DE3005029A1 - Antihypertensive pharmazeutische zubereitungen - Google Patents
Antihypertensive pharmazeutische zubereitungenInfo
- Publication number
- DE3005029A1 DE3005029A1 DE19803005029 DE3005029A DE3005029A1 DE 3005029 A1 DE3005029 A1 DE 3005029A1 DE 19803005029 DE19803005029 DE 19803005029 DE 3005029 A DE3005029 A DE 3005029A DE 3005029 A1 DE3005029 A1 DE 3005029A1
- Authority
- DE
- Germany
- Prior art keywords
- pharmaceutical preparations
- active ingredients
- preparations according
- active ingredient
- endralazine
- 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.)
- Granted
Links
- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 21
- 230000003276 anti-hypertensive effect Effects 0.000 title claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 44
- ALAXZYHFVBSJKZ-UHFFFAOYSA-N endralazine Chemical compound C1CC=2N=NC(NN)=CC=2CN1C(=O)C1=CC=CC=C1 ALAXZYHFVBSJKZ-UHFFFAOYSA-N 0.000 claims description 13
- 229960002029 endralazine Drugs 0.000 claims description 13
- 230000000054 salidiuretic effect Effects 0.000 claims description 13
- 206010020772 Hypertension Diseases 0.000 claims description 12
- 229960002508 pindolol Drugs 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 10
- LBXHRAWDUMTPSE-AOOOYVTPSA-N 4-chloro-N-[(2S,6R)-2,6-dimethyl-1-piperidinyl]-3-sulfamoylbenzamide Chemical compound C[C@H]1CCC[C@@H](C)N1NC(=O)C1=CC=C(Cl)C(S(N)(=O)=O)=C1 LBXHRAWDUMTPSE-AOOOYVTPSA-N 0.000 claims description 9
- 229960004070 clopamide Drugs 0.000 claims description 9
- 238000002360 preparation method Methods 0.000 claims description 8
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims description 7
- 229960002003 hydrochlorothiazide Drugs 0.000 claims description 7
- AQCHWTWZEMGIFD-UHFFFAOYSA-N metolazone Chemical compound CC1NC2=CC(Cl)=C(S(N)(=O)=O)C=C2C(=O)N1C1=CC=CC=C1C AQCHWTWZEMGIFD-UHFFFAOYSA-N 0.000 claims description 6
- 229960002817 metolazone Drugs 0.000 claims description 6
- 150000003839 salts Chemical group 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- PHUTUTUABXHXLW-UHFFFAOYSA-N pindolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=NC=C[C]12 PHUTUTUABXHXLW-UHFFFAOYSA-N 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 description 11
- JZQKKSLKJUAGIC-UHFFFAOYSA-N pindolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=C1C=CN2 JZQKKSLKJUAGIC-UHFFFAOYSA-N 0.000 description 11
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 239000003826 tablet Substances 0.000 description 7
- 229920002261 Corn starch Polymers 0.000 description 6
- 239000008120 corn starch Substances 0.000 description 6
- 229940099112 cornstarch Drugs 0.000 description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Chemical compound 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
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 239000002253 acid Substances 0.000 description 3
- 239000002220 antihypertensive agent Substances 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- SSEAPVMQZPKNQZ-UHFFFAOYSA-N 2-(aminomethyl)-4-tert-butyl-6-iodophenol Chemical compound CC(C)(C)C1=CC(I)=C(O)C(CN)=C1 SSEAPVMQZPKNQZ-UHFFFAOYSA-N 0.000 description 2
- CPLXHLVBOLITMK-UHFFFAOYSA-N Magnesium oxide Chemical compound [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- 206010030113 Oedema Diseases 0.000 description 2
- 229940030600 antihypertensive agent Drugs 0.000 description 2
- 102000015005 beta-adrenergic receptor activity proteins Human genes 0.000 description 2
- 108040006818 beta-adrenergic receptor activity proteins Proteins 0.000 description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000012458 free base Substances 0.000 description 2
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 230000001631 hypertensive effect Effects 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000002093 peripheral effect Effects 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 235000012239 silicon dioxide Nutrition 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- WCOXQTXVACYMLM-UHFFFAOYSA-N 2,3-bis(12-hydroxyoctadecanoyloxy)propyl 12-hydroxyoctadecanoate Chemical class CCCCCCC(O)CCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCC(O)CCCCCC)COC(=O)CCCCCCCCCCC(O)CCCCCC WCOXQTXVACYMLM-UHFFFAOYSA-N 0.000 description 1
- JBMKAUGHUNFTOL-UHFFFAOYSA-N Aldoclor Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NC=NS2(=O)=O JBMKAUGHUNFTOL-UHFFFAOYSA-N 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 208000001871 Tachycardia Diseases 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 229940127088 antihypertensive drug Drugs 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- BFAKENXZKHGIGE-UHFFFAOYSA-N bis(2,3,5,6-tetrafluoro-4-iodophenyl)diazene Chemical compound FC1=C(C(=C(C(=C1F)I)F)F)N=NC1=C(C(=C(C(=C1F)F)I)F)F BFAKENXZKHGIGE-UHFFFAOYSA-N 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 229960001523 chlortalidone Drugs 0.000 description 1
- JIVPVXMEBJLZRO-UHFFFAOYSA-N chlorthalidone Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C2(O)C3=CC=CC=C3C(=O)N2)=C1 JIVPVXMEBJLZRO-UHFFFAOYSA-N 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- -1 fumaric Chemical compound 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- DMDGGSIALPNSEE-UHFFFAOYSA-N hydroflumethiazide Chemical compound C1=C(C(F)(F)F)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O DMDGGSIALPNSEE-UHFFFAOYSA-N 0.000 description 1
- 229960003313 hydroflumethiazide Drugs 0.000 description 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 description 1
- IXCSERBJSXMMFS-UHFFFAOYSA-N hydrogen chloride Substances Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- 150000002689 maleic acids Chemical class 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 239000000810 peripheral vasodilating agent Substances 0.000 description 1
- 229960002116 peripheral vasodilator Drugs 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid group Chemical group S(O)(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- 239000007939 sustained release tablet Substances 0.000 description 1
- 230000006794 tachycardia Effects 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- LMJSLTNSBFUCMU-UHFFFAOYSA-N trichlormethiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NC(C(Cl)Cl)NS2(=O)=O LMJSLTNSBFUCMU-UHFFFAOYSA-N 0.000 description 1
- 229960004813 trichlormethiazide Drugs 0.000 description 1
- 230000000304 vasodilatating effect Effects 0.000 description 1
- 230000024883 vasodilation Effects 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—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
-
- 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
- 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)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH178579A CH643457A5 (de) | 1979-02-22 | 1979-02-22 | Pharmazeutische praeparate zur behandlung der hypertonie. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE3005029A1 true DE3005029A1 (de) | 1980-09-04 |
| DE3005029C2 DE3005029C2 (he) | 1987-02-12 |
Family
ID=4218544
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19803005029 Granted DE3005029A1 (de) | 1979-02-22 | 1980-02-11 | Antihypertensive pharmazeutische zubereitungen |
Country Status (20)
| Country | Link |
|---|---|
| JP (1) | JPS55115823A (he) |
| AT (1) | AT378915B (he) |
| AU (1) | AU538599B2 (he) |
| BE (1) | BE881763A (he) |
| CA (1) | CA1147657A (he) |
| CH (1) | CH643457A5 (he) |
| DE (1) | DE3005029A1 (he) |
| FR (1) | FR2449450A1 (he) |
| GB (1) | GB2044101B (he) |
| HU (1) | HU187271B (he) |
| IE (1) | IE49073B1 (he) |
| IL (1) | IL59432A (he) |
| IT (1) | IT1145433B (he) |
| MY (1) | MY8500619A (he) |
| NL (1) | NL8001000A (he) |
| NZ (1) | NZ192924A (he) |
| PH (1) | PH17118A (he) |
| PT (1) | PT70855A (he) |
| SE (2) | SE8001121L (he) |
| ZA (1) | ZA801018B (he) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2537434A1 (fr) * | 1982-12-09 | 1984-06-15 | Sandoz Sa | Composition pharmaceutique d'endralazine sous forme retard |
| GB2367242B (en) * | 2000-09-21 | 2004-07-28 | Henderson Morley Res & Dev Ltd | Antiviral treatment |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2458155A1 (de) * | 1973-12-19 | 1975-07-03 | Sandoz Ag | Neue pharmazeutische praeparate |
-
1979
- 1979-02-22 CH CH178579A patent/CH643457A5/de not_active IP Right Cessation
-
1980
- 1980-02-11 DE DE19803005029 patent/DE3005029A1/de active Granted
- 1980-02-13 SE SE8001121A patent/SE8001121L/ not_active Application Discontinuation
- 1980-02-15 GB GB8005245A patent/GB2044101B/en not_active Expired
- 1980-02-18 BE BE1/9727A patent/BE881763A/fr not_active IP Right Cessation
- 1980-02-19 NL NL8001000A patent/NL8001000A/nl not_active Application Discontinuation
- 1980-02-20 IL IL59432A patent/IL59432A/xx unknown
- 1980-02-20 CA CA000346083A patent/CA1147657A/en not_active Expired
- 1980-02-20 AU AU55742/80A patent/AU538599B2/en not_active Ceased
- 1980-02-20 PT PT70855A patent/PT70855A/pt unknown
- 1980-02-20 FR FR8003669A patent/FR2449450A1/fr active Granted
- 1980-02-20 IE IE336/80A patent/IE49073B1/en unknown
- 1980-02-20 NZ NZ192924A patent/NZ192924A/en unknown
- 1980-02-20 IT IT47950/80A patent/IT1145433B/it active
- 1980-02-21 HU HU80402A patent/HU187271B/hu unknown
- 1980-02-21 PH PH23672A patent/PH17118A/en unknown
- 1980-02-21 JP JP1980480A patent/JPS55115823A/ja active Pending
- 1980-02-21 AT AT0095580A patent/AT378915B/de not_active IP Right Cessation
- 1980-02-22 ZA ZA00801018A patent/ZA801018B/xx unknown
-
1982
- 1982-04-15 SE SE8202357A patent/SE8202357L/xx not_active Application Discontinuation
-
1985
- 1985-12-30 MY MY619/85A patent/MY8500619A/xx unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2458155A1 (de) * | 1973-12-19 | 1975-07-03 | Sandoz Ag | Neue pharmazeutische praeparate |
Non-Patent Citations (2)
| Title |
|---|
| Helwig, B.: Moderne Arzneimittel, 4. Aufl., S. 912-913, 1972 * |
| Rote Liste Nr. 16087 u. 16090, 1977/78 * |
Also Published As
| Publication number | Publication date |
|---|---|
| ATA95580A (de) | 1985-03-15 |
| CH643457A5 (de) | 1984-06-15 |
| AT378915B (de) | 1985-10-25 |
| NL8001000A (nl) | 1980-08-26 |
| SE8001121L (sv) | 1980-08-23 |
| MY8500619A (en) | 1985-12-31 |
| SE8202357L (en) | 1982-04-15 |
| HU187271B (en) | 1985-12-28 |
| GB2044101A (en) | 1980-10-15 |
| JPS55115823A (en) | 1980-09-06 |
| ZA801018B (en) | 1981-09-30 |
| AU5574280A (en) | 1980-08-28 |
| IT8047950A0 (it) | 1980-02-20 |
| NZ192924A (en) | 1984-05-31 |
| IE800336L (en) | 1980-08-22 |
| IT1145433B (it) | 1986-11-05 |
| FR2449450B1 (he) | 1983-07-22 |
| IE49073B1 (en) | 1985-07-24 |
| PH17118A (en) | 1984-06-01 |
| DE3005029C2 (he) | 1987-02-12 |
| GB2044101B (en) | 1983-09-07 |
| AU538599B2 (en) | 1984-08-23 |
| CA1147657A (en) | 1983-06-07 |
| FR2449450A1 (fr) | 1980-09-19 |
| PT70855A (fr) | 1980-03-01 |
| BE881763A (fr) | 1980-08-18 |
| IL59432A0 (en) | 1980-05-30 |
| IL59432A (en) | 1984-08-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8110 | Request for examination paragraph 44 | ||
| 8125 | Change of the main classification |
Ipc: A61K 31/50 |
|
| D2 | Grant after examination | ||
| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |