DD282392A5 - Umhuellte retardformen - Google Patents

Info

Publication number

DD282392A5

DD282392A5 DD88319869A DD31986988A DD282392A5 DD 282392 A5 DD282392 A5 DD 282392A5 DD 88319869 A DD88319869 A DD 88319869A DD 31986988 A DD31986988 A DD 31986988A DD 282392 A5 DD282392 A5 DD 282392A5

Authority

DD

German Democratic Republic

Prior art keywords

component

membrane

sustained release

body fluid

optionally

Prior art date

1987-09-18

Links

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• Global Dossier
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• 239000012528 membrane Substances 0.000 claims abstract description 26
• 239000012730 sustained-release form Substances 0.000 claims abstract description 21
• 238000000034 method Methods 0.000 claims abstract description 18
• 239000013543 active substance Substances 0.000 claims abstract description 17
• 210000001124 body fluid Anatomy 0.000 claims abstract description 17
• 239000010839 body fluid Substances 0.000 claims abstract description 17
• 239000000126 substance Substances 0.000 claims abstract description 13
• 238000002360 preparation method Methods 0.000 claims abstract description 5
• 239000007787 solid Substances 0.000 claims abstract description 5
• 229920002451 polyvinyl alcohol Polymers 0.000 claims description 34
• 239000000203 mixture Substances 0.000 claims description 33
• UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical group [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 22
• 239000004372 Polyvinyl alcohol Substances 0.000 claims description 20
• 239000003795 chemical substances by application Substances 0.000 claims description 15
• 210000004051 gastric juice Anatomy 0.000 claims description 14
• CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims description 12
• 235000017557 sodium bicarbonate Nutrition 0.000 claims description 11
• 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 11
• 239000002775 capsule Substances 0.000 claims description 10
• 238000009472 formulation Methods 0.000 claims description 10
• 230000002496 gastric effect Effects 0.000 claims description 10
• 239000003380 propellant Substances 0.000 claims description 10
• 230000008961 swelling Effects 0.000 claims description 9
• KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 claims description 7
• 229960000794 baclofen Drugs 0.000 claims description 6
• 239000001569 carbon dioxide Substances 0.000 claims description 6
• 229910002092 carbon dioxide Inorganic materials 0.000 claims description 6
• 238000000576 coating method Methods 0.000 claims description 6
• 239000007888 film coating Substances 0.000 claims description 6
• 238000009501 film coating Methods 0.000 claims description 6
• 230000037406 food intake Effects 0.000 claims description 6
• 239000008177 pharmaceutical agent Substances 0.000 claims description 6
• 239000004014 plasticizer Substances 0.000 claims description 6
• 239000011248 coating agent Substances 0.000 claims description 5
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
• 229910052799 carbon Inorganic materials 0.000 claims description 2
• 210000004211 gastric acid Anatomy 0.000 claims 1
• 239000002552 dosage form Substances 0.000 abstract description 9
• 210000002784 stomach Anatomy 0.000 abstract description 9
• 230000000737 periodic effect Effects 0.000 abstract description 3
• 238000013268 sustained release Methods 0.000 abstract description 3
• 239000000470 constituent Substances 0.000 abstract 1
• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 33
• -1 z. For example Substances 0.000 description 25
• 235000019422 polyvinyl alcohol Nutrition 0.000 description 22
• VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 18
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 14
• 235000002639 sodium chloride Nutrition 0.000 description 14
• 239000000243 solution Substances 0.000 description 14
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 13
• 239000004480 active ingredient Substances 0.000 description 13
• 229920001223 polyethylene glycol Polymers 0.000 description 11
• 235000010980 cellulose Nutrition 0.000 description 10
• 229920002678 cellulose Polymers 0.000 description 10
• 239000001913 cellulose Substances 0.000 description 10
• 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 9
• 239000011780 sodium chloride Substances 0.000 description 9
• 239000002202 Polyethylene glycol Substances 0.000 description 8
• 150000003839 salts Chemical class 0.000 description 8
• 239000011734 sodium Substances 0.000 description 8
• 229910052708 sodium Inorganic materials 0.000 description 8
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
• VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 7
• 239000003814 drug Substances 0.000 description 7
• 239000000463 material Substances 0.000 description 7
• 229920000036 polyvinylpyrrolidone Polymers 0.000 description 7
• 239000001267 polyvinylpyrrolidone Substances 0.000 description 7
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 7
• PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 6
• 229940079593 drug Drugs 0.000 description 6
• CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 6
• 230000001225 therapeutic effect Effects 0.000 description 6
• 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 5
• UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 5
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 5
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 5
• 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 5
• UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 5
• 229910052500 inorganic mineral Inorganic materials 0.000 description 5
• 235000010755 mineral Nutrition 0.000 description 5
• 239000011707 mineral Substances 0.000 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 description 4
• 239000001856 Ethyl cellulose Substances 0.000 description 4
• ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 4
• XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 4
• FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 4
• 239000000654 additive Substances 0.000 description 4
• 229920001577 copolymer Polymers 0.000 description 4
• 235000014113 dietary fatty acids Nutrition 0.000 description 4
• 210000001198 duodenum Anatomy 0.000 description 4
• 235000019325 ethyl cellulose Nutrition 0.000 description 4
• 229920001249 ethyl cellulose Polymers 0.000 description 4
• 239000000194 fatty acid Substances 0.000 description 4
• 229930195729 fatty acid Natural products 0.000 description 4
• 239000007789 gas Substances 0.000 description 4
• 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 4
• 230000007062 hydrolysis Effects 0.000 description 4
• 238000006460 hydrolysis reaction Methods 0.000 description 4
• 239000011777 magnesium Substances 0.000 description 4
• 229910052749 magnesium Inorganic materials 0.000 description 4
• 229920000609 methyl cellulose Polymers 0.000 description 4
• TZIHFWKZFHZASV-UHFFFAOYSA-N methyl formate Chemical compound COC=O TZIHFWKZFHZASV-UHFFFAOYSA-N 0.000 description 4
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
• 235000010981 methylcellulose Nutrition 0.000 description 4
• 239000001923 methylcellulose Substances 0.000 description 4
• 229940068918 polyethylene glycol 400 Drugs 0.000 description 4
• 229920000642 polymer Polymers 0.000 description 4
• BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 4
• 238000006467 substitution reaction Methods 0.000 description 4
• 239000004604 Blowing Agent Substances 0.000 description 3
• 229920002134 Carboxymethyl cellulose Polymers 0.000 description 3
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 3
• 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 3
• ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 3
• AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 3
• 240000004808 Saccharomyces cerevisiae Species 0.000 description 3
• 235000014680 Saccharomyces cerevisiae Nutrition 0.000 description 3
• 229920001800 Shellac Polymers 0.000 description 3
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical class [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
• 229920002472 Starch Polymers 0.000 description 3
• QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 3
• 238000010521 absorption reaction Methods 0.000 description 3
• 239000002253 acid Substances 0.000 description 3
• 150000005215 alkyl ethers Chemical class 0.000 description 3
• 239000008346 aqueous phase Substances 0.000 description 3
• 239000007864 aqueous solution Substances 0.000 description 3
• 229910000019 calcium carbonate Inorganic materials 0.000 description 3
• 229960003563 calcium carbonate Drugs 0.000 description 3
• 235000010216 calcium carbonate Nutrition 0.000 description 3
• 235000010948 carboxy methyl cellulose Nutrition 0.000 description 3
• 239000001768 carboxy methyl cellulose Substances 0.000 description 3
• 239000008112 carboxymethyl-cellulose Substances 0.000 description 3
• 230000003111 delayed effect Effects 0.000 description 3
• 230000000694 effects Effects 0.000 description 3
• 238000001704 evaporation Methods 0.000 description 3
• 230000008020 evaporation Effects 0.000 description 3
• 238000011049 filling Methods 0.000 description 3
• IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 3
• 229910052739 hydrogen Inorganic materials 0.000 description 3
• 239000001257 hydrogen Substances 0.000 description 3
• 125000002887 hydroxy group Chemical class [H]O* 0.000 description 3
• 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 3
• 239000001863 hydroxypropyl cellulose Substances 0.000 description 3
• 238000004519 manufacturing process Methods 0.000 description 3
• 239000008194 pharmaceutical composition Substances 0.000 description 3
• 239000012071 phase Substances 0.000 description 3
• 229920001983 poloxamer Polymers 0.000 description 3
• 238000006116 polymerization reaction Methods 0.000 description 3
• 229920002689 polyvinyl acetate Polymers 0.000 description 3
• 239000011118 polyvinyl acetate Substances 0.000 description 3
• 239000011591 potassium Substances 0.000 description 3
• 229910052700 potassium Inorganic materials 0.000 description 3
• NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 description 3
• 230000002035 prolonged effect Effects 0.000 description 3
• 210000001187 pylorus Anatomy 0.000 description 3
• 239000011347 resin Substances 0.000 description 3
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• 239000004208 shellac Substances 0.000 description 3
• 235000013874 shellac Nutrition 0.000 description 3
• 229940113147 shellac Drugs 0.000 description 3
• ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 3
• 229910000029 sodium carbonate Inorganic materials 0.000 description 3
• 239000004094 surface-active agent Substances 0.000 description 3
• VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
• 229940088594 vitamin Drugs 0.000 description 3
• 229930003231 vitamin Natural products 0.000 description 3
• 235000013343 vitamin Nutrition 0.000 description 3
• 239000011782 vitamin Substances 0.000 description 3
• YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 2
• GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 description 2
• 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
• MYRTYDVEIRVNKP-UHFFFAOYSA-N 1,2-Divinylbenzene Chemical compound C=CC1=CC=CC=C1C=C MYRTYDVEIRVNKP-UHFFFAOYSA-N 0.000 description 2
• CHRJZRDFSQHIFI-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;styrene Chemical compound C=CC1=CC=CC=C1.C=CC1=CC=CC=C1C=C CHRJZRDFSQHIFI-UHFFFAOYSA-N 0.000 description 2
• RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
• NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
• 229920001817 Agar Polymers 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
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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 2
• ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 2
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• ZZHLYYDVIOPZBE-UHFFFAOYSA-N Trimeprazine Chemical compound C1=CC=C2N(CC(CN(C)C)C)C3=CC=CC=C3SC2=C1 ZZHLYYDVIOPZBE-UHFFFAOYSA-N 0.000 description 2
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• XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
• IJCWFDPJFXGQBN-RYNSOKOISA-N [(2R)-2-[(2R,3R,4S)-4-hydroxy-3-octadecanoyloxyoxolan-2-yl]-2-octadecanoyloxyethyl] octadecanoate Chemical class CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCCCCCCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCCCCCCCCCCCC IJCWFDPJFXGQBN-RYNSOKOISA-N 0.000 description 2
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• OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 description 2
• 210000001035 gastrointestinal tract Anatomy 0.000 description 2
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