CA2183952C - Produit ou comprime granulaire contenant un systeme effervescent et un principe actif pharmaceutique, et son procede de preparation - Google Patents
Produit ou comprime granulaire contenant un systeme effervescent et un principe actif pharmaceutique, et son procede de preparation Download PDFInfo
- Publication number
- CA2183952C CA2183952C CA002183952A CA2183952A CA2183952C CA 2183952 C CA2183952 C CA 2183952C CA 002183952 A CA002183952 A CA 002183952A CA 2183952 A CA2183952 A CA 2183952A CA 2183952 C CA2183952 C CA 2183952C
- Authority
- CA
- Canada
- Prior art keywords
- weight
- acid
- granular product
- tablet
- effervescent
- 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.)
- Expired - Fee Related
Links
- 239000003814 drug Substances 0.000 title claims description 29
- 238000002360 preparation method Methods 0.000 title claims description 26
- 238000000034 method Methods 0.000 title claims description 22
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims abstract description 140
- 239000002253 acid Substances 0.000 claims abstract description 72
- 239000000126 substance Substances 0.000 claims abstract description 66
- 230000007935 neutral effect Effects 0.000 claims abstract description 48
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 39
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 36
- 239000013543 active substance Substances 0.000 claims abstract description 35
- 238000000576 coating method Methods 0.000 claims abstract description 32
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims abstract description 31
- 239000013078 crystal Substances 0.000 claims abstract description 31
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims abstract description 30
- 239000011248 coating agent Substances 0.000 claims abstract description 30
- 150000007524 organic acids Chemical class 0.000 claims abstract description 28
- 229960001380 cimetidine Drugs 0.000 claims abstract description 22
- CCGSUNCLSOWKJO-UHFFFAOYSA-N cimetidine Chemical compound N#CNC(=N/C)\NCCSCC1=NC=N[C]1C CCGSUNCLSOWKJO-UHFFFAOYSA-N 0.000 claims abstract description 22
- 239000003513 alkali Substances 0.000 claims abstract description 21
- 239000007787 solid Substances 0.000 claims abstract description 21
- 229960005132 cisapride Drugs 0.000 claims abstract description 20
- DCSUBABJRXZOMT-IRLDBZIGSA-N cisapride Chemical compound C([C@@H]([C@@H](CC1)NC(=O)C=2C(=CC(N)=C(Cl)C=2)OC)OC)N1CCCOC1=CC=C(F)C=C1 DCSUBABJRXZOMT-IRLDBZIGSA-N 0.000 claims abstract description 20
- DCSUBABJRXZOMT-UHFFFAOYSA-N cisapride Natural products C1CC(NC(=O)C=2C(=CC(N)=C(Cl)C=2)OC)C(OC)CN1CCCOC1=CC=C(F)C=C1 DCSUBABJRXZOMT-UHFFFAOYSA-N 0.000 claims abstract description 20
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims abstract description 14
- OENHQHLEOONYIE-UKMVMLAPSA-N all-trans beta-carotene Natural products CC=1CCCC(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C OENHQHLEOONYIE-UKMVMLAPSA-N 0.000 claims abstract description 10
- 239000011648 beta-carotene Substances 0.000 claims abstract description 10
- TUPZEYHYWIEDIH-WAIFQNFQSA-N beta-carotene Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CCCC1(C)C)C=CC=C(/C)C=CC2=CCCCC2(C)C TUPZEYHYWIEDIH-WAIFQNFQSA-N 0.000 claims abstract description 10
- 235000013734 beta-carotene Nutrition 0.000 claims abstract description 10
- 229960002747 betacarotene Drugs 0.000 claims abstract description 10
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 claims abstract description 10
- 150000001720 carbohydrates Chemical class 0.000 claims abstract description 7
- 239000000416 hydrocolloid Substances 0.000 claims abstract description 7
- 238000002844 melting Methods 0.000 claims abstract description 7
- 230000008018 melting Effects 0.000 claims abstract description 7
- 229960000620 ranitidine Drugs 0.000 claims abstract description 7
- VMXUWOKSQNHOCA-LCYFTJDESA-N ranitidine Chemical compound [O-][N+](=O)/C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-LCYFTJDESA-N 0.000 claims abstract description 7
- -1 for example Substances 0.000 claims abstract description 6
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract 5
- 239000003826 tablet Substances 0.000 claims description 87
- 239000000047 product Substances 0.000 claims description 65
- 239000000203 mixture Substances 0.000 claims description 49
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 46
- 239000000243 solution Substances 0.000 claims description 40
- 239000008187 granular material Substances 0.000 claims description 36
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 34
- 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 claims description 28
- 238000006243 chemical reaction Methods 0.000 claims description 28
- 239000000600 sorbitol Substances 0.000 claims description 28
- 235000010356 sorbitol Nutrition 0.000 claims description 28
- 239000007938 effervescent tablet Substances 0.000 claims description 27
- 229940079593 drug Drugs 0.000 claims description 26
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 22
- 239000002518 antifoaming agent Substances 0.000 claims description 21
- 238000002156 mixing Methods 0.000 claims description 21
- 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 claims description 19
- 229930195725 Mannitol Natural products 0.000 claims description 19
- 239000011230 binding agent Substances 0.000 claims description 19
- 239000000594 mannitol Substances 0.000 claims description 19
- 235000010355 mannitol Nutrition 0.000 claims description 19
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 17
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 16
- 238000001035 drying Methods 0.000 claims description 15
- 239000002245 particle Substances 0.000 claims description 14
- 238000007792 addition Methods 0.000 claims description 12
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 claims description 12
- 229940083037 simethicone Drugs 0.000 claims description 12
- 230000002209 hydrophobic effect Effects 0.000 claims description 10
- HWPKGOGLCKPRLZ-UHFFFAOYSA-M monosodium citrate Chemical compound [Na+].OC(=O)CC(O)(C([O-])=O)CC(O)=O HWPKGOGLCKPRLZ-UHFFFAOYSA-M 0.000 claims description 9
- 235000003599 food sweetener Nutrition 0.000 claims description 8
- 235000018342 monosodium citrate Nutrition 0.000 claims description 8
- 239000002524 monosodium citrate Substances 0.000 claims description 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 8
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 8
- 239000003765 sweetening agent Substances 0.000 claims description 8
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 7
- 239000005913 Maltodextrin Substances 0.000 claims description 6
- 229920002774 Maltodextrin Polymers 0.000 claims description 6
- 230000003254 anti-foaming effect Effects 0.000 claims description 6
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims description 6
- 229940035034 maltodextrin Drugs 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 5
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 5
- 239000007864 aqueous solution Substances 0.000 claims description 5
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 5
- 239000001630 malic acid Substances 0.000 claims description 5
- 235000011090 malic acid Nutrition 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 5
- 230000008569 process Effects 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 4
- 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 claims description 4
- 229910002092 carbon dioxide Inorganic materials 0.000 claims description 4
- 239000007795 chemical reaction product Substances 0.000 claims description 4
- 238000002425 crystallisation Methods 0.000 claims description 4
- 230000008025 crystallization Effects 0.000 claims description 4
- 239000000796 flavoring agent Substances 0.000 claims description 4
- 239000008101 lactose Substances 0.000 claims description 4
- 229960001520 ranitidine hydrochloride Drugs 0.000 claims description 4
- GGWBHVILAJZWKJ-KJEVSKRMSA-N ranitidine hydrochloride Chemical compound [H+].[Cl-].[O-][N+](=O)\C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 GGWBHVILAJZWKJ-KJEVSKRMSA-N 0.000 claims description 4
- 238000009736 wetting Methods 0.000 claims description 4
- 229940122957 Histamine H2 receptor antagonist Drugs 0.000 claims description 3
- 239000000872 buffer Substances 0.000 claims description 3
- 238000010438 heat treatment Methods 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 238000002161 passivation Methods 0.000 claims description 3
- 229920000642 polymer Polymers 0.000 claims description 3
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-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
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 claims description 2
- 238000001704 evaporation Methods 0.000 claims description 2
- 235000013355 food flavoring agent Nutrition 0.000 claims description 2
- FOYKKGHVWRFIBD-UHFFFAOYSA-N gamma-tocopherol acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1 FOYKKGHVWRFIBD-UHFFFAOYSA-N 0.000 claims description 2
- 229910052938 sodium sulfate Inorganic materials 0.000 claims description 2
- 235000011152 sodium sulphate Nutrition 0.000 claims description 2
- 238000012360 testing method Methods 0.000 claims description 2
- 229910052783 alkali metal Inorganic materials 0.000 claims 4
- 150000001447 alkali salts Chemical class 0.000 claims 4
- 239000010410 layer Substances 0.000 claims 4
- 239000000375 suspending agent Substances 0.000 claims 4
- 229910052784 alkaline earth metal Inorganic materials 0.000 claims 3
- CDOUZKKFHVEKRI-UHFFFAOYSA-N 3-bromo-n-[(prop-2-enoylamino)methyl]propanamide Chemical compound BrCCC(=O)NCNC(=O)C=C CDOUZKKFHVEKRI-UHFFFAOYSA-N 0.000 claims 2
- 150000001342 alkaline earth metals Chemical class 0.000 claims 2
- 239000012928 buffer substance Substances 0.000 claims 2
- 239000001569 carbon dioxide Substances 0.000 claims 2
- 229940008099 dimethicone Drugs 0.000 claims 2
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims 2
- 239000004205 dimethyl polysiloxane Substances 0.000 claims 2
- 239000002798 polar solvent Substances 0.000 claims 2
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims 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 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- 229910000288 alkali metal carbonate Inorganic materials 0.000 claims 1
- 150000008041 alkali metal carbonates Chemical class 0.000 claims 1
- 150000001340 alkali metals Chemical class 0.000 claims 1
- 239000007900 aqueous suspension Substances 0.000 claims 1
- 235000010323 ascorbic acid Nutrition 0.000 claims 1
- 229960005070 ascorbic acid Drugs 0.000 claims 1
- 239000011668 ascorbic acid Substances 0.000 claims 1
- 230000000881 depressing effect Effects 0.000 claims 1
- 239000011874 heated mixture Substances 0.000 claims 1
- 238000003825 pressing Methods 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 239000002344 surface layer Substances 0.000 claims 1
- 229940069428 antacid Drugs 0.000 abstract description 4
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- 238000004090 dissolution Methods 0.000 description 19
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- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 15
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 description 13
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- 239000000605 aspartame Substances 0.000 description 8
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- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
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- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
- 239000011734 sodium Substances 0.000 description 5
- 229910052708 sodium Inorganic materials 0.000 description 5
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 4
- 229960000878 docusate sodium Drugs 0.000 description 4
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- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 description 4
- ILJOYZVVZZFIKA-UHFFFAOYSA-M sodium;1,1-dioxo-1,2-benzothiazol-3-olate;hydrate Chemical compound O.[Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 ILJOYZVVZZFIKA-UHFFFAOYSA-M 0.000 description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
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- 239000001509 sodium citrate Substances 0.000 description 3
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 3
- 235000011083 sodium citrates Nutrition 0.000 description 3
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- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 2
- 239000002585 base Substances 0.000 description 2
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- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
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- 206010024769 Local reaction Diseases 0.000 description 1
- VMXUWOKSQNHOCA-UHFFFAOYSA-N N1'-[2-[[5-[(dimethylamino)methyl]-2-furanyl]methylthio]ethyl]-N1-methyl-2-nitroethene-1,1-diamine Chemical compound [O-][N+](=O)C=C(NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-UHFFFAOYSA-N 0.000 description 1
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- 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 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 238000004873 anchoring Methods 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
- 235000013361 beverage Nutrition 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- 230000009172 bursting Effects 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 150000001860 citric acid derivatives Chemical class 0.000 description 1
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 239000002274 desiccant Substances 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 235000013681 dietary sucrose Nutrition 0.000 description 1
- 238000010981 drying operation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 239000003485 histamine H2 receptor antagonist Substances 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 150000004682 monohydrates Chemical class 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000376 reactant Substances 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 235000019613 sensory perceptions of taste Nutrition 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 238000009492 tablet coating Methods 0.000 description 1
- 239000002700 tablet coating Substances 0.000 description 1
- 230000035923 taste sensation Effects 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 238000009489 vacuum treatment Methods 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Classifications
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
L'invention concerne un produit granulaire à système effervescent comprenant des principes actifs pharmaceutiques sensibles à l'acide tels que, par exemple, le bêta-carotène, la cimétidine, la ranitidine ou le cisapride. Ce produit est particulièrement utile pour prévenir l'action antiacide, présentant une capacité de fixation de l'acide inférieure à 5 meq, à un poids d'environ 1,6 à 2,3 grammes. Les grains effervescents sont constitués de cristaux véhiculeurs comprenant au moins un acide organique solide comestible, de préférence de l'acide citrique, se présentent sous forme de produit granulaire, séparés du principe actif pharmaceutique, et sont enrobés d'au moins une couche de substance neutre soluble dans l'eau et/ou d'alcool capable de provoquer une chute du point de fusion des grains d'acide à leur surface, comme, par exemple, un polymère soluble dans l'eau, un alcool supérieur, un hydrate de carbone et/ou un hydrocolloïde. Une seconde couche contient au moins une partie de l'alcali et/ou du carbonate alcalino-terreux prévu pour le dosage total.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEP4406641.4 | 1994-03-01 | ||
| DE4406641 | 1994-03-01 | ||
| CH87394 | 1994-03-23 | ||
| CH873/94-6 | 1994-03-23 | ||
| EP94203112.1 | 1994-10-26 | ||
| EP94203112A EP0670160B1 (fr) | 1994-03-01 | 1994-10-26 | Produit granulaire ou comprimé contenant un système effervescent et un agent actif pharmaceutique, et son procédé de préparation |
| PCT/EP1995/000650 WO1995023594A1 (fr) | 1994-03-01 | 1995-02-23 | Produit ou comprime granulaire contenant un systeme effervescent et un principe actif pharmaceutique, et son procede de preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2183952A1 CA2183952A1 (fr) | 1995-09-08 |
| CA2183952C true CA2183952C (fr) | 2007-01-16 |
Family
ID=27172490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002183952A Expired - Fee Related CA2183952C (fr) | 1994-03-01 | 1995-02-23 | Produit ou comprime granulaire contenant un systeme effervescent et un principe actif pharmaceutique, et son procede de preparation |
Country Status (15)
| Country | Link |
|---|---|
| JP (1) | JPH09509669A (fr) |
| CN (1) | CN1213739C (fr) |
| AU (1) | AU681256B2 (fr) |
| BR (1) | BR9506964A (fr) |
| CA (1) | CA2183952C (fr) |
| CZ (1) | CZ291710B6 (fr) |
| DE (1) | DE670160T1 (fr) |
| FI (1) | FI118033B (fr) |
| HU (1) | HU228147B1 (fr) |
| NO (1) | NO315308B1 (fr) |
| NZ (1) | NZ281228A (fr) |
| PL (1) | PL181714B1 (fr) |
| RU (1) | RU2153331C2 (fr) |
| TW (1) | TW403658B (fr) |
| WO (1) | WO1995023594A1 (fr) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5840737A (en) | 1996-01-04 | 1998-11-24 | The Curators Of The University Of Missouri | Omeprazole solution and method for using same |
| US6489346B1 (en) | 1996-01-04 | 2002-12-03 | The Curators Of The University Of Missouri | Substituted benzimidazole dosage forms and method of using same |
| US20030070584A1 (en) | 2001-05-15 | 2003-04-17 | Cynthia Gulian | Dip coating compositions containing cellulose ethers |
| US8309118B2 (en) | 2001-09-28 | 2012-11-13 | Mcneil-Ppc, Inc. | Film forming compositions containing sucralose |
| DE10224607B4 (de) * | 2002-06-04 | 2008-03-13 | Lts Lohmann Therapie-Systeme Ag | Filmförmige, zerfallsfähige Zubereitungen zur Wirkstofffreisetzung und Verfahren zu deren Herstellung |
| US7429619B2 (en) | 2002-08-02 | 2008-09-30 | Mcneil Consumer Healthcare | Polyacrylic film forming compositions |
| WO2004050068A1 (fr) | 2002-11-29 | 2004-06-17 | Janssen Pharmaceutica N.V. | Compositions pharmaceutiques comprenant un compose medicamenteux respectivement basique, tensioactif et base respectivement acide hydrosoluble et tolerable physiologiquement |
| US8993599B2 (en) | 2003-07-18 | 2015-03-31 | Santarus, Inc. | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them |
| US8906940B2 (en) | 2004-05-25 | 2014-12-09 | Santarus, Inc. | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them |
| JPWO2006059716A1 (ja) * | 2004-12-03 | 2008-06-05 | 武田薬品工業株式会社 | 固形製剤 |
| BR112012015923A2 (pt) | 2010-02-26 | 2020-09-08 | Toray Industries, Inc. | "preparação sólida revestida" |
| MX374994B (es) | 2011-12-09 | 2025-03-06 | Merck Patent Gmbh | Carbonato de sodio anhidro que tiene un bajo contenido de poros. |
| WO2014065890A1 (fr) * | 2012-10-25 | 2014-05-01 | Otc Nutrition Llc | Compositions de complément minéral de calcium solide à dissolution rapide et procédé de préparation |
| NZ708741A (en) | 2012-12-19 | 2019-11-29 | Bayer Animal Health Gmbh | Tablets with improved acceptance and good storage stability |
| CN105670003A (zh) * | 2014-11-21 | 2016-06-15 | 常州坤宇环保科技有限公司 | 高吸水树脂防结块剂 |
| EP3318135A1 (fr) * | 2016-11-03 | 2018-05-09 | Perfetti Van Melle S.p.A. | Matériau de bonbon effervescent, son procédé de préparation et produits fabriqués à partir de celui-ci |
| MX2022004643A (es) * | 2019-10-17 | 2022-07-27 | Isp Investments Llc | Una composición de excipiente coprocesado efervescente estable y un proceso de preparación de la misma. |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1039170A (en) * | 1969-02-24 | 1971-07-22 | Abbott Laboratories | Tableting medium |
| US4704269A (en) * | 1985-06-11 | 1987-11-03 | Hudson Pharmaceutical Corporation | Effervescent antacid and analgesic compositions |
| CA2023493C (fr) * | 1989-08-31 | 2000-01-04 | Masami Moroi | Melange servant a l'administration d'un produit moussant |
| CA2112663C (fr) * | 1991-07-01 | 2002-04-23 | Thomas Gergely | Systemes effervescents utilisant des agents d'enduction formes par la reaction des elements constituants |
-
1994
- 1994-10-26 DE DE0670160T patent/DE670160T1/de active Pending
-
1995
- 1995-02-23 BR BR9506964A patent/BR9506964A/pt not_active Application Discontinuation
- 1995-02-23 CN CN95191882.6A patent/CN1213739C/zh not_active Expired - Fee Related
- 1995-02-23 AU AU18114/95A patent/AU681256B2/en not_active Ceased
- 1995-02-23 JP JP7522671A patent/JPH09509669A/ja active Pending
- 1995-02-23 CZ CZ19962519A patent/CZ291710B6/cs not_active IP Right Cessation
- 1995-02-23 HU HU9602380A patent/HU228147B1/hu not_active IP Right Cessation
- 1995-02-23 RU RU96120083/14A patent/RU2153331C2/ru not_active IP Right Cessation
- 1995-02-23 WO PCT/EP1995/000650 patent/WO1995023594A1/fr not_active Ceased
- 1995-02-23 NZ NZ281228A patent/NZ281228A/en unknown
- 1995-02-23 CA CA002183952A patent/CA2183952C/fr not_active Expired - Fee Related
- 1995-03-01 TW TW084101871A patent/TW403658B/zh not_active IP Right Cessation
-
1996
- 1996-08-22 PL PL95316113A patent/PL181714B1/pl unknown
- 1996-08-28 NO NO19963588A patent/NO315308B1/no not_active IP Right Cessation
- 1996-08-30 FI FI963385A patent/FI118033B/fi not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| PL316113A1 (en) | 1996-12-23 |
| NZ281228A (en) | 1997-06-24 |
| JPH09509669A (ja) | 1997-09-30 |
| RU2153331C2 (ru) | 2000-07-27 |
| PL181714B1 (en) | 2001-09-28 |
| FI963385L (fi) | 1996-10-30 |
| HU228147B1 (en) | 2012-12-28 |
| CZ291710B6 (cs) | 2003-05-14 |
| CZ251996A3 (en) | 1997-01-15 |
| FI963385A0 (fi) | 1996-08-30 |
| HU9602380D0 (en) | 1996-10-28 |
| AU681256B2 (en) | 1997-08-21 |
| CA2183952A1 (fr) | 1995-09-08 |
| NO963588D0 (no) | 1996-08-28 |
| AU1811495A (en) | 1995-09-18 |
| NO315308B1 (no) | 2003-08-18 |
| TW403658B (en) | 2000-09-01 |
| BR9506964A (pt) | 1997-09-09 |
| HUT75677A (en) | 1997-05-28 |
| NO963588L (no) | 1996-10-31 |
| CN1213739C (zh) | 2005-08-10 |
| DE670160T1 (de) | 1996-03-14 |
| WO1995023594A1 (fr) | 1995-09-08 |
| CN1142182A (zh) | 1997-02-05 |
| FI118033B (fi) | 2007-06-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |