NL8203457A - PHARMACEUTICAL PREPARATIONS. - Google Patents
PHARMACEUTICAL PREPARATIONS. Download PDFInfo
- Publication number
- NL8203457A NL8203457A NL8203457A NL8203457A NL8203457A NL 8203457 A NL8203457 A NL 8203457A NL 8203457 A NL8203457 A NL 8203457A NL 8203457 A NL8203457 A NL 8203457A NL 8203457 A NL8203457 A NL 8203457A
- Authority
- NL
- Netherlands
- Prior art keywords
- preparation according
- pharmaceutical preparation
- ranitidine
- indomethacin
- ibuprofen
- Prior art date
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- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 9
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 20
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims description 10
- 229960001680 ibuprofen Drugs 0.000 claims description 10
- 229960000905 indomethacin Drugs 0.000 claims description 10
- 229960000620 ranitidine Drugs 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 8
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 5
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 5
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 5
- 230000009885 systemic effect Effects 0.000 claims description 5
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
- RBBWCVQDXDFISW-UHFFFAOYSA-N Feprazone Chemical compound O=C1C(CC=C(C)C)C(=O)N(C=2C=CC=CC=2)N1C1=CC=CC=C1 RBBWCVQDXDFISW-UHFFFAOYSA-N 0.000 claims description 2
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims description 2
- 229960001671 azapropazone Drugs 0.000 claims description 2
- WOIIIUDZSOLAIW-NSHDSACASA-N azapropazone Chemical compound C1=C(C)C=C2N3C(=O)[C@H](CC=C)C(=O)N3C(N(C)C)=NC2=C1 WOIIIUDZSOLAIW-NSHDSACASA-N 0.000 claims description 2
- 229960004277 benorilate Drugs 0.000 claims description 2
- FEJKLNWAOXSSNR-UHFFFAOYSA-N benorilate Chemical compound C1=CC(NC(=O)C)=CC=C1OC(=O)C1=CC=CC=C1OC(C)=O FEJKLNWAOXSSNR-UHFFFAOYSA-N 0.000 claims description 2
- 229960001259 diclofenac Drugs 0.000 claims description 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims description 2
- 229960000616 diflunisal Drugs 0.000 claims description 2
- HUPFGZXOMWLGNK-UHFFFAOYSA-N diflunisal Chemical compound C1=C(O)C(C(=O)O)=CC(C=2C(=CC(F)=CC=2)F)=C1 HUPFGZXOMWLGNK-UHFFFAOYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- ZPAKPRAICRBAOD-UHFFFAOYSA-N fenbufen Chemical compound C1=CC(C(=O)CCC(=O)O)=CC=C1C1=CC=CC=C1 ZPAKPRAICRBAOD-UHFFFAOYSA-N 0.000 claims description 2
- 229960001395 fenbufen Drugs 0.000 claims description 2
- 229960000489 feprazone Drugs 0.000 claims description 2
- 229960004369 flufenamic acid Drugs 0.000 claims description 2
- LPEPZBJOKDYZAD-UHFFFAOYSA-N flufenamic acid Chemical compound OC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 LPEPZBJOKDYZAD-UHFFFAOYSA-N 0.000 claims description 2
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 2
- 229960000991 ketoprofen Drugs 0.000 claims description 2
- 229960003464 mefenamic acid Drugs 0.000 claims description 2
- HYYBABOKPJLUIN-UHFFFAOYSA-N mefenamic acid Chemical compound CC1=CC=CC(NC=2C(=CC=CC=2)C(O)=O)=C1C HYYBABOKPJLUIN-UHFFFAOYSA-N 0.000 claims description 2
- 229960002009 naproxen Drugs 0.000 claims description 2
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- -1 phenoprofen Chemical compound 0.000 claims description 2
- 229960001017 tolmetin Drugs 0.000 claims description 2
- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 claims description 2
- VMXUWOKSQNHOCA-LCYFTJDESA-N ranitidine Chemical compound [O-][N+](=O)/C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-LCYFTJDESA-N 0.000 claims 3
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 229960002390 flurbiprofen Drugs 0.000 claims 1
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims 1
- 229960000649 oxyphenbutazone Drugs 0.000 claims 1
- HFHZKZSRXITVMK-UHFFFAOYSA-N oxyphenbutazone Chemical compound O=C1C(CCCC)C(=O)N(C=2C=CC=CC=2)N1C1=CC=C(O)C=C1 HFHZKZSRXITVMK-UHFFFAOYSA-N 0.000 claims 1
- 229960002702 piroxicam Drugs 0.000 claims 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims 1
- 229960000894 sulindac Drugs 0.000 claims 1
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 14
- 239000000203 mixture Substances 0.000 description 13
- VMXUWOKSQNHOCA-UKTHLTGXSA-N ranitidine Chemical compound [O-][N+](=O)\C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-UKTHLTGXSA-N 0.000 description 8
- 229960001520 ranitidine hydrochloride Drugs 0.000 description 8
- GGWBHVILAJZWKJ-KJEVSKRMSA-N ranitidine hydrochloride Chemical compound [H+].[Cl-].[O-][N+](=O)\C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 GGWBHVILAJZWKJ-KJEVSKRMSA-N 0.000 description 8
- 235000019359 magnesium stearate Nutrition 0.000 description 7
- 229920002472 Starch Polymers 0.000 description 5
- 239000002775 capsule Substances 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 239000008107 starch Substances 0.000 description 5
- 229940032147 starch Drugs 0.000 description 5
- 235000019698 starch Nutrition 0.000 description 5
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 4
- 230000002496 gastric effect Effects 0.000 description 4
- 239000007903 gelatin capsule Substances 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 3
- 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 3
- 238000002360 preparation method Methods 0.000 description 3
- 238000011282 treatment Methods 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 208000007107 Stomach Ulcer Diseases 0.000 description 2
- 230000000202 analgesic effect Effects 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 238000013270 controlled release Methods 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229960001340 histamine Drugs 0.000 description 2
- 230000004968 inflammatory condition Effects 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000829 suppository 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
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 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
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-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
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 201000002661 Spondylitis Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000000172 allergic effect Effects 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000011260 co-administration Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 208000000718 duodenal ulcer Diseases 0.000 description 1
- 239000008157 edible vegetable oil Substances 0.000 description 1
- 235000010944 ethyl methyl cellulose Nutrition 0.000 description 1
- IDKAXRLETRCXKS-UHFFFAOYSA-N fenclofenac Chemical compound OC(=O)CC1=CC=CC=C1OC1=CC=C(Cl)C=C1Cl IDKAXRLETRCXKS-UHFFFAOYSA-N 0.000 description 1
- 229950006236 fenclofenac Drugs 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 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
- 239000000463 material Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 229920003087 methylethyl cellulose Polymers 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000001562 ulcerogenic effect Effects 0.000 description 1
- 239000000080 wetting agent Substances 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
-
- 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
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
jT' * * Ϊ - . ~ ..............jT '* * Ϊ -. ~ ..............
VO 3689VO 3689
Farmaceutische preparaten.Pharmaceutical preparations.
De uitvinding betreft verbeteringen bij formuleren van ontstaking remmende geneesmiddelen.The invention relates to improvements in formulation of anti-inflammatory drugs.
Systemische niet-steroide oatsteking remmende middelen, zoals acetosal, indomethacine en ibuprofen zijn bekend om hun ongewenste ne-” 5 veneffecten. In bet bijzonder is van hen bekend, dat ze ulcerogeen zijn en derhalve maagzweren kunnen veroorzaken bij orale toediening..Systemic non-steroidal anti-inflammatory agents such as acetosal, indomethacin and ibuprofen are known for their undesirable side effects. In particular, they are known to be ulcerogenic and therefore can cause gastric ulcers when administered orally.
Dit neveneffeet kan verder worden versterkt bij een combinatie met an-dere factoren, zoals stress. Aangezien bij sommige benandelingen deze verbindingen soms lange tijd moeten worden gebruikt, ktinnen deze effec-10 ten een belangrijk nadeel vormen.This side effect can be further enhanced when combined with other factors, such as stress. Since in some treatments these compounds sometimes have to be used for a long time, these effects are an important drawback.
Ranitidine is de goedgekeurde naam voor N-/' 2-/V £ 5-(dimethyl-amino) methyl_7-2-furanyl__7methyl_7thio_7ethyl-N ’ -methyl-2-nitro-l ,1-etheendiamine, dat beschreven is in de Britse octrooibeschrijving 1.565.966. Het is een sterke histamine Hg-antagonist, die kan worden ge-15 bruikt bij een behandeling van toestanden, waarbij bet gunstig is de maagzuurgraad te verlagen, speciaaJL bij maag- en darmzweren en bij het behandelen van allergische en ontstekingstoestanden, waarbij histamine ~een bekende mediator is. Er werd nu gevonden, dat mucosebeschadigingen van het maagdarmkanaal,~veroorzaakt door systemische, niet-steroide ont-20 steking remmende geneesmiddelen aanmerkelijk ktinnen worden verminderd door een gelijktijdige toediening van ranitidine.Ranitidine is the approved name for N- / '2- / V £ 5- (dimethyl-amino) methyl-7-2-furanyl-7-methyl-7thio-7-ethyl-N' -methyl-2-nitro-1,1-ethylenediamine, which is described in the British patent specification 1,565,966. It is a strong histamine Hg antagonist, which can be used in a treatment of conditions, in which it is beneficial to reduce gastric acidity, especially in gastric and duodenal ulcers and in the treatment of allergic and inflammatory conditions, where histamine is a known mediator. It has now been found that mucose damage of the gastrointestinal tract caused by systemic, non-steroidal anti-inflammatory drugs is significantly reduced by co-administration of ranitidine.
De uitvinding betreft derhalve farmaceutische preparaten met daar-in een systemisch niet-steroide ontsteking remmend middel en ranitidine of een fysiologisch geschikt zout daarvan.The invention therefore relates to pharmaceutical preparations containing a systemic non-steroidal anti-inflammatory agent and ranitidine or a physiologically suitable salt thereof.
25 In het bijzonder brtiikbaar zijn farmaceutische preparaten vol- gens de uitvinding in een vorm die geschikt is voor orale of rectale toediening.In particular, pharmaceutical compositions of the invention are in a form suitable for oral or rectal administration.
De systemische niet-steroide ontsteking remmende middelen, die bij de uitvinding worden toegepast, vertonen tevens een duidelijke anal-30 getische activiteit en omvatten b.v. acetosal, indomethacine, ibuprofen, 8203457 - 2- fenoprofen, ketoprofen, naproxen, mefenaminezuur, diflunisal, benory-laat, azapropazon, diclofenac, fenbufen, feprazon, fenclofenac, flufen-aminezuur, flu'rbiprofen, oxyfenbutazon, fenylbutazon, piroxicam, su-lindac en tolmetine. Zij kunnen in de onderhavige preparaten worden 5 toegepast in hun gebruikelijke doseringshoeveelheden b.v. 50 mg tot 1 g acetosal, 10 - 100 mg indomethacine en 100 - 500 mg ibuprofen per dose-' ringseenheid, velke een-of meermalsn per dag volgens een normale thera-pie voor het betreffende middel kan vorden toegediend.The systemic non-steroidal anti-inflammatory agents used in the invention also exhibit clear analgesic activity and include, e.g. acetosal, indomethacin, ibuprofen, 8203457 - 2-phenoprofen, ketoprofen, naproxen, mefenamic acid, diflunisal, benorylate, azapropazone, diclofenac, fenbufen, feprazone, fenclofenac, flufen-amic acid, flu'rbutazone phenyl, oxybutazone phenyl lindac and tolmetin. They can be used in the present compositions in their usual dosage amounts, e.g. 50 mg to 1 g of acetosal, 10 to 100 mg of indomethacin and 100 to 500 mg of ibuprofen per dosage unit, can be administered once or several times a day according to normal therapy for the particular agent.
Bij voorkeur vordt bet ranitidine toegepast in het preparaat in 10 de vorm van een fysiologisch geschikt zout. Dergelijke zouten omvatten zouten van anorganische of organische zuren, zoals het hydrochloride· , hydrobromide , sulfaat , acetaat , maleaat , succinaat en het fumaraat, Het hydrochloride verdient bijzondere voorkeur. De hoeveelheid ranitidine, bij voorkeur in de vorm van een fysiologisch zout, dat vordt toe-15 gepast in de onderhavige preparaten moet voldoende zijn om de maagdarm-bezvaren, veroorzaakt door de ontsteking remmende middelen, te vermin-deren en ligt bij voorkeur in het traject van 10 - 200 mg per doserings-eenheid.Preferably, the ranitidine used in the composition is in the form of a physiologically suitable salt. Such salts include salts of inorganic or organic acids, such as the hydrochloride, hydrobromide, sulfate, acetate, maleate, succinate, and the fumarate. The hydrochloride is particularly preferred. The amount of ranitidine, preferably in the form of a physiological salt, which is used in the present compositions should be sufficient to reduce the gastrointestinal problems caused by the anti-inflammatory agents and is preferably in the range of 10-200 mg per dosage unit.
De onderhavige preparaten kunnen met behulp van tenminste een 20 farmaceutische drager of excipiens vorden vervaardigd. Het preparaat kan b.v. de vorm hebben van tabletten, capsules, vouwpoeders, granules, oplossingen, stropen, suspensies of zetpillen, velke met gebruikelijke excipientia op een passende vijze vorden vervaardigd. Het preparaat kan aldus als. excipientia b.v, bevatten: bindmiddelen, tabletteerhulpmidde-25 len, vulstoffen, glijmiddelen, uiteenvalmiddelen en bevochtigingsmidde- len. Desgevenst kunnen ook andere actieve bestanddelen in dit soort preparaten aanwezig zijn. Tabletten kunnen op een gebruikelijke vijze vorden.bekleed, b.v. met een passend filmvormend materiaal, zoals me-thylcellulose, ethylcellulos.e, en/of hydroxypropylmethylcellulose, of 30 met s.uiker,The present compositions can be made using at least one pharmaceutical carrier or excipient. The preparation can e.g. in the form of tablets, capsules, folding powders, granules, solutions, syrups, suspensions or suppositories, which are prepared with suitable excipients in an appropriate manner. The preparation can thus be used as. excipients, for example, contain: binders, tableting aids, fillers, lubricants, disintegrants and wetting agents. Additionally, other active ingredients may also be present in this type of formulation. Tablets can be coated in a conventional medium, e.g. with an appropriate film-forming material, such as methyl cellulose, ethyl cellulose, and / or hydroxypropyl methyl cellulose, or with sugar,
De vloeibare preparaten kunnen tevens b.v. eetbare olien, zoals aardnotenolie, bevatten.-Zetpillen kunnen b,v, in vet oplosbare of met water mengbare bases bevatten.The liquid preparations can also e.g. contain edible oils, such as groundnut oil. Suppositories may contain, for example, fat-soluble or water-miscible bases.
De farmaceutica volgens de uitvinding kunnen volgens gebruike-35 lijke technieken die in de farmaceutische Industrie gangbaar zijn, vor- 8203457 .-3- den bereid. Zo vorden b .v. liefst het ontsteking remmende middel en het ranitidine of het ranitidinezout samen gemengd, en desgevenst voorzien van passende excipientia. Tabletten kunnen b.v. vorden vervaardigd door een dergelijk mengsel direct tot tabletten te slaan. Capsules kunnen 5 vorden .bereid door het mengsel tezamen met geschikte excipientia in gelatinecapsules af te vullen, en vel onder toepassing van een geschikte vulmachine.The pharmaceuticals of the invention can be prepared according to conventional techniques common in the pharmaceutical industry. For example, v. preferably the anti-inflammatory agent and the ranitidine or the ranitidine salt mixed together, and optionally provided with appropriate excipients. Tablets can e.g. are manufactured by directly crushing such a mixture into tablets. Capsules can be prepared by filling the mixture into gelatin capsules together with suitable excipients, and sheet using a suitable filling machine.
Ook kunnen de onderhavige preparaten in de vorm vorden gegoten van een passende vorm met geregelde afgifte, en vel zodanig dat het ra-10 nitidine of zijn zout snel voor resorptie vordt afgegeven en het niet-steroxde ontsteking remmende middel langzaam vordt vrijgesteld. De al-dus verkregen farmaceutica zijn geschikt voor orale of rectale toedie-ning en veelal gebracht in een vorm voor geregelde afgifte.Also, the present compositions may be poured into an appropriate controlled release form, and sheet such that the ra-nitidine or its salt is rapidly released for absorption and the non-steroidal anti-inflammatory agent is slowly released. The pharmaceuticals thus obtained are suitable for oral or rectal administration and often are presented in a controlled release form.
De onderhavige preparaten kunnen vorden toegepast voor het hehan-15 delen van ontstekingstoestanden, speciaal acute en chronische spier- skeletontstekingen, zoals rheumatoide en osteo-artritis alsmede an^ylosies spondylitis en bij toestanden vaarin een pijnstillend neveneffect vordt gevenst, zoals bij dysmenorrhoea, speciaal indien de toepassing van het ontsteking remmende middel vordt beperkt door maagdarm-neveneffec-20 ten.The present compositions may be used to heal inflammatory conditions, especially acute and chronic musculoskeletal infections, such as rheumatoid and osteoarthritis, as well as spondylitis and an analgesic side effect, such as dysmenorrhoea, when in conditions thereof. the use of the anti-inflammatory agent is limited by gastrointestinal side effects.
De uitvinding vordt nader toegelicht door de volgende niet beper-kende voorbeelden.The invention is further illustrated by the following nonlimiting examples.
VoOrbeeld I - Tabletten.Example I - Tablets.
(a} mg/tablet 25 ranitidine-hydrochloride l58,00x ibuprofen if-00,00 lactose 387,00 hydroxypropylmethylcellulose 5,00 natriumzetmeelglycolaat 30,00 30 magnesiumstearaat 10,00 tabletgevicht 1000,00 x equivalent met 150 mg ranitidine-base.(a} mg / tablet 25 ranitidine hydrochloride 158.00x ibuprofen if-00.00 lactose 387.00 hydroxypropylmethyl cellulose 5.00 sodium starch glycolate 30.00 30 magnesium stearate 10.00 tablet weight 1000.00 x equivalent with 150 mg ranitidine base.
Het ranitidinehydrochloride en het ibuprofen verden gezeefd door een zeef van 25Q ym en met de lactose gemengd. Dit mengsel verd gegra-35 nuleerd met een oplossing van de hydroxypropylmethylcellulose. De granu- 8203457 * - k - les verden gedroogd, gezeefd en gemengd met het natr iumzet me elglycolaat en het magnesiumstearaat. Deze van een glijmiddel voorziene granules verden tot tabletten geslagen onder toepassing van stempels van 12,5 mm.The ranitidine hydrochloride and the ibuprofen were then screened through a 25 µm screen and mixed with the lactose. This mixture is granulated with a solution of the hydroxypropylmethylcellulose. The granules 8203457 * - k - les were then dried, sieved and mixed with the sodium binder glycolate and the magnesium stearate. These lubricated granules were then beaten into tablets using 12.5 mm punches.
5 (b) mg/tablet ranitidinehydrochloride 168,00 indomethacine 50,00 microkristallijne cellulose 79,00 magnesiumstearaat 3,00 10 tabletgewi cht 300,005 (b) mg / tablet ranitidine hydrochloride 168.00 indomethacin 50.00 microcrystalline cellulose 79.00 magnesium stearate 3.00 10 tablet weight 300.00
Het ranitidinehydrochloride en het indomethacine verden gemengd met de microkristallijne cellulose en het magnesiumstearaat en tot tabletten geslagen onder toepassing van stempels van 9,5 mm.The ranitidine hydrochloride and indomethacin were then mixed with the microcrystalline cellulose and the magnesium stearate and beaten into tablets using 9.5 mm punches.
Voorbeeld II - Capsules 15 (a) mg/capsule ranitidinehydrochloride l68,00 ibuprofen 1*00,00 zetmeel 1500231 228,00Example II - Capsules 15 (a) mg / capsule ranitidine hydrochloride 168.00 ibuprofen 1 * 00.00 starch 1500 231 228.00
magnesiumstearaat U,0Qmagnesium stearate U, 0Q
20 vulgevicht 800,00 ** Een vorm van een direct tabletteerbaar zetmeel van Colorcon Ltd., Orpington, Kent.20 fillvicht 800.00 ** A form of a direct tablable starch from Colorcon Ltd., Orpington, Kent.
Het ranitidine-hydrochloride en het ibuprofen verden gezeefd door een zeef van 250 ym en met het zetmeel 1500 en het magnesiumstea-25 raat gemengd. Het verkregen mengsel verd afgevuld in harde gelatine- capsules van de grootte 0 onder toepassing van een passende vulmachine. (b) mg/capsule ranitidinehydrochloride 168,00 indomethacine 50,00 30 zetmeel 1500 80,50 magnesiumstearaat 1,50.The ranitidine hydrochloride and the ibuprofen were then screened through a 250 µm screen and mixed with the starch 1500 and the magnesium stearate. The resulting mixture was filled into size 0 hard gelatin capsules using an appropriate filling machine. (b) mg / capsule ranitidine hydrochloride 168.00 indomethacin 50.00 starch 1500 80.50 magnesium stearate 1.50.
vulgevi cht. 300,00fillfight. 300.00
Het ranitidinehydrochloride en het indomethacine verden gezeefd door een zeef van 250 ym en gemengd met het zetmeel 1500 en het magne-35 slumstearaat.The ranitidine hydrochloride and the indomethacin were then screened through a 250 µm screen and mixed with the starch 1500 and the magnesium slum stearate.
8203457 - 5 -8203457 - 5 -
Het verkregen mengsel werd afgevuld in harde gelatinecapsules van de grootte 2 onder toepassing van een passende vulmachine.The resulting mixture was filled into size 2 hard gelatin capsules using an appropriate filling machine.
82034578203457
Claims (6)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8126786 | 1981-09-04 | ||
| GB8126786 | 1981-09-04 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NL8203457A true NL8203457A (en) | 1983-04-05 |
| NL193821B NL193821B (en) | 2000-08-01 |
| NL193821C NL193821C (en) | 2000-12-04 |
Family
ID=10524316
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NL8203457A NL193821C (en) | 1981-09-04 | 1982-09-03 | Pharmaceutical preparation. |
Country Status (15)
| Country | Link |
|---|---|
| JP (1) | JPS5865215A (en) |
| AU (1) | AU564018B2 (en) |
| BE (1) | BE894285A (en) |
| CH (1) | CH652304A5 (en) |
| DE (1) | DE3232830C2 (en) |
| FR (1) | FR2512342B1 (en) |
| HK (1) | HK91387A (en) |
| IE (1) | IE54149B1 (en) |
| IT (1) | IT1208432B (en) |
| KE (1) | KE3739A (en) |
| MY (1) | MY8700560A (en) |
| NL (1) | NL193821C (en) |
| SE (1) | SE8205034L (en) |
| SG (1) | SG59387G (en) |
| ZA (1) | ZA826477B (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8516083D0 (en) * | 1985-06-25 | 1985-07-31 | Glaxo Group Ltd | Heterocyclic compounds |
| JPH01197444A (en) * | 1986-03-04 | 1989-08-09 | Bristol Myers Co | Effect of combination of beta-adrenergic agent to damage of digestive tract generated by non-steroidal anti-inflammatory composition and certain kind of histamine h1-and/or h2-receptor blocker |
| AU627775B2 (en) * | 1988-09-20 | 1992-09-03 | Glaxo Group Limited | Pharmaceutical compositions |
| EP1171161A1 (en) * | 1999-04-19 | 2002-01-16 | Richard Weisbart | Treatment of adult rheumatoid arthritis by oral administration of pooled human immunoglobulin and an antacid |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2360306A1 (en) * | 1976-08-03 | 1978-03-03 | Huguet Georgette | Analgesic and antibacterial agents - esp. for dental application contg. a salicylic acid deriv. and a nitro-furan |
| GB1565966A (en) * | 1976-08-04 | 1980-04-23 | Allen & Hanburys Ltd | Aminoalkyl furan derivatives |
-
1982
- 1982-09-02 BE BE0/208936A patent/BE894285A/en not_active IP Right Cessation
- 1982-09-03 NL NL8203457A patent/NL193821C/en not_active IP Right Cessation
- 1982-09-03 IE IE2152/82A patent/IE54149B1/en not_active IP Right Cessation
- 1982-09-03 IT IT8249071A patent/IT1208432B/en active
- 1982-09-03 FR FR8215042A patent/FR2512342B1/en not_active Expired
- 1982-09-03 ZA ZA826477A patent/ZA826477B/en unknown
- 1982-09-03 DE DE3232830A patent/DE3232830C2/en not_active Expired - Lifetime
- 1982-09-03 JP JP57153791A patent/JPS5865215A/en active Pending
- 1982-09-03 AU AU87997/82A patent/AU564018B2/en not_active Expired
- 1982-09-03 CH CH5245/82A patent/CH652304A5/en not_active IP Right Cessation
- 1982-09-03 SE SE8205034A patent/SE8205034L/en unknown
-
1987
- 1987-07-10 KE KE3739A patent/KE3739A/en unknown
- 1987-07-22 SG SG593/87A patent/SG59387G/en unknown
- 1987-12-03 HK HK913/87A patent/HK91387A/en not_active IP Right Cessation
- 1987-12-30 MY MY560/87A patent/MY8700560A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| FR2512342B1 (en) | 1986-09-05 |
| NL193821C (en) | 2000-12-04 |
| DE3232830C2 (en) | 1994-12-08 |
| JPS5865215A (en) | 1983-04-18 |
| IE822152L (en) | 1983-03-04 |
| ZA826477B (en) | 1984-04-25 |
| CH652304A5 (en) | 1985-11-15 |
| AU564018B2 (en) | 1987-07-30 |
| SE8205034D0 (en) | 1982-09-03 |
| HK91387A (en) | 1987-12-11 |
| SE8205034L (en) | 1983-03-05 |
| BE894285A (en) | 1983-03-02 |
| FR2512342A1 (en) | 1983-03-11 |
| IT8249071A0 (en) | 1982-09-03 |
| KE3739A (en) | 1987-09-04 |
| IE54149B1 (en) | 1989-07-05 |
| AU8799782A (en) | 1983-03-10 |
| SG59387G (en) | 1987-10-23 |
| IT1208432B (en) | 1989-06-12 |
| NL193821B (en) | 2000-08-01 |
| DE3232830A1 (en) | 1983-03-24 |
| MY8700560A (en) | 1987-12-31 |
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