CN104257758A - Method for preparing melaleuca alternifolia volatile oil microcapsules and application thereof - Google Patents
Method for preparing melaleuca alternifolia volatile oil microcapsules and application thereof Download PDFInfo
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- CN104257758A CN104257758A CN201410550338.4A CN201410550338A CN104257758A CN 104257758 A CN104257758 A CN 104257758A CN 201410550338 A CN201410550338 A CN 201410550338A CN 104257758 A CN104257758 A CN 104257758A
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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)
- A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
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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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
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- C—CHEMISTRY; METALLURGY
- C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
- C11B—PRODUCING, e.g. BY PRESSING RAW MATERIALS OR BY EXTRACTION FROM WASTE MATERIALS, REFINING OR PRESERVING FATS, FATTY SUBSTANCES, e.g. LANOLIN, FATTY OILS OR WAXES; ESSENTIAL OILS; PERFUMES
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Abstract
The invention discloses a method for preparing melaleuca alternifolia volatile oil microcapsules and application thereof. The method comprises the following steps: dissolving beta-cyclodextrin and Arabic gum in water to form a wall material solution; stirring and adding an emulsifier monoglyceride and melaleuca alternifolia volatile oil in the solution, and homogenizing to obtain emulsified liquid; homogenizing the obtained emulsified liquid at high pressure and then spray-drying to obtain the melaleuca alternifolia volatile oil microcapsules. The method is simple and easy to operate, and the prepared microcapsules are high in stability, good in solubility and good in embedding rate. Pharmacodynamic evaluation proves that the microcapsules have significant effects of diminishing inflammation and alleviating pain and a wide application prospect.
Description
Technical field
The present invention is specifically related to a kind of preparation method and application thereof of Melaleuca Alternifolia volatile oil microcapsule.
Background technology
Melaleuca Alternifolia is a kind of plant of Fructus Rhodomyrti Melaleuca, and its fresh branch and leaf can extract quintessence oil, become tea tree oil, is the primary product of Melaleuca Alternifolia, can plays antibacterial, antipruritic effect, and effective to the treatment of skin burn.The domestic research about tea tree oil becomes increasingly active, and tentatively establishes the quality standard of China's tea tree oil.Tea tree oil has good broad-spectrum antibacterial health-care effect, and has pleasant Semen Myristicae fragrance, is generally acknowledged excellent natural aromatic agent, antibacterial, antiseptic, is mainly used in the industries such as daily use chemicals, pharmacy, food.But the rarely seen report of research of other pharmacological action of domestic relevant Melaleuca Alternifolia volatile oil.
Due to the high volatility of volatile oil, easily oxidized, cause it to preserve and use all being very restricted.Utilize microcapsule technology that Melaleuca Alternifolia volatile oil is carried out micro encapsulation, greatly can improve the stable of product, be convenient to storage and utilize.
Microcapsule technology is a kind of filmogen the technology of solid or the coated formation fine particle of liquid.To extensive concern in the fields such as pharmacy, food, agricultural chemicals, spice, feed additive and household chemicals, in recent years, microcapsule technology is one of focus attracted people's attention in high added value volatile oil product preparation field.Volatile oil, by after micro encapsulation, can reduce the volatilization of volatile oil, prevents the oxidation of photosensitive material, thus improves stability and the bioavailability of volatile oil.
Summary of the invention
The object of the present invention is to provide a kind of preparation method of Melaleuca Alternifolia volatile oil microcapsule and preparing the application had in the medicine of anti-inflammatory analgesic action.
The present invention completes by following technical solution:
(1) by W/W, by 50 ~ 60%
β-cyclodextrin and arabic gum are dissolved in the hot water of 70 DEG C, stir, and form wall material solution;
(2) joined while stirring in above-mentioned solution by the Melaleuca Alternifolia volatile oil of 2 ~ 4% emulsifying agent monoglycerides and 38 ~ 46%, make it dispersed, high pressure homogenize twice under the condition of pressure 20 ~ 30MPa, temperature 70 ~ 80 DEG C, each 5min, obtains emulsion;
(3) by gained emulsion under the condition of intake air temperature 180 ~ 200 DEG C, air outlet temperature 80 ~ 90 DEG C, atomizing pressure 0.2MPa ~ 0.5MPa, spraying dry, obtains Melaleuca Alternifolia volatile oil microcapsule.
Described in step (1)
βthe mass ratio of-cyclodextrin and arabic gum is 2:1.
The anti-inflammatory analgesic action research of Melaleuca Alternifolia volatile oil microcapsule:
A. antiinflammatory experiment (rat polyclonal antibodies)
Get male mice 50, body weight 18 ~ 22g, often organize 10, model group (edible soybean oil), positive controls (hydrocortisone, 25mg/kg), administration component is low dose group (100mg/kg), middle dosage group (200mg/kg) and high dose group (400mg/kg), after the reagent of difference lumbar injection 0.2mL variable concentrations, dimethylbenzene is coated with in mouse right ear, left ear maintains the original state, after 30min, de-neck is put to death, cut two ear 8mm card punch and lay round auricle at same position respectively, electronic balance precise weighing, only poor for swelling with left and right auricle weight, calculate suppression ratio:
Suppression ratio=(blank group average swelling-equal swelling of administration group product)/average swelling × 100% of blank group
Table 1 Melaleuca Alternifolia volatile oil microcapsule xylol cause mice auricle swelling impact (
± S)
| Group | Number of animals | Dosage (mg/kg) | Swelling (mg) | Ear swelling suppression ratio (%) |
| Model group | 10 | － | 12.89±1.89 | ? |
| Positive controls | 10 | 25 | 3.98±0.24 ▲▲ | 69.12 |
| Low dose group | 10 | 100 | 9.01±1.45 ▲ | 30.10 |
| Middle dosage group | 10 | 200 | 6.33±1.86 ▲▲ | 50.89 |
| High dose group | 10 | 400 | 4.24±1.21 ▲▲ | 67.11 |
Compare with blank group,
▲p < 0.05,
▲ ▲p < 0.01.
Shown by table 1 result, positive controls, administration group more all have obvious effect with model group, middle dosage group and high dose group have significant difference, all obviously can resist dimethylbenzene induced mice auricle edema, and the effect of the anti-inflammatory effects of high dose group and positive controls are suitable.
B. analgesic experiment (acetic acid causes mouse writhing reaction)
(1) experiment material
Animal: Kun Ming mice, body weight 22 ~ 26g, totally 50;
Equipment: syringe (1.0mL), balance
Medicine and reagent: 0.7% acetic acid (now joining), 0.9% sodium chloride injection, hydrochloric acid dolantin 2mg/mL, Melaleuca Alternifolia volatile oil microcapsule be configured to Graded amounts be 5,10, the medicinal liquid of 20mg/mL.
(2) Methods and steps
Random is a component group by test white mice by 10, and wherein one group is blank group, gives 0.9% sodium chloride injection by 0.2mL/10g body weight dose with lumbar injection; Positive controls gives aspirin by 60mg/kg dosage with lumbar injection.All the other are for giving the trial drug group of Melaleuca Alternifolia volatile oil microcapsule by various dose gradient gavage.The administration solvent of each gastric infusion group is 0.2ml/10g body weight.Successive administration 5 days, administration every day 1 time.Within 5th day, administration 20min pneumoretroperitoneum only injects 0.7% acetum 0.2mL/, after observed and recorded injection acetum in 20min the writhing response of every mice (abdominal part back leg is upheld, buttocks is raised) number of times, and adopt SPSS15.0 software to carry out statistical analysis, with mouse writhing response inhabitation rate evaluate efficacy to experimental result.
Suppression ratio %=(blank group writhing mean-medicine group writhing mean)/blank group writhing mean × 100%
(3) experimental result
Experimental result is as shown in table 2:
The table 2 Dichlorodiphenyl Acetate writhing method threshold of pain experiment impact (n=10,
± S)
| Group | Writhing number of times | Suppression ratio (%) |
| Blank group | 79.00±5.35 | ? |
| Aspirin group | 48.69±3.79 ** | 38.37 |
| Low dose group | 53.34±4.76 * | 32.48 |
| Middle dosage group | 47.64±6.24 ** | 39.70 |
| High dose group | 36.88±5.31 ** | 53.32 |
Note: compare with blank group,
*p < 0.05,
*p < 0.01.
The pain stimulation that mice can be caused more lasting after injection acetic acid, mice occurs that abdominal part back leg is upheld repeatedly, and hips up (writhing) is reacted.Result shows, and aspirin group, administration group compare with blank group, all have significant difference.Aspirin Dichlorodiphenyl Acetate induced mice writhing number of times obviously declines (P < 0.01), and clearly, its pain suppression ratio is 38.37% to analgesic activity.Melaleuca Alternifolia volatile oil microcapsule respectively organizes the mouse writhing reaction that all can reduce in various degree caused by acetic acid, have obvious analgesic activity, and in dose dependent, the effect of high dose group is better than aspirin group.
Preparation method of the present invention is simple, and prepared Microcapsules Size is even and embedding rate is higher, and product has good heat stability and dissolution dispersity, through pharmacodynamic evaluation, has the effect of obvious anti-inflammatory analgesic.
Further illustrate the present invention below in conjunction with detailed description of the invention, but the scope of protection of present invention is not limited to following embodiments.
detailed description of the invention:
Embodiment 1:
Be the 50g's of 2:1 by mass ratio
β-cyclodextrin and arabic gum are dissolved in the hot water of 70 DEG C, stir, and form wall material solution; Joined while stirring in above-mentioned solution by the Melaleuca Alternifolia volatile oil of 4g emulsifying agent monoglyceride and 46g, make it dispersed, high pressure homogenize twice under the condition of pressure 30MPa, temperature 70 C, each 5min, obtains emulsion; By gained emulsion under the condition of intake air temperature 180 DEG C, air outlet temperature 80 DEG C, atomizing pressure 0.5MPa, spraying dry, obtains Melaleuca Alternifolia volatile oil microcapsule, and its embedding rate is 96.4%.
Embodiment 2:
Be the 60g's of 2:1 by mass ratio
β-cyclodextrin and arabic gum are dissolved in the hot water of 70 DEG C, stir, and form wall material solution; Joined while stirring in above-mentioned solution by the Melaleuca Alternifolia volatile oil of 2g emulsifying agent monoglyceride and 38g, make it dispersed, high pressure homogenize twice under the condition of pressure 25MPa, temperature 75 DEG C, each 5min, obtains emulsion; By gained emulsion under the condition of intake air temperature 200 DEG C, air outlet temperature 90 DEG C, atomizing pressure 0.2MPa, spraying dry, obtains Melaleuca Alternifolia volatile oil microcapsule, and its embedding rate is 98.1%.
Embodiment 3:
Be the 55g's of 2:1 by mass ratio
β-cyclodextrin and arabic gum are dissolved in the hot water of 70 DEG C, stir, and form wall material solution; Joined while stirring in above-mentioned solution by the Melaleuca Alternifolia volatile oil of 3g emulsifying agent monoglyceride and 42g, make it dispersed, high pressure homogenize twice under the condition of pressure 20MPa, temperature 80 DEG C, each 5min, obtains emulsion; By gained emulsion under the condition of intake air temperature 190 DEG C, air outlet temperature 85 DEG C, atomizing pressure 0.3MPa, spraying dry, obtains Melaleuca Alternifolia volatile oil microcapsule, and its embedding rate is 95.2%.
Claims (3)
1. a preparation method for Melaleuca Alternifolia volatile oil microcapsule, is characterized in that, comprises the steps:
(1) by W/W, by 50 ~ 60%
β-cyclodextrin and arabic gum are dissolved in the hot water of 70 DEG C, stir, and form wall material solution;
(2) joined while stirring in above-mentioned solution by the Melaleuca Alternifolia volatile oil of 2 ~ 4% emulsifying agent monoglycerides and 38 ~ 46%, make it dispersed, high pressure homogenize twice under the condition of pressure 20 ~ 30MPa, temperature 70 ~ 80 DEG C, each 5min, obtains emulsion;
(3) by gained emulsion under the condition of intake air temperature 180 ~ 200 DEG C, air outlet temperature 80 ~ 90 DEG C, atomizing pressure 0.2MPa ~ 0.5MPa, spraying dry, obtains Melaleuca Alternifolia volatile oil microcapsule.
2., according to the preparation method of a kind of Melaleuca Alternifolia volatile oil microcapsule described in claim 1, it is characterized in that, described in step (1)
βthe mass ratio of-cyclodextrin and arabic gum is 2:1.
3. the Melaleuca Alternifolia volatile oil microcapsule obtained according to the method described in claim 1 or 2 is preparing the application had in the medicine of anti-inflammatory analgesic action.
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| CN201410550338.4A CN104257758A (en) | 2014-10-17 | 2014-10-17 | Method for preparing melaleuca alternifolia volatile oil microcapsules and application thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105385502A (en) * | 2015-12-10 | 2016-03-09 | 上海应用技术学院 | Preparation method of tea tree essential oil nano particle |
| CN113244296A (en) * | 2021-05-19 | 2021-08-13 | 中国中医科学院中药研究所 | Medicinal volatile oil composition and preparation method and application thereof |
-
2014
- 2014-10-17 CN CN201410550338.4A patent/CN104257758A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105385502A (en) * | 2015-12-10 | 2016-03-09 | 上海应用技术学院 | Preparation method of tea tree essential oil nano particle |
| CN105385502B (en) * | 2015-12-10 | 2019-12-03 | 上海应用技术学院 | A kind of preparation method of tea tree ethereal oil nanoparticle |
| CN113244296A (en) * | 2021-05-19 | 2021-08-13 | 中国中医科学院中药研究所 | Medicinal volatile oil composition and preparation method and application thereof |
| CN113244296B (en) * | 2021-05-19 | 2022-05-17 | 中国中医科学院中药研究所 | Medicinal volatile oil composition and preparation method and application thereof |
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Application publication date: 20150107 |