CN103285371A - Antibacterial peptide stable preparation and preparation method thereof - Google Patents
Antibacterial peptide stable preparation and preparation method thereof Download PDFInfo
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- CN103285371A CN103285371A CN2013100443151A CN201310044315A CN103285371A CN 103285371 A CN103285371 A CN 103285371A CN 2013100443151 A CN2013100443151 A CN 2013100443151A CN 201310044315 A CN201310044315 A CN 201310044315A CN 103285371 A CN103285371 A CN 103285371A
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Abstract
The invention provides an antibacterial peptide stable preparation and a preparation method thereof. The preparation takes an antibacterial peptide liquid fermentation product as a main component, and is prepared from the antibacterial peptide liquid fermentation product, polyethylene glycol and beta-cyclodextrin according to certain process. Compared with other preparations, the preparation provided in the invention can prevent the antibacterial peptide from degrading and inactivating in a digestive tract. Also, the preparation process is simple and has high bioavailability, thus being very suitable for industrial production.
Description
Technical field
The present invention relates to a kind of antibacterial peptide stabilization formulations and preparation method thereof, said preparation is main component with the antibacterial peptide liquid fermentation production, and is formulated by certain technology with Polyethylene Glycol, beta-schardinger dextrin-.Preparation of the present invention is compared with other preparations, can make antibacterial peptide avoid the inactivation that is degraded in digestive tract, and preparation technology is simple, bioavailability is high, is fit to very much suitability for industrialized production.
Background technology
(antibacterial peptides is a kind of little peptide of cation with strong antibacterial action that organism produces ABP) to antibacterial peptide, is the important composition composition of biological innate immunity.Up to now, comprised more than 2000 kind of antibacterial active peptide of discovery in insecticide, birds, animal, plant and the prokaryote at many biologies.Effect studies show that antibacterial peptide is broad-spectrum antiseptic not only, can press down kill endurance strain, and its bactericidal mechanism makes pathogen be difficult for producing the drug resistance sudden change, thereby becomes one of antibiotic succedaneum of tool DEVELOPMENT PROSPECT.
Antibacterial peptide has broad spectrum antibiotic activity, and finds that wherein some kind has the ability of antitumor, virus, fungus.In recent years experimentation shows, antibiotic Toplink promotes wound healing.Antibiotic Toplink stimulates the propagation of fibroblast, lymphocyte and vascular endothelial cell, promote granulation tissue hyperplasia, accelerate wound healing, burn with the Ointment in Treatment white mice that antibacterial peptide Cytoporin and silver sulfadiazine are made, faster with the silver sulfadiazine wound healing than simple, cicatrix is little.Shahabuddin etc. (1998) find that the different times that insect antimicrobial peptide is grown the plasmodium that infects mosquito has different effects, mainly causes obvious damage to plasmodial egg capsule phase and zygoblast phase.Efron etc. (2002) report, the plasmodium of antibacterial polypeptide demasepin that obtains from South America Ye Pao frog skin shows inhibitory action.
Because the antibacterial mechanisms of antibacterial peptide uniqueness, become the antibiotic succedaneum of tool DEVELOPMENT PROSPECT.Study the antibacterial peptide of comparative heat now both at home and abroad, include cecropin (cecropin), mammal and people's alexin, people's BPI (albumen sterilizes/infiltration-strengthen), the magainins of Amphibian etc., melittin that extracts in the Venenum apis of Apis etc.And obtain genetic engineering antibiotic peptides by the DNA recombinant technique, then become the focus of antibacterial peptide research.In recent years, the drug residue owing to a large amount of uses of feeding antibiotic cause descends the quality of animal meat, eggs and milk and aquatic products day by day, and the occurring in a large number of Drug resistance pathogenic bacterium makes disease resistance of animals such as poultry also in continuous decline.Along with the antibiotic medicine development is rapid, and be widely used in veterinary clinic, the dosage of use is also increasing, and Resistant strain also increases gradually, causes undesirable element to clinical treating disease, causes food safety, environmental pollution and drug resistance problem also to receive much concern.At present various countries just actively encourage and the development of advocating the green safety feed additive with apply.
(antibacterial peptides is a kind of little peptide of cation with strong antibacterial action that organism produces ABP) to antibacterial peptide, is the important composition composition of biological innate immunity.Up to now, comprised more than 2000 kind of antibacterial active peptide of discovery in insecticide, birds, animal, plant and the prokaryote at many biologies.Effect studies show that antibacterial peptide is broad-spectrum antiseptic not only, can press down kill endurance strain, and its bactericidal mechanism makes pathogen be difficult for producing the drug resistance sudden change, thereby becomes one of antibiotic succedaneum of tool DEVELOPMENT PROSPECT.
Because polypeptide is degraded and inactivation in digestive tract by orally using easily, so the use of polypeptide generally is based on injection system at present.Injection is extremely inconvenient when reality is used, and especially is applied to the aspect that prevents and treats of Animal diseases, has increased the burden of user simultaneously.
Summary of the invention
Primary and foremost purpose of the present invention is to overcome the shortcoming of prior art with not enough, Perorally administrable antimicrobial peptide formulations of provide a kind of and prevent from degrading, drug effect is fast, bioavailability is high and preparation method thereof.
The present invention relates to a kind of antibacterial peptide stabilization formulations, be a kind of oral solid formulation, it is main component with the antibacterial peptide, be that component is formulated with beta-schardinger dextrin-, Polyethylene Glycol, the weight proportion of each component is: antibacterial peptide tunning 1000g(wet thallus), beta-schardinger dextrin-50-200g, Polyethylene Glycol 2-4g.
The preparation method of antimicrobial peptide preparation provided by the invention is:
(1) antibacterial peptide liquid fermentation production, 8000rpm is centrifugal, gets thalline.(2) beta-schardinger dextrin-dissolves 55 ℃ of water-baths, adds the centrifugal thalline that step (1) obtains, fully
Stir hydrotropy, until dissolving fully.
(3) with ℃ lyophilization of step (2) product-70.
(4) with Polyethylene Glycol dissolving, the ratio of itself and water is 1:1.5, and polyglycol solution is sprayed to step
(3) on the product, stir while spraying.
(5) with step (4) product dry in the sun, cross 80 mesh sieves, get product.
System of the present invention antimicrobial peptide preparation, have the polypeptide of preventing hydrolysis, rapid-action, bioavailability advantages of higher, and a technology simple possible, be fit to very much suitability for industrialized production.
The specific embodiment
The present invention is described in further detail below in conjunction with embodiment, but embodiments of the present invention are not limited thereto.
Embodiment 1
Unless otherwise indicated, described each set of dispense ratio of sample is
The compound method of antimicrobial peptide preparation is:
(1) antibacterial peptide liquid fermentation production, 8000rpm is centrifugal, gets the 1000g thalline.
(2) get the 50g beta-schardinger dextrin-and dissolve 55 ℃ of water-baths, add the centrifugal thalline that step (1) obtains, fully stir hydrotropy, until dissolving fully.
With ℃ lyophilization of step (2) product-70.
(3) get 2g Polyethylene Glycol dissolving, the ratio of itself and water is 1:1.5, and polyglycol solution is sprayed to
On step (3) product, stir while spraying.
(5) with step (4) product dry in the sun, cross 80 mesh sieves, get product.
Embodiment 2
Unless otherwise indicated, described each set of dispense ratio of sample is
The compound method of antimicrobial peptide preparation is:
(1) antibacterial peptide liquid fermentation production, 8000rpm is centrifugal, gets the 1000g thalline.
(2) get the 200g beta-schardinger dextrin-and dissolve 55 ℃ of water-baths, add the centrifugal thalline that step (1) obtains, fully stir hydrotropy, until dissolving fully.
(4) with ℃ lyophilization of step (2) product-70.
(5) get 4g Polyethylene Glycol dissolving, the ratio of itself and water is 1:1.5, and polyglycol solution is sprayed to
On step (3) product, stir while spraying.
(5) with step (4) product dry in the sun, cross 80 mesh sieves, get product.
Embodiment 3
The antimicrobial peptide preparation through the bag quilt with embodiment 1 and embodiment 2 gained is dissolved by preceding antibacterial peptide product with bag, detects its water solublity and to the bacteriostatic test of staphylococcus aureus, concrete steps are as follows:
To wait to try bacterium staphylococcus aureus (Staphylococcus aureus) cultivation and be diluted to 1 * 10
6CFU/ml adds the 2g liquid fermentation production, adds the 6ml deionized water, fully dissolving.8000rpm is centrifugal, gets honest and upright and thrifty 5ml, with 0.25 μ m membrane filtration.Add the LB culture medium of 2 times of concentration of equal-volume in supernatant, and inoculate escherichia coli that 50 μ l shake in each bottle, overnight incubation.12 as a child got respectively and shake in the bottle bacterium liquid and measure the OD value.
Sample number into spectrum | Embodiment 1A | Embodiment 1B | Embodiment 2A | Embodiment 2B |
Before the bag quilt | 0.231 | 0.219 | 0.205 | 0.238 |
Behind the bag quilt | 1.361 | 1.297 | 1.151 | 1.072 |
Experimental result shows that the antimicrobial peptide preparation through the bag quilt can reduce the burst size in aqueous solution, and this just helps the stability of antimicrobial peptide preparation in digestive tract, thereby brings into play its physiological function to greatest extent.
Claims (3)
1. antimicrobial peptide preparation, it is characterized by: being main component with the antibacterial peptide, is that component is formulated with beta-schardinger dextrin-, Polyethylene Glycol.
2. according to the described a kind of antimicrobial peptide preparation of claim 1, the weight proportion of each component is: antibacterial peptide tunning 1000g(wet thallus), and beta-schardinger dextrin-50-200g, Polyethylene Glycol 2-4g.
3. the described antimicrobial peptide preparation of claim 1 and claim 2, its preparation method is:
(1) antibacterial peptide liquid fermentation production, 8000rpm is centrifugal, gets thalline;
(2) beta-schardinger dextrin-dissolves 55 ℃ of water-baths, adds the centrifugal thalline that step (1) obtains, and fully stirs hydrotropy, until dissolving fully;
(3) with ℃ lyophilization of step (2) product-70; (4) with Polyethylene Glycol dissolving, its ratio with water is 1:1.5, polyglycol solution is sprayed on step (3) product stirring while spraying;
(5) with step (4) product dry in the sun, cross 80 mesh sieves, get product.
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN104491837A (en) * | 2014-10-30 | 2015-04-08 | 广东海纳川药业股份有限公司 | Antibacterial peptide preparation, and preparation method and application thereof |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
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CN1154970A (en) * | 1996-01-16 | 1997-07-23 | 中国农业科学院生物技术研究中心 | Antibiotic peptide and production method and application thereof |
CN101766805A (en) * | 2009-12-24 | 2010-07-07 | 深圳市圣西马生物技术有限公司 | Stabilized antibacterial peptide preparation and preparation method thereof |
CN102824332A (en) * | 2012-09-14 | 2012-12-19 | 东北农业大学 | Preparation method of antimicrobial peptide slow-release microcapsules |
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2013
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Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1154970A (en) * | 1996-01-16 | 1997-07-23 | 中国农业科学院生物技术研究中心 | Antibiotic peptide and production method and application thereof |
CN101766805A (en) * | 2009-12-24 | 2010-07-07 | 深圳市圣西马生物技术有限公司 | Stabilized antibacterial peptide preparation and preparation method thereof |
CN102824332A (en) * | 2012-09-14 | 2012-12-19 | 东北农业大学 | Preparation method of antimicrobial peptide slow-release microcapsules |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104491837A (en) * | 2014-10-30 | 2015-04-08 | 广东海纳川药业股份有限公司 | Antibacterial peptide preparation, and preparation method and application thereof |
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Application publication date: 20130911 |