CN102836129A - Cefprozil dry suspension and preparation method thereof - Google Patents
Cefprozil dry suspension and preparation method thereof Download PDFInfo
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- CN102836129A CN102836129A CN2011101689450A CN201110168945A CN102836129A CN 102836129 A CN102836129 A CN 102836129A CN 2011101689450 A CN2011101689450 A CN 2011101689450A CN 201110168945 A CN201110168945 A CN 201110168945A CN 102836129 A CN102836129 A CN 102836129A
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Abstract
The invention discloses a cefprozil dry suspension and preparation method thereof. The invention aims at solving a cefprozil defect of instability to heat and humidity. According to the invention, cefprozil is subjected to pellet coating, such that stability and compressibility of cefprozil are improved. With the pellet coating method, odor of cefprozil is covered. With the assistance of a sweetening agent and an essence, the taste is well improved. Therefore, a cefprozil dry suspension is provided. The invention also discloses a cold processing dry granulation method for granulating. During an extrusion process, water circulation (wherein the inner part of an extrusion roller does not contact the material) is carried out for cooling the extrusion roller, such that the material does not contact moisture and high temperature during the entire processing process. Therefore, stability and treatment effect of cefprozil medicines are ensured.
Description
One, technical field
The present invention relates to cefprozil dry suspension and preparation method thereof.
Two, background technology:
Cefprozil (Cefprozil) is the oral cephalosporin of drugs approved by FDA listing in the end of the year 1991, executes your treasured by the U.S. and produces listing in 1992.Cefprozil is roughly similar to the inhibitory action and the first generation cephalosporin of gram positive bacteria, and the inhibitory action of most gram negative bacterias is obviously strengthened, and is efficient and stable to multiple beta-lactamase to anaerobe.
Cefprozil is as cephalosporins of new generation; Because of it has has a broad antifungal spectrum; Antibacterial activity is strong; To the mould characteristics of beta-lactam, become clinically that treatment is light, one of moderate respiratory tract infection choice drug, and be one of choice drug of the treatment community acquired pneumonia of generally acknowledging both at home and abroad with good stable property.
The cefprozil oral absorption is good; There is 95% dosage to be absorbed approximately; Longer relatively because of its plasma half-life, make cefprozil be administered once in one day or secondary also can provide lasting antibacterial action, therapeutic regimen is easy; Improve patient's compliance and compliance, practiced thrift patient's treatment cost simultaneously.
Cefprozil has good safety; The more traditional cephalosporin incidence rate of untoward reaction is low; And nephrotoxicity has bigger alleviating than former generation, cefprozil become drugs approved by FDA first can be used for treating the cephalosporins of child's otitis media and sinusitis.
The cefprozil dry suspension is compared with tablet, more is applicable to child patient, compares with oral liquid, syrup; Advantage is to need not in the production process to add any antiseptic; Be convenient to transportation, product adopts unit dose package, and all ages and classes section child all has clear and definite usage and dosage; It is poor to have solved stability of Oral, and the syrup medication dose is difficult to control, repeatedly uses problems such as pollution easily.
Three, summary of the invention
The present invention is just to the shortcoming of cefprozil to heat and moist lability method; Thereby it is carried out the micropill parcel increases its stability, improves compressibility; The abnormal flavour that hides cefprozil itself cooperates the adding of sweeting agent and essence well to improve mouthfeel, and a kind of cefprozil dry suspension that provides.
Technical scheme of the present invention is following:
A kind of cefprozil dry suspension uses polyvinylpyrrolidone, ethyl cellulose, hydroxypropyl methylcellulose or Polyethylene Glycol that cefprozil is carried out the micropill parcel, mainly is made up of cefprozil micropill and citric acid.Their quality proportioning is: cefprozil A gram, polyvinylpyrrolidone, ethyl cellulose, hydroxypropyl methylcellulose or Polyethylene Glycol (0.03～0.2) A gram, citric acid, tartaric acid or adipic acid (1～3) A gram.
Above-mentioned cefprozil dry suspension can add edible essence (0.1～1) A gram in its component.
Above-mentioned cefprozil dry suspension can add sweeting agent (5～20) A gram in its component.Said sweeting agent can be sucrose, glucose, aspartame or stevioside etc.
Above-mentioned cefprozil dry suspension can add food coloring (0.3～0.6) A gram in its component.
Cefprozil dry suspension to mentioned component; The present invention also relates to the method for preparing of cefprozil dry suspension simultaneously: above-mentioned cefprozil dry suspension uses dry granulation method system granule; Use the cold working granulating process; In extrusion process, pinch roller is lowered the temperature simultaneously, make material in whole process of production, not touch moisture content and high temperature, guaranteed the stability and the curative effect of cefprozil medicine through water cycle.
Concrete method for preparing is following:
(1) former, adjuvant were all placed under 50 ℃ dry 4 hours in advance, it is subsequent use to cross 60 mesh sieves;
(2) use polyvinylpyrrolidone, ethyl cellulose, hydroxypropyl methylcellulose or Polyethylene Glycol carry out the micropill parcel to cefprozil, make micropill;
(3) get cefprozil micropill and citric acid, tartaric acid or adipic acid add or do not add sweeting agent, edible essence, mix, and must mix powder;
(4) get mixed powder and carry out the cold working dry granulation, in granule extrusion process, pinch roller is lowered the temperature, make granule avoid contacting moisture content and high temperature through water cycle;
(5) pack after getting dried granule, maybe, promptly get cefprozil dry suspension of the present invention packing behind dried granule and the food coloring mixing.
In sum, medicine of the present invention has following characteristics:
1, the cephalo propylene feedstocks is adopted polyvinylpyrrolidone; Ethyl cellulose, hydroxypropyl methylcellulose or Polyethylene Glycol wrap up, and ratio accounts for 3%～20% of cefprozil; Can effectively hide the abnormal flavour of cefprozil, and all increase significantly for stability of drug.
2, the present invention adopts dry suspension, adds an amount of correctives and makes abnormal smells from the patient fragrance, and taste is fragrant and sweet, has hidden the abnormal flavour of cefprozil itself, therefore is particularly suitable for children taking.
3, the present invention adds citric acid after this has fully studied the character of cefprozil, and tartaric acid or adipic acid not only have raising preferably and after brewing, make cefprozil under acid condition for stability of drug products, increase its dissolubility.
4, the preparation technology of dried mix suspension grain adopts cold working dry granulation technology to granulate; In extrusion process, pinch roller is lowered the temperature simultaneously through water cycle (pinch roller inside does not contact with material); Make material in whole process of production, not touch moisture content and high temperature, guaranteed the stability and the curative effect of cefprozil medicine.
Four, the specific embodiment
Embodiment 1 (by 1000 bags of calculating of preparation)
Prescription
At first, former, adjuvant are all placed under 50 ℃ of conditions dry 4 hours in advance, subsequent use: as to get cefprozil then; Use polyvinylpyrrolidone that cefprozil is carried out the micropill coating; Get aspartame, citric acid, strawberry essence again,, cross 60 mesh sieves by equivalent incremental method mix homogeneously; Cross 18 mesh sieve granulate behind the cold working dry granulation, with the food coloring mixing.The aluminum-plastic composite membrane packing, every bag 1.8g contains cefprozil 100mg.
Embodiment 2 (by 1000 bags of calculating of preparation)
At first, former, adjuvant are all placed under 50 ℃ of conditions dry 4 hours in advance, subsequent use: as to get cefprozil then; Use ethyl cellulose that cefprozil is carried out the micropill coating; Get aspartame, tartaric acid, strawberry essence again,, cross 60 mesh sieves by equivalent incremental method mix homogeneously; Cross 18 mesh sieve granulate behind the cold working dry granulation, with the food coloring mixing.The aluminum-plastic composite membrane packing, every bag 1.5g contains cefprozil 100mg.
Embodiment 3 (by 1000 bags of calculating of preparation)
At first, former, adjuvant are all placed under 50 ℃ of conditions dry 4 hours in advance, subsequent use: as to get cefprozil then; Use hydroxypropyl methylcellulose that cefprozil is carried out the micropill coating; Get aspartame, citric acid, strawberry essence again,, cross 60 mesh sieves by equivalent incremental method mix homogeneously; Cross 18 mesh sieve granulate behind the cold working dry granulation, with the food coloring mixing.The aluminum-plastic composite membrane packing, every bag 1.5g contains cefprozil 100mg.
Embodiment 4 (by 1000 bags of calculating of preparation)
At first, former, adjuvant are all placed under 50 ℃ of conditions dry 4 hours in advance, subsequent use: as to get cefprozil 100g then; Use polyvinylpyrrolidone that cefprozil is carried out the micropill coating; Get sucrose, adipic acid, strawberry essence again,, cross 60 mesh sieves by equivalent incremental method mix homogeneously; Cross 18 mesh sieve granulate behind the cold working dry granulation, with the food coloring mixing.The aluminum-plastic composite membrane packing, every bag 1.5g contains cefprozil 100mg.
Embodiment 5 (by 1000 bags of calculating of preparation)
At first, former, adjuvant are all placed under 50 ℃ of conditions dry 4 hours in advance, subsequent use: as to get cefprozil then; Use Polyethylene Glycol that cefprozil is carried out the micropill coating; Get glucose, tartaric acid, strawberry essence again,, cross 60 mesh sieves by equivalent incremental method mix homogeneously; Cross 18 mesh sieve granulate behind the cold working dry granulation, with the food coloring mixing.The aluminum-plastic composite membrane packing, every bag 1.5g contains cefprozil 100mg.
Embodiment 6 (by 1000 bags of calculating of preparation)
At first, former, adjuvant are all placed under 50 ℃ of conditions dry 4 hours in advance, subsequent use: as to get cefprozil then; Use the 30g hydroxypropyl methyl fiber that cefprozil is carried out the micropill coating; Get aspartame, citric acid, strawberry essence again,, cross 60 mesh sieves by equivalent incremental method mix homogeneously; Cross 18 mesh sieve granulate behind the cold working dry granulation, with the food coloring mixing.The aluminum-plastic composite membrane packing, every bag 1.5g contains cefprozil 100mg.
Five. the stability test data are relatively
Getting the cefprozil dry suspension of instance of the present invention 1, embodiment 3 and embodiment 5 preparations and cefprozil dry suspension that expensive precious pharmaceutical Co. Ltd is executed in Shanghai is 40 ℃ ± 2 ℃ in temperature, and relative humidity is 75% ± 5% condition held 6 months.
Investigation project: character, related substance and content.The investigation result is following:
Result of the test shows, the product quality of instance of the present invention 1, embodiment 3 and embodiment 5 preparations is more stable, and the variation of content and related substance is less, and explain by the cefprozil dry suspension of the present invention's technology preparation has superiority in raising aspect stable.
Claims (8)
1. a cefprozil dry suspension is characterized in that: use polyvinylpyrrolidone, ethyl cellulose; Hydroxypropyl methylcellulose or Polyethylene Glycol carry out the micropill parcel to cefprozil, and it is mainly by cefprozil micropill and citric acid, and tartaric acid or adipic acid are formed; Their quality proportioning is: cefprozil: polyvinylpyrrolidone; Ethyl cellulose, hydroxypropyl methylcellulose or Polyethylene Glycol: citric acid, tartaric acid or adipic acid=1: 0.03～0.2: 1～3.
2. cefprozil dry suspension according to claim 1 is characterized in that: in its component, add edible essence, the mass ratio of cefprozil and edible essence is: cefprozil: edible essence=1: 0.1～1.
3. cefprozil dry suspension according to claim 1 and 2 is characterized in that: in its component, add sweeting agent, the mass ratio of cefprozil and sweeting agent is: cefprozil: sweeting agent=1: 5～20.
4. cefprozil dry suspension according to claim 3 is characterized in that: the sweeting agent of being selected for use is sucrose, glucose, aspartame or stevioside etc.
5. cefprozil dry suspension according to claim 1 and 2 is characterized in that, in its component, adds food coloring, and the mass ratio of cefprozil and food coloring is: cefprozil: food coloring=1: 0.1～0.8.
6. method for preparing claim 1 or 2 described cefprozil dry suspension is characterized in that it is made up of the lower class step:
(1) former, adjuvant were all placed under 50 ℃ of conditions dry 4 hours in advance, it is subsequent use to cross 60 mesh sieves;
(2) use polyvinylpyrrolidone, ethyl cellulose, hydroxypropyl methylcellulose or Polyethylene Glycol carry out the micropill parcel to cefprozil, get cefprozil micropill and citric acid behind the parcel, and tartaric acid or adipic acid add or do not add edible essence, mix, and must mix powder;
(3) use the dry granulation machine to granulate, make the dried granule about 18 orders;
(4), maybe, promptly get the cefprozil dry suspension with packing behind dried granule and the food coloring mixing with dried granule packaging.
7. the method for making of cefprozil dry suspension according to claim 5 is characterized in that: in the step (2), also be added with sweeting agent.
8. the method for making of cefprozil dry suspension according to claim 5; It is characterized in that: adopt cold working dry granulation technology in the step (3); In extrusion process, pinch roller is lowered the temperature simultaneously through water cycle (pinch roller inside does not contact with material); Make material in whole process of production, not touch moisture content and high temperature, guaranteed the stability and the curative effect of cefprozil medicine.
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| CN201110168945.0A CN102836129B (en) | 2011-06-22 | 2011-06-22 | Cefprozil dry suspension and preparation method thereof |
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| CN201110168945.0A CN102836129B (en) | 2011-06-22 | 2011-06-22 | Cefprozil dry suspension and preparation method thereof |
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| CN102836129B CN102836129B (en) | 2014-06-11 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110960498A (en) * | 2019-12-25 | 2020-04-07 | 南京亿华药业有限公司 | Preparation method of heat-unstable pharmaceutical composition |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101152159A (en) * | 2006-09-28 | 2008-04-02 | 莫敬柱 | Cefuroxime axetil taste masking pellet and method of preparing the same |
| CN101953789A (en) * | 2010-06-17 | 2011-01-26 | 王丽燕 | Dry suspension containing cefprozil liposome and preparation method thereof |
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2011
- 2011-06-22 CN CN201110168945.0A patent/CN102836129B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101152159A (en) * | 2006-09-28 | 2008-04-02 | 莫敬柱 | Cefuroxime axetil taste masking pellet and method of preparing the same |
| CN101953789A (en) * | 2010-06-17 | 2011-01-26 | 王丽燕 | Dry suspension containing cefprozil liposome and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 王从品等: "掩味头孢丙烯干混悬剂的制备及质", 《中国药房》, vol. 20, no. 34, 31 December 2009 (2009-12-31), pages 2689 - 2691 * |
| 王从品等: "掩味头孢丙烯干混悬剂的制备及质量控制", 《中国药房》, vol. 20, no. 34, 31 December 2009 (2009-12-31), pages 2689 - 2691 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110960498A (en) * | 2019-12-25 | 2020-04-07 | 南京亿华药业有限公司 | Preparation method of heat-unstable pharmaceutical composition |
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