CN102743389A - Cefuroxime sodium pharmaceutical composition, powder-injection thereof and method for producing cefuroxime sodium pharmaceutical composition - Google Patents
Cefuroxime sodium pharmaceutical composition, powder-injection thereof and method for producing cefuroxime sodium pharmaceutical composition Download PDFInfo
- Publication number
- CN102743389A CN102743389A CN2012102337063A CN201210233706A CN102743389A CN 102743389 A CN102743389 A CN 102743389A CN 2012102337063 A CN2012102337063 A CN 2012102337063A CN 201210233706 A CN201210233706 A CN 201210233706A CN 102743389 A CN102743389 A CN 102743389A
- Authority
- CN
- China
- Prior art keywords
- cefuroxime sodium
- pharmaceutical composition
- cefuroxime
- sodium
- weight
- 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.)
- Granted
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to a cefuroxime sodium pharmaceutical composition, a powder-injection thereof and a method for producing the cefuroxime sodium pharmaceutical composition. The pharmaceutical composition consists of cefuroxime sodium and hydroxypropyl-beta-cyclodextrin, wherein the weight of hydroxypropyl-beta-cyclodextrin is 5%-15% the weight of cefuroxime sodium, preferentially 10%. The cefuroxime sodium pharmaceutical composition has good stability, the impurity content is far less than the cefuroxime sodium preparation product on the market, the gastrointestinal tract side effects are small, and the quality and safety of cefuroxime sodium are greatly improved.
Description
Technical field
The invention belongs to the drug invention field, the pharmaceutical composition of particularly a kind of Cefuroxime Sodium and HP-, its injectable powder and preparation method thereof.
Background technology
Cefuroxime Sodium is a second generation cephalosporin class antibiotic.Chemical name is: (6R, 7R)-7-[2-furyl (methoxyimino) acetylamino] 3-carbamyl oxygen methyl-8-oxo-5-thia-1-azabicyclic [4.2.0] oct-2-ene-2-formic acid sodium salt, structural formula is following:
Cefuroxime Sodium is similar with first generation cephalosporin or slightly poor to the antibacterial activity of gram-positive cocci, but the beta-lactamase quite stable that staphylococcus and gram negative bacilli are produced.Its mechanism of action be with bacterial cell membrane on penicillin-binding protein (PBPs) combine, make the transpeptidase acidylate, suppress the synthetic of bacteria cell wall; The intersection that influences the cell wall mucopeptide composition links; Cell division and growth are suppressed, and ne ar is elongated, dissolving at last and dead.Cefuroxime Sodium is used for respiratory tract infection, department of otorhinolaryngology infection, urinary tract infection, skin and soft tissue infection, bone and the infection of joint, obstetrics and gynecological infection, gonorrhea and other infection due to the sensitive organism.
CN200410048080.4 discloses a kind of Cefuroxime Sodium compound preparation, forms aseptic subpackaged making by the antibiotic compound medicinal formulation of cefuroxime or its physiologically acceptable salt and a kind of beta-lactamase inhibitor.
CN200510090387.5 discloses a kind of Cefuroxime Sodium and Tazobactam Sodium composition of sodium, is made up of aseptic subpackaged making Cefuroxime Sodium and sodium-tazobactam.
CN201010139958.0 discloses the pharmaceutical composition of Cefuroxime Sodium, sodium glucuronate and glutathion.Cefuroxime Sodium: sodium glucuronate: the ratio of weight and number of glutathion is 0.25-2.0:0.1-0.3:0.02-0.04.The disclosed compositions of this patent is through adding stabilizing agent improving the stability of Cefuroxime Sodium, the means of using always for those skilled in the art.
CN200910036828.1 discloses a kind of cefuroxime composition of sodium, and said composition comprises Cefuroxime Sodium and a kind of or be no less than two kinds medicinal stabilizing agent.Described stabilizing agent is a kind of in citrate, sulphite or the phosphate or is no less than two kinds combination.The disclosed compositions of this patent is through adding stabilizing agent improving the stability of Cefuroxime Sodium, the means of using always for those skilled in the art.
CN200810158319.1 discloses a kind of cefuroxime sodium freeze dry power pin that does not contain any pharmaceutic adjuvant, and its water content is below 2.0%.
In the injection preparation product, add too much stabilizing agent and may produce harmful effect or side effect human body.The stability of simultaneously commercially available Cefuroxime Sodium formulation products is still bad, influences the quality and the safety of medicine.
In order to obtain a kind of green, stable, cefuroxime sodium pharmaceutical composition that safety is good, the applicant is through a large amount of pharmaceutical compositions of the present invention of having discovered, for the cefuroxime preparation of sodium provides new prescription, specially proposes the present invention.
Summary of the invention
The object of the present invention is to provide a kind of cefuroxime sodium pharmaceutical composition, this pharmaceutical composition is made up of Cefuroxime Sodium and HP-.This pharmaceutical composition has improved the stability of Cefuroxime Sodium, has reduced the gastrointestinal side effect of Cefuroxime Sodium.
The present invention realizes through following technical scheme:
A kind of cefuroxime sodium pharmaceutical composition is made up of Cefuroxime Sodium and HP-, and the weight of described HP-is 5%～15% of Cefuroxime Sodium weight, and preferred 10%.
In order to prove the stability of cefuroxime sodium pharmaceutical composition of the present invention; The applicant carries out accelerated test simultaneously with cefuroxime sodium pharmaceutical composition of the present invention and commercially available Cefuroxime Sodium formulation products; Before accelerated test; Cefuroxime sodium pharmaceutical composition of the present invention is all consistent on outward appearance, color and impurity content with commercially available Cefuroxime Sodium formulation products; But both obvious differences after accelerated test: cefuroxime sodium pharmaceutical composition of the present invention is white or off-white powder from seeing in appearance, and the appearance color of commercially available Cefuroxime Sodium formulation products gradually becomes buff powder, yellow powder by white powder, explains that variations such as degraded take place commercially available Cefuroxime Sodium formulation products; Produced more impurity, product colour is deepened.Equally; Solution colour through each sample point of accelerated test is measured; Find: when accelerated test 1 month, 2 months, 3 months and 6 months, the solution colour of cefuroxime sodium pharmaceutical composition of the present invention all obviously is shallower than commercially available Cefuroxime Sodium formulation products, and stability is fine.The dirt content test result shows: in 6 months accelerated test, maximum single assorted content of commercially available Cefuroxime Sodium formulation products increases to 4.6% by 0.2%, has increased 23 times; Total assorted content increases to 7.8% by 0.5%, has increased 15.6 times; And maximum single assorted content increases to 0.7% by 0.2% in the cefuroxime sodium pharmaceutical composition of the present invention, has only increased 3.5 times, and always assorted content increases to 2.2% by 0.5%, has only increased 4.4 times.No matter be that the impurity content in the cefuroxime sodium pharmaceutical composition of the present invention all is significantly less than the impurity content of commercially available Cefuroxime Sodium formulation products, shows outstanding stability from the single assorted content of maximum or total assorted content.
Particularly when the weight of HP-be Cefuroxime Sodium weight 10% the time; After 6 months accelerated test, the maximum single assorted content in the cefuroxime sodium pharmaceutical composition is lower, and always assorted content is lower; Total assorted content is less than 1.8%, and maximum single assorted stable content is 0.6%.
A purpose more of the present invention provides a kind of Cefuroxime Sodium preparation of drug combination method.
A kind of Cefuroxime Sodium preparation of drug combination method comprises: behind Cefuroxime Sodium and HP-crushing screening, proportionally mix homogeneously gets the cefuroxime sodium pharmaceutical composition.
Or prepare: with the Cefuroxime Sodium crushing screening, take by weighing Cefuroxime Sodium, join in the coating machine by following step; HP-is dissolved in ethanol or concentration expressed in percentage by volume is the ethanol water of 50-70%, the solution after the dissolving all is ejected into equably the particle layer surface of Cefuroxime Sodium; Drying obtains the cefuroxime sodium pharmaceutical composition.
Described drying can be drum-type drying, box-type drying, vacuum drying, fluid bed drying, spray drying, lyophilization, infrared drying, the preferred fluid bed drying of the present invention.
Above-mentioned cefuroxime sodium pharmaceutical composition can further be sub-packed in the cillin bottle, tamponade, rolls lid, lamp inspection, is up to the standards, and labeling, packing promptly get its injectable powder.
Maximum single assorted content of cefuroxime sodium pharmaceutical composition injectable powder of the present invention is all less than 0.8%; Total assorted content is all less than 2.3%; Better controlled critical impurities content and total assorted content in the product, show stability preferably, thereby can reduce the gastrointestinal side reaction.
The preparation of aforementioned pharmaceutical compositions and injectable powder thereof is all carried out under the condition that Chinese GMP (2010) requires.
The cefuroxime sodium pharmaceutical composition is used for the purposes of the medicine of mammal (comprising the people) bacterial infection in preparation.
Only contain aseptic Cefuroxime Sodium in the prescription of commercially available Cefuroxime Sodium formulation products of the present invention, do not contain other any pharmaceutic adjuvant, directly obtain through the packing of cefuroxime sodium sterilized raw.
Compared with prior art, the beneficial effect of technical scheme of the present invention:
1) low (maximum single assorted content is all less than 0.8% for the maximum single assorted content of cefuroxime sodium pharmaceutical composition of the present invention and preparation thereof and total assorted content; Total assorted content is all less than 2.3%); Improved the quality of formulation products; Can reduce the incidence rate of its side reaction, improve the compliance of patient's Drug therapy.
2) cefuroxime sodium pharmaceutical composition of the present invention and stability of formulation thereof promote greatly, stable in properties such as outward appearance, color, and the safety that has improved medicine has guaranteed the quality of medicine, can prolong the memory time of medicine;
3) gastrointestinal side effect of cefuroxime sodium pharmaceutical composition of the present invention and preparation thereof is little.
The specific embodiment
Below in conjunction with embodiment the present invention is described in further detail, but embodiment of the present invention is not limited thereto.
Embodiment 1
Prescription: Cefuroxime Sodium 2000g
HP-100g
Preparation technology: the supplementary material Cefuroxime Sodium was pulverized 80 mesh sieves, get the 2000g Cefuroxime Sodium and drop in the coating machine; The 100g HP-is dissolved in an amount of 50% (concentration expressed in percentage by volume) alcoholic solution, this solution is sprayed in Cefuroxime Sodium particle layer surface fully, get the cefuroxime sodium pharmaceutical composition through fluid bed drying.
Embodiment 2
Prescription: Cefuroxime Sodium 2000g
HP-300g
Preparation technology: the supplementary material Cefuroxime Sodium was pulverized 80 mesh sieves, get the 2000g Cefuroxime Sodium and drop in the coating machine; The 300g HP-is dissolved in an amount of 50% (concentration expressed in percentage by volume) alcoholic solution, this solution is sprayed in Cefuroxime Sodium particle layer surface fully, get the cefuroxime sodium pharmaceutical composition through fluid bed drying.
Embodiment 3
Prescription: Cefuroxime Sodium 2000g
HP-200g
Preparation technology: supplementary material Cefuroxime Sodium and HP-pulverize separately are crossed 80 mesh sieves, get the 2000g Cefuroxime Sodium, the 200g HP-, mix homogeneously gets the cefuroxime sodium pharmaceutical composition.
Embodiment 4
Get the cefuroxime sodium pharmaceutical composition 1000g that embodiment 3 prepares, measure content and be sub-packed in 1000 cillin bottles after qualified, tamponade, roll lid, lamp inspection, be up to the standards, labeling, packing promptly gets the cefuroxime sodium injection.
Embodiment 5
Get 3 totally batches of the cefuroxime sodium pharmaceutical compositions (being numbered 20120101S, 20120102S, 20120103S in order respectively) that embodiment 1 to embodiment 3 prepares; Carry out accelerated test (40 ℃ of temperature; In humidity 75% climatic chamber); Detect by method under 2010 editions Pharmacopoeia of the People's Republic of China cefuroxime sodium for injection items, the testing result of testing after 0 month, 1 month, 2 months, 3 months, 6 months is following:
Table 1 cefuroxime sodium pharmaceutical composition of the present invention accelerated test result
The data show of table 1: when the weight of HP-is the 5%-15% of Cefuroxime Sodium weight; Cefuroxime sodium pharmaceutical composition outward appearance of the present invention, solution colour change little; Clarity is clarification; Total assorted content is all less than 2.3%, and maximum list is mixed content all less than 0.8%, having good stability between each batch.When the weight of HP-is 10% (20120103S) of Cefuroxime Sodium weight; After 6 months accelerated test, maximum single assorted content of pharmaceutical composition is all littler with total assorted content, and always assorted content is less than 1.8%; Maximum single assorted stable content is 0.6%, and stability is better.
Embodiment 6
Cefuroxime sodium pharmaceutical composition and the commercially available Cefuroxime Sodium formulation products of getting embodiment 2 preparations carry out accelerated test (40 ℃ of temperature; In humidity 75% climatic chamber); Detect by method under 2010 editions Pharmacopoeia of the People's Republic of China cefuroxime sodium for injection items, the testing result of testing after 0 month, 1 month, 2 months, 3 months, 6 months is following:
Table 2 cefuroxime sodium pharmaceutical composition of the present invention and commercially available Cefuroxime Sodium formulation products accelerated test result
Can know from table 2 data: before accelerated test; Cefuroxime sodium pharmaceutical composition of the present invention is all consistent on outward appearance, color and impurity content with commercially available Cefuroxime Sodium formulation products; But both obvious differences after accelerated test: cefuroxime sodium pharmaceutical composition of the present invention is white or off-white powder from seeing in appearance; And the appearance color of commercially available Cefuroxime Sodium formulation products product after accelerated test gradually becomes buff powder, yellow powder by white powder; Explain that variations such as degraded take place commercially available Cefuroxime Sodium formulation products, produce more impurity, product colour is deepened.Equally; Solution colour through each sample point of accelerated test is measured; Find: when accelerated test 1 month, 2 months, 3 months and 6 months, the solution colour of cefuroxime sodium pharmaceutical composition of the present invention all obviously is shallower than commercially available Cefuroxime Sodium formulation products, and stability is fine.The dirt content test result shows: in 6 months accelerated test, maximum single assorted content of commercially available Cefuroxime Sodium formulation products increases to 4.6% by 0.2%, has increased 23 times, and total impurities content increases to 7.8% by 0.5%, has increased 15.6 times; And maximum single assorted content increases to 0.7% by 0.2% in the cefuroxime sodium pharmaceutical composition of the present invention, has only increased 3.5 times, and total impurities content increases to 2.2% by 0.5%, has only increased 4.4 times.No matter be that the impurity content in the cefuroxime sodium pharmaceutical composition of the present invention all is significantly less than the impurity content of commercially available Cefuroxime Sodium formulation products, shows outstanding stability from the single assorted content of maximum or total assorted content.
To sum up, accelerated test result shows that outward appearance, the change color of cefuroxime sodium pharmaceutical composition of the present invention are little, and maximum single assorted content is low with total assorted content, good stability.
The foregoing description is a preferred implementation of the present invention; But embodiment of the present invention is not restricted to the described embodiments; Other any do not deviate from change, the modification done under spirit of the present invention and the principle, substitutes, combination, simplify; All should be the substitute mode of equivalence, be included within protection scope of the present invention.
Claims (7)
1. cefuroxime sodium pharmaceutical composition, it is characterized in that: be made up of Cefuroxime Sodium and HP-, the weight of described HP-is the 5%-15% of Cefuroxime Sodium weight.
2. cefuroxime sodium pharmaceutical composition as claimed in claim 1 is characterized in that: the weight of described HP-is 10% of Cefuroxime Sodium weight.
3. cefuroxime sodium pharmaceutical composition as claimed in claim 1 is characterized in that: the weight of each component is respectively in the pharmaceutical composition: Cefuroxime Sodium 2000g
HP-200g.
4. like each described Cefuroxime Sodium preparation of drug combination method of claim 1-3, it is characterized in that this method may further comprise the steps: with the Cefuroxime Sodium crushing screening, take by weighing Cefuroxime Sodium, join in the coating machine; HP-is dissolved in ethanol or concentration expressed in percentage by volume is the ethanol water of 50-70%, the solution after the dissolving all is ejected into equably the particle layer surface of Cefuroxime Sodium; Drying obtains the cefuroxime sodium pharmaceutical composition.
5. like each described Cefuroxime Sodium preparation of drug combination method of claim 1-3; It is characterized in that this method may further comprise the steps: behind Cefuroxime Sodium and HP-crushing screening; Proportionally mix homogeneously gets the cefuroxime sodium pharmaceutical composition.
6. like each described cefuroxime sodium pharmaceutical composition of claim 1-3, it is characterized in that: described preparation of pharmaceutical compositions becomes powder ampoule agent for injection.
7. the purposes that is used for the medicine of mammal bacterial infection like each described cefuroxime sodium pharmaceutical composition of claim 1-3 in preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210233706 CN102743389B (en) | 2012-07-06 | 2012-07-06 | Cefuroxime sodium pharmaceutical composition, powder-injection thereof and method for producing cefuroxime sodium pharmaceutical composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210233706 CN102743389B (en) | 2012-07-06 | 2012-07-06 | Cefuroxime sodium pharmaceutical composition, powder-injection thereof and method for producing cefuroxime sodium pharmaceutical composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102743389A true CN102743389A (en) | 2012-10-24 |
| CN102743389B CN102743389B (en) | 2013-06-12 |
Family
ID=47024120
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201210233706 Expired - Fee Related CN102743389B (en) | 2012-07-06 | 2012-07-06 | Cefuroxime sodium pharmaceutical composition, powder-injection thereof and method for producing cefuroxime sodium pharmaceutical composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102743389B (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103908673A (en) * | 2014-01-22 | 2014-07-09 | 邓学峰 | Ceftriaxone combinatorial drug |
| CN104910187A (en) * | 2015-05-28 | 2015-09-16 | 浙江长典医药有限公司 | Children cefuroxime sodium compound entity and preparation thereof |
| CN114191375A (en) * | 2021-12-20 | 2022-03-18 | 广东金城金素制药有限公司 | Cefuroxime sodium for injection and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101002782A (en) * | 2007-01-10 | 2007-07-25 | 南京师范大学 | Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method |
| CN101849948A (en) * | 2010-04-06 | 2010-10-06 | 邓学峰 | Cefuroxime axetil composite medicine |
-
2012
- 2012-07-06 CN CN 201210233706 patent/CN102743389B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101002782A (en) * | 2007-01-10 | 2007-07-25 | 南京师范大学 | Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method |
| CN101849948A (en) * | 2010-04-06 | 2010-10-06 | 邓学峰 | Cefuroxime axetil composite medicine |
Non-Patent Citations (2)
| Title |
|---|
| 邵建华，等: "头孢呋辛钠疗效和安全性再评价", 《沈阳药科大学学报》 * |
| 鲍威，等: "注射用头孢呋辛钠", 《药学进展》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103908673A (en) * | 2014-01-22 | 2014-07-09 | 邓学峰 | Ceftriaxone combinatorial drug |
| CN104910187A (en) * | 2015-05-28 | 2015-09-16 | 浙江长典医药有限公司 | Children cefuroxime sodium compound entity and preparation thereof |
| CN114191375A (en) * | 2021-12-20 | 2022-03-18 | 广东金城金素制药有限公司 | Cefuroxime sodium for injection and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102743389B (en) | 2013-06-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102743389B (en) | Cefuroxime sodium pharmaceutical composition, powder-injection thereof and method for producing cefuroxime sodium pharmaceutical composition | |
| CN104940158A (en) | Medicine composition containing cefuroxime axetil and preparation method of medicine composition | |
| CN102525963B (en) | Netilmicin sulfate lyophiled powder injection and preparation method thereof | |
| CN103524533B (en) | A kind of cefprozil compound, its dispersible tablet, dry suspensoid and preparation method | |
| CN106176646B (en) | Tosufloxacin tosylate dispersible tablets and preparation method thereof | |
| CN103446075A (en) | Cefaclor capsule and preparation method thereof | |
| CN102327270B (en) | Beta-lactam compound antibiotic composition | |
| CN101780052B (en) | Ceftizoxime sodium liposome injection | |
| CN103145733B (en) | Amoxicillin compound and pharmaceutical composition of amoxicillin compound and potassium clavulanate | |
| CN102525948A (en) | Dry suspension of cefpodoxime proxetil composition and preparation method thereof | |
| CN104688713A (en) | Cefradine capsule and preparation method thereof | |
| CN103893132B (en) | A kind of cefdinir granules and preparation technology thereof | |
| CN101565105A (en) | Method for preparing ceftizoxime powder injection for injection and use thereof | |
| CN102755325A (en) | Cefoxitin sodium medicinal composition, powder injection and preparation method thereof | |
| CN103432076B (en) | Cefprozil dry suspension and preparation method thereof | |
| CN103301075B (en) | A kind of cefixime composition mix suspension grain agent and preparation method thereof | |
| CN102247375A (en) | Cefotetan disodium for injection, and preparation method thereof | |
| CN103230367B (en) | Cefpodoxime proxetil composition dry suspension and preparation method thereof | |
| CN103284958A (en) | Cefdinir composition granule and preparation method thereof | |
| CN102824304A (en) | Cefepime hydrochloride composition for injection and its preparation method | |
| CN112587563A (en) | Antibacterial Chinese and western medicine powder for amoxicillin and scutellaria baicalensis for livestock and preparation method thereof | |
| CN108186587A (en) | A kind of pharmaceutical composition containing Method of cefcapene pivoxil hydrochloride | |
| CN102351886A (en) | Cefteram pivoxil crystal and preparation method thereof and composition tablets containing crystal | |
| CN102824309B (en) | Cefmetazole sodium powder for injection and preparation method thereof | |
| CN104382849B (en) | A kind of cefaclor dry suspension and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20130612 Termination date: 20200706 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |