CN104983670A - Preparation method of curcumin-polyvinylpyrrolidone composite nanofiber solid dispersion - Google Patents
Preparation method of curcumin-polyvinylpyrrolidone composite nanofiber solid dispersion Download PDFInfo
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- CN104983670A CN104983670A CN201510414227.5A CN201510414227A CN104983670A CN 104983670 A CN104983670 A CN 104983670A CN 201510414227 A CN201510414227 A CN 201510414227A CN 104983670 A CN104983670 A CN 104983670A
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Abstract
The invention discloses a preparation method of a curcumin-polyvinylpyrrolidone composite nanofiber solid dispersion, which comprises the steps of step 1, respectively weighing polyvinylpyrrolidone and an organic solvent and uniformly stirring, wherein the mass ratio of the polyvinylpyrrolidone to the organic solvent is (0.5-1.5g):10ml, and the organic solvent is dimethylformamide or ethyl acetate; step 2, weighing curcumin, adding into the obtained mixed solution, uniformly mixing through an ultrasound or stirring manner and preparing a spinning solution, wherein the mass ratio of the polyvinylpyrrolidone to the curcumin is (10-15):4; step 3, electro-spinning the spinning solution by adopting an electrostatic spinning process, and collecting a product. The preparation method of the curcumin-polyvinylpyrrolidone composite nanofiber solid dispersion is simple in process, low in device requirements, easy to operate, low in cost and capable of being widely applied in fast dissolving and release of the curcumin.
Description
Technical field
The present invention relates to a kind of method preparing medicine solid dispersion, particularly, relate to the preparation method of a kind of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion.
Background technology
Curcumin is as a kind of effective ingredient extracted Rhizoma Curcumae Longae from Chinese medicine zingiberaceous plant.The multiple pharmacological effect such as modern study finds that curcumin has antitumor, inflammation-inhibiting, antioxidation, antibacterial, blood fat reducing, protects the liver, function of gallbladder promoting and resisting rheumatoid disease.In recent years, about curcumin pharmacological action report more, but about the report of curcumin preparation relatively less.Its main cause is that curcumin dissolubility in water is little, and water-soluble hardly, body absorption is poor, the unstable easily degraded of curcumin, responsive to factors such as light, heat and iron ions.Above factor limits curcumin to a great extent in clinical application.Wherein, dissolubility is the intrinsic physics and chemistry attribute of curcumin, and it is to the availability important of biology.Reason is, the dissolving of curcumin and dissolution rate directly affect the absorption of body to curcumin, thus bioavailability is poor.Therefore, in order to promote curcumin absorption in vivo, improving curative effect of medication, having become one of the emphasis and focus of contemporary pharmaceutical preparation exploitation.
Along with the development of pharmaceutics, utilize solid dispersion to be by insoluble drug, by selecting certain method, by drug target with states such as colloid, molecule or ultrafine particles, dispersion load are at some physiology inert in carrier soluble in water.After medicine carrying solid dispersion enters gastrointestinal tract, water miscible carrier dissolves rapidly, and agent structure is disintegrated, and makes medicine rapidly and fully discharges with more small-particle state from carrier, thus produces and act on fast and effectively.Meanwhile, solid dispersion also has increases drug substance stable, hide the advantages such as medicine self bad smell, unlikely stomach obstacle, significant in raising bioavailability.
At present, the common carrier preparing solid dispersion mainly contains Polyethylene Glycol, carbamide, polyvinylpyrrolidone, poloxamer, succinic acid and galactose etc.The preparation method that solid dispersion is conventional comprises fusion method, solvent method, polishing, spray drying method, freeze-drying etc.In recent years, along with the fast development of science and technology, some new technology such as torching mark, supercritical fluid technology and electrostatic rotating platen press are also applied to the preparation of solid dispersion.
Summary of the invention
The object of this invention is to provide a kind of method of solid dispersion preparation of the curcumin for indissoluble, technique is simple, apparatus requires low, easy to operate, with low cost, contribute to suitability for industrialized production, the solid dispersion of preparation has good biocompatibility, the problem such as simultaneously also solve that curcumin aqueous is poor, rate of release is slow and absorbance is low, can be widely used in rapid solution and the release of curcumin, improve the bioavailability of curcumin, have a good application prospect.
In order to achieve the above object, the invention provides the preparation method of a kind of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, wherein, the method comprises: step 1, takes polyvinylpyrrolidone and organic solvent respectively, is fully stirred to evenly; Step 2, takes curcumin, joins in the mixed solution of step 1 gained, mix homogeneously, obtained spinning liquid; Step 3, adopts the technique of electrostatic spinning to carry out electrospinning to the spinning liquid of step 2 gained, collects product, namely obtain curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion.
The preparation method of above-mentioned curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, wherein, the mass volume ratio of described polyvinylpyrrolidone and described organic solvent is that (0.5 ~ 1.5 g): 10 ml.
The preparation method of above-mentioned curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, wherein, described organic solvent is dimethyl formamide or ethyl acetate.
The preparation method of above-mentioned curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, wherein, the mass ratio of described polyvinylpyrrolidone and described curcumin is (10 ~ 15): 1.
The preparation method of above-mentioned curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, wherein, the electrostatic spinning described in step 3, its technological parameter is: voltage is 13 ~ 18 kV, the propelling speed of boost pump is 1 ~ 2 ml/h, and the distance between needle point and receiving device is 10 ~ 20 cm.
The preparation method of above-mentioned curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, wherein, the mix homogeneously described in step 2 is by ultrasonic or alr mode mix homogeneously.
The preparation method of curcumin provided by the invention-polyvinylpyrrolidone composite nano fiber solid dispersion has the following advantages:
(1) present invention process is simple, and manufacturing cycle is fast, easy to operate, with low cost, contributes to the production in enormous quantities of curcumin composite nano fiber solid dispersion.
(2) the curcumin composite nano fiber solid dispersion prepared of the present invention, can significantly improve water solublity and the bioavailability of curcumin to a certain extent.
(3) the curcumin composite nano fiber solid dispersion that prepared by the present invention has good biocompatibility, stability high.
Accompanying drawing explanation
Fig. 1 is the electrostatic spinning apparatus schematic diagram adopted in the preparation method of curcumin of the present invention-polyvinylpyrrolidone composite nano fiber solid dispersion.
Fig. 2 is the scanning electron microscope (SEM) photograph of the embodiment of the preparation method of curcumin of the present invention-polyvinylpyrrolidone composite nano fiber solid dispersion.
Fig. 3 is the release in vitro figure of the preparation method of curcumin of the present invention-polyvinylpyrrolidone composite nano fiber solid dispersion.
Detailed description of the invention
Below in conjunction with accompanying drawing, the specific embodiment of the present invention is further described.
The preparation method of curcumin provided by the invention-polyvinylpyrrolidone composite nano fiber solid dispersion, it comprises:
Step 1, takes polyvinylpyrrolidone and organic solvent respectively, is fully stirred to evenly.Wherein the mass volume ratio of polyvinylpyrrolidone and organic solvent is that (0.5 ~ 1.5 g): 10 ml; Organic solvent is dimethyl formamide or ethyl acetate.
Step 2, takes curcumin, joins in the mixed solution of step 1 gained, by ultrasonic or alr mode mix homogeneously, and obtained spinning liquid.Wherein the mass ratio of polyvinylpyrrolidone and curcumin is (10 ~ 15): 1.
Step 3, adopts the technique of electrostatic spinning to carry out electrospinning to the spinning liquid of step 2 gained, collects product, namely obtain curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion.
The technological parameter of electrostatic spinning is: voltage is 13 ~ 18 kV, and the propelling speed of boost pump is 1 ~ 2 ml/h, and the distance between needle point and receiving device is 10 ~ 20 cm.The device of electrostatic spinning is shown in Figure 1.
Below in conjunction with embodiment the present invention done and further describe.
Embodiment 1
Take the polyvinylpyrrolidone of 1g, be dissolved in the ethyl acetate solution of 10ml, under 40 DEG C of conditions, at the uniform velocity stir 4 h with the rotating speed of 200 revs/min, until transparent; Add 0.1g curcumin again, stir 2 h at 37 DEG C with the rotating speed of 200 revs/min, obtained mixed liquor.
Be drawn into by the spinning liquid prepared in 5 ml syringes, select 20 G injection needles, connect the negative pole of high voltage power supply, aluminium foil connects positive pole as acceptance is dull and stereotyped, controls the flow velocity of solution with boost pump.Opening power, is adjusted to 2 ml/h by the speed of syringe pump, and receiving range is adjusted to 15 cm, then starts high voltage power supply, voltage is set to 15 kV, i.e. obtained curcumin composite nano fiber solid dispersion.
Embodiment 2
Take the polyvinylpyrrolidone of 1g, be dissolved in the dimethyl formamide solution of 10 ml, the shaking table of 39 DEG C rotates with the speed of 200 revs/min and shakes up 4 h, until transparent; Add the curcumin of 0.08g again, on shaking table, 37 DEG C shake up 2 h with the speed of 100 revs/min rotation, obtain mixed liquor.
Be drawn into by the spinning liquid prepared in 2.5 ml syringes, select 20 G injection needles, connect the negative pole of high voltage power supply, aluminium foil fiber accepts dull and stereotyped connection positive pole, controls the flow velocity of solution with boost pump.Opening power, is adjusted to 1.5 ml/h by the speed of syringe pump, and receiving range is adjusted to 20 cm, then starts high voltage power supply, voltage is set to 13 kV, i.e. obtained curcumin composite nano fiber solid dispersion.
Embodiment 3
Take the polyvinylpyrrolidone of 0.8g, be dissolved in the dimethyl formamide solution of 10 ml, the shaking table of 30 DEG C rotates with the speed of 250 revs/min and shakes up 4 h, take out, obtain clear solution; Add the curcumin of 0.225g again, on shaking table, 37 DEG C shake up 2 h with the rotation of the speed of 100rpm, obtain mixed liquor.
Be drawn into by the spinning liquid prepared in 10 ml syringes, select 20 G injection needles, connect the negative pole of high voltage power supply, aluminium foil fiber accepts dull and stereotyped connection positive pole, controls the flow velocity of solution with boost pump.Opening power, is adjusted to 2 ml/h by the speed of syringe pump, and receiving range is adjusted to 20 cm, then starts high voltage power supply, voltage is set to 18 kV, i.e. obtained curcumin composite nano fiber solid dispersion.
As shown in Figure 2, In-vitro release curves as shown in Figure 3 for the scanning electron microscope (SEM) photograph of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion that embodiment 1 ~ 3 is obtained.
The preparation method of curcumin provided by the invention-polyvinylpyrrolidone composite nano fiber solid dispersion, content comprises the electrostatic spinning preparation of curcumin composite nano fiber solid dispersion, the proportioning of solid dispersion material, the selection of electrostatic spinning solvent, the selection etc. of electrostatic spinning process design parameter.Utilize method of electrostatic spinning to prepare curcumin composite nano fiber solid dispersion, Static Spinning is carried out by the polyvinylpyrrolidone and curcumin of selecting different quality ratio, obtain the curcumin of different drug loading, obtain ideal solute effect, water solublity and the bioavailability of curcumin can be significantly improved.
Generally speaking, the preparation method of curcumin provided by the invention-polyvinylpyrrolidone composite nano fiber solid dispersion, for curcumin slightly solubility, select polyvinylpyrrolidone as solid dispersion substrate, utilize the method for electrostatic spinning, prepare a kind of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion.This curcumin composite nano fiber solid dispersion is remarkable to the dissolubility effect improving curcumin, accelerates the dissolution rate of medicine, thus improves the bioavailability of curcumin, the release of controlled pharmacy.This carrier is improving the bioavailability of curcumin, ensures safe, the effective and reliable important role of clinical application.
Although content of the present invention has done detailed introduction by above preferred embodiment, will be appreciated that above-mentioned description should not be considered to limitation of the present invention.After those skilled in the art have read foregoing, for multiple amendment of the present invention and substitute will be all apparent.Therefore, protection scope of the present invention should be limited to the appended claims.
Claims (6)
1. a preparation method for curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion, it is characterized in that, the method comprises:
Step 1, takes polyvinylpyrrolidone and organic solvent respectively, stirs;
Step 2, takes curcumin, joins in the mixed solution of step 1 gained, mix homogeneously, obtained spinning liquid;
Step 3, adopts the technique of electrostatic spinning to carry out electrospinning to the spinning liquid of step 2 gained, collects product, namely obtain curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion.
2. the preparation method of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion as claimed in claim 1, it is characterized in that, the mass volume ratio of described polyvinylpyrrolidone and described organic solvent is that (0.5 ~ 1.5 g): 10 ml.
3. the preparation method of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion as claimed in claim 2, it is characterized in that, described organic solvent is dimethyl formamide or ethyl acetate.
4. the preparation method of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion as claimed in claim 1, it is characterized in that, the mass ratio of described polyvinylpyrrolidone and described curcumin is (10 ~ 15): 1.
5. the preparation method of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion as claimed in claim 1, it is characterized in that, electrostatic spinning described in step 3, its technological parameter is: voltage is 13 ~ 18 kV, the propelling speed of boost pump is 1 ~ 2 ml/h, and the distance between needle point and receiving device is 10 ~ 20 cm.
6. the preparation method of curcumin-polyvinylpyrrolidone composite nano fiber solid dispersion as claimed in claim 1, it is characterized in that, the mix homogeneously described in step 2, is by ultrasonic or alr mode mix homogeneously.
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| CN113122960A (en) * | 2021-04-29 | 2021-07-16 | 大连工业大学 | Fucoxanthin composite nanofiber and preparation method thereof |
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| CN101638830A (en) * | 2009-08-25 | 2010-02-03 | 江南大学 | Method for preparing nanofibre membrane |
| CN101664380A (en) * | 2009-09-11 | 2010-03-10 | 东华大学 | Method for preparing hydrophobic drug nanofibre felty solid dispersion by high-voltage electrostatic spinning |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101638830A (en) * | 2009-08-25 | 2010-02-03 | 江南大学 | Method for preparing nanofibre membrane |
| CN101664380A (en) * | 2009-09-11 | 2010-03-10 | 东华大学 | Method for preparing hydrophobic drug nanofibre felty solid dispersion by high-voltage electrostatic spinning |
Non-Patent Citations (1)
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| 关辉等: ""姜黄素固体分散体的制备和溶出度考察"", 《沈阳药科大学学报》 * |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN113122960A (en) * | 2021-04-29 | 2021-07-16 | 大连工业大学 | Fucoxanthin composite nanofiber and preparation method thereof |
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