CN107669627A - A kind of Angelica grosseserrata volatile oil nano-emulsion and preparation method thereof - Google Patents
A kind of Angelica grosseserrata volatile oil nano-emulsion and preparation method thereof Download PDFInfo
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- CN107669627A CN107669627A CN201710830161.7A CN201710830161A CN107669627A CN 107669627 A CN107669627 A CN 107669627A CN 201710830161 A CN201710830161 A CN 201710830161A CN 107669627 A CN107669627 A CN 107669627A
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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)
- A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
- A61K36/232—Angelica
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
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Abstract
The invention discloses a kind of Angelica grosseserrata volatile oil nano-emulsion and preparation method thereof, represented with parts by weight, mainly by 30 ~ 50 parts of EL, 40,1 ~ 10 part of 1,2 propane diols, 1 ~ 10 part of Angelica grosseserrata volatile oil, enough distilled water compositions.The present invention screens the Angelica grosseserrata volatile oil nano-emulsion particle diameter prepared of Angelica grosseserrata volatile oil nano-emulsion prescription between 10~100 nm by drawing pseudo-ternary phase diagram, has good stability；Gained nano-emulsion is oil-in-water type nano-emulsion, can use water infinite dilution, and under transmission electron microscope, nano-emulsion is rounded, without being adhered.Detected through transmission electron microscope, for droplet diameter distribution between 10~100 nm, outward appearance is yellow or colourless transparent liquid, is had good stability.
Description
Technical field
The present invention relates to nano-emulsion preparation field, in particular to a kind of Angelica grosseserrata volatile oil nano-emulsion and preparation method thereof.
Background technology
Nanoemulsions（nanoemulsion）Also known as microemulsion（microemulsion）, it is by water, oil, EL-40 and 1,2-
Propane diols etc. spontaneously forms, and particle diameter is 1~100nm Thermodynamically stable, isotropism, transparent or semitransparent homogeneous dispersion
Be in general, nano-emulsion is divided into three types, i.e. oil-in-water type nano-emulsion (O/W), water-in-oil type nanoemulsion (W/O and double
Continuous type nano-emulsion (B.C), nineteen forty-three are found and report this dispersion first by Hoar and Schulman.Until 1959
Year, Schulman just proposes " microemulsion " this concept.Hereafter, the theory of nano-emulsion and application study obtain fast
The development of speed.At present, nanometer emulsified technology has penetrated into daily-use chemical industry, fine chemistry industry, petrochemical industry, material science, biological skill
The field such as art and environmental science, turn into the current research field in the world with huge applications potentiality.
Nano-emulsion has the advantages of many other preparations are incomparable：1. being isotropic transparency liquid, belong to thermodynamics
Systems stabilisation, it can not be allowed to be layered through pressure sterilizing or centrifugation；2. technique is simple, preparation process is not required to special installation, can be certainly
Hair is formed, and nano-emulsion particle diameter is generally 1~100nm；3. viscosity is low, pain during injection can be reduced；4. with sustained release and targeting
Effect；5. improving the solubility of medicine, the enzymolysis of medicine in vivo is reduced, the protective effect to medicine can be formed and improve stomach and intestine
Absorption of the road to medicine, improve the bioavilability of medicine.Therefore nano-emulsion is widely paid close attention to as a kind of pharmaceutical carrier.
Angelica grosseserrata volatile oil（Rifaximin）, it is Ryfamycin derivative, is semi-synthetic antibiotic, is first non-ammonia
Base glucoside enteron aisle antibiotic.Its has a broad antifungal spectrum, antibacterial action are strong, compared with other intestines and stomach antibiotic, are orally not easy by intestines
Road absorbs, and toxic side effect is extremely low, there is higher concentration in enteron aisle, to a variety of Grain-positives, gram negative aerobic bacteria and anaerobic bacteria
There is height antibacterial activity.But the solubility of Angelica grosseserrata volatile oil and stability have been short of, in terms of clinical application is carried out,
By very big restriction.
The content of the invention
It is an object of the invention to provide a kind of effective Angelica grosseserrata volatile oil nano-emulsion for improving Angelica grosseserrata volatile oil stability.
It is another object of the present invention to provide the preparation method of above-mentioned Angelica grosseserrata volatile oil nano-emulsion.
The present invention is achieved through the following technical solutions：A kind of Angelica grosseserrata volatile oil nano-emulsion, is represented with parts by weight, mainly by 30
~ 50 parts of EL-40,1 ~ 10 part of 1,2-PD, 1 ~ 10 part of Angelica grosseserrata volatile oil, enough distilled water compositions.
In order to which the present invention is better achieved, further, represented with parts by weight, the EL-40 is 32 parts, 1,2-PD
It it is 8 parts for 3 parts, Angelica grosseserrata volatile oil, and distilled water is 57 parts.
A kind of preparation method of above-mentioned Angelica grosseserrata volatile oil nano-emulsion, comprises the following steps：
（1）EL-40, Angelica grosseserrata volatile oil are added in four-hole boiling flask, stirring makes it well mixed；
（2）Four-hole boiling flask is fixed under water bath condition, water temperature is maintained at 40 ~ 60 DEG C, after raw material fully melts, starts stirring
Device, mixing speed are 150 ~ 200rpm；
（3）After material temperature in four-hole boiling flask up to after 40 ~ 60 DEG C, stop stirring, add oil, 1,2-PD, continue to stir, hold
Continuous 30min；
（4）Stop stirring, 40 ~ 60 DEG C of hot distilled waters are added dropwise with rubber head dropper, after 3 ~ 8h is added dropwise to complete, 1h is incubated in 40 ~ 60 DEG C；
（5）Heating water bath is closed, after being cooled to normal temperature, adds bactericide, continues to stir 30min；
（6）After 5 ~ 10 DEG C being cooled to using cold bath, filtering and discharging.
In order to which the preparation of nano-emulsion in the present invention is better achieved, further, the stirring used in the preparation process
Device is magnetic stirring apparatus.
In order to which the preparation of nano-emulsion in the present invention is better achieved, further, the step（4）In, thermal distillation is added dropwise
Water uses rubber head dropper.
In order to which the preparation of nano-emulsion in the present invention is better achieved, further, the step（4）In, thermal distillation is added dropwise
The process of water is that a drop is added dropwise in every 3 ~ 4min, per 2 ~ 3ml of dropper.
The present invention compared with prior art, has advantages below and beneficial effect：
（1）The Angelica grosseserrata volatile oil nanometer that the present invention screens Angelica grosseserrata volatile oil nano-emulsion prescription and prepared by drawing pseudo-ternary phase diagram
Milk particle footpath has good stability between 10~100 nm；
（2）It is oil-in-water type nano-emulsion that the present invention, which prepares gained nano-emulsion, can use water infinite dilution, under transmission electron microscope, nano-emulsion
Rounded, nothing is adhered.Average grain diameter（Z-Average）For 13.2 nm, polydispersity coefficient（PDI）For 0.232.At 25 DEG C,
The average zeta current potentials of Angelica grosseserrata volatile oil nano-emulsion after 5 times of dilution are（-11.2±0.1）MV, with thermostatic accelerated experiment result
Collectively show that its have good stability.
Embodiment
The present invention is described in further detail with reference to embodiment, but the implementation of the present invention is not limited to this,
Without departing from the idea case in the present invention described above, according to ordinary skill knowledge and customary means, various replace is made
Change and change, all should be included within the scope of the invention.
Embodiment：
The Angelica grosseserrata volatile oil nano-emulsion of the present embodiment, as mass fraction,：w（Angelica grosseserrata volatile oil）=8%, w（EL-40）=32%,
w（1,2-PD）=3%, w（Distilled water）= 57%.
Its preparation method, comprise the following steps：
（1）EL-40, Angelica grosseserrata volatile oil are added in four-hole boiling flask, stirring makes it well mixed；
（2）Four-hole boiling flask is fixed under water bath condition, water temperature is maintained at 40 ~ 60 DEG C, after raw material fully melts, starts stirring
Device, mixing speed are 150 ~ 200rpm；
（3）After material temperature in four-hole boiling flask up to after 40 ~ 60 DEG C, stop stirring, add oil, 1,2-PD, continue to stir, hold
Continuous 30min；
（4）Stop stirring, 40 ~ 60 DEG C of hot distilled waters are added dropwise with rubber head dropper, after 3 ~ 8h is added dropwise to complete, 1h is incubated in 40 ~ 60 DEG C；
（5）Heating water bath is closed, after being cooled to normal temperature, adds bactericide, continues to stir 30min；
（6）After 5 ~ 10 DEG C being cooled to using cold bath, filtering and discharging.
The present embodiment screens prescription, and it is carried out using Angelica grosseserrata volatile oil as reagent thing by drawing pseudo-ternary phase diagram
Quality evaluation.Differentiate the type of nano-emulsion with decoration method, form is investigated with transmission electron microscope, with Zetasizer Nano
ZS analyzers and photon correlation spectroscopy measure particle diameter and polydispersity coefficient, after by thermostatic accelerated experiment examine its stable
Property, finally study its in-vitro percutaneous drug release effect on mouse skin.
Angelica grosseserrata volatile oil has special absworption peak at 283 nm, and noiseless with nano-emulsion matrix absworption peak, establishes levisticum
Volatile oil content testing regression equation is y=0.17444x+0.27391（r 2 =0.99476）.Angelica grosseserrata volatile oil nano-emulsion formula
Middle no azone and the apparent transdermal coefficient that azone content is 2% and 5%（Kp×10 -3 ）Respectively 14.907 ± 0.014,
15.026 ± 0.005 and 10.382 ± 0.017 cmh -1, and the apparent transdermal system of the ethanol solution of Angelica grosseserrata volatile oil 20%
Number（Kp×10 -3 ）It is（4.628±0.063）Cmh -1, illustrate that the transdermal effect of Angelica grosseserrata volatile oil nano-emulsion is better than it
Ethanol solution, and significant difference（P<0.01）, its be formulated in without transdermal enhancer azone.
Embodiment 2：
It is equal further to limit the agitator used in the preparation process in order to preferably realize the preparation of nano-emulsion for the present embodiment
For magnetic stirring apparatus.The present embodiment other parts are same as the previously described embodiments, repeat no more here.
Embodiment 3：
The present embodiment further limits the step to preferably realize the preparation of nano-emulsion（4）In, hot distilled water, which is added dropwise, to be made
It is rubber head dropper.The present embodiment other parts are same as the previously described embodiments, repeat no more here.
Embodiment 4；
The present embodiment further limits the step to preferably realize the preparation of nano-emulsion（4）In, hot distilled water is added dropwise
Process is that a drop is added dropwise in every 3 ~ 4min, per 2 ~ 3ml of dropper.The present embodiment other parts are same as the previously described embodiments, here no longer
Repeat.
Although an embodiment of the present invention has been shown and described, it will be understood by those skilled in the art that：Not
A variety of change, modification, replacement and modification can be carried out to these embodiments by departing under the principle and objective of the present invention, of the invention
Scope is limited by claim and its equivalent.
Claims (6)
- A kind of 1. Angelica grosseserrata volatile oil nano-emulsion, it is characterised in that：Represented with parts by weight, mainly by 30 ~ 50 parts of EL-40,1 ~ 10 part 1,2-PD, 1 ~ 10 part of Angelica grosseserrata volatile oil, enough distilled water compositions.
- A kind of 2. Angelica grosseserrata volatile oil nano-emulsion according to claim 1, it is characterised in that：Represented with parts by weight, the EL- 40 be 32 parts, 1,2-PD is 3 parts, Angelica grosseserrata volatile oil is 8 parts, and distilled water is 57 parts.
- 3. the preparation method of a kind of Angelica grosseserrata volatile oil nano-emulsion according to claim 1 or claim 2, it is characterised in that including following Step：（1）EL-40, Angelica grosseserrata volatile oil are added in four-hole boiling flask, stirring makes it well mixed；（2）Four-hole boiling flask is fixed under water bath condition, water temperature is maintained at 40 ~ 60 DEG C, after raw material fully melts, starts stirring Device, mixing speed are 150 ~ 200rpm；（3）After material temperature in four-hole boiling flask up to after 40 ~ 60 DEG C, stop stirring, add oil, 1,2-PD, continue to stir, hold Continuous 30min；（4）Stop stirring, 40 ~ 60 DEG C of hot distilled waters are added dropwise with rubber head dropper, after 3 ~ 8h is added dropwise to complete, 1h is incubated in 40 ~ 60 DEG C；（5）Heating water bath is closed, after being cooled to normal temperature, adds bactericide, continues to stir 30min；（6）After 5 ~ 10 DEG C being cooled to using cold bath, filtering and discharging.
- A kind of 4. Angelica grosseserrata volatile oil nano-emulsion according to claim 3, it is characterised in that：Used in the preparation process Agitator is magnetic stirring apparatus.
- A kind of 5. Angelica grosseserrata volatile oil nano-emulsion according to claim 3 or 4, it is characterised in that：The step（4）In, drop Heating distilled water uses rubber head dropper.
- A kind of 6. Angelica grosseserrata volatile oil nano-emulsion according to claim 5, it is characterised in that：The step（4）In, heat is added dropwise The process of distilled water is that a drop is added dropwise in every 3 ~ 4min, per 2 ~ 3ml of dropper.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201710830161.7A CN107669627A (en) | 2017-09-15 | 2017-09-15 | A kind of Angelica grosseserrata volatile oil nano-emulsion and preparation method thereof |
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| CN201710830161.7A CN107669627A (en) | 2017-09-15 | 2017-09-15 | A kind of Angelica grosseserrata volatile oil nano-emulsion and preparation method thereof |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102327215A (en) * | 2011-09-25 | 2012-01-25 | 西北农林科技大学 | Medecamycin nanoemulsion antibacterial drug and preparation method thereof |
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- 2017-09-15 CN CN201710830161.7A patent/CN107669627A/en not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102327215A (en) * | 2011-09-25 | 2012-01-25 | 西北农林科技大学 | Medecamycin nanoemulsion antibacterial drug and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 周莹: "独活挥发油纳米乳的制备及其体外透皮试验", 《畜牧与兽医》 * |
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Application publication date: 20180209 |