CN108697126A - 新颖的包衣体系(i) - Google Patents
新颖的包衣体系(i) Download PDFInfo
- Publication number
- CN108697126A CN108697126A CN201780013484.5A CN201780013484A CN108697126A CN 108697126 A CN108697126 A CN 108697126A CN 201780013484 A CN201780013484 A CN 201780013484A CN 108697126 A CN108697126 A CN 108697126A
- Authority
- CN
- China
- Prior art keywords
- coated
- pufa
- composition
- cyclodextrin
- systems
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims abstract description 53
- 235000020777 polyunsaturated fatty acids Nutrition 0.000 claims abstract description 44
- 229920000858 Cyclodextrin Polymers 0.000 claims abstract description 33
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims abstract description 24
- 239000002245 particle Substances 0.000 claims abstract description 23
- 150000003839 salts Chemical class 0.000 claims abstract description 18
- 235000015872 dietary supplement Nutrition 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims abstract description 11
- 229940079593 drug Drugs 0.000 claims abstract description 11
- 235000013305 food Nutrition 0.000 claims abstract description 10
- 239000007787 solid Substances 0.000 claims abstract description 9
- 239000011248 coating agent Substances 0.000 claims abstract description 8
- 238000000576 coating method Methods 0.000 claims abstract description 8
- 239000000047 product Substances 0.000 claims description 16
- 239000011324 bead Substances 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 5
- 239000006185 dispersion Substances 0.000 claims description 4
- 239000000463 material Substances 0.000 claims description 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 3
- 239000003595 mist Substances 0.000 claims description 2
- 239000002002 slurry Substances 0.000 claims description 2
- 238000001694 spray drying Methods 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 abstract description 5
- 239000002202 Polyethylene glycol Substances 0.000 description 10
- 229920001223 polyethylene glycol Polymers 0.000 description 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 8
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 7
- 150000001875 compounds Chemical class 0.000 description 7
- MBMBGCFOFBJSGT-KUBAVDMBSA-N all-cis-docosa-4,7,10,13,16,19-hexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 description 6
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 description 6
- -1 cyclic oligosaccharide Chemical class 0.000 description 6
- 235000020673 eicosapentaenoic acid Nutrition 0.000 description 6
- 239000004014 plasticizer Substances 0.000 description 6
- 239000000843 powder Substances 0.000 description 6
- 241000251468 Actinopterygii Species 0.000 description 5
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 5
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 5
- 150000001720 carbohydrates Chemical group 0.000 description 5
- 235000020669 docosahexaenoic acid Nutrition 0.000 description 5
- 229920001450 Alpha-Cyclodextrin Polymers 0.000 description 4
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 4
- 239000001116 FEMA 4028 Substances 0.000 description 4
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 4
- 229930195725 Mannitol Natural products 0.000 description 4
- 229930006000 Sucrose Natural products 0.000 description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
- DTOSIQBPPRVQHS-PDBXOOCHSA-N alpha-linolenic acid Chemical compound CC\C=C/C\C=C/C\C=C/CCCCCCCC(O)=O DTOSIQBPPRVQHS-PDBXOOCHSA-N 0.000 description 4
- 229960004853 betadex Drugs 0.000 description 4
- 235000020664 gamma-linolenic acid Nutrition 0.000 description 4
- VZCCETWTMQHEPK-QNEBEIHSSA-N gamma-linolenic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/CCCCC(O)=O VZCCETWTMQHEPK-QNEBEIHSSA-N 0.000 description 4
- 235000011187 glycerol Nutrition 0.000 description 4
- 239000000594 mannitol Substances 0.000 description 4
- 235000010355 mannitol Nutrition 0.000 description 4
- 229920001451 polypropylene glycol Polymers 0.000 description 4
- 239000005720 sucrose Substances 0.000 description 4
- HOBAELRKJCKHQD-UHFFFAOYSA-N (8Z,11Z,14Z)-8,11,14-eicosatrienoic acid Natural products CCCCCC=CCC=CCC=CCCCCCCC(O)=O HOBAELRKJCKHQD-UHFFFAOYSA-N 0.000 description 3
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 3
- HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 description 3
- 229940043377 alpha-cyclodextrin Drugs 0.000 description 3
- 159000000007 calcium salts Chemical class 0.000 description 3
- 239000007857 degradation product Substances 0.000 description 3
- HOBAELRKJCKHQD-QNEBEIHSSA-N dihomo-γ-linolenic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/CCCCCCC(O)=O HOBAELRKJCKHQD-QNEBEIHSSA-N 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 150000004676 glycans Chemical class 0.000 description 3
- 235000019580 granularity Nutrition 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 239000001103 potassium chloride Substances 0.000 description 3
- 235000011164 potassium chloride Nutrition 0.000 description 3
- 159000000000 sodium salts Chemical group 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Chemical group OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 230000000996 additive effect Effects 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 230000001070 adhesive effect Effects 0.000 description 2
- JAZBEHYOTPTENJ-JLNKQSITSA-N all-cis-5,8,11,14,17-icosapentaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O JAZBEHYOTPTENJ-JLNKQSITSA-N 0.000 description 2
- 235000020661 alpha-linolenic acid Nutrition 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 235000021342 arachidonic acid Nutrition 0.000 description 2
- 229940114079 arachidonic acid Drugs 0.000 description 2
- 235000014633 carbohydrates Nutrition 0.000 description 2
- 238000012512 characterization method Methods 0.000 description 2
- 239000000975 dye Substances 0.000 description 2
- 229960005135 eicosapentaenoic acid Drugs 0.000 description 2
- JAZBEHYOTPTENJ-UHFFFAOYSA-N eicosapentaenoic acid Natural products CCC=CCC=CCC=CCC=CCC=CCCCC(O)=O JAZBEHYOTPTENJ-UHFFFAOYSA-N 0.000 description 2
- 235000019197 fats Nutrition 0.000 description 2
- 239000000945 filler Substances 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- VZCCETWTMQHEPK-UHFFFAOYSA-N gamma-Linolensaeure Natural products CCCCCC=CCC=CCC=CCCCCC(O)=O VZCCETWTMQHEPK-UHFFFAOYSA-N 0.000 description 2
- 229960002733 gamolenic acid Drugs 0.000 description 2
- 230000007407 health benefit Effects 0.000 description 2
- 239000000416 hydrocolloid Substances 0.000 description 2
- 235000020778 linoleic acid Nutrition 0.000 description 2
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 description 2
- 229960004488 linolenic acid Drugs 0.000 description 2
- 229920001542 oligosaccharide Polymers 0.000 description 2
- 230000003647 oxidation Effects 0.000 description 2
- 238000007254 oxidation reaction Methods 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 235000020995 raw meat Nutrition 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 229920000856 Amylose Polymers 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 235000021298 Dihomo-γ-linolenic acid Nutrition 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000006297 dehydration reaction Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000000378 dietary effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229940090949 docosahexaenoic acid Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000000428 dust Substances 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 238000005243 fluidization Methods 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 description 1
- 229940080345 gamma-cyclodextrin Drugs 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000008131 glucosides Chemical group 0.000 description 1
- 235000004280 healthy diet Nutrition 0.000 description 1
- 230000000999 hypotriglyceridemic effect Effects 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 150000002617 leukotrienes Chemical class 0.000 description 1
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- 229910052700 potassium Inorganic materials 0.000 description 1
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- 229910052708 sodium Inorganic materials 0.000 description 1
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- 238000005507 spraying Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/30—Foods or foodstuffs containing additives; Preparation or treatment thereof containing carbohydrate syrups; containing sugars; containing sugar alcohols, e.g. xylitol; containing starch hydrolysates, e.g. dextrin
- A23L29/35—Degradation products of starch, e.g. hydrolysates, dextrins; Enzymatically modified starches
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
- A23P20/00—Coating of foodstuffs; Coatings therefor; Making laminated, multi-layered, stuffed or hollow foodstuffs
- A23P20/10—Coating with edible coatings, e.g. with oils or fats
- A23P20/12—Apparatus or processes for applying powders or particles to foodstuffs, e.g. for breading; Such apparatus combined with means for pre-moistening or battering
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
- A23D9/00—Other edible oils or fats, e.g. shortenings, cooking oils
- A23D9/02—Other edible oils or fats, e.g. shortenings, cooking oils characterised by the production or working-up
- A23D9/04—Working-up
- A23D9/05—Forming free-flowing pieces
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
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- A23K20/158—Fatty acids; Fats; Products containing oils or fats
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K20/00—Accessory food factors for animal feeding-stuffs
- A23K20/10—Organic substances
- A23K20/163—Sugars; Polysaccharides
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23K—FODDER
- A23K40/00—Shaping or working-up of animal feeding-stuffs
- A23K40/30—Shaping or working-up of animal feeding-stuffs by encapsulating; by coating
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A—HUMAN NECESSITIES
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
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- A—HUMAN NECESSITIES
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- A23P10/00—Shaping or working of foodstuffs characterised by the products
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A23P20/00—Coating of foodstuffs; Coatings therefor; Making laminated, multi-layered, stuffed or hollow foodstuffs
- A23P20/10—Coating with edible coatings, e.g. with oils or fats
- A23P20/15—Apparatus or processes for coating with liquid or semi-liquid products
- A23P20/18—Apparatus or processes for coating with liquid or semi-liquid products by spray-coating, fluidised-bed coating or coating by casting
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K31/202—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
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Abstract
本发明申请涉及用于包被包含PUFA(和/或其盐)的固体颗粒的新颖包衣体系,其中所述包衣包含至少一种环糊精。此外,本发明申请涉及包被有所述包衣体系的组合物,以及所述组合物在生产食品、饲料、膳食补充剂和/或药品中的用途。
Description
本专利申请涉及用于包被包含PUFA(和/或其盐)的固体颗粒的新颖包衣体系,其中所述包衣包含至少一种环糊精。此外,本专利申请涉及包被有所述包衣体系的组合物,以及所述组合物在生产食品、饲料、膳食补充剂和/或药品中的用途。
多不饱和脂肪酸(PUFA)及其盐(例如Na、K或Ca盐)是非常熟知的用于健康饮食的化合物(尤其是ω-3脂肪酸)。PUFA(尤其是ω-3脂肪酸)具有多种健康益处,例如针对心血管疾病(CVD)的健康益处,包括公认的降低血甘油三酯(hypotriglyceridemic)和抗炎效果。
PUFA可以在多种植物和动物中找到。ω-3脂肪酸的一种非常好的来源是,即鱼。
或者,PUFA也可以合成生产。
由于实际上许多消费者不喜欢鱼,因此将PUFA(和/或其盐)添加到其他膳食产品中(使这些产品富含PUFA)是非常常见的。
PUFA及其盐的问题在于:它们具有强烈的氧化倾向。这导致产品中的PUFA损失,并且(甚至更糟地)导致产生强烈且非常难闻的气味。
随着双键数目的增加,PUFA经受增加的氧化降解并产生不期望的“异味”,主要是鱼腥和腐臭的气味和味道。
挥发性降解产物即使在非常低的浓度下也会导致异味。即使在可以分析检测到PUFA损失之前,产品的感官特性也可变得不可接受。
通过形成包合配合物来稳定PUFA是公知的用于包封疏水性物质的技术。然而,作为PUFA的递送形式,这些包合配合物具有一些严重的缺点。
由于包合配合物以1:1的摩尔比形成的事实。这限制了所得粉末的最大有效负载。还认为,在PUFA甘油三酯的情况下,仅一个PUFA链进入环糊精的空腔,而其它的未得到保护(并且它们可以容易被氧化)。最后,包封的PUFA形式的主要缺点不是PUFA氧化的损失,而是形成非常少量的挥发性降解产物,从而导致产品的鱼腥、颜料(painty)或腐臭气味。如Hadaruga等(Hadaruga,Daniel I.;Unlusayin,Mustafa;Gruia,Alexandra T.;Birau,Cristina;Rusu,Gerlinde;Hadaruga,Nicoleta G.,Beilstein Journal of OrganicChemistry(2016),12,179-191,doi:10.3762/bjoc.12.20)所示,含有环糊精的包合配合物可以减少但不能完全防止PUFA氧化,因此少量挥发性降解产物的问题不能通过在环糊精包合配合物中包封PUFA来解决。
现在,本发明的目的是提供具有高含量PUFA(基于粉末制剂的总重量,通常多于10重量%(wt-%))的粉末制剂,其在产生不期望的“异味”方面具有显著改善的稳定性。
换句话说,根据本发明的具有高含量PUFA(和/或其盐)的粉末制剂即使在储存后也不会有不好的气味(鱼腥味)。
出乎意料地发现:当使用包含至少10重量%(基于包衣体系的总重量)的至少一种环糊精的包衣体系时,包含PUFA(和/或其盐)的这种经包被的固体颗粒没有(或具有显著降低的)产生不希望的“异味”的倾向。
我们发现:当含有PUFA的粉末包被有环糊精层时,能够获得对PUFA制剂的感官稳定性的有益效果。在这种情况下,环糊精不与PUFA形成包合配合物,而是与上述少量挥发性降解产物形成包合配合物。由于不需要与PUFA的1:1摩尔比,因此能够实现高得多的有效负载。
因此,本发明涉及包衣体系(CS),其包含
基于所述包衣体系的总重量,至少10重量%的环糊精。
环糊精(有时称为环状直链淀粉(cycloamyloses))是由结合在一起成环的糖分子(环状低聚糖)构成的化合物家族。
环糊精是从淀粉通过酶促转化产生的。它们由5个或更多个1->4连接的α-D-吡喃葡萄糖苷单元构成,如在直链淀粉(淀粉片段)中那样。5元大环不是天然的。目前,最大的充分表征的环糊精含有32个1,4-脱水吡喃葡萄糖苷单元,而作为未充分表征的混合物,还已知至少150元的环状低聚糖。
典型的环糊精在环中含有范围为6至8个单元的数量的葡萄糖单体,形成锥形。它们可分为三组:
α(阿尔法)-环糊精:6元糖环分子
β(贝塔)-环糊精:7-元糖环分子
γ(伽马)-环糊精:8元糖环分子。
包衣体系可以是纯的环糊精(其可以是单一环糊精或α-环糊精和/或β-环糊精和/或γ-环糊精的混合物)。
因此,本发明涉及包衣体系(CS1),其是由环糊精组成的包衣体系(CS)。
因此,本发明涉及包衣体系(CS1'),其是由单一环糊精组成的包衣体系(CS1)。
因此,本发明涉及包衣体系(CS1”),其是由α-环糊精和/或β-环糊精和/或γ-环糊精的混合物组成的包衣体系(CS1)。
因此,本发明涉及包衣体系(CS2),其是包含单一环糊精的包衣体系(CS)。
因此,本发明涉及包衣体系(CS2'),其是包含α-环糊精和/或β-环糊精和/或γ-环糊精的混合物的包衣体系(CS)。
包衣体系可以包含另外的辅助化合物,例如粘合剂,形成化合物(例如水胶体,其可以是多糖或蛋白质),塑化剂(例如糖类,如蔗糖或糖衍生物(甘露醇、山梨糖醇),甘油,甘油单酯和甘油二酯,乙酰化甘油单酯,聚乙二醇(PEG),聚丙二醇),填料,染料,香料,抗氧化剂等。
基于包衣体系的总重量,这些成分的用量可以为至多90重量%。
因此,本发明涉及包衣体系(CS3),其是这样的包衣体系(CS)、(CS2)或(CS2'),其包含至少一种辅助化合物(基于包衣体系的总重量,至多90重量%的至少一种辅助化合物)。
因此,本发明涉及包衣体系(CS3'),其是这样的包衣体系(CS3),其中至少一种辅助化合物选自粘合剂,形成化合物(例如水胶体,其可以是多糖或蛋白质),塑化剂(例如糖类,如蔗糖或糖衍生物(甘露醇、山梨糖醇),甘油,甘油单酯和甘油二酯,乙酰化甘油单酯,聚乙二醇(PEG),聚丙二醇),填料,染料,香料和抗氧化剂。
根据本发明的优选塑化剂是糖类,如蔗糖或糖衍生物(甘露醇、山梨糖醇),甘油,甘油单酯和甘油二酯,乙酰化甘油单酯,聚乙二醇(PEG),聚丙二醇。优选地,PEG的分子量为200-6000。显然,可以使用一种单一的塑化剂以及两种或更多种塑化剂的混合物。
因此,本发明涉及包衣体系(CS3”),其是这样的包衣体系(CS3)或(CS3'),其至少包含选自以下的塑化剂:蔗糖或糖衍生物(甘露醇、山梨糖醇),甘油,甘油单酯和甘油二酯,乙酰化甘油单酯,聚乙二醇(PEG),聚丙二醇(优选地,PEG的分子量为200-6000)。
根据本发明的包衣体系被用于包被包含PUFA(和/或其盐)的(颗粒状)固体制剂。这种经包被的体系包含核(包含一种PUFA或多种PUFA的混合物)和包衣体系。
根据分子的碳链中双键的位置,PUFA被分类为n-9PUFA、n-6PUFA或n-3PUFA。n-6PUFA的实例是亚油酸(C18:2),花生四烯酸(C20:4),γ-亚麻酸(GLA,C18:13)和二高-γ-亚麻酸(DGLA,C20:3)。n-3PUFA的实例是α-亚麻酸(C18:13),二十碳五烯酸(EPA,C20:5)和二十二碳六烯酸(DHA,C22:6)。特别地,EPA和DHA近年来引起了食品行业的兴趣。这两种脂肪酸的最有用来源是鱼和从其中提取的海洋油。合适的PUFA盐是钠盐、钾盐或钙盐。
因此,本发明还涉及经包被的组合物(CC),所述组合物包含
(a)核,其是包含至少一种PUFA(和/或其盐)的固体制剂,和
(b)包衣体系,其包含
(i)至少一种环糊精。
PUFA未被包封在环糊精中。
因此,本发明还涉及经包被的组合物(CC1),其是这样的经包被的组合物(CC),其中至少一种PUFA选自n-9PUFA、n-6PUFA或n-3PUFA和/或其盐(尤其是钠盐、钾盐或钙盐)。
因此,本发明还涉及经包被的组合物(CC1'),其是这样的经包被的组合物(CC)或(CC1),其中至少一种PUFA选自亚油酸(C18:2)、花生四烯酸(C20:4)、γ-亚麻酸(GLA,C18:13)、二高-γ-亚麻酸(DGLA,C20:3)、α-亚麻酸(C18:13)、二十碳五烯酸(EPA,C20:5)和二十二碳六烯酸(DHA,C22:6)和/或其盐(尤其是钠盐、钾盐或钙盐)。
包衣体系(b)的所有优选都适用于上述经包被的组合物。
此外,核可以包含另外的成分,通常是用于生产所述化合物的添加剂,或可用于向其中掺入本发明组合物的产品的添加剂。组合物的核可以是任何形式。例如可以是包含活性成分的珠粒(beadlet)形式。可以用根据本发明的包衣体系包被的合适的珠粒可以在WO2007/045488中找到。
此外,本发明涉及经包被的组合物(CC2),其是这样的经包被的组合物(CC)、(CC1)或(CC1'),其包含
(i)基于所述组合物的总重量,70-99.5重量%的核,和
(ii)基于所述组合物的总重量,0.5-30重量%的包衣体系。
基于核的总重量,核通常含有至少10重量%、优选至少15重量%至多达50重量%的PUFA(和/或其盐)。
因此,本发明涉及经包被的组合物(CC3),其是这样的经包被的组合物(CC)、(CC1)、(CC1')或(CC2),其中基于核的总重量,核包含至少10重量%的PUFA(和/或其盐)。
因此,本发明涉及经包被的组合物(CC3'),其是这样的经包被的组合物(CC)、(CC1)、(CC1')或(CC2),其中基于核的总重量,核包含15重量%至50重量%的PUFA(和/或其盐)。
核的形状以及经包被的颗粒的形状不是本发明的必要特征。形状可以是球形或任何其他形式(也可以是各种形状的混合物)。通常且优选地,颗粒是球状的。
根据本发明的包衣体系以层的形式围绕核。通常(并且理想地),包衣覆盖颗粒的整个表面。此外,所述层在核的表面上通常(并且理想地)等厚。
包衣体系的所有优选都适用于上述组合物。
核的尺寸以及经包被颗粒的尺寸不是本发明的必要特征。
经包被的颗粒通常具有使得可以压制片剂的尺寸。
合适的尺寸在50-1000μm(优选100-800μm)之间;尺寸通过颗粒的最长维度的直径来限定,并通过公知的方法(如激光衍射)测量。
因此,本发明涉及经包被的组合物(CC4),其是这样的经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)或(CC3'),其中经包被颗粒的平均粒度为50-1000μm。
因此,本发明涉及经包被的组合物(CC4'),其是这样的经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)或(CC3'),其中经包被颗粒的平均粒度为100-800μm。
使用英国Malvern Instruments Ltd.的“Master-sizer 3000”,通过激光衍射技术测定所有粒度。关于该粒度表征方法的进一步信息可以例如参见"Basic principles ofparticle size analytics",Dr.Alan Rawle,Malvern Instruments Limited,EnigmaBusiness Part,Grovewood Road,Malvern,Worcestershire,WR14 1XZ,UK和"Manual ofMalvern particle size analyzer"。特别参考用户手册号MAN 0096,第1.0期,1994年11月。如果没有其他说明,提到的所有粒度都是通过激光衍射测定的Dv90值(体积直径,总体的90%低于该点,10%高于该点)。粒度可以以干燥形式测定。
经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)、(CC3')、(CC4)和(CC4')可以根据非常熟知的方法生产,例如喷雾干燥、转鼓干燥、喷雾造粒、附聚或珠粒。通常,如下制备经包被的颗粒:
(i)通过公知且广泛使用的方法生产核(其包含PUFA);
(ii)在第二步中用包衣材料(环糊精)的溶液、分散体或浆体包被核(固体颗粒)。通常通过将包衣材料溶解或悬浮在水或水溶液中来制备溶液、分散体或浆体。也可以使用其他合适的溶剂,例如醇-水混合物。可以通过公知的技术(如流化床包被或Wurster包被)施加包衣;
(iii)然后将经包被的颗粒干燥并可用于其他目的。
经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)、(CC3')、(CC4)和(CC4')发明可用于其中此类脂溶性成分的使用有用的任何种类的制剂中。通常用于食品、饲料产品、膳食补充剂和/或药品中。
因此,本发明涉及经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)、(CC3')、(CC4)和(CC4')在生产食品、饲料产品、膳食补充剂和/或药品中的用途。
因此,本发明涉及食品、饲料产品、膳食补充剂和/或药品的生产,其中使用经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)、(CC3')、(CC4)和(CC4')。
食品、饲料产品、膳食补充剂和/或药品可以是任何形式(液体、凝胶状或固体)。
如上所述,这些经包被的组合物在储存后不会“有鱼腥味”。
根据本发明的组合物还可以用作膳食补充剂或用于膳食补充剂中。膳食补充剂可以是任何形式。
根据本发明的经包被的组合物还可以用于药品中。药品可以是任何盖仑制剂形式,通常是片剂形式。
本发明的另一个实施方式涉及食品、饲料产品、膳食补充剂和/或药品,其包含至少一种经包被的组合物(CC)、(CC1)、(CC1')、(CC2)、(CC3)、(CC3')、(CC4)和/或(CC4')。
附图:
图1示出了本发明的构思。其将根据本发明的经包被的组合物与现有技术实施方式进行比较。
通过以下实施例阐释本发明。所有温度均以℃给出,所有份和百分比均与重量相关。
实施例1:
通过将9gβ-环糊精溶解/分散在216g水中来制备含有4%β-环糊精的水溶液。
使用Wurster技术在实验室规模的流化床处理器中将含有约400mg/g PUFA(主要是DHA和EPA)的150g珠粒流化。在55-64℃的产物温度下,将环糊精溶液喷雾在流化颗粒上。喷雾后,将产物在处理器中在49-59℃下干燥。获得了经包被的珠粒的自由流动粉末。产物具有中性气味,察觉不到鱼腥味或腐臭味。
Claims (6)
1.一种包衣体系,其包含
基于所述包衣体系的总重量,至少10重量%的环糊精。
2.一种经包被的组合物,其包含
(a)核,所述核是包含至少一种PUFA(和/或其盐)的固体制剂,和
(b)根据权利要求1所述的包衣体系。
3.根据权利要求2所述的经包被的组合物,其包含
(a)基于所述组合物的总重量,70-99.5重量%的核,和
(b)基于所述组合物的总重量,0.5-30重量%的包衣体系。
4.一种生产根据权利要求2或3所述的经包被的组合物的方法,其特征在于
(i)在第一步中通过珠粒法、喷雾干燥或喷雾造粒制备所述核(其包含PUFA(和/或其盐)),
(ii)在第二步中用包衣材料(环糊精)的溶液、分散体或浆体包被这些核(固体颗粒),和
(iii)然后干燥经包被的颗粒。
5.根据权利要求2或3所述的经包被的颗粒在食品、饲料产品、膳食补充剂和/或药品中的用途。
6.食品、饲料产品、膳食补充剂和/或药品,其包含至少一种根据权利要求2或3所述的经包被的组合物。
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EP16157690.5 | 2016-02-26 | ||
EP16157690 | 2016-02-26 | ||
PCT/EP2017/053860 WO2017144436A1 (en) | 2016-02-26 | 2017-02-21 | Novel coating system (i) |
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CN108697126A true CN108697126A (zh) | 2018-10-23 |
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CN201780013484.5A Pending CN108697126A (zh) | 2016-02-26 | 2017-02-21 | 新颖的包衣体系(i) |
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US (2) | US20190053531A1 (zh) |
EP (1) | EP3419438A1 (zh) |
JP (2) | JP2019515964A (zh) |
KR (1) | KR20180115763A (zh) |
CN (1) | CN108697126A (zh) |
BR (1) | BR112018017339B1 (zh) |
WO (1) | WO2017144436A1 (zh) |
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CN107788519A (zh) * | 2017-11-09 | 2018-03-13 | 重庆壹姐润物食品科技有限公司 | 一种增强记忆力的即食燕窝及其制备方法 |
CN108420795B (zh) * | 2018-03-28 | 2020-08-21 | 湖南安邦制药有限公司 | 止血调经颗粒的制备方法 |
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Also Published As
Publication number | Publication date |
---|---|
BR112018017339A2 (pt) | 2018-12-26 |
EP3419438A1 (en) | 2019-01-02 |
WO2017144436A1 (en) | 2017-08-31 |
US20230148650A1 (en) | 2023-05-18 |
JP2021191749A (ja) | 2021-12-16 |
US20190053531A1 (en) | 2019-02-21 |
JP2019515964A (ja) | 2019-06-13 |
KR20180115763A (ko) | 2018-10-23 |
BR112018017339B1 (pt) | 2022-11-16 |
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