CN104188917A - Preparation method of controlled-release aspirin powder - Google Patents
Preparation method of controlled-release aspirin powder Download PDFInfo
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- CN104188917A CN104188917A CN201410460431.6A CN201410460431A CN104188917A CN 104188917 A CN104188917 A CN 104188917A CN 201410460431 A CN201410460431 A CN 201410460431A CN 104188917 A CN104188917 A CN 104188917A
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- aspirin
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Abstract
The invention discloses a preparation method of controlled-release aspirin powder. The preparation method of the controlled-release aspirin powder comprises the steps of preparing a hollow nanosilicon dioxide drug carrier, loading aspirin on the hollow nanosilicon dioxide drug carrier and carrying out secondary coating on the loaded aspirin. The prepared aspirin-loaded drug carrier is immersed in nanosilicon dioxide ethyl alcohol sol, and stirring or ultrasonic treatment is carried out for 0.5-1 hour, so that secondary coating is carried out on the loaded aspirin by virtue of nanosilicon dioxide particles, and the coating thickness is optimized to be 10-20nm; in simulated body fluid, the release rate of the loaded aspirin subjected to the secondary coating in 24 hours is 40-55%, and the release rate of the loaded aspirin subjected to the secondary coating in 48 hours is 70-90%. The preparation method of the controlled release aspirin powder has the advantages that the problem that the existing controlled release aspirin medicine is high in release rate is solved, long-acting controlled release and controlled release can be realized, medication is easy, and the drug side effect is reduced.
Description
Technical field
The present invention relates to a kind of preparation method of controllable release aspirin powder, particularly a kind of hollow nano silicon of using, as pharmaceutical carrier, is realized the aspirin powder preparation method of 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 controllable release Genprin, to facilitate medication and to reduce drug side effect.Adopting the coated aspirin of hollow nanometer silicon dioxide is a kind of simple and easy to do 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.< < 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, the drug loading of aspirin can reach 34%, and in simulated body fluid, aspirin is about 88% after front 20h discharges 80%, 48h, the same too fast problem of rate of release in early stage that exists.
Summary of the invention
The rate of release of controllable release aspirin powder is mainly by pharmaceutical carrier hollow nanometer SiO
2performance determines.Prepare at present hollow nanometer SiO
2the conventional method of method comprise: (1) adds surfactant, organic polymer or organic solvent to do masterplate agent in aqueous solution, thereon clad nano SiO
2, then high temperature sintering is removed organic masterplate agent, obtains hollow nano silicon shell; (2) in solution, add the molten inorganic nano-particle of theobromine, thereon clad nano SiO
2presoma, hydrolysis forms nano silicon shell, and then the sour molten inorganic nano core of removing, obtains hollow nano silicon shell; (3) silester is dispersed into the nano-liquid droplet of oil-in-water type in aqueous solution, and it starts hydrolysis from boundary, forms hollow nano silicon shell; (4) solid silicon ball is protected by water soluble polymer, then carry out corrosion with NaOH, retain the pattern of solid silicon ball, obtain the SiO of porous or hollow
2nano microsphere.
The present invention is directed to existing hollow nano silicon as the too fast problem of aspirin pharmaceutical carrier rate of release, adopting nano silicon dioxide sol to carry out secondary to load aspirin medicine is coated, to reduce on silica shell hole density or to dwindle the aperture on silica shell, thereby realize aspirin long-acting slow-release and controllable release, the secondary of the loading of the preparation, aspirin that the technical scheme of taking comprises hollow nano silicon pharmaceutical carrier on pharmaceutical carrier and load aspirin is coated, and concrete implementation step is.
(1) in deionized water, add surfactant, 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, filter the white precipitate forming, with deionized water wash 2-3 time, being deposited in 105 ℃ is dried, put into Muffle furnace calcines 1-5h and obtains hollow nano silicon pharmaceutical carrier at 550 ℃, 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) aspirin is dissolved in to dehydrated alcohol, obtain the alcoholic solution of aspirin mass percentage concentration 0.5%-3.0%, hollow nano silicon pharmaceutical carrier is immersed in wherein, stir or supersound process 1-5h, the aspirin being dissolved in alcohol solvent enters silicon dioxide granule cavity 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 hollow nano silicon pharmaceutical carrier mass percentage concentration 0.5%-3.0% in solution.
(3) silester is dissolved in to dehydrated alcohol, add deionized water and dilute hydrochloric acid, control material molar ratio: silester: ethanol: water: hydrochloric acid=1:30-50:3-5:0.05-0.1, stir at normal temperatures 2-4h, standing 12-20h makes silester complete hydrolysis, generate the nano silicon dioxide sol of mean diameter 10nm, then with weak ammonia, regulate alcosol pH6-8; By the pharmaceutical carrier dipping of the load aspirin of preparing above wherein, stir or supersound process 0.5-1h, the aspirin that makes load is that nano-silicon dioxide particle secondary is coated, optimize coated thickness 10-20nm, the aspirin medicine that isolated by filtration secondary is coated, natural drying, the pharmaceutical 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 40-55%, at the release rate 70-90% of 48h.
The cavity diameter of hollow nano silicon is preferably 20-100nm, if the diameter of cavity is less than 20nm, aspirin useful load is too little; If the diameter of cavity is greater than 100nm, the behavior of aspirin drug release may be difficult to control.On silica shell, aperture is preferably 2-10nm, when the aperture on silica shell is less than 2nm, exists aspirin drug releasing rate too slow; When the pore size of silica shell is greater than 10nm, exist aspirin drug release efficiency to be difficult to control.The thickness of hollow nano silicon shell is preferably 5-50 nm, if the thickness of silica shell is less than 5nm, aspirin drug loading stability reduces; If the thickness of silica shell is greater than 50nm, aspirin drug releasing rate is very slow, and hollow nanometer silicon dioxide particle diameter is preferably 30-250 nm.
The present invention is solid nano silicon for the coated nano silicon dioxide sol of secondary, mean diameter 10nm, and coated thickness can change by nano silicon dioxide sol concentration, viscosity, acidity and dip time, optimizes coated thickness 10-20nm.
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) 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
Measure 120mL deionized water and be heated to 80 ℃, under strong agitation, add 0.6g Shuangzi quaternary ammonium salts surfactant, add strong aqua ammonia 3ml regulator solution pH to be greater than 11, add 5mL silester, isothermal reaction 2h at 80 ℃, to complete hydrolysis, cold filtration precipitation then, and with deionized water wash, after drying at room temperature, sample is put into Muffle furnace, calcine 1h at 550 ℃ to obtain hollow nano silicon pharmaceutical carrier sample.
Take 0.20g aspirin crude drug, be dissolved in 50 ml dehydrated alcohol, obtain aspirin alcoholic solution.0.5g hollow silica pharmaceutical carrier is immersed in wherein, adopts the form of dynamic adsorption, stirring or supersound process 20 minutes are filtered after adsorption equilibrium, and the loading mass ratio of pharmaceutical carrier reaches 50%.
3.5mL silester is dissolved in to 50mL dehydrated alcohol, the dilute hydrochloric acid 0.85mL that adds deionized water 1.5mL and 1.0mol/L, stirs 4h at normal temperatures, and standing 20h makes silester complete hydrolysis, generate the nano silicon dioxide sol of mean diameter 10nm, then with weak ammonia, regulate alcoholic solution pH6-8; By the pharmaceutical carrier dipping of the load aspirin of preparing above wherein, supersound process 0.5h, the aspirin that makes load is that nano-silicon dioxide particle secondary is coated, the aspirin medicine that isolated by filtration secondary is coated, natural drying.In simulated body fluid, aspirin reaches 55% at front 24h release rate, and rate of release slows down, and at the release rate of 48h, is about 90%.
Embodiment 2
Measure 120mL deionized water and be heated to 60 ℃, under strong agitation, add 0.6g Shuangzi quaternary ammonium salts surfactant, add strong aqua ammonia 3ml regulator solution pH to be greater than 11, add 5mL silester, isothermal reaction 0.5-2h at 80 ℃, to complete hydrolysis, cold filtration precipitation then, and with deionized water wash, after drying at room temperature, sample is put into Muffle furnace, calcine 1-5h at 550 ℃ to obtain hollow nano silicon pharmaceutical carrier sample.
Take 0.20g aspirin crude drug, be dissolved in 50 ml dehydrated alcohol, obtain aspirin alcoholic solution.0.5g hollow 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 30%.
3.5mL silester is dissolved in to 50mL dehydrated alcohol, the dilute hydrochloric acid 0.85mL that adds deionized water 1.5mL and 1.0mol/L, stirs 4h at normal temperatures, and standing 20h makes silester complete hydrolysis, generate the nano silicon dioxide sol of mean diameter 10nm, then with weak ammonia, regulate alcoholic solution pH6-8; By the pharmaceutical carrier dipping of the load aspirin of preparing above wherein, stir process 0.5h, the aspirin that makes load is that nano-silicon dioxide particle secondary is coated, the aspirin medicine that isolated by filtration secondary is coated, natural drying.In simulated body fluid, aspirin reaches 45% at front 24h release rate, and rate of release slows down, and at the release rate of 48h, is about 80%.
Reference examples 1
According to embodiment 1 method, aspirin crude drug is loaded on hollow silica pharmaceutical carrier, the loading mass of pharmaceutical carrier ratio reaches 50%, does not carry out secondary and is coated.In simulated body fluid, aspirin reaches 65% at 4h release rate, at the release rate of 24h, is 86%.
Reference examples 2
According to embodiment 2 methods, aspirin crude drug is loaded on hollow silica pharmaceutical carrier, the loading mass of pharmaceutical carrier ratio reaches 30%, does not carry out secondary and is coated.In simulated body fluid, aspirin reaches 60% at 4h release rate, at the release rate of 24h, is 80%.
Claims (3)
1. a preparation method for controllable release aspirin powder, is characterized in that the secondary of loading on pharmaceutical carrier of preparation, aspirin that preparation process comprises hollow nano silicon pharmaceutical carrier and load aspirin is coated.
2. the preparation method of controllable release aspirin powder according to claim 1, is characterized in that the preparation method of hollow nano silicon pharmaceutical carrier is:
(1) in deionized water, add surfactant, 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, 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) white precipitate that cooling, filtration forms, with deionized water wash 2-3 time, precipitate is dry at 105 ℃;
(3) dry precipitate is put into Muffle furnace and calcine 1-5h at 550 ℃, obtains hollow nano silicon pharmaceutical carrier.
3. the preparation method of controllable release aspirin powder according to claim 1, is characterized in that the coated process of secondary of load aspirin is:
(1) silester is dissolved in to dehydrated alcohol, add deionized water and dilute hydrochloric acid, control material molar ratio: silester: ethanol: water: hydrochloric acid=1:30-50:3-5:0.05-0.1, stir at normal temperatures 2-4h, standing 12-20h makes silester complete hydrolysis, generate the nano silicon alcosol of mean diameter 10nm, then with weak ammonia, regulate alcosol pH6-8;
(2) by the pharmaceutical carrier dipping of the load aspirin of preparation wherein, stir or supersound process 0.5-1h, the aspirin that makes load is that nano-silicon dioxide particle secondary is coated, optimize coated thickness 10-20nm, the pharmaceutical carrier of described load aspirin is mass percentage concentration 0.5%-5.0% in solution;
(3) the coated aspirin medicine of isolated by filtration secondary, natural drying, obtains long-acting slow-release and controllable release aspirin.
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| CN201410460431.6A CN104188917A (en) | 2014-09-11 | 2014-09-11 | Preparation method of controlled-release aspirin powder |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109160519A (en) * | 2018-09-14 | 2019-01-08 | 广东工业大学 | A kind of hollow mesoporous silica microsphere, hollow mesoporous silica microsphere load sun-screening agent and its preparation method and application |
| CN109925512A (en) * | 2019-01-07 | 2019-06-25 | 安徽理工大学 | A kind of novel aspirin two-dimensional nano load medicine and slow-releasing system |
| CN113876963A (en) * | 2021-09-30 | 2022-01-04 | 广州凌玮科技股份有限公司 | Preparation method of aspirin-silicon dioxide sustained-release body |
-
2014
- 2014-09-11 CN CN201410460431.6A patent/CN104188917A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109160519A (en) * | 2018-09-14 | 2019-01-08 | 广东工业大学 | A kind of hollow mesoporous silica microsphere, hollow mesoporous silica microsphere load sun-screening agent and its preparation method and application |
| CN109160519B (en) * | 2018-09-14 | 2022-03-04 | 广东工业大学 | Hollow mesoporous silica microsphere, sun-screening agent loaded on hollow mesoporous silica microsphere, and preparation method and application of sun-screening agent |
| CN109925512A (en) * | 2019-01-07 | 2019-06-25 | 安徽理工大学 | A kind of novel aspirin two-dimensional nano load medicine and slow-releasing system |
| CN113876963A (en) * | 2021-09-30 | 2022-01-04 | 广州凌玮科技股份有限公司 | Preparation method of aspirin-silicon dioxide sustained-release body |
| CN113876963B (en) * | 2021-09-30 | 2023-07-25 | 广州凌玮科技股份有限公司 | Preparation method of aspirin-silicon dioxide slow-release body |
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Application publication date: 20141210 |