CN102397252A - Cefradine lipidosome for injection and preparation method thereof - Google Patents
Cefradine lipidosome for injection and preparation method thereof Download PDFInfo
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- CN102397252A CN102397252A CN2011102296073A CN201110229607A CN102397252A CN 102397252 A CN102397252 A CN 102397252A CN 2011102296073 A CN2011102296073 A CN 2011102296073A CN 201110229607 A CN201110229607 A CN 201110229607A CN 102397252 A CN102397252 A CN 102397252A
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- injection
- cefradine
- cefaloridine
- liposome
- dspe
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Abstract
The invention relates to the technical field of medical technology and discloses cefradine lipidosome for injection and a preparation method thereof. The cefradine lipidosome comprises the following raw materials in parts by weight: 1 part of cefradine lipidosome (aseptic), 0.03-0.1 part of sodium carbonate, 3-5 parts of soybean lecithin, 0.8-2 parts of cholesterol, 0.03-0.1 part of vitamin E and 0.2-0.3 part of DSPE-PEG (Dipalmitoylphosphatidylethanolamine-Polyethylene Glycol). The product has the advantages of high stability, small side effect, effective reduction in the toxic and side effects of a medicament, reduction in the dosage of the medicament, relieving in the injection pain and contribution to enhancing the treatment compliance of a patient. Cracking caused by dehydration, fusion, crystal generation and the like does not occur in the freeze drying process, high envelop rate can be kept after water freezing, and convenience is brought to product transportation and storage.
Description
Technical field
The present invention relates to medical technical field, related in particular to a kind of cefaloridine for injection liposome and preparation method thereof.
Background technology
The cefaloridine for injection Main Ingredients and Appearance is a cefradine, its chemical being called (6R, 7R)-7 [(R)-2-amino-2-(1, the 4-cyclohexenyl group) acetylamino]-3-methyl-8-oxo-5-thia-1-azabicyclo (4.2.0) oct-2-ene-2-carboxylic acid, molecular formula C
16H
19N
3O
4S, molecular weight 349.40; These article are that first generation cephalosporin is not to producing penicillinase and the good antibacterial action of part bacterial strain tool that produces penicillinase gold Portugal bacterium, CN-S, GPCs such as A group Hemolytic streptococcus, streptococcus pneumoniae and Streptococcus viridans.How responsive the anaerobism gram positive bacteria is to these article, and bacteroides fragilis presents drug resistance to these article.Methicillin-resistant staphylococcus, Enterococcus are to this article drug resistance.These article are similar with cefalexin with the effect of gram-negative bacteria to gram positive bacteria, and these article have certain effect to gonococcus, and also tool is active to producing the enzyme gonococcus; Active relatively poor to hemophilus influenza.These article mainly are applicable to respiratory tract infection urogenital infections such as acute pharyngitis tonsillitis otitis media, bronchitis and the pneumonia due to the sensitive organism and skin soft-tissue infection etc.
Because cefradine stability toxic and side effects not high, medicine is bigger, particularly intravenous injection pain, patient's compliance is poor, has influenced therapeutic effect.
Liposome is a kind of microcapsule of bimolecular tunic, and similar is in human body cell, and microcapsule diameter is hundreds of to several thousand dusts.Liposome can be delivered to diseased region to improve the Drug therapy index with medicine parcel back orientation as pharmaceutical carrier, can effectively reduce the toxic and side effects of medicine; Can significantly improve the stability of drug products; Alleviate injection pain simultaneously, help improving the compliance of patient, improve therapeutic effect.
Summary of the invention
It is high to the purpose of this invention is to provide a kind of stability, can effectively reduce the toxic and side effects of medicine, can alleviate the medicine injection pain, helps improving the patient compliance, improves the cefaloridine for injection liposome and the method for preparing of therapeutic effect.
In order to solve the problems of the technologies described above, the present invention is able to solve through following technical proposals:
The cefaloridine for injection liposome comprises the raw material of following weight portion:
1 part of cefradine (aseptic);
0.03～0.1 part of sodium carbonate;
3～5 parts of soybean lecithins;
0.8～2 part in cholesterol;
0.03～0.1 part of vitamin E;
0.2～0.3 part of DSPE-PEG.
As preferably, contain cefradine 500g, sodium carbonate 20g, soybean lecithin 1500g, cholesterol 500g, vitamin E 20g, DSPE-PEG 125g in described per 1000 bottles of cefaloridine for injection liposomees.
As preferably, contain cefradine 1000g, sodium carbonate 40g, soybean lecithin 3000g, cholesterol 1000g, vitamin E 40g, DSPE-PEG 250g in described per 1000 bottles of cefaloridine for injection liposomees.
DSPE-PEG (Polyethylene Glycol-DSPE) is a kind of liposome dressing agent, and liposome membrane is carried out modifying and decorating, can make liposome residence time in blood prolong the effect that has effectively prolonged medicine.The selectivity of medicine to target tissue also is provided simultaneously, can have escaped the seizure of reticuloendothelial system, effectively reduced poisonous side effect of medicine and untoward reaction.
The method of the cefaloridine for injection liposome described in the preparation technique scheme comprises the following steps:
(1) soybean lecithin, cholesterol, vitamin E, DSPE-PEG are dissolved in the chloroform organic solvent by said ratio; Heated and stirred is uniformly dispersed; Organic solvent is removed in decompression on rotary film evaporator; Make immobilized artificial membrane, adding an amount of pH value again is 5.6 citric acid-buffer solution stirring and dissolving, obtains blank liposome solution;
(2) cefradine (aseptic) and the sodium carbonate with recipe quantity is dissolved in the 3000-6000ml water for injection; Fully dissolving adds above-mentioned blank liposome solution then, and temperature is controlled at 45-60 ℃ and stirred 20-40 minute; Stir fully dissolving; Mix homogeneously, solution obtain the cefradine liposome solutions with the membrane filtration of 0.22 μ m;
(3) above-mentioned solution is carried out spray drying, packing is 1000 bottles under aseptic condition, makes the cefaloridine for injection Liposomal formulation.
The present invention has significant technique effect owing to adopted above technical scheme:
Product stability of the present invention is high, and side effect is little, can effectively reduce the toxic and side effects of medicine, reduces drug dose, alleviates injection pain simultaneously, helps improving the compliance of patient.
Can not break in the freeze-drying process, after aquation is melted again, can keep good envelop rate, make things convenient for Product transport and storage because of dehydration, fusion, ice crystal generation etc.
The specific embodiment
Below in conjunction with embodiment the present invention is described in further detail:
Embodiment 1
The cefaloridine for injection liposome comprises following raw materials according and content in per 1000 bottles of cefaloridine for injection liposomees:
Cefradine (aseptic) 500g;
Sodium carbonate 20g;
Soybean lecithin 1500g;
Cholesterol 500g;
Vitamin E 20g;
DSPE-PEG 125g。
Prepare the method for above-mentioned cefaloridine for injection liposome, comprise the following steps:
(1) soybean lecithin, cholesterol, vitamin E, DSPE-PEG are dissolved in the chloroform organic solvent by said ratio; Heated and stirred is uniformly dispersed; Organic solvent is removed in decompression on rotary film evaporator; Make immobilized artificial membrane, adding an amount of pH value again is 5.6 citric acid-buffer solution stirring and dissolving, obtains blank liposome solution;
(2) cefradine (aseptic) and the sodium carbonate with recipe quantity is dissolved in the 3000ml water for injection; Fully dissolving adds above-mentioned blank liposome solution then, and temperature is controlled at 50 ℃ and stirred 30 minutes; Stir fully dissolving; Mix homogeneously, solution obtain the cefradine liposome solutions with the membrane filtration of 0.22 μ m;
(3) above-mentioned solution is carried out spray drying, packing is 1000 bottles under aseptic condition, makes the cefaloridine for injection Liposomal formulation.
Embodiment 2
The cefaloridine for injection liposome comprises following raw materials according and content in per 1000 bottles of cefaloridine for injection liposomees:
Cefradine (aseptic) 1000g;
Sodium carbonate 40g;
Soybean lecithin 3000g;
Cholesterol 1000g;
Vitamin E 40g;
DSPE-PEG 250g。
Prepare the method for above-mentioned cefaloridine for injection liposome, comprise the following steps:
(1) soybean lecithin, cholesterol, vitamin E, DSPE-PEG are dissolved in the chloroform organic solvent by said ratio; Heated and stirred is uniformly dispersed; Organic solvent is removed in decompression on rotary film evaporator; Make immobilized artificial membrane, adding an amount of pH value again is 5.6 citric acid-buffer solution stirring and dissolving, obtains blank liposome solution;
(2) cefradine (aseptic) and the sodium carbonate with recipe quantity is dissolved in the 6000ml water for injection; Fully dissolving adds above-mentioned blank liposome solution then, and temperature is controlled at 50 ℃ and stirred 30 minutes; Stir fully dissolving; Mix homogeneously, solution obtain the cefradine liposome solutions with the membrane filtration of 0.22 μ m;
(3) above-mentioned solution is carried out spray drying, packing is 1000 bottles under aseptic condition, makes the cefaloridine for injection Liposomal formulation.
Stability study:
1, accelerated test
Get 3 lot sample article, simulation listing packing is put 40 ℃ ± 2 ℃ of temperature; Placed 6 months in the constant temperature and humidity incubator of relative humidity 75% ± 5%,, measure each item and investigate index in placing each sampling at 1,2,3,6 the end of month once; And compare with 0 month result, the result sees table 1-1:
Table 1-1 cefaloridine for injection liposome accelerated test result
2, long term test
Get 3 lot sample article, simulation listing packing is put 25 ℃ ± 2 ℃ of temperature; Placed 24 months in the constant temperature and humidity incubator of relative humidity 60% ± 10%,, measure each item and investigate index in placing each sampling at 0,3,6,9,12,18,24 the end of month once; And compare with 0 month result, the result sees table 1-2:
Table 1-2 cefaloridine for injection liposome long-term test results
Result of the test:
Accelerated test: these article accelerated test 6 months under 40 ℃ ± 2 ℃, RH75% ± 5% condition, content, each item indexs such as related substance, polymer have no significant change.
Long term test: these article long term test 24 months under 25 ℃ ± 2 ℃, RH60% ± 10% condition, content, each item indexs such as related substance, polymer have no significant change.
In a word, the above is merely preferred embodiment of the present invention, and all equalizations of doing according to claim of the present invention change and modify, and all should belong to the covering scope of patent of the present invention.
Claims (4)
1. the cefaloridine for injection liposome is characterized in that, comprises the raw material of following weight portion:
1 part of cefradine (aseptic);
0.03～0.1 part of sodium carbonate;
3～5 parts of soybean lecithins;
0.8～2 part in cholesterol;
0.03～0.1 part of vitamin E;
0.2～0.3 part of DSPE-PEG.
2. cefaloridine for injection liposome according to claim 1 is characterized in that: contain cefradine 500g, sodium carbonate 20g, soybean lecithin 1500g, cholesterol 500g, vitamin E 20g, DSPE-PEG 125g in per 1000 bottles of cefaloridine for injection liposomees.
3. cefaloridine for injection liposome according to claim 1 is characterized in that: contain cefradine 1000g, sodium carbonate 40g, soybean lecithin 3000g, cholesterol 1000g, vitamin E 40g, DSPE-PEG 250g in per 1000 bottles of cefaloridine for injection liposomees.
4. preparation is characterized in that like the method for the described cefaloridine for injection liposome of claim 1-3, may further comprise the steps:
(1) soybean lecithin, cholesterol, vitamin E, DSPE-PEG are dissolved in the chloroform organic solvent by said ratio; Heated and stirred is uniformly dispersed; Organic solvent is removed in decompression on rotary film evaporator; Make immobilized artificial membrane, adding an amount of pH value again is 5.6 citric acid-buffer solution stirring and dissolving, obtains blank liposome solution;
(2) cefradine (aseptic) and the sodium carbonate with recipe quantity is dissolved in the 3000-6000ml water for injection; Fully dissolving adds above-mentioned blank liposome solution then, and temperature is controlled at 45-60 ℃ and stirred 20-40 minute; Stir fully dissolving; Mix homogeneously, solution obtain the cefradine liposome solutions with the membrane filtration of 0.22 μ m;
(3) above-mentioned solution is carried out spray drying, packing is 1000 bottles under aseptic condition, makes the cefaloridine for injection Liposomal formulation.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2011102296073A CN102397252A (en) | 2011-08-11 | 2011-08-11 | Cefradine lipidosome for injection and preparation method thereof |
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| CN2011102296073A CN102397252A (en) | 2011-08-11 | 2011-08-11 | Cefradine lipidosome for injection and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5874455A (en) * | 1993-11-05 | 1999-02-23 | Gakko Hojin Kinki Daigaku | Method for treatment of cataract with radical scavenger |
| CN101623263A (en) * | 2009-08-24 | 2010-01-13 | 海南美大制药有限公司 | Cefminox sodium liposome preparation |
-
2011
- 2011-08-11 CN CN2011102296073A patent/CN102397252A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5874455A (en) * | 1993-11-05 | 1999-02-23 | Gakko Hojin Kinki Daigaku | Method for treatment of cataract with radical scavenger |
| CN101623263A (en) * | 2009-08-24 | 2010-01-13 | 海南美大制药有限公司 | Cefminox sodium liposome preparation |
Non-Patent Citations (4)
| Title |
|---|
| 《J. Pharrn. Pharmacol》 19801231 TOSHIKIRO KIMURA, MICHIYO YOSHIKAWA, MASATO YASUHARA AND HITOSHI The use of liposomes as a model for drug absorption: beta-lactam antibiotics 394-398,第394页右栏最后1段 1-4 第32卷, * |
| TOSHIKIRO KIMURA, MICHIYO YOSHIKAWA, MASATO YASUHARA AND HITOSHI: "The use of liposomes as a model for drug absorption: β-lactam antibiotics", 《J. PHARRN. PHARMACOL》 * |
| 周勤等，: "碳酸钠对头孢拉定助溶效果的研究", 《中国医药工业杂志》 * |
| 王昭等,: "甲氧基聚乙二醇-二-硬脂酰磷脂酰乙醇胺长循环脂质体的制备", 《世界最新医学信息文摘》 * |
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Application publication date: 20120404 |