CN105815771A - Preparation method of erinacine/PLGA microsphere - Google Patents
Preparation method of erinacine/PLGA microsphere Download PDFInfo
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- 239000004005 microsphere Substances 0.000 title claims abstract description 59
- 229930191277 erinacine Natural products 0.000 title claims abstract description 51
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 title claims abstract description 51
- 238000002360 preparation method Methods 0.000 title claims abstract description 35
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims abstract description 57
- 238000003756 stirring Methods 0.000 claims abstract description 25
- 108010010803 Gelatin Proteins 0.000 claims abstract description 15
- 229920000159 gelatin Polymers 0.000 claims abstract description 15
- 239000008273 gelatin Substances 0.000 claims abstract description 15
- 235000019322 gelatine Nutrition 0.000 claims abstract description 15
- 235000011852 gelatine desserts Nutrition 0.000 claims abstract description 15
- 239000000725 suspension Substances 0.000 claims abstract description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 239000012153 distilled water Substances 0.000 claims abstract description 5
- 238000004108 freeze drying Methods 0.000 claims abstract description 5
- 239000000284 extract Substances 0.000 claims abstract description 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 24
- 230000001804 emulsifying effect Effects 0.000 claims description 17
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 12
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 12
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 8
- 238000000605 extraction Methods 0.000 claims description 8
- 208000035126 Facies Diseases 0.000 claims description 7
- 240000000588 Hericium erinaceus Species 0.000 claims description 6
- 235000007328 Hericium erinaceus Nutrition 0.000 claims description 6
- 244000309464 bull Species 0.000 claims description 6
- 229960004275 glycolic acid Drugs 0.000 claims description 6
- 239000004310 lactic acid Substances 0.000 claims description 6
- 235000014655 lactic acid Nutrition 0.000 claims description 6
- 239000000178 monomer Substances 0.000 claims description 5
- 239000003208 petroleum Substances 0.000 claims description 5
- 239000007788 liquid Substances 0.000 claims description 4
- 238000004062 sedimentation Methods 0.000 claims description 4
- 241000289667 Erinaceus Species 0.000 claims description 3
- 238000002481 ethanol extraction Methods 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 238000005538 encapsulation Methods 0.000 abstract description 16
- 238000004945 emulsification Methods 0.000 abstract description 6
- 238000005516 engineering process Methods 0.000 abstract description 5
- 239000012074 organic phase Substances 0.000 abstract 2
- 238000005119 centrifugation Methods 0.000 abstract 1
- 238000013268 sustained release Methods 0.000 abstract 1
- 239000012730 sustained-release form Substances 0.000 abstract 1
- 238000009210 therapy by ultrasound Methods 0.000 abstract 1
- 238000005406 washing Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 description 10
- 230000000694 effects Effects 0.000 description 6
- 235000021050 feed intake Nutrition 0.000 description 4
- 235000013305 food Nutrition 0.000 description 4
- 239000000872 buffer Substances 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 208000024827 Alzheimer disease Diseases 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- 238000002835 absorbance Methods 0.000 description 2
- 238000013019 agitation Methods 0.000 description 2
- 235000013361 beverage Nutrition 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000003094 microcapsule Substances 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- -1 Diterpenes Chemical class 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 102000015336 Nerve Growth Factor Human genes 0.000 description 1
- 108010025020 Nerve Growth Factor Proteins 0.000 description 1
- 208000007443 Neurasthenia Diseases 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- UGAPHEBNTGUMBB-UHFFFAOYSA-N acetic acid;ethyl acetate Chemical compound CC(O)=O.CCOC(C)=O UGAPHEBNTGUMBB-UHFFFAOYSA-N 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 206010003549 asthenia Diseases 0.000 description 1
- 210000000467 autonomic pathway Anatomy 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229930004069 diterpene Natural products 0.000 description 1
- 125000000567 diterpene group Chemical group 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 239000002024 ethyl acetate extract Substances 0.000 description 1
- 238000000556 factor analysis Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 235000013402 health food Nutrition 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000011031 large-scale manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- VUZPPFZMUPKLLV-UHFFFAOYSA-N methane;hydrate Chemical compound C.O VUZPPFZMUPKLLV-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 229940053128 nerve growth factor Drugs 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Abstract
The invention provides a preparation method of an erinacine/PLGA microsphere. The preparation method comprises the following steps: dissolving PLGA into dichloromethane to form an organic phase; adding erinacine extract into the obtained organic phase, carrying out an ultrasonic treatment to obtain suspension; adding the suspension into a gelatin water solution, stirring the solution in a speed of 300 to 1500 rpm/min at a temperature of 5 to 30 DEG C to carry out emulsification for 5 to 85 minutes, then stirring the solution in a speed of 100 to 500 rpm/min at a room temperature to completely evaporate dichloromethane so as to precipitate the microspheres; carrying out centrifugation at a temperature of 0 to 4 DEG C, collecting the precipitated microspheres, washing the microspheres by distilled water, and freeze-drying microspheres in vacuum to obtain the finished product. The preparation method has the advantages that the encapsulation rate of prepared erinacine/PLGA microsphere is high, moreover, the erinacine/PLGA microsphere has a sustained-release function, the bioavailability is high, the preparation technology is simple and convenient, the preparation cost is low, the technological repeatability is good, the using amount of sample is little, and the preparation method has an important meaning for industrial application.
Description
(1) technical field
The present invention relates to the preparation method of a kind of health product, be specifically related to the preparation method of a kind of erinacine/PLGA microsphere.
(2) background technology
Erinacine, chemical composition is the micromolecular compounds such as Diterpenes, can promote the synthesis of nerve growth factor, fails intellectual deterioration, neurasthenia and autonomic nerve, especially Alzheimer's disease and dementia is had good effect.Additionally, erinacine all has certain health-care effect in many-sides such as improving immunity of organisms, anti-cancer and inhibiting tumor, blood pressure lowering, blood sugar lowering.It is widely used in the middle of food, beverage, medical treatment, and it has higher edible and medical value.Erinacine is usually white crystal, for low-polarity component, is soluble in lipophylic organic solvents, dissolves in alcohol, is insoluble in water.
Microcapsule technology be material fine dispersion is coated with after, and the method discharged required when.It is widely used at field of food, have developed much micro encapsulation food, as powdered oil, capsule beverage, nutrition enhancer such as vitamin, aminoacid etc., micro encapsulation food additive have been widely used in production the most.It is convenient that microcapsule technology is also applied to bakery, health food and fixed yeast cultivation etc., and application in the food industry will constantly be widened.
Poly(D,L-lactide-co-glycolide [poly (lactic-co-glycolicacid), PLGA] it is to be polymerized at random by two kinds of monomers (lactic acid and hydroxyacetic acid), it it is a kind of Biodegradable high-molecular organic compound, its catabolite lactic acid and hydroxyacetic acid may participate in the metabolism of human body, ultimately form carbon dioxide and water is excreted.Due to it, there is good biocompatibility and biodegradability and degradation speed is controlled, have been widely used at biomedical sector tool.
Prepare medicine carrying microballoons with PLGA, the stability of erinacine can be increased, cover its poor taste, control its rate of release and realize long-acting purpose, improve bioavailability.
(3) summary of the invention
It is an object of the invention to provide the preparation method of a kind of erinacine/PLGA microsphere, the inventive method technique is simple, and the cycle is short, and is applicable to large-scale production.
For achieving the above object, the present invention adopts the following technical scheme that
A kind of preparation method of erinacine/PLGA microsphere, described preparation method comprises the following steps:
(1) PLGA is dissolved in dichloromethane, forms organic facies；
(2) being added in the organic facies that step (1) obtains by erinacine extractum, (20～60KHz) ultrasonic (20～60min) obtain suspension；Described erinacine extractum is the extractum that Hericium erinaceus (Bull. Ex Fr.) Pers. mycelium prepares through ethanol extraction；
(3) suspension that step (2) obtains is added drop-wise in aqueous gelatin solution, then first at 5～30 DEG C with the speed stirring and emulsifying 5～85min (preferably 25～65min) of 300～1500rpm (preferably 600～1000rpm), stir with the speed of 100～500rpm (preferably 150～300rpm) under room temperature (20～30 DEG C) until dichloromethane volatilization is complete, microsphere settles out, then centrifugal at 0～4 DEG C, collect the microsphere of sedimentation, with distilled water wash, vacuum lyophilization, obtains described erinacine/PLGA microsphere；
Preparation method of the present invention, in step (1), described PLGA (Poly(D,L-lactide-co-glycolide) molecular weight is 5000～50000dal (preferably 30000dal), and the mol ratio of PLGA monomer lactic acid/hydroxyacetic acid is 75:25～50:50 (preferably 50:50).
In the organic facies that step (1) is formed, the mass concentration of PLGA is 2.5%～20%, preferably 5%～15%.
In step (2), the most described erinacine extractum obtains with the method for alcohol extraction, after Hericium erinaceus (Bull. Ex Fr.) Pers. mycelium is with ethanol extraction, extracting solution is first with petroleum ether extraction, collect raffinate, being extracted with ethyl acetate, collect extract, rotation is evaporated off ethyl acetate and obtains described erinacine extractum.Concrete, described erinacine extractum can be prepared as follows:
Hericium erinaceus (Bull. Ex Fr.) Pers. erinaceus mycelium powder is mixed with feed liquid mass ratio 1:20 with 95wt% ethanol, stand 1h, then microwave (power is 500w) extraction 25min at 60 DEG C, then with petroleum ether extraction, collect raffinate, being extracted with ethyl acetate, collect extract, rotation is evaporated off ethyl acetate and obtains described erinacine extractum.
In step (2), described erinacine extractum is 1:0.5～15 with the mass ratio that feeds intake of PLGA in step (1), preferably 1:2～10.
In step (3), the mass concentration of institute's gelatin water solution is 0.1%～1%, preferably 0.5%；Described suspension is 1:1～30 with the mass ratio of aqueous gelatin solution, preferably 1:10～25.
The beneficial effects of the present invention is:
1, the erinacine/PLGA microsphere using the inventive method to prepare has higher envelop rate under conditions of ensureing erinacine stability, high encapsulation rate reaches 98.87%, and the microsphere prepared has slow release effect, internal optimal concentration can be kept, and the time of prolongation effect, improve bioavailability；
2, this preparation method have that simple process, preparation cost be low, technique favorable reproducibility, feature that sample requirement is few, the prescription of experiment sieving and technique is also scalable to commercial production scale, and therefore the application to industrialization has directive significance.
(4) accompanying drawing explanation
Fig. 1 is the erinacine/PLGA microsphere scanning electron microscope (SEM) photograph of embodiment 1 preparation；
Fig. 2 is the PLGA concentration impact on microsphere encapsulation rate in embodiment 2；
Fig. 3 is the impact of embodiment 2 SMIS wall comparison microsphere encapsulation rate；
Fig. 4 is the stirring and emulsifying speed impact on microsphere encapsulation rate in embodiment 2；
Fig. 5 is the emulsification times impact on microsphere encapsulation rate in embodiment 2；
Fig. 6 is erinacine in embodiment 3/PLGA microsphere release in vitro result.
(5) detailed description of the invention
Below by specific embodiment, the invention will be further described, but protection scope of the present invention is not limited to that.
Embodiment 1: emulsifying volatility process prepares erinacine/PLGA microsphere
(1) erinacine extractum is prepared
Take 5g Hericium erinaceus (Bull. Ex Fr.) Pers. erinaceus mycelium powder (Beijing Fu Erkang biotechnology research institute) in 250mL there-necked flask, add 100mL95% ethanol (solid-liquid ratio is 1:20), stand 1h, then microwave (power 500w) extraction 25min under the conditions of temperature is 60 DEG C, then with petroleum ether extraction (500mL × 3), discard petroleum ether extraction liquid, collect raffinate and be extracted with ethyl acetate (500mL × 3) again, merge and collect acetic acid ethyl acetate extract, rotation is evaporated off ethyl acetate, obtains erinacine extractum 0.6g；
(2) erinacine/PLGA microsphere is prepared
First, taking PLGA (molecular weight is 30000dal, and the mol ratio of monomer lactic acid/hydroxyacetic acid is 50:50) 100mg and join in 2mL dichloromethane, be subsequently adding the erinacine extractum of the above-mentioned preparation of 25mg, the ultrasonic 30min of 40KHz obtains suspension；Gained suspension is slowly dropped in 50mL0.5wt% aqueous gelatin solution, the most first with the speed magnetic agitation emulsifying 30min of 1200rpm, the most at room temperature decelerate to 300rpm stirring 3h and volatilize dichloromethane, microsphere settles out, centrifugal at 0 DEG C afterwards, collect the microsphere of sedimentation, with distilled water wash, vacuum lyophilization, obtains described erinacine/PLGA microsphere 0.2g.Scanning electron microscopic observation thus obtained microsphere form, result is shown in Fig. 1, the full rounding of microsphere form.
Embodiment 2: microspheres is studied
(1) the PLGA concentration impact on microsphere encapsulation rate
The preparation manipulation of erinacine/PLGA microsphere is with embodiment 1, therein feed intake and operating parameter condition is: choose dichloromethane 2.0mL, 0.5% gelatin solution 50mL, PLGA100mg, core wall ratio (erinacine extractum and PLGA mass ratio) be 2:1, stirring and emulsifying speed 900rpm, emulsification times 30min, stir 3h under 300rpm to volatilize to dichloromethane, investigate the different PLGA concentration impact on microsphere embedding rate.PLGA concentration takes 2.5%, 5%, 10%, 15%, 20%.
The result that affects of microsphere encapsulation rate is shown in Fig. 2 by PLGA concentration.
(2) erinacine extractum and the PLGA mass ratio (the core wall ratio) impact on microsphere encapsulation rate
The preparation manipulation of erinacine/PLGA microsphere is with embodiment 1, therein feed intake and operating parameter condition is: choose dichloromethane 2.0mL, 0.5% gelatin solution 50mL, PLGA100mg, stirring and emulsifying speed 900rpm, emulsification times 30min, stir 3h under 300rpm to volatilize to dichloromethane, investigate the impact of different core wall comparison microsphere embedding rate.Core wall ratio takes 1:1,1:2,1:5,1:10,1:15.
The result that affects of core wall comparison microsphere encapsulation rate is shown in Fig. 3.
(3) the stirring and emulsifying speed impact on microsphere encapsulation rate
The preparation manipulation of erinacine/PLGA microsphere is with embodiment 1, therein feed intake and operating parameter condition is: choose dichloromethane 2.0mL, 0.5% gelatin solution 50mL, PLGA100mg, core wall than for 2:1, emulsification times 30min, stir 3h under 300rpm to volatilize to dichloromethane, investigate the different stirring and emulsifying speed impact on microsphere embedding rate.Stirring and emulsifying speed takes 300rpm, 600rpm, 900rpm, 1200rpm, 1500rpm.
The result that affects of microsphere encapsulation rate is shown in Fig. 4 by stirring and emulsifying speed.
(4) the stirring and emulsifying time impact on microsphere encapsulation rate
The preparation manipulation of erinacine/PLGA microsphere is with embodiment 1, therein feed intake and operating parameter condition is: choose dichloromethane 2.0mL, 0.5% gelatin solution 50mL, PLGA100mg, core wall than for 2:1, stirring and emulsifying speed 900rpm, stir 3h under 300rpm to volatilize to dichloromethane, investigate the different stirring and emulsifying time impact on microsphere embedding rate.Emulsification times takes 5min, 25min, 45min, 65min, 85min.
The result that affects of microsphere encapsulation rate is shown in Fig. 5 by the stirring and emulsifying time.
Comprehensive above each factor, it can be seen that PLGA is fine to the embedding effect of erinacine, by single factor analysis, selects the prescription that optimum condition is prepared as microsphere, and preparation technology is as follows:
First, (molecular weight is 30000dal to take PLGA, the mol ratio of monomer lactic acid/hydroxyacetic acid is 50:50) 300mg joins in 2mL dichloromethane, is subsequently adding the erinacine extractum that 150mg is prepared according to embodiment 1 method, and the ultrasonic 30min of 40KHz prepares suspension；Gained suspension is slowly dropped in the aqueous gelatin solution of 50mL0.5%, the most first with the speed magnetic agitation emulsifying 50min of 900rpm, then decelerate to 300rpm stirring 3h and volatilize dichloromethane, microsphere settles out, centrifugal at 0 DEG C afterwards, collect the microsphere of sedimentation, with distilled water wash, vacuum lyophilization, obtains described erinacine/PLGA microsphere 0.7g.Take the supernatant of centrifugal gained, survey absorbance with ultraviolet spectrophotometer.
Computational envelope rate according to the following formula
Recording envelop rate is 98.99%.
Embodiment 3: erinacine/PLGA microsphere extracorporeal releasing experiment
Weigh the erinacine/PLGA microsphere 0.3g prepared under optimum condition in embodiment 2, it is dispersed in respectively in the phosphate buffer of the hydrochloride buffer of 50mLpH1.5, the phosphate buffer of 50mLpH6.8,50mLpH7.4, under 37 DEG C of 100rpm, carries out dissolution experiment；Sample 5mL respectively at the set time, and add isopyknic buffer, at 210.0nm, measure absorbance with ultraviolet spectrophotometer；Calculate cumulative release percentage rate.Using preparation as vertical coordinate, draw drug release profiles figure with the time for abscissa, it is judged that the control release performance of microsphere.Release profiles is shown in Fig. 6.
From In-vitro release curves it can be seen that this erinacine/PLGA microsphere has slow release effect.Before in the solution of pH1.5,200h release is the fastest, and when the relatively slow and burst size discharged afterwards does not has pH6.8, pH7.4, release rate is high；In pH6.8, pH7.4 buffer, releasing trend is identical, and in pH7.4 solution, release is relatively fast in pH6.8 solution.
Claims (10)
1. the preparation method of erinacine/PLGA microsphere, it is characterised in that described preparation method comprises the following steps:
(1) PLGA is dissolved in dichloromethane, forms organic facies；In the organic facies formed, the mass concentration of PLGA is 2.5%～20%；
(2) erinacine extractum is added in step (1) organic facies that obtains, ultrasonic obtain suspension；Described erinacine extractum is 1:0.5～15 with the mass ratio that feeds intake of PLGA in step (1)；Described erinacine extractum is the extractum that Hericium erinaceus (Bull. Ex Fr.) Pers. mycelium prepares through ethanol extraction；
(3) suspension that step (2) obtains is added drop-wise in aqueous gelatin solution, then first at 5～30 DEG C with 300～1500rpm speed stirring and emulsifying 5～85min, stir with the speed of 100～500rpm the most at room temperature until dichloromethane volatilization is complete, microsphere settles out, then centrifugal at 0～4 DEG C, collect the microsphere of sedimentation, with distilled water wash, vacuum lyophilization, obtains described erinacine/PLGA microsphere；The mass concentration of institute's gelatin water solution is 0.1%～1%；Described suspension is 1:1～30 with the mass ratio of aqueous gelatin solution.
2. preparation method as claimed in claim 1, it is characterised in that in step (1), described PLGA molecular weight is 5000～50000dal, and the mol ratio of PLGA monomer lactic acid/hydroxyacetic acid is 75:25～50:50.
3. preparation method as claimed in claim 1, it is characterised in that in step (1), in described organic facies, the mass concentration of PLGA is 5%～15%.
4. preparation method as claimed in claim 1, it is characterised in that in step (2), described erinacine extractum is prepared as follows:
Hericium erinaceus (Bull. Ex Fr.) Pers. erinaceus mycelium powder is mixed with feed liquid mass ratio 1:20 with 95wt% ethanol, stand 1h, then at 60 DEG C, microwave extracting 25min under the conditions of 500w, then with petroleum ether extraction, collect raffinate, being extracted with ethyl acetate, collect extract, rotation is evaporated off ethyl acetate and obtains described erinacine extractum.
5. preparation method as claimed in claim 1, it is characterised in that in step (2), described ultrasonic power is 20～60KHz, and the time is 20～60min.
6. preparation method as claimed in claim 1, it is characterised in that in step (2), described erinacine extractum is 1:2～10 with the mass ratio that feeds intake of PLGA in step (1).
7. preparation method as claimed in claim 1, it is characterised in that in step (3), the mass concentration of institute's gelatin water solution is 0.5%.
8. preparation method as claimed in claim 1, it is characterised in that in step (3), described suspension is 1:10～25 with the mass ratio of aqueous gelatin solution.
9. preparation method as claimed in claim 1, it is characterised in that in step (3), the speed of described stirring and emulsifying is 600～1000rpm, and the time is 25～65min.
10. preparation method as claimed in claim 1, it is characterised in that in step (3), the speed with 150～300rpm stirs until dichloromethane volatilization is complete.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060093678A1 (en) * | 2002-12-19 | 2006-05-04 | Chickering Donald E Iii | Methods for making pharmaceutical formulations comprising deagglomerated microparticles |
| CN101773475A (en) * | 2010-01-14 | 2010-07-14 | 中国人民武装警察部队医学院 | Preparation method of capsicine micro spheres |
| CN104497059A (en) * | 2014-12-29 | 2015-04-08 | 浙江工业大学 | Efficient extraction method of total erinacine in hericium erinaceus mycelium |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060093678A1 (en) * | 2002-12-19 | 2006-05-04 | Chickering Donald E Iii | Methods for making pharmaceutical formulations comprising deagglomerated microparticles |
| CN101773475A (en) * | 2010-01-14 | 2010-07-14 | 中国人民武装警察部队医学院 | Preparation method of capsicine micro spheres |
| CN104497059A (en) * | 2014-12-29 | 2015-04-08 | 浙江工业大学 | Efficient extraction method of total erinacine in hericium erinaceus mycelium |
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