CN1028962C - 稳定性药物的生产方法 - Google Patents
稳定性药物的生产方法 Download PDFInfo
- Publication number
- CN1028962C CN1028962C CN88108057A CN88108057A CN1028962C CN 1028962 C CN1028962 C CN 1028962C CN 88108057 A CN88108057 A CN 88108057A CN 88108057 A CN88108057 A CN 88108057A CN 1028962 C CN1028962 C CN 1028962C
- Authority
- CN
- China
- Prior art keywords
- physiology
- compatible
- ramipril
- active substance
- alkyl
- 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 - Lifetime
Links
- 238000004519 manufacturing process Methods 0.000 title abstract description 18
- 239000003814 drug Substances 0.000 title description 5
- 238000000034 method Methods 0.000 claims abstract description 26
- 150000001875 compounds Chemical class 0.000 claims abstract description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 4
- 229960003401 ramipril Drugs 0.000 claims description 45
- HDACQVRGBOVJII-JBDAPHQKSA-N ramipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 HDACQVRGBOVJII-JBDAPHQKSA-N 0.000 claims description 45
- 239000000203 mixture Substances 0.000 claims description 32
- 239000013543 active substance Substances 0.000 claims description 31
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- 229920000642 polymer Polymers 0.000 claims description 16
- 230000035479 physiological effects, processes and functions Effects 0.000 claims description 14
- 239000000872 buffer Substances 0.000 claims description 12
- 239000011248 coating agent Substances 0.000 claims description 12
- 238000000576 coating method Methods 0.000 claims description 12
- 230000000694 effects Effects 0.000 claims description 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 10
- 238000002360 preparation method Methods 0.000 claims description 9
- 239000000126 substance Substances 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 3
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 238000005984 hydrogenation reaction Methods 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000007888 film coating Substances 0.000 claims 1
- 238000009501 film coating Methods 0.000 claims 1
- 239000000463 material Substances 0.000 description 47
- 239000003826 tablet Substances 0.000 description 25
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 13
- 238000005469 granulation Methods 0.000 description 13
- 230000003179 granulation Effects 0.000 description 13
- 239000008108 microcrystalline cellulose Substances 0.000 description 13
- 229940016286 microcrystalline cellulose Drugs 0.000 description 13
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 13
- 230000006641 stabilisation Effects 0.000 description 13
- 239000010408 film Substances 0.000 description 12
- 108010061435 Enalapril Proteins 0.000 description 11
- 229960000873 enalapril Drugs 0.000 description 11
- GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 description 11
- PRRLDUXWTHUCAO-UHFFFAOYSA-N [Na].C(C=CC(=O)O)(=O)O.CCCCCCCCCCCCCCCCCC Chemical compound [Na].C(C=CC(=O)O)(=O)O.CCCCCCCCCCCCCCCCCC PRRLDUXWTHUCAO-UHFFFAOYSA-N 0.000 description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 9
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 9
- 239000008187 granular material Substances 0.000 description 8
- 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 7
- 229930195725 Mannitol Natural products 0.000 description 7
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 7
- 239000007864 aqueous solution Substances 0.000 description 7
- 239000002775 capsule Substances 0.000 description 7
- 238000007907 direct compression Methods 0.000 description 7
- 239000000594 mannitol Substances 0.000 description 7
- 235000010355 mannitol Nutrition 0.000 description 7
- 238000000354 decomposition reaction Methods 0.000 description 6
- -1 dioxo piperazine chemical compound Chemical class 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
- 239000012928 buffer substance Substances 0.000 description 5
- 239000002552 dosage form Substances 0.000 description 5
- 238000004898 kneading Methods 0.000 description 5
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 4
- 229920003134 Eudragit® polymer Polymers 0.000 description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 239000006185 dispersion Substances 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 238000011105 stabilization Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- 239000011149 active material Substances 0.000 description 3
- 235000010980 cellulose Nutrition 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 3
- 239000001913 cellulose Substances 0.000 description 3
- 239000011521 glass Substances 0.000 description 3
- 238000012856 packing Methods 0.000 description 3
- 239000002245 particle Substances 0.000 description 3
- 239000007921 spray Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 241001411320 Eriogonum inflatum Species 0.000 description 2
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 description 2
- 229920000881 Modified starch Polymers 0.000 description 2
- 239000004368 Modified starch Substances 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- VXFJYXUZANRPDJ-WTNASJBWSA-N Trandopril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@H]2CCCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 VXFJYXUZANRPDJ-WTNASJBWSA-N 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 2
- 229960001021 lactose monohydrate Drugs 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 235000019426 modified starch Nutrition 0.000 description 2
- RZJRJXONCZWCBN-UHFFFAOYSA-N octadecane Chemical compound CCCCCCCCCCCCCCCCCC RZJRJXONCZWCBN-UHFFFAOYSA-N 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 238000012545 processing Methods 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 description 2
- 229940080313 sodium starch Drugs 0.000 description 2
- 229940032147 starch Drugs 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 235000012222 talc Nutrition 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- OOSZCNKVJAVHJI-UHFFFAOYSA-N 1-[(4-fluorophenyl)methyl]piperazine Chemical compound C1=CC(F)=CC=C1CN1CCNCC1 OOSZCNKVJAVHJI-UHFFFAOYSA-N 0.000 description 1
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 description 1
- OPHFPFFVGABYTB-UHFFFAOYSA-N 2H-oxazine piperazine Chemical class O1NC=CC=C1.N1CCNCC1 OPHFPFFVGABYTB-UHFFFAOYSA-N 0.000 description 1
- FHHHOYXPRDYHEZ-COXVUDFISA-N Alacepril Chemical compound CC(=O)SC[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 FHHHOYXPRDYHEZ-COXVUDFISA-N 0.000 description 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
- 241000790917 Dioxys <bee> Species 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- 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 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 108010007859 Lisinopril Proteins 0.000 description 1
- 229920003091 Methocel™ Polymers 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- VQVDYMMONWLOMA-UHFFFAOYSA-N [Na+].[Si](O)(O)(O)O.[O-2].[O-2].[Ti+4] Chemical compound [Na+].[Si](O)(O)(O)O.[O-2].[O-2].[Ti+4] VQVDYMMONWLOMA-UHFFFAOYSA-N 0.000 description 1
- 229950007884 alacepril Drugs 0.000 description 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 description 1
- 238000010539 anionic addition polymerization reaction Methods 0.000 description 1
- 125000000129 anionic group Chemical group 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 229920002301 cellulose acetate Polymers 0.000 description 1
- 230000002301 combined effect Effects 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 238000006482 condensation reaction Methods 0.000 description 1
- 238000007334 copolymerization reaction Methods 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 229910001882 dioxygen Inorganic materials 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 229940071826 hydroxyethyl cellulose Drugs 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 229950009810 indolapril Drugs 0.000 description 1
- 229960002394 lisinopril Drugs 0.000 description 1
- RLAWWYSOJDYHDC-BZSNNMDCSA-N lisinopril Chemical compound C([C@H](N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 RLAWWYSOJDYHDC-BZSNNMDCSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 229940038384 octadecane Drugs 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 229960002582 perindopril Drugs 0.000 description 1
- IPVQLZZIHOAWMC-QXKUPLGCSA-N perindopril Chemical compound C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 description 1
- LGRFSURHDFAFJT-UHFFFAOYSA-N phthalic anhydride Chemical compound C1=CC=C2C(=O)OC(=O)C2=C1 LGRFSURHDFAFJT-UHFFFAOYSA-N 0.000 description 1
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 1
- 229920006254 polymer film Polymers 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 238000012797 qualification Methods 0.000 description 1
- 229960001455 quinapril Drugs 0.000 description 1
- JSDRRTOADPPCHY-HSQYWUDLSA-N quinapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)CC1=CC=CC=C1 JSDRRTOADPPCHY-HSQYWUDLSA-N 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229940001593 sodium carbonate Drugs 0.000 description 1
- 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 1
- 229960000999 sodium citrate dihydrate Drugs 0.000 description 1
- 229940074545 sodium dihydrogen phosphate dihydrate Drugs 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 229960002051 trandolapril Drugs 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G59/00—Polycondensates containing more than one epoxy group per molecule; Macromolecules obtained by polymerising compounds containing more than one epoxy group per molecule using curing agents or catalysts which react with the epoxy groups
- C08G59/18—Macromolecules obtained by polymerising compounds containing more than one epoxy group per molecule using curing agents or catalysts which react with the epoxy groups ; e.g. general methods of curing
- C08G59/40—Macromolecules obtained by polymerising compounds containing more than one epoxy group per molecule using curing agents or catalysts which react with the epoxy groups ; e.g. general methods of curing characterised by the curing agents used
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- 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
- A61K9/48—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
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Polymers & Plastics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEP3739690.0 | 1987-11-24 | ||
| DE19873739690 DE3739690A1 (de) | 1987-11-24 | 1987-11-24 | Stabilisierte arzneistoffe, verfahren zu ihrer herstellung sowie stabile arzneizubereitungen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1042917A CN1042917A (zh) | 1990-06-13 |
| CN1028962C true CN1028962C (zh) | 1995-06-21 |
Family
ID=6341084
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN88108057A Expired - Lifetime CN1028962C (zh) | 1987-11-24 | 1988-11-23 | 稳定性药物的生产方法 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US5151433A (enExample) |
| EP (1) | EP0317878B1 (enExample) |
| JP (1) | JPH0768140B2 (enExample) |
| KR (1) | KR970004908B1 (enExample) |
| CN (1) | CN1028962C (enExample) |
| AT (1) | ATE74513T1 (enExample) |
| AU (1) | AU615495B2 (enExample) |
| CA (1) | CA1338344C (enExample) |
| DE (2) | DE3739690A1 (enExample) |
| DK (1) | DK168423B1 (enExample) |
| ES (1) | ES2033400T3 (enExample) |
| FI (1) | FI93693C (enExample) |
| GR (1) | GR3004925T3 (enExample) |
| HU (1) | HU202100B (enExample) |
| IE (1) | IE61173B1 (enExample) |
| IL (1) | IL88460A0 (enExample) |
| NO (1) | NO176550C (enExample) |
| NZ (1) | NZ227032A (enExample) |
| PH (1) | PH27416A (enExample) |
| PT (1) | PT89061B (enExample) |
| ZA (1) | ZA888734B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170190877A1 (en) * | 2015-12-31 | 2017-07-06 | Eternal Materials Co., Ltd. | Thermally polymerizable composition, combined solution formed therefrom and use thereof |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| US6300361B1 (en) | 1990-07-25 | 2001-10-09 | Novartis Ag | Stabilized pharmaceutical compositions comprising acid donors |
| TW483763B (en) * | 1994-09-02 | 2002-04-21 | Astra Ab | Pharmaceutical composition comprising of ramipril and dihydropyridine compound |
| WO1997024109A1 (en) * | 1995-12-27 | 1997-07-10 | Janssen Pharmaceutica N.V. | Bioadhesive solid dosage form |
| SE9903028D0 (sv) * | 1999-08-27 | 1999-08-27 | Astra Ab | New use |
| KR20020040795A (ko) * | 1999-08-30 | 2002-05-30 | 로버트 흐라이탁, 미쉘 베스트 | 심혈관 사고 예방용 레닌-안지오텐신 시스템 억제제의 용도 |
| US20030225124A1 (en) * | 1999-08-31 | 2003-12-04 | Spiridon Spireas | Stable formulations of ACE inhibitors, and methods for preparation thereof |
| FR2824477B1 (fr) * | 2001-05-09 | 2005-09-09 | Ethypharm Lab Prod Ethiques | Granules enrobes a base d'inhibiteur de l'enzyme de conversion de l'anfiotensine, leur procede de preparation et comprimes orodispersibles contenant les granules enrobes |
| CA2357982A1 (en) * | 2001-09-28 | 2003-03-28 | Bernard Charles Sherman | Solid compositions comprising ramipril |
| WO2003059330A1 (en) * | 2002-01-15 | 2003-07-24 | Ranbaxy Laboratories Limited | Stable pharmaceutical compositions comprising ace inhibitor(s) |
| GB0301471D0 (en) * | 2003-01-22 | 2003-02-19 | Biochemie Gmbh | Organic compounds |
| US20060177498A1 (en) * | 2003-01-22 | 2006-08-10 | Ramaswami Bharatrajan | Solid pharmaceutical composition comprising ramipril |
| EP1635792B1 (en) * | 2003-06-26 | 2009-03-04 | Teva Pharmaceutical Industries Limited | Stable pharmaceutical compositions of 2-aza-bicyclo¬3.3.0 -octane-3-carboxylic acid derivatives |
| US6869963B2 (en) * | 2003-07-11 | 2005-03-22 | Sandoz Ag | Stable pharmaceutical compositions containing an ACE inhibitor |
| WO2005041940A1 (en) * | 2003-10-30 | 2005-05-12 | Lupin Ltd. | Stable formulations of ace inhibitors and methods for preparation thereof |
| GB2394660A (en) * | 2003-12-17 | 2004-05-05 | Niche Generics Ltd | Stabilisation of pharmaceutical compositions comprising ACE inhibitor by absence of acidic excipients having large specific surface area, eg silicon dioxide |
| GB2411355B (en) * | 2004-02-27 | 2006-02-22 | Niche Generics Ltd | Pharmaceutical composition |
| EP1734931A2 (en) * | 2004-03-24 | 2006-12-27 | Actavis Group | Formulations of ramipril |
| US20060045911A1 (en) * | 2004-08-27 | 2006-03-02 | Sun Pharmaceutical Industries Ltd. | Stable pharmaceutical formulations |
| CN101098681A (zh) * | 2004-11-05 | 2008-01-02 | 国王医药研究与发展有限公司 | 稳定化的单个涂布的雷米普利颗粒、组合物和方法 |
| WO2006048895A1 (en) * | 2004-11-08 | 2006-05-11 | Rubicon Research Pvt. Ltd. | Aqueous pharmaceutical coating |
| GB0518129D0 (en) * | 2005-09-06 | 2005-10-12 | Arrow Int Ltd | Ramipril formulation |
| KR100679166B1 (ko) | 2005-10-04 | 2007-02-06 | 신풍제약주식회사 | 안정성이 증진된 약제학적 조성물 및 그의 제조방법 |
| US20070098782A1 (en) * | 2005-10-28 | 2007-05-03 | Selamine Limited | Ramipril Formulation |
| GB2431579A (en) * | 2005-10-28 | 2007-05-02 | Arrow Int Ltd | Ramipril formulations |
| BRPI0708842A2 (pt) * | 2006-03-28 | 2011-06-14 | Gelesis Inc | uso de materiais polimÉricos com outras substÂncias para aumento do desempenho |
| US20070232680A1 (en) * | 2006-04-04 | 2007-10-04 | Vijayabhaskar Bolugoddu | Preparation of ramipril and stable pharmaceutical compositions |
| MX2008013374A (es) * | 2006-04-19 | 2008-11-12 | Teva Pharma | Composiciones farmaceuticas estables de derivados del acido 2-aza-biciclo[3.3.0]-octano-3-carboxilico. |
| DE602006000402T8 (de) * | 2006-06-02 | 2009-04-09 | Teva Pharmaceutical Industries Ltd. | Stabile Zubereitung enthaltend eine feuchtigkeitsempfindliche aktive Substanz und Verfahren zur Herstellung der Zubereitung. |
| MX2008015343A (es) * | 2006-06-02 | 2008-12-16 | Teva Pharma | Formulacion estable que comprende farmacos sensibles a la humedad y procedimiento de fabricacion de ella. |
| US20070281000A1 (en) * | 2006-06-02 | 2007-12-06 | Michael Fox | Stable formulation comprising moisture sensitive drug/s and manufacturing procedure thereof |
| US20100035955A1 (en) * | 2006-06-30 | 2010-02-11 | Panagiotis Keramidas | Stabilised Composition Comprising ACE Inhibitors |
| KR20090042976A (ko) * | 2006-08-28 | 2009-05-04 | 사노피-아벤티스 도이칠란트 게엠베하 | 글루코즈 수준을 저하시키는 방법 |
| GB0624084D0 (en) * | 2006-12-01 | 2007-01-10 | Selamine Ltd | Ramipril amino acid salts |
| GB0624087D0 (en) * | 2006-12-01 | 2007-01-10 | Selamine Ltd | Ramipril combination salt |
| GB0624090D0 (en) * | 2006-12-01 | 2007-01-10 | Selamine Ltd | Ramipril amine salts |
| PL382311A1 (pl) * | 2007-04-27 | 2008-11-10 | Zakłady Farmaceutyczne POLPHARMA Spółka Akcyjna | Kompozycja farmaceutyczna o polepszonej stabilności zawierająca inhibitor acetylocholinoesterazy lub farmaceutycznie dopuszczalną jego sól oraz sposób jej wytwarzania |
| CN101980701A (zh) | 2008-03-28 | 2011-02-23 | 菲尔若国际公司 | 用于预防心血管疾病的胶囊 |
| US20100062062A1 (en) * | 2008-09-11 | 2010-03-11 | Aethos Pharmaceuticals, Inc. | Stabilized Coating for Pharmaceutical Formulations |
| TR200906322A2 (tr) | 2009-08-17 | 2011-07-21 | Bi̇lgi̇ç Mahmut | Çözünürlük ve stabilite özellikleri geliştirilmiş granüller. |
| ES2364011B1 (es) | 2009-11-20 | 2013-01-24 | Gp Pharm, S.A. | Cápsulas de principios activos farmacéuticos y ésteres de ácidos grasos poliinsaturados para el tratamiento de enfermedades cardiovasculares. |
| EA030466B1 (ru) | 2012-02-17 | 2018-08-31 | Эгиш Дьёдьсердьяр Зрт. | Фармацевтическая композиция, обладающая улучшенной стабильностью |
| PL227900B1 (pl) | 2012-11-15 | 2018-01-31 | Adamed Spolka Z Ograniczona Odpowiedzialnoscia | Kompozycja farmaceutyczna zawierająca inhibitor ACE i bloker kanałów wapniowych, sposób jej wytwarzania i jednostka dawkowania zawierająca tę kompozycję |
| HUP1300496A2 (hu) | 2013-08-16 | 2015-03-02 | Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag | Stabil kombinációs gyógyszerkészítmény |
| EP3275432A1 (en) | 2016-07-25 | 2018-01-31 | H e x a l Aktiengesellschaft | Dosage form with ace inhibitor |
| EP4103158B1 (en) | 2020-02-10 | 2024-09-04 | Adamed Pharma S.A. | Composition comprising ramipril and indapamide |
| CN115068434B (zh) * | 2022-08-03 | 2023-05-09 | 昆山龙灯瑞迪制药有限公司 | 一种雷米普利片的制备方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3565559A (en) * | 1968-03-11 | 1971-02-23 | Sumitomo Chemical Co | Process for making microcapsules |
| IL58849A (en) * | 1978-12-11 | 1983-03-31 | Merck & Co Inc | Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them |
| US4344949A (en) * | 1980-10-03 | 1982-08-17 | Warner-Lambert Company | Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids |
| DE3039073A1 (de) * | 1980-10-16 | 1982-05-19 | Röhm GmbH, 6100 Darmstadt | Umhuelltes acetylsalicylsaeurepraeparat |
| DE3174844D1 (en) * | 1980-10-23 | 1986-07-24 | Schering Corp | Carboxyalkyl dipeptides, processes for their production and pharmaceutical compositions containing them |
| US4425355A (en) * | 1981-02-17 | 1984-01-10 | Warner-Lambert Company | Substituted acyl derivatives of chair form of octahydro-1H-indole-2-carboxylic acids |
| DE3226768A1 (de) * | 1981-11-05 | 1983-05-26 | Hoechst Ag, 6230 Frankfurt | Derivate der cis, endo-2-azabicyclo-(3.3.0)-octan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung |
| WO1985003436A1 (en) * | 1984-02-10 | 1985-08-15 | A/S Alfred Benzon | Diffusion coated multiple-units dosage form |
| DE3413710A1 (de) * | 1984-04-12 | 1985-10-24 | Hoechst Ag, 6230 Frankfurt | Verfahren zur behandlung der herzinsuffizienz |
| CA1232488A (en) * | 1984-04-13 | 1988-02-09 | Macewans Machinery Limited | Heating apparatus |
| CA1259924A (en) * | 1985-03-25 | 1989-09-26 | Wallace E. Becker | Pharmaceutical tableting method |
| DE3610391A1 (de) * | 1986-03-27 | 1987-10-08 | Hoechst Ag | Verbindungen mit nootroper wirkung, diese enthaltende mittel und deren verwendung bei der behandlung und prophylaxe cognitiver dysfunktionen |
| GB8616669D0 (en) * | 1986-07-09 | 1986-08-13 | Merk Sharpe & Dohme Ltd | Pharmaceutical compositions |
| US4743450A (en) * | 1987-02-24 | 1988-05-10 | Warner-Lambert Company | Stabilized compositions |
| CA1323833C (en) * | 1987-04-28 | 1993-11-02 | Yatindra M. Joshi | Pharmaceutical compositions in the form of beadlets and method |
| US4808413A (en) * | 1987-04-28 | 1989-02-28 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions in the form of beadlets and method |
| US4898732A (en) * | 1988-05-04 | 1990-02-06 | The Clinipad Corporation | Inhibiting of tumor growth with an antagonist of the renin-angioten-sin system |
-
1987
- 1987-11-24 DE DE19873739690 patent/DE3739690A1/de not_active Withdrawn
-
1988
- 1988-11-15 ES ES198888119014T patent/ES2033400T3/es not_active Expired - Lifetime
- 1988-11-15 EP EP88119014A patent/EP0317878B1/de not_active Expired - Lifetime
- 1988-11-15 DE DE8888119014T patent/DE3869919D1/de not_active Expired - Lifetime
- 1988-11-15 AT AT88119014T patent/ATE74513T1/de not_active IP Right Cessation
- 1988-11-22 NZ NZ227032A patent/NZ227032A/en unknown
- 1988-11-22 PH PH37849A patent/PH27416A/en unknown
- 1988-11-22 HU HU885992A patent/HU202100B/hu unknown
- 1988-11-22 US US07/274,598 patent/US5151433A/en not_active Expired - Lifetime
- 1988-11-22 ZA ZA888734A patent/ZA888734B/xx unknown
- 1988-11-22 FI FI885398A patent/FI93693C/fi not_active IP Right Cessation
- 1988-11-22 JP JP63293761A patent/JPH0768140B2/ja not_active Expired - Lifetime
- 1988-11-23 DK DK653688A patent/DK168423B1/da not_active IP Right Cessation
- 1988-11-23 PT PT89061A patent/PT89061B/pt not_active IP Right Cessation
- 1988-11-23 IL IL88460A patent/IL88460A0/xx not_active IP Right Cessation
- 1988-11-23 CN CN88108057A patent/CN1028962C/zh not_active Expired - Lifetime
- 1988-11-23 IE IE350588A patent/IE61173B1/en not_active IP Right Cessation
- 1988-11-23 CA CA000583952A patent/CA1338344C/en not_active Expired - Lifetime
- 1988-11-23 AU AU25818/88A patent/AU615495B2/en not_active Expired
- 1988-11-23 NO NO885213A patent/NO176550C/no unknown
- 1988-11-23 KR KR1019880015400A patent/KR970004908B1/ko not_active Expired - Lifetime
-
1992
- 1992-06-17 GR GR920401112T patent/GR3004925T3/el unknown
-
1994
- 1994-02-10 US US08/194,634 patent/US5442008A/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170190877A1 (en) * | 2015-12-31 | 2017-07-06 | Eternal Materials Co., Ltd. | Thermally polymerizable composition, combined solution formed therefrom and use thereof |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1028962C (zh) | 稳定性药物的生产方法 | |
| CN1025151C (zh) | 含酸不稳定化合物的口服药用制剂的制备方法 | |
| CN85109190A (zh) | 生产稳定的尼可地尔制剂的方法 | |
| CN1180769C (zh) | 聚合物基质的速溶片剂及其制备方法 | |
| CN1182841C (zh) | 新的药物制剂及其制备方法 | |
| CN1160058C (zh) | 附聚物 | |
| CN1020852C (zh) | 用作口服的新的药用制剂 | |
| CN1282456C (zh) | 帕罗西汀控释组合物 | |
| CN100337687C (zh) | 含有γ－氨基丁酸衍生物的固体组合物及其制备方法 | |
| CN1284867A (zh) | 生产咀嚼分散片的方法 | |
| CN1809341A (zh) | 多层口溶型片剂 | |
| CN1638803A (zh) | 口腔内速崩解性片剂 | |
| CN1440425A (zh) | 纤维素粉末 | |
| CN1968683A (zh) | 包含两亲性淀粉的药用组合物 | |
| CN1655767A (zh) | 持续释放的包衣颗粒和含有这种颗粒的片剂 | |
| CN1507347A (zh) | 基于血管紧张素转化酶抑制剂的涂布颗粒 | |
| CN1277535C (zh) | 布洛芬活性成分制剂 | |
| CN1206986C (zh) | 包膜马来酸三甲丁酯片剂 | |
| CN1009525B (zh) | 生产稳定的尼柯地尔制剂的方法 | |
| CN1237969C (zh) | 慢性关节风湿病的治疗剂 | |
| CN1561200A (zh) | 快速熔融口服剂型 | |
| CN1111413C (zh) | 含阴离子交换树脂的片剂 | |
| CN1321084A (zh) | 含有布洛芬和多潘立酮的药用组合物 | |
| CN1225580A (zh) | 钾、钠和三羟甲基氨基甲烷噁丙秦盐药物配方 | |
| CN1092074A (zh) | 二氮杂䓬衍生物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C53 | Correction of patent of invention or patent application | ||
| COR | Change of bibliographic data |
Free format text: CORRECT: PATENTEE; FROM: HOECHST AKTIENGESELLSCHAFT (DE) TO: AVENTIS PHARMACY (GERMANY)INTERNATIONAL CO., LTD. |
|
| CP01 | Change in the name or title of a patent holder |
Patentee after: Awentis Medicines Deutschland GmbH Patentee before: Hechester JSC |
|
| C15 | Extension of patent right duration from 15 to 20 years for appl. with date before 31.12.1992 and still valid on 11.12.2001 (patent law change 1993) | ||
| OR01 | Other related matters | ||
| C56 | Change in the name or address of the patentee |
Owner name: SANOFI- AVENTIS GERMAN CO., LTD. Free format text: FORMER NAME OR ADDRESS: AVENTIS PHARMACY (GERMANY)INTERNATIONAL CO., LTD. |
|
| CP03 | Change of name, title or address |
Address after: Frankfurt, Germany Patentee after: Hoechst Marion Roussel de GmbH Address before: Frankfurt, Federal Republic of Germany Patentee before: Awentis Medicines Deutschland GmbH |
|
| C17 | Cessation of patent right | ||
| CX01 | Expiry of patent term |