DE2362123A1 - PHARMACEUTICAL PREPARATIONS - Google Patents
PHARMACEUTICAL PREPARATIONSInfo
- Publication number
- DE2362123A1 DE2362123A1 DE2362123A DE2362123A DE2362123A1 DE 2362123 A1 DE2362123 A1 DE 2362123A1 DE 2362123 A DE2362123 A DE 2362123A DE 2362123 A DE2362123 A DE 2362123A DE 2362123 A1 DE2362123 A1 DE 2362123A1
- Authority
- DE
- Germany
- Prior art keywords
- weight
- parts
- pharmaceutical preparations
- hydroxy
- acid
- 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.)
- Pending
Links
- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 9
- -1 Ouinoterol Chemical compound 0.000 claims description 10
- 239000000150 Sympathomimetic Substances 0.000 claims description 9
- 239000002253 acid Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 7
- 230000001148 spastic effect Effects 0.000 claims description 7
- 150000001412 amines Chemical class 0.000 claims description 5
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 claims description 4
- LSLYOANBFKQKPT-DIFFPNOSSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]benzene-1,3-diol Chemical compound C([C@@H](C)NC[C@H](O)C=1C=C(O)C=C(O)C=1)C1=CC=C(O)C=C1 LSLYOANBFKQKPT-DIFFPNOSSA-N 0.000 claims description 4
- 229960001117 clenbuterol Drugs 0.000 claims description 4
- STJMRWALKKWQGH-UHFFFAOYSA-N clenbuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(Cl)=C1 STJMRWALKKWQGH-UHFFFAOYSA-N 0.000 claims description 4
- QSRHLIUOSXVKTG-UHFFFAOYSA-N eprozinol Chemical compound C=1C=CC=CC=1C(OC)CN(CC1)CCN1CCC(O)C1=CC=CC=C1 QSRHLIUOSXVKTG-UHFFFAOYSA-N 0.000 claims description 4
- 229960001022 fenoterol Drugs 0.000 claims description 4
- 229960000708 hexoprenaline Drugs 0.000 claims description 4
- OXLZNBCNGJWPRV-UHFFFAOYSA-N hexoprenaline Chemical compound C=1C=C(O)C(O)=CC=1C(O)CNCCCCCCNCC(O)C1=CC=C(O)C(O)=C1 OXLZNBCNGJWPRV-UHFFFAOYSA-N 0.000 claims description 4
- 230000001975 sympathomimetic effect Effects 0.000 claims description 4
- 229960000195 terbutaline Drugs 0.000 claims description 4
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 claims description 3
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 3
- 229960002338 eprozinol Drugs 0.000 claims description 3
- 229960001317 isoprenaline Drugs 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 229960001457 rimiterol Drugs 0.000 claims description 3
- IYMMESGOJVNCKV-SKDRFNHKSA-N rimiterol Chemical compound C([C@@H]1[C@@H](O)C=2C=C(O)C(O)=CC=2)CCCN1 IYMMESGOJVNCKV-SKDRFNHKSA-N 0.000 claims description 3
- 229960002052 salbutamol Drugs 0.000 claims description 3
- OXBBIHZWNDPBMQ-UHFFFAOYSA-N 2-[2-(4-benzhydrylpiperazin-1-yl)ethoxy]ethanol Chemical compound C1CN(CCOCCO)CCN1C(C=1C=CC=CC=1)C1=CC=CC=C1 OXBBIHZWNDPBMQ-UHFFFAOYSA-N 0.000 claims description 2
- 208000008238 Muscle Spasticity Diseases 0.000 claims description 2
- 229940124630 bronchodilator Drugs 0.000 claims description 2
- 230000001813 broncholytic effect Effects 0.000 claims description 2
- 229950002790 decloxizine Drugs 0.000 claims description 2
- 208000018198 spasticity Diseases 0.000 claims description 2
- FVNFBBAOMBJTST-UHFFFAOYSA-N 8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one Chemical compound O1C(=O)NCC11CCN(CCC=2C=CC=CC=2)CC1 FVNFBBAOMBJTST-UHFFFAOYSA-N 0.000 claims 2
- PHSMOUBHYUFTDM-UHFFFAOYSA-N colterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(O)=C1 PHSMOUBHYUFTDM-UHFFFAOYSA-N 0.000 claims 2
- 229960002912 fenspiride Drugs 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 description 23
- 239000003826 tablet Substances 0.000 description 20
- 238000002360 preparation method Methods 0.000 description 18
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 14
- 239000000243 solution Substances 0.000 description 10
- 239000004615 ingredient Substances 0.000 description 9
- 230000037396 body weight Effects 0.000 description 8
- 235000019359 magnesium stearate Nutrition 0.000 description 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 230000003111 delayed effect Effects 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 229920002261 Corn starch Polymers 0.000 description 5
- 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 5
- 229920002472 Starch Polymers 0.000 description 5
- 239000008120 corn starch Substances 0.000 description 5
- 239000008101 lactose Substances 0.000 description 5
- 235000019698 starch Nutrition 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 239000008119 colloidal silica Substances 0.000 description 4
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 4
- 235000010262 sodium metabisulphite Nutrition 0.000 description 4
- 239000008107 starch Substances 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- 229920002845 Poly(methacrylic acid) Polymers 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- LMOINURANNBYCM-UHFFFAOYSA-N metaproterenol Chemical compound CC(C)NCC(O)C1=CC(O)=CC(O)=C1 LMOINURANNBYCM-UHFFFAOYSA-N 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- HLWRUJAIJJEZDL-UHFFFAOYSA-M sodium;2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetate Chemical compound [Na+].OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC([O-])=O HLWRUJAIJJEZDL-UHFFFAOYSA-M 0.000 description 3
- QUSNBJAOOMFDIB-UHFFFAOYSA-N Ethylamine Chemical compound CCN QUSNBJAOOMFDIB-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000003708 ampul Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 230000008602 contraction Effects 0.000 description 2
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 2
- 239000008298 dragée Substances 0.000 description 2
- 239000000644 isotonic solution Substances 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229960002657 orciprenaline Drugs 0.000 description 2
- 150000002894 organic compounds Chemical class 0.000 description 2
- XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical compound OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- QPYZEEKXUYXZBK-UHFFFAOYSA-N 4-[hydroxy(piperidin-2-yl)methyl]benzene-1,2-diol;hydrobromide Chemical compound Br.C=1C=C(O)C(O)=CC=1C(O)C1CCCCN1 QPYZEEKXUYXZBK-UHFFFAOYSA-N 0.000 description 1
- 125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 description 1
- IHOXNOQMRZISPV-YJYMSZOUSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-methoxyphenyl)propan-2-yl]azaniumyl]ethyl]-2-oxo-1h-quinolin-8-olate Chemical compound C1=CC(OC)=CC=C1C[C@@H](C)NC[C@H](O)C1=CC=C(O)C2=C1C=CC(=O)N2 IHOXNOQMRZISPV-YJYMSZOUSA-N 0.000 description 1
- BDDLHHRCDSJVKV-UHFFFAOYSA-N 7028-40-2 Chemical compound CC(O)=O.CC(O)=O.CC(O)=O.CC(O)=O BDDLHHRCDSJVKV-UHFFFAOYSA-N 0.000 description 1
- YIUIVFFUEVPRIU-UHFFFAOYSA-N 8-chlorotheophylline Chemical compound O=C1N(C)C(=O)N(C)C2=NC(Cl)=N[C]21 YIUIVFFUEVPRIU-UHFFFAOYSA-N 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 208000009079 Bronchial Spasm Diseases 0.000 description 1
- 208000014181 Bronchial disease Diseases 0.000 description 1
- 206010006458 Bronchitis chronic Diseases 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- 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
- 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 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 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 1
- MKFFGUZYVNDHIH-UHFFFAOYSA-N [2-(3,5-dihydroxyphenyl)-2-hydroxyethyl]-propan-2-ylazanium;sulfate Chemical compound OS(O)(=O)=O.CC(C)NCC(O)C1=CC(O)=CC(O)=C1.CC(C)NCC(O)C1=CC(O)=CC(O)=C1 MKFFGUZYVNDHIH-UHFFFAOYSA-N 0.000 description 1
- QILXPCHTWXAUHE-UHFFFAOYSA-N [Na].NCCN Chemical compound [Na].NCCN QILXPCHTWXAUHE-UHFFFAOYSA-N 0.000 description 1
- 235000011054 acetic acid Nutrition 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 230000003182 bronchodilatating effect Effects 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 239000012876 carrier material Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 208000023819 chronic asthma Diseases 0.000 description 1
- 208000007451 chronic bronchitis Diseases 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 125000004188 dichlorophenyl group Chemical group 0.000 description 1
- 239000006196 drop Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- OEZNULIHEQCKJR-UHFFFAOYSA-N ethanol;hydrobromide Chemical compound Br.CCO OEZNULIHEQCKJR-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 150000002605 large molecules Chemical class 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 230000003387 muscular Effects 0.000 description 1
- XQOIBQBPAXOVGP-UHFFFAOYSA-N n-ethyl-2-methylpropan-2-amine Chemical compound CCNC(C)(C)C XQOIBQBPAXOVGP-UHFFFAOYSA-N 0.000 description 1
- QHCCDDQKNUYGNC-UHFFFAOYSA-N n-ethylbutan-1-amine Chemical compound CCCCNCC QHCCDDQKNUYGNC-UHFFFAOYSA-N 0.000 description 1
- RLSOCANKJLKLPN-UHFFFAOYSA-N n-ethylbutan-1-amine;hydrochloride Chemical compound Cl.CCCCNCC RLSOCANKJLKLPN-UHFFFAOYSA-N 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 229940060184 oil ingredients Drugs 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 210000002027 skeletal muscle Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000008223 sterile water Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 229940064707 sympathomimetics Drugs 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 238000005303 weighing Methods 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
Description
BOEHRINGER INGELHEIM GMBH, INGELHEIM/RHEIN Pharmazeutische ZubereitungenBOEHRINGER INGELHEIM GMBH, INGELHEIM / RHINE Pharmaceutical preparations
Die Erfindung betrifft pharmazeutische Zubereitungen für die Behandlung spastischer Zustände.The invention relates to pharmaceutical preparations for Treatment of spastic conditions.
Es- ist begannt, daß syssgatnomlmetische Amine ein breites Spektrum pharmakolögisclier Wirkungen tesit^esio Öles® Wirkungen finden sich feei den verschiedenen Verbindungen in unterschiedlicher Kombination und Stärke„ Einig© der imine t©ig@K eine starke broncfrodilatatorisch© Wirkung-und eignen sich insbesondere zur Behandlung von Bronchospasmen* zeB. bei chronischer Bronchitis oder Asthma0 It has begun that syssgatnomlmetic amines have a wide range of pharmacological effects, tesit ^ esio oils® effects can be found in the various compounds in different combinations and strengths for the treatment of bronchospasm * z e as chronic bronchitis or asthma 0
Die vorliegende Erfindung basiert auf der Entdeckung, daß sympathomimetische Amine, insbesondere sympathomimetisch© Amine mit bronchodilatorischer Wirkung, zur Behandlung spastischer Zustände geeignet sind. Spastische Zustände9 wie sie mit denrerfindungsgemäßeji Mitteln behandelt .werden.können 9 sind.durch eine/muskulär^"Hypertosii® charakterisiert0 UIq auf aktiver Kontraktion der SkelettmuskulaäüF basierte Die .Bedeutussg der Erfindung beruixt vor allep darauf, daß bisher kein Mittel bekannt geworden i'sts das eine Behandlung. spastischer Zustände durch Beeinflussung der KontraktionThe present invention is based on the discovery that sympathomimetic amines, in particular sympathomimetic amines with a bronchodilatory effect, are suitable for the treatment of spastic conditions. Spasticity 9 as .werden.können treated with denrerfindungsgemäßeji means 9 sind.durch a / muscular ^ "Hypertosii® characterized 0 UIQ on active contraction of SkelettmuskulaäüF based The .Bedeutussg the invention beruixt before allep that so far no means known i 's st the treatment. spastic states by influencing the contraction
409825/1137409825/1137
der Skelettmuskulatur ermöglicht.the skeletal muscles.
Gegenstand der Erfindung sind nun pharmazeutische Zubereitungen für die Behandlung von spastischen Zuständen, die als Wirkstoff ein sympathomimetisches Amin oder ein pharmakologisch unbedenkliches Säureadditionssalz davon enthalten. Als Wirkstoffe besonders geeignete sympathomimetische Amine sind solche, die eine starke brancholytische Wirkung haben. Die Zubereitungen können auch Bestandteile enthalten, die eine verzögerte Wirkstoff freigäbe bewirken. The invention now relates to pharmaceutical preparations for the treatment of spastic conditions, which as an active ingredient a sympathomimetic amine or a pharmacologically acceptable acid addition salt thereof contain. Sympathomimetic amines which are particularly suitable as active ingredients are those which have a strong brancholytic effect to have. The preparations can also contain ingredients that would cause a delayed release of active ingredient.
Sympathomimetische Amine, die erfindungsgemäß verwendet
werden können, sind beispielsweise in äen britischen Patentschriften
920 623, 1 028 805, 1 178 191 und 1 235 399,
in dem deutschen Patent 1 215 729 und in den deutschen
Offenlegungsschriften 1 96O 499» 1 962 497, 2 115 926 und
2 220 480 beschrieben.Sympathomimetic amines that can be used in the invention are, for example, in AEEN British Patents 920,623, 1,028,805, 1,178,191 and 1,235,399,
in German Patent 1,215,729 and in the German
Offenlegungsschriften 1,960,499, 1,962,497, 2,115,926 and 2,220,480.
Im einzelnen sind folgende Verbindungen zu nennen:The following connections are to be mentioned in detail:
1- (3,5-Dihydroxyphenyl)-l-hydroxy-2-isopropylaminoäthan (0rciprenalin$;1- (3,5-dihydroxyphenyl) -1-hydroxy-2-isopropylaminoethane (0rciprenaline $;
1- (4-Amino-3,5-dichlorphenyl) -l-hydroxy-2-tert. -butylaminoäthan (Clenbuterol);1- (4-Amino-3,5-dichlorophenyl) -l-hydroxy-2-tert. -butylaminoethane (Clenbuterol);
1- ( 3-Hy droxymethyl-4-hydroxyphenyl) -l-hydroxy-2-tert. butylaminoäthan (Salbutamol);1- (3-Hydroxymethyl-4-hydroxyphenyl) -l-hydroxy-2-tert. butylaminoethane (Salbutamol);
l-( 3,5-Dihydroxyphenyl)-l-hydroxy-2-[l-C4—hydro3cybenzyl)äthyl] aminoäthan (Fenoterol)j1- (3,5-Dihydroxyphenyl) -l-hydroxy-2- [1- C4-hydro3cybenzyl) ethyl] aminoethane (fenoterol) j
l-( 315-DihvdroxYphenvl)-l-hydroxy-2-tert. -butylaminoäthan (Terbutalin^;1- (315-DihvdroxYphenvl) -l-hydroxy-2- tert . -butylaminoethane (terbutaline ^;
N,N»-Bis-[1-(3,4-dihydroxyphenyl)-l-hydroxyäthyl(2)3-hexamethylendiamin (Hexoprenalinl5N, N »-Bis- [1- (3,4-dihydroxyphenyl) -1-hydroxyethyl (2) 3-hexamethylenediamine (Hexoprenaline 5
409825/1137409825/1137
1- ( 3,4-Dihydf öxyphenyl) -l-hydroxy-2-isopropylaminoäthan (Isoprenalind;1- (3,4-Dihydrofoxyphenyl) -1-hydroxy-2-isopropylaminoethane (Isoprenalind;
2- [ ( 3,4-Dihydroxyphenyl) hydroxyme thyl ]piperidinium-hydrobromid (Rimiterol);2- [(3,4-Dihydroxyphenyl) hydroxymethyl] piperidinium hydrobromide (Rimiterol);
8-Hydroxy-5-( l-hydroxy-2-isoprGpylaminaäthyl) chinolin (Quinoterol);8-Hydroxy-5- (1-hydroxy-2-isopropylamine ethyl) quinoline (Quinoterol);
l-Diphenylmethyl-4-hydroxyäthoxyäthyl-plp.erazin (Decloxizine) jl-Diphenylmethyl-4-hydroxyethoxyethyl plp.erazine (Decloxizine) j
1-(2-Phenyl-2-methoxyäthyl)-4-(3-hydroxy-3-phenylpropyl)piperazin (Eprozinol);1- (2-phenyl-2-methoxyethyl) -4- (3-hydroxy-3-phenylpropyl) piperazine (Eprozinol);
1-(3 ρ 4-Dihydroxyphenyl)-l-hydroxy-2-tert.-butylaminoäthan.1- (3 ρ 4-dihydroxyphenyl) -l-hydroxy-2-tert-butylaminoethane.
Die Wirkstoffe der erfindungsgemäßen Zubereitungen sind organische Basen und können daher in Form von Säureadditionssalzen mit anorganischen oder organischen Säuren vorliegen. Beispiele für solche Säuren sind Salzsäure, Bromwasserstoffsäure , Schwefelsäure 9 Phosphorsäure» Salpetersäure, Essigsäure , Propionsäure, Oxalsäure, Malonsäure, Bernsteinsäure, Maleinsäure, Fumarsäure s Milchsäure, Weinsäure, Zitronensäure, Benzoesäure, Phthalsäure, Salicylsäure, Nikotinsäure, 8-Chlortheophyllinc,The active ingredients of the preparations according to the invention are organic bases and can therefore be in the form of acid addition salts with inorganic or organic acids. Examples of such acids are hydrochloric acid, hydrobromic acid, sulfuric acid 9 phosphoric acid »nitric acid, acetic acid, propionic acid , oxalic acid, malonic acid, succinic acid, maleic acid, fumaric acid s lactic acid, tartaric acid, citric acid, benzoic acid, phthalic acid, salicylic acid, nicotinic acid, 8-chlorotheophylline,
Als Wirkstoffe für die Verwendung in den erfindungsgemäßen Zubereitungen eignen sich besonders Cleributeröl, Fenoterol und Salbutamol. Diese Verbindungen zeichnen sich auch durch eine lange anhaltende Wirkung aus. Sie kommen damit dem Bestreben entgegen, eine anhaltende Wirkung mit höchstens zwei oder drei Applikationen pro Tag zu erreichen.As active ingredients for use in the inventive Preparations are particularly suitable cleributer oil, fenoterol and salbutamol. These connections are also characterized by a long-lasting effect. You thus meet the endeavor to have a lasting effect with at most to achieve two or three applications per day.
409825/1137 .409825/1137.
Die erfindungsgemäßen Zubereitungen werden nach den üblichen Methoden der galenischen Pharmazie mit Hilfs- und Trägerstoffen zu oral oder parenteral anwendbaren Zubereitungen verarbeitet, beispielsweise zu Tabletten, Dragees, Granulaten, Kapseln, Sirupen, Emulsionen, Suspensionen oder Tropfen. Geeignete Trägerstoffe für feste Zubereitungen, wie Tabletten, Kapseln, sind u.a. Lactose, Maisstärke, Kartoffelstärke, lösliche Stärken oder Magnesiumstearat,The preparations according to the invention are prepared using the customary methods of galenic pharmacy with auxiliaries and carriers processed into preparations that can be used orally or parenterally, for example tablets, dragees, granules, Capsules, syrups, emulsions, suspensions or drops. Suitable carriers for solid preparations such as tablets, Capsules, include lactose, corn starch, potato starch, soluble starches or magnesium stearate,
Für die parenterale Anwendung kommen sterile Flüssigkeiten, wie steriles Wasser oder ein für die parenterale Anwendung geeignetes Öl,in Betracht.Sterile liquids are used for parenteral use, such as sterile water or an oil suitable for parenteral use.
Die oral oder parenteral anwendbaren Zubereitungen können zusätzlich einen Stoff enthalten, der eine verzögerte Wirkstofffreigabe bewirkt und damit eine Verlängerung der Wirkungsdauer ermöglichst. Für diesen Zweck können übliche Verzögerungszusätze verwendet werden. Beispiele für solche Zusätze sind bei festen Zubereitungen z.B. hochmolekulare organische Verbindungen, mit denen die Wirkstoffe gemischt werden oder die als Matrix für die Wirkstoffe dienen. Beispiele für solche hochmolekularen Verbindungen sind Natr!^carboxymethylcellulose, PoIymethacrylsäure oder Polyvinylchlorid. Pur die Herstellung flüssiger Zubereitungen mit verzögerter Wirkstofffreigabe werden hauptsächlich solche Substanzen zugesetzt, welche die Viskosität der Zubereitung erhöhen. Dies sind im allgemeinen hochmolekulare organische Verbindungen, beispielsweise Natriumcarboxymethylcellulose oder PolyvinylpyuDlidon.The preparations which can be used orally or parenterally can additionally contain a substance which retards a Release of active ingredients causes and thus an extension of the Duration of effect possible. Common delay additives can be used for this purpose. Examples of such additives in solid preparations are, for example, high molecular weight organic compounds with which the Active ingredients are mixed or which serve as a matrix for the active ingredients. Examples of such high molecular weight Compounds are sodium carboxymethyl cellulose, polymethacrylic acid or polyvinyl chloride. Purely for the production of liquid preparations with delayed release of active ingredients those substances are mainly added which increase the viscosity of the preparation. These are in general high molecular weight organic compounds, for example sodium carboxymethyl cellulose or polyvinylpyuDlidon.
Die Größe der Einzeldosis der erfindungsgemäß verwendbaren sympathomimetischen Amine hängt u.a. davon ab, ob es sich > um eine Zubereitung mit normaler oder verzögerter Wirkstofffreigabe handelt. Bei normaler Wirkstofffreigabe beträgtThe size of the single dose of the sympathomimetic amines useful in this invention depends on, among other things, whether it> is a preparation with normal or sustained release. With normal release of active ingredients is
409825/113409825/113
die Einzeldosis ungefähr die Hälfte der broncholytisch wirksamen Dosis. Im Einzelfall können jedoch deutliche Abweichungen von diesem Wert, insbesondere nach unten, festgestellt werden.the single dose is about half that of the broncholytic effective dose. In individual cases, however, significant Deviations from this value, especially downwards, to be established.
Für Orciprenaline beispielsweise beträgt die Einzeldosis bei parenteraler Anwendung etwa 0,00167 bis 0,0066? mg/kg, vorzugsweise etwa 0,004 mg/kg Körpergewicht, während bei oralen" Zubereitungen die Einzeldosis zwischen etwa 0,05 und 0,117 mg/kg beträgt. Die Tagesdosis.ist im allgemeinen zwei- bis dreimal so groß wie die Einzeldosis und beträgt beim Orciprenaline etwa 0,00333 bis 0,0833 mg/kg Körpergewicht für die parenterale Anwendung und etwa 0,1 bis 1,67 mg/kg Körpergewicht für die orale Anwendung.For Orciprenaline, for example, the single dose is for parenteral use about 0.00167 to 0.0066? mg / kg, preferably about 0.004 mg / kg body weight, while with oral "preparations the single dose between about 0.05 and Is 0.117 mg / kg. The daily dose. Is in general two to three times as large as the single dose and for Orciprenaline is about 0.00333 to 0.0833 mg / kg body weight for parenteral use and about 0.1 to 1.67 mg / kg body weight for oral use.
Bei Clenbuterol ist die parenterale Einzeldosis 0,0833 bis 0,833 Ύ pro kg,vorzugsweise 0,333 y/kg Körpergewichts während die orale Einzeldosis O0167 bis 1S67 y/kg? vorzugsweise 0,833 y/kg Körpergewicht beträgt« Im Falle der Zubereitungen mit verzögerter Wirkstofffreigäbe ist die parenterale Dosis 0,333 Ms 1S6? y/kg: Körpergewicht, vorzugsweise 0^833 y/^ge w& ίϋ® orale Dosis Ist 0,5 bis 2p5 y/kgi, vorzugsweise 1?67 y/kg„ Die Tagesdosis beträgt vorzugsweise 0s000167 bis' OpOOl67 mg/kg Körpergewicht bei parenteraler und O900035 Ms Ο-,, 0033 mg/kg Körpergewicht bei oraler Anwendung, In der folgenden Tabelle sind die entsprechenden Angaben für eine Reihe weiterer Sympathomimetika gemacht.With Clenbuterol, the parenteral single dose is 0.0833 to 0.833 Ύ per kg, preferably 0.333 y / kg of body weight, while the oral single dose is 0 167 to 1 S 67 y / kg ? preferably 0.833 y / kg body weight is «In the case of the preparations with delayed release of active ingredient, the parenteral dose is 0.333 Ms 1 S 6? y / kg: body weight, preferably 0 ^ 833 y / ^ ge w & ίϋ® oral dose Is 0.5 to 2p5 y / kgi, preferably 1 ? 67 y / kg “The daily dose is preferably 0 s 000167 to 'O p OOl67 mg / kg body weight for parenteral and O 9 00035 Ms Ο- ,, 0033 mg / kg body weight for oral use. The following table gives the corresponding information for made a number of other sympathomimetics.
4 0 9 8 2 5/11374 0 9 8 2 5/1137
- 10 mg1 - 1 mg
- 10 mg
oralparenteral
orally
10,
1
2 - 30 mg0.2-3 mg
2 - 30 mg
- 10 mg025-0.2 mg
- 10 mg
oralparenteral
orally
1 O,
1
1 - 1 mg- 20 γ
1 - 1 mg
2 - 30 mg0.05-0.6 mg
2 - 30 mg
oralparenteral
orally
o, 2
O,
0,2 - 3 mg4 - 60 γ
0.2-3 mg
In jedem Fall liegt die bevorzugte Einzeldosis ungefähr in der Mitte des angegebenen Bereichs.In either case, the preferred single dose is approximately in the center of the specified area.
409825/113?409825/113?
Für die in der Tabelle ausgeführten Sysspa-thomimetika liegt die bevorzugte Anwendungsdosis.--.etwa in der Mitte der angegebenen Dosisbereiche.For the Sysspa thomimetics listed in the table the preferred application dose -. approximately in the middle of the specified Dose ranges.
Die folgenden Beispiele sollen die Herstellung der erfindungsgemäßenZubereitungen näher erläutern:The following examples are intended to illustrate the preparation of the preparations according to the invention explain in more detail:
Eine InjektionslÖsung mit verzögerter Wirkstoff freigäbe wird in üblicher Weise unter sterilen Bedingungen aus denA solution for injection with a delayed active ingredient would be released is in the usual way under sterile conditions from the
folgenden Bestandteilen hergestellt;the following components manufactured;
1- ( 3 ρ 5-Dihydroxyphenyl) -1-hy droxy-2-isopropylaminoäthanhydrobromid 1,0 Gew.-Teile1- (3 ρ 5-dihydroxyphenyl) -1-hydroxy-2-isopropylaminoethane hydrobromide 1.0 part by weight
Natriumearboxymethylcellulose . 50,0 Gew.-TeileSodium arboxymethyl cellulose. 50.0 parts by weight
Natriumsalz der Ethylendiamintetraessigsäure 3,0 Gew.-TeileEthylenediaminetetraacetic acid sodium salt 3.0 parts by weight
Natriumpyrosulfit 5,0 Gew.-TeileSodium pyrosulfite 5.0 parts by weight
dest. Wasser - ad 1000,0 Volum-Teileleast. Water - ad 1000.0 parts by volume
Jeweils 1 ml der Zubereitung wird in eine Kapsel abgefüllt, sodaß jede Kapsel 1 mg des Wirkstoffs enthält.Each 1 ml of the preparation is filled into a capsule, so that each capsule contains 1 mg of the active ingredient.
In.j ektionslösung /. I n.j ection solution /.
Eine Injektionslösung mit verzögerter Wirkstofffreigäbe wurde unter sterilen Bedingungen in üblicher Weise aus den folgenden Wirkstoffen hergestellt:A delayed release solution for injection was prepared under sterile conditions in the usual way from the following active ingredients:
1- (4-Amino-3,5-idichlorphenyl) -1—hydroxy-2-tert. -butylaminoäthan-hydrobromid ' 0,08 Gew.-Teile1- (4-Amino-3,5- i dichlorophenyl) -1-hydroxy-2-tert. -butylaminoethane hydrobromide '0.08 part by weight
Natriumcarboxymethylcellulose 50,0 Gew.—TeileSodium carboxymethyl cellulose 50.0 parts by weight
Natriumsalz der Äthylendiamintetraessigsäure Ethylenediaminetetraacetic acid sodium salt
NatriumpyrosulfitSodium pyrosulfite
dest. Wasser , adleast. Water, ad
409825/1137409825/1137
■ 2362T23■ 2362T23
*™ O "■* ™ O "■
Jeweils 1 ml der Zubereitung wird in eine Ampulle gefüllt, sodaß jede Ampulle 0,0$ mg der Aminoäthanverbindung In each case 1 ml of the preparation is filled into an ampoule, so that each ampoule contains 0.0 mg of the aminoethane compound
enthält.contains.
Beispiel 3 Ine.jektionslÖsungExample 3 Injection solution
Eine Injektionslösung wird nach üblichen Methoden unter sterilen Bedingungen aus den folgenden Bestandteilen zusammengesetzt: An injection solution is composed of the following components according to the usual methods under sterile conditions:
l-(3,5-Dihydroxyphenyl)-l-hydroxy-2-tert.-butyl-l- (3,5-dihydroxyphenyl) -l-hydroxy-2-tert.-butyl-
aminoäthan 0,25 Gew.-Teileaminoethane 0.25 parts by weight
NatriumpyrosulfitSodium pyrosulfite
Natriumsalz der Äthylendiamintetraessigsäure Ethylenediaminetetraacetic acid sodium salt
0,1 η Salzsäure ad pH0.1 η hydrochloric acid ad pH
Natriumchlorid zur Einstellung einer isotonischen LösungSodium chloride to adjust an isotonic solution
dest. Wasser · adleast. Water ad
Die Lösung wird zu jeweils 1 ml in Ampullen gefüllt, von denen jede dann 0,25 mg des Wirkstoffs enthält.The solution is filled into ampoules of 1 ml each, each of which then contains 0.25 mg of the active ingredient.
Injektionslösung Injection solution
Eine Injektionslösung wird aus den folgenden Bestandteilen A solution for injection is made up of the following ingredients
zusammengesetzt:composed:
1-(3-Hydroxymethyl-4-hydroxyphenyl)-1-hydroxy- 1- (3-hydroxymethyl-4-hydroxyphenyl) -1-hydroxy-
2-tert.-butylaminoäthan 0,02 Gew.-Teile2-tert-butylaminoethane 0.02 part by weight
Natriumpyrosulfit 2,5 Gew.-Teile Sodium pyrosulfite 2.5 parts by weight
Natriumsalz der Äthylendiamin-Ethylenediamine sodium salt
tetraessigsäure 3,0 Gew.--Teile tetraacetic acid 3.0 parts by weight
0,ln Salzsäure ad pH 3#50.1 ln hydrochloric acid to pH 3 # 5
Natriumchlorid bis zur EinstellungSodium chloride to adjust to
einei? isotonischen Lösung . "an egg? isotonic solution. "
dest. V/asser ad 1000,0 Volup-Teile least. V / ater ad 1000.0 volup parts
409825/1137409825/1137
Die Lösung wird zu jeweils 1 ml in Ampullen gefüllt, sodaß jede 0,02 mg des Wirkstoffs enthält„The solution is filled into ampoules of 1 ml each, so that each 0.02 mg of the active ingredient contains "
Beispiel 5 - ■ Example 5 - ■
TablettenTablets
Tabletten können in üblicher Weise aus den folgenden Bestandteilen hergestellt werden?Tablets can be made in the usual way from the following ingredients getting produced?
1-(3,5-Dihydroxyphenyl)-1-hydroxy—2-isopropylaminoäthan-sulfat . - 10,0 Gew.-Teile1- (3,5-Dihydroxyphenyl) -1-hydroxy-2-isopropylaminoethane sulfate . - 10.0 parts by weight
Maisstärke 140,0 Gew.-TeileCorn starch 140.0 parts by weight
Lac^tose, gepulvert « -, 138,0~ Gew.-TeileLac ^ tose, powdered «-, 138.0 parts by weight
kolloidale Kieselsäure 5p0 Gew.-Teilecolloidal silica 5 p 0 parts by weight
Magnesiumstearat ·" 2,0 Gew,-TeileMagnesium stearate · "2.0 parts by weight
lösliche Stärke 5,0 Gew.-Teilesoluble starch 5.0 parts by weight
Die Bestandteile werden zu Tabletten mit einem Wirkstoffgehalt von 10,0 mg verarbeitet. :The ingredients become tablets with an active ingredient content of 10.0 mg processed. :
Beispiel 6 ■ Example 6 ■
Tabletten ' ' Tablets ''
Erfindungsgemäße Tabletten werden in üblicher Weise aus den folgenden Bestandteilen erhalten?Tablets according to the invention are made in the usual way from the the following ingredients?
1-(3,5-Dihydrcxyphenyl)-1-hydroxy-2-tert.-buty1-aminoäthan-hydrochlorid 5,0 Gew.-Teile1- (3,5-Dihydroxyphenyl) -1-hydroxy-2-tert-buty1-aminoethane hydrochloride 5.0 parts by weight
Maisstärke 1^5,0 Gew.-TeileCorn starch 1 ^ 5.0 parts by weight
Lactose, gepulvert 138,0 Gew.-TeileLactose, powdered 138.0 parts by weight
kolloidale Kieselsäure 5s0 Gew.-Teilecolloidal silica 5 s 0 parts by weight
Magnesiumstearat 2,0 Gew„-TeileMagnesium stearate 2.0 parts by weight
lösliche Stärke 5,0 Gewo-Teilesoluble starch 5.0 weight parts by o
4 0 9 8 25/113 74 0 9 8 25/113 7
Aus den Bestandteilen werden Tabletten von. 300 mg Gewicht hergestellt, so daß jede Tablette 5,0 mg des WirkstoffsThe ingredients become tablets of. 300 mg weight made so that each tablet 5.0 mg of the active ingredient
enthält. .contains. .
TablettenTablets
Erfindungsgemäße Tabletten werden in üblicher Weise ausTablets according to the invention are made in the usual way
folgenden Bestandteilen hergestellt:the following components:
1- (4-Amino- 3,5-dichlorphenyl) -l-foydfoxy-2-tert. -1- (4-Amino-3,5-dichlorophenyl) -l-foydfoxy-2-tert. -
butylaminoäthan-hydrochlorid 0,025 Gew.-Teilebutylaminoethane hydrochloride 0.025 part by weight
Maisstärke X40,G Gew.-TeileCorn starch X40, G parts by weight
Lactose, gepulvert v 1?β,0 Gew.-TeileLactose, powdered v 1? Β, 0 parts by weight
kolloidale Kieselsäure * 5,0 Gew.-Teilecolloidal silica * 5.0 parts by weight
Magnesiumstearat 2,0 Gew.-TeileMagnesium stearate 2.0 parts by weight
lösliche Stärke 5,0 Gew.-Teilesoluble starch 5.0 parts by weight
Aus den Bestandteilen werden Tabletten von 290 mg Gewicht gepreßt, so daß jede Tablette 0,025 mg des Wirkstoffs enthält.The ingredients become tablets weighing 290 mg pressed so that each tablet contains 0.025 mg of the active ingredient.
Beispiel 8 TablettenExample 8 Tablets
Erfindungsgemäße Tabletten werden aus den folgenden Bestandteilen hergestellt:Tablets according to the invention are made up of the following ingredients manufactured:
l-( 3,5-Dihydroxyphenyl)-2-[l-(4-hydroxybenzyl)-äthylamino}-l- (3,5-dihydroxyphenyl) -2- [l- (4-hydroxybenzyl) ethylamino} -
äthanol-hydrobromid 3,0 Gew.-Teileethanol hydrobromide 3.0 parts by weight
Maisstärke 147,0 Gew.-TeileCorn starch 147.0 parts by weight
Lactose, gepulvert 138,0 Gew.—TeilePowdered lactose, 138.0 parts by weight
kolloidale Kieselsäure 5,0 Gew.-Teilecolloidal silica 5.0 parts by weight
Magnesiumstearat 2,0 Gew.-TeileMagnesium stearate 2.0 parts by weight
lösliche Stärke ■ 5,0 Gew.-Teilesoluble starch ■ 5.0 parts by weight
.4 09825/1137.4 09825/1137
Die Bestandteile werden zu Tabletten von 300 mg Gewicht
verpreßt, so daß jede Tablette 3 mg des ,Wirkstoffs enthält.The ingredients become tablets of 300 mg in weight
compressed so that each tablet contains 3 mg of the active ingredient.
Der Tabiettenkern wird aus den folgenden BestandteilenThe tablet core is made up of the following components
hergestellt:manufactured:
1-(3,5—Bihydroxyphenyl) —1—hydroxy—2-isopropylaminoäthan-1- (3,5-Bihydroxyphenyl) -1-hydroxy-2-isopropylaminoethane-
sulfat 40,0 Gew;-Teilesulfate 40.0 parts by weight
Lactose, gepulvert 119,2 Gew.-TeileLactose, powdered 119.2 parts by weight
Pölymethacrylsäure 40,0 Gew.-TeilePoly methacrylic acid 40.0 parts by weight
Natriumchlorid 20,0 Gew.-TeileSodium chloride 20.0 parts by weight
Magnesiumstearat 0,8 Gew.-TeileMagnesium stearate 0.8 part by weight
Die Kerne werden zunächst mit einer iSisciiung aus den folgenden Bestandteilen überzogen:The nuclei are first selected from the following Coated components:
Pölymethacrylsäure 19,8 Gew.-TeilePoly methacrylic acid 19.8 parts by weight
Magnesiumstearat - 8,22 Gew.-TeileMagnesium stearate - 8.22 parts by weight
Di-n-butylphthalat 1,95 Gew.-TeileDi-n-butyl phthalate 1.95 parts by weight
Die Außehschicht der Dragees besteht aus folgenden Bestandteilen: " . ·
1^-( 3,5-Dihydroxyphenyl)-l-hydroxy-2-Isopropylaminoäthah-sülfat
. 10,0 Gew.-Teile Träger ad 150,0 Gew.-TeileThe outer layer of the coated tablets consists of the following components: ". ·
1 ^ - (3,5-dihydroxyphenyl) -l-hydroxy-2-isopropylaminoethane sulfate. 10.0 parts by weight of carrier to 150.0 parts by weight
Jedes Dragee hat ein Gewicht von 400 mg und enthält insge- . samt 50 mg des Wirkstoffs.Each coated tablet has a weight of 400 mg and contains a total of. including 50 mg of the active ingredient.
Analog den obigen Beispielen können auch die anderen er-Analogous to the above examples, the other
findungsgemäß verwendbaren sympathoiaimetischen Amine zu
üblichen galenischeii Zubereitungen verarbeitet werden»according to the invention usable sympathoimetic amines
usual galenic preparations are processed »
409 8 25/1137409 8 25/1137
Statt der angegebenen Säureadditionssalze können auch andere pharmakologisch annehmbare Säureadditionssalze eingesetzt werden. Auch kann die Menge der verwendeten Wirkstoffe pro Einzeldosis innerhalb der oben angegebenen Grenzen variiert werden. Gewünschtenfalls können auch Art und Menge der verwendeten Hilfs- und Trägerstoffe den jeweiligen Erfordernissen angepaßt werden.Instead of the specified acid addition salts can also other pharmacologically acceptable acid addition salts can be used. Also can be the amount of used Active ingredients per single dose can be varied within the limits given above. If desired, can also Type and amount of the auxiliary and carrier materials used be adapted to the respective requirements.
Λ09825/1.137Λ09825 / 1.137
Claims (5)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB5808872A GB1453034A (en) | 1972-12-15 | 1972-12-15 | Pharmaceutical composition for treating spasticity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE2362123A1 true DE2362123A1 (en) | 1974-06-20 |
Family
ID=10480743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE2362123A Pending DE2362123A1 (en) | 1972-12-15 | 1973-12-14 | PHARMACEUTICAL PREPARATIONS |
Country Status (6)
| Country | Link |
|---|---|
| BE (1) | BE808662A (en) |
| DE (1) | DE2362123A1 (en) |
| GB (1) | GB1453034A (en) |
| IE (1) | IE38655B1 (en) |
| IL (1) | IL43820A (en) |
| ZA (1) | ZA739480B (en) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4237141A (en) * | 1977-06-02 | 1980-12-02 | Nippon Kayaku Kabushiki Kaisha | Derivatives of α-methyl-β-aminopropiophenone and use thereof |
| EP0022932A1 (en) * | 1979-07-20 | 1981-01-28 | Chemie Linz Aktiengesellschaft | Composition with prolonged broncholytic and tokolytic activity, process for preparing it, and broncholytically and tokolytically active agent |
| DE3319356A1 (en) * | 1982-05-27 | 1983-12-01 | Glaxo Group Ltd., London | DRUG |
| FR2551974A1 (en) * | 1983-09-16 | 1985-03-22 | Shionogi & Co | PREPARATION OF DOBUTAMINE FOR ORAL ADMINISTRATION |
| EP0251425A1 (en) * | 1986-04-03 | 1988-01-07 | Hercon Laboratories Corporation | Article for administration of pharmacologically-active substances |
| US5310559A (en) * | 1982-09-01 | 1994-05-10 | Hercon Laboratories Corporation | Device for controlled release and delivery to mammalian tissue of pharmacologically active agents incorporating a rate controlling member which comprises an alkylene-alkyl acrylate copolymer |
| US5468501A (en) * | 1982-09-01 | 1995-11-21 | Hercon Laboratories Corporation | Article useful for administration of pharmacologically-active substances transdermally, orally or by means of implant |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4525359A (en) * | 1982-12-10 | 1985-06-25 | Greenway Frank L Iii | Treatment for selective weight control |
| US4751071A (en) * | 1983-12-01 | 1988-06-14 | Alza Corporation | Composition comprising salbutamol |
| US4777049A (en) * | 1983-12-01 | 1988-10-11 | Alza Corporation | Constant release system with pulsed release |
| US4851229A (en) * | 1983-12-01 | 1989-07-25 | Alza Corporation | Composition comprising a therapeutic agent and a modulating agent |
-
1972
- 1972-12-15 GB GB5808872A patent/GB1453034A/en not_active Expired
-
1973
- 1973-12-14 ZA ZA00739480*DA patent/ZA739480B/en unknown
- 1973-12-14 IE IE2267/73A patent/IE38655B1/en unknown
- 1973-12-14 BE BE138890A patent/BE808662A/en unknown
- 1973-12-14 DE DE2362123A patent/DE2362123A1/en active Pending
- 1973-12-14 IL IL43820A patent/IL43820A/en unknown
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4237141A (en) * | 1977-06-02 | 1980-12-02 | Nippon Kayaku Kabushiki Kaisha | Derivatives of α-methyl-β-aminopropiophenone and use thereof |
| EP0022932A1 (en) * | 1979-07-20 | 1981-01-28 | Chemie Linz Aktiengesellschaft | Composition with prolonged broncholytic and tokolytic activity, process for preparing it, and broncholytically and tokolytically active agent |
| DE3319356A1 (en) * | 1982-05-27 | 1983-12-01 | Glaxo Group Ltd., London | DRUG |
| US5310559A (en) * | 1982-09-01 | 1994-05-10 | Hercon Laboratories Corporation | Device for controlled release and delivery to mammalian tissue of pharmacologically active agents incorporating a rate controlling member which comprises an alkylene-alkyl acrylate copolymer |
| US5468501A (en) * | 1982-09-01 | 1995-11-21 | Hercon Laboratories Corporation | Article useful for administration of pharmacologically-active substances transdermally, orally or by means of implant |
| FR2551974A1 (en) * | 1983-09-16 | 1985-03-22 | Shionogi & Co | PREPARATION OF DOBUTAMINE FOR ORAL ADMINISTRATION |
| EP0251425A1 (en) * | 1986-04-03 | 1988-01-07 | Hercon Laboratories Corporation | Article for administration of pharmacologically-active substances |
Also Published As
| Publication number | Publication date |
|---|---|
| IE38655B1 (en) | 1978-05-10 |
| AU6364773A (en) | 1975-06-19 |
| ZA739480B (en) | 1975-08-27 |
| BE808662A (en) | 1974-06-14 |
| GB1453034A (en) | 1976-10-20 |
| IE38655L (en) | 1974-06-15 |
| IL43820A (en) | 1977-08-31 |
| IL43820A0 (en) | 1974-03-14 |
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