found to have high blocking resistance, good appearance, and excellent disintegration properties.

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Abstract

L'invention concerne une composition de coque de capsule et similaire ayant une excellente maniabilité.　La composition de coque de capsule comprend une carraghénane amidon et iota, ainsi qu'une gomme, la teneur en carraghénane étant de 2 % en masse ou plus par rapport à la composition de coque de capsule, qui est prise en tant que 100 % en masse, et la teneur de la gomme est de 0,3 % à 14 % en masse par rapport à la composition d'enveloppe de capsule, qui est prise en tant que 100 % en masse.
PCT/JP2022/029330 2021-07-30 2022-07-29 Composition de coque de capsule et capsule obtenue à l'aide de celle-ci WO2023008567A1 (fr)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006526057A (ja) * 2003-04-14 2006-11-16 エフ　エム　シー　コーポレーション 均一で熱可逆性の低粘度ポリマンナンガムフィルム及びそれからつくったソフトカプセル
JP2021100917A (ja) * 2019-12-24 2021-07-08 中日本カプセル 株式会社 ソフトカプセル皮膜、ソフトカプセル、及び、ソフトカプセルの製造方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006526057A (ja) * 2003-04-14 2006-11-16 エフ　エム　シー　コーポレーション 均一で熱可逆性の低粘度ポリマンナンガムフィルム及びそれからつくったソフトカプセル
JP2007525551A (ja) * 2003-04-14 2007-09-06 エフ　エム　シー　コーポレーション カッパ−２カラゲニンを含有する均一で熱可逆性のゲルフィルム及びそれからつくったソフトカプセル
JP2007528357A (ja) * 2003-04-14 2007-10-11 エフ　エム　シー　コーポレーション ゲルフィルムを製造するための方法
JP2021100917A (ja) * 2019-12-24 2021-07-08 中日本カプセル 株式会社 ソフトカプセル皮膜、ソフトカプセル、及び、ソフトカプセルの製造方法

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