CN104161756A - Olprinone hydrochloride injection composition - Google Patents
Olprinone hydrochloride injection composition Download PDFInfo
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- CN104161756A CN104161756A CN201410261301.XA CN201410261301A CN104161756A CN 104161756 A CN104161756 A CN 104161756A CN 201410261301 A CN201410261301 A CN 201410261301A CN 104161756 A CN104161756 A CN 104161756A
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- injection
- olprinone
- olprinone hcl
- polyethylene glycol
- propylene glycol
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Abstract
The invention relates to an olprinone hydrochloride injection composition. Every liter of the injection composition comprises 1 g of olprinone hydrochloride, 30-60 g of sorbitol, 0.5-1.0 g of citric acid, 10-20 g of polyethylene glycol, 5-10 g of propylene glycol and injection water. The prepared olprinone hydrochloride injection has the advantages of low content of impurities and high stability.
Description
Technical field
The invention belongs to medical technical field, relate to a kind of Olprinone HCl injection compositions.
Background technology
Acute heart failure claims again acute cardiac insufficiency, be by cardiac output in a short time sharply reduce due to.When being more common in essential hypertension blood pressure and raising suddenly significantly, when the acute myocardium diffuse lesion such as acute myocarditis, acute myocardial infarction; Valve Serious Stenosis, ventricular outflow tract block, atrial myxoma or auricular ball valve thrombus cause acute mechanical obstruction, when heart row blood is obstructed; When ventricular fibrillation, ventricular standstill, remarkable tachycardia etc. cause fatal arrhythmia; When limited the and fast incorrect a large amount of blood transfusions of the ventricular diastoles such as acute heart tamponade, transfusion etc.
Olprinone HCl (Olprinone Hydrochloride) is the medicine of the treatment acute heart failure of Japanese ェ-ザ ィ Co., Ltd. exploitation, and commodity are called コ ア テ ッ Network
?(Coretec
?), chemistry 1,2-dihydro-5-imidazo [1,2-a] pyridine-6-base-6-methyl-2-oxo-3-pyridine carbon cyanogen hydrochloride monohydrate by name, molecular formula C
14h
10n
4oHClH
2o, structural formula is as follows:
Olprinone HCl optionally hinders the special phosphodiesterase (PDE of adenosine cyclophosphate
), there is the contractile force of enhancing and angiectatic effect.Olprinone HCl began one's study in nineteen eighty-two, and 1986 start clinical trial, prove acute heart failure effective.Clinical trial also proves, Olprinone HCl does not increase myocardium oxygen consumption, and increases cardiac output, than catecholamines preparation to improve cardiac energy effective percentage high.
Although prior art, for example CN101919814A and CN101152146A, disclose some Olprinone HCl injections, and its its related substances is higher, and the stability of injection still exists some problems.For the consideration of patient's drug safety, still need those skilled in the art that the Olprinone HCl injection composition and method of making the same that a kind of stability is higher is provided.
Summary of the invention
Through great many of experiments, inventor has found the Olprinone HCl injection composition prescription that a kind of stability is high, and the preparation technology of this injecta composition is simple, is applicable to suitability for industrialized production.
Particularly, the invention provides one, in injecta composition every liter described, comprise Olprinone HCl 1g, sorbitol 30-60g, citric acid 0.5-1.0g, Polyethylene Glycol 10-20g, propylene glycol 5-10g and water for injection.
In above-mentioned Olprinone HCl injection compositions provided by the invention, preferably it being regulated to pH with sodium bicarbonate is 3.5-4.5.
And for above-mentioned Olprinone HCl injection compositions provided by the invention, when wherein Polyethylene Glycol is 2:1 with the ratio of the weight content of propylene glycol, its stability is higher.
For above-mentioned Olprinone HCl injection compositions provided by the invention, more specifically, the present invention relates to following Olprinone HCl injection compositions:
(1) an Olprinone HCl injection compositions, wherein every liter of described injecta composition comprises Olprinone HCl 1g, sorbitol 30g, citric acid 0.5g, Polyethylene Glycol 10g, propylene glycol 5g and water for injection.
(2) an Olprinone HCl injection compositions, wherein every liter of described injecta composition comprises Olprinone HCl 1g, sorbitol 60g, citric acid 0.7g, Polyethylene Glycol 15g, propylene glycol 7.5g and water for injection.
(3) an Olprinone HCl injection compositions, wherein every liter of described injecta composition comprises Olprinone HCl 1g, sorbitol 50g, citric acid 1.0g, Polyethylene Glycol 20g, propylene glycol 10g and water for injection.
As preferred version of the present invention, the Polyethylene Glycol of described Olprinone HCl injection compositions is PEG-200, PEG-400, PEG-600, most preferably PEG-200.
Detailed description of the invention
Following detailed description of the invention provided by the invention, only for further illustrating the present invention, should not be interpreted as any limitation of the invention.
prescription and the preparation method of embodiment 1-5 Olprinone HCl injection compositions of the present invention
Prescription:
| ? | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 |
| Olprinone HCl | 1g | 1g | 1g | 1g | 1g |
| Polyethylene Glycol (PEG-200) | 10g | 15g | 20g | 10g | 15g |
| Propylene glycol | 5g | 7.5g | 10g | 10g | 20g |
| Sorbitol | 30g | 60g | 50g | 30g | 50g |
| Citric acid | 0.5 | 0.7 | 1.0 | 0.8 | 0.6 |
| 0.2M sodium hydroxide regulates pH extremely | 3.5 | 4.5 | 4.0 | 4.5 | 3.5 |
| Water for injection adds to | 1L | 1L | 1L | 1L | 1L |
| Make | 200 | 200 | 200 | 200 | 200 |
Note: in embodiment 1-3, the weight ratio of Polyethylene Glycol and propylene glycol is 2:1.
Preparation method:
(1) take Polyethylene Glycol, propylene glycol, sorbitol and the citric acid of recipe quantity, add in appropriate water for injection, stirring and dissolving, adds 0.05% active carbon and stirs, and leaves standstill 15 minutes, and de-charcoal, with 0.22 μ m membrane filtration.
(2) take the Olprinone HCl of recipe quantity, add in the solution that step (1) obtains, stir, benefit injects water to enough, with appropriate 0.2M sodium hydroxide adjusting pH value, adds 0.01% needle-use activated carbon, more than 50 DEG C be incubated 15 minutes, filter, measure pH value and content, qualified rear mistake 0.22 μ m filter membrane fine straining, the fill of filtrate inflated with nitrogen, in ampoule, is sealed, in 121 DEG C of sterilizings 15 minutes, lamp inspection, packaging, warehouse-in.
embodiment 6 long-time stability experiments
The Olprinone HCl injection of the present invention that utilizes embodiment 1-5 to prepare, carries out long-time stability experiment.
In the probation of 2 years by a definite date, the character of embodiment 1-5 injection, pH value, content etc. all meet relevant regulations, and without significant difference.Compared with the Olprinone HCl injection (CN101919814A embodiment 1) of preparing with prior art, related substance % is obviously lower for Olprinone HCl injection of the present invention (embodiment 1-5).Stability that it should be noted that the injection (embodiment 1-3) that Polyethylene Glycol and the ratio of the weight content of propylene glycol are 2:1 is best, is better than injection (embodiment 4-5) prepared by other embodiment.
Related substance % testing result is as following table:
| Time (moon) | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Prior art (CN101919814A embodiment 1) |
| 0 | 0.07 | 0.08 | 0.08 | 0.16 | 0.15 | 0.28 |
| 3 | 0.07 | 0.08 | 0.08 | 0.16 | 0.15 | 0.29 |
| 6 | 0.07 | 0.08 | 0.08 | 0.17 | 0.15 | 0.29 |
| 9 | 0.08 | 0.08 | 0.08 | 0.17 | 0.15 | 0.31 |
| 12 | 0.08 | 0.09 | 0.08 | 0.17 | 0.16 | 0.34 |
| 18 | 0.08 | 0.09 | 0.09 | 0.17 | 0.16 | 0.35 |
| 24 | 0.09 | 0.09 | 0.09 | 0.18 | 0.16 | 0.35 |
Claims (8)
1. an Olprinone HCl injection compositions, in injecta composition every liter described, comprises Olprinone HCl 1g, sorbitol 30-60g, citric acid 0.5-1.0g, Polyethylene Glycol 10-20g, propylene glycol 5-10g and water for injection.
2. Olprinone HCl injection compositions according to claim 1, is characterized in that, its pH value is 3.5-4.5.
3. Olprinone HCl injection compositions according to claim 1 and 2, wherein Polyethylene Glycol is 2:1 with the ratio of the weight content of propylene glycol.
4. Olprinone HCl injection compositions according to claim 3, wherein every liter of described injecta composition comprises Olprinone HCl 1g, sorbitol 30g, citric acid 0.5g, Polyethylene Glycol 10g, propylene glycol 5g and water for injection.
5. Olprinone HCl injection compositions according to claim 3, wherein every liter of described injecta composition comprises Olprinone HCl 1g, sorbitol 60g, citric acid 0.7g, Polyethylene Glycol 15g, propylene glycol 7.5g and water for injection.
6. Olprinone HCl injection compositions according to claim 3, wherein every liter of described injecta composition comprises Olprinone HCl 1g, sorbitol 50g, citric acid 1.0g, Polyethylene Glycol 20g, propylene glycol 10g and water for injection.
7. according to the arbitrary described Olprinone HCl injection compositions of claim 1-6, wherein said Polyethylene Glycol is PEG-200, PEG-400 or PEG-600.
8. Olprinone HCl injection compositions according to claim 7, wherein said Polyethylene Glycol is PEG-200.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410261301.XA CN104161756B (en) | 2014-06-13 | 2014-06-13 | Olprinone hydrochloride injection composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410261301.XA CN104161756B (en) | 2014-06-13 | 2014-06-13 | Olprinone hydrochloride injection composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104161756A true CN104161756A (en) | 2014-11-26 |
| CN104161756B CN104161756B (en) | 2017-02-01 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108619090A (en) * | 2018-05-30 | 2018-10-09 | 河北爱尔海泰制药有限公司 | A kind of high stability Olprinone HCl injection composition |
| CN114099426A (en) * | 2021-11-10 | 2022-03-01 | 芜湖杨燕制药有限公司 | Preparation method of olprinone hydrochloride injection |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006063714A1 (en) * | 2004-12-14 | 2006-06-22 | Menarini Ricerche S.P.A. | Pharmaceutical compositions for the treatment of cellulite |
| CN101152146A (en) * | 2006-09-29 | 2008-04-02 | 北京德众万全药物技术开发有限公司 | Hydrochloric acid olprinone injection and method for preparing the same |
| CN101683320A (en) * | 2008-09-27 | 2010-03-31 | 西安万隆制药有限责任公司 | Olprinone hydrochloric parenteral solution and method for preparing same |
| CN101919814A (en) * | 2010-08-02 | 2010-12-22 | 无锡万全医药技术有限公司 | Stable Olprinone HCl injection |
| WO2013170317A1 (en) * | 2012-05-18 | 2013-11-21 | Luoda Pharma Pty Ltd | Liquid formulation |
-
2014
- 2014-06-13 CN CN201410261301.XA patent/CN104161756B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006063714A1 (en) * | 2004-12-14 | 2006-06-22 | Menarini Ricerche S.P.A. | Pharmaceutical compositions for the treatment of cellulite |
| CN101152146A (en) * | 2006-09-29 | 2008-04-02 | 北京德众万全药物技术开发有限公司 | Hydrochloric acid olprinone injection and method for preparing the same |
| CN101683320A (en) * | 2008-09-27 | 2010-03-31 | 西安万隆制药有限责任公司 | Olprinone hydrochloric parenteral solution and method for preparing same |
| CN101919814A (en) * | 2010-08-02 | 2010-12-22 | 无锡万全医药技术有限公司 | Stable Olprinone HCl injection |
| WO2013170317A1 (en) * | 2012-05-18 | 2013-11-21 | Luoda Pharma Pty Ltd | Liquid formulation |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108619090A (en) * | 2018-05-30 | 2018-10-09 | 河北爱尔海泰制药有限公司 | A kind of high stability Olprinone HCl injection composition |
| CN108619090B (en) * | 2018-05-30 | 2020-12-08 | 河北爱尔海泰制药有限公司 | High-stability olprinone hydrochloride injection composition |
| CN114099426A (en) * | 2021-11-10 | 2022-03-01 | 芜湖杨燕制药有限公司 | Preparation method of olprinone hydrochloride injection |
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| Publication number | Publication date |
|---|---|
| CN104161756B (en) | 2017-02-01 |
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Effective date of registration: 20190827 Address after: 050035 Taishan Street 219, Shijiazhuang High-tech Industrial Development Zone, Hebei Province Patentee after: Hebei Ideal & Hightech Pharmaceutical Co., Ltd. Address before: 050035 No. 219, Taishan street, hi tech Industrial Development Zone, Hebei, Shijiazhuang Patentee before: Hebei Zhitong Pharmaceutical Group Co., Ltd. |