JP2521612C - - Google Patents

Info

Publication number

JP2521612C

JP2521612C JP2521612C JP 2521612 C JP2521612 C JP 2521612C JP 2521612 C JP2521612 C JP 2521612C

Authority

JP

Japan

Prior art keywords

cyclodextrin

weight

parts

mcc

tablet

Prior art date

1999-11-15

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.)

Expired - Lifetime

Links

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• 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 25
• 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 25
• 239000008108 microcrystalline cellulose Substances 0.000 claims description 25
• 229940016286 microcrystalline cellulose Drugs 0.000 claims description 25
• 229920000858 Cyclodextrin Polymers 0.000 claims description 22
• 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 claims description 18
• 229960004853 betadex Drugs 0.000 claims description 17
• 239000001116 FEMA 4028 Substances 0.000 claims description 15
• 235000011175 beta-cyclodextrine Nutrition 0.000 claims description 15
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 14
• 239000000203 mixture Substances 0.000 claims description 13
• 239000011230 binding agent Substances 0.000 claims description 9
• 238000001035 drying Methods 0.000 claims description 9
• 238000002156 mixing Methods 0.000 claims description 9
• 238000000034 method Methods 0.000 claims description 8
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 7
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
• 229920001450 Alpha-Cyclodextrin Polymers 0.000 claims description 4
• 238000005550 wet granulation Methods 0.000 claims description 4
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 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 claims description 3
• 229940043377 alpha-cyclodextrin Drugs 0.000 claims description 3
• 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 claims description 3
• 229940080345 gamma-cyclodextrin Drugs 0.000 claims description 3
• 239000008240 homogeneous mixture Substances 0.000 claims 1
• 239000011872 intimate mixture Substances 0.000 claims 1
• 238000011049 filling Methods 0.000 description 7
• 239000000843 powder Substances 0.000 description 5
• 239000000463 material Substances 0.000 description 4
• 239000002245 particle Substances 0.000 description 4
• 239000000725 suspension Substances 0.000 description 4
• 239000013543 active substance Substances 0.000 description 3
• 238000004519 manufacturing process Methods 0.000 description 3
• 239000000047 product Substances 0.000 description 3
• 239000007921 spray Substances 0.000 description 3
• RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
• BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 2
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
• 235000021355 Stearic acid Nutrition 0.000 description 2
• 229960001138 acetylsalicylic acid Drugs 0.000 description 2
• 238000009826 distribution Methods 0.000 description 2
• 238000005469 granulation Methods 0.000 description 2
• 230000003179 granulation Effects 0.000 description 2
• 239000004615 ingredient Substances 0.000 description 2
• 238000002347 injection Methods 0.000 description 2
• 239000007924 injection Substances 0.000 description 2
• 239000008101 lactose Substances 0.000 description 2
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
• 229960005489 paracetamol Drugs 0.000 description 2
• 238000012216 screening Methods 0.000 description 2
• 239000007787 solid Substances 0.000 description 2
• 238000001694 spray drying Methods 0.000 description 2
• 238000005507 spraying Methods 0.000 description 2
• 239000008117 stearic acid Substances 0.000 description 2
• 238000003756 stirring Methods 0.000 description 2
• 239000000126 substance Substances 0.000 description 2
• FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
• 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 1
• 235000019739 Dicalciumphosphate Nutrition 0.000 description 1
• WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
• 239000007864 aqueous solution Substances 0.000 description 1
• 239000007900 aqueous suspension Substances 0.000 description 1
• WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
• 239000001506 calcium phosphate Substances 0.000 description 1
• 235000010980 cellulose Nutrition 0.000 description 1
• 229920002678 cellulose Polymers 0.000 description 1
• 239000001913 cellulose Substances 0.000 description 1
• 239000013065 commercial product Substances 0.000 description 1
• 238000007906 compression Methods 0.000 description 1
• 230000006835 compression Effects 0.000 description 1
• 239000008121 dextrose Substances 0.000 description 1
• NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
• 229940038472 dicalcium phosphate Drugs 0.000 description 1
• 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
• 239000007884 disintegrant Substances 0.000 description 1
• 239000012153 distilled water Substances 0.000 description 1
• 238000007580 dry-mixing Methods 0.000 description 1
• 239000000945 filler Substances 0.000 description 1
• 239000012467 final product Substances 0.000 description 1
• 239000012530 fluid Substances 0.000 description 1
• 238000011068 loading method Methods 0.000 description 1
• 230000001050 lubricating effect Effects 0.000 description 1
• 235000019359 magnesium stearate Nutrition 0.000 description 1
• 239000006069 physical mixture Substances 0.000 description 1
• 229920001592 potato starch Polymers 0.000 description 1
• 238000002360 preparation method Methods 0.000 description 1
• 239000000600 sorbitol Substances 0.000 description 1
• 235000010356 sorbitol Nutrition 0.000 description 1