CN101837126A - Cephalosporin antibacterial combination and medicinal preparation thereof - Google Patents
Cephalosporin antibacterial combination and medicinal preparation thereof Download PDFInfo
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- CN101837126A CN101837126A CN 201010158968 CN201010158968A CN101837126A CN 101837126 A CN101837126 A CN 101837126A CN 201010158968 CN201010158968 CN 201010158968 CN 201010158968 A CN201010158968 A CN 201010158968A CN 101837126 A CN101837126 A CN 101837126A
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Abstract
The invention relates to a cephalosporin antibacterial combination and a medicinal preparation thereof. Cefetamet and Beta-lactamase inhibitor are mixed to prepare the cephalosporin antibacterial combination, additive, such as L-arginine, sodium carbonate or sodium bicarbonate, can be added in the cephalosporin antibacterial combination as well, and the compound medicinal preparation is prepared according to the conventional preparation technique of powder injection or lyophilized powder injection. The invention not only is particularly applicable to the treatment on infections caused by sensitive bacteria, but also has higher antibacterial activity and wider antibacterial spectrum compared with cefetamet antibacterial containing a single ingredient. Meanwhile, since the combination of the Beta-lactamase inhibitor and the cefetamet has a remarkable synergistic antibacterial effect, the problem of cefetamet resistance of clinical pathogenic bacteria is effectively solved.
Description
Technical field
The present invention relates to the antibacterial combination and the pharmaceutical preparation thereof of third generation cephalosporins cefetamet (Cefetamet).
Background technology
Cefetamet is a third generation cephalosporins, to gram positive bacterias such as Streptococcus (except the streptococcus faecalis), streptococcus pneumoniae; And gram-negative bacterias such as escherichia coli, hemophilus influenza, Klebsiella, Salmonella, Shigella, Diplococcus gonorrhoeae all have very strong antibacterial activity, and are especially more obvious to the antibacterial activity of the low Serratia of cephalosporin sensitivity, the positive Bacillus proteus of indole, Enterobacter and citric acid Pseudomonas.Simultaneously, this antibiotic is also very stable to bacteriogenic beta-lactamase.But it is invalid to resistant micro-organism such as false monospore bacillus, mycoplasma, chlamydia, enterococcus.
Up to now, cefetamet only uses as oral antibiotic with its precursor Cefetamet Pivoxil Hydrochloride form.After oral, mainly take off ester and discharge free acid with antibacterial activity through the intestinal wall esterase---cefetamet and playing a role.Along with the prolongation of clinical practice time, some produced drug resistance gradually to its responsive antibacterial originally.Studies show that, in most of the cases, bacterial resistance be since the beta-lactamase of its generation to due to the antibiotic hydrolysis.Therefore, research and develop very necessity of a kind of new cefetamet antibacterials
Summary of the invention
Purpose of the present invention is exactly at the cefetamet antibacterials that contain single component, insensitive to cefetamet fastbacteria and beta-lactamase-producing, the defective that curative effect is not good enough provides a kind of antimicrobial spectrum is wider, antibacterial action is stronger cefetamet antibacterial combination and pharmaceutical preparation thereof.
Pharmaceutical composition of the present invention is mixed by cefetamet and beta-lactamase inhibitor, and the weight ratio of cefetamet and beta-lactamase inhibitor is 1: 1～1: 0.1.
Also can add necessary additives in the described pharmaceutical composition, as L-arginine, sodium carbonate or sodium bicarbonate; Wherein the mol ratio of cefetamet and L-arginine or sodium bicarbonate is 1: 0.8～1: 1.2, and the mol ratio of cefetamet and sodium carbonate is 1: 0.4～1: 0.6.
Described pharmaceutical composition obtains compound medicinal formulation by the conventional preparation technology of injectable powder or lyophilized injectable powder.
Described cefetamet can be cefetamet alkali metal salt or cefetamet inner salt or cefetamet hydrochlorate or cefetamet hydrochloride hydrate.
Described beta-lactamase inhibitor can be sulbactam (Sulbactam) and derivant thereof, or Tazobactam Sodium (Tazobactam) and derivant thereof, or clavulanic acid (Clavulanic acid) and derivant thereof.
Described sulbactam derivant can be sulbactam alkali metal salt, for example sulbactam sodium; The Tazobactam Sodium derivant can be the alkali metal salt of Tazobactam Sodium, for example sodium-tazobactam; The clavulanic acid derivant can be the alkali metal salt of clavulanic acid, for example clavulanate potassium.
Drug combination preparation of the present invention is generally drug administration by injection, can do intravenous injection, intravenous drip or intramuscular injection.Cefetamet suitable accumulated dose every day is 1500～6000mg, every day two or three administrations.
Clinical application it should be noted, has allergies person to forbid this product to penicillin or cephalosporins or beta-lactamase inhibitor.
The pharmaceutical composition of the present invention that mixes by effective ingredient antibiotic cefetamet and beta-lactamase inhibitor, not only be specially adapted to treatment to the infected by microbes of beta-lactam antibiotic sensitivity, and with respect to the cefetamet antibacterials that contain single component also have stronger antibacterial activity, antimicrobial spectrum is wider.As can be used for responsive microbial respiratory tract infection (comprising pneumonia and bronchitis), ear, nose, throat infect (as otitis media, sinusitis, pharyngitis, tonsillitis etc.), urinary tract infection [comprising non-complex urinary tract infection, complexity urinary tract infection (as pyelonephritis), male's acute gonococcal urethritis etc.], skin and skin soft-tissue infection, abdominal cavity infection (comprising peritonitis and biliary tract infection), department of obstetrics and gynecology infection etc.
Below by in vitro tests (mensuration of minimum inhibitory concentration), the pharmacological effect of pharmaceutical composition of the present invention is described further.
The mensuration of pharmaceutical composition minimum inhibitory concentration MIC: adopt the plate doubling dilution.With the bacterium liquid dilution of incubated overnight, be inoculated on the agar plate that contains serial given the test agent with multiple spot inoculation instrument, inoculum density is 10
5CFU/ml, 37 ℃ of incubated overnight are observed and are suppressed the antibacterial production, do not see that with naked eyes the given the test agent concentration of bacterial clump growth is MIC.The results are shown in Table 1,2 and 3.
Table 1 cefetamet and cefetamet/sulbactam are to G
-The MIC of bacterium (μ g/mL)
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.50 | ??2 | |
| ??CFT/SBT(2∶1) | ??0.06～64 | ??0.25 | ??4 | |
| ??CFT/SBT(4∶1) | ??0.12～128 | ??0.25 | ??32 | |
| ??CFT/SBT(8∶1) | ??0.12～128 | ??0.50 | ??16 | |
| ??CFT/SBT(10∶1) | ??0.12～128 | ??0.50 | ??32 | |
| ??Klebsiella?pneumoniae(15) | ||||
| ??CFT | ??0.06～128 | ??0.12 | ??64 | |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.06 | ??32 | |
| ??CFT/SBT(2∶1) | ??0.06～128 | ??0.12 | ??32 | |
| ??CFT/SBT(4∶1) | ??0.12～64 | ??0.25 | ??64 |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.50 | ??2 | |
| ??CFT/SBT(8∶1) | ??0.12～128 | ??1 | ??64 | |
| ??CFT/SBT(10∶1) | ??0.12～128 | ??1 | ??64 | |
| ??Shigella?sp.(21) | ||||
| ??CFT | ??0.06～8 | ??0.50 | ??4 | |
| ??CFT/SBT(1∶1) | ??0.06～2 | ??0.12 | ??0.50 | |
| ??CFT/SBT(2∶1) | ??0.06～4 | ??0.25 | ??0.50 | |
| ??CFT/SBT(4∶1) | ??0.12～4 | ??0.50 | ??1 | |
| ??CFT/SBT(8∶1) | ??0.12～16 | ??2 | ??8 | |
| ??CFT/SBT(10∶1) | ??0.12～16 | ??2 | ??8 | |
| ??Salmonella?typhe(21) | ||||
| ??CFT | ??0.06～4 | ??1 | ??2 | |
| ??CFT/SBT(1∶1) | ??0.125～0.50 | ??0.12 | ??0.25 | |
| ??CFT/SBT(2∶1) | ??0.06～1 | ??0.06 | ??1 | |
| ??CFT/SBT(4∶1) | ??0.50～2 | ??1 | ??2 | |
| ??CFT/SBT(8∶1) | ??0.50～8 | ??2 | ??8 | |
| ??CFT/SBT(10∶1) | ??0.50～8 | ??2 | ??8 | |
| ??Proteus?vulgaris(15) | ||||
| ??CFT | ??0.12～128 | ??2 | ??64 | |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.25 | ??8 | |
| ??CFT/SBT(2∶1) | ??0.12～128 | ??0.50 | ??4 | |
| ??CFT/SBT(4∶1) | ??0.06～128 | ??2 | ??16 | |
| ??CFT/SBT(8∶1) | ??0.25～128 | ??2 | ??16 |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.50 | ??2 | |
| ??CFT/SBT(10∶1) | ??0.25～128 | ??2 | ??16 | |
| ??Enterobacter?sp.(16) | ||||
| ??CFT | ??0.06～128 | ??64 | ??128 | |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??16 | ??32 | |
| ??CFT/SBT(2∶1) | ??0.06～128 | ??32 | ??32 | |
| ??CFT/SBT(4∶1) | ??0.50～128 | ??32 | ??64 | |
| ??CFT/SBT(8∶1) | ??0.25～128 | ??32 | ??64 | |
| ??CFT/SBT(10∶1) | ??0.25～128 | ??32 | ??64 | |
| ??Citrobacter?freund(15) | ||||
| ??CFT | ??0.25～128 | ??2 | ??32 | |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.12 | ??8 | |
| ??CFT/SBT(2∶1) | ??0.12～128 | ??0.50 | ??4 | |
| ??CFT/SBT(4∶1) | ??0.50～128 | ??1 | ??64 | |
| ??CFT/SBT(8∶1) | ??1～128 | ??2 | ??32 | |
| ??CFT/SBT(10∶1) | ??1～128 | ??2 | ??32 | |
| ??Serratia?marcesce(13) | ||||
| ??CFT | ??0.25～128 | ??8 | ??64 | |
| ??CFT/SBT(1∶1) | ??0.12～128 | ??0.50 | ??2 | |
| ??CFT/SBT(2∶1) | ??0.06～128 | ??0.25 | ??4 | |
| ??CFT/SBT(4∶1) | ??1～128 | ??1 | ??2 | |
| ??CFT/SBT(8∶1) | ??0.50～128 | ??16 | ??64 | |
| ??CFT/SBT(10∶1) | ??0.50～128 | ??16 | ??64 |
| ??CFT/SBT(1∶1) | ??0.06～128 | ??0.50 | ??2 | |
| ??Pseudomonas?aeruginl(20) | ||||
| ??CFT | ??8～128 | ??8 | ??64 | |
| ??CFT/SBT(1∶1) | ??0.50～128 | ??2 | ??8 | |
| ??CFT/SBT(2∶1) | ??2～128 | ??4 | ??16 | |
| ??CFT/SBT(4∶1) | ??4～128 | ??16 | ??64 | |
| ??CFT/SBT(8∶1) | ??2～128 | ??8 | ??128 | |
| ??CFT/SBT(10∶1) | ??2～128 | ??8 | ??128 |
CFT: cefetamet; SBT: sulbactam.
Table 2 cefetamet and cefetamet/sulbactam are to G
+The MIC of bacterium (μ g/mL)
| ??CFT/SBT(8∶1) | ??0.50～32 | ??16 | ??32 | |
| ??CFT/SBT(10∶1) | ??0.50～32 | ??16 | ??32 | |
| ??MSSCN(10) | ??CFT | ??0.50～32 | ??1 | ??4 |
| ??CFT/SBT(1∶1) | ??0.06～8 | ??0.25 | ??4 | |
| ??CFT/SBT(2∶1) | ??0.12～16 | ??0.5 | ??4 | |
| ??CFT/SBT(4∶1) | ??0.50～16 | ??8 | ??16 | |
| ??CFT/SBT(8∶1) | ??0.25～32 | ??16 | ??32 | |
| ??CFT/SBT(10∶1) | ??0.25～32 | ??16 | ??32 |
CFT: cefetamet; SBT: sulbactam; MRSA: methicillin-resistant staphylococcus aureus; MSSA: MSSA; MRSCN: methicillin-resistant coagulase negative staphylococcus; MSSCN: coagulase negative staphylococcus.
Table 3 cefetamet and cefetamet/Tazobactam Sodium are to G
-The MIC of bacterium (μ g/mL)
| ??CFT/TAZ(8∶1) | ??0.06～128 | ??16 | ??128 | |
| ??CFT/TAZ(10∶1) | ??0.06～128 | ??16 | ??128 | |
| ??Enterobacter?cloacae.(11) | ||||
| ??CFT | ??0.125～128 | ??128 | ??＞128 | |
| ??CFT/TAZ(1∶1) | ??0.03～128 | ??8 | ??64 | |
| ??CFT/TAZ(2∶1) | ??0.03～128 | ??8 | ??64 | |
| ??CFT/TAZ(4∶1) | ??0.25～128 | ??16 | ??64 | |
| ??CFT/TAZ(8∶1) | ??0.25～128 | ??16 | ??128 |
| ??CFT/TAZ(8∶1) | ??0.06～128 | ??16 | ??128 | |
| ??CFT/TAZ(10∶1) | ??0.25～128 | ??32 | ??128 | |
| ??Acinetobacter?baumannii(15) | ||||
| ??CFT | ??0.25～128 | ??＞128 | ??＞128 | |
| ??CFT/TAZ(1∶1) | ??0.125～128 | ??16 | ??64 | |
| ??CFT/TAZ(2∶1) | ??0.125～128 | ??16 | ??64 | |
| ??CFT/TAZ(4∶1) | ??0.125～128 | ??64 | ??128 | |
| ??CFT/TAZ(8∶1) | ??0.125～128 | ??64 | ??128 | |
| ??CFT/TAZ(10∶1) | ??0.25～128 | ??64 | ??128 | |
| ??Serratia(13) | ||||
| ??CFT | ??0.5～128 | ??32 | ??128 | |
| ??CFT/TAZ(1∶1) | ??0.125～128 | ??1 | ??16 | |
| ??CFT/TAZ(2∶1) | ??0.03～128 | ??2 | ??16 | |
| ??CFT/TAZ(4∶1) | ??0.03～128 | ??2 | ??32 | |
| ??CFT/TAZ(8∶1) | ??0.03～128 | ??2 | ??32 | |
| ??CFT/TAZ(10∶1) | ??0.25～128 | ??4 | ??64 | |
| ??Proteus(21) | ||||
| ??CFT | ??0.5～128 | ??8 | ??64 | |
| ??CFT/TAZ(1∶1) | ??0.03～128 | ??2 | ??16 | |
| ??CFT/TAZ(2∶1) | ??0.03～128 | ??4 | ??16 | |
| ??CFT/TAZ(4∶1) | ??0.06～128 | ??4 | ??32 | |
| ??CFT/TAZ(8∶1) | ??0.06～128 | ??8 | ??32 | |
| ??CFT/TAZ(10∶1) | ??0.5～128 | ??8 | ??64 | |
| ??Morganella?morganii(16) | ||||
| ??CFT | ??2～128 | ??64 | ??128 | |
| ??CFT/TAZ(1∶1) | ??0.125～128 | ??2 | ??64 | |
| ??CFT/TAZ(2∶1) | ??0.125～128 | ??2 | ??128 | |
| ??CFT/TAZ(4∶1) | ??0.5～128 | ??4 | ??128 |
| ??CFT/TAZ(8∶1) | ??0.06～128 | ??16 | ??128 | |
| ??CFT/TAZ(8∶1) | ??0.5～128 | ??4 | ??128 | |
| ??CFT/TAZ(10∶1) | ??0.5～128 | ??4 | ??＞128 |
CFT: cefetamet; TAZ: Tazobactam Sodium.
---this shows that the advantage that the present invention gives prominence to shows:
Because mixing with cefetamet, the beta-lactamase inhibitor in the pharmaceutical composition of the present invention has significant synergism, thereby can effectively suppress the activity of beta-lactamase, help its antibacterial action of the stable performance of cefetamet, can obviously strengthen the antibacterial activity and the antimicrobial spectrum of cefetamet, thereby solved at present increasing antibacterial effectively to the drug resistance problem that cefetamet produces, strengthened the clinical efficacy of medicine cefetamet.
The specific embodiment
Embodiment 1: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sulbactam sodium 0.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 2: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sulbactam sodium 1.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 3: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sulbactam sodium 2.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 4: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sulbactam sodium 0.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 5: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sodium-tazobactam 0.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 6: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sodium-tazobactam 1.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 7: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sodium-tazobactam 2.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 8: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with sodium-tazobactam 0.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 9: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with clavulanate potassium 0.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 10: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with clavulanate potassium 1.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 11: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with clavulanate potassium 2.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 12: under aseptic cleaning condition, Ro 15-8074/001 (by free acid) 2.5kg is mixed with clavulanate potassium 0.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 13: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sulbactam sodium 0.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 14: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sulbactam sodium 1.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 15: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sulbactam sodium 2.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 16: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sulbactam sodium 0.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 17: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sodium-tazobactam 0.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 18: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sodium-tazobactam 1.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 19: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sodium-tazobactam 2.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 20: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with sodium-tazobactam 0.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 21: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with clavulanate potassium 0.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 22: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with clavulanate potassium 1.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 23: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with clavulanate potassium 2.5kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 24: under aseptic cleaning condition, hydrochloric acid cefetamet (by free acid) 2.5kg is mixed with clavulanate potassium 0.25kg (by free acid), press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 25: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 0.5kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 26: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 1.25kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 27: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 2.5kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 28: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 0.25kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 29: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 0.5kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 30: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 1.25kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 31: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 2.5kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 32: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 0.25kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 33: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 0.5kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 34: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 1.25kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 35: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 2.5kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 36: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 0.25kg (by free acid) and L-arginine 1.09kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 37: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 0.5kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 38: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 1.25kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 39: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 2.5kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 40: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 0.25kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 41: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 0.5kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 42: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 1.25kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 43: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 2.5kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 44: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 0.25kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 45: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 0.5kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 46: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 1.25kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 47: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 2.5kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 48: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 0.25kg (by free acid) and sodium carbonate 0.33kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 49: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 0.5kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 50: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 1.25kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 51: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 2.5kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 52: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sulbactam sodium 0.25kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 53: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 0.5kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 54: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 1.25kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 55: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 2.5kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 56: under aseptic cleaning condition, cefetamet 2.5kg is mixed with sodium-tazobactam 0.25kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 57: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 0.5kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 58: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 1.25kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 59: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 2.5kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Embodiment 60: under aseptic cleaning condition, cefetamet 2.5kg is mixed with clavulanate potassium 0.25kg (by free acid) and sodium bicarbonate 0.52kg, press the preparation of injection procedure operation, prepare 10000 of injectable powder of the present invention.
Claims (8)
1. a cephalosporin antibacterial combination is characterized in that being mixed by cefetamet and beta-lactamase inhibitor, and the weight ratio of cefetamet and beta-lactamase inhibitor is 1: 1～1: 0.1.
2. cephalosporins medicine compositions according to claim 1, it is characterized in that also being added with in this pharmaceutical composition L-arginine, sodium carbonate or sodium bicarbonate, wherein the mol ratio of cefetamet and L-arginine or sodium bicarbonate is 1: 0.8～1: 1.2, and the mol ratio of cefetamet and sodium carbonate is 1: 0.4～1: 0.6.
3. cephalosporin antibacterial combination according to claim 1 is characterized in that described cefetamet is specially cefetamet alkali metal salt, cefetamet inner salt, cefetamet hydrochlorate or cefetamet hydrochloride hydrate.
4. cephalosporin antibacterial combination according to claim 1 is characterized in that described beta-lactamase inhibitor is selected from sulbactam and derivant thereof, Tazobactam Sodium and derivant thereof, or clavulanic acid and derivant thereof.
5. according to claim 1 or 4 described cephalosporin antibacterial combinations, it is characterized in that described sulbactam derivant is the sulbactam alkali metal salt.
6. according to claim 1 or 4 described cephalosporin antibacterial combinations, it is characterized in that described Tazobactam Sodium derivant is the Tazobactam Sodium alkali metal salt.
7. according to claim 1 or 4 described cephalosporin antibacterial combinations, it is characterized in that described clavulanic acid derivant is the clavulanic acid alkali metal salt.
8. cephalosporin antibacterial combination according to claim 1 and 2 is characterized in that this pharmaceutical composition obtains compound medicinal formulation by the conventional preparation technology of injectable powder or lyophilized injectable powder.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104876947A (en) * | 2015-05-06 | 2015-09-02 | 山东罗欣药业集团股份有限公司 | Cefetamet pivoxil hydrochloride hydrate crystals and dispersible tablet thereof |
| CN104873501A (en) * | 2015-05-15 | 2015-09-02 | 苗怡文 | Sulbactam sodium composition for treating infectious diseases |
| WO2022198378A1 (en) * | 2021-03-22 | 2022-09-29 | 广州新创忆药物临床研究有限公司 | β-LACTAMASE INHIBITOR COMPOSITION WITH STABLE QUALITY, USE THEREOF AND METHOD THEREFOR |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1565456A (en) * | 2003-06-14 | 2005-01-19 | 张哲峰 | Cefepime compound antibacterial drugs |
| CN1616100A (en) * | 2004-10-14 | 2005-05-18 | 崔晓廷 | Beta-lactam antibiotic compound oral preparation and its preparing method |
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- 2010-04-27 CN CN 201010158968 patent/CN101837126A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1565456A (en) * | 2003-06-14 | 2005-01-19 | 张哲峰 | Cefepime compound antibacterial drugs |
| CN1616100A (en) * | 2004-10-14 | 2005-05-18 | 崔晓廷 | Beta-lactam antibiotic compound oral preparation and its preparing method |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104876947A (en) * | 2015-05-06 | 2015-09-02 | 山东罗欣药业集团股份有限公司 | Cefetamet pivoxil hydrochloride hydrate crystals and dispersible tablet thereof |
| CN104873501A (en) * | 2015-05-15 | 2015-09-02 | 苗怡文 | Sulbactam sodium composition for treating infectious diseases |
| WO2022198378A1 (en) * | 2021-03-22 | 2022-09-29 | 广州新创忆药物临床研究有限公司 | β-LACTAMASE INHIBITOR COMPOSITION WITH STABLE QUALITY, USE THEREOF AND METHOD THEREFOR |
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