CN102397405A - Compound bergamot oil nano-emulsion composition and preparation method thereof - Google Patents

Compound bergamot oil nano-emulsion composition and preparation method thereof Download PDF

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CN102397405A
CN102397405A CN2011103844111A CN201110384411A CN102397405A CN 102397405 A CN102397405 A CN 102397405A CN 2011103844111 A CN2011103844111 A CN 2011103844111A CN 201110384411 A CN201110384411 A CN 201110384411A CN 102397405 A CN102397405 A CN 102397405A
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oil
bergamot oil
emulsion composition
bergamot
compound recipe
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欧阳五庆
郑星星
郭建军
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Northwest A&F University
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Abstract

The invention discloses a compound bergamot oil nano-emulsion composition, which is characterized in that: the granularity of the nano-emulsion is 1nm to 100nm, and comprises the following substances by weight mass: 23 to 35 percent of surface active agent, 0.3 to 8 percent of cosurfacant, 1.5 to 10 percent of bergamot oil, 0.5 to 5.5 percent of patchouli, 0.4 to 4.5 percent of tea tree oil, 0.3 to 2.2 percent of pennyroyal and distilled water, wherein the sum of the mass percentage of the ingredients is 100 percent. The compound bergamot oil nano-emulsion composition is broad-spectrum antimicrobic, has good treatment effect on eczema, psoriasis, herpes, dermatitis, blain, wound, acne, urinary infection and the like, the permeability is strong, the stability is good, content of active ingredients is high, transdermal absorption effect is remarkable, action time is durable, the preparation method is simple and is easy to popularize and use, and the medicine has vast application prospect on the medical market.

Description

A kind of compound recipe bergamot oil nano emulsion composition and preparation method thereof
Technical field
The invention belongs to field of medicaments, relate to a kind of compound recipe bergamot oil nano emulsion composition and preparation method thereof with treatment eczema, chronic eczema, dermatitis, pustule, wound, acne, urinary tract infection.
Background technology
Antibacterials play a part very important in the control human infectious disease, and the antibacterials of usefulness mainly contain Western medicine clinically at present, but along with it is widely used, the bacterial drug resistance problem has become very important problem.Because new drug development relatively lags behind, the mankind are being faced with " antibacterials crisis ".Plant is the natural treasure-house of bioactive compound, has the natural product of antibacterial activity because untoward reaction is few, and safety has no side effect, and has become the focus that people pay close attention at present.
Summary of the invention
To problem that exists in the above-mentioned prior art and defective, the object of the present invention is to provide a kind of compound recipe bergamot oil nano emulsion composition with treatment eczema, chronic eczema, dermatitis, pustule, wound, acne, urinary tract infection, this nano emulsion composition permeability is strong; Good stability; Active constituent content is high, and the Transdermal absorption effect is remarkable, and action time is lasting; And method for preparing is simple, and is easy to utilize.
The technical method of realizing the foregoing invention purpose is a kind of compound recipe bergamot oil nano emulsion composition, is made up of the material of following mass percent:
Surfactant 23.0%~35.0%, cosurfactant 0.3%~8.0%, bergamot oil 1.5%~10.0%, patchouli oil 0.5%~5.5%, tea tree oil 0.4%~4.5%, Oleum menthae 0.3%~2.2%, surplus are distilled water, and the mass percent sum of above-mentioned substance is 100%.
The formula optimization mass percent of preparation medicine of the present invention is: surfactant 25.6%~32.9%,
Cosurfactant 0.7%~6.4%, bergamot oil 3.5%~8.5%, patchouli oil 0.8%~4.3%, tea tree oil 0.7%~3.8%, Oleum menthae 0.4%~1.7%, surplus are distilled water, and the mass percent sum of above-mentioned substance is 100%.
The prescription best in quality percentage ratio of preparation medicine of the present invention is: RH-40 29.2%, dehydrated alcohol
4.1%, bergamot oil 7.5%, patchouli oil 2.2%, tea tree oil 2.0%, Oleum menthae 0.8%, distilled water 54.2%.
Described surfactant is polyoxyethylene ether Oleum Ricini (EL-40), polyoxyethylene (40) hydrogenation
The mixture of one or more in Oleum Ricini (RH-40) and the tween 80.
Described cosurfactant is a dehydrated alcohol, 1, the mixture of one or more in 2-propylene glycol, glycerin and the Macrogol 600.
On surfactant selection, the present invention selects the nonionic surfactant of avirulence and good biocompatibility for use.Nonionic surfactant is more stable in solution, is not subject to the influence of strong electrolyte, inorganic salts, also is not subject to the influence of soda acid, and good with the compatibility of other surfactants, haemolysis is less.In theory; The HLB value that the preparation of O/W type nanometer emulsion needs surfactant is between 8~18; Consider preparation technology's simplicity; Be the easy formation property of nano-emulsion and the stability of nano-emulsion, the present invention selects the liquid nonionic surfactant of HLB between 10~15 for use, and is perhaps composite with the nonionic surfactant of a kind of HLB<10.Available surfactant has: one or more mixture in EL-40, RH-40 and the tween 80.
The HLB value of common emulsifying agent can be found in some chemical industry handbooks, like " the chemical products handbook of chemical industry publication.Because hydrophile-lipophile balance (HLB) value of surfactant has additive properties, the available quality averaging method is obtained the HLB value of surfactant.For example, after two kinds of surfactant A, B mix, the hydrophile-lipophile balance value HLB of its mixed surfactant ABValue does
HLB AB=(W A?×HLB A+W B?×HLB B)/(W A+W B)
WA in the formula, the quality of WB-mixed surfactant A, B;
HLBA, the HLB value of HLBB-surfactant A, B.
In the selection of cosurfactant; The HLB of cosurfactant ability reconciliation statement surface-active agent; And can reduce oil water interfacial tension; Nano-emulsion multiselect short chain alcohol and medium chain alcohol are cosurfactant, and the cosurfactant that the present invention selects for use is a dehydrated alcohol, 1, any in 2-propylene glycol, glycerin and the Macrogol 600 or several kinds of mixture.
This Fructus Citri Sarcodactylis (Bergamot) formal name used at school (Citrus medica L. Va) that invention is selected for use is the mutation of Rutaceae (Rataceal) orange Fructus Citri, and bergamot oil is to get from the peel squeezing of Fructus Citri Sarcodactylis, and taste is pure and fresh, has a little the fragrance of a flower.Bergamot oil has stronger spectrum antibacterial activity, and each bacterioid, epidermis fungus are all had inhibitory action, and is all effective in cure to the seborrheic dermatitis of eczema, chronic eczema, acne, scabies, wound, bubble rash, skin and scalp; Be good urethra antibacterial, can improve cystitis; Good the intestines and stomach antibacterial is driven away intestinal parasite, and is obviously eliminated cholelithiasis.
The patchouli oil that this invention is selected for use is the volatile oil of extraction from Labiatae thorn stamen grass platymiscium Herba Pogostemonis (pogostemon cablin Banth); Aspect the skin curative effect; Mainly be used for promoting the wound stammerer; The prevention inflammation promotes cell metabolism, to cicatrix, burn, dermatitis, decubital ulcer, bacterial infection, pustule, eczema, psoriasis, tinea pedis etc. have better curative effect.
The tea tree oil that this invention is selected for use is the pure natural plant quintessence oil that from the wood Myrtaceae Folium Melaleucae Leucadendrae of port, extracts with distillatory mode, and the wide spectrum antimicrobial is a kind of natural disinfectant, has very great help for treatment numerous disease, wound.Like incised wound, scratch, by insect bite, acne, burn, vaginal infection, tinea etc.It also is used to control antibacterial and mycete in the air conditioning system.
The Oleum menthae band that this invention is selected for use is pungent and refrigerant, and intensive scurrying property is arranged, and is mainly used in skin or mucosa and produces refrigerant sense to alleviate discomfort, main pain.
A further object of the invention is to provide the method for above-mentioned compound recipe bergamot oil nano emulsion composition, comprises the following steps:
1) by formula proportion take by weighing surfactant, cosurfactant, bergamot oil, patchouli oil,
Tea tree oil, Oleum menthae, distilled water, subsequent use;
2) bergamot oil, patchouli oil, tea tree oil and the Oleum menthae with said amount stirs, as oil phase;
3) surfactant and the cosurfactant with said amount joins mixing in the oil phase;
4) with distilled water as water, at room temperature stir oil phase rapidly, slowly drip water in the time of stirring, constantly stir and be transparent liquid until system, promptly get compound recipe bergamot oil nano emulsion composition.
Compound recipe bergamot oil nano emulsion composition of the present invention has the effect of treatment eczema, chronic eczema, dermatitis, pustule, wound, acne.Usage: perhaps directly smear each 0.1mL/cm according to the oral each 0.25g of the state of an illness at skin surface 2
The present invention detects through transmission electron microscope, and droplet diameter distribution is between 1~100nm, and outward appearance is yellow or colourless transparent liquid, has good stability:
1. ageing stability
Ageing stability is meant that outward appearance in time when nanometer emulsion oral liquid was preserved under room temperature nature change condition
The degree that prolongs and change.This compound recipe bergamot oil nano emulsion composition is transparent lastingly, does not find muddy or deposition, explains that its ageing stability is good.
2. heat storage stability
This compound recipe bergamot oil nano emulsion composition is placed test tube, and sealing places 37 ℃ of waters bath with thermostatic control
Stored 14 days in the case, this liquid appearance after storage is transparent.
3. anti-freeze-stable property
This compound recipe bergamot oil nano emulsion composition in-4 ℃ of one weeks of preservation, is returned to room temperature after the taking-up.This compound recipe bergamot oil nano emulsion composition becomes solid in the time of-4 ℃, return to after the room temperature it and return to transparently, and places after a week still transparently, explains that this nanometer emulsion freezing-resistance is good.
4. accelerated stability
This compound recipe bergamot oil nano emulsion composition is placed test tube, and sealing is in the centrifugal 20min of 15000r/min, not layering, still clear.
Compound recipe bergamot oil nano emulsion composition of the present invention compared with prior art has the following advantages:
1) thermodynamic stability is good, and bin stability is high, put for a long time not stratified, through centrifugal acceleration test layering not yet;
2) the invention belongs to nano-grade medicine, the outward appearance clear, the emulsion droplet dispersion is good, and any inhomogeneities or precipitate all are prone to come to light, and sensible quality improves;
3) applied range, all effective to treating various scytitiss, urinary tract infection, vaginal infection;
4) active constituent content is high, and the Transdermal absorption effect is remarkable, and bioavailability is high, and safety has no side effect;
5) preparation technology is simple, and is safe, easy to utilize.
The specific embodiment
Below come further to set forth the beneficial effect of medicine according to the invention through pharmacodynamics test and contrast test.
Test Example 1The antibacterial activity in vitro test of compound recipe bergamot oil nano emulsion composition
Difference inoculated and cultured escherichia coli, staphylococcus aureus, bacillus subtilis, yeast, Candida albicans, Cryptococcus histolyticus (above strain provides by my school Microbiological Lab) on different culture medium; Slowly on culture medium, drip compound recipe bergamot oil nano emulsion composition and each 5ml of blank nano-emulsion of 1%, 3%, 6%, 9% after cultivating 24h at 37 ℃; After cultivating 12h; Observe antibacterial situation, result such as table 1:
The antibacterial activity in vitro test of table 1 compound recipe bergamot oil nano emulsion composition
The effect of the compound recipe bergamot oil nano-emulsion of
Figure 202108DEST_PATH_IMAGE001
variable concentrations
test strain 1% 3% 6% 9% blank nano-emulsions
escherichia coli gold++++-
Staphylococcus aureus++++-
Bacillus subtilis++++-
Yeast++++-
Candida albicans++++-
Cryptococcus histolyticus++++-
Figure 296469DEST_PATH_IMAGE003
annotates: "-" expression is invalid, and "+" expression effectively.
 
Test Example 2The external comparative efficacy test of compound recipe bergamot oil nano emulsion composition and other drug preparation
On different culture medium, inoculate escherichia coli, staphylococcus aureus, yeast, Candida albicans, Cryptococcus histolyticus (above strain provides by my school Microbiological Lab) respectively, after 4 days, make concentration respectively and be approximately 5 * 10 37 ℃ of cultivations 6~9 * l0 6The bacteria suspension of CFU/mL is evenly coated experiment with the culture medium flat plate surface with bacteria suspension.Punch on the culture medium of card punch after being coated with bacterium with diameter 6mm, respectively 10% compound ketoconazole ointment, 10% amikacin injection, 6% compound recipe bergamot oil nanoemulsions are added in the hand-hole, make ointment concordant with bore edges and fully contact.32 ℃ observe each hole after cultivating 6 days around inhibition zone size and write down its diameter mm value, the result is as shown in table 2 below:
Table 2 Compound recipe bergamot oil nano emulsion composition and compound ketoconazole ointment, amikacin injection
Average diameter of inhibition zone is (mm) relatively
Figure 127284DEST_PATH_IMAGE004
Can find out that from table 2 fungistatic effect of compound recipe bergamot oil nano emulsion composition is obviously because compound ketoconazole ointment and amikacin injection.
Test Example 3The skin irritation test
Choose 6 of the new zealand rabbits of healthy no skin injury, body weight 2.6 ± 0.3kg is divided into two groups; Every group 3; 24h gives the skin depilatory of tame rabbit back center spine post both sides before test, and every side depilation district is to be advisable about 2cm * 3cm, and a side baring skin is coated with compound recipe bergamot oil nano-emulsion 0.4g; And the covering gauze, fix with adhesive tape; Opposite side skin is coated with the equivalent distilled water and compares, and the drug of topical application time is 4h.Behind coating 4 h, clean coating position, both sides, tried 1,24 behind the thing, 48h, observe coating position, both sides dermoreaction respectively at removing with warm saline.The result shows, tried rabbit administration 4h after, not show speckle or edema of both sides skin in each observation period is 0 to the integrated value of skin irritation reaction, shows that this compound recipe bergamot oil nano emulsion composition has no stimulation to local skin.
Test Example 4Compound recipe bergamot oil nano emulsion composition and other preparation for treating eczema effect comparison tests
Choosing suffers from patient 90 people of eczema symptom clinically; Be divided into three groups at random; Give compound dexamethason acetate ointment, folk prescription bergamot oil nano-emulsion and compound recipe bergamot oil nano emulsion composition respectively, patient every day be applied in the affected part three times, 1 week the back observe therapeutic effect.Produce effects 8 examples in compound dexamethason acetate ointment group 30 examples as a result, effective 13 examples, invalid 9 examples, obvious effective rate 26.7%, total effective rate 70%; Produce effects 7 examples in folk prescription bergamot oil nano-emulsion group 30 examples, effective 11 examples, invalid 12 examples, obvious effective rate 23.3%, total effective rate 60%; Produce effects 11 examples in compound recipe bergamot oil nano-emulsion group 30 examples, effective 14 examples, invalid 5 examples, obvious effective rate 36.7%, effective percentage 83.3%.Therefore, the treatment eczema effect that can find out compound recipe bergamot oil nano emulsion composition obviously is superior to compound dexamethason acetate ointment and folk prescription bergamot oil nano-emulsion.
Embodiment 1
1) take by weighing RH-40 29.2g, dehydrated alcohol 4.1g, bergamot oil 7.5g, patchouli oil 2.2g, tea tree oil 2.0g, Oleum menthae 0.8g, distilled water 54.2g, subsequent use;
2) bergamot oil, patchouli oil, tea tree oil and Oleum menthae are stirred, as oil phase;
3) RH-40 and dehydrated alcohol are joined mixing in the oil phase;
4) with distilled water as water, at room temperature stir oil phase rapidly, slowly drip water in the time of stirring, constantly stir and be transparent liquid until system, promptly get compound recipe bergamot oil nano emulsion composition.
Embodiment 2
By RH-40 28.9g, 1,2-propylene glycol 4.2g, bergamot oil 8.3g, patchouli oil 1.8g, tea tree oil 1.6g, Oleum menthae 0.7g, distilled water 54.5g form.
Embodiment 3
Form by EL-40 30.5g, dehydrated alcohol 2.7g, bergamot oil 5.8g, patchouli oil 1.6g, tea tree oil 1.9g, Oleum menthae 0.4g, distilled water 57.1g.
Embodiment 4
Form by tween 80 32.9g, glycerin 1.2g, bergamot oil 3.5g, patchouli oil 1.4g, tea tree oil 1.2g, Oleum menthae 0.4g, distilled water 59.4g.
Embodiment 5
Form by RH-40 33.4g, Macrogol 600 0.7g, bergamot oil 3.7g, patchouli oil 0.8g, tea tree oil 0.7g, Oleum menthae 0.3g, distilled water 60.4g.
Embodiment6
Form by RH-40 29.8g, dehydrated alcohol 2.9g, bergamot oil 6.8g, patchouli oil 2.2g, tea tree oil 1.5g, Oleum menthae 0.7g, distilled water 56.1g.
Embodiment 7
By EL-40 25.6g, 1,2-propylene glycol 5.9g, bergamot oil 8.5g, patchouli oil 3.8g, tea tree oil 3.0g, Oleum menthae 1.7g, distilled water 51.5g form.
Embodiment 8
Form by RH-40 26.3g, dehydrated alcohol 3.9g, bergamot oil 7.7g, patchouli oil 4.3g, tea tree oil 3.8g, Oleum menthae 1.3g, distilled water 52.7g.
Embodiment 9
Form by tween 80 31.5g, dehydrated alcohol 1.6g, bergamot oil 4.2g, patchouli oil 2.0g, tea tree oil 1.6g, Oleum menthae 0.4g, distilled water 58.7g.
Embodiment 10
Form by RH-40 30.2g, glycerin 3.7g, bergamot oil 8.3g, patchouli oil 1.7g, tea tree oil 1.6g, Oleum menthae 0.8g, distilled water 53.7g.
Embodiment 11
Form by RH-40 28.6g, dehydrated alcohol 3.3g, bergamot oil 7.2g, patchouli oil 3.7g, tea tree oil 3.5g, Oleum menthae 1.8g, distilled water 51.9g.

Claims (5)

1. a compound recipe bergamot oil nano emulsion composition is characterized in that, is made up of the material of following mass percent:
Surfactant 23.0%~35.0%, cosurfactant 0.3%~8.0%, bergamot oil 1.5%~10.0%, patchouli oil 0.5%~5.5%, tea tree oil 0.4%~4.5%, Oleum menthae 0.3%~2.2%, surplus are distilled water, and the mass percent sum of mentioned component is 100%;
Described surfactant is polyoxyethylene ether Oleum Ricini, polyoxyethylene ether 40 hydrogenations
The mixture of one or more in Oleum Ricini and the tween 80;
Described cosurfactant is a dehydrated alcohol, 1, the mixture of one or more in 2-propylene glycol, glycerin and the Macrogol 600.
2. compound recipe bergamot oil nano emulsion composition according to claim 1 is characterized in that, is made up of the material of following mass percent:
Surfactant 25.6%~32.9%, cosurfactant 0.7%~6.4%, bergamot oil 3.5%~
8.5%, patchouli oil 0.8%~4.3%, tea tree oil 0.7%~3.8%, Oleum menthae 0.4%~1.7%, surplus are distilled water, and the mass percent sum of mentioned component is 100%.
3. a compound recipe bergamot oil nano emulsion composition is characterized in that, is made up of the raw material of following component:
RH-40 29.2%, dehydrated alcohol 4.1%, bergamot oil 7.5%, patchouli oil 2.2%, tea tree oil 2.0%, Oleum menthae 0.8%, distilled water 54.2%.
4. compound recipe bergamot oil nano emulsion composition according to claim 1 is characterized in that the particle diameter of this nano-emulsion is between 1~100nm.
5. prepare the method for the said compound recipe bergamot oil of claim 1 nano emulsion composition, it is characterized in that, comprise the following steps:
1) by formula proportion take by weighing surfactant, cosurfactant, bergamot oil, patchouli oil,
Tea tree oil, Oleum menthae, distilled water, subsequent use;
2) bergamot oil, patchouli oil, tea tree oil and the Oleum menthae with said amount stirs, as oil phase;
3) surfactant and the cosurfactant with said amount joins mixing in the oil phase;
4) with distilled water as water, at room temperature stir oil phase rapidly, slowly drip water in the time of stirring, constantly stir and be transparent liquid until system, promptly get compound recipe bergamot oil nano emulsion composition.
CN2011103844111A 2011-11-28 2011-11-28 Compound bergamot oil nano-emulsion composition and preparation method thereof Pending CN102397405A (en)

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103301038A (en) * 2013-06-14 2013-09-18 张晓燕 Tea tree oil nanoemulsion and preparation method thereof
CN104940361A (en) * 2015-06-04 2015-09-30 青岛大学附属医院 Anti-acne paste and preparation method thereof
CN105796640A (en) * 2016-04-19 2016-07-27 田春燕 Traditional Chinese medicine composition and preparation with acne treatment function
CN114214117A (en) * 2021-12-13 2022-03-22 云南中烟工业有限责任公司 Method for improving release balance of limonene in bergamot oil essence

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1931232A (en) * 2006-09-21 2007-03-21 西北农林科技大学 Oil-in-water nanometer perilla seed oil emulsion oral liquid and its prepn process

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1931232A (en) * 2006-09-21 2007-03-21 西北农林科技大学 Oil-in-water nanometer perilla seed oil emulsion oral liquid and its prepn process

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103301038A (en) * 2013-06-14 2013-09-18 张晓燕 Tea tree oil nanoemulsion and preparation method thereof
CN104940361A (en) * 2015-06-04 2015-09-30 青岛大学附属医院 Anti-acne paste and preparation method thereof
CN104940361B (en) * 2015-06-04 2018-05-29 青岛大学附属医院 A kind of Whelk-eliminating paste and preparation method thereof
CN105796640A (en) * 2016-04-19 2016-07-27 田春燕 Traditional Chinese medicine composition and preparation with acne treatment function
CN114214117A (en) * 2021-12-13 2022-03-22 云南中烟工业有限责任公司 Method for improving release balance of limonene in bergamot oil essence
CN114214117B (en) * 2021-12-13 2023-09-15 云南中烟工业有限责任公司 Method for improving limonene release balance in bergamot oil essence

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Application publication date: 20120404