CN107648183A - A kind of icariin nanoparticle and preparation method thereof - Google Patents
A kind of icariin nanoparticle and preparation method thereof Download PDFInfo
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- CN107648183A CN107648183A CN201710957309.3A CN201710957309A CN107648183A CN 107648183 A CN107648183 A CN 107648183A CN 201710957309 A CN201710957309 A CN 201710957309A CN 107648183 A CN107648183 A CN 107648183A
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- icariin
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- pva
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/29—Berberidaceae (Barberry family), e.g. barberry, cohosh or mayapple
- A61K36/296—Epimedium
Abstract
The invention discloses a kind of icariin nanoparticle and preparation method thereof.Its preparation method：Icariin solution and PVA solution are configured, then icariin solution is added in PVA solution, after mixing, carries out emulsification treatment；After emulsification terminates, mixed solution is collected, evaporates organic solvent；Sample is centrifuged, purifying water washing precipitation, centrifuges, operates repeatedly again, nanoparticle is cleaned up, you can obtain icariin nanoparticle.Icariin nanoparticle average hydrodynamic diameter is between 100 ~ 400nm made from this method, compared with icariin bulk drug, its solubility property in water improves more than 100 times, and dispersive property is also significantly improved, so as to effectively improve its bioavilability and drug effect.The preparation method of the present invention need not be easy to operate, reproducible using carrier, the material simple cheap, the preparation process that use.
Description
Technical field
The invention belongs to technical field of traditional Chinese medicine pharmacy, and in particular to a kind of icariin nanoparticle and preparation method thereof.
Technical background
Icariin is the effective active composition extracted from Herba Epimedii, is a kind of flavonoid glycoside compound, has
It is antitumor, promote bone cell proliferation and differentiation, protect the pharmacological activity such as cerebral anoxia, regulation immunity of organism.But icariin
Water is insoluble in, oral absorptivity is poor, and bioavilability is low.Drug absorption needs suitably water-soluble and fat-soluble, so as to energy thoroughly
Cross biomembrane lipid bilayer.With modern nanometer technology, by insoluble drug nanosizing, can greatly improve dissolubility,
Dispersiveness, strengthen bioactivity and target utilization rate；Reduce the usage amount of organic solvent simultaneously, reduce toxic side effect with it is bad anti-
Should.Using modern nanometer technology, it is to improve icariin solubility property, raising medicine biology that icariin is prepared into nanoparticle
Utilization rate and drug effect, reduce the important channel of toxic side effect.
The content of the invention
The purpose of the present invention is overcome the deficiencies in the prior art, there is provided a kind of preparation technology is simple, utilization ratio of drug is high, grain
Footpath is evenly distributed, physical property is stablized and can significantly improve water miscible icariin nanoparticle and preparation method thereof.
A kind of preparation method of icariin nanoparticle, its preparation method are：
Step 1: configuration solution：Icariin is added in organic solvent, fully after dissolving, obtains icariin solution；Will
PVA is added in deionized water, and PVA solution is obtained after being completely dissolved；The organic solvent is methanol, ethyl acetate, dichloromethane
One or more in alkane and chloroform；
Step 2: emulsification：Icariin solution is added in PVA solution, mixed, carries out emulsification treatment；
Step 3: remove organic solvent：After emulsification terminates, mixed solution is collected, passes through removed by evaporation organic solvent；
Step 4: purifying：The sample for removing organic solvent is centrifuged, is precipitated with purifying water washing, is centrifuged, grasp repeatedly again
Make 3-5 times, nanoparticle is cleaned up, you can obtain icariin nanoparticle；
The PVA is the abbreviation of polyvinyl alcohol.
Further, the concentration of the PVA solution in the step 1 is between the mg/ml of 1 mg/ml ~ 100.
It is further preferred that the concentration of PVA solution is between the mg/ml of 10 mg/ml ~ 50 in the step 1.
Further, the volume ratio of the icariin solution in the step 2 and PVA solution is 1:1~1:Between 20.
It is further preferred that the volume ratio of icariin solution and PVA solution is 1 in the step 2:3~1:Between 9.
And the icariin nano-particle that the above method is produced.
Advantages of the present invention：Compared with icariin bulk drug, icariin nanoparticle prepared by the present invention is in water
Solubility property improves more than 100 times, while dispersive property is significantly improved, so as to effectively improve its biology profit
Expenditure and drug effect.The preparation method of the present invention need not use carrier, the material simple cheap used, preparation process operation letter
Just it is, reproducible.The nano particle diameter of preparation is evenly distributed, and average hydrodynamic diameter is between 100 ~ 300nm.
Brief description of the drawings
Fig. 1 is the grain size distribution of icariin nanoparticle prepared by embodiment 1；
Fig. 2 is the grain size distribution of icariin nanoparticle prepared by embodiment 4；
Fig. 3 is the grain size distribution of icariin nanoparticle prepared by embodiment 7.
Embodiment
Below by the drawings and specific embodiments, the present invention is further detailed explanation.
Following examples are intended to make the present invention embodiment explanation, but protection scope of the present invention, are not limited to
This.
Embodiment 1
10 mg icariin bulk drugs are dissolved in 10 ml methanol/ethyl acetate solution（Volume ratio is 1:1）, configure dense
Spend the icariin solution for 1.0 mg/ml；300 mgPVA are dissolved in 10 ml water, configuration concentration is 30 mg/ml's
PVA solution.Measure 0.75 ml icariin solution to be added in 2.25 mlPVA solution, mixed liquor is then subjected to ultrasound breast
Change；Supersonic frequency is 20-25 KHz, and power is 250 W, and ultrasonic time is 6 min, per 5 s of ultrasound, is spaced 10 s.Will emulsification
Solution is transferred in Rotary Evaporators afterwards, and the min of rotary evaporation 10 is by methanol, dichloromethane, chloroform evaporating completely under normal temperature
Fall, then by the min of sample high speed centrifugation 30（4 DEG C, 20,000 rpm）, precipitation is collected, deionized water is added and suspends again, then
Secondary centrifugation.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Average hydrodynamic diameter is
192.44 nm, polydispersity coefficient 0.338.
Such as the grain size distribution that Fig. 1 is icariin nanoparticle prepared by embodiment 1.
Embodiment 2
20 mg icariin bulk drugs are dissolved in 10 ml methanol/dichloromethane solution（Volume ratio is 5:1）, configure dense
Spend the icariin solution for 2.0 mg/ml；300 mgPVA are dissolved in 10 ml water, configuration concentration is 30 mg/ml's
PVA solution.Measure 0.75 ml icariin solution to be added in 2.25 mlPVA solution, mixed liquor is then subjected to ultrasound breast
Change；Supersonic frequency is 20-25 KHz, and power is 100 W, and ultrasonic time is 6 min, per 5 s of ultrasound, is spaced 10 s.Will emulsification
Solution is transferred in Rotary Evaporators afterwards, and the min of rotary evaporation 10 is by methanol, dichloromethane, chloroform evaporating completely under normal temperature
Fall, then by the min of sample high speed centrifugation 30（4 DEG C, 20,000 rpm）, precipitation is collected, deionized water is added and suspends again, then
Secondary centrifugation.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Average hydrodynamic diameter is
297.11nm polydispersity coefficient 0.356.
Embodiment 3
30 mg icariin bulk drugs are dissolved in 10 ml methanol/chloroform soln（Volume ratio is 9:1）, configure dense
Spend the icariin solution for 3.0 mg/ml；300 mgPVA are dissolved in 10 ml water, configuration concentration is 30 mg/ml's
PVA solution.Measure 0.75 ml icariin solution to be added in 2.25 mlPVA solution, mixed liquor is then subjected to ultrasound breast
Change；Supersonic frequency is 20-25 KHz, and power is 400 W, and ultrasonic time is 6 min, per 5 s of ultrasound, is spaced 10 s.Will emulsification
Solution is transferred in Rotary Evaporators afterwards, and the min of rotary evaporation 10 is by methanol, dichloromethane, chloroform evaporating completely under normal temperature
Fall, then by the min of sample high speed centrifugation 30（4 DEG C, 20,000rpm）, precipitation is collected, deionized water is added and suspends again, again
Centrifugation.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Average hydrodynamic diameter is
325.42nm polydispersity coefficient 0.341.
Embodiment 4
20 mg icariin bulk drugs are dissolved in 10 ml methanol/ethyl acetate/dichloromethane solution（Volume ratio is 2:
1:1）, configuration concentration is 2.0 mg/ml icariin solution；100 mgPVA are dissolved in 10 ml water, configuration concentration
For 10 mg/ml PVA solution.0.50 ml icariin solution is measured to be added in 2.50 mlPVA solution, then will mixing
Liquid carries out ultrasonic emulsification；Supersonic frequency is 20-25 KHz, and power is 500 W, and ultrasonic time is 3 min, per 5 s of ultrasound, interval
10 s.Solution after emulsification is transferred in Rotary Evaporators, the min of rotary evaporation 10 is by methanol, dichloromethane, trichlorine under normal temperature
Methane evaporating completely is fallen, then by the min of sample high speed centrifugation 30（4 DEG C, 20,000 rpm）, precipitation is collected, adds deionized water
Suspend, centrifuge again again.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Mean flow
Kinetic diameter is 238.91nm, polydispersity coefficient 0.292.
Such as the grain size distribution that Fig. 2 is icariin nanoparticle prepared by embodiment 4.
Embodiment 5
20 mg icariin bulk drugs are dissolved in 10 ml ethanol/methylene/chloroform soln（Volume ratio is 6:
1:1）, configuration concentration is 2.0 mg/ml icariin solution；500 mgPVA are dissolved in 10 ml water, configuration concentration
For 50 mg/ml PVA solution.0.30 ml icariin solution is measured to be added in 2.70 mlPVA solution, then will mixing
Liquid carries out ultrasonic emulsification；Supersonic frequency is 20-25 KHz, and power is 600 W, and ultrasonic time is 6 min, per 5 s of ultrasound, interval
10 s.Solution after emulsification is transferred in Rotary Evaporators, the min of rotary evaporation 10 is by methanol, dichloromethane, trichlorine under normal temperature
Methane evaporating completely is fallen, then by sample high speed centrifugation 30min（4 DEG C, 20,000 rpm）, precipitation is collected, adds deionized water
Suspend, centrifuge again again.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Mean flow
Kinetic diameter is 196.52nm, polydispersity coefficient 0.356.
Embodiment 6
30 mg icariin bulk drugs are dissolved in 10 ml ethanol/methylene/chloroform soln（Volume ratio is
10:1:1）, configuration concentration is 3.0 mg/ml icariin solution；100 mgPVA are dissolved in 10 ml water, configuration is dense
Spend for 10 mg/ml PVA solution.0.50 ml icariin solution is measured to be added in 2.50 mlPVA solution, then will be mixed
Close liquid and carry out ultrasonic emulsification；Supersonic frequency is 20-25 KHz, and power is 200 W, and ultrasonic time is 9 min, per 5 s of ultrasound,
Every 10 s.Solution after emulsification is transferred in Rotary Evaporators, the min of rotary evaporation 10 is by methanol, dichloromethane, three under normal temperature
Chloromethanes evaporating completely is fallen, then by the min of sample high speed centrifugation 30（4 DEG C, 20,000 rpm）, precipitation is collected, adds deionization
Water suspends again, centrifuges again.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Mean flow
The a diameter of 357.96nm of body dynamics, polydispersity coefficient 0.292.
Embodiment 7
30 mg icariin bulk drugs are dissolved in 10 ml ethanol/methylene/chloroform soln（Volume ratio is
18:1:1）, configuration concentration is 3.0 mg/ml icariin solution；500 mgPVA are dissolved in 10 ml water, configuration is dense
Spend for 50 mg/ml PVA solution.0.30 ml icariin solution is measured to be added in 2.70 mlPVA solution, then will be mixed
Close liquid and carry out ultrasonic emulsification；Supersonic frequency is 20-25 KHz, and power is 300 W, and ultrasonic time is 9 min, per 5 s of ultrasound,
Every 10 s.Solution after emulsification is transferred in Rotary Evaporators, the min of rotary evaporation 10 is by methanol, dichloromethane, three under normal temperature
Chloromethanes evaporating completely is fallen, then by the min of sample high speed centrifugation 30（4 DEG C, 20,000 rpm）, precipitation is collected, adds deionization
Water suspends again, centrifuges again.Operate 5 times repeatedly, nanoparticle is cleaned up, produces icariin nano-particle.Mean flow
The a diameter of 283.28nm of body dynamics, polydispersity coefficient 0.430.
Such as the grain size distribution that Fig. 3 is icariin nanoparticle prepared by embodiment 7.
Claims (6)
1. the preparation method of icariin nanoparticle, it is characterised in that its preparation method is：
Step 1: configuration solution：Icariin is added in organic solvent, fully after dissolving, obtains icariin solution；Will
PVA is added in deionized water, and PVA solution is obtained after being completely dissolved；The organic solvent is methanol, ethyl acetate, dichloromethane
One or more in alkane and chloroform；
Step 2: emulsification：Icariin solution is added in PVA solution, mixed, carries out emulsification treatment；
Step 3: remove organic solvent：After emulsification terminates, mixed solution is collected, passes through removed by evaporation organic solvent；
Step 4: purifying：The sample for removing organic solvent is centrifuged, is precipitated with purifying water washing, is centrifuged, grasp repeatedly again
Make 3-5 times, nanoparticle is cleaned up, you can obtain icariin nanoparticle；
The PVA is the abbreviation of polyvinyl alcohol.
2. the preparation method of icariin nanoparticle according to claim 1, it is characterised in that：In the step 1
The concentration of PVA solution is between the mg/ml of 1 mg/ml ~ 100.
3. the preparation method of icariin nanoparticle according to claim 1, it is characterised in that：PVA in the step 1
The concentration of solution is between the mg/ml of 10 mg/ml ~ 50.
4. the preparation method of icariin nanoparticle according to claim 1, it is characterised in that：It is excessive in the step 2
The volume ratio of sheep leaves of pulse plants glycosides solution and PVA solution is 1:1~1:Between 20.
5. the preparation method of icariin nanoparticle according to claim 1, it is characterised in that：Excessive sheep in the step 2
The volume ratio of leaves of pulse plants glycosides solution and PVA solution is 1:3~1:Between 9.
A kind of 6. icariin nano-particle that as claimed in claim 1 prepared by method.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109276544A (en) * | 2018-11-12 | 2019-01-29 | 中国医学科学院药用植物研究所 | A kind of hydrated icaritin nanoparticle and its preparation method and application |
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| CN104758261A (en) * | 2015-04-30 | 2015-07-08 | 中国医学科学院生物医学工程研究所 | Icariin PLGA nano particles and preparing method and application thereof |
| CN106361727A (en) * | 2016-11-25 | 2017-02-01 | 遵义医学院 | Bilobalide-PVA nanoparticle and preparation method thereof |
-
2017
- 2017-10-16 CN CN201710957309.3A patent/CN107648183A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104758261A (en) * | 2015-04-30 | 2015-07-08 | 中国医学科学院生物医学工程研究所 | Icariin PLGA nano particles and preparing method and application thereof |
| CN106361727A (en) * | 2016-11-25 | 2017-02-01 | 遵义医学院 | Bilobalide-PVA nanoparticle and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109276544A (en) * | 2018-11-12 | 2019-01-29 | 中国医学科学院药用植物研究所 | A kind of hydrated icaritin nanoparticle and its preparation method and application |
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