CN1582942A - Cefuroxime sodium compound preparation - Google Patents
Cefuroxime sodium compound preparation Download PDFInfo
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- CN1582942A CN1582942A CN 200410048080 CN200410048080A CN1582942A CN 1582942 A CN1582942 A CN 1582942A CN 200410048080 CN200410048080 CN 200410048080 CN 200410048080 A CN200410048080 A CN 200410048080A CN 1582942 A CN1582942 A CN 1582942A
- Authority
- CN
- China
- Prior art keywords
- cefuroxime
- sodium
- tazobactam
- beta
- compositions
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229960000534 cefuroxime sodium Drugs 0.000 title claims abstract description 29
- URDOHUPGIOGTKV-JTBFTWTJSA-M Cefuroxime sodium Chemical compound [Na+].N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C([O-])=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 URDOHUPGIOGTKV-JTBFTWTJSA-M 0.000 title claims abstract description 25
- 238000002360 preparation method Methods 0.000 title claims abstract description 17
- JFPVXVDWJQMJEE-IZRZKJBUSA-N cefuroxime Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(O)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 JFPVXVDWJQMJEE-IZRZKJBUSA-N 0.000 claims abstract description 32
- 229960001668 cefuroxime Drugs 0.000 claims abstract description 28
- 239000003781 beta lactamase inhibitor Substances 0.000 claims abstract description 22
- 229940126813 beta-lactamase inhibitor Drugs 0.000 claims abstract description 22
- 150000003839 salts Chemical class 0.000 claims abstract description 22
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 claims abstract description 22
- 230000000844 anti-bacterial effect Effects 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 25
- 229960003865 tazobactam Drugs 0.000 claims description 15
- 239000007924 injection Substances 0.000 claims description 10
- 238000002347 injection Methods 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 5
- 239000000890 drug combination Substances 0.000 claims description 3
- 208000035143 Bacterial infection Diseases 0.000 claims description 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims 2
- 235000015424 sodium Nutrition 0.000 claims 2
- 229940122601 Esterase inhibitor Drugs 0.000 claims 1
- 239000002329 esterase inhibitor Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 abstract description 5
- 239000000843 powder Substances 0.000 description 21
- 229940090044 injection Drugs 0.000 description 9
- NDIURPSCHWTXDC-UHFFFAOYSA-N 2-(4,5-dimethoxy-2-nitrophenyl)acetohydrazide Chemical compound COC1=CC(CC(=O)NN)=C([N+]([O-])=O)C=C1OC NDIURPSCHWTXDC-UHFFFAOYSA-N 0.000 description 7
- 239000003814 drug Substances 0.000 description 7
- 229960000373 tazobactam sodium Drugs 0.000 description 7
- 239000002904 solvent Substances 0.000 description 5
- 102000004190 Enzymes Human genes 0.000 description 4
- 108090000790 Enzymes Proteins 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 238000001228 spectrum Methods 0.000 description 4
- 238000005303 weighing Methods 0.000 description 4
- 206010059866 Drug resistance Diseases 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
- 229940088710 antibiotic agent Drugs 0.000 description 3
- 230000001580 bacterial effect Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 241000894006 Bacteria Species 0.000 description 2
- HZZVJAQRINQKSD-UHFFFAOYSA-N Clavulanic acid Natural products OC(=O)C1C(=CCO)OC2CC(=O)N21 HZZVJAQRINQKSD-UHFFFAOYSA-N 0.000 description 2
- 108090000204 Dipeptidase 1 Proteins 0.000 description 2
- 241000588747 Klebsiella pneumoniae Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229910052783 alkali metal Inorganic materials 0.000 description 2
- -1 alkali metal salt Chemical class 0.000 description 2
- 150000001447 alkali salts Chemical class 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 102000006635 beta-lactamase Human genes 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- HZZVJAQRINQKSD-PBFISZAISA-N clavulanic acid Chemical compound OC(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 HZZVJAQRINQKSD-PBFISZAISA-N 0.000 description 2
- 229960003324 clavulanic acid Drugs 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 229940093181 glucose injection Drugs 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 210000002429 large intestine Anatomy 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 2
- 239000008354 sodium chloride injection Substances 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- FKENQMMABCRJMK-RITPCOANSA-N sulbactam Chemical compound O=S1(=O)C(C)(C)[C@H](C(O)=O)N2C(=O)C[C@H]21 FKENQMMABCRJMK-RITPCOANSA-N 0.000 description 2
- 229960005256 sulbactam Drugs 0.000 description 2
- 241000588624 Acinetobacter calcoaceticus Species 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 241000193830 Bacillus <bacterium> Species 0.000 description 1
- KEJCWVGMRLCZQQ-YJBYXUATSA-N Cefuroxime axetil Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(=O)OC(C)OC(C)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 KEJCWVGMRLCZQQ-YJBYXUATSA-N 0.000 description 1
- 229930186147 Cephalosporin Natural products 0.000 description 1
- 241000588921 Enterobacteriaceae Species 0.000 description 1
- 206010034133 Pathogen resistance Diseases 0.000 description 1
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 239000004411 aluminium Substances 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 230000002924 anti-infective effect Effects 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 239000003782 beta lactam antibiotic agent Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 229960002620 cefuroxime axetil Drugs 0.000 description 1
- 229940124587 cephalosporin Drugs 0.000 description 1
- 150000001780 cephalosporins Chemical class 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 229940041006 first-generation cephalosporins Drugs 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000012155 injection solvent Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 229940041008 second-generation cephalosporins Drugs 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 239000002132 β-lactam antibiotic Substances 0.000 description 1
- 229940124586 β-lactam antibiotics Drugs 0.000 description 1
- 150000003952 β-lactams Chemical class 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a cefuroxime sodium compound preparation, in particular to an antibacterial compound medicinal preparation containing cefuroxime or a physiologically acceptable salt thereof and a beta-lactamase inhibitor, wherein the weight ratio of the cefuroxime or the physiologically acceptable salt thereof to the beta-lactamase inhibitor is 8: 1-1: 8, preferably 8: 1-2: 1, and more preferably 8: 1-4: 1.
Description
Technical field:
The present invention relates to a kind of compound medicinal formulation, particularly contain the antibiotic compound medicinal formulation of cefuroxime or its physiologically acceptable salt and a kind of beta-lactamase inhibitor.
Background technology:
Extensive use along with beta-lactam antibiotic, the resistant rate of various bacterial antibiotics also day by day increases, one of its reason is exactly to make antibacterial produce new beta-lactamase, be induction type beta-lactamase (inducible enzyme) and extended spectrum (super wide spectrum enzyme), and become the main mechanism of bacterial resistance in the current anti-infective therapy clinically, bring new difficulty for antibiotic treatment.Extended spectrum is mainly produced by enterobacteriaceae lactobacteriaceae, serves as main representative with Klebsiella Pneumoniae and large intestine Ai Xishi bacterium especially.It is high to produce the extended spectrum bacterial drug resistance, to the equal drug resistance of all first and second generation cephalosporins.Cefuroxime is a second generation cephalosporin, is widely used in clinically at home, but along with its extensively a large amount of application, bacterial drug resistance constantly produces.The main path one that solves the anti-Beta-lactam medicine of antibacterial at present is the development of new antibiotics of anti-the enzyme, and another approach is to unite use with beta-lactamase inhibitor, and the hydrolysis of beta-lactamase inhibitor inhibitory enzyme strengthens the Beta-lactam medicine curative effect.The beta-lactamase inhibitor of present domestic listing has clavulanic acid, sulbactam, Tazobactam Sodium.
Cefuroxime or its physiologically acceptable salt and beta-lactamase inhibitor be used in combination does not still have bibliographical information.
The invention reside in, cefuroxime or its physiologically acceptable salt and beta-lactamase inhibitor in conjunction with making a kind of compound medicinal formulation, be found through experiments, both are in conjunction with the effectiveness that has improved cefuroxime or its physiologically acceptable salt greatly.
Summary of the invention:
The present invention by with cefuroxime or its physiologically acceptable salt and beta-lactamase inhibitor in conjunction with making a kind of compound medicament composition.Pharmaceutical composition of the present invention, contain cefuroxime or its physiologically acceptable salt and a kind of beta-lactamase inhibitor, wherein, the part by weight of cefuroxime or its physiologically acceptable salt and beta-lactamase inhibitor is 8: 1-1: 8, preferably 8: 1-2: 1, more preferably 8: 1-4: 1
Compositions of the present invention, cefuroxime wherein or its physiologically acceptable salt comprise alkali metal salt or alkali salt and their hydrate and the CEFUROXIME AXETIL etc. of cefuroxime acid, cefuroxime acid.The preferably potassium salt of cefuroxime and sodium salt.Particularly preferably be the cefuroxime sodium salt,
Compositions of the present invention, beta-lactamase inhibitor wherein can be clavulanic acid, sulbactam, Tazobactam Sodium or its physiologically acceptable salt, and these physiologically acceptable salts can be alkali metal salt or alkali salt, preferably potassium salt and sodium salt.For beta-lactamase inhibitor, the present invention is Tazobactam Sodium or its physiologically acceptable salt, preferably sodium-tazobactam preferably.
The present invention preferably fills a prescription, and to form be Cefuroxime Sodium and sodium-tazobactam, and both part by weight are 8: 1-1: 8, preferably 8: 1-2: 1, more preferably 8: 1-4: 1.
Compositions of the present invention can prepare by the following method, with cefuroxime or its physiologically acceptable salt and the mixing of a kind of beta-lactamase inhibitor, makes pharmaceutical preparation according to the routine techniques of galenic pharmacy.
Compositions of the present invention, cefuroxime or its physiologically acceptable salt and a kind of beta-lactamase inhibitor are as active component, can add the medicine acceptable carrier in case of necessity, if add the medicine acceptable carrier, cefuroxime or its physiologically acceptable salt and a kind of beta-lactamase inhibitor can account for 0.1%～99.9% of composition weight, and all the other are the medicine acceptable carrier.
The present invention also provides the preparation of drug combination method and with their application of preparation in antibacterials.
Preferred pharmaceutical composition of the present invention is the dosage form of the pharmaceutical dosage forms as parenteral, particularly drug administration by injection.
The invention provides a kind of stablizing and store and water-soluble pharmaceutical preparation, so that be applied to clinical treatment by the medical domain expert with the powder formulation form administration.
Injection of the present invention can be an injectable powder.
The present invention also comprises the preparation box that injectable powder and injection solvent are formed.The said preparation box, include the solvent that injectable powder of the present invention and a kind of injectable are used, the solvent that injectable powder and injectable are used is discrete, be packaged in the same packing box, the proportioning of the quantity of solvent that injectable powder and injectable are used is according to the using method preparation, and the injectable powder of every 100mg dosage is equipped with the solvent that 5ml～the 500ml injectable is used.Described injectable is selected from solvent: water for injection, sodium chloride injection, glucose injection.
Specifically can be: every injectable powder be equipped with 0.9% sodium chloride injection or 5% glucose injection of 5ml or 10ml water or 100ml or 250ml or 500ml.
The present invention also provides the preparation method of dry powder injection, comprise with Cefuroxime Sodium of the present invention and Tazobactam Sodium sodium raw materials mix, fill, jump a queue and make with the aluminium lid sealing.
Intravenous drip that the present invention also provides is with the preparation method of transfusion, comprise preparation of the present invention and glucose or sodium chloride added the dissolving of injection water after, promptly.
Injection of the present invention, cefuroxime or its physiologically acceptable salt and a kind of beta-lactamase inhibitor totally 0.4～4g can be contained in each preparation unit, as.Cefuroxime Sodium 1.00g and sodium-tazobactam 0.25g, Cefuroxime Sodium 2.00g and sodium-tazobactam 0.50g,
Preparation of the present invention is determined usage and dosage according to patient's situation in use, but obeys every day 1～3 time, each 1～20 dose, as: 1～20.
The present invention comprises that also Cefuroxime Sodium and sodium-tazobactam are united use, are used for the treatment of bacterial infection, in use according to Cefuroxime Sodium and sodium-tazobactam weight ratio 8: 1-1: 8 drug combinations.
Compositions of the present invention, through the pharmacological effect experiment confirm, compositions of the present invention has obtained beyond thought effect, and side effect simultaneously reduces, and drug dose reduces, and easy to make, both have synergism.
The specific embodiment:
The present invention is described further for following examples, but be not any limitation of the invention.
Embodiment 1
Adopt the agar doubling dilution, cefuroxime folk prescription and cefuroxime/Tazobactam Sodium compound recipe have been carried out antibacterial activity in vitro relatively.Comparative result sees Table 1
Table 1 cefuroxime, cefuroxime/Tazobactam Sodium antibacterial activity in vitro relatively (MIC, mg/L)
| Strain (strain) | Cefuroxime | Cefuroxime/Tazobactam Sodium | |
| ????4∶1 | ????8∶1 | ||
| Klebsiella Pneumoniae (31) | ??＞128 | ????8～16 | ????16 |
| Acinetobacter calcoaceticus (25) | ??＞128 | ????16 | ????16 |
| Negative bacillus (9) | ??＞128 | ????16 | ????8 |
| Large intestine Ai Xishi bacterium (18) | ??＞128 | ????8 | ????16 |
| Pseudomonas aeruginosa (10) | ??＞128 | ????4～16 | ????8 |
Embodiment 2
Precision takes by weighing Cefuroxime Sodium aseptic powder 1.00g and sodium-tazobactam aseptic powder 0.25g, mixes under gnotobasis, and sterile powder for injection is made in fill.
Embodiment 3
Precision takes by weighing Cefuroxime Sodium aseptic powder 2.00g and sodium-tazobactam aseptic powder 0.50g, mixes under gnotobasis, and sterile powder for injection is made in fill.
Embodiment 4
Precision takes by weighing Cefuroxime Sodium aseptic powder 1.00g and sodium-tazobactam aseptic powder 0.125g, mixes under gnotobasis, and sterile powder for injection is made in fill.
Embodiment 5
Precision takes by weighing Cefuroxime Sodium aseptic powder 2.00g and sodium-tazobactam aseptic powder 0.25g, mixes under gnotobasis, and sterile powder for injection is made in fill.
Claims (10)
1. antibacterial combination, it is characterized in that, said composition contains cefuroxime or its physiologically acceptable salt or ester and at least a beta-lactamase inhibitor, and wherein, the part by weight of cefuroxime or its physiologically acceptable salt or ester and beta-lactamase inhibitor is 8: 1-1: 8.
2. the compositions of claim 1, wherein cefuroxime or its physiologically acceptable salt are Cefuroxime Sodiums, and wherein beta-lactamase inhibitor is a sodium-tazobactam, and both part by weight in compositions are 8: 1-1: 8.
3. the compositions of claim 2 is characterized in that, Cefuroxime Sodium and the sodium-tazobactam part by weight in compositions is 8: 1-4: 1.
4. the compositions of claim 3 is characterized in that, Cefuroxime Sodium and the sodium-tazobactam part by weight in compositions is 8: 1.
5. the compositions of claim 3 is characterized in that, Cefuroxime Sodium and the sodium-tazobactam part by weight in compositions is 4: 1.
6. the compositions of claim 1 is an injection.
7. the preparation of compositions method of claim 1 is characterized in that, with cefuroxime or its physiologically acceptable salt and beta-lactamase inhibitor mixing.
8. the preparation method of claim 7 is characterized in that, cefuroxime or its physiologically acceptable salt are Cefuroxime Sodiums, and beta-lactamase inhibitor is a sodium-tazobactam.
9. the preparation method of claim 8 is characterized in that, Cefuroxime Sodium and sodium-tazobactam, and both part by weight in compositions are 8: 1-4: 1.
10. Cefuroxime Sodium and sodium-tazobactam are united use, are used for the treatment of bacterial infection, in use according to Cefuroxime Sodium and sodium-tazobactam weight ratio 8: 1-1: 8 drug combinations.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410048080 CN1582942A (en) | 2004-06-14 | 2004-06-14 | Cefuroxime sodium compound preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410048080 CN1582942A (en) | 2004-06-14 | 2004-06-14 | Cefuroxime sodium compound preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1582942A true CN1582942A (en) | 2005-02-23 |
Family
ID=34602068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410048080 Pending CN1582942A (en) | 2004-06-14 | 2004-06-14 | Cefuroxime sodium compound preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1582942A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101850105A (en) * | 2010-04-06 | 2010-10-06 | 邓学峰 | Cefuroxime sodium composite medicine |
| CN101491502B (en) * | 2008-10-24 | 2010-12-29 | 邢建荣 | Cefuroxime sodium freeze dry power preparation method |
| CN102652750A (en) * | 2011-03-04 | 2012-09-05 | 珠海联邦制药股份有限公司 | Pharmaceutical composition containing cefuroxime, preparation of composition, and preparation method of composition |
-
2004
- 2004-06-14 CN CN 200410048080 patent/CN1582942A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101491502B (en) * | 2008-10-24 | 2010-12-29 | 邢建荣 | Cefuroxime sodium freeze dry power preparation method |
| CN101850105A (en) * | 2010-04-06 | 2010-10-06 | 邓学峰 | Cefuroxime sodium composite medicine |
| CN101850105B (en) * | 2010-04-06 | 2012-06-27 | 邓学峰 | Cefuroxime sodium composite medicine |
| CN102652750A (en) * | 2011-03-04 | 2012-09-05 | 珠海联邦制药股份有限公司 | Pharmaceutical composition containing cefuroxime, preparation of composition, and preparation method of composition |
| CN102652750B (en) * | 2011-03-04 | 2014-04-02 | 珠海联邦制药股份有限公司 | Pharmaceutical composition containing cefuroxime, preparation of composition, and preparation method of composition |
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