CN102631684A - Stable cephalosporin composition - Google Patents
Stable cephalosporin composition Download PDFInfo
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- CN102631684A CN102631684A CN2012101163825A CN201210116382A CN102631684A CN 102631684 A CN102631684 A CN 102631684A CN 2012101163825 A CN2012101163825 A CN 2012101163825A CN 201210116382 A CN201210116382 A CN 201210116382A CN 102631684 A CN102631684 A CN 102631684A
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- cephalosporin
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Abstract
The invention relates to a stable cephalosporin composition and a preparation method thereof. The cephalosporin is selected from one of cefaclor, cefixime, cefalexin and cefradine. The preparation method is characterized by comprising the steps of: inclusion of the cephalosporin by using dextrin; and then preparation according to the normal method in the industry. According to the invention, the stability problem of the cephalosporin composition at the normal temperature in summer, namely, the problem of content decreasing of main drugs in a storage process is solved; and the cephalosporin composition with stable quality is provided.
Description
Technical field the present invention relates to a kind of stable cephalosporin based composition and method for preparing.
The background technology cephalosporin is a kind of widely used clinically antimicrobial drug; Be mainly used in the infection that staphylococcus, streptococcus, Diplococcus pneumoniae, hemophilus influenza etc. cause; Be widely used in the mild to moderate respiratory tract infection of treatment clinically, and skin infection, urinary tract infection etc.The antibiotic mutual supplement with each other's advantages of such medicine and quinolones, curative effect is remarkable.
Because cephalosporin is understable to moisture, temperature, the many form productions of commercially available cephalosporin with granule or capsule, and the condition of storage of regulation is shading, sealing, and dark dry place preserves in cold, and according to the pharmacopeia regulation, the cool place is meant and is no more than 20 ℃ temperature.Such condition of storage has brought certain degree of difficulty for the transportation and the storage in summer, and especially the damp and hot weather of areas to the south, the Changjiang river especially is not suitable for the storage of these article.
The technical problem that the present invention will solve provides a kind of stable composition of cephalosporin, to solve the stability problem of at present commercially available cephalosporin preparation.For clinical a kind of stable cephalosporins preparation that can relieved use is provided.
Summary of the invention
Goal of the invention of the present invention is: solve the stability problem of cephalosporin based composition, promptly the drug content decline problem in the summer storage process provides a kind of stay-in-grade cephalosporin based composition.
Through great deal of experimental, the inventor has found a kind of stable cephalosporin based composition.Technical scheme of the present invention is:
A kind of stable cephalo gram bacteriums compositions is characterized in that containing the cephalosporin behind the useful dextrin enclose.Said cephalosporin is selected from a kind of in cefaclor, cefixime, cefalexin, the cefradine.
The present composition can be capsule, also can be granule or tablet.
Technical scheme of the present invention is in the inclusion process, and the mol ratio of dextrin and cephalosporin is 3～5: 1.
Dextrin according to the invention is an alpha-cyclodextrin.
Dextrin according to the invention is a beta-schardinger dextrin-.
Preparation of compositions method according to the invention is characterized in that:
The first step is pulverized adjuvant, crosses 100 mesh sieves;
The mol ratio of second step by dextrin and cephalosporin is 3～5: 1, takes by weighing a certain amount of dextrin, and the purified water dissolving with 3 times of weight adds cephalosporin, and solution temperature is remained on 30 ± 2 ℃ of grindings;
The 3rd step filtered and grinds back material, washing, drying;
The content of cephalosporin in the 4th pacing amount clathrate.
The 5th step was formulated prescription.
The 6th step took by weighing raw material and adjuvant by prescription, granulated by conventional method of granulating.
The 7th step packing.
For improving the mouthfeel of the present composition, can select adjuvants such as mannitol, sucrose to add in granulation step.
Preparation of compositions method according to the invention, the bake out temperature that it is characterized in that the cefaclor clathrate is 40 ± 5 ℃.
Preparation of compositions method according to the invention, the bake out temperature that it is characterized in that the cefixime clathrate is 40 ± 5 ℃.
Preparation of compositions method according to the invention, the bake out temperature that it is characterized in that cefalexin, cefradine clathrate is 60 ± 5 ℃.
The invention has the beneficial effects as follows provides a kind of stable composition of cephalosporin, has solved puzzlement cephalosporin preparation storage problem in summer in industry.
Embodiment 1 cefaclor 125g, maltodextrin 800g.
The first step is crossed 100 mesh sieves with raw material pulverizing;
Second step took by weighing a certain amount of dextrin by prescription, and the purified water dissolving with 3 times of weight adds cefaclor, and 30 ± 2 ℃ were ground 5 hours;
The 3rd step filtered and grinds the back material, and washing will be deposited in 40 ± 5 ℃ of dryings.
The 4th step was measured the cefaclor content in the clathrate according to the content assaying method of Pharmacopoeia of People's Republic of China regulation, was 34.36%.
The 5th step was formulated prescription.Clathrate 368mg, mannitol 800mg, sucrose 595mg, hypromellose (E5) 2.4mg.
The 6th step took by weighing adjuvant by prescription, granulated by conventional method of granulating.
The 7th step packing whenever comprises cefaclor 125mg.
Embodiment 2 cefaclor 250g, beta-schardinger dextrin-4500g.Step by embodiment 1 is carried out enclose, measures cefaclor content 21.32% in the clathrate.Formulate prescription, clathrate 1190mg, sucrose 595mg, hypromellose (E5) 2.4mg.Granulate by conventional method of granulating.Packing whenever comprises cefaclor 250mg.
Embodiment 3 cefaclor 125g, powder-beta-dextrin 2240g carries out enclose by the step of embodiment 1.Cefaclor content is 21.46% in the mensuration clathrate.Formulate prescription, clathrate 595mg, sucrose 595mg, mannitol 500mg, hypromellose (E5) 2.4mg.Granulate by conventional method of granulating.Packing whenever comprises cefaclor 125mg.
Embodiment 4 cefaclor 250g, alpha-cyclodextrin 1890g.Step by embodiment 1 is carried out enclose, measures cefaclor content 27.39% in the clathrate.Formulate prescription, clathrate 912mg, sucrose 595mg, mannitol 500mg, hypromellose (E5) 2.4mg.Granulate by conventional method of granulating.Packing whenever comprises cefaclor 250mg.
Embodiment 5 cefixime 125g, alpha-cyclodextrin 1360g, methanol 20ml.
The first step is crossed 100 mesh sieves with raw material pulverizing;
Second step took by weighing a certain amount of alpha-cyclodextrin by prescription, and the purified water dissolving with 3 times of weight adds the cefixime with dissolve with methanol, and 30 ± 2 ℃ were ground 3 hours;
The 3rd step filtered and grinds the back material, and washing will be deposited in 40 ± 5 ℃ of dryings.
The cefixime content that the 4th step measured in the clathrate according to the content assaying method of Pharmacopoeia of People's Republic of China regulation is 30.89%.
The 5th step was formulated prescription, clathrate 393mg, mannitol 800mg, sucrose 595mg, hypromellose (E5) 2.4mg.
The 6th step took by weighing adjuvant by prescription, granulated by conventional method of granulating.
The 7th step packing whenever comprises cefixime 125mg.
Embodiment 6 cefixime 250g, beta-schardinger dextrin-3040g, methanol 30ml.Enclose step by embodiment 5 is carried out enclose.The content of measuring cefixime in the clathrate is 23.36%, formulates prescription: clathrate 1070mg, mannitol 300mg, sucrose 295mg, hypromellose (E5) 2.4mg; Take by weighing adjuvant by prescription, granulate by conventional method of granulating, packing whenever comprises cefixime 250mg.
Embodiment 7 cefixime 250g, beta-schardinger dextrin-2285g,, methanol 30ml carries out enclose by the enclose step of embodiment 5.The content of measuring cefixime in the clathrate is 24.06%, formulates prescription: clathrate 1039mg, mannitol 300mg, sucrose 295mg, hypromellose (E5) 2.4mg; Take by weighing adjuvant by prescription, granulate by conventional method of granulating, packing whenever comprises cefixime 250mg.
Embodiment 8 cefalexin 125g, alpha-cyclodextrin 1760g, acetone 20ml.
The first step is crossed 100 mesh sieves with raw material pulverizing;
Second step took by weighing a certain amount of alpha-cyclodextrin by prescription, and the purified water dissolving with 3 times of weight adds the cefalexin with acetone solution, and 30 ± 2 ℃ were ground 3 hours;
The 3rd step filtered and grinds the back material, and washing will be deposited in 60 ± 5 ℃ of dryings.
The 4th step was measured the cefalexin content in the clathrate, 25.08% according to the content assaying method of Pharmacopoeia of People's Republic of China regulation.
The 5th step was formulated prescription, clathrate 498.4mg, mannitol 800mg, sucrose 595mg, hypromellose (E5) 2.4mg
The 6th step took by weighing adjuvant by prescription, granulated by conventional method of granulating.
The 7th step packing whenever comprises cefalexin 125mg.
Embodiment 9 cefalexin 250g, beta-schardinger dextrin-3980g, acetone 25ml carries out enclose by the enclose step of embodiment 8.The content of measuring cefalexin in the clathrate is 19.09%, formulates prescription: clathrate 1309.6mg, mannitol 300mg, sucrose 295mg, hypromellose (E5) 2.4mg; Take by weighing adjuvant by prescription, granulate by conventional method of granulating, packing whenever comprises cefalexin 250mg.
Embodiment 10 cefalexin 250g, alpha-cyclodextrin 2103g, acetone 25ml carries out enclose by the enclose step of embodiment 8.The content of measuring cefalexin in the clathrate is 25.48%, formulates prescription: clathrate 981.2mg, mannitol 600mg, sucrose 295mg, hypromellose (E5) 2.4mg; Take by weighing adjuvant by prescription, granulate by conventional method of granulating, packing whenever comprises cefalexin 250mg.
Embodiment 11 cefradine 125g, alpha-cyclodextrin 1760g, acetone 20ml
The first step is crossed 100 mesh sieves with raw material pulverizing;
Second step took by weighing a certain amount of alpha-cyclodextrin by prescription, and the purified water dissolving with 3 times of weight adds the cefradine with acetone solution, and 30 ± 2 ℃ were ground 3 hours;
The 3rd step filtered and grinds the back material, and washing will be deposited in 60 ± 5 ℃ of dryings.
The cefradine content that the 4th step measured in the clathrate according to the content assaying method of Pharmacopoeia of People's Republic of China regulation is 25.18%.
The 5th step was formulated prescription, clathrate 496.4mg, mannitol 800mg, sucrose 595mg, hypromellose (E5) 2.4mg
The 6th step took by weighing adjuvant by prescription, granulated by conventional method of granulating.
The 7th step packing whenever comprises cefradine 125mg.
Embodiment 12 cefradine 250g, beta-schardinger dextrin-3980g, acetone 25ml.Enclose step by embodiment 11 is carried out enclose.The content of measuring cefradine in the clathrate is 19.86%, formulates prescription: clathrate 1258.8mg, mannitol 300mg, sucrose 295mg, hypromellose (E5) 2.4mg; Take by weighing adjuvant by prescription, granulate by conventional method of granulating, packing whenever comprises cefradine 250mg.
Embodiment 13 cefradine 250g, alpha-cyclodextrin 2093g, acetone 25ml carries out enclose by the enclose step of embodiment 11.The content of measuring cefradine in the clathrate is 25.58%, formulates prescription: clathrate 977.3mg, mannitol 600mg, sucrose 295mg, hypromellose (E5) 2.4mg; Take by weighing adjuvant by prescription, granulate by conventional method of granulating, packing whenever comprises cefradine 250mg.
Reference examples 1 commercially available prescription cefaclor 125g, mannitol 800g, sucrose 500g, hypromellose (E5) 3g.Preparation according to the following steps.
The first step is pulverized adjuvant, crosses 100 mesh sieves.
Second step took by weighing the hypromellose of recipe quantity, prepare adhesive.
Mannitol, cefaclor, the sucrose of the 3rd step with recipe quantity adds granulator successively, does and mixes.Add binding agent, wet mixing, preparation soft material.
The 4th step 40 ± 5 ℃ of dryings.Packing 1000 bags.
Reference examples 2 commercially available prod prescription: cefixime 125g, mannitol 800g, sucrose 600g, hypromellose (E5) 2.4g.Process 1000 bags by the method for preparing of reference examples 1.
Reference examples 3 commercially available prod prescription cefalexin 125g, mannitol 800g, sucrose 600g, hypromellose (E5) 2.4g.Process 1000 bags according to the method for preparing of example 1, different is that bake out temperature is 60 ± 5 ℃.
Reference examples 4 commercially available prod prescription cefradine 125g, mannitol 800g, sucrose 600g, hypromellose (E5) 2.4g.Process 1000 bags by the method for preparing of reference examples 1, different is that bake out temperature is 60 ± 5 ℃.
Test Example 1, stability study
The granule of embodiment and reference examples is packed with listing, placed climatic chamber (SH05N), carry out stability test research (40 ℃),, detect cephalosporin content respectively at sampling in 0 day, 10 days, 20 days, 40 days, 80 days.Test data sees the following form.
Table 1 cefaclor granule stability result of the test
| 0 day | 10 days | 20 days | 40 days | 80 days | |
| Embodiment 1 | 100.3 | 99.5 | 98.6 | 97.6 | 96.2 |
| Embodiment 2 | 99.8 | 99.6 | 99.3 | 98.9 | 98.2 |
| Embodiment 3 | 99.9 | 99.3 | 98.6 | 97.6 | 97.1 |
| Embodiment 4 | 100.0 | 99.8 | 99.2 | 98.6 | 98.3 |
| Reference examples 1 | 100.3 | 98.6 | 97.2 | 93.5 | 90.8 |
The test data explanation, granule of the present invention changes very little at the drug content of stability test after 80 days, and in the sample size fall 4% of embodiment 1-4, the content fall of sample after 80 days of commercially available prod prescription reference examples 1 is about 9.2%.Explain that technical scheme of the present invention has played positive effect to the stability of cefaclor.
Table 2 cefixime granule stability result of the test
| 0 day | 10 days | 20 days | 40 days | 80 days | |
| Embodiment 5 | 98.9 | 98.5 | 98.2 | 98.6 | 97.8 |
| Embodiment 6 | 99.8 | 99.3 | 98.3 | 97.6 | 97.2 |
| Embodiment 7 | 99.6 | 99.0 | 98.1 | 97.4 | 96.8 |
| Reference examples 2 | 100.6 | 98.9 | 96.2 | 92.5 | 89.3 |
The test data explanation, granule of the present invention changes very little at the drug content of stability test after 80 days, and in the sample size fall 4% of embodiment 5-7, the content fall of the sample of commercially available prescription reference examples 2 after 80 days is 10.7%.Explain that technical scheme of the present invention has played positive effect to the stability of cefixime.
Table 3 cefalexin granule stability result of the test
| 0 day | 10 days | 20 days | 40 days | 80 days | |
| Embodiment 8 | 100.3 | 99.8 | 99.6 | 99.3 | 99.0 |
| Embodiment 9 | 99.8 | 99.6 | 99.5 | 99.4 | 98.6 |
| Embodiment 10 | 99.9 | 99.2 | 98.8 | 98.6 | 97.6 |
| Reference examples 3 | 100.3 | 98.6 | 97.2 | 96.5 | 94.3 |
The test data explanation, granule of the present invention changes very little at the drug content of stability test after 80 days, and in the sample size fall 3% of embodiment 8-10, the content fall of the sample of reference examples 3 after 80 days is 5.7%.Explain that technical scheme of the present invention has played positive effect to the stability of cefalexin.
Table 4 cefradine granule stability result of the test
| 0 day | 10 days | 20 days | 40 days | 80 days | |
| Embodiment 11 | 100.3 | 99.5 | 99.2 | 98.8 | 98.2 |
| Embodiment 12 | 99.8 | 99.4 | 98.9 | 98.7 | 98.3 |
| Embodiment 13 | 99.9 | 99.4 | 98.3 | 97.8 | 97.1 |
| Reference examples 4 | 100.3 | 98.6 | 96.8 | 93.2 | 90.1 |
The test data explanation, granule of the present invention changes very little at the drug content of stability test after 80 days, and in the sample size fall 3% of embodiment 11-13, the content fall of the sample of commercially available prescription reference examples 4 after 80 days is about 9.9%.Explain that technical scheme of the present invention has played positive effect to the stability of cefradine.
Claims (10)
1. stable cephalosporins pharmaceutical composition is characterized in that containing the cephalosporin behind the useful dextrin enclose.
2. the said cephalosporin of claim 1 is selected from a kind of in cefaclor, cefixime, cefalexin, the cefradine.
3. the said compositions of claim 1 is characterized in that in the inclusion process, and the mol ratio of dextrin and cephalosporin is 3～5: 1.
4. claim 1,2 or 3 said dextrin are alpha-cyclodextrin.
5. claim 1,2 or 3 said dextrin are beta-schardinger dextrin-.
6. the said preparation of compositions method of claim 1 is characterized in that:
The first step is pulverized adjuvant, crosses 100 mesh sieves;
The mol ratio of second step by dextrin and cephalosporin is 3～5: 1, takes by weighing a certain amount of dextrin, and the purified water dissolving with 3 times of weight adds cephalosporin, grinds;
The 3rd step filtered and grinds back material, washing, drying;
The 4th step was measured the content of cephalosporin in the clathrate according to the content assaying method of Pharmacopoeia of People's Republic of China regulation;
The 5th step was formulated prescription;
The 6th step was prepared raw material according to prescription, granulated by conventional method of granulating;
The 7th step packing.
7. the said preparation of compositions method of claim 6 is characterized in that cefaclor, cefixime clathrate bake out temperature are 40 ± 5 ℃.
8. the said preparation of compositions method of claim 6, the bake out temperature that it is characterized in that cefalexin, cefradine clathrate is 60 ± 5 ℃.
9. the said preparation of compositions method of claim 6, it is characterized in that implementing second step before, cefixime is used dissolve with methanol.
10. the said preparation of compositions method of claim 6, it is characterized in that implementing second step before, cefalexin or cefradine are used acetone solution.
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| CN2012101163825A CN102631684A (en) | 2012-04-11 | 2012-04-11 | Stable cephalosporin composition |
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| CN2012101163825A CN102631684A (en) | 2012-04-11 | 2012-04-11 | Stable cephalosporin composition |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103349646A (en) * | 2013-05-24 | 2013-10-16 | 海口市制药厂有限公司 | Medicinal composition containing cefaclor particles, and preparation method and application thereof |
| CN105287599A (en) * | 2015-10-14 | 2016-02-03 | 康普药业股份有限公司 | Cefradine pharmaceutical composition |
| CN109893663A (en) * | 2019-04-22 | 2019-06-18 | 苏州东瑞制药有限公司 | A kind of cefmetazole for injection composition and preparation method thereof |
Citations (1)
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| CN101264086A (en) * | 2007-03-14 | 2008-09-17 | 南京师范大学 | Medicinal composition containing cefixime cyclodextrin inclusion compound and preparation thereof |
-
2012
- 2012-04-11 CN CN2012101163825A patent/CN102631684A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101264086A (en) * | 2007-03-14 | 2008-09-17 | 南京师范大学 | Medicinal composition containing cefixime cyclodextrin inclusion compound and preparation thereof |
Non-Patent Citations (2)
| Title |
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| 张强 武凤兰主编: "《药剂学》", 31 January 2005 * |
| 张晓红等: ""羟丙基-beta-环糊精对头抱拉定的包合作用"", 《化学工程师》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103349646A (en) * | 2013-05-24 | 2013-10-16 | 海口市制药厂有限公司 | Medicinal composition containing cefaclor particles, and preparation method and application thereof |
| CN103349646B (en) * | 2013-05-24 | 2015-11-18 | 海口市制药厂有限公司 | A kind of pharmaceutical composition of cefaclor granule, its preparation method and application |
| CN105287599A (en) * | 2015-10-14 | 2016-02-03 | 康普药业股份有限公司 | Cefradine pharmaceutical composition |
| CN109893663A (en) * | 2019-04-22 | 2019-06-18 | 苏州东瑞制药有限公司 | A kind of cefmetazole for injection composition and preparation method thereof |
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Application publication date: 20120815 |