CN101590061B - Medicinal composition of cefotetan disodium - Google Patents
Medicinal composition of cefotetan disodium Download PDFInfo
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- CN101590061B CN101590061B CN2009101068335A CN200910106833A CN101590061B CN 101590061 B CN101590061 B CN 101590061B CN 2009101068335 A CN2009101068335 A CN 2009101068335A CN 200910106833 A CN200910106833 A CN 200910106833A CN 101590061 B CN101590061 B CN 101590061B
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Abstract
The invention discloses a medicinal composition of cefotetan disodium, which comprises the cefotetan disodium, and also comprises minor ingredients; the percentage by mass of the cefotetan disodium is 50 to 99 percent; and the percentage by mass of the minor ingredients is 1 to 50 percent. The medicinal composition of the cefotetan disodium is added with the minor ingredients capable of strengthening the stability of the cefotetan disodium to inhibit the quick degradation of the cefotetan disodium when the cefotetan disodium meets water in the processes of production, storage and use and improve the stability of the cefotetan disodium, so that a high-efficiency and stable medicinal composition product of the cefotetan disodium is obtained.
Description
Technical field
The present invention relates to a kind of medicine, relate in particular to a kind of pharmaceutical composition of Cefotetan Disodium of injection.
Background technology
Existing more at present cephalosporins listing is widely used in clinical, and the treatment that catches is played an important role.But analyze, the cephalosporins that has gone on the market mostly is cephalosporin (Cephalosporin) class.Cefotaxime from the cefalexin of the first generation, cefadroxil to a new generation, ceftriaxone, cefpirome etc., though each respectively has characteristics for cephalosporins, but such antibiotic common limit that lacks is a beta-lactamase instability to some Production by Bacteria, therefore can produce the therapeutic effect that infects due to the bacterial strain of beta-lactamase to some and be affected.After in streptomycete (S.Lactamdurans), finding cephamycin C (Cephamycin C), transform side chain and obtain some cephamycin-type antibiotic medicines through synthetic modification.This type of antibiotic structurally is different from cephalosporins, a trans methoxyl group is arranged on 7 carbon atoms, though its antibacterial action is lower than the first generation cephalosporin class to the effect of gram positive bacteria, but to gram negative bacteria antibacterial action excellence, anti-beta-lactamase (comprising the gram negative bacteria beta-lactamase) performance is strong.This has very important meaning clinically.
Cefotetan is a kind of semi-synthetic novel cephamycin-type antibiotic of the wild mycin G of fawn that is produced by Streptomyces Oganonensis.It has the substituent cephalosporin structure of 7 α-methylamino, this structural change makes the effect of its anti-beta-lactamase strengthen, and antibacterial activity is more extensive, particularly anti-gram negative bacteria, strong than the first generation and second generation cephalosporin, and demonstrate good anti-anaerobic activity.Can resist most of beta-lactamases, as stronger than cefmetazole, cefoxitin to the antibacterial action of escherichia coli, Citrobacter, Klebsiella, husky bacterium Pseudomonas, Proteus, hemophilus influenza.Antibacterial action to gram positive bacteria such as staphylococcus, Streptococcus is more weak.To the equal stabilizer pole of various bacteriogenic beta lactamases, very strong antibacterial action is also arranged to producing the beta lactamase bacterial strain.In addition, after the cefotetan injection, have the blood drug level of higher and lasting long period and in skin, tonsil, sputum, uterus, ovary, cerebrospinal fluid, amniotic fluid, distribute, but distribution is less in milk.Cefotetan is discharged in the main urine certainly in vivo not by metabolism.Be used for shallow secondary infection, tonsillitis, respiratory system infection, empyema, biliary tract infection, peritonitis, urinary tract infection, gynecological infections etc. such as responsive microbial septicemia, burn and operative incision.
Limit or technologic difficulty owing to raw material at present, relatively weaker to the antibiotic exploitation of cephamycin-type.The Cefotetan Disodium curative effect is through clinical approval, but because Cefotetan Disodium salt is very unstable, meeting the water capacity in production, storage and use easily degrades, related substance can increase sharply, cause product defective, can not use, this gives and produces, stores and uses and all brought great difficulty.
Therefore, prior art haves much room for improvement and improves.
Summary of the invention
The objective of the invention is to,, provide a kind of Cefotetan Disodium in production, storage and use, to be difficult for degrading the pharmaceutical composition of the stable Cefotetan Disodium that is used to inject at above problems of the prior art.
The invention provides a kind of pharmaceutical composition of Cefotetan Disodium, its composition for injection for adopting freeze drying technology to make comprises Cefotetan Disodium, and wherein, described compositions also comprises adjuvant; Wherein, the mass percent of described Cefotetan Disodium is 50%～99%; The mass percent of described adjuvant is 1%～50%; Described adjuvant is the mixture of glucose and mannitol.
Compositions of the present invention, wherein, the mass percent of described Cefotetan Disodium is 60%～80%.
Compositions of the present invention, wherein, the mass percent of described adjuvant is 20%～40%.
Compositions of the present invention, wherein, the mass percent of described Cefotetan Disodium is 65%～75%.
Compositions of the present invention, wherein, the mass percent of described adjuvant is 25%～35%.
The present invention is by adding the adjuvant that can strengthen Cefotetan Disodium stability in the pharmaceutical composition of Cefotetan Disodium, suppress the rapid degraded Cefotetan Disodium is met water in production, storage and use after, improve Cefotetan Disodium stability, thereby obtained the pharmaceutical composition product of efficient, stable Cefotetan Disodium.
Below preferred embodiment of the present invention is described in detail.
In the present embodiment, the preparation technology that described pharmaceutical composition all adopts is freeze drying technology or non-freeze drying technology, specifically be meant Cefotetan Disodium is dissolved in the aqueous solution of adjuvant, add needle-use activated carbon and stir and remove by filter active carbon, aseptic filtration, lyophilizing manufactured goods in the freezer dryer are put in fill, or Cefotetan Disodium raw material and adjuvant are directly mixed packing make finished product.
In the compositions of the Cefotetan Disodium in the present embodiment, the dosage of demand when the amount of Cefotetan Disodium depends on drug use in the contained compositions accounts for 50%～99% of prescription gross weight, is preferably 60%～80%, more preferably 65%～75%.
The specific embodiment
Adjuvant in the present embodiment can in sodium benzoate, lactose, glucose, mannitol, sodium chloride, sodium bicarbonate or the sodium carbonate one or more etc.The preferred glucose that adopts is as adjuvant.Through a large amount of verification experimental verifications, glucose can significantly strengthen the stability of Cefotetan Disodium, all can obviously strengthen the stability of Cefotetan Disodium in water when mixing with above-mentioned other adjuvants when independent use glucose or with glucose, its consumption changes along with the variation of the amount of Cefotetan Disodium, general consumption is to account for 1%～50% of compositions gross weight, be preferably 20%～40%, more preferably 25%～35%.
Below provide 8 groups of specific embodiments, with the optimal component example of pharmaceutical composition that cefalexin provided by the present invention is described.In following examples, single dose comprises Cefotetan Disodium 500mg to 1000mg.
Embodiment 1:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 1 below.
The composition component one of table 1 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 500 | 50 |
| Glucose | 500 | 50 |
According to above component, adopt freeze drying technology to make the 500mg/ bottle Cefotetan Disodium of injection.Detailed process is: Cefotetan Disodium is dissolved in the aqueous solution of glucose, adds needle-use activated carbon and stir, and remove by filter active carbon, carry out aseptic filtration again, fill places the freezer dryer lyophilizing then, makes finished product.
After the prescription dosing, cross leaching filtrate and detect related substance, the prescription that does not add glucose compares, the result shows that the related substance of the prescription dosing rear filtrate that does not add glucose is 5.4%, and the related substance that adds glucose is 3.5%, and visible glucose can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 2:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 2 below.
The composition component two of table 2 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 500 | 60 |
| Glucose | 333 | 40 |
According to above component, adopt freeze drying technology to make cefotetan for inj disodium 500mg/ bottle.Detailed process is: Cefotetan Disodium is dissolved in the aqueous solution of glucose, adds needle-use activated carbon and stir, and remove by filter active carbon, carry out aseptic filtration again, fill places the freezer dryer lyophilizing then, makes finished product.
After the prescription dosing, cross leaching filtrate and detect related substance, the prescription that does not add glucose compares, the result shows that the related substance of the prescription dosing rear filtrate that does not add glucose is 5.4%, and the related substance that adds glucose is 3.7%, and visible glucose can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 3:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 3 below.
The composition component three of table 3 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 500 | 65 |
| Glucose | 233 | 35 |
According to above component, adopt freeze drying technology to make cefotetan for inj disodium 500mg/ bottle.Detailed process is: Cefotetan Disodium is dissolved in the aqueous solution of glucose, adds needle-use activated carbon and stir, and remove by filter active carbon, carry out aseptic filtration again, fill places the freezer dryer lyophilizing then, makes finished product.
After the prescription dosing, cross leaching filtrate and detect related substance, the prescription that does not add glucose compares, the result shows that the related substance of the prescription dosing rear filtrate that does not add glucose is 5.4%, and the related substance that adds glucose is 3.2%, and visible glucose can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 4:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 4 below.
The composition component four of table 4 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 500 | 70.03 |
| Glucose | 143 | 20.03 |
| Mannitol | 71 | 9.94 |
According to above component, adopt freeze drying technology to make cefotetan for inj disodium 500mg/ bottle.Detailed process is: Cefotetan Disodium is dissolved in the aqueous solution of glucose and mannitol, adds needle-use activated carbon and stir, and remove by filter active carbon, carry out aseptic filtration again, fill places the freezer dryer lyophilizing then, makes finished product.
After the prescription dosing, cross leaching filtrate and detect related substance, the prescription that does not add glucose and mannitol compares, the result show do not add glucose and mannitol the related substance of prescription dosing rear filtrate be 5.4%, and the related substance that adds glucose and mannitol is 3.8%, and visible glucose and mannitol can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 5:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 5 below.
The composition component five of table 5 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 500 | 75 |
| Glucose | 100 | 15 |
| Lactose | 66.7 | 10 |
According to above component, adopt freeze drying technology to make cefotetan for inj disodium 500mg/ bottle.Detailed process is: Cefotetan Disodium is dissolved in the aqueous solution of glucose and lactose, adds needle-use activated carbon and stir, and remove by filter active carbon, carry out aseptic filtration again, fill places the freezer dryer lyophilizing then, makes finished product.
After the prescription dosing, cross leaching filtrate and detect related substance, the prescription that does not add glucose and lactose compares, the result shows that the related substance of the prescription dosing rear filtrate that does not add glucose and lactose is 5.4%, and the related substance that adds glucose and lactose is 3.8%, and visible glucose and lactose can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 6:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 6 below.
The composition component six of table 6 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 1000 | 80 |
| Glucose | 187.5 | 15 |
| Sodium chloride | 62.5 | 5 |
According to above component, adopt aseptic subpackaged technology to make cefotetan for inj disodium 1000mg/ bottle.Detailed process is: Cefotetan Disodium raw material and glucose, sodium chloride adjuvant are directly mixed packing, make finished product.
The sample dissolution that makes is detected related substance in water for injection, the prescription that does not add glucose and sodium chloride compares, the result shows that the prescription do not add glucose and sodium chloride is dissolved in that related substance is 5.7% behind the water for injection, and the related substance that adds glucose and sodium chloride is 4.0%, and visible glucose and sodium chloride can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 7:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 6 below.
The composition component seven of table 7 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 1000 | 90 |
| Glucose | 100 | 9 |
| Sodium bicarbonate | 11 | 1 |
According to above component, adopt aseptic subpackaged technology to make cefotetan for inj disodium 1000mg/ bottle.Detailed process is: Cefotetan Disodium raw material and glucose, sodium bicarbonate adjuvant are directly mixed packing, make finished product.
The sample dissolution that makes is detected related substance in water for injection, the prescription that does not add glucose and sodium bicarbonate compares, the result shows that the prescription do not add glucose and sodium bicarbonate is dissolved in that related substance is 5.7% behind the water for injection, and the related substance that adds glucose and sodium bicarbonate is 4.2%, and visible glucose and sodium bicarbonate can significantly strengthen the stability of Cefotetan Disodium in water.
Embodiment 8:
In the present embodiment, the concrete content of each composition of the pharmaceutical composition of Cefotetan Disodium is as shown in table 6 below.
The composition component eight of table 8 Cefotetan Disodium
| Component | Dosage (mg) | Account for compositions gross mass percentage ratio (%) |
| Cefotetan Disodium | 1000 | 99 |
| Glucose | 10.1 | 1 |
According to above component, adopt aseptic subpackaged technology to make cefotetan for inj disodium 1000mg/ bottle.Detailed process is: Cefotetan Disodium raw material and glucose adjuvant are directly mixed packing, make finished product.
The sample dissolution that makes is detected related substance in water for injection, the prescription that does not add glucose compares, the result shows that the prescription do not add glucose is dissolved in that related substance is 5.7% behind the water for injection, and the related substance that adds glucose is 4.4%, and visible glucose can significantly strengthen the stability of Cefotetan Disodium in water.
The pharmaceutical composition of the Cefotetan Disodium in the embodiment of the invention exists with the form of loose block or amorphous solid, and with the form administration that intravenous injection or quiet notes instil, single dose comprises Cefotetan Disodium 500mg to 1000mg.Adult's dosage is generally 1～2g on the one, 2 times on the one; Child dose is that every day is by body weight 40～60mg/kg, 2～3 times on the one.
In sum, the present invention is by adding the adjuvant that can strengthen Cefotetan Disodium stability in the pharmaceutical composition of Cefotetan Disodium, suppress to degrade rapidly Cefotetan Disodium is met water in production, storage and use after, improve the stability of Cefotetan Disodium, thereby obtained the pharmaceutical composition product of efficient, stable Cefotetan Disodium.
Should be appreciated that above-mentioned description at specific embodiment is comparatively detailed, can not therefore think the restriction to scope of patent protection of the present invention, scope of patent protection of the present invention should be as the criterion with claims.
Claims (5)
1. the pharmaceutical composition of a Cefotetan Disodium, its composition for injection for adopting freeze drying technology to make comprises Cefotetan Disodium, it is characterized in that described compositions also comprises adjuvant; Wherein, the mass percent of described Cefotetan Disodium is 50%～99%; The mass percent of described adjuvant is 1%～50%; Described adjuvant is the mixture of glucose and mannitol.
2. compositions as claimed in claim 1 is characterized in that, the mass percent of described adjuvant is 20%～40%.
3. compositions as claimed in claim 2 is characterized in that, the mass percent of described Cefotetan Disodium is 60%～80%.
4. compositions as claimed in claim 1 is characterized in that, the mass percent of described Cefotetan Disodium is 65%～75%.
5. compositions as claimed in claim 4 is characterized in that, the mass percent of described adjuvant is 25%～35%.
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| CN103724359B (en) * | 2012-10-16 | 2016-12-21 | 深圳信立泰药业股份有限公司 | A kind of amorphous cefotetan acid and prepared the method for Cefotetan Disodium and containing the pharmaceutical composition of this Cefotetan Disodium by it |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1034670A (en) * | 1988-01-18 | 1989-08-16 | 赫彻斯特股份公司 | The stable composition that cephalosporins derivatives and the common drying of a kind of stabilizing agent are made the stable method of this derivant and contain cephalosporins derivatives |
| CN101129382A (en) * | 2006-08-25 | 2008-02-27 | 天津和美生物技术有限公司 | Antibiotic compound containing beta-lactam antibiotic and buffering component |
| CN101129381A (en) * | 2006-08-25 | 2008-02-27 | 天津和美生物技术有限公司 | Antibiotic compound containing beta-lactam antibiotic and ion chelating agent |
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2009
- 2009-04-14 CN CN2009101068335A patent/CN101590061B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1034670A (en) * | 1988-01-18 | 1989-08-16 | 赫彻斯特股份公司 | The stable composition that cephalosporins derivatives and the common drying of a kind of stabilizing agent are made the stable method of this derivant and contain cephalosporins derivatives |
| CN101129382A (en) * | 2006-08-25 | 2008-02-27 | 天津和美生物技术有限公司 | Antibiotic compound containing beta-lactam antibiotic and buffering component |
| CN101129381A (en) * | 2006-08-25 | 2008-02-27 | 天津和美生物技术有限公司 | Antibiotic compound containing beta-lactam antibiotic and ion chelating agent |
Non-Patent Citations (1)
| Title |
|---|
| A. NOVELLI et al.The penetration of intramuscular cefotetan disodium into human extra-vascular fluid and maternal milk secretion.CHEMIOTERAPIA.1983,2(5),337-342. * |
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