KR890006226A - 신규 약제 및 그의 제조 방법 - Google Patents
신규 약제 및 그의 제조 방법 Download PDFInfo
- Publication number
- KR890006226A KR890006226A KR1019880013076A KR880013076A KR890006226A KR 890006226 A KR890006226 A KR 890006226A KR 1019880013076 A KR1019880013076 A KR 1019880013076A KR 880013076 A KR880013076 A KR 880013076A KR 890006226 A KR890006226 A KR 890006226A
- Authority
- KR
- South Korea
- Prior art keywords
- metoprolol
- dihydropyridine
- formulation
- castor oil
- water
- Prior art date
Links
- 239000002547 new drug Substances 0.000 title 1
- RZTAMFZIAATZDJ-HNNXBMFYSA-N 5-o-ethyl 3-o-methyl (4s)-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate Chemical group CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC(Cl)=C1Cl RZTAMFZIAATZDJ-HNNXBMFYSA-N 0.000 claims description 2
- 229960003580 felodipine Drugs 0.000 claims description 2
- 229960002237 metoprolol Drugs 0.000 claims 10
- IUBSYMUCCVWXPE-UHFFFAOYSA-N metoprolol Chemical compound COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 IUBSYMUCCVWXPE-UHFFFAOYSA-N 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 10
- YNGDWRXWKFWCJY-UHFFFAOYSA-N 1,4-Dihydropyridine Chemical compound C1C=CNC=C1 YNGDWRXWKFWCJY-UHFFFAOYSA-N 0.000 claims 9
- 238000009472 formulation Methods 0.000 claims 8
- 239000011324 bead Substances 0.000 claims 4
- 239000004359 castor oil Substances 0.000 claims 4
- 235000019438 castor oil Nutrition 0.000 claims 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- WSWCOQWTEOXDQX-MQQKCMAXSA-M (E,E)-sorbate Chemical group C\C=C\C=C\C([O-])=O WSWCOQWTEOXDQX-MQQKCMAXSA-M 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 239000011159 matrix material Substances 0.000 claims 2
- 239000012528 membrane Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 241000894007 species Species 0.000 claims 2
- 230000008961 swelling Effects 0.000 claims 2
- 229920003176 water-insoluble polymer Polymers 0.000 claims 2
- 108090000312 Calcium Channels Proteins 0.000 claims 1
- 102000003922 Calcium Channels Human genes 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- RGHAZVBIOOEVQX-UHFFFAOYSA-N Metoprolol succinate Chemical class OC(=O)CCC(O)=O.COCCC1=CC=C(OCC(O)CNC(C)C)C=C1.COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 RGHAZVBIOOEVQX-UHFFFAOYSA-N 0.000 claims 1
- 241000047703 Nonion Species 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 239000003405 delayed action preparation Substances 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- 150000002148 esters Chemical group 0.000 claims 1
- 125000005313 fatty acid group Polymers 0.000 claims 1
- 150000002314 glycerols Chemical class 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 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 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229960001597 nifedipine Drugs 0.000 claims 1
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical group COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 claims 1
- 239000008389 polyethoxylated castor oil Substances 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical group OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 1
- 230000002459 sustained effect Effects 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 건가안 피실험자에 단일 투여량을 투여한 후 혈장에서 펠로디핀의 평균 농도를 나타낸 그래프임.
Claims (11)
- 메토프롤롤을, 가용성 주성분으로서 수불용성 중합체막으로 피복시킨 메토프롤롤의 염을 함유하는 소형 비드의 형태에 포함시키고, 디히드로피리딘을 비이온계 가용화제 중에 분산시킴으로써, 분산된 디히드로피리딘과 메토프롤롤을 함유하는 비드를 모두 물과 접촉하여 팽윤겔을 형성하는 매트릭스에 혼입시키는 것을 특징으로 하는, 메토프롤롤 및 디히드로피리딘 종류의 불충분한 수용성 칼슘 통로 차단계의 배합물을 함유하는 1일 1회 투여용 지속제 제제.
- 제1항에 있어서, 비이온계 가용화제가 폴리에톡실화피마자유, 폴리에톡실화 수소 첨가 피마자유, 피마자유에서 얻은 폴리에톡실화 지방산 또는 첨가 피마자유에서 얻은 폴리에톡실화 지방산 군 중에서 선택된 것을 특징으로 하는 제제.
- 제1항에 있어서, 비이온계 가용화제가 수소 첨가피마자유 지방산과 옥시에틸화 글리세린과의 에스테르인 것을 특징으로 하는 제제.
- 제1항에 있어서, 디히드로피리딘이 펠로디핀인 것을 특징으로 하는 제제.
- 제1항에 있어서, 디히드로피리딘이 니페디핀인 것을 특징으로 하는 제제.
- 제1항에 있어서, 겔-형성 매트릭스가 히드록시프로필 메틸셀룰로오스를 함유하는 것을 특징으로 하는 제제.
- 제1항에 있어서, 메토프롤롤이 그의 숙신산염 형태인 것을 특징으로 하는 제제.
- 제1항에 있어서, 디히드로피리딘의 2.5mg 내지 80mg 사이에서 변화시키고, 메토프롤롤 숙신산염 라세미체의 양을 40mg 내지 200mg 사이에서 변화시키는 것을 특징으로 하는 제제.
- 제1항에 있어서, 메토프롤롤이 S-에난티오머의소르브산염 형태이며, 양을 25mg 내지 120mg 사이에서 변화시키는 것을 특징으로 하는 제제.
- 제1항에 있어서, 메토프롤롤이 메토프롤로의 S-에난티오머의 벤조산염 또는 소르브산염 형태인 것을 특징으로 하는 제제.
- 메토프롤롤을, 가용성 주성분으로서 메토프롤로의 염을 함유하는 소형 비드의 형태에 포함시키고, 이 비드를 양성자 전이기가 없는 셀룰로오스의 유도체를 함유하는, 수불용성 중합체 막으로 분무 피복시키고, 디히드로 피리딘을 비이온계 가용화제 중에 분산시킨 후, 비드와 디히드로피리딘을 모두 물과 접촉하여 팽윤 겔을 형성하는 매트릭스에 혼입시키는 것을 특징으로 하는, 케토프롤롤 및 디히드로피리딘 종류의 불충분한 수용성 칼슘 통로 차단제의 배합물을 함유하는 지속성 제제의 제조방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE8703881-6 | 1987-10-08 | ||
SE8703881A SE8703881D0 (sv) | 1987-10-08 | 1987-10-08 | New pharmaceutical preparation |
Publications (2)
Publication Number | Publication Date |
---|---|
KR890006226A true KR890006226A (ko) | 1989-06-12 |
KR960009411B1 KR960009411B1 (en) | 1996-07-19 |
Family
ID=20369795
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR88013076A KR960009411B1 (en) | 1987-10-08 | 1988-10-07 | Controlled release preparation containing metoprolol and dihydropyridine |
Country Status (26)
Country | Link |
---|---|
US (1) | US4942040A (ko) |
EP (1) | EP0311582B1 (ko) |
JP (1) | JP2619936B2 (ko) |
KR (1) | KR960009411B1 (ko) |
CN (1) | CN1029935C (ko) |
AT (1) | ATE84412T1 (ko) |
AU (1) | AU615211B2 (ko) |
CA (1) | CA1312286C (ko) |
CY (1) | CY1896A (ko) |
DE (1) | DE3877492T2 (ko) |
DK (1) | DK175085B1 (ko) |
ES (1) | ES2053815T3 (ko) |
FI (1) | FI92903C (ko) |
GR (1) | GR3006788T3 (ko) |
HK (1) | HK6296A (ko) |
HU (1) | HU210461A9 (ko) |
IE (1) | IE63084B1 (ko) |
IL (1) | IL87922A (ko) |
IS (1) | IS1584B (ko) |
MX (1) | MX169243B (ko) |
MY (1) | MY104065A (ko) |
NO (1) | NO177375C (ko) |
NZ (1) | NZ226245A (ko) |
PH (1) | PH25568A (ko) |
PT (1) | PT88711B (ko) |
SE (1) | SE8703881D0 (ko) |
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US5834496A (en) * | 1991-12-02 | 1998-11-10 | Sepracor, Inc. | Methods for treating hypertension using optically pure S(-) felodipine |
IL104192A (en) * | 1992-02-17 | 1998-01-04 | Siegfried Ag Pharma | Pharmaceutical dosage forms having prolonged release rate of zero order of the active ingredient |
US6726930B1 (en) | 1993-09-09 | 2004-04-27 | Penwest Pharmaceuticals Co. | Sustained release heterodisperse hydrogel systems for insoluble drugs |
US5662933A (en) * | 1993-09-09 | 1997-09-02 | Edward Mendell Co., Inc. | Controlled release formulation (albuterol) |
US5773025A (en) | 1993-09-09 | 1998-06-30 | Edward Mendell Co., Inc. | Sustained release heterodisperse hydrogel systems--amorphous drugs |
US5455046A (en) * | 1993-09-09 | 1995-10-03 | Edward Mendell Co., Inc. | Sustained release heterodisperse hydrogel systems for insoluble drugs |
US6080428A (en) | 1993-09-20 | 2000-06-27 | Bova; David J. | Nicotinic acid compositions for treating hyperlipidemia and related methods therefor |
US6746691B2 (en) | 1993-09-20 | 2004-06-08 | Kos Pharmaceuticals, Inc. | Intermediate release nicotinic acid compositions for treating hyperlipidemia having unique biopharmaceutical characteristics |
US6676967B1 (en) | 1993-09-20 | 2004-01-13 | Kos Pharmaceuticals, Inc. | Methods for reducing flushing in individuals being treated with nicotinic acid for hyperlipidemia |
US6129930A (en) | 1993-09-20 | 2000-10-10 | Bova; David J. | Methods and sustained release nicotinic acid compositions for treating hyperlipidemia at night |
US6818229B1 (en) | 1993-09-20 | 2004-11-16 | Kos Pharmaceuticals, Inc. | Intermediate release nicotinic acid compositions for treating hyperlipidemia |
US5399358A (en) * | 1993-11-12 | 1995-03-21 | Edward Mendell Co., Inc. | Sustained release formulations for 24 hour release of metroprolol |
US5399359A (en) * | 1994-03-04 | 1995-03-21 | Edward Mendell Co., Inc. | Controlled release oxybutynin formulations |
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MX9801835A (es) | 1996-07-08 | 1998-08-30 | Mendell Co Inc Edward | Matriz de liberacion sostenida para medicamentos insolubles de dosis altas. |
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ATE526950T1 (de) | 1999-10-29 | 2011-10-15 | Euro Celtique Sa | Hydrocodon-formulierungen mit gesteuerter freisetzung |
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CZ301790B6 (cs) * | 2000-04-11 | 2010-06-23 | Sankyo Company Limited | Farmaceutický prípravek obsahující blokátor vápníku |
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-
1987
- 1987-10-08 SE SE8703881A patent/SE8703881D0/xx unknown
-
1988
- 1988-09-16 AU AU22374/88A patent/AU615211B2/en not_active Expired
- 1988-09-20 NZ NZ226245A patent/NZ226245A/xx unknown
- 1988-09-22 ES ES88850319T patent/ES2053815T3/es not_active Expired - Lifetime
- 1988-09-22 DE DE8888850319T patent/DE3877492T2/de not_active Expired - Lifetime
- 1988-09-22 EP EP88850319A patent/EP0311582B1/en not_active Expired - Lifetime
- 1988-09-22 AT AT88850319T patent/ATE84412T1/de not_active IP Right Cessation
- 1988-09-27 NO NO884269A patent/NO177375C/no not_active IP Right Cessation
- 1988-09-27 IE IE292188A patent/IE63084B1/en not_active IP Right Cessation
- 1988-09-29 PH PH37615A patent/PH25568A/en unknown
- 1988-09-29 US US07/250,945 patent/US4942040A/en not_active Expired - Lifetime
- 1988-10-05 IL IL87922A patent/IL87922A/xx active Protection Beyond IP Right Term
- 1988-10-06 MX MX013316A patent/MX169243B/es unknown
- 1988-10-06 IS IS3398A patent/IS1584B/is unknown
- 1988-10-06 MY MYPI88001120A patent/MY104065A/en unknown
- 1988-10-06 DK DK198805586A patent/DK175085B1/da active
- 1988-10-07 CA CA000579566A patent/CA1312286C/en not_active Expired - Lifetime
- 1988-10-07 FI FI884636A patent/FI92903C/fi not_active IP Right Cessation
- 1988-10-07 KR KR88013076A patent/KR960009411B1/ko not_active IP Right Cessation
- 1988-10-07 JP JP63252209A patent/JP2619936B2/ja not_active Expired - Lifetime
- 1988-10-07 PT PT88711A patent/PT88711B/pt not_active IP Right Cessation
- 1988-10-08 CN CN88109129A patent/CN1029935C/zh not_active Expired - Lifetime
-
1993
- 1993-01-14 GR GR930400002T patent/GR3006788T3/el unknown
-
1994
- 1994-12-15 HU HU94P/P00056P patent/HU210461A9/hu unknown
-
1996
- 1996-01-11 HK HK6296A patent/HK6296A/xx not_active IP Right Cessation
- 1996-09-27 CY CY189696A patent/CY1896A/xx unknown
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