WO2000064442A1 - Nouvelle composition injectable d'un anticoagulant - Google Patents
Nouvelle composition injectable d'un anticoagulant Download PDFInfo
- Publication number
- WO2000064442A1 WO2000064442A1 PCT/FR2000/001083 FR0001083W WO0064442A1 WO 2000064442 A1 WO2000064442 A1 WO 2000064442A1 FR 0001083 W FR0001083 W FR 0001083W WO 0064442 A1 WO0064442 A1 WO 0064442A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- citric acid
- solution
- sodium citrate
- injectable composition
- injectable
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Definitions
- the present invention relates to a new stable injectable dosage form containing as active ingredient (2S) -2 [4 - [[(3S) -1-acetimidoyl-3-pyrrolidinyl] oxy] phenyl] -3- (7- amidino-2-naphthyl) propanoic acid or one of its salts, hydrates and solvates, preferably the hydrochloride pentahydrate named DX 9065a corresponding to the following formula:
- the active ingredient which is described in EP 540051, is a specific factor Xa inhibitor and is used as an anticoagulant.
- the dosage forms available to date are either a form of syrup for oral administration or an injectable form for intravenous administration.
- the subject of the present invention is therefore a stable injectable composition containing (2S) -2 [4 - [[(3S) -1-acetimidoyl-3-pyrrolidinyl] oxy] phenyl] -3- (7-amidino-2) acid. -naphthyl) propanoic acid or one of its salts, hydrates and solvates, in the presence of a stabilizing amount of citric acid and sodium citrate.
- a stable solution for injection containing 0.1 to 100 mg / ml of DX 9065a and 2.5 to 100 mM / l of citric acid - sodium citrate buffer is preferred.
- the pH of this buffer is between 3.7 and 4.3.
- the solutions may possibly contain other excipients normally used in injections.
- the active principle citric acid, sodium citrate and optionally other excipients are added in 50 to 95% of the total amount of water present in the final solution, then the final volume (or adjusted to 100%) is adjusted with water to give the desired concentration.
- the dissolution is complete, the solution is sterilized by filtration and the sterile solution obtained is packaged in inactinic tinted glass.
- the weighings as well as the filtrations are carried out in an inactinic room and the preparation is carried out in a stainless steel tank, fitted with a motor and a turbine speed variator.
- DX 9065a, citric acid, sodium citrate and sodium chloride are added in 67% of the total amount of PPI water present in the final formula, then the final volume is adjusted with PPI water .
- the dissolution takes place for 20 minutes at room temperature, with stirring at 205 rpm.
- the solution is collected in a stainless steel beaker and then filtered through Millipack 20.
- the sterile solution is distributed in 3 ml brown glass vials, at a rate of 2.2 ml per vial to give a unit composition as described in TABLE 2 below.
Abstract
Description
Claims
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP00922734A EP1173171A1 (fr) | 1999-04-26 | 2000-04-25 | Nouvelle composition injectable d'un anticoagulant |
AU43033/00A AU4303300A (en) | 1999-04-26 | 2000-04-25 | Novel anticoagulant injectable composition |
CA002370576A CA2370576A1 (fr) | 1999-04-26 | 2000-04-25 | Nouvelle composition injectable d'un anticoagulant |
JP2000613433A JP2002542288A (ja) | 1999-04-26 | 2000-04-25 | 注射可能な新規抗凝固薬組成物 |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR99/05345 | 1999-04-26 | ||
FR9905345A FR2793687B1 (fr) | 1999-04-26 | 1999-04-26 | Nouvelle composition injectable d'un anticoagulant |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2000064442A1 true WO2000064442A1 (fr) | 2000-11-02 |
Family
ID=9544937
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/FR2000/001083 WO2000064442A1 (fr) | 1999-04-26 | 2000-04-25 | Nouvelle composition injectable d'un anticoagulant |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP1173171A1 (fr) |
JP (1) | JP2002542288A (fr) |
AU (1) | AU4303300A (fr) |
CA (1) | CA2370576A1 (fr) |
FR (1) | FR2793687B1 (fr) |
WO (1) | WO2000064442A1 (fr) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2003094889A1 (fr) * | 2002-05-13 | 2003-11-20 | Daiichi Pharmaceutical Co., Ltd. | Produit de lyophilisation |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0540051A1 (fr) * | 1991-10-31 | 1993-05-05 | Daiichi Pharmaceutical Co., Ltd. | Dérivés aromatiques à fonction amidines et leurs sels |
JPH092977A (ja) * | 1995-06-21 | 1997-01-07 | Dai Ichi Seiyaku Co Ltd | 経口投与用医薬組成物 |
WO1998003202A1 (fr) * | 1996-07-23 | 1998-01-29 | Daiichi Pharmaceutical Co., Ltd. | Agents absorptifs |
WO1998026803A1 (fr) * | 1996-12-19 | 1998-06-25 | Daiichi Pharmaceutical Co., Ltd. | Composition pharmaceutique pour administration par voie orale |
WO1998056365A1 (fr) * | 1997-06-13 | 1998-12-17 | Sanofi-Synthelabo | INHIBITEUR DU FACTEUR Xa SEUL OU EN COMBINAISON AVEC UN ANTIAGREGANT PLAQUETTAIRE, CONTRE LA THROMBOSE ARTERIELLE |
JPH1180032A (ja) * | 1997-09-12 | 1999-03-23 | Dai Ichi Seiyaku Co Ltd | 複合体 |
-
1999
- 1999-04-26 FR FR9905345A patent/FR2793687B1/fr not_active Expired - Fee Related
-
2000
- 2000-04-25 WO PCT/FR2000/001083 patent/WO2000064442A1/fr not_active Application Discontinuation
- 2000-04-25 AU AU43033/00A patent/AU4303300A/en not_active Abandoned
- 2000-04-25 EP EP00922734A patent/EP1173171A1/fr not_active Withdrawn
- 2000-04-25 CA CA002370576A patent/CA2370576A1/fr not_active Abandoned
- 2000-04-25 JP JP2000613433A patent/JP2002542288A/ja active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0540051A1 (fr) * | 1991-10-31 | 1993-05-05 | Daiichi Pharmaceutical Co., Ltd. | Dérivés aromatiques à fonction amidines et leurs sels |
JPH092977A (ja) * | 1995-06-21 | 1997-01-07 | Dai Ichi Seiyaku Co Ltd | 経口投与用医薬組成物 |
WO1998003202A1 (fr) * | 1996-07-23 | 1998-01-29 | Daiichi Pharmaceutical Co., Ltd. | Agents absorptifs |
WO1998026803A1 (fr) * | 1996-12-19 | 1998-06-25 | Daiichi Pharmaceutical Co., Ltd. | Composition pharmaceutique pour administration par voie orale |
WO1998056365A1 (fr) * | 1997-06-13 | 1998-12-17 | Sanofi-Synthelabo | INHIBITEUR DU FACTEUR Xa SEUL OU EN COMBINAISON AVEC UN ANTIAGREGANT PLAQUETTAIRE, CONTRE LA THROMBOSE ARTERIELLE |
JPH1180032A (ja) * | 1997-09-12 | 1999-03-23 | Dai Ichi Seiyaku Co Ltd | 複合体 |
Non-Patent Citations (4)
Title |
---|
CHEMICAL ABSTRACTS, vol. 126, no. 13, 25 March 1997, Columbus, Ohio, US; abstract no. 176892, XP002127641 * |
CHEMICAL ABSTRACTS, vol. 128, no. 11, 16 March 1998, Columbus, Ohio, US; abstract no. 132457, XP002128055 * |
CHEMICAL ABSTRACTS, vol. 129, no. 8, 24 August 1998, Columbus, Ohio, US; abstract no. 100033, XP002128056 * |
CHEMICAL ABSTRACTS, vol. 130, no. 21, 24 May 1999, Columbus, Ohio, US; abstract no. 287053, XP002127640 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2003094889A1 (fr) * | 2002-05-13 | 2003-11-20 | Daiichi Pharmaceutical Co., Ltd. | Produit de lyophilisation |
Also Published As
Publication number | Publication date |
---|---|
JP2002542288A (ja) | 2002-12-10 |
FR2793687B1 (fr) | 2001-08-24 |
EP1173171A1 (fr) | 2002-01-23 |
FR2793687A1 (fr) | 2000-11-24 |
AU4303300A (en) | 2000-11-10 |
CA2370576A1 (fr) | 2000-11-02 |
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