HRP20140476T1 - Stabilni oblik amorfnih soli perindoprila, postupak njihove pripreme, posebno industrijske pripreme i njihova uporaba u lijeäśenju hipertenzije - Google Patents
Stabilni oblik amorfnih soli perindoprila, postupak njihove pripreme, posebno industrijske pripreme i njihova uporaba u lijeäśenju hipertenzije Download PDFInfo
- Publication number
- HRP20140476T1 HRP20140476T1 HRP20140476TT HRP20140476T HRP20140476T1 HR P20140476 T1 HRP20140476 T1 HR P20140476T1 HR P20140476T T HRP20140476T T HR P20140476TT HR P20140476 T HRP20140476 T HR P20140476T HR P20140476 T1 HRP20140476 T1 HR P20140476T1
- Authority
- HR
- Croatia
- Prior art keywords
- preparation
- granules
- perindopril
- added
- hypertension
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title claims 7
- IPVQLZZIHOAWMC-QXKUPLGCSA-N perindopril Chemical class C1CCC[C@H]2C[C@@H](C(O)=O)N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H]21 IPVQLZZIHOAWMC-QXKUPLGCSA-N 0.000 title claims 4
- 238000000034 method Methods 0.000 title claims 3
- 239000000203 mixture Substances 0.000 title claims 2
- 206010020772 Hypertension Diseases 0.000 title 1
- 238000009472 formulation Methods 0.000 title 1
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 239000008187 granular material Substances 0.000 claims 5
- 229960002582 perindopril Drugs 0.000 claims 3
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims 2
- 229940060367 inert ingredients Drugs 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 159000000000 sodium salts Chemical class 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 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 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 1
- 230000003276 anti-hypertensive effect Effects 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 229940099112 cornstarch Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000008240 homogeneous mixture Substances 0.000 claims 1
- 229960001375 lactose Drugs 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 229960001021 lactose monohydrate Drugs 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 229940057948 magnesium stearate Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 229960003929 perindopril erbumine Drugs 0.000 claims 1
- IYNMDWMQHSMDDE-MHXJNQAMSA-N perindopril erbumine Chemical compound CC(C)(C)N.C1CCC[C@@H]2N(C(=O)[C@H](C)N[C@@H](CCC)C(=O)OCC)[C@H](C(O)=O)C[C@@H]21 IYNMDWMQHSMDDE-MHXJNQAMSA-N 0.000 claims 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims 1
- 235000017557 sodium bicarbonate Nutrition 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 238000005507 spraying Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 229940033134 talc Drugs 0.000 claims 1
- 235000012222 talc Nutrition 0.000 claims 1
- 229940074410 trehalose Drugs 0.000 claims 1
- 230000000304 vasodilatating effect Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- 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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
-
- 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)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (5)
1. Postupak pripreme, posebno industrijske pripreme, stabilnog oblika amorfne natrijeve soli perindoprila formule I:
[image]
naznačen time što se perindopril erbumin formule II:
[image]
otapa u vodi ili smjesi alkohola/vode u bilo kojem omjeru, toj se otopini dodaje vodena otopina natrijevog hidrogenkarbonata u omjeru 1 mol na 1 mol perindopril erbumina te se sve miješa i dodaje prskanjem na homogenu smjesu inertnih sastojaka za pripremu granulata, suši se u struji toplog zraka temperature iznad 40°C, dodaju se tvari koje pomažu oblikovanje u tablete, homogenizira se i dobiva se granulat.
2. Postupak prema zahtjevu 1, naznačen time što se kao inertni sastojci za pripremu granulata koriste laktoza, laktoza u obliku monohidrata, trehaloza, kukuruzni škrob, mikrokristalinična celuloza, talk i magnezijev stearat.
3. Stabilni oblik granulata amorfne natrijeve soli perindoprila koji se može dobiti postupkom prema zahtjevima 1-2.
4. Oblik prema zahtjevu 3, naznačen time što je to oblik granulata, tablete ili kapsule.
5. Uporaba oblika prema zahtjevima 3-4 za pripremu lijeka koji ima antihipertenzivno i vazodilatorno djelovanje.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SI200500314 | 2005-11-17 | ||
| SI200600177A SI22339A (sl) | 2006-07-31 | 2006-07-31 | Stabilna formulacija amorfnega perindopril erbumina, postopek za njeno pripravo v industrijskem merilu in njena uporaba za zdravljenje hipertenzije |
| PCT/SI2006/000034 WO2007058634A1 (en) | 2005-11-17 | 2006-11-08 | Stable formulation of amorphous perindopril salts, a process for their preparation, especially industrial preparation, and their use in the therapy of hypertension |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20140476T1 true HRP20140476T1 (hr) | 2014-07-18 |
Family
ID=37801135
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20140476TT HRP20140476T1 (hr) | 2005-11-17 | 2014-05-28 | Stabilni oblik amorfnih soli perindoprila, postupak njihove pripreme, posebno industrijske pripreme i njihova uporaba u lijeäśenju hipertenzije |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1948224B1 (hr) |
| HR (1) | HRP20140476T1 (hr) |
| ME (1) | ME01879B (hr) |
| PL (1) | PL1948224T3 (hr) |
| PT (1) | PT1948224E (hr) |
| RS (1) | RS53324B (hr) |
| RU (1) | RU2429878C2 (hr) |
| SI (1) | SI1948224T1 (hr) |
| WO (1) | WO2007058634A1 (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI22542A (sl) * | 2007-06-04 | 2008-12-31 | Diagen D.O.O. | Stabilna formulacija amorfnih soli perindoprila, postopek za njeno pripravo v industrijskem merilu in njena uporaba za zdravljenje hipertenzije |
| SI22543A (sl) | 2007-06-27 | 2008-12-31 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Nove soli perindoprila |
| EP2413924B1 (en) | 2009-04-03 | 2017-09-27 | Ocera Therapeutics, Inc. | L-ornithine phenyl acetate and methods of making thereof |
| EP2625162B1 (en) | 2010-10-06 | 2019-03-13 | Ocera Therapeutics, Inc. | Methods of making l-ornithine phenyl acetate |
| WO2016178591A2 (en) | 2015-05-05 | 2016-11-10 | Gene Predit, Sa | Genetic markers and treatment of male obesity |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4743450A (en) * | 1987-02-24 | 1988-05-10 | Warner-Lambert Company | Stabilized compositions |
| YU48602B (sh) * | 1991-11-25 | 1998-12-23 | Krka Tovarna Zdravil P.O. | Postupak za dobijanje stabilne formulacije soli enalaprila |
| US5573780A (en) * | 1995-08-04 | 1996-11-12 | Apotex Usa Inc. | Stable solid formulation of enalapril salt and process for preparation thereof |
| JP4446463B2 (ja) * | 2000-10-16 | 2010-04-07 | 第一三共株式会社 | 口腔内速崩壊性医薬組成物およびその製造方法 |
| AU2003217916A1 (en) * | 2002-03-08 | 2003-09-22 | Teva Pharmeceuticals Usa, Inc. | Stable formulations of angiotensin converting enzyme (ace) inhibitors |
| SI21704A (en) * | 2004-01-14 | 2005-08-31 | Lek Farmacevtska Druzba Dd | New crystal form of perindopril, procedure of its preparation, pharmaceutical preparations containing this form and their application in treatment of hypertensia |
| SI21703A (en) * | 2004-01-14 | 2005-08-31 | Lek Farmacevtska Druzba Dd | Inclusion complexes of perindopril, procedure of their preparation, pharmaceutical compositions containing these complexes and their application in treatment of hypertensia |
| WO2005094793A1 (en) | 2004-03-29 | 2005-10-13 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Process for preparing a solid pharmaceutical composition |
-
2006
- 2006-11-08 RS RS20140267A patent/RS53324B/en unknown
- 2006-11-08 ME MEP-2014-54A patent/ME01879B/me unknown
- 2006-11-08 RU RU2008123615/15A patent/RU2429878C2/ru not_active IP Right Cessation
- 2006-11-08 PL PL06813152T patent/PL1948224T3/pl unknown
- 2006-11-08 EP EP06813152.3A patent/EP1948224B1/en active Active
- 2006-11-08 PT PT68131523T patent/PT1948224E/pt unknown
- 2006-11-08 WO PCT/SI2006/000034 patent/WO2007058634A1/en active Application Filing
- 2006-11-08 SI SI200631785T patent/SI1948224T1/sl unknown
-
2014
- 2014-05-28 HR HRP20140476TT patent/HRP20140476T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP1948224B1 (en) | 2014-03-12 |
| WO2007058634B1 (en) | 2007-07-26 |
| WO2007058634A1 (en) | 2007-05-24 |
| PT1948224E (pt) | 2014-06-12 |
| PL1948224T3 (pl) | 2014-10-31 |
| RU2429878C2 (ru) | 2011-09-27 |
| RS53324B (en) | 2014-10-31 |
| EP1948224A1 (en) | 2008-07-30 |
| ME01879B (me) | 2014-12-20 |
| RU2008123615A (ru) | 2009-12-27 |
| SI1948224T1 (sl) | 2014-07-31 |
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