FI88872B - Foerfarande foer framstaellning av sferoider, som aostadkommer laongvarig foerdroejd frigoering av en som kalciumkanalblockerare anvaend dihydropyridin - Google Patents
Foerfarande foer framstaellning av sferoider, som aostadkommer laongvarig foerdroejd frigoering av en som kalciumkanalblockerare anvaend dihydropyridin Download PDFInfo
- Publication number
- FI88872B FI88872B FI870380A FI870380A FI88872B FI 88872 B FI88872 B FI 88872B FI 870380 A FI870380 A FI 870380A FI 870380 A FI870380 A FI 870380A FI 88872 B FI88872 B FI 88872B
- Authority
- FI
- Finland
- Prior art keywords
- alkyl
- spheroids
- calcium channel
- acting
- long
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/82—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
-
- 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)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Claims (6)
1. Förfarande för framställning av sferoider, som ästadkommer längvarig fördröjd frigöring av en terapeu- 5 tiskt effektiv mängd av en som kalciumkanalblockerare an-vänd dihydropyridin, kännetecknat därav, att a) man bildar en väsentligen vattenhaltig vät massa, som innehäller en effektiv mängd av kalciumkanal-blockeraren tillsammans med ett pH-beroende bindemedel, 10 som är mindre lösligt i lägre pH-värden och mera lösligt i högre pH-värden, varvid bindemedlet utgör ätminstone 3 vikt-% av mängden av torra komponenter i massan; b) den väta massan strängpressas, varvid det bildas stängformade väsentligen cylindriska stycken med en diame- 15 ter av högst 1,2 mm; c) de stängformade styckena formas till sferoider; och d) sferoiderna torkas för bildning av sferoider, i vilka förhällandet mellan ytradie och omkretsradie är mel- 20 lan 0,85 - 1,0.
2. Förfarande enligt patentkravet 1, kännetecknat därav, att sferoiderna formas pä en rote-rande skiva eller panna.
3. Förfarande enligt patentkravet 1, k ä n n e - 25 tecknat därav, att det pH-beroende bindemedlet är ett enkelt material eller en blandning av material valda ur grupperna a och b, som omfattar; a) ftalsyraderivat av vinylpolymerer och -sampoly-merer, hydroxialkylcellulosa, alkylcellulosa, cellulosa- 30 acetat, hydroxialkylcellulosaacetat, cellulosaetrar, al- kylcellulosaacetat och partiella estrar av dessa; och b) polymerer och sampolymerer av lägre alkylakryl-syror och lägre alkylakrylat och partiella estrar av dessa. 35
4. Förfarande enligt patentkravet 3, känne tecknat därav, att det pH-beroende bindemedlet är 4i 888 7? en sampolymer av metakrylsyra och en metakrylsyra- eller akrylsyraester.
5. Förfarande enligt patentkravet 1, känne- t e c k n a t därav, att som kalciumkanalblockerare an-5 vänds en dihydropyridin med formeln (ö)~h
0 AA 0 10 ε,ΑΑΛ 0R^ (il (Γ J A E, CH3 O 15 i vilken R3 är -N02, -CF3 eller en halogen; R2 är en alkyl eller -CH2CH2OCH3; R6 är väte eller en alkyl; och
20 R3 är en alkyl, alkylenyloxialkyl, halogenalkyl, substitue-rad eller leke substltuerad fenylalkyl, substituerad eller leke substituerad naftylalkyl, eller /R* -AN^ , vilken \ 25 R5 A är en alkylen; R4 är en alkyl, alkoxi eller en substituerad eller icke substituerad fenyl eller en substituerad eller icke subs-30 tituerad fenylalkyl; och R5 är väte eller en alkyl; eller ett farmaceutiskt godtagbart sait av denna.
6. Förfarande enligt patentkravet 5, känne- t e c k n a t därav, att den som kalciumkanalblockerare . 35 aktiva dihydropyridinen är nikardipin eller ett farmaceu tiskt godtagbart sait av denna.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82389686A | 1986-01-30 | 1986-01-30 | |
| US82389686 | 1986-01-30 | ||
| US94087886A | 1986-12-10 | 1986-12-10 | |
| US94087886 | 1986-12-10 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| FI870380A0 FI870380A0 (fi) | 1987-01-29 |
| FI870380A FI870380A (fi) | 1987-07-31 |
| FI88872B true FI88872B (fi) | 1993-04-15 |
| FI88872C FI88872C (sv) | 1993-07-26 |
Family
ID=27124769
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI870380A FI88872C (sv) | 1986-01-30 | 1987-01-29 | Förfarande för framställning av sferoider, som åstadkommer långvarig f ördröjd frigöring av en som kalciumkanalblockerare använd dihydropyrid in |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP0231026B1 (sv) |
| JP (1) | JP2524990B2 (sv) |
| KR (1) | KR900005009B1 (sv) |
| AU (1) | AU604672B2 (sv) |
| CA (1) | CA1285227C (sv) |
| DE (1) | DE3782439T2 (sv) |
| DK (1) | DK175216B1 (sv) |
| ES (1) | ES2052500T3 (sv) |
| FI (1) | FI88872C (sv) |
| GR (1) | GR3006148T3 (sv) |
| HU (1) | HU196709B (sv) |
| IE (1) | IE61879B1 (sv) |
| IL (2) | IL81419A0 (sv) |
| IT (1) | IT1206876B (sv) |
| NO (1) | NO174325C (sv) |
| NZ (1) | NZ219090A (sv) |
| PH (1) | PH26366A (sv) |
| PT (1) | PT84213B (sv) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4940556A (en) * | 1986-01-30 | 1990-07-10 | Syntex (U.S.A.) Inc. | Method of preparing long acting formulation |
| IE63321B1 (en) * | 1986-02-03 | 1995-04-05 | Elan Corp Plc | Drug delivery system |
| JP2804048B2 (ja) * | 1987-09-11 | 1998-09-24 | イー・アール・スクイブ・アンド・サンズ・インコーポレイテッド | 高薬物含量医薬組成物およびその製造法 |
| JP2528706B2 (ja) * | 1988-05-30 | 1996-08-28 | ゼリア新薬工業株式会社 | ジヒドロピリジン化合物の製剤組成物 |
| US4925676A (en) * | 1989-02-02 | 1990-05-15 | Warner-Lambert Company | Extended release gemfibrozil composition |
| HU203041B (en) * | 1989-03-14 | 1991-05-28 | Egyt Gyogyszervegyeszeti Gyar | Process for producing pharmaceutical compositions of controlled releasing factor containing nifedipin |
| JPH0729926B2 (ja) * | 1989-07-25 | 1995-04-05 | 大塚製薬株式会社 | 易吸収性製剤用組成物 |
| DE69231499T2 (de) * | 1991-12-30 | 2001-05-03 | Fmc Corp | Zusammensetzung auf der basis von mikrokristalliner zellulose für die herstellung von kugelförmigen teilchen |
| GB9203689D0 (en) * | 1992-02-20 | 1992-04-08 | Euro Celtique Sa | Pharmaceutical composition |
| DE69311394T2 (de) * | 1992-02-20 | 1997-10-30 | Euro Celtique Sa | Arzneimittel verzögerter Wirkstoffabgabe |
| HRP970485A2 (en) * | 1996-09-13 | 1998-08-31 | Joerg Rosenberg | Process for producing solid pharmaceutical forms |
| US6303607B1 (en) * | 1998-09-10 | 2001-10-16 | Cv Therapeutics, Inc. | Method for administering a sustained release ranolanolazine formulation |
| US6479496B1 (en) * | 1998-09-10 | 2002-11-12 | Cv Therapeutics, Inc. | Methods for treating angina with ranolazine |
| DE60039377D1 (de) | 1999-02-09 | 2008-08-21 | Pfizer Prod Inc | Zusammensetzungen basischer Arzneistoffe mit verbesserter Bioverfügbarkeit |
| US20090208579A1 (en) * | 2004-12-27 | 2009-08-20 | Eisai R & D Management Co., Ltd. | Matrix Type Sustained-Release Preparation Containing Basic Drug or Salt Thereof, and Method for Manufacturing the Same |
| RU2401125C2 (ru) | 2004-12-27 | 2010-10-10 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Способ стабилизации лекарственного средства против деменции |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE795766A (fr) * | 1972-02-22 | 1973-08-22 | Lilly Co Eli | Particules de napsylate de propoxyphene retard et procede de fabrication de ces particules |
| JPS5846019A (ja) * | 1981-09-14 | 1983-03-17 | Kanebo Ltd | 持続性ニフエジピン製剤 |
| FR2581541B1 (fr) * | 1985-05-09 | 1988-05-20 | Rhone Poulenc Sante | Nouvelles compositions pharmaceutiques permettant la liberation prolongee d'un principe actif et leur procede de preparation |
-
1986
- 1986-01-29 IL IL81419A patent/IL81419A0/xx unknown
-
1987
- 1987-01-26 PH PH34763A patent/PH26366A/en unknown
- 1987-01-26 CA CA000528174A patent/CA1285227C/en not_active Expired - Lifetime
- 1987-01-28 KR KR1019870000682A patent/KR900005009B1/ko not_active IP Right Cessation
- 1987-01-29 IL IL81419A patent/IL81419A/xx not_active IP Right Cessation
- 1987-01-29 NO NO870368A patent/NO174325C/no unknown
- 1987-01-29 NZ NZ219090A patent/NZ219090A/en unknown
- 1987-01-29 ES ES87101203T patent/ES2052500T3/es not_active Expired - Lifetime
- 1987-01-29 FI FI870380A patent/FI88872C/sv not_active IP Right Cessation
- 1987-01-29 DE DE8787101203T patent/DE3782439T2/de not_active Expired - Lifetime
- 1987-01-29 EP EP87101203A patent/EP0231026B1/en not_active Expired - Lifetime
- 1987-01-29 IT IT8767057A patent/IT1206876B/it active
- 1987-01-29 DK DK198700477A patent/DK175216B1/da not_active IP Right Cessation
- 1987-01-29 AU AU68102/87A patent/AU604672B2/en not_active Expired
- 1987-01-29 HU HU87274A patent/HU196709B/hu unknown
- 1987-01-29 IE IE22987A patent/IE61879B1/en not_active IP Right Cessation
- 1987-01-29 PT PT84213A patent/PT84213B/pt unknown
- 1987-01-29 JP JP62021668A patent/JP2524990B2/ja not_active Expired - Lifetime
-
1992
- 1992-11-05 GR GR920401768T patent/GR3006148T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL81419A (en) | 1991-07-18 |
| NO870368L (no) | 1987-07-31 |
| NO174325B (no) | 1994-01-10 |
| DK47787D0 (da) | 1987-01-29 |
| EP0231026A1 (en) | 1987-08-05 |
| JPS62252732A (ja) | 1987-11-04 |
| PH26366A (en) | 1992-06-01 |
| PT84213A (en) | 1987-02-01 |
| EP0231026B1 (en) | 1992-11-04 |
| IL81419A0 (en) | 1987-08-31 |
| FI88872C (sv) | 1993-07-26 |
| DE3782439T2 (de) | 1993-05-19 |
| PT84213B (pt) | 1989-03-30 |
| KR870007121A (ko) | 1987-08-17 |
| IT8767057A0 (it) | 1987-01-29 |
| IE870229L (en) | 1987-07-30 |
| IT1206876B (it) | 1989-05-11 |
| HUT42950A (en) | 1987-09-28 |
| DK47787A (da) | 1987-07-31 |
| NO174325C (no) | 1994-04-20 |
| HU196709B (en) | 1989-01-30 |
| DK175216B1 (da) | 2004-07-12 |
| JP2524990B2 (ja) | 1996-08-14 |
| KR900005009B1 (ko) | 1990-07-16 |
| GR3006148T3 (sv) | 1993-06-21 |
| NO870368D0 (no) | 1987-01-29 |
| FI870380A0 (fi) | 1987-01-29 |
| ES2052500T3 (es) | 1994-07-16 |
| FI870380A (fi) | 1987-07-31 |
| DE3782439D1 (de) | 1992-12-10 |
| NZ219090A (en) | 1990-04-26 |
| AU604672B2 (en) | 1991-01-03 |
| CA1285227C (en) | 1991-06-25 |
| IE61879B1 (en) | 1994-11-30 |
| AU6810287A (en) | 1987-08-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| BB | Publication of examined application | ||
| FD | Application lapsed | ||
| FG | Patent granted |
Owner name: SYNTEX (U.S.A.) INC. |
|
| MA | Patent expired |