CN101422428A - Injection containing sodium pidotimod - Google Patents
Injection containing sodium pidotimod Download PDFInfo
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- CN101422428A CN101422428A CNA200810056254XA CN200810056254A CN101422428A CN 101422428 A CN101422428 A CN 101422428A CN A200810056254X A CNA200810056254X A CN A200810056254XA CN 200810056254 A CN200810056254 A CN 200810056254A CN 101422428 A CN101422428 A CN 101422428A
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- pidotimod
- injection
- sodium
- infection
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Abstract
The invention discloses an injection containing pidotimod sodium, which is characterized in that an active component of pidotimod in the injection exists in the form of pidotimod salt, which not only increases the stability of the pidotimod, but also leads the pH value to more approach to the pH value of a human body. The invention contains the transfusion prepared by the pidotimod natrium and used for intravenous administration as well as injecta which can be added into 5 percent dextrose or 0.9 percent solium chloride injecta, a solvent crystallization split charging powder needle and a freezing-drying powder needle. The injection containing the pidotimod sodium provided by the invention is prepared as follows: the pidotimod and sodium hydroxide with equal mol react in water or ethanol or the mixed liquid of the two to generate the pidotimod sodium; and then the pidotimod sodium is prepared into the injection. The chemical name of the pidotimod sodium is (R)-3-[(S)-(5-O-2-pyrrolidinyl) carboxide]-thiazolidine-4-sodium carboxylate. The molecular formula is C9H11N2O4SNa; the molecular weight is 266.28. The injection containing the pidotimod sodium is used for curing (1) recurrent upper and lower respiratory infections (pharyngitis, tracheitis, bronchitis and amygdalitis); (2) recurrent infection in otorhinolaryngology (rhinitis, nasosinusitis and otitis); (3) urinary system infection; (4) gynae infection; (5) the clinic patients with weakened cellular immune function after chemo-treatment; and (6) specific and nonspecific immunodeficiency diseases such as cancer, and the like. The injection containing the pidotimod sodium is used for reducing the times of acute attack, shortening the course of disease and lightening the attack degree; moreover, the injection containing the pidotimod sodium can also be used as for the auxiliary treatment of antibiotics during acute infection.
Description
Technical field
The invention belongs to the medicine new technical field, relate to a kind of injection that contains pidotimod sodium.1. this injection is used for the treatment of the last lower respiratory infection (pharyngitis, tracheitis, bronchitis, tonsillitis) of outbreak repeatedly; 2. department of otorhinolaryngology repeated infection (rhinitis, sinusitis, otitis); 3. urinary system infection; 4. gynecological infection; 5. the low clinical patients of cellular immune function after the chemotherapy; 6. specificity and nonspecific immunity defective disorders such as cancers etc.In order to reduce the number of times of acute attack, shorten the course of disease, alleviate the degree of outbreak; Antibiotic auxiliary treatment when also can be used as actute infection.Specifically a kind of preparation and application thereof that contains the injection of pidotimod sodium.
Background technology
The immune system of human body is being defended the health of human body just as a well-trained crack troops.Immune system is people's usually said " immunity ", " resistance " to the defence capability of pathogen.
People's defence capability comprises nonspecific immunity and specific immunity.Nonspecific immunity is to be born with the man day, so be called the inherency immunity again, comprise the skin, mucosa of body barrier effect to pathogen, phagocyte in the blood, neutrophilic granulocyte be to the phagocytosis of pathogen, and complement, lyase bacterium, properdin, interferon etc. are to the killing action of pathogen.Specific immunity is meant human body to the resistance targetedly that certain pathogen had, and this immunity varies with each individual, and generally can obtain by prophylactic immunization, ill or inapparent infection.Specific immunity mainly forms after the people is born, so be acquired immunity again.
Sound immunity is to guarantee that body avoids the key factor of pathogen invasion and attack, and in fact, for some reason or other, often causes people's hypoimmunity.
Pidotimod (pidotimod) is a kind of brand-new chemosynthesis immunopotentiating agent, and its similar is in dipeptides.The later stage eighties 20th century is successfully synthesized by Italian Poli industria chimica S.P.A chemical company, and gets permission listing in 1993 and be used for clinical.
Pharmacodynamic study shows that pidotimod is an immunopotentiating agent, can promote nonspecific immune reaction, can promote specific immune response again.Pidotimod can promote the activate the phagocytic capacity of macrophage and neutrophilic granulocyte, improves its chemotaxis; Activate natural killer cell; The former lymphopoiesis that causes of mitosis promoting, the helper T lymphocyte (CD that reduces when making immunologic hypofunction
4 +) and suppressor T lymphocyte (CD
8 +) ratio raise to recover normal; By stimulating interleukin-2 and gamma interferon to promote cell immune response.
Although all showing pidotimod, animal experiment and clinical trial do not have directly antibiotic and antiviral activity, by bringing into play the curative effect that significant treatment antibacterial (Diplococcus pneumoniae, escherichia coli, bacillus pyocyaneus, Bacillus proteus etc.) and virus (influenza virus, herpes simplex virus, murine encephalomyocarditis virus and Mengo virus etc.) infect to the promotion of the immunologic function of human body.
Pidotimod is by cellular immunization, humoral immunization approach performance antibacterium, antiviral, the antifungic action of enhancing body.Clinical practice has all obtained good effect in repeatedly respiratory tract infection of control child, old people's chronic bronchitis, urinary system infection, malignant tumor and the chemotherapy of outbreak repeatedly, the auxiliary treatment after the radiotherapy.The multicenter open clinical trial shows that curative effect is reliable, and the human tolerance is good, and toxic and side effects is little.
Pidotimod was taken in the 31st edition Martin's pharmacopeia in 1996.Tianjin Jinshi Pharmaceutical Co., Ltd. has successfully developed the granule dosage form of pidotimod in 2000, and is four kind new medicines by state approval.Calendar year 2001, there has been pidotimod tablet (trade name " Wan Shining ") production in China's sun-stone (Tangshan) Pharma Inc., we can say that the imported product of pidotimod and production domesticization product have been on the same starting line.
The present invention is a kind of injection that contains pidotimod sodium, and the effective active composition pidotimod in its injection is that the form with the pidotimod sodium salt exists, and has increased the stability of pidotimod, has also improved the water solublity of pidotimod simultaneously.The injection that contains pidotimod sodium of the present invention, safety is good, and good stability, pH value need not to add other adjuvant more near pH value of human body.
The chemical structural formula of pidotimod sodium is:
Molecular formula: C
9H
12N
2O
4SNa
Molecular weight: 266.28
Summary of the invention
A kind of common method for making that contains the pidotimod sodium injection of the present invention is pidotimod is dissolved in or is suspended in water or the ethanol, add equimolar sodium hydroxide then, after at room temperature being stirred to fully dissolving, by concentrating, lyophilizing and the method that adds organic solvent obtain.
The present invention also provides a kind of injection type that pidotimod sodium is prepared into muscle or intravenously administrable that contains, and it is characterized in that it is the infusion solution that is used for intravenously administrable that is made by the aqueous solution that pidotimod sodium and water form and can adds to 5% glucose or the injection of 0.9% sodium chloride injection, solvent crystal packing powder pin and lyophilized powder pin.Above-mentioned aqueous solution can be that pidotimod and sodium hydroxide react in water and the pidotimod sodium water solution that directly forms, also can be it is the soluble in water and aqueous solution that forms after obtaining pidotimod sodium.Do not separating out solid by the injection that contains pidotimod sodium of the present invention during in long term store, and composition is still stable.
A kind of preparation process that contains the injection of pidotimod sodium provided by the invention includes but not limited to following several:
(1) pidotimod and the sodium hydroxide of getting equimolar amounts joins in an amount of water for injection, stirring makes dissolving fully, adds or do not add acceptable accessories such as mannitol, dextran series, sorbitol, sodium chloride, glucose etc., adds an amount of pin charcoal, and the continuation stirring was incubated 20 minutes in 20 minutes or 60 ℃, filter decarburization, add water for injection to needed amount, fine straining degerming, packing, in 115 ℃ of sterilizations down, make injection or transfusion;
Or packing after the fine straining degerming, put in the freeze dryer after the lyophilization, make injection powder pin.
(2) pidotimod and the sodium hydroxide of getting equimolar amounts joins in an amount of ethanol, stirs to make dissolving fully, filters.The concentrating under reduced pressure after drying is flung to ethanol and is promptly got powdered pidotimod sodium.Join again in an amount of water for injection, add or do not add acceptable accessories such as mannitol, dextran series, sorbitol, sodium chloride, glucose etc., add an amount of pin charcoal, and the continuation stirring was incubated 20 minutes in 20 minutes or 60 ℃, the filtration decarburization, add water for injection to needed amount, the fine straining degerming, packing is in 115 ℃ of sterilizations down, make injection or transfusion;
Or packing after the fine straining degerming, put in the freeze dryer after the lyophilization, make injection powder pin.
(3) pidotimod and the sodium hydroxide of getting equimolar amounts joins in an amount of ethanol, stirs to make dissolving fully, filters.The concentrating under reduced pressure after drying is flung to ethanol and is promptly got powdered pidotimod sodium.Aseptic subpackaged in cillin bottle, promptly get injection powder pin.
Injection of the present invention is preferably in the scope of pH6～8 in pH4～9.The powder pin adds pH6～8 of its solution behind an amount of water for injection.
Advantage of the present invention is:
1, the dissolubility of the pidotimod sodium of Xing Chenging in water is big and improved the stability of pidotimod.
2, the pidotimod sodium of Xing Chenging make injection the time, pH value is more near human body pH.
The specific embodiment
Following examples are to be used for illustrating the present invention, but do not limit the present invention in any way.
Embodiment 1: injection (specification 2ml:0.1g)
Getting 244.26g pidotimod and 40.01g sodium hydroxide joins in the 3500ml water for injection, stirring makes dissolving fully, add 4g pin charcoal, and continue to stir 20 minutes, filter decarburization, add water for injection to 4485.2ml, the fine straining degerming, packing, 2ml/ props up, in 115 ℃ of 30min that sterilize down, make injection.
Embodiment 2: injection (specification 5ml:0.2g)
Getting 244.26g pidotimod and 40.01g sodium hydroxide joins in the 4000ml water for injection, stirring makes dissolving fully, add 50g sodium chloride and 4g pin charcoal, 60 ℃ were stirred 20 minutes, filtered decarburization, add water for injection to 6106.5ml, the fine straining degerming, packing, 5ml/ props up, in 115 ℃ of 30min that sterilize down, make injection.
Embodiment 3: injection (specification 5ml:0.2g)
Get 244.26g pidotimod and 40.01g sodium hydroxide and join in the 2000ml ethanol, stir and make dissolving fully, filter, concentrating under reduced pressure reclaims ethanol, volatilizes, and gets pressed powder, is pidotimod sodium.
Above-mentioned pidotimod sodium is joined in the 4000ml water for injection, stir and make dissolving fully, add 4g pin charcoal, stirred 20 minutes, filter decarburization, add water for injection to 6100ml, fine straining degerming, packing, 5ml/ props up, and in 115 ℃ of 30min that sterilize down, makes injection.
Embodiment 4: injection powder pin (specification 0.2g)
Get 244.26g pidotimod and 40.01g sodium hydroxide and join in the 2000ml ethanol, stir and make dissolving fully, add 3g pin charcoal, stir 20min, filter decarburization, fine straining, concentrating under reduced pressure reclaims ethanol, volatilize under the aseptic condition, get pressed powder, be pidotimod sodium.
Direct packaging is in cillin bottle under aseptic condition with pidotimod sodium, and every bottled amount is counted 0.2g by pidotimod.Promptly.
Embodiment 5: injection powder pin (specification 0.2g)
Getting 244.26g pidotimod and 40.01g sodium hydroxide joins in the 4000ml water for injection, stirring makes dissolving fully, adds 200g mannitol and 4g pin charcoal, and 60 ℃ were stirred 20 minutes, filter decarburization, add water for injection to 4485ml, the fine straining degerming is counted the 0.2g fill by every bottle in cillin bottle with pidotimod, half tamponade, pre-freeze is 3 hours under-40 ℃ of conditions, is warming up to 30 ℃ by 3～5 ℃/hour then, is incubated dehydration in 3 hours.The lock aluminium lid is taken out in tamponade.Promptly.
Embodiment 5: transfusion (specification 100ml:0.2g)
Get 244.26g pidotimod and 40.01g sodium hydroxide and join in the 5000ml water for injection, stir and make dissolving fully, add 4g pin charcoal, 60 ℃ were stirred 20 minutes, standby after the filtration decarburization;
After getting the 50000ml water for injection dissolving that 1099.17g sodium chloride joins, add 15g pin charcoal, 80 ℃ were stirred 30 minutes, filtered decarburization, and filter is standby to the clarification repeatedly;
Above-mentioned two solution are mixed, and add water for injection to 122130ml, fine straining, packing, the 100ml/ bottle is in 115 ℃ of 45min that sterilize down, promptly.
Claims (8)
1. injection that contains pidotimod sodium is characterized in that the chemical name of the pidotimod sodium that contains in the injection is (R)-3-[(S)-(5-oxygen-2-pyrrolidinyl) carbonyl]-Thiazolidine-4-carboxylic acid sodium.Molecular formula: C
9H
11N
2O
4SNa, molecular weight: 266.28.
2. the injection of a kind of pidotimod sodium according to claim 1 is characterized in that active component pidotimod in this injection is that form with pidotimod sodium exists.
3. the injection of a kind of pidotimod sodium according to claim 1 is characterized in that it is to be used for the infusion solution of intravenously administrable and can to add to 5% glucose or the injection of 0.9% sodium chloride injection, aseptic subpackaged powder pin and lyophilized powder pin.
4. the injection of a kind of pidotimod sodium according to claim 3, the pH value that it is characterized in that the solution of this injection is 5.0～8.0, the best is 6.5～7.5.
5. the injection of a kind of pidotimod sodium according to claim 3 is characterized in that every of this injection or every bottle of amount that contains pidotimod sodium count 20mg～800mg with pidotimod, and the best is 50mg～500mg.
6. the injection of a kind of pidotimod sodium according to claim 2 is characterized in that pidotimod sodium is to be added by pidotimod to make after equimolar sodium hydroxide reacts in The suitable solvent (water or ethanol or the mixed liquor of the two).
7. the injection of a kind of pidotimod sodium according to claim 2 is characterized in that the preparation process of injection includes but not limited to following several:
(1) pidotimod and the sodium hydroxide of getting equimolar amounts joins in an amount of water for injection, stirring makes dissolving fully, adds or do not add acceptable accessories such as mannitol, dextran series, sorbitol, sodium chloride, glucose etc., adds an amount of pin charcoal, and the continuation stirring was incubated 20 minutes in 20 minutes or 60 ℃, filter decarburization, add water for injection to needed amount, fine straining degerming, packing, in 115 ℃ of sterilizations down, make injection or transfusion; Or packing after the fine straining degerming, put in the freeze dryer after the lyophilization, make injection powder pin.
(2) pidotimod and the sodium hydroxide of getting equimolar amounts joins in an amount of ethanol, stirs to make dissolving fully, filters.The concentrating under reduced pressure after drying is flung to ethanol and is promptly got powdered pidotimod sodium.Join again in an amount of water for injection, add or do not add acceptable accessories such as mannitol, dextran series, sorbitol, sodium chloride, glucose etc., add an amount of pin charcoal, and the continuation stirring was incubated 20 minutes in 20 minutes or 60 ℃, the filtration decarburization, add water for injection to needed amount, the fine straining degerming, packing is in 115 ℃ of sterilizations down, make injection or transfusion; Or packing after the fine straining degerming, put in the freeze dryer after the lyophilization, make injection powder pin.
(3) pidotimod and the sodium hydroxide of getting equimolar amounts joins in an amount of ethanol, stirs to make dissolving fully, filters.The concentrating under reduced pressure after drying is flung to ethanol and is promptly got powdered pidotimod sodium.Aseptic subpackaged in cillin bottle, promptly get injection powder pin.
8. a kind of injection that contains pidotimod sodium according to claim 1 is characterized in that 1. this injection is used for the treatment of the last lower respiratory infection (pharyngitis, tracheitis, bronchitis, tonsillitis) of outbreak repeatedly; 2. department of otorhinolaryngology repeated infection (rhinitis, sinusitis, otitis); 3. urinary system infection; 4. gynecological infection; 5. the low clinical patients of cellular immune function after the chemotherapy; 6. specificity and nonspecific immunity defective disorders such as cancers etc.In order to reduce the number of times of acute attack, shorten the course of disease, alleviate the degree of outbreak; Antibiotic auxiliary treatment when also can be used as actute infection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200810056254XA CN101422428A (en) | 2008-01-16 | 2008-01-16 | Injection containing sodium pidotimod |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200810056254XA CN101422428A (en) | 2008-01-16 | 2008-01-16 | Injection containing sodium pidotimod |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101422428A true CN101422428A (en) | 2009-05-06 |
Family
ID=40613457
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200810056254XA Pending CN101422428A (en) | 2008-01-16 | 2008-01-16 | Injection containing sodium pidotimod |
Country Status (1)
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|---|---|
| CN (1) | CN101422428A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101843580A (en) * | 2010-05-24 | 2010-09-29 | 南京威尔曼药物研究所 | Preparation method of pidotimod injection preparation |
| CN112898291A (en) * | 2021-01-27 | 2021-06-04 | 北京金城泰尔制药有限公司沧州分公司 | Preparation method of pidotimod sodium |
-
2008
- 2008-01-16 CN CNA200810056254XA patent/CN101422428A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101843580A (en) * | 2010-05-24 | 2010-09-29 | 南京威尔曼药物研究所 | Preparation method of pidotimod injection preparation |
| CN112898291A (en) * | 2021-01-27 | 2021-06-04 | 北京金城泰尔制药有限公司沧州分公司 | Preparation method of pidotimod sodium |
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Open date: 20090506 |