CN108553417A - A kind of Osthole self-emulsifying drug delivery system and preparation method thereof and purposes - Google Patents
A kind of Osthole self-emulsifying drug delivery system and preparation method thereof and purposes Download PDFInfo
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Abstract
The present invention provides a kind of Osthole self-emulsifying drug delivery systems, it is the preparation being prepared by Osthole and auxiliary material, and Osthole accounts for the 0.1%~10% of quality point, and auxiliary material accounts for the 90%~99.9% of quality point；The auxiliary material includes oil phase, surfactant and cosurfactant, wherein the mass percent that oil phase, surfactant and cosurfactant account for auxiliary material is respectively：Oil phase 25%~55%, surfactant 5%~45%, remaining is cosurfactant.The present invention also provides the preparation methods and purposes of above-mentioned Osthole self-emulsifying drug delivery system.Osthole self-emulsifying drug delivery system provided by the invention, emulsification is rapid after being contacted with water, gained emulsion droplet average grain diameter small (31.8 ± 1.6nm), In Vitro Dissolution is rapid and dissolution rate is high, and patient only need to be in before use plus the dilution of appropriate water, (mist) is sprayed in skin surface, it is easy to operate, greatly improve the compliance of patient.The present invention improves the dissolubility of Osthole by preparation technique, improves the bioavilability of Osthole in human body, has preferable potential applicability in clinical practice.
Description
Technical field
The invention belongs to field of medicaments, and in particular to a kind of Osthole self-emulsifying drug delivery system and preparation method thereof with
On the way.
Background technology
Osthole (Osthole) belongs to alkyl coumarin kind compound, is the dry fruit from samphire cnidium monnieri
A kind of active ingredient that extraction is isolated in frutus cnidii (CnidiummonnieriL.Cuss), is clinically mainly used for treating wet
The skin diseases such as rash, tinea of feet and hands, nettle rash.Recent study, which shows that Osthole has, improves arrhythmia cordis, anti-hypertension, suppression
Growth of tumour cell processed, inhibits the clinical effectiveness such as allergy at easing pain and diminishing inflammation.
Since Osthole water solubility is poor, cause drug absorption poor, clinical therapeutic efficacy cannot be reached.Therefore having must
The dissolubility that improve Osthole by preparation technique, improves drug absorption speed and degree, reaches good clinical treatment
Effect.
Invention content
To solve the above problems, the present invention provides a kind of Osthole self-emulsifying drug delivery systems.
The Osthole self-emulsifying drug delivery system of the present invention, it is the preparation being prepared by Osthole and auxiliary material, cnidium monnieri
Sub- element accounts for the 0.1%~10% of quality point, and auxiliary material accounts for the 90%~99.9% of quality point；The auxiliary material includes oil phase, surface work
Property agent and cosurfactant, wherein oil phase, surfactant and cosurfactant account for the mass percent difference of auxiliary material
For：Oil phase 25%~55%, surfactant 5%~45%, remaining is cosurfactant.
Wherein, the Osthole is with auxiliary material quality proportioning：Osthole 1%, auxiliary material 99%.
Wherein, in the auxiliary material, oil phase, surfactant and cosurfactant account for the mass percent difference of auxiliary material
For：Oil phase 35%~55%, surfactant 15%~35%, cosurfactant 15%~30%.
Further, in the auxiliary material, oil phase, surfactant and cosurfactant account for the mass percent point of auxiliary material
It is not：Oil phase 40%~50%, surfactant 25%~35%, cosurfactant 20%~25%.
Further, in the auxiliary material, oil phase, surfactant and cosurfactant account for the mass percent point of auxiliary material
It is not：Oil phase 46.9%, surfactant 29.9%, cosurfactant 23.2%.
Wherein, the oil phase is selected from one or more of Sefsol 218, Capmul MCM C8, ethyl oleate
Composition.
Further, the oil phase is Capmul MCM C8.
Wherein, the surfactant is selected from Emulsifier EL-60,40 stearate of polyethylene glycol, the poly- second of caprylic capric
The composition of one or more of glycol glyceride, Tween 20, Tween 80.
Further, the surfactant is Tween 20.
Wherein, the cosurfactant is selected from the composition of one or both of propylene glycol and PEG400.
Further, the cosurfactant is PEG400.
Wherein, the preparation is external preparation, it is preferable that the preparation is liquid preparation, soft capsule.
The present invention also provides a kind of Cnidiadin emulsions, it is characterised in that：It is released by above-mentioned Osthole self-emulsifying
Medicine system is mixed with water and the preparation that is formed.
Further, the Cnidiadin emulsion is to be diluted with water to 100 by above-mentioned Osthole self-emulsifying drug delivery system
The preparation formed again.
The present invention also provides the preparation methods of above-mentioned Osthole self-emulsifying drug delivery system, include the following steps：
It takes the oil phase, surfactant and cosurfactant of recipe quantity to mix, is added with stirring Osthole dissolving, i.e.,
.
The present invention also provides the preparation methods of above-mentioned Cnidiadin emulsion, include the following steps：
Take Osthole self-emulsifying drug delivery system, be diluted with water to get.
The present invention also provides above-mentioned Osthole self-emulsifying drug delivery systems to prepare treatment eczema, tinea of feet and hands, nettle rash
Purposes in the drug of equal skin diseases.
The present invention also provides above-mentioned Cnidiadin emulsions to prepare the skin diseases such as treatment eczema, tinea of feet and hands, nettle rash
Drug in purposes.
Self-emulsifying drug delivery system (Self-emulsifying drug delivery system, SEDDS) be by oil phase,
Isotropic mixture that is that surfactant and cosurfactant are constituted and including drug, contacted with aqueous medium and
A kind of isotropism, heating power of the transparent or semitransparent, average grain diameter between 20-500nm can be spontaneously formed under mild stirring
Learn stable liquid dispersion system (such as micro emulsion).Self-micro-emulsification medicine-releasing system refer to after emulsification size droplet diameter less than 100nm from
Emulsify drug delivery system.
Osthole self-emulsifying drug delivery system provided by the invention, microemulsified is rapid after being contacted with water, gained emulsion droplet is average
Grain size small (31.8 ± 1.6nm), In Vitro Dissolution is rapid and dissolution rate is high.Osthole self-emulsifying drug delivery provided by the invention system
System, patient only need to be in before use plus the dilution of appropriate water, and sprinkling (mist) is easy to operate in skin surface, greatly improves
The compliance of patient.The present invention improves the dissolubility of Osthole by preparation technique, improves the absorption speed of Osthole
Degree and degree, that is, improve the bioavilability of Osthole in human body, has preferable potential applicability in clinical practice.
Obviously, the above according to the present invention is not being departed from according to the ordinary technical knowledge and customary means of this field
Under the premise of the above-mentioned basic fundamental thought of the present invention, the modification, replacement or change of other diversified forms can also be made.
The specific implementation mode of form by the following examples remakes further specifically the above of the present invention
It is bright.But the range that this should not be interpreted as to the above-mentioned theme of the present invention is only limitted to example below.It is all to be based on the above of the present invention
The technology realized all belongs to the scope of the present invention.
Description of the drawings
The particle diameter distribution of Osthole micro emulsion and Zeta electricity after Fig. 1 Osthole self-emulsifying drug delivery system self-emulsifyings of the present invention
Bitmap
The transmission electron microscope photo of Osthole micro emulsion after Fig. 2 Osthole self-emulsifying drug delivery system self-emulsifyings of the present invention
Fig. 3 Osthole self-emulsifying drug delivery systems of the present invention and Osthole bulk pharmaceutical chemicals In Vitro Dissolution curve (n=6)
Specific implementation mode
The preparation of 1 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 2 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 3 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 4 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 5 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 6 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 7 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 8 Osthole self-emulsifying drug delivery system of the present invention of embodiment
1 composition
2 preparation methods
The Capmul MCM C8, Tween 20 and PEG400 of recipe quantity are taken, is uniformly mixed, is added with stirring Osthole,
Continue stir 30min so that Osthole is fully dissolved, packaging to get.
The preparation of 9 Cnidiadin emulsion of the present invention of embodiment
1 composition
2 preparation methods
1) prepared by self-emulsifying drug delivery system：Take the Capmul MCM C8, Tween 20 and PEG400 of recipe quantity, mixing equal
It is even, be added with stirring Osthole, continue stir 30min so that Osthole is fully dissolved to get；
2) prepared by emulsion：Take self-emulsifying drug delivery system obtained by step 1), be diluted with water to 100 times to get.
Illustrate beneficial effects of the present invention below by way of the mode of experimental example：
The self-emulsifying drug delivery system for meeting medication requirement needs to have the following conditions：Drug is answered in self-emulsifying drug delivery system
There is larger solvability, to reduce the usage amount of self-emulsifying drug delivery system auxiliary material, especially surfactant and surface is helped to live
The dosage of property agent；Oil phase, surfactant and cosurfactant intermiscibility are preferable, can form uniform, transparent, isotropism
Solution；Self-emulsifying drug delivery system can emulsify rapidly to form homogeneous system after Jia Shui is gently mixed.
Instrument and material
DF-101S type heat collecting type constant temperature blender with magnetic force (Yuhua Instrument Co., Ltd., Gongyi City)；Agilent-
1100 high performance liquid chromatographs (Anjelen Sci. ＆ Tech. Inc)；FA1004N assay balances (the limited public affairs of Shanghai precision instrumentation
Department)；Malvern Zetasizer (Nano ZS90) dynamic light scattering (Malvern company of Britain)；JEM-1400 120kV are saturating
Penetrate electron microscope (Jeol Ltd.)；RCZ-6B intelligence digestion instrument (Shanghai Huanghai Sea medicine inspection instrument plant)；Bag filter (is cut
Stay molecular weight：12,000 dalton, the Shanghai bio tech ltd Yuan Ye).
Osthole reference substance (is purchased from Nat'l Pharmaceutical ＆ Biological Products Control Institute)；Osthole bulk pharmaceutical chemicals (Baoji Fang Sheng
Biological development corporation, Ltd., content：80%)；Sefsol 218 (Capryol 90, Jia Fa lion trade Co., Ltd)；It is single
Glycerol caprylate (Capmul MCM C8, Jia Fa lions trade Co., Ltd)；Ethyl oleate (BASF AG)；Polyoxyethylene castor
Sesame oil (Cremophor EL, BASF AG)；40 stearate of polyethylene glycol (Cremophor RH 40, BASF application
Work Co., Ltd)；Labraso (Labrasol, Jia Fa lion trade Co., Ltd)；Tween 80/
Tween 20 (Nanjing WeiEr chemical engineering Co., Ltd)；Polyethylene glycol 400 (PEG400, the limited duty of Hubei Ge Dian people's good fortune pharmaceutic adjuvant
Ren companies), 1,2-PD (Tianjin great Mao chemical reagent factories).
Experimental example 1 screens oil phase, surfactant and cosurfactant by solubility experiment
Using high performance liquid chromatography, solubility of the Osthole in each auxiliary material is measured, determines the preferred of all kinds of auxiliary materials
Mode.
1 chromatographic condition
Chromatographic column：Phenomenex C18 columns (250mm × 4.6mm, 5 μm)；Mobile phase：Methanol-water (70:30, v/v),
Flow velocity：1.0mL·min-1；Detection wavelength：322nm；Column temperature：25℃；Sample size：20μL.
The preparation of 2 reference substance solutions
Precision weighs Osthole reference substance 4.8mg, sets in 10m L volumetric flasks, adds methanol to dissolve and is diluted to scale, shakes
It is even；Up to 0.48mg/m L Osthole reference substance storing solutions；Use methanol dilute successively above-mentioned Osthole reference substance storing solution
Release the Osthole reference substance solution that 0.348,0.288,0.192,0.096mg/m L are made respectively.
The preparation of 3 sample solutions
Solubility of the Osthole in each oil phase, surfactant and cosurfactant is measured with fask oscillating method.Take snake
Machine tool element 0.02g is added in each screw-cap glass bottle containing 2mL auxiliary materials, mixture is placed on turbine mixer
Upper vortex mixed 5min makes drug be sufficiently mixed with auxiliary material, and it is small that mixture is placed on concussion dissolving 72 in constant temperature shaking water-bath
When, so that drug is fully dissolved and reach saturation state, 10min is then centrifuged under the conditions of 5000rpm, takes supernatant, with 0.22 μm
Membrane filtration takes filtrate 1mL, with methanol dilution 50 again to get sample solution.
4 dissolution determinations
Reference substance solution and sample solution are drawn respectively and injects high performance liquid chromatograph, in external standard method each sample solution
Content of Osthole, and calculate solubility of the Osthole in each auxiliary material.
5 experimental results
It the results are shown in Table 1.
Solubility (n=3) of 1 Osthole of table in each auxiliary material
By solubility experiment result it is found that solubility of the Osthole in oil phase Capmul MCMC8 is maximum, solubility
Reach (84.21 ± 0.37) mg/mL, solubility in surfactant Tween 20 is maximum, solubility reach (194.34 ±
0.69) mg/mL, the solubility in cosurfactant PEG400 is maximum, and solubility reaches (36.78 ± 0.19) mg/mL.
Therefore, preferred oil phases of the Capmul MCMC8 as Osthole self-emulsifying drug delivery system, Tween in the present invention
20 are used as surfactant, and PEG400 is as cosurfactant.
The comparison of 2 Osthole self-emulsifying drug delivery system different auxiliary material prescription of the present invention of experimental example proportioning
The percentage composition that Capmul MCMC8,20 Tween, PEG400 are accounted for auxiliary material respectively selects flat as prescription variable
Equal grain size, self-emulsifying time and 15min release amount of medicine are as evaluation index, Osthole when comparing different auxiliary material prescription proportioning
The emulsifying effectiveness and drug release ability of self-emulsifying drug delivery system.
Each auxiliary material is prepared by proportioning shown in table 2, and Osthole and each prepared auxiliary material are pressed 1%：99% quality
Proportioning is prepared into the Osthole self-emulsifying drug delivery system of 11 groups of present invention.Three component proportion summations are 100%.
2 each auxiliary material prescription component of table and its proportioning
The average grain diameter of above-mentioned prepared 11 groups of Osthole self-emulsifying drug delivery systems is measured by the following method, from breast
Change time and 15min release amount of medicine：
Each group Osthole self-emulsifying drug delivery system is diluted to 100 times with distilled water, uses Malvern Zetasizer
(Nano ZS90) measures the average grain diameter for forming micro emulsion；
Using dissolution testing apparatus paddle method, is continuously stirred at 37 ± 0.5 DEG C and 1mL Ostholes are added under (50rpm) certainly
It emulsifies in medicine-releasing system to 900mL distilled water, measures the time needed for each group substantially uniformity dispersion, the as breast certainly of each group
Change the time；
Using《Chinese Pharmacopoeia》Version four " general rule 0931 " second method of dissolution method measures each group frutus cnidii within 2015
Plain self-emulsifying drug delivery system 15min release amount of medicine (Y3).Dissolution medium is the pH 6.8 containing 0.5% (w/v) Tween 80
Phosphate buffer, medium volume 900mL, medium temperature are (37 ± 0.5 DEG C), and agitating paddle speed is 50rpm.Open dissolution
Instrument takes the self-emulsifying drug delivery system for being equivalent to 50mg Ostholes to be added in dissolution medium, and when 15min samples, and sample is through 20
10min is centrifuged under the conditions of 000rpm, takes supernatant, uses HPLC analysis method determination sample drug contents, as frutus cnidii
Plain self-emulsifying drug delivery system 15min release amount of medicine.
Experimental result is shown in Table 3：
3 different auxiliary material prescription of table is to average grain diameter, the influence of self-emulsifying time and 15min release amount of medicine
It is above-mentioned the experimental results showed that：
1) after Capmul MCMC8 (oil phase) quality proportioning is more than 55% in auxiliary material prescription (prescription 10,11,12,13),
Gained self-emulsifying drug delivery system 15min drug release amounts are less than 95%, and with Capmul MCMC8 (oil phase) quality in auxiliary material prescription
The increase of proportioning and reduce, particularly, (prescription after Capmul MCMC8 (oil phase) quality proportioning reaches 80% in auxiliary material prescription
12), gained self-emulsifying drug delivery system 15min drug release amounts are only 75.2%, when Capmul MCMC8 (oil phase) matter in auxiliary material prescription
After amount proportioning reaches 85.2% (prescription 13), gained self-emulsifying drug delivery system 15min drug release amounts are only 62.0%；When auxiliary material prescription
After middle Capmul MCMC8 (oil phase) quality proportioning is less than 25% (prescription 9), self-emulsifying drug delivery system can not emulsify shape after meeting water
At particle.Therefore Capmul MCMC8 (oil phase) quality proportioning preferably 25%~55% in auxiliary material prescription；
2) prescription 5 is the most preferably auxiliary material prescription of the present invention, and the gained self-emulsifying drug delivery system self-emulsifying time is most short, only
13s, 15min drug release amount highest, up to 99.9%；
3) in prescription 14, Tween20 (surfactant) quality proportioning is 52.6% in auxiliary material prescription, is more than 45%, institute
It is only 72.1% to obtain self-emulsifying drug delivery system 15min drug release amounts, so Tween20 (surfactant) quality is matched in auxiliary material prescription
Than being preferably 5%~45%.
To sum up, in Osthole self-emulsifying drug delivery system of the present invention, auxiliary material prescription proportioning is：Oil phase 25%~55%, table
Face activating agent 5%~45%, remaining is cosurfactant.The present invention most preferably auxiliary material prescription, which matches, is：Oil phase 46.9%, table
Face activating agent 29.9%, cosurfactant 23.2%.
Self-emulsifying time, formation below by way of the optimal Osthole self-emulsifying drug delivery system prescription of the experimental evaluation present invention
Micro emulsion appearance, average grain diameter, PdI, Zeta potential, microscopic pattern and release in vitro situation.
3 Osthole self-emulsifying drug delivery system quality determination of the present invention of experimental example
It is that the present invention made from the embodiment of the present invention 1 is optimal to test involved Osthole self-emulsifying drug delivery system below
The Osthole self-emulsifying drug delivery system of prescription.
1 self-emulsifying time
Using dissolution testing apparatus paddle method, is continuously stirred at 37 ± 0.5 DEG C and 1mL Ostholes are added under (50rpm) certainly
Emulsify medicine-releasing system to 900mL distilled water in, measure substantially uniformity dispersion needed for time, and record the self-emulsifying time with
And appearance.
The experimental results showed that the Osthole self-emulsifying drug delivery system self-emulsifying time is (15.2 ± 1.4) second, show cnidium monnieri
Sub- element self-emulsifying drug delivery system can quickly form light blue transparent opalescence shape solution when being contacted with water.
The measurement of 2 average grain diameters and Zeta potential
Osthole self-emulsifying drug delivery system is diluted to 100 times with distilled water, uses Malvern Zetasizer
(Nano ZS90) measures the average grain diameter and Zeta potential for forming micro emulsion.
Measurement result is as shown in Figure 1.
The experimental results showed that the average grain diameter of Osthole micro emulsion is (31.8 ± 1.6) nm, PdI values is 0.164 ±
0.014, lower PdI values indicate that average particle size distribution is more uniform, Zeta potential value is-
(26.1 ± 1.4) mV, negative electrical charge may be due in prescription there are surfactant and cosurfactant caused by.
3 scanning electron microscopic observations
Osthole self-emulsifying drug delivery system is diluted with distilled water, and microemulsion is added drop-wise to the double faced adhesive tape of aluminium bar
On, sample is put into scanning electron microscope room, is 1.0nm in resolution ratio, Osthole micro emulsion is scanned under the conditions of accelerating potential 15kv,
Shoot electromicroscopic photograph.
Experimental result is as shown in Figure 2.
It can be observed by transmission electron microscope photo, Osthole micro emulsion is in rounding, regular spherical, the grain size of most of particle
In 30nm or so.
4 study in vitro dissolution
Using《Chinese Pharmacopoeia》It is former that version four " general rule 0931 " second method of dissolution method in 2015 measures Osthole
Expect medicine and the external drug dissolution of Osthole self-emulsifying drug delivery system.Dissolution medium is to contain 0.5% (w/v) Tween's 80
6.8 phosphate buffers of pH, medium volume 900mL, medium temperature are (37 ± 0.5 DEG C), and agitating paddle speed is 50rpm.It opens
Digestion instrument is opened, take 50mg Ostholes bulk pharmaceutical chemicals respectively and the self-emulsifying drug delivery system for being equivalent to 50mg Ostholes is taken to be added to
In dissolution medium, sampled respectively in the predetermined time of 0,5,10,15,30,45,60,75,90,120,150 and 180min, sample
Through centrifuging 10min under the conditions of 20 000rpm, supernatant is taken, HPLC analysis method determination sample drug contents are used.
Measurement result is as shown in Figure 3.
Stripping curve studies have shown that dissolution rate of the Osthole bulk pharmaceutical chemicals in 180min less than 40%, and Osthole
Self-micro-emulsification medicine-releasing system can reach 90% or more in 45min, illustrate that self-emulsifying drug delivery system significantly improves frutus cnidii
The dissolution rate of element.
To sum up, Osthole self-emulsifying drug delivery system provided by the invention, microemulsified is rapid after being contacted with water, gained emulsion droplet
Average grain diameter small (31.8 ± 1.6nm), In Vitro Dissolution is rapid and dissolution rate is high.The present invention improves frutus cnidii by preparation technique
The dissolubility of element, improves the infiltration rate and degree of Osthole, that is, improves the biological utilisation of Osthole in human body
Degree has preferable potential applicability in clinical practice.
Claims (18)
1. a kind of Osthole self-emulsifying drug delivery system, it is characterised in that：It is the preparation being prepared by Osthole and auxiliary material,
Osthole accounts for the 0.1%~10% of quality point, and auxiliary material accounts for the 90%~99.9% of quality point；The auxiliary material includes oil phase, table
Face activating agent and cosurfactant, wherein oil phase, surfactant and cosurfactant account for the mass percent point of auxiliary material
It is not：Oil phase 25%~55%, surfactant 5%~45%, remaining is cosurfactant.
2. self-emulsifying drug delivery system according to claim 1, it is characterised in that：The Osthole and auxiliary material quality proportioning
For：Osthole 1%, auxiliary material 99%.
3. self-emulsifying drug delivery system according to claim 1, it is characterised in that：In the auxiliary material, oil phase, surfactant
The mass percent that auxiliary material is accounted for cosurfactant is respectively：Oil phase 35%~55%, helps surfactant 15%~35%
Surfactant 15%~30%.
4. self-emulsifying drug delivery system according to claim 1, it is characterised in that：In the auxiliary material, oil phase, surfactant
The mass percent that auxiliary material is accounted for cosurfactant is respectively：Oil phase 40%~50%, helps surfactant 25%~35%
Surfactant 20%~25%.
5. self-emulsifying drug delivery system according to claim 1, it is characterised in that：In the auxiliary material, oil phase, surfactant
The mass percent that auxiliary material is accounted for cosurfactant is respectively：Oil phase 46.9%, helps surface-active at surfactant 29.9%
Agent 23.2%.
6. according to any one of them self-emulsifying drug delivery system of claim 1 or 3~5, it is characterised in that：The oil phase is selected from third
The composition of one or more of glycol list caprylate, Capmul MCM C8, ethyl oleate.
7. self-emulsifying drug delivery system according to claim 6, it is characterised in that：The oil phase is Capmul MCM C8.
8. according to any one of them self-emulsifying drug delivery system of claim 1 or 3~5, it is characterised in that：The surfactant
Selected from Emulsifier EL-60,40 stearate of polyethylene glycol, Labraso, Tween 20, Tween
One or more of 80 composition.
9. self-emulsifying drug delivery system according to claim 8, it is characterised in that：The surfactant is Tween 20.
10. according to any one of them self-emulsifying drug delivery system of claim 1 or 3~5, it is characterised in that：It is described that surface is helped to live
Property agent be selected from the composition of one or both of propylene glycol and PEG400.
11. self-emulsifying drug delivery system according to claim 10, it is characterised in that：The cosurfactant is
PEG400。
12. self-emulsifying drug delivery system according to claim 1, it is characterised in that：The preparation is external preparation, preferably
Ground, the preparation are liquid preparation, soft capsule.
13. a kind of Cnidiadin emulsion, it is characterised in that：It is mixed with water by above-mentioned Osthole self-emulsifying drug delivery system and
The preparation of formation.
14. emulsion according to claim 13, it is characterised in that：It is added by above-mentioned Osthole self-emulsifying drug delivery system
Water is diluted to 100 times and the preparation of formation.
15. the preparation method of claim 1~12 any one of them Osthole self-emulsifying drug delivery system, it is characterised in that：
It includes the following steps：
Take the oil phase, surfactant and cosurfactant of recipe quantity to mix, be added with stirring Osthole dissolving to get.
16. the preparation method of claim 13 or 14 any one of them Cnidiadin emulsions, it is characterised in that：It includes as follows
Step：
Take Osthole self-emulsifying drug delivery system, be diluted with water to get.
17. claim 1~12 any one of them Osthole self-emulsifying drug delivery system prepare treatment eczema, tinea of feet and hands,
Purposes in the drug of the skin diseases such as nettle rash.
18. claim 13 or 14 any one of them Cnidiadin emulsions are preparing the skins such as treatment eczema, tinea of feet and hands, nettle rash
Purposes in the drug of skin disease.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110711177A (en) * | 2019-09-23 | 2020-01-21 | 山东第一医科大学(山东省医学科学院) | Osthole microemulsion and preparation method and application thereof |
| CN112107541A (en) * | 2019-06-21 | 2020-12-22 | 陕西中医药大学 | Astragaloside IV self-emulsifying drug delivery system and preparation method thereof |
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| CN102119926A (en) * | 2011-03-07 | 2011-07-13 | 沈阳药科大学 | Valsartan self-emulsifying medicament transfer system and preparation method thereof |
| KR20170030836A (en) * | 2015-09-10 | 2017-03-20 | 주식회사 엘지생활건강 | External composition for antiaging comprising osthole |
| CN107456443A (en) * | 2017-07-21 | 2017-12-12 | 苏州信恩医药科技有限公司 | A kind of Osthole self-emulsifiable preparation and preparation method thereof |
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| CN102119926A (en) * | 2011-03-07 | 2011-07-13 | 沈阳药科大学 | Valsartan self-emulsifying medicament transfer system and preparation method thereof |
| KR20170030836A (en) * | 2015-09-10 | 2017-03-20 | 주식회사 엘지생활건강 | External composition for antiaging comprising osthole |
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| CN112107541A (en) * | 2019-06-21 | 2020-12-22 | 陕西中医药大学 | Astragaloside IV self-emulsifying drug delivery system and preparation method thereof |
| CN112107541B (en) * | 2019-06-21 | 2023-07-25 | 陕西中医药大学 | Astragaloside IV self-emulsifying drug release system and preparation method thereof |
| CN110711177A (en) * | 2019-09-23 | 2020-01-21 | 山东第一医科大学(山东省医学科学院) | Osthole microemulsion and preparation method and application thereof |
| CN110711177B (en) * | 2019-09-23 | 2022-03-25 | 山东第一医科大学(山东省医学科学院) | Osthole microemulsion and preparation method and application thereof |
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