NZ236834A - Oral medicaments comprising pimobendan in dry mixture with citric acid - Google Patents
Oral medicaments comprising pimobendan in dry mixture with citric acidInfo
- Publication number
- NZ236834A NZ236834A NZ236834A NZ23683491A NZ236834A NZ 236834 A NZ236834 A NZ 236834A NZ 236834 A NZ236834 A NZ 236834A NZ 23683491 A NZ23683491 A NZ 23683491A NZ 236834 A NZ236834 A NZ 236834A
- Authority
- NZ
- New Zealand
- Prior art keywords
- pimobendan
- composition
- pellets
- citric acid
- granulate
- Prior art date
Links
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 title claims abstract 15
- 229960002164 pimobendan Drugs 0.000 title claims abstract 6
- GLBJJMFZWDBELO-UHFFFAOYSA-N pimobendane Chemical compound C1=CC(OC)=CC=C1C1=NC2=CC=C(C=3C(CC(=O)NN=3)C)C=C2N1 GLBJJMFZWDBELO-UHFFFAOYSA-N 0.000 title claims abstract 6
- 239000000203 mixture Substances 0.000 title claims 7
- 239000003814 drug Substances 0.000 title 1
- 239000008187 granular material Substances 0.000 claims 5
- 239000008188 pellet Substances 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 239000002775 capsule Substances 0.000 claims 2
- 239000011248 coating agent Substances 0.000 claims 2
- 238000000576 coating method Methods 0.000 claims 2
- 239000012530 fluid Substances 0.000 claims 2
- 238000005469 granulation Methods 0.000 claims 2
- 230000003179 granulation Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 241001125671 Eretmochelys imbricata Species 0.000 claims 1
- 239000007884 disintegrant Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000007908 dry granulation Methods 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 239000002552 dosage form Substances 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
-
- 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
-
- 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
- A61K9/4841—Filling excipients; Inactive ingredients
-
- 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
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Plant Substances (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Cosmetics (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
Pimobendan dosage forms for oral administration contain citric acid, ensuring constantly good absorption even with large pH variations in the gastrointestinal tract.
Description
2368 3 4 Priority Date(s): Complete Specs'Sca-lion Flies": Class: Publication Date: P.O. Journal Ho: Ml Patents Form No. 5 NEW ZEALAND JL> 'V\ PATENTS ACT 1953 ff '
Claims (11)
1. An orally administrable pimobendan-containing pharmaceutial composition comprising an intimate, dry mixture of citric acid and pimobendan in a weight ratio of at least 5:1, optionally together with one or more pharmaceutical carriers or excipients.
2. A composition as claimed in claim 1 in the form of a granulate, powder or pellets, optionally packed into capsules.
3. A composition as claimed in claim 1, in the form of the granulate, powder or pellets compressed with a suitable excipient into tablets which are optionally provided with a flavour-masking coating.
4. A composition as claimed in any of claims 1 to 3, wherein the weight ratio of pimobendan to citric acid is between 1:10 and 1:20.
5. A composition as claimed in any of claims 1 to 4 containing a disintegrant.
6. A process for preparing a pharmaceutical composition as claimed in claim 1, wherein citric acid and pimobendan in a weight ratio of at least 5:1 are brought into an intimately mixed form by granulation.
7. A process as claimed in claim 6 wherein granulation is effected by dry granulation or in the presence of an aqueous or non-aqueous granulating fluid with metered addition of granulating fluid and simultaneous drying.
8. A process as claimed in either of claims 6 and 7 wherein the resulting granulate is processed i^ pellets. "28 JAN1993 236834 18
9. A process as claimed in any one of claims 6 to 8 wherein the resulting granulate or pellets are compressed with suitable excipients into tablets which are optionally provided with a flavour-masking coating.
10. A process as claimed in any one of claims 6 to 8 wherein the resulting granulate or pellets are packed into capsules.
11. Pharmaceutical compositions as defined in claim 1 substantially as herein disclosed in any one of the Examples. DR KARL THOMAE GMBH By Their Attorneys BALDWIN, SON & CAREY
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4001622A DE4001622A1 (en) | 1990-01-20 | 1990-01-20 | ORAL DRUGS OF PIMOBENDAN |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ236834A true NZ236834A (en) | 1995-10-26 |
Family
ID=6398467
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ236834A NZ236834A (en) | 1990-01-20 | 1991-01-18 | Oral medicaments comprising pimobendan in dry mixture with citric acid |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP0439030B1 (en) |
| JP (1) | JP2608183B2 (en) |
| KR (1) | KR0163056B1 (en) |
| AT (1) | ATE87481T1 (en) |
| AU (1) | AU630536B2 (en) |
| CA (1) | CA2034569C (en) |
| DE (2) | DE4001622A1 (en) |
| DK (1) | DK0439030T3 (en) |
| ES (1) | ES2054379T3 (en) |
| FI (1) | FI96274C (en) |
| HK (1) | HK175796A (en) |
| HU (1) | HU207948B (en) |
| IE (1) | IE64659B1 (en) |
| IL (1) | IL96995A (en) |
| NO (1) | NO176305C (en) |
| NZ (1) | NZ236834A (en) |
| PT (1) | PT96506B (en) |
| ZA (1) | ZA91372B (en) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2753904B1 (en) * | 1996-10-01 | 1998-10-30 | Gattefosse Ets Sa | PHARMACEUTICAL COMPOSITION WITH MODIFIED RELEASE OF ACTIVE SUBSTANCE, INCLUDING A MATRIX, AND MANUFACTURING PROCESS |
| DE102004011512B4 (en) * | 2004-03-08 | 2022-01-13 | Boehringer Ingelheim Vetmedica Gmbh | Pharmaceutical preparation containing pimobendan |
| US8980894B2 (en) | 2004-03-25 | 2015-03-17 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the treatment of asymptomatic (occult) heart failure |
| EP1579862A1 (en) | 2004-03-25 | 2005-09-28 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the reduction of heart size in mammals suffering from heart failure |
| WO2005107719A2 (en) * | 2004-05-06 | 2005-11-17 | Sandoz Ag | Pharmaceutical composition comprising hydrophobic drug having improved solubility |
| WO2005123040A1 (en) * | 2004-06-22 | 2005-12-29 | Shionogi & Co., Ltd. | Tablet rapidly disintegrating in mouth |
| JP4572293B2 (en) * | 2004-07-21 | 2010-11-04 | トーアエイヨー株式会社 | Pimobendan oral dosage formulation |
| JP4572296B2 (en) * | 2004-07-21 | 2010-11-04 | トーアエイヨー株式会社 | Pimobendan oral dosage formulation |
| JP2006028130A (en) * | 2004-07-21 | 2006-02-02 | Toa Eiyo Ltd | Pimobendan oral dosage formulation |
| WO2007035874A1 (en) * | 2005-09-21 | 2007-03-29 | Bristol-Myers Squibb Company | Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof |
| JP4572300B2 (en) * | 2006-01-19 | 2010-11-04 | トーアエイヨー株式会社 | Pimobendan oral dosage formulation |
| EP1920785A1 (en) | 2006-11-07 | 2008-05-14 | Boehringer Ingelheim Vetmedica Gmbh | Liquid preparation comprising a complex of pimobendan and cyclodextrin |
| PE20081482A1 (en) * | 2006-12-20 | 2008-12-23 | Novartis Ag | GELATINE CAPSULES CONTAINING AN ACID |
| FR2934156B1 (en) * | 2008-07-23 | 2010-09-24 | Virbac | ORAL ADMINISTRATION MEDICAMENT IN SOLID FORM |
| WO2010055119A2 (en) * | 2008-11-17 | 2010-05-20 | Novartis Ag | Pharmaceutical composition comprising pimobendan |
| NZ592927A (en) | 2008-11-25 | 2013-07-26 | Boehringer Ingelheim Vetmed | PHOSPHODIESTERASE TYPE III (PDE III) INHIBITORS OR CA2+-SENSITIZING AGENTS such as pimobendan FOR THE TREATMENT OF HYPERTROPHIC CARDIOMYOPATHY |
| NL1037569C2 (en) | 2009-12-18 | 2011-06-21 | Eurovet Animal Health B V | Crystalline pimobendan, process for the preparation thereof, pharmaceutical composition and use. |
| WO2011081117A1 (en) * | 2009-12-29 | 2011-07-07 | 興和株式会社 | Solid pharmaceutical composition for oral administration |
| WO2011081118A1 (en) * | 2009-12-29 | 2011-07-07 | 興和株式会社 | Pharmaceutical composition for oral administration |
| WO2013135852A1 (en) | 2012-03-15 | 2013-09-19 | Boehringer Ingelheim Vetmedica Gmbh | Pharmaceutical tablet formulation for the veterinary medical sector, method of production and use thereof |
| JP6272475B2 (en) | 2013-07-19 | 2018-01-31 | ベーリンガー インゲルハイム フェトメディカ ゲーエムベーハーBoehringer Ingelheim Vetmedica GmbH | Liquid aqueous pharmaceutical composition containing antiseptic etherified cyclodextrin derivative |
| EA034054B1 (en) * | 2013-12-04 | 2019-12-23 | Бёрингер Ингельхайм Ветмедика Гмбх | Improved pharmaceutical compositions of pimobendan |
| US10537570B2 (en) | 2016-04-06 | 2020-01-21 | Boehringer Ingelheim Vetmedica Gmbh | Use of pimobendan for the reduction of heart size and/or the delay of onset of clinical symptoms in patients with asymptomatic heart failure due to mitral valve disease |
| CN106729723A (en) * | 2016-11-21 | 2017-05-31 | 青岛农业大学 | A kind of pharmaceutical composition containing UD-CG115BS.acardi and preparation method thereof |
| KR20220006776A (en) * | 2020-07-09 | 2022-01-18 | 주식회사유한양행 | Pharmaceutical compositions comprising a diaminopyrimidine derivative or pharmaceutically acceptable salt thereof and processes for preparing the same |
| WO2024126434A1 (en) | 2022-12-15 | 2024-06-20 | Boehringer Ingelheim Vetmedica Gmbh | Solid dispersions comprising amorphous pimobendan and one or more stabilizing polymers |
| JP7659339B1 (en) | 2023-11-21 | 2025-04-09 | 東海カプセル株式会社 | Oral film formulation containing pimobendan |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES482789A0 (en) * | 1978-08-25 | 1980-12-01 | Thomae Gmbh Dr K | PROCEDURE FOR THE PREPARATION OF NEW BENZHIMIDAZOLES REPLACED IN POSITION 5 OR 6 WITH A PYRIDAZINONE RING |
| DE2837161A1 (en) * | 1978-08-25 | 1980-03-06 | Thomae Gmbh Dr K | 5-Alkyl:pyridazinyl substd. benzimidazole derivs. - useful as cardiovascular agents, antivirals, interferon inducers and ulcer inhibitors |
| JPS56110612A (en) * | 1980-02-08 | 1981-09-01 | Yamanouchi Pharmaceut Co Ltd | Readily disintegrable and absorbable compression molded article of slightly soluble drug |
| JPS60163823A (en) * | 1984-02-03 | 1985-08-26 | Taisho Pharmaceut Co Ltd | Orally administered formulation |
| DE3776269D1 (en) * | 1986-11-03 | 1992-03-05 | Schering Corp | LABETALOL TABLET WITH DELAYED DELIVERY OF ACTIVE SUBSTANCES. |
| DE3728244A1 (en) * | 1987-08-25 | 1989-03-09 | Thomae Gmbh Dr K | NEW (-) - BENZIMIDAZOLE, THEIR PREPARATION AND MEDICAMENTS CONTAINING THESE COMPOUNDS |
| EP0306846A3 (en) * | 1987-09-11 | 1990-05-02 | Dr. Karl Thomae GmbH | Synergistic combination comprising a phosphodiesterase inhibitor and a thromboxane-a2 antagonist, and its use or preparation |
| DE3805635A1 (en) * | 1988-02-24 | 1989-09-07 | Thomae Gmbh Dr K | USE OF BENZIMIDAZOLES FOR THE MANUFACTURE OF A MEDICAMENT WITH ANTI-MIXIC EFFECTS ON THE HEART AND ITS COMBINATIONS WITH SS-BLOCKERS OR BRADYCARDICA |
| JPH01258621A (en) * | 1988-04-06 | 1989-10-16 | Fujimoto Seiyaku Kk | Dilazep tablet with regulated absorption |
| JPH023609A (en) * | 1988-06-21 | 1990-01-09 | Fujimoto Seiyaku Kk | Long-acting drug preparation containing nicardipine hydrochloride as active component |
-
1990
- 1990-01-20 DE DE4001622A patent/DE4001622A1/en not_active Withdrawn
-
1991
- 1991-01-11 DE DE9191100309T patent/DE59100067D1/en not_active Expired - Lifetime
- 1991-01-11 EP EP91100309A patent/EP0439030B1/en not_active Expired - Lifetime
- 1991-01-11 DK DK91100309.3T patent/DK0439030T3/en active
- 1991-01-11 AT AT91100309T patent/ATE87481T1/en not_active IP Right Cessation
- 1991-01-11 ES ES91100309T patent/ES2054379T3/en not_active Expired - Lifetime
- 1991-01-17 PT PT96506A patent/PT96506B/en not_active IP Right Cessation
- 1991-01-18 AU AU69454/91A patent/AU630536B2/en not_active Expired
- 1991-01-18 IE IE16591A patent/IE64659B1/en not_active IP Right Cessation
- 1991-01-18 CA CA002034569A patent/CA2034569C/en not_active Expired - Lifetime
- 1991-01-18 FI FI910263A patent/FI96274C/en active
- 1991-01-18 ZA ZA91372A patent/ZA91372B/en unknown
- 1991-01-18 HU HU91177A patent/HU207948B/en unknown
- 1991-01-18 NZ NZ236834A patent/NZ236834A/en unknown
- 1991-01-18 NO NO910213A patent/NO176305C/en not_active IP Right Cessation
- 1991-01-18 JP JP3004069A patent/JP2608183B2/en not_active Expired - Lifetime
- 1991-01-18 KR KR1019910000822A patent/KR0163056B1/en not_active Expired - Lifetime
- 1991-01-22 IL IL9699591A patent/IL96995A/en not_active IP Right Cessation
-
1996
- 1996-09-19 HK HK175796A patent/HK175796A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| NO176305C (en) | 1995-03-15 |
| PT96506B (en) | 1998-06-30 |
| KR0163056B1 (en) | 1998-12-01 |
| HU910177D0 (en) | 1991-08-28 |
| ES2054379T3 (en) | 1994-08-01 |
| AU6945491A (en) | 1991-07-25 |
| FI96274B (en) | 1996-02-29 |
| HK175796A (en) | 1996-09-27 |
| EP0439030A2 (en) | 1991-07-31 |
| IL96995A (en) | 1994-11-11 |
| IE64659B1 (en) | 1995-08-23 |
| KR910014120A (en) | 1991-08-31 |
| DK0439030T3 (en) | 1993-08-16 |
| IE910165A1 (en) | 1991-07-31 |
| ATE87481T1 (en) | 1993-04-15 |
| IL96995A0 (en) | 1992-03-29 |
| CA2034569A1 (en) | 1991-07-21 |
| NO910213L (en) | 1991-07-22 |
| FI96274C (en) | 1996-06-10 |
| JP2608183B2 (en) | 1997-05-07 |
| DE4001622A1 (en) | 1991-07-25 |
| PT96506A (en) | 1991-10-15 |
| HU207948B (en) | 1993-07-28 |
| JPH04210919A (en) | 1992-08-03 |
| EP0439030A3 (en) | 1991-10-16 |
| HUT56494A (en) | 1991-09-30 |
| CA2034569C (en) | 2002-03-19 |
| FI910263L (en) | 1991-07-21 |
| FI910263A0 (en) | 1991-01-18 |
| DE59100067D1 (en) | 1993-05-06 |
| AU630536B2 (en) | 1992-10-29 |
| ZA91372B (en) | 1992-09-30 |
| NO176305B (en) | 1994-12-05 |
| EP0439030B1 (en) | 1993-03-31 |
| NO910213D0 (en) | 1991-01-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RENW | Renewal (renewal fees accepted) |