CN105018376B - A kind of micro-capsule for recovering drug-fast bacteria sensitiveness and preparation method thereof - Google Patents
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness and preparation method thereof Download PDFInfo
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Abstract
The invention belongs to field of medicine preparing technology, it particularly relates to a kind of micro-capsule and preparation method thereof for recovering drug-fast bacteria sensitiveness.The micro-capsule is formed by the emulsification of β galactosylation azo alkene father-in-law glycol, ampicillin, the reaction product of lysine and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant and additive preparing；β galactosylation azo alkene father-in-law glycol, ampicillin, the mass ratio of isopropylthiogalactoside and lysine are 12:1‑6:1‑4:1‑8；Based on micro-capsule gross mass percentage, capsule material is 1.5% 3.5%, emulsifying agent is 0.1% 0.5%, sweetener 0.03%, preservative are 0.01% 0.05%, antioxidant is 0.1% 0.2%, additives 0.25%.Compared with prior art, β galactosylations azo alkene father-in-law glycol and ampicillin synergy are stronger in micro-capsule of the present invention, and can anti-decomposition, accomplish steady quality, controllable.
Description
Technical field
The invention belongs to field of medicine preparing technology, it particularly relates to it is a kind of recover drug-fast bacteria sensitiveness micro-capsule
And preparation method thereof.
Background technology
Nitric oxide (nitric oxide, NO) is a kind of gas molecules material with multiple biological activities.In body
Interior acted on by NO precursor substances L-arginine under nitricoxide synthase (NOS) catalysis with oxygen molecule produces NO and L- guanidine ammonia
Acid.NO is prevalent in the various cells of vertebrate, is iuntercellular and thin in endothelial cell, macrophage, nerve cell
The important regulatory factor of intracellular information transmission, while a kind of still CF in host immune response.It is proved have
There is various biological active, this includes regulation blood vessel dilatation and blood flow, nerve signal transmission, signal transduction, immunomodulation, cell
Redox state, liver cell apoptosis and defence microorganism etc..Nitric oxide donors (NO donor) refer to that one kind can be
Enzymatically reaction or non-enzymatic reaction introduce and discharge exogenous NO a kind of pro-drug in vivo.NO is in pathophysiological process
Have the function that extensive and important, as what NO was recognized deepens continuously, people are to the research interest of NO donors also more and more higher.
In the nearly more than ten years, the NO donors that many has different biological characteristic and treatment potentiality have all been synthesized, by its knot
Structure type, conventional generally comprises organic nitrates esters such as nitroglycerin (NG), sydnone imines such as molsidomine, nitroso sulphur
Alcohols such as S-nitrosoglutathione captopril, NO- donors complex class such as NO- aspirin (NCX-4061) and metal-NO complexs
Class such as sodium nitroprussiate etc..But traditional NO donors are when in use, on the one hand, it only discharges NO in the solution, because NO biology partly declines
Phase is extremely short, only 10s or so, once generation will cause intracellular NO to be extremely difficult to valid density by rapid oxidation；It is another
Aspect, NO releases, which lack specificity, makes it also to kill normal cell while aim cell is attacked, and such as promotes liver cell fine
Dimensionization etc..Therefore, the tissue specificity of NO donors is increasingly taken seriously in NO controlled releases.
There is document report, designed and synthesized a new glycosylation NO compound donator beta galactose base azo alkene
Father-in-law's glycol (β-Gal-NONOate), it connects azo alkene father-in-law's glycol end oxygen to protect in aqueous easily certainly using galactolipin
Hair decomposes the azo alkene father-in-law's glycol for producing NO, in addition, more important is due to introducing galactolipin in molecule, make it to high table
Specificity is provided with up to the germ of beta galactosidase and tumour cell.Experiment shows：In isopropylthiogalactoside
(IPTG) under induction, beta galactose base azo alkene father-in-law's glycol has the function that to recover drug-fast bacteria sensitiveness, and blue or green with ammonia benzyl
There is synergy after mycin (Amp) use in conjunction.However, beta galactose base azo alkene father-in-law glycol and ampicillin are being located
When managing drug-fast bacteria, reaching maximum to the cooperative effect for making recovery sensitiveness, how NO donors are connected with ampicillin, so as to
Realize targetingDissolving NO donor medicines and ampicillin optimum solvent this how to selectHow much is ratioUsing which kind of system
Agent technology, can just enable that composition of medicine is more stable, action time is more longlasting, action effect is more preferableThese problems all do not solve also
Certainly.
The content of the invention
In order to solve the above technical problems, the invention provides the recovery drug-fast bacteria that a kind of stability is good, synergy is strong is quick
Micro-capsule of perception and preparation method thereof.
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness of the present invention is by beta galactose base azo alkene father-in-law glycol, ammonia benzyl
Penicillin, the reaction product of lysine and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant
Formed with additive preparing emulsification；Beta galactose base azo alkene father-in-law glycol, ampicillin, isopropylthiogalactoside with
The mass ratio of lysine is 1-2:1-6:1-4:1-8；Based on micro-capsule gross mass percentage, capsule material 1.5%-3.5%, emulsifying agent
For 0.1%-0.5%, sweetener 0.03%, preservative 0.01%-0.05%, antioxidant 0.1%-0.2%, additives
For 0.25%.
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness of the present invention, the capsule material is sodium alginate；The sweetener
For saccharin sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is sodium pyrosulfite or little Hua
Gold is picked one's ears plain；The additives are local analgesia agent lidocaine.
The preparation method of the micro-capsule of the present invention for recovering drug-fast bacteria sensitiveness, the preparation method are specially：1) exist
Under room temperature environment, beta galactose base azo alkene father-in-law's glycol is configured to the phosphate buffer solution for the 10mM that pH is 7；2) then
Ampicillin is added, the lower sodium hydroxide solution maintenance system pH with 2wt% of stirring is 7, is heated to seething with excitement, distillation reaction is complete
Bi Hou, volatile ingredient is taken, filter off insoluble matter, the concentrated silicagel column of filtrate is eluted with alcohol solution, collect what is flowed out at first
Colour band, obtain ampicillin-beta galactose base azo alkene father-in-law's diester；3) by ampicillin-beta galactose base azo alkene
Father-in-law's diester is formulated in alcohol solution with bad ammonia, and wherein ampicillin-ester concentration of beta galactose base azo alkene father-in-law two is 2-
5mg/ml, it is 70-105 DEG C, reaction time 1-1.5h to control temperature, filters out reaction solution, produces ampicillin-beta galactose base
Change azo alkene father-in-law diester and lysine compound；4) by sodium alginate water wiring solution-forming, then with ampicillin-beta galactose
Base azo alkene father-in-law diester and lysine compound, isopropylthiogalactoside, sweetener, preservative, antioxidant, additives
And Tween 80 is emulsified, emulsion is added into CaCl2In solution, cohesion, solidification, spontaneously dry and produce micro-capsule.
The preparation method of the micro-capsule of the present invention for recovering drug-fast bacteria sensitiveness, the alcohol solution are 1 by mol ratio:
1 polyethylene glycol is formulated with pure water.
The CaCl2Concentration of polymer solution is 2%.
Compared with prior art, the micro-capsule of the composition of medicine of the present invention for recovering drug-fast bacteria sensitiveness is with beta galactose base
It is leading medicine to change azo alkene father-in-law glycol and ampicillin, lysine binding, effectively improves the suction of insoluble drug in vivo
Receive, improve its bioavilability, it has preferable tissue specificity, targeting；Polyethylene glycol 400 is added, except taking it
It is preferable to the solute effect of beta galactose base azo alkene father-in-law glycol and ampicillin, beta galactose baseization can also be promoted even
The synergy of nitrence father-in-law glycol and ampicillin；It is even to solve ampicillin-beta galactose baseization using microcapsule technology
Nitrence father-in-law's diester half-life period is shorter, less stable, and makes composition of medicine action effect stronger.Experiment shows：Ampicillin-
The synergy of the ester micro capsule composition of medicine of beta galactose base azo alkene father-in-law two is most strong, anti-decomposition, has accomplished stable, controllable.
Embodiment
With reference to specific embodiment to micro-capsule of recovery drug-fast bacteria sensitiveness of the present invention and preparation method thereof
It is described further, but protection scope of the present invention is not limited to this.
Embodiment 1
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness is by beta galactose base azo alkene father-in-law glycol, ampicillin, bad ammonia
The reaction product of acid and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant and additive preparing
Emulsification forms；Beta galactose base azo alkene father-in-law glycol, ampicillin, the quality of isopropylthiogalactoside and lysine
Than for 1:6:4:8；It is capsule material 1.5%, emulsifying agent 0.1%, sweetener 0.03%, anti-based on micro-capsule gross mass percentage
Rotten agent is 0.01%, antioxidant 0.1%, additives 0.25%.The capsule material is sodium alginate；The sweetener is saccharin
Sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is sodium pyrosulfite；The additives
For local analgesia agent lidocaine.The preparation method of the micro-capsule of described recovery drug-fast bacteria sensitiveness, the preparation method are specific
For：1) under room temperature environment, the phosphate-buffered for beta galactose base azo alkene father-in-law's glycol being configured to the 10mM that pH is 7 is molten
Liquid；2) and then ampicillin being added, the lower sodium hydroxide solution maintenance system pH with 2wt% of stirring is 7, is heated to seething with excitement,
After distillation reaction, volatile ingredient is taken, insoluble matter is filtered off, the concentrated silicagel column of filtrate is eluted with alcohol solution, is collected
The colour band flowed out at first, obtain ampicillin-beta galactose base azo alkene father-in-law's diester；3) by ampicillin-beta galactose
Base azo alkene father-in-law diester is formulated in alcohol solution with bad ammonia, wherein ampicillin-beta galactose base azo alkene father-in-law two
Ester concentration is 2mg/ml, and it is 70 DEG C, reaction time 1h to control temperature, filters out reaction solution, produces ampicillin-beta galactose base
Change azo alkene father-in-law diester and lysine compound；4) by sodium alginate water prepare mass concentration be 2% solution, then with ammonia benzyl
Penicillin-beta galactose base azo alkene father-in-law diester and lysine compound, isopropylthiogalactoside, sweetener, anti-corrosion
Agent, antioxidant, additives and Tween 80 are emulsified, and emulsion is added to 2wt% CaCl2In solution, stir, stir
Time 10min is mixed, is quickly cooled to less than 0 DEG C, continues to stir 30min, is solidified, obtain solidfied material solution；By solidfied material
Solution is placed in aqueous isopropanol after dehydration 20min, cools down 24h；Then first washed with aqueous isopropanol, washed again with n-hexane
Wash, remove solvent, drying, that is, obtain milky ampicillin-beta galactose base azo alkene father-in-law diester and answered with lysine
Compound micro-capsule.The alcohol solution is 1 by mol ratio:1 polyethylene glycol is formulated with pure water.
Embodiment 2
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness is by beta galactose base azo alkene father-in-law glycol, ampicillin, bad ammonia
The reaction product of acid and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant and additive preparing
Emulsification forms；Beta galactose base azo alkene father-in-law glycol, ampicillin, the quality of isopropylthiogalactoside and lysine
Than for 2:1:4:2；It is capsule material 2.0%, emulsifying agent 0.3%, sweetener 0.03%, anti-based on micro-capsule gross mass percentage
Rotten agent is 0.05%, antioxidant 0.2%, additives 0.25%.The capsule material is sodium alginate；The sweetener is saccharin
Sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is sodium pyrosulfite；The additives
For local analgesia agent lidocaine.The preparation method of the micro-capsule of described recovery drug-fast bacteria sensitiveness, the preparation method are specific
For：1) under room temperature environment, the phosphate-buffered for beta galactose base azo alkene father-in-law's glycol being configured to the 10mM that pH is 7 is molten
Liquid；2) and then ampicillin being added, the lower sodium hydroxide solution maintenance system pH with 2wt% of stirring is 7, is heated to seething with excitement,
After distillation reaction, volatile ingredient is taken, insoluble matter is filtered off, the concentrated silicagel column of filtrate is eluted with alcohol solution, is collected
The colour band flowed out at first, obtain ampicillin-beta galactose base azo alkene father-in-law's diester；3) by ampicillin-beta galactose
Base azo alkene father-in-law diester is formulated in alcohol solution with bad ammonia, wherein ampicillin-beta galactose base azo alkene father-in-law two
Ester concentration is 2.6mg/ml, and it is 80 DEG C, reaction time 1.25h to control temperature, filters out reaction solution, produces ampicillin-β-half
Breast glycosylation azo alkene father-in-law diester and lysine compound；4) sodium alginate water is prepared into the solution that mass concentration is 5%, then
With ampicillin-beta galactose base azo alkene father-in-law diester and lysine compound, isopropylthiogalactoside, sweet taste
Agent, preservative, antioxidant, additives and Tween 80 are emulsified, and emulsion is added to 2wt% CaCl2In solution, stirring
Uniformly, mixing time 15min, less than 5 DEG C are quickly cooled to, continue to stir 30min, solidified, obtain solidfied material solution；Will
Solidfied material solution is placed in 40 parts of aqueous isopropanols after dehydration 20min, cools down 24h；Then first washed with 85 parts of aqueous isopropanol
Wash, washed again with 85 parts of n-hexanes, remove solvent, drying, that is, obtain milky ampicillin-beta galactose base azo
Alkene father-in-law diester and lysine compound micro-capsule.The alcohol solution is 1 by mol ratio:1 polyethylene glycol is formulated with pure water.
Embodiment 3
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness is by beta galactose base azo alkene father-in-law glycol, ampicillin, bad ammonia
The reaction product of acid and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant and additive preparing
Emulsification forms；Beta galactose base azo alkene father-in-law glycol, ampicillin, the quality of isopropylthiogalactoside and lysine
Than for 2:3:2:1；It is capsule material 2.5%, emulsifying agent 0.5%, sweetener 0.03%, anti-based on micro-capsule gross mass percentage
Rotten agent is 0.03%, antioxidant 0.1%, additives 0.25%.The capsule material is sodium alginate；The sweetener is saccharin
Sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is sodium pyrosulfite；The additives
For local analgesia agent lidocaine.The preparation method of the micro-capsule of described recovery drug-fast bacteria sensitiveness, the preparation method are specific
For：1) under room temperature environment, the phosphate-buffered for beta galactose base azo alkene father-in-law's glycol being configured to the 10mM that pH is 7 is molten
Liquid；2) and then ampicillin being added, the lower sodium hydroxide solution maintenance system pH with 2wt% of stirring is 7, is heated to seething with excitement,
After distillation reaction, volatile ingredient is taken, insoluble matter is filtered off, the concentrated silicagel column of filtrate is eluted with alcohol solution, is collected
The colour band flowed out at first, obtain ampicillin-beta galactose base azo alkene father-in-law's diester；3) by ampicillin-beta galactose
Base azo alkene father-in-law diester is formulated in alcohol solution with bad ammonia, wherein ampicillin-beta galactose base azo alkene father-in-law two
Ester concentration is 5mg/ml, and it is 90 DEG C, reaction time 1.5h to control temperature, filters out reaction solution, produces ampicillin-beta galactose
Base azo alkene father-in-law diester and lysine compound；4) sodium alginate water is prepared into mass concentration as 10% solution, then and
Ampicillin-beta galactose base azo alkene father-in-law diester and lysine compound, isopropylthiogalactoside, sweetener,
Preservative, antioxidant, additives and Tween 80 are emulsified, and emulsion is added to 2% CaCl2In solution, stir,
Mixing time 20min, less than 10 DEG C are quickly cooled to, continue to stir 30min, solidified, obtain solidfied material solution；Will solidification
Thing solution is placed in 50 parts of aqueous isopropanols after dehydration 20min, cools down 24h；Then first washed with 100 parts of aqueous isopropanol,
Washed again with 100 parts of n-hexanes, remove solvent, drying, that is, obtain milky ampicillin-beta galactose base azo alkene
Father-in-law's diester and lysine compound micro-capsule.The alcohol solution is 1 by mol ratio:1 polyethylene glycol is formulated with pure water.
Embodiment 4
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness is by beta galactose base azo alkene father-in-law glycol, ampicillin, bad ammonia
The reaction product of acid and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant and additive preparing
Emulsification forms；Beta galactose base azo alkene father-in-law glycol, ampicillin, the quality of isopropylthiogalactoside and lysine
Than for 1:3:2:4；It is capsule material 2.5%, emulsifying agent 0.5%, sweetener 0.03%, anti-based on micro-capsule gross mass percentage
Rotten agent is 0.03%, antioxidant 0.15%, additives 0.25%.The capsule material is sodium alginate；The sweetener is sugar
Smart sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is sodium pyrosulfite；It is described additional
Agent is local analgesia agent lidocaine.The preparation method of the micro-capsule of described recovery drug-fast bacteria sensitiveness, the preparation method tool
Body is：1) under room temperature environment, the phosphate-buffered for beta galactose base azo alkene father-in-law's glycol being configured to the 10mM that pH is 7 is molten
Liquid；2) and then ampicillin being added, the lower sodium hydroxide solution maintenance system pH with 2wt% of stirring is 7, is heated to seething with excitement,
After distillation reaction, volatile ingredient is taken, insoluble matter is filtered off, the concentrated silicagel column of filtrate is eluted with alcohol solution, is collected
The colour band flowed out at first, obtain ampicillin-beta galactose base azo alkene father-in-law's diester；3) by ampicillin-beta galactose
Base azo alkene father-in-law diester is formulated in alcohol solution with bad ammonia, wherein ampicillin-beta galactose base azo alkene father-in-law two
Ester concentration is 2mg/ml, and it is 90 DEG C, reaction time 1h to control temperature, filters out reaction solution, produces ampicillin-beta galactose base
Change azo alkene father-in-law diester and lysine compound；4) by sodium alginate water prepare mass concentration be 5% solution, then with ammonia benzyl
Penicillin-beta galactose base azo alkene father-in-law diester and lysine compound, isopropylthiogalactoside, sweetener, anti-corrosion
Agent, antioxidant, additives and Tween 80 are emulsified, and emulsion is added to 2% CaCl2In solution, stir, stir
Time 20min, less than 10 DEG C are quickly cooled to, continue to stir 30min, solidified, obtain solidfied material solution；Solidfied material is molten
Liquid is placed in 50 parts of aqueous isopropanols after dehydration 20min, cools down 24h；Then first washed with 100 parts of aqueous isopropanol, used again
100 parts of n-hexane washings, remove solvent, drying, that is, obtain milky ampicillin-beta galactose base azo alkene father-in-law two
Ester and lysine compound micro-capsule.The alcohol solution is 1 by mol ratio:1 polyethylene glycol is formulated with pure water.
Embodiment 5
A kind of micro-capsule for recovering drug-fast bacteria sensitiveness is by beta galactose base azo alkene father-in-law glycol, ampicillin, bad ammonia
The reaction product of acid and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative, antioxidant and additive preparing
Emulsification forms；Beta galactose base azo alkene father-in-law glycol, ampicillin, the quality of isopropylthiogalactoside and lysine
Than for 1:3:2:4；It is capsule material 2.5%, emulsifying agent 0.5%, sweetener 0.03%, anti-based on micro-capsule gross mass percentage
Rotten agent is 0.03%, antioxidant 0.15%, additives 0.25%.The capsule material is sodium alginate；The sweetener is sugar
Smart sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is little Hua gold earpick elements (4 β-acetyl
Epoxide-pseudo- guainane-11 (the 13)-α of alkene-12,8-lactone)；The additives are local analgesia agent lidocaine.Described is extensive
The preparation method of the micro-capsule of multiple drug-fast bacteria sensitiveness, the preparation method are specially：1) under room temperature environment, beta galactose base
Change the phosphate buffer solution that azo alkene father-in-law's glycol is configured to the 10mM that pH is 7；2) and then ampicillin is added, stirs lower use
2wt% sodium hydroxide solution maintenance system pH is 7, is heated to seething with excitement, after distillation reaction, takes volatile ingredient, is filtered off
Insoluble matter, the concentrated silicagel column of filtrate is eluted with alcohol solution, collect the colour band flowed out at first, obtain ampicillin-β-half
Breast glycosylation azo alkene father-in-law's diester；3) ampicillin-beta galactose base azo alkene father-in-law diester and bad ammonia are formulated in alcohol water
In solution, wherein ampicillin-ester concentration of beta galactose base azo alkene father-in-law two is 2mg/ml, control temperature for 90 DEG C, it is anti-
1h between seasonable, filters out reaction solution, produces ampicillin-beta galactose base azo alkene father-in-law diester and lysine compound；4)
By sodium alginate water prepare mass concentration be 5% solution, then with ampicillin-beta galactose base azo alkene father-in-law's diester
Breast is carried out with lysine compound, isopropylthiogalactoside, sweetener, preservative, antioxidant, additives and Tween 80
Change, emulsion is added to 2% CaCl2In solution, stir, mixing time 20min, be quickly cooled to less than 10 DEG C,
Continue to stir 30min, solidified, obtain solidfied material solution；Solidfied material solution is placed in 50 parts of aqueous isopropanols and is dehydrated
After 20min, 24h is cooled down；Then first washed with 100 parts of aqueous isopropanol, washed again with 100 parts of n-hexanes, removed solvent, do
It is dry, that is, obtain milky ampicillin-beta galactose base azo alkene father-in-law diester and lysine compound micro-capsule.The alcohol
The aqueous solution is 1 by mol ratio:1 polyethylene glycol is formulated with pure water.
Quality testing and compliance test result
Ampicillin-beta galactose base azo alkene father-in-law diester and lysine compound obtained by Example 1-5 is micro-
Capsule, ampicillin therein-beta galactose base azo alkene father-in-law diester and Lysine binding percentage are measured.Take reality
Ampicillin-beta galactose base azo alkene father-in-law the diester and lysine compound micro-capsule obtained by a 1-5 are applied, with independent β-half
The resistance for the micro-capsule not obtained when only being reacted under breast glycosylation azo alkene father-in-law glycol and identical preparation method using distillation dehydration
Bacterium recovery rate is compared, and wherein drug-fast bacteria is to be handled 30 days with ampicillin-resistant, and MIC value is 2mg e. coli k12
Drug-fast bacteria, three kinds of medicines recover processing 15 days.1 is shown in Table with reference to percentage and antibody-resistant bacterium sensitivity recovery rate.
Table 1 combines percentage and antibody-resistant bacterium sensitivity recovery rate
Claims (4)
1. a kind of micro-capsule for recovering drug-fast bacteria sensitiveness, it is characterised in that the micro-capsule is by beta galactose base azo alkene father-in-law two
Alcohol, ampicillin, the reaction product of lysine and isopropylthiogalactoside, capsule material, emulsifying agent, sweetener, preservative,
Antioxidant and additive preparing emulsification form；Beta galactose base azo alkene father-in-law glycol, ampicillin, isopropylthio gala
The mass ratio of glucosides and lysine is 1-2: 1-6 : 1-4 : 1-8；Based on micro-capsule gross mass percentage, capsule material 1.5%-
3.5%th, emulsifying agent be 0.1%- 0.5%, sweetener 0.03%, preservative 0.01%-0.05%, antioxidant 0.1%-0.2%,
Additives are 0.25%；
It is described recover drug-fast bacteria sensitiveness the preparation method of micro-capsule be specially：1）Under room temperature environment, beta galactose base
Azo alkene father-in-law's glycol is configured to the phosphate buffer solution for the 10mM that pH is 7；2）Then ampicillin is added, stirs lower use
2wt% sodium hydroxide solution maintenance system pH is 7, is heated to seething with excitement, and after distillation reaction, takes volatile ingredient, filters off not
Molten thing, the concentrated silicagel column of filtrate is eluted with alcohol solution, collect the colour band flowed out at first, obtain ampicillin-β-gala
Glycosylate azo alkene father-in-law's diester；3）Ampicillin-beta galactose base azo alkene father-in-law diester and lysine are formulated in alcohol water
In solution, wherein ampicillin-ester concentration of beta galactose base azo alkene father-in-law two is 2-5mg/ml, and it is 70-105 to control temperature
DEG C, reaction time 1-1.5h, filter out reaction solution, produce ampicillin-beta galactose base azo alkene father-in-law diester and lysine
Compound；4）By sodium alginate water wiring solution-forming, then with ampicillin-beta galactose base azo alkene father-in-law diester and bad ammonia
Sour compound, isopropylthiogalactoside, sweetener, preservative, antioxidant, additives and Tween 80 are emulsified, by breast
Change liquid and add CaCl2In solution, cohesion, solidification, spontaneously dry and produce micro-capsule.
2. a kind of micro-capsule for recovering drug-fast bacteria sensitiveness according to claim 1, it is characterised in that the capsule material is marine alga
Sour sodium；The sweetener is saccharin sodium；The emulsifying agent is Tween 80；The preservative is eucalyptus oil 80；The antioxidant is
Sodium pyrosulfite or little Hua gold are picked one's ears plain；The additives are local analgesia agent lidocaine.
3. it is according to claim 1 recover drug-fast bacteria sensitiveness micro-capsule, it is characterised in that the alcohol solution by mole
Than for 1:1 polyethylene glycol is formulated with pure water.
4. the micro-capsule according to claim 1 for recovering drug-fast bacteria sensitiveness, it is characterised in that the CaCl2Solution quality is dense
Spend for 2%.
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| CN103007253A (en) * | 2012-12-12 | 2013-04-03 | 北京化工大学 | Pharmaceutical composition containing beta-galactosylation azo ene glycol and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103007253A (en) * | 2012-12-12 | 2013-04-03 | 北京化工大学 | Pharmaceutical composition containing beta-galactosylation azo ene glycol and preparation method thereof |
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| A Glycosylated Nitric Oxide Donor, β-Gal-NONOate, and its;Chang Chen等;《Arch. Pharm. Chem. Life Sci.》;20061231;第339卷;366-371 * |
| Delivery of Nitric Oxide Released from β-Gal-NONOate Activation by β-Galactosidase and Its Activity against Escherichia coli;Chang CHEN等;《Biol. Pharm. Bull.》;20060630;第29卷(第6期);1239-1241 * |
| 一氧化氮供体最新研究进展及应用前景;李松等;《中国生化药物杂志》;20061231;第27卷(第6期);374-378 * |
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| 新型一氧化氮供体-β半乳糖基化偶氮烯翁二醇的抗菌、抗肿瘤作用途径研究;陈畅;《中国博士学位论文全文数据库》;20070915(第03期);E079-17 * |
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