CN104188985A - Method for preparing targeted controlled release aspirin powder - Google Patents
Method for preparing targeted controlled release aspirin powder Download PDFInfo
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- CN104188985A CN104188985A CN201410460471.0A CN201410460471A CN104188985A CN 104188985 A CN104188985 A CN 104188985A CN 201410460471 A CN201410460471 A CN 201410460471A CN 104188985 A CN104188985 A CN 104188985A
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- aspirin
- magnetic
- magnetic core
- pharmaceutical carrier
- nano silicon
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Abstract
The invention discloses a method for preparing targeted controlled release aspirin powder. The preparation process comprises the following four steps: preparing a magnetic core-shell nano-silica drug carrier, partially dissolving a magnetic core, loading aspirin on the magnetic drug carrier and performing secondary coating of the aspirin. According to the invention, the magnetic core is partially dissolved by adopting an acid-soluble mode, the cavity diameter of the magnetic core-shell nano-silica is enlarged, and the drug loading capacity is improved. The aspirin-loaded drug is subjected to secondary coating by using polyvinylpyrrolidone polymer sol, and the pore density on the silica shell is reduced. The problem that the conventional slow release aspirin drug is extremely high in release speed is solved, and long-lasting release and controlled release can be realized. The drug carrier has magnetic property, the drug can reach the target tissues under guide of a magnetic field, targeted drug delivery is realized, and the treatment efficiency is improved.
Description
Technical field
The present invention relates to a kind of preparation method of controllable release aspirin powder, particularly a kind of magnetic Nano silicon dioxide with cavity is as pharmaceutical carrier, the aspirin powder preparation method that realizes targeting long-acting slow-release, belongs to fine chemistry industry and field of nanometer technology.
Background technology
Aspirin is used for curing cold, generates heat, headache, toothache, arthralgia, rheumatism, can also anticoagulant, for preventing and treat ischemic heart desease, angina pectoris, cardiopulmonary infraction, cerebral thrombosis, it recommends usage and dosage is to take 3-4 time for 1st.For adapting to modern fast pace life style, market demand targeting controllable release Genprin, to facilitate medication, reduce drug side effect and to improve therapeutic effect.Adopting the coated aspirin of magnetic Nano silica supports is a kind of simple and easy to do targeting controllable release mode.
< < Chemical Engineer > > magazine 2013, the 12nd phase, 54-56 page, research one literary composition at silicon-based nano material for aspirin long-acting slow-release, report adopts silester hydrolysis preparation hollow silica pharmaceutical carrier under cetyl trimethyl ammonium bromide exists, maximum medicine carrying concentration is 45mg/g, the rate of release of aspirin is very fast, during sample 4h, release rate reaches 72%, because rate of release is too fast, do not reach long-acting slow-release object, there is no targeting release function.< < material Leader > > magazine 2014, the 5th phase, 12-15 page, in the preparation and drug release behavioral study one literary composition of magnetic mesoporous nano-silicon microsphere, report be take octadecyl trimethoxy silane and has at room temperature been prepared nucleocapsid structure Fe as template
3o
4meso-porous nano silicon ball, granule has good homogeneity, and particle diameter is about 100nm, in each Nano microsphere, only has a diameter to be about the Fe of 20nm
3o
4ferromagnetic core, but the drug loading of aspirin can only reach 34%, has the too low problem of pharmaceutical carrier drug loading.
Summary of the invention
The drug loading of targeting controllable release aspirin powder and rate of release are mainly by pharmaceutical carrier magnetic Nano SiO
2performance determines.Prepare at present magnetic Nano SiO
2method comprise: (1) adds surfactant and Fe in aqueous solution
3o
4magnetic powder is done masterplate agent, thereon clad nano SiO
2presoma silester, silicate hydrolyzate forms nuclear shell structure nano silicon dioxide; (2) coated magnetic Fe on porous nano silica
3o
4colloidal sol, forms magnetic Nano SiO
2pharmaceutical carrier; (3) prepare nanometer SiO
2and nanometer Fe
3o
4mixed sols, obtains magnetic Nano SiO after gel
2pharmaceutical carrier.Pharmaceutical carrier has magnetic, and medicine just can arrive destination organization under the guiding in magnetic field, realizes target administration, avoids other organs of drug damages and improves therapeutic efficiency.
The too fast problem of the too low rate of release of drug loading while the present invention is directed to existing magnetic Nano silicon dioxide as aspirin pharmaceutical carrier, adopt sour molten mode that the part magnetic core of magnetic core-shell nano silicon is dissolved, expand the cavity diameter of core-shell nano silicon dioxide, to improve drug loading; With polymeric sol, load aspirin medicine is carried out to secondary and be coated, to reduce hole density on silica shell, thereby realize aspirin long-acting slow-release and controllable release.The secondary of the loading of being partly dissolved of preparation, magnetic core, aspirin that the technical scheme of taking comprises magnetic core-shell nano silicon pharmaceutical carrier on magnetic medicine carrier and aspirin is coated, and concrete implementation step is.
(1) in deionized water, add surfactant, Fe
3o
4magnetic core colloidal sol, add again the strong aqua ammonia regulator solution pH of mass percentage concentration 25% to be greater than 11, be heated to 60-80 ℃, under strong agitation, add silester, isothermal reaction 0.5-2h, to silester complete hydrolysis, cooling, to filter formation black precipitate, with deionized water wash 2-3 time, obtains magnetic core-shell nano silicon pharmaceutical carrier, described surfactant is Shuangzi quaternary ammonium salts surfactant, mass percentage concentration 0.1%-1.0% in solution; Described silester is mass percentage concentration 0.5%-5.0% in solution.
(2) magnetic core-shell nano silicon pharmaceutical carrier is immersed in the dilute hydrochloric acid of 1mol/L, strong agitation 1-2h, part magnetic core is dissolved, by the insoluble precipitation of attraction, with the weak ammonia of 1mol/L, flood and washing precipitation again, use attraction precipitation separation, 105 ℃ drying precipitated, put into Muffle furnace and at 550 ℃, calcine the magnetic Nano silicon dioxide pharmaceutical carrier that 1-5h obtains having cavity.
(3) aspirin is dissolved in to dehydrated alcohol, the alcoholic solution of preparing aspirin mass percentage concentration 0.5%-3.0%, the magnetic Nano silicon dioxide pharmaceutical carrier with cavity is immersed in wherein, stir or supersound process 1-5h, the aspirin being dissolved in alcohol solvent enters the cavity of silicon dioxide granule through the micropore on silica shell, also can be loaded in the hole between silicon dioxide granule by adsorption, reach the pharmaceutical carrier of isolated by filtration load aspirin after load balance, described magnetic Nano silicon dioxide pharmaceutical carrier mass percentage concentration 0.5%-3.0% in solution with cavity, aspirin and carrier loading mass ratio reach 40%-70%.
(4) polyvinylpyrrolidone is dissolved in to the clear solution that dehydrated alcohol forms mass percentage concentration 1.0%-5.0%, by the magnetic medicine carrier dipping of the load aspirin of preparing above wherein, stir or supersound process 0.5-1h, the aspirin that makes load is that polyvinylpyrrolidone secondary is coated, macromolecule layer thickness 5-20nm, the aspirin medicine that isolated by filtration macromolecule layer secondary is coated, natural drying, the magnetic medicine carrier of described load aspirin is mass percentage concentration 0.5%-5.0% in solution.In simulated body fluid, aspirin is at 24h release rate 60%-75%, at the release rate 80%-95% of 48h.
The diameter of magnetic core-shell nano silicon is preferably 100-300nm, magnetic core diameter 20-100nm, if magnetic core diameter is less than 20nm, and can be too little too little with aspirin useful load for the cavity expanding; If the diameter of magnetic core is greater than 100nm, can be difficult to control with the behavior of aspirin drug release for the cavity expanding is too little.On silica shell, aperture is preferably 5-20nm, when the aperture on silica shell is less than 5nm, exists aspirin medicine loading and rate of release too slow; When the pore size of silica shell is greater than 20nm, exist aspirin drug release efficiency to be difficult to control.The thickness of magnetic core-shell nano silicon shell is preferably 10-50 nm, if the thickness of silica shell is less than 10nm, aspirin drug loading stability reduces; If the thickness of silica shell is greater than 50 nm, aspirin drug releasing rate is very slow, and the thickness of silica shell and aperture can be controlled by reaction density, time and surfactant concentration.
The concentration of medicine aspirin in solution can adopt UV-VIS spectrophotometry to measure, and aspirin has absorption maximum at 273nm place, according to medicine initial concentration and the residual concentration in solution, can calculate the useful load of aspirin in carrier.By water bath with thermostatic control temperature control at 37 ℃, a certain amount of controllable release aspirin sustained release body is added in the beaker of simulated gastric fluid, high-speed stirred, the sustained-release liquid of certain volume is drawn in timing, utilize aspirin content in ultraviolet-visible light splitting photometry test solution, can calculate the rate of release of aspirin.
The beneficial effect that the present invention obtains is:
(1) the invention solves the too fast problem of existing slow release aspirin drug releasing rate, realize long-acting slow-release and controllable release;
(2) pharmaceutical carrier of the present invention has magnetic, can under the guiding in magnetic field, arrive destination organization, realizes target administration and improves therapeutic efficiency;
(3) controllable release aspirin of the present invention adapts to modern fast pace life style, can facilitate medication and reduce drug side effect.
The specific embodiment
Embodiment 1
Take 0.54 gram of ferric chloride (FeC1
36H
2o) and 0.78 gram of Ferrous ammonium sulfate (NH
4)
2fe (SO
4)
2.6H
2o), be dissolved in 50 ml deionized waters, under strong agitation, join in the ammonia that 50 ml concentration are 10%, in 50 ℃ of water-baths, react 15 minutes, by attraction, isolate the Fe of black
3o
4solid, obtains by washed with de-ionized water the Fe that particle diameter is 20-100 nm for 3-5 time
3o
4nanocrystalline.
Measure 120mL deionized water and be heated to 80 ℃, under strong agitation, add the Fe of above preparation
3o
4nanocrystalline and 0.6g Shuangzi quaternary ammonium salts surfactant, obtains Fe for ultrasonic 10 minutes
3o
4nanocrystalline colloidal sol, adds strong aqua ammonia 3ml regulator solution pH to be greater than 11, adds 10mL silester, isothermal reaction 2h at 80 ℃, and to complete hydrolysis, cold filtration precipitation then, and with deionized water wash, obtain magnetic core-shell nano silicon pharmaceutical carrier.
Magnetic core-shell nano silicon pharmaceutical carrier is immersed in the dilute hydrochloric acid of 200mL 1mol/L, strong agitation 2h, by the insoluble precipitation of attraction, with the weak ammonia of 200mL 1mol/L, flood and washing again, separated by attraction, at 105 ℃, be dried, put into Muffle furnace and at 550 ℃, calcine the magnetic Nano silicon dioxide pharmaceutical carrier that 1h obtains having cavity.
Take 3.3g aspirin crude drug, be dissolved in 150ml dehydrated alcohol, obtain aspirin alcoholic solution.Above magnetic silica pharmaceutical carrier is immersed in wherein, adopts the form of dynamic adsorption, supersound process 20 minutes is filtered after adsorption equilibrium, and the loading mass ratio of pharmaceutical carrier reaches 70%.
1.0g polyvinylpyrrolidone is dissolved in to 100ml dehydrated alcohol and forms clear solution, by the magnetic medicine carrier dipping of the load aspirin of preparing above wherein, supersound process 0.5h, the aspirin that makes load is that polyvinylpyrrolidone secondary is coated, macromolecule layer thickness 10nm, the aspirin medicine that isolated by filtration macromolecule layer secondary is coated, natural drying, obtains targeting controllable release aspirin powder.In simulated body fluid, aspirin is at 24h release rate 75%, at the release rate 95% of 48h.
Embodiment 2
Take 0.54 gram of ferric chloride (FeC1
36H
2o) and 0.78 gram of Ferrous ammonium sulfate (NH
4)
2fe (SO
4)
2.6H
2o), be dissolved in 50 ml deionized waters, under strong agitation, join in the ammonia that 50 ml concentration are 10%, in 50 ℃ of water-baths, react 15 minutes, by attraction, isolate the Fe of black
3o
4solid, obtains by washed with de-ionized water the Fe that particle diameter is 20-100 nm for 3-5 time
3o
4nanocrystalline.
Measure 120mL deionized water and be heated to 60 ℃, under strong agitation, add the Fe of above preparation
3o
4nanocrystalline and 0.6g Shuangzi quaternary ammonium salts surfactant, obtains Fe for ultrasonic 10 minutes
3o
4nanocrystalline colloidal sol, adds strong aqua ammonia 3ml regulator solution pH to be greater than 11, adds 10mL silester, isothermal reaction 2h at 60 ℃, and to complete hydrolysis, cold filtration precipitation then, and with deionized water wash, obtain magnetic core-shell nano silicon pharmaceutical carrier.
Magnetic core-shell nano silicon pharmaceutical carrier is immersed in the dilute hydrochloric acid of 200mL 1mol/L, strong agitation 1-2h, by the insoluble precipitation of attraction, with the weak ammonia of 200mL 1mol/L, flood and washing again, separated by attraction, at 105 ℃, be dried, put into Muffle furnace and at 550 ℃, calcine the magnetic Nano silicon dioxide pharmaceutical carrier that 1-5h obtains having cavity.
Take 3.3g aspirin crude drug, be dissolved in 150ml dehydrated alcohol, obtain aspirin alcoholic solution.Above magnetic silica pharmaceutical carrier is immersed in wherein, adopts the form of dynamic adsorption, stir process 20 minutes is filtered after adsorption equilibrium, and the loading mass ratio of pharmaceutical carrier reaches 40%.
1.0g polyvinylpyrrolidone is dissolved in to 100ml dehydrated alcohol and forms clear solution, by the magnetic medicine carrier dipping of the load aspirin of preparing above wherein, supersound process 0.5h, the aspirin that makes load is that polyvinylpyrrolidone secondary is coated, macromolecule layer thickness 10nm, the aspirin medicine that isolated by filtration macromolecule layer secondary is coated, natural drying, obtains targeting controllable release aspirin powder.In simulated body fluid, aspirin is at 24h release rate 60%, at the release rate 80% of 48h.
Claims (3)
1. a preparation method for targeting controllable release aspirin powder, is characterized in that the secondary of loading on magnetic medicine carrier of being partly dissolved of preparation, magnetic core, aspirin that preparation process comprises magnetic core-shell nano silicon pharmaceutical carrier and aspirin is coated.
2. the preparation method of targeting controllable release aspirin powder according to claim 1, the preparation method that it is characterized in that having the magnetic core-shell nano silicon pharmaceutical carrier of cavity is:
(1) in deionized water, add surfactant, Fe
3o
4magnetic core colloidal sol, add again the strong aqua ammonia regulator solution pH of mass percentage concentration 25% to be greater than 11, be heated to 60-80 ℃, under strong agitation, add silester, isothermal reaction 0.5-2h, to silester complete hydrolysis, cooling, to filter formation black precipitate, with deionized water wash 2-3 time, obtains magnetic core-shell nano silicon pharmaceutical carrier, described surfactant is Shuangzi quaternary ammonium salts surfactant, mass percentage concentration 0.1%-1.0% in solution; Described silester is mass percentage concentration 0.5%-5.0% in solution;
(2) magnetic core-shell nano silicon pharmaceutical carrier is immersed in the dilute hydrochloric acid of 1mol/L, strong agitation 1-2h, by the insoluble precipitation of attraction, with the weak ammonia of 1mol/L, flood and washing precipitation again, use attraction precipitation separation, 105 ℃ drying precipitated, put into Muffle furnace and at 550 ℃, calcine the magnetic Nano silicon dioxide pharmaceutical carrier that 1-5h obtains having cavity.
3. the preparation method of targeting controllable release aspirin powder according to claim 1, is characterized in that the secondary coating method of aspirin is:
(1) the magnetic Nano silicon dioxide pharmaceutical carrier with cavity is immersed in the alcoholic solution of aspirin mass percentage concentration 0.5%-3.0%, stir or supersound process 1-5h, medicine reaches the pharmaceutical carrier of isolated by filtration load aspirin after load balance, described magnetic Nano silicon dioxide pharmaceutical carrier mass percentage concentration 0.5%-3.0% in solution with cavity, the loading mass ratio of aspirin reaches 40%-70%;
(2) magnetic medicine carrier of the load aspirin of preparation is immersed in the polyvinylpyrrolidone alcoholic solution of mass percentage concentration 1.0%-5.0%, stir or supersound process 0.5-1h, the aspirin that makes load is that polyvinylpyrrolidone secondary is coated, polyvinylpyrrolidonemacromolecule macromolecule layer thickness 5-20nm, the aspirin medicine that isolated by filtration macromolecule layer secondary is coated, natural drying, the magnetic medicine carrier of described load aspirin is mass percentage concentration 0.5%-5.0% in solution.
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|---|---|---|---|
| CN201410460471.0A CN104188985A (en) | 2014-09-11 | 2014-09-11 | Method for preparing targeted controlled release aspirin powder |
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|---|---|---|---|
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105836750A (en) * | 2016-04-21 | 2016-08-10 | 南京理工大学 | Preparation method of magnetic nano-silica hollow spheres |
| CN109628547A (en) * | 2018-12-14 | 2019-04-16 | 陕西师范大学 | A kind of modified magnetic bead, preparation method and applications |
-
2014
- 2014-09-11 CN CN201410460471.0A patent/CN104188985A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105836750A (en) * | 2016-04-21 | 2016-08-10 | 南京理工大学 | Preparation method of magnetic nano-silica hollow spheres |
| CN109628547A (en) * | 2018-12-14 | 2019-04-16 | 陕西师范大学 | A kind of modified magnetic bead, preparation method and applications |
| CN109628547B (en) * | 2018-12-14 | 2022-02-25 | 陕西师范大学 | Modified magnetic bead, preparation method and application thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20141210 |
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| WD01 | Invention patent application deemed withdrawn after publication |