CN105407742A - 具有芳环体系的有机酸或酯的改进粉末制剂 - Google Patents
具有芳环体系的有机酸或酯的改进粉末制剂 Download PDFInfo
- Publication number
- CN105407742A CN105407742A CN201480041773.2A CN201480041773A CN105407742A CN 105407742 A CN105407742 A CN 105407742A CN 201480041773 A CN201480041773 A CN 201480041773A CN 105407742 A CN105407742 A CN 105407742A
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- Prior art keywords
- powder formulation
- weight
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- calcium
- sodium
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- 239000000203 mixture Substances 0.000 title claims abstract description 54
- 238000009472 formulation Methods 0.000 title claims abstract description 46
- 150000007524 organic acids Chemical class 0.000 title abstract description 6
- 150000002148 esters Chemical class 0.000 title abstract description 5
- 125000003118 aryl group Chemical group 0.000 title abstract description 4
- 235000005985 organic acids Nutrition 0.000 title abstract description 3
- 239000000843 powder Substances 0.000 claims description 58
- 238000002360 preparation method Methods 0.000 claims description 53
- 150000001875 compounds Chemical class 0.000 claims description 38
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 18
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 14
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 12
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 12
- LFVGISIMTYGQHF-UHFFFAOYSA-N ammonium dihydrogen phosphate Chemical compound [NH4+].OP(O)([O-])=O LFVGISIMTYGQHF-UHFFFAOYSA-N 0.000 claims description 12
- 229910000387 ammonium dihydrogen phosphate Inorganic materials 0.000 claims description 12
- 239000012876 carrier material Substances 0.000 claims description 12
- 235000019837 monoammonium phosphate Nutrition 0.000 claims description 12
- 239000011780 sodium chloride Substances 0.000 claims description 9
- 235000002639 sodium chloride Nutrition 0.000 claims description 9
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims description 8
- 230000015572 biosynthetic process Effects 0.000 claims description 7
- 238000003786 synthesis reaction Methods 0.000 claims description 7
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 6
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 6
- 229940072033 potash Drugs 0.000 claims description 6
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Substances [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 6
- 235000015320 potassium carbonate Nutrition 0.000 claims description 6
- OTYBMLCTZGSZBG-UHFFFAOYSA-L potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 claims description 6
- 229910052939 potassium sulfate Inorganic materials 0.000 claims description 6
- 235000011151 potassium sulphates Nutrition 0.000 claims description 6
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- 239000001506 calcium phosphate Substances 0.000 claims description 5
- 235000013305 food Nutrition 0.000 claims description 5
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims description 4
- CBOCVOKPQGJKKJ-UHFFFAOYSA-L Calcium formate Chemical compound [Ca+2].[O-]C=O.[O-]C=O CBOCVOKPQGJKKJ-UHFFFAOYSA-L 0.000 claims description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- 229920001732 Lignosulfonate Polymers 0.000 claims description 4
- -1 MAP Substances 0.000 claims description 4
- CPLXHLVBOLITMK-UHFFFAOYSA-N Magnesium oxide Chemical compound [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims description 4
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims description 4
- DLRVVLDZNNYCBX-UHFFFAOYSA-N Polydextrose Polymers OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(O)O1 DLRVVLDZNNYCBX-UHFFFAOYSA-N 0.000 claims description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
- 235000019255 calcium formate Nutrition 0.000 claims description 4
- 239000004281 calcium formate Substances 0.000 claims description 4
- 229940044172 calcium formate Drugs 0.000 claims description 4
- PASHVRUKOFIRIK-UHFFFAOYSA-L calcium sulfate dihydrate Chemical compound O.O.[Ca+2].[O-]S([O-])(=O)=O PASHVRUKOFIRIK-UHFFFAOYSA-L 0.000 claims description 4
- 239000004927 clay Substances 0.000 claims description 4
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims description 4
- 235000013773 glyceryl triacetate Nutrition 0.000 claims description 4
- 239000001087 glyceryl triacetate Substances 0.000 claims description 4
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000377 silicon dioxide Substances 0.000 claims description 4
- 229910052938 sodium sulfate Inorganic materials 0.000 claims description 4
- 235000011152 sodium sulphate Nutrition 0.000 claims description 4
- 229910019142 PO4 Inorganic materials 0.000 claims description 3
- 229920002472 Starch Polymers 0.000 claims description 3
- 239000000440 bentonite Substances 0.000 claims description 3
- 229910000278 bentonite Inorganic materials 0.000 claims description 3
- SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 claims description 3
- KMQAPZBMEMMKSS-UHFFFAOYSA-K calcium;magnesium;phosphate Chemical compound [Mg+2].[Ca+2].[O-]P([O-])([O-])=O KMQAPZBMEMMKSS-UHFFFAOYSA-K 0.000 claims description 3
- GUJOJGAPFQRJSV-UHFFFAOYSA-N dialuminum;dioxosilane;oxygen(2-);hydrate Chemical compound O.[O-2].[O-2].[O-2].[Al+3].[Al+3].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O GUJOJGAPFQRJSV-UHFFFAOYSA-N 0.000 claims description 3
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims description 3
- 229940038472 dicalcium phosphate Drugs 0.000 claims description 3
- 150000004675 formic acid derivatives Chemical class 0.000 claims description 3
- 239000003292 glue Substances 0.000 claims description 3
- 239000004571 lime Substances 0.000 claims description 3
- 229910052901 montmorillonite Inorganic materials 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 3
- 102000004169 proteins and genes Human genes 0.000 claims description 3
- 108090000623 proteins and genes Proteins 0.000 claims description 3
- 235000019698 starch Nutrition 0.000 claims description 3
- 239000008107 starch Substances 0.000 claims description 3
- 239000010455 vermiculite Substances 0.000 claims description 3
- 235000019354 vermiculite Nutrition 0.000 claims description 3
- 229910052902 vermiculite Inorganic materials 0.000 claims description 3
- AOSFMYBATFLTAQ-UHFFFAOYSA-N 1-amino-3-(benzimidazol-1-yl)propan-2-ol Chemical compound C1=CC=C2N(CC(O)CN)C=NC2=C1 AOSFMYBATFLTAQ-UHFFFAOYSA-N 0.000 claims description 2
- 239000005995 Aluminium silicate Substances 0.000 claims description 2
- 239000005695 Ammonium acetate Substances 0.000 claims description 2
- WZUKKIPWIPZMAS-UHFFFAOYSA-K Ammonium alum Chemical compound [NH4+].O.O.O.O.O.O.O.O.O.O.O.O.[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O WZUKKIPWIPZMAS-UHFFFAOYSA-K 0.000 claims description 2
- ATRRKUHOCOJYRX-UHFFFAOYSA-N Ammonium bicarbonate Chemical compound [NH4+].OC([O-])=O ATRRKUHOCOJYRX-UHFFFAOYSA-N 0.000 claims description 2
- 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 claims description 2
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims description 2
- 229910000503 Na-aluminosilicate Inorganic materials 0.000 claims description 2
- 229920001100 Polydextrose Polymers 0.000 claims description 2
- 239000004113 Sepiolite Substances 0.000 claims description 2
- 229940037003 alum Drugs 0.000 claims description 2
- 235000012211 aluminium silicate Nutrition 0.000 claims description 2
- 235000019257 ammonium acetate Nutrition 0.000 claims description 2
- 229940043376 ammonium acetate Drugs 0.000 claims description 2
- 239000001099 ammonium carbonate Substances 0.000 claims description 2
- 235000012501 ammonium carbonate Nutrition 0.000 claims description 2
- 235000019270 ammonium chloride Nutrition 0.000 claims description 2
- 235000012241 calcium silicate Nutrition 0.000 claims description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Inorganic materials [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 2
- 235000011132 calcium sulphate Nutrition 0.000 claims description 2
- OIBDMJFLVFSCDS-UHFFFAOYSA-K calcium;magnesium;sodium;phosphate Chemical compound [Na+].[Mg+2].[Ca+2].[O-]P([O-])([O-])=O OIBDMJFLVFSCDS-UHFFFAOYSA-K 0.000 claims description 2
- XFWJKVMFIVXPKK-UHFFFAOYSA-N calcium;oxido(oxo)alumane Chemical compound [Ca+2].[O-][Al]=O.[O-][Al]=O XFWJKVMFIVXPKK-UHFFFAOYSA-N 0.000 claims description 2
- 239000004202 carbamide Substances 0.000 claims description 2
- 235000013877 carbamide Nutrition 0.000 claims description 2
- SHFGJEQAOUMGJM-UHFFFAOYSA-N dialuminum dipotassium disodium dioxosilane iron(3+) oxocalcium oxomagnesium oxygen(2-) Chemical compound [O--].[O--].[O--].[O--].[O--].[O--].[O--].[O--].[Na+].[Na+].[Al+3].[Al+3].[K+].[K+].[Fe+3].[Fe+3].O=[Mg].O=[Ca].O=[Si]=O SHFGJEQAOUMGJM-UHFFFAOYSA-N 0.000 claims description 2
- 235000011187 glycerol Nutrition 0.000 claims description 2
- 229910052622 kaolinite Inorganic materials 0.000 claims description 2
- 239000004310 lactic acid Substances 0.000 claims description 2
- 235000014655 lactic acid Nutrition 0.000 claims description 2
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 2
- 239000001095 magnesium carbonate Substances 0.000 claims description 2
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 2
- 235000014380 magnesium carbonate Nutrition 0.000 claims description 2
- 239000000395 magnesium oxide Substances 0.000 claims description 2
- 235000012245 magnesium oxide Nutrition 0.000 claims description 2
- GVALZJMUIHGIMD-UHFFFAOYSA-H magnesium phosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 claims description 2
- 239000004137 magnesium phosphate Substances 0.000 claims description 2
- 229960002261 magnesium phosphate Drugs 0.000 claims description 2
- 229910000157 magnesium phosphate Inorganic materials 0.000 claims description 2
- 235000010994 magnesium phosphates Nutrition 0.000 claims description 2
- 229960003390 magnesium sulfate Drugs 0.000 claims description 2
- 229910052943 magnesium sulfate Inorganic materials 0.000 claims description 2
- 235000019341 magnesium sulphate Nutrition 0.000 claims description 2
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims description 2
- 235000019799 monosodium phosphate Nutrition 0.000 claims description 2
- RHFUXPCCELGMFC-UHFFFAOYSA-N n-(6-cyano-3-hydroxy-2,2-dimethyl-3,4-dihydrochromen-4-yl)-n-phenylmethoxyacetamide Chemical compound OC1C(C)(C)OC2=CC=C(C#N)C=C2C1N(C(=O)C)OCC1=CC=CC=C1 RHFUXPCCELGMFC-UHFFFAOYSA-N 0.000 claims description 2
- 239000010451 perlite Substances 0.000 claims description 2
- 235000019362 perlite Nutrition 0.000 claims description 2
- 239000001259 polydextrose Substances 0.000 claims description 2
- 235000013856 polydextrose Nutrition 0.000 claims description 2
- 229940035035 polydextrose Drugs 0.000 claims description 2
- DJEHXEMURTVAOE-UHFFFAOYSA-M potassium bisulfite Chemical compound [K+].OS([O-])=O DJEHXEMURTVAOE-UHFFFAOYSA-M 0.000 claims description 2
- 229940099427 potassium bisulfite Drugs 0.000 claims description 2
- 235000010259 potassium hydrogen sulphite Nutrition 0.000 claims description 2
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical class CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 claims description 2
- 239000011435 rock Substances 0.000 claims description 2
- 235000019355 sepiolite Nutrition 0.000 claims description 2
- 229910052624 sepiolite Inorganic materials 0.000 claims description 2
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 claims description 2
- 235000012239 silicon dioxide Nutrition 0.000 claims description 2
- 239000000429 sodium aluminium silicate Substances 0.000 claims description 2
- 235000012217 sodium aluminium silicate Nutrition 0.000 claims description 2
- GJPYYNMJTJNYTO-UHFFFAOYSA-J sodium aluminium sulfate Chemical compound [Na+].[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GJPYYNMJTJNYTO-UHFFFAOYSA-J 0.000 claims description 2
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 claims description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 2
- VWDWKYIASSYTQR-UHFFFAOYSA-N sodium nitrate Chemical compound [Na+].[O-][N+]([O-])=O VWDWKYIASSYTQR-UHFFFAOYSA-N 0.000 claims description 2
- 239000001488 sodium phosphate Substances 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 229960002622 triacetin Drugs 0.000 claims description 2
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 2
- 229910000391 tricalcium phosphate Inorganic materials 0.000 claims description 2
- 235000019731 tricalcium phosphate Nutrition 0.000 claims description 2
- 229940078499 tricalcium phosphate Drugs 0.000 claims description 2
- 235000010216 calcium carbonate Nutrition 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 abstract description 6
- PVNIIMVLHYAWGP-UHFFFAOYSA-N nicotinic acid Natural products OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 13
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- 229960003512 nicotinic acid Drugs 0.000 description 8
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- 238000005259 measurement Methods 0.000 description 4
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- 238000005516 engineering process Methods 0.000 description 3
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- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
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- 229930003537 Vitamin B3 Natural products 0.000 description 1
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- 230000000994 depressogenic effect Effects 0.000 description 1
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- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
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- 125000000627 niacin group Chemical group 0.000 description 1
- DFPAKSUCGFBDDF-UHFFFAOYSA-N nicotinic acid amide Natural products NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
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Classifications
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- 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
- A23L3/00—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs
- A23L3/34—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs by treatment with chemicals
- A23L3/3454—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs by treatment with chemicals in the form of liquids or solids
- A23L3/3463—Organic compounds; Microorganisms; Enzymes
- A23L3/3481—Organic compounds containing oxygen
- A23L3/3508—Organic compounds containing oxygen containing carboxyl groups
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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
- 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
- A23L33/15—Vitamins
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- A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
- A23P10/00—Shaping or working of foodstuffs characterised by the products
- A23P10/40—Shaping or working of foodstuffs characterised by the products free-flowing powder or instant powder, i.e. powder which is reconstituted rapidly when liquid is added
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- A—HUMAN NECESSITIES
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- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0241—Containing particulates characterized by their shape and/or structure
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- A—HUMAN NECESSITIES
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
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- A61K8/24—Phosphorous; Compounds thereof
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- A—HUMAN NECESSITIES
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
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Abstract
本发明涉及包含大量的至少一种具有芳环体系的有机酸或酯的改进粉末制剂以及所述制剂的生产。
Description
本发明涉及改进的粉末制剂以及所述制剂的生产。
具有芳环体系的有机酸或酯的粉末制剂非常常见并且是有用的制剂。
这种有机酸或酯的实例是烟酸和苯甲酸。
烟酸(又名维生素B3、尼克酸和维生素PP)是必不可少的人营养素。
饮食中缺乏烟酸可引起糙皮病，其特征为腹泻、皮炎和痴呆，以及下颈部的“项链”损伤、色素沉着过度、皮肤增厚、口和舌发炎、消化失调、健忘症、精神错乱，以及如果不予治疗的话的最终死亡。烟酸缺乏还可引起精神病症状，例如易怒、精神集中不良、焦虑、疲乏、坐立不安、冷漠和抑郁。
苯甲酸及其盐被用作食品防腐剂。
遗憾的是，当以粉末形式使用这些有机酸时，这些制剂的确有爆炸的倾向。
即使粉末具有显著量的较大颗粒，也始终存在一定量的小颗粒。这些小颗粒是爆炸风险的原因。
在任何使用粉末的工艺中，粉尘爆炸都是巨大的风险。因此需要爆炸风险低的粉末制剂。但是粉末制剂必须仍然具有粉末的基本(和有利)特征，例如可自由流动、易于运输和易于配制剂量等。
从现有技术中已知，某些辅助化合物和载体材料可以使包含维生素E的粉末制剂的爆炸风险降至最低。
由于这种非爆炸性制剂的重要性，所以始终需要改进的制剂。
出人意料地，已发现：这样的粉末制剂的确具有低爆炸风险，所述粉末制剂包含大量(至少65重量％(wt-％))的
至少一种式(I)的化合物，
以及包含一种或更多种特定化合物(辅助化合物)，以及任选地
至少一种载体材料，
在式(I)中
X是–N-或–CH-，和
R1是H或C1-C4烷基部分。
因此，本申请涉及粉末制剂(I)，其包含：
(i)基于粉末制剂的总重量，65-95重量％(wt-％)的至少一种式(I)的化合物
其中
X是–N-或–CH-，和
R1是H或C1-C4烷基部分，以及
(ii)基于粉末制剂的总重量，5-35重量％的至少一种选自以下的辅助化合物：硫酸铝铵、硫酸铝钾、乙酸铵、亚硫酸氢铵、碳酸铵、氯化铵、磷酸二氢铵、碳酸氢铵、膨润土(bentonite)、蒙脱石(montmorillonite)、铝酸钙、碳酸钙、硅酸钙、合成二水硫酸钙、硫酸钙、高岭石黏土(例如高岭土)、硅藻土、珍珠岩、亚硫酸氢钾、碳酸氢钾、硫酸钾、碳酸钾、海泡石黏土(sepioliticclays)、硅酸、合成铝硅酸钠、硫酸铝钠、硫酸氢钠、碳酸钠、氯化钠、碳酸氢钠、硫酸钠、蛭石(vermiculite)、碳酸钙、碳酸镁、石灰质海藻(calcareousmarinealgae)、氧化镁、硫酸镁、磷酸二钙、磷酸三钙、磷酸一二钙(mono-dicalciumphosphate)、去氟磷酸岩、磷酸一钙、磷酸钙镁(calcium-magnesiumphosphate)、磷酸一铵、磷酸镁、磷酸钠钙镁(sodium-calcium-magnesiumphosphate)、磷酸一钠、甘油、丙二醇(E1520)、三乙酸甘油酯(E1518)、山梨糖醇(E420)、聚葡萄糖、乳酸和尿素，以及任选地
(iii)基于粉末制剂的总重量，至多40重量％的载体材料。
优选地，在式(I)的定义中，R1是H、CH3、CH2CH3、(CH2)2CH3和(CH2)3CH3。更优选地，R1是H或CH3。
因此，本发明涉及粉末制剂(I’)，其是制剂(I)，其中在式(I)的定义中，R1是H、CH3、CH2CH3、(CH2)2CH3和(CH2)3CH3。
因此，本发明涉及粉末制剂(I”)，其是制剂(I)，其中在式(I)的定义中，R1是H或CH3。
在本发明的语境中，特定化合物(ii)也被定义为辅助化合物。
式(Ia)和(Ib)的化合物是优选的
因此，本发明涉及粉末制剂(II)，其是制剂(I)、(I’)或(I”)，其中式(I)的化合物是式(Ia)和/或(Ib)的化合物
优选地，辅助化合物的平均粒径(d0.5)(在粉末制剂中)为10μm-100μm。
因此，本发明涉及粉末制剂(III)，其是制剂(I)、(I’)、(I”)或(II)，其中辅助化合物的平均粒径(d0.5)(在粉末制剂中)为10μm-100μm。
此外，本发明的一个优选实施方式涉及粉末制剂，其包含基于粉末制剂的总重量的70-90重量％的至少一种式(I)的化合物。
此外，本发明的一个优选实施方式涉及粉末制剂，其包含基于粉末制剂的总重量的10-30重量％的至少一种辅助化合物。
因此，本发明还涉及制剂(IV)，其是制剂(I)、(I’)、(I”)、(II)或(III)，其中所述制剂包含基于粉末制剂的总重量的70-90重量％的至少一种式(I)的化合物。
因此，本发明还涉及制剂(V)，其是制剂(I)、(I’)、(I”)、(II)、(III)或(IV)，其中所述制剂包含基于粉末制剂的总重量的10-30重量％的至少一种辅助化合物。
利用MalvernMasterSizer2000测量平均粒径。在该激光衍射测量中，使颗粒通过聚焦激光束。这些颗粒以与其大小成反比的角度散射光。然后使用一系列光敏探测器测量散射光的角强度。相对于角的散射强度图谱是用于计算粒径的主要信息来源。对于干材料(例如应用的添加剂)的测量，使用干粉送料机(MalvernScirocco)。
通常利用标准化方法(EN13821:2002(测量粉尘/空气混合物的最低着火能量))来测量粉末(粉尘)的爆炸风险。使用该方法测量本专利申请中的所有MIE值。该方法允许测量粉末的最低着火能量(MIE)。MIE是(例如由于静电放电)引燃可燃烟雾、气体或尘雾所需的最低能量的量。MIE以焦耳(J)测量。
用于根据EN13821:2002中的程序测量的粉末颗粒的平均粒径为≤63μm。
使用可购于AdolfKühnerAG(Birsfelden，CH)的改进Hartmann管(MIKE3型)测量本专利申请中的所有MIE值。该器材经专门设计以允许测量极低的着火能量。通过安装不同的电容器实现该目的。电容器被设计为储存1mJ、3mJ、10mJ、30mJ、100mJ、300mJ和1000mJ的能量。
当测量包含至少一种式(I)的化合物的市售粉末制剂的MIE时，它们通常在1-3mJ的范围内。这意味着极低量的能量足以引起爆炸。
另一方面，根据本发明的制剂的MIE值为10-1000mJ(或甚至高于1000mJ)。
因此，本发明涉及制剂(VI)，其为制剂(I)、(I’)、(I”)、(II)、(III)、(IV)或(V)，其的MIE值为10-1000mJ(通过EN13821:2002的方法测量)。MIE值甚至可以高于1000mJ。
根据本发明的制剂是干燥的粉末。但取决于生产工艺和贮存条件，所述制剂可包含一些水。水含量通常低于基于制剂的总重量的5重量％。
因此，本发明的另一个实施方式涉及制剂(VII)，其为制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)或(VI)，其中存在基于制剂的总重量的0-5重量％的水。
优选地，所述粉末制剂不包含以上所公开的成分/化合物之外的其它成分/化合物。它们不包含任何常用的稳定剂、表面活性成分或糖。
式(I)的化合物可以来自天然来源或者它们可以被合成。由于分离工艺或生产工艺的性质，可能存在微量的副产物。
任选地用于根据本发明所述制剂的载体材料是通常已知和使用的载体材料。合适的载体材料是合成生产的沉淀二氧化硅或甲酸盐(例如甲酸钙)。这种载体材料由多孔的颗粒组成。其它合适的载体材料是蛋白质、淀粉、木质素磺酸盐(lignosulfonates)和胶(gum)。
本发明的一些优选制剂是制剂(VIII)，其中制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)或(VII)包含
(ii)基于制剂的总重量，5-35重量％(优选地10-30重量％)的至少一种选自以下的化合物：磷酸二氢铵、(纯化的)硅藻土、碳酸氢钾、硫酸钾、碳酸钾、氯化钠和碳酸氢钠。
更优选的是制剂(VIII’)，其是MIE值为10-1000mJ(通过EN13821:2002的方法测量)的制剂(VIII)。MIE值甚至可以高于1000mJ。
还更优选的是制剂(VIII”)，其是制剂(VIII’)，其中辅助化合物的平均粒径(d0.5)为10μm-100μm。
还优选的是制剂(IX)，其是制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)、(VIII’)或(VIII”)，其包含
(iii)基于制剂的总重量，至多40重量％的至少一种选自以下的载体材料：合成生产的沉淀二氧化硅、甲酸盐(例如甲酸钙)、蛋白质、淀粉、木质素磺酸盐和胶。
本发明的一个尤其优选的实施方式涉及制剂(X)，其由以下组成：
(i)基于粉末制剂的总重量，65-95重量％(优选地70-90重量％)的
和
(ii)基于粉末制剂的总重量，5-35重量％(优选地10-30重量％)的至少一种选自以下的辅助化合物：磷酸二氢铵、(纯化的)硅藻土、碳酸氢钾、硫酸钾、碳酸钾、氯化钠、硫酸钠和碳酸氢钠，和
基于粉末制剂的总重量，0-5重量％的水。
为了生产根据本发明所述的粉末(制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)、(VIII’)、(VIII”)、(IX)或(X))，将至少一种式(I)的化合物与至少一种辅助化合物混合。该过程可通过利用任何常用的混合器(blender)来实施。对本发明而言，添加化合物的顺序并不关键。
如果使用载体材料，则通过将至少一种式(I)的化合物喷在载体材料上，然后加入至少一种辅助化合物并混合制剂来生产根据本发明的粉末(制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)、(VIII’)、(VIII”)、(IX)或(X))。
还可以将至少一种式(I)的化合物喷在至少一种载体材料和至少一种辅助化合物的混合物上。
所有以上所公开的制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)、(VIII’)、(VIII”)、(IX)或(X)都可原样使用或用于食品、饲料产品和个人护理品中。
所有以上所公开的制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)、(VIII’)、(VIII”)、(IX)或(X)都可原样用于食品、饲料产品和个人护理品的生产中。
此外，本发明还涉及包含制剂(I)、(I’)、(I”)、(II)、(III)、(IV)、(V)、(VI)、(VII)、(VIII)、(VIII’)、(VIII”)、(IX)或(X)中的至少一种的食品、饲料产品和个人护理品。
通过下述实施例阐释本发明。给出的所有温度均为℃，所有的份和百分比均与重量相关。
实施例
实施例1
将900g苯甲酸(纯度99.9％)填充至合适的搅拌器(Nauta)中，加入63g粒径为54μm(利用激光衍射测定)的氯化钠。之后加入27g二氧化硅、5g甲酸钙和5g磷酸一钙，混合上述混合物10分钟。将得到的自由流动的白色粉末填充至容器中。
随后，在合适的设备(AlpineMultiprocessunit100AFG/50ATP)中使用60m3/h的空气流和2200rpm的筛轮转速对混合物进行空气分级，并收集细料(fines)。
利用激光衍射评估，颗粒平均为34μm，氯化钠含量为20.2重量％，苯甲酸含量为70.1重量％。根据上述EN13821:2002对细料进行分析，发现最低着火能量为10-30mJ。
实施例2
将750g烟酸(来自DSM的烟酸)(纯度99.5％)填充至合适的混合器(Turbula)中，并加入250g粒径为54μm(通过激光衍射分析)的氯化钠，然后混合上述混合物10分钟。然后将材料转移到RetschGrindomixer中并研磨(10000rpm/1分钟)。这种材料的中值粒径为23μm。将得到的白色粉末填充至容器中。
根据上述EN13821:2002对粉末进行分析，发现最低着火能量为300-1000mJ。
Claims (11)
1.粉末制剂，其包含:
(i)基于所述粉末制剂的总重量，65-95重量％的至少一种式(I)的化合物
其中
X是–N-或–CH-，和
R1是H或C1-C4烷基部分，以及
(ii)基于所述粉末制剂的总重量，5-35重量％的至少一种选自以下的辅助化合物：硫酸铝铵、硫酸铝钾、乙酸铵、亚硫酸氢铵、碳酸铵、氯化铵、磷酸二氢铵、碳酸氢铵、膨润土、蒙脱石、铝酸钙、碳酸钙、硅酸钙、合成二水硫酸钙、硫酸钙、高岭石黏土(例如高岭土)、硅藻土、珍珠岩、亚硫酸氢钾、碳酸氢钾、硫酸钾、碳酸钾、海泡石黏土、硅酸、合成铝硅酸钠、硫酸铝钠、硫酸氢钠、碳酸钠、氯化钠、碳酸氢钠、硫酸钠、蛭石、碳酸钙、碳酸镁、石灰质海藻、氧化镁、硫酸镁、磷酸二钙、磷酸三钙、磷酸一二钙、去氟磷酸岩、磷酸一钙、磷酸钙镁、磷酸一铵、磷酸镁、磷酸钠钙镁、磷酸一钠、甘油、丙二醇(E1520)、三乙酸甘油酯(E1518)、山梨糖醇(E420)、聚葡萄糖、乳酸和尿素。
2.根据权利要求1所述的粉末制剂，其中式(I)的化合物为式(Ia)和/或(Ib)的化合物
3.根据在前权利要求中任一项所述的粉末制剂，其中所述辅助化合物的平均粒径(d0.5)(在粉末制剂中)为10μm-100μm。
4.根据在前权利要求中任一项所述的粉末制剂，其中所述制剂的MIE值为10-1000mJ。
5.根据在前权利要求1-3中任一项所述的粉末制剂，其中所述制剂的MIE值大于1000mJ。
6.根据在前权利要求中任一项所述的粉末制剂，其包含基于所述制剂的总重量的0-5重量％的水。
7.根据在前权利要求中任一项所述的粉末制剂，其中所述制剂包含：
(ii)基于所述制剂的总重量，10-30重量％的至少一种选自以下的化合物：磷酸二氢铵、(纯化的)硅藻土、碳酸氢钾、硫酸钾、碳酸钾、氯化钠和碳酸氢钠。
8.根据在前权利要求中任一项所述的粉末制剂，其中所述制剂包含：
(iii)基于所述制剂的总重量，至多40重量％的至少一种选自以下的载体材料：合成生产的沉淀二氧化硅、甲酸盐(例如甲酸钙)、蛋白质、淀粉、木质素磺酸盐和胶。
9.粉末，其由以下组成：
(i)基于粉末制剂的总重量，65-95重量％(优选地70-90重量％)的
(ii)基于粉末制剂的总重量，5-35重量％(优选地10-30重量％)的至少一种选自以下的辅助化合物：磷酸二氢铵、(纯化的)硅藻土、碳酸氢钾、硫酸钾、碳酸钾、氯化钠、硫酸钠和碳酸氢钠，和
基于粉末制剂的总重量，0-5重量％的水。
10.至少一种根据权利要求1-9中任一项所述的制剂在食品、饲料产品和个人护理品中的用途。
11.食品、饲料产品和个人护理品，其包含至少一种根据权利要求1-9中任一项所述的制剂。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13178144 | 2013-07-26 | ||
| EP13178144.5 | 2013-07-26 | ||
| PCT/EP2014/066050 WO2015011271A1 (en) | 2013-07-26 | 2014-07-25 | Improved powderous formulations of organic acids or esters having an aromatic ring system |
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| Publication Number | Publication Date |
|---|---|
| CN105407742A true CN105407742A (zh) | 2016-03-16 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| CN201480041773.2A Pending CN105407742A (zh) | 2013-07-26 | 2014-07-25 | 具有芳环体系的有机酸或酯的改进粉末制剂 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9693938B2 (zh) |
| EP (1) | EP3033328B1 (zh) |
| JP (1) | JP6572475B2 (zh) |
| KR (1) | KR20160036559A (zh) |
| CN (1) | CN105407742A (zh) |
| BR (1) | BR112016001539B1 (zh) |
| ES (1) | ES2632766T3 (zh) |
| WO (1) | WO2015011271A1 (zh) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| TR201601828A2 (tr) * | 2016-02-11 | 2016-06-21 | Ramazan Sevgi | İnsanlarin ve kanatli hayvanlarin gida takvi̇yesi̇nde kullanilan saf pekmez topraği elde etme metodu |
| ES2899218T3 (es) * | 2017-02-14 | 2022-03-10 | Dsm Ip Assets Bv | Formulaciones dispersables en agua |
| CN113955837A (zh) * | 2021-10-18 | 2022-01-21 | 神美科技有限公司 | 一种无机-有机复合高分子水处理除氟絮凝剂及其制备方法 |
| WO2023186256A1 (en) * | 2022-03-28 | 2023-10-05 | Symrise Ag | Fireproofing agents |
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- 2014-07-25 EP EP14745109.0A patent/EP3033328B1/en not_active Not-in-force
- 2014-07-25 KR KR1020167001902A patent/KR20160036559A/ko active IP Right Grant
- 2014-07-25 WO PCT/EP2014/066050 patent/WO2015011271A1/en active Application Filing
- 2014-07-25 CN CN201480041773.2A patent/CN105407742A/zh active Pending
- 2014-07-25 BR BR112016001539A patent/BR112016001539B1/pt not_active IP Right Cessation
- 2014-07-25 ES ES14745109.0T patent/ES2632766T3/es active Active
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| US5008118A (en) * | 1987-06-23 | 1991-04-16 | Nippon Oil And Fats | Method for producing organic agent coated with powders of coating agent |
| EP0611590A1 (en) * | 1993-02-18 | 1994-08-24 | Asahi Glass Company Ltd. | Method for operating a filtration apparatus for flue gas |
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Also Published As
| Publication number | Publication date |
|---|---|
| EP3033328B1 (en) | 2017-05-17 |
| JP2016539636A (ja) | 2016-12-22 |
| US20160166483A1 (en) | 2016-06-16 |
| WO2015011271A1 (en) | 2015-01-29 |
| ES2632766T3 (es) | 2017-09-15 |
| JP6572475B2 (ja) | 2019-09-11 |
| US9693938B2 (en) | 2017-07-04 |
| BR112016001539B1 (pt) | 2020-06-09 |
| BR112016001539A8 (pt) | 2020-01-21 |
| KR20160036559A (ko) | 2016-04-04 |
| BR112016001539A2 (zh) | 2017-07-25 |
| EP3033328A1 (en) | 2016-06-22 |
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