CN104382909A - Compound cefalexin injection - Google Patents
Compound cefalexin injection Download PDFInfo
- Publication number
- CN104382909A CN104382909A CN201410642085.3A CN201410642085A CN104382909A CN 104382909 A CN104382909 A CN 104382909A CN 201410642085 A CN201410642085 A CN 201410642085A CN 104382909 A CN104382909 A CN 104382909A
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- China
- Prior art keywords
- injection
- cefalexin
- fatty acid
- smooth
- ethyl cellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dermatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a method for preparing compound cefalexin injection. The composition comprises the following components in parts by weight: 2-5 parts of cefalexin, 1-2 parts of protostemonine, 1-5 parts of PVC (Polyvinyl Chloride), 1-2 parts of ethyecellulose, 1-3 parts of lecithin, 0.5-1 part of sorbitan fatty acid, 0.5-1 part of polysorbate and 1-3 parts of PEG. The composition disclosed by the invention is high in drug stability, high in solubility and simple in preparation process.
Description
Technical field
The present invention relates to a kind of preparation method of compound cefalexin injection.
Background technology
Cefalexin chemical name is: (6R, 7R)-3-methyl-7-[(R)-2-amino-2-phenylacetylamino]-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-formic acid-hydrate.Cefalexin belongs to first generation cephalosporin, except Enterococcus, methicillin-resistant Staphylococci, and streptococcus pneumoniae, Hemolytic streptococcus, product or not produce the staphylococcic most of bacterial strain of penicillinase responsive to this product.This product has better antibacterial action to neisseria, but the sensitivity of hemophilus influenza to this product is poor; This product has certain antibacterial action to part escherichia coli, proteus mirabilis, salmonella and shigella dysenteriae.All the other enterobacteriaceae lactobacteriaceaes, acinetobacter calcoaceticus, Pseudomonas aeruginosa, bacteroides fragilis all present drug resistance to this product.Fusobacterium and Wei Rong coccus are generally responsive to this product, and anaerobism gram positive coccus is to this product medium sensitivity.Be applicable to the respiratory tract infection such as the acute tonsillitis caused by sensitive organism, angina, otitis media, sinusitis, bronchitis, pneumonia, urinary tract infection and skin soft-tissue infection etc.This product is dissolved in methanol/ethanol, does not dissolve in water.Along with antibacterials abuse clinically, cause the drug resistance of antibacterial very general, as the curative effect of medication such as gentamycin, oxytetracycline, norfloxacin, norfloxacin conventional clinically reduces.Prevent with other, Therapeutic Method compares, Chinese herbal medicine has non-specific antimicrobial effect, and residual toxicity is lower, and animal generally not easily produces drug resistance to it.And Chinese medicine and Western medicine are carried out effective compatibility, the generation of Resistant strain can be slowed down.
Summary of the invention
The invention provides a kind of preparation method of compound cefalexin injection; This injection has the features such as solubility is good, good stability, and drug loading is high, safety of clinical trials is good, overcomes the deficiencies in the prior art part.
In compositions, the parts by weight of each component are: cefalexin 2-5 part; Protostermonine 1-2 part; PVC1-5 part; Ethyl cellulose 1-2 part; Lecithin 1-3 part; The smooth 0.5-1 part of fatty acid Pyrusussuriensis; Polysorbate 0.5-1 part; PEG1-3 part.
Described PVC molecular weight is between 5000-20000.
As preferably, it is characterized in that described emulsifying agent is the mixture of the smooth and Polysorbate of fatty acid Pyrusussuriensis, its ratio is than being 0.5:1-1:2.
As preferably, PVC is 3-5 part.
As preferably, fatty acid Pyrusussuriensis used is smooth is fatty acid Pyrusussuriensis smooth 80,40,20; Polysorbate is polyoxyethylene sorbitan monoleate, 40,20.
As preferably, described ethyl cellulose is selected from ethyl cellulose-4000 or ethyl cellulose-6000.
The preparation method of above-mentioned injection cefalexin, comprises the steps:
(1) each component is taken by formula proportion;
(2) cefalexin and ethyl cellulose, lecithin add in water for injection successively, and stirring and dissolving obtains interior aqueous phase W1;
(3) PVC, protostermonine, fatty acid Pyrusussuriensis is smooth and Polysorbate is dissolved in volume ratio is in the dichloromethane/acetone of 3: 1, obtains oil phase;
(4) PEG adds in water for injection to be stirred to and dissolves completely, obtains outer aqueous phase W2;
(5) under agitation slowly added in oil phase by W1, under ice bath, supersound process 20s obtains colostrum; Slowly added in W2 by colostrum and stir 10min and obtain emulsion, poured into by emulsion in the aqueous solution for injection of sodium chloride, ice bath stirs 4h volatile residue organic solvent, and collect microsphere by 0.45 μm of filtering with microporous membrane, water for injection washs 3 times, vacuum lyophilization.
Detailed description of the invention
Embodiment 1: a kind of compound cefalexin injection
Cefalexin 500g;
Protostermonine 100g
PVC400g；
Ethyl cellulose 100g;
Lecithin 100g;
The smooth 2050g of fatty acid Pyrusussuriensis;
Polysorbate 40 50g;
PEG100g；
Cefalexin and ethyl cellulose, lecithin are added successively in water for injection, stirring and dissolving obtains interior aqueous phase W1;
By PVC, protostermonine, fatty acid Pyrusussuriensis, smooth and Polysorbate is dissolved in volume ratio is in the dichloromethane/acetone of 3: 1, obtains oil phase; PEG is added in water for injection to be stirred to and dissolve completely, obtain outer aqueous phase W2; Under agitation slowly added in oil phase by W1, under ice bath, supersound process 20s obtains colostrum; Slowly added in W2 by colostrum and stir 10min and obtain emulsion, poured into by emulsion in the aqueous solution for injection of sodium chloride, ice bath stirs 4h volatile residue organic solvent, and collect microsphere by 0.45 μm of filtering with microporous membrane, water for injection washs 3 times, vacuum lyophilization.
Embodiment 2: a kind of compound cefalexin injection
Cefalexin 300g;
Protostermonine 100g
PVC100g；
Ethyl cellulose 200g;
Lecithin 50g;
The smooth 2050g of fatty acid Pyrusussuriensis;
Polysorbate 40 50g;
PEG200g；
Cefalexin and ethyl cellulose, lecithin are added successively in water for injection, stirring and dissolving obtains interior aqueous phase W1; By PVC, protostermonine, fatty acid Pyrusussuriensis, smooth and Polysorbate is dissolved in volume ratio is in the dichloromethane/acetone of 3: 1, obtains oil phase; PEG is added in water for injection to be stirred to and dissolve completely, obtain outer aqueous phase W2; Under agitation slowly added in oil phase by W1, under ice bath, supersound process 20s obtains colostrum; Slowly added in W2 by colostrum and stir 10min and obtain emulsion, poured into by emulsion in the aqueous solution for injection of sodium chloride, ice bath stirs 4h volatile residue organic solvent, and collect microsphere by 0.45 μm of filtering with microporous membrane, water for injection washs 3 times, vacuum lyophilization.
Embodiment 3: a kind of compound cefalexin injection
Cefalexin 100g;
Protostermonine 100g
PVC30g；
Ethyl cellulose 100g;
Lecithin 100g;
The smooth 2050g of fatty acid Pyrusussuriensis;
Polysorbate 40 100g;
PEG100g；
Cefalexin and ethyl cellulose, lecithin are added successively in water for injection, stirring and dissolving obtains interior aqueous phase W1; By PVC, protostermonine, fatty acid Pyrusussuriensis, smooth and Polysorbate is dissolved in volume ratio is in the dichloromethane/acetone of 3: 1, obtains oil phase; PEG is added in water for injection to be stirred to and dissolve completely, obtain outer aqueous phase W2; Under agitation slowly added in oil phase by W1, under ice bath, supersound process 20s obtains colostrum; Slowly added in W2 by colostrum and stir 10min and obtain emulsion, poured into by emulsion in the aqueous solution for injection of sodium chloride, ice bath stirs 4h volatile residue organic solvent, and collect microsphere by 0.45 μm of filtering with microporous membrane, water for injection washs 3 times, vacuum lyophilization.
Embodiment 4: droplet measurement
The injection of Example 1-3, is dissolved in water into the solution of every 1mL containing 1mg cefalexin, measures with laser diffraction particle size instrument.The cefalexin injection that acetonideexample 1-3 prepares is spherical shape, and even particle size distribution, whole particle diameter is between 300-550nm.
Embodiment 5: envelop rate detects
The injection of cefalexin is dissolved in water into the solution of every 1mL containing cefalexin 1mg, with the centrifugation 15min of 6000r/min, gets supernatant 1mL, with dissolve with ethanol, measure the content of cefalexin.
Dose in envelop rate=microsphere/(dose in the dose+medium in microsphere) × 100%
The envelop rate of injection prepared by embodiment 1-3, between 80%-90%.
Claims (7)
1. a compound cefalexin injection, is characterized in that the parts by weight of component are:
Cefalexin 1-5 part
Protostermonine 1-2 part
PVC1-5 part
Ethyl cellulose 1-2 part
Lecithin 1-3 part
The smooth 0.5-1 part of fatty acid Pyrusussuriensis
Polysorbate 0.5-1 part
PEG1-3 part
Described PVC molecular weight is between 5000-20000.
2. pharmaceutical composition as claimed in claim 1, is characterized in that the ratio of described cefalexin and protostermonine is 1:1-5:1.
3. pharmaceutical composition as claimed in claim 1, it is characterized in that described emulsifying agent is the mixture of the smooth and Polysorbate of fatty acid Pyrusussuriensis, its ratio is than being 0.5:1-1:2.
4. pharmaceutical composition as claimed in claim 1, is characterized in that PVC is 3-5 part.
5. pharmaceutical composition as claimed in claim 1, it is characterized in that fatty acid Pyrusussuriensis used smooth be fatty acid Pyrusussuriensis smooth 80,40,20; Polysorbate is polyoxyethylene sorbitan monoleate, 40,20.
6. pharmaceutical composition as claimed in claim 1, is characterized in that described ethyl cellulose is selected from ethyl cellulose-4000 or ethyl cellulose-6000.
7. the preparation method of compound cefalexin injection as described in claim arbitrary in claim 1-5, comprises the steps:
(1) each component is taken by formula proportion;
(2) cefalexin and ethyl cellulose, lecithin add in water for injection successively, and stirring and dissolving obtains interior aqueous phase W1;
(3) PVC, protostermonine, fatty acid Pyrusussuriensis is smooth and Polysorbate is dissolved in volume ratio is in the dichloromethane/acetone of 3: 1, obtains oil phase;
(4) PEG adds in water for injection to be stirred to and dissolves completely, obtains outer aqueous phase W2;
(5) under agitation slowly added in oil phase by W1, under ice bath, supersound process 20s obtains colostrum; Slowly added in W2 by colostrum and stir 10min and obtain emulsion, poured into by emulsion in the aqueous solution for injection of sodium chloride, ice bath stirs 4h volatile residue organic solvent, and collect microsphere by 0.45 μm of filtering with microporous membrane, water for injection washs 3 times, vacuum lyophilization.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410642085.3A CN104382909A (en) | 2014-11-13 | 2014-11-13 | Compound cefalexin injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410642085.3A CN104382909A (en) | 2014-11-13 | 2014-11-13 | Compound cefalexin injection |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104382909A true CN104382909A (en) | 2015-03-04 |
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ID=52600935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410642085.3A Pending CN104382909A (en) | 2014-11-13 | 2014-11-13 | Compound cefalexin injection |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104382909A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106806372A (en) * | 2015-12-01 | 2017-06-09 | 上海交通大学 | Purposes of the protostermonine in anti-asthmatic medicament is prepared |
| CN107496430A (en) * | 2017-09-13 | 2017-12-22 | 南通荣成医药化工有限公司 | A kind of Cefradine pharmaceutical composition |
| CN107519173A (en) * | 2017-09-13 | 2017-12-29 | 南通荣成医药化工有限公司 | A kind of new Cefuroxime axetil pharmaceutical composition |
| CN107569489A (en) * | 2017-09-13 | 2018-01-12 | 南通荣成医药化工有限公司 | A kind of compound preparation of ceftiofur sodium |
| CN107595801A (en) * | 2017-09-13 | 2018-01-19 | 南通荣成医药化工有限公司 | A kind of new Cefuroxime axetil pharmaceutical composition |
-
2014
- 2014-11-13 CN CN201410642085.3A patent/CN104382909A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106806372A (en) * | 2015-12-01 | 2017-06-09 | 上海交通大学 | Purposes of the protostermonine in anti-asthmatic medicament is prepared |
| CN106806372B (en) * | 2015-12-01 | 2019-10-08 | 上海交通大学 | Protostermonine is preparing the purposes in anti-asthmatic medicament |
| CN107496430A (en) * | 2017-09-13 | 2017-12-22 | 南通荣成医药化工有限公司 | A kind of Cefradine pharmaceutical composition |
| CN107519173A (en) * | 2017-09-13 | 2017-12-29 | 南通荣成医药化工有限公司 | A kind of new Cefuroxime axetil pharmaceutical composition |
| CN107569489A (en) * | 2017-09-13 | 2018-01-12 | 南通荣成医药化工有限公司 | A kind of compound preparation of ceftiofur sodium |
| CN107595801A (en) * | 2017-09-13 | 2018-01-19 | 南通荣成医药化工有限公司 | A kind of new Cefuroxime axetil pharmaceutical composition |
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Application publication date: 20150304 |
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| WD01 | Invention patent application deemed withdrawn after publication |