CN107157921A - Aescinate A, B lipidosome gels and preparation method thereof - Google Patents
Aescinate A, B lipidosome gels and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a kind of Aescinate A, B lipidosome gels, it is made up of compositions such as Aescinate A, Aescinate B, soybean lecithin, cholesterol, carbomer, triethanolamine, EDTA2Na, menthols.The invention also discloses preparation method, including prepare liposome and prepare two steps of lipidosome gel.Compared with ordinary gel agent, lipidosome gel disclosed by the invention not only has more preferable Transdermal absorption effect, and with slow-releasing and controlled-releasing action, can slowly it be discharged with given pace, so as to form constant blood concentration in skin, be conducive to extending the treatment time of medicine, the present invention can also reduce the incidence of skin wound repair.
Description
Technical field
The invention belongs to pharmaceutical field, and in particular to it is a kind of using Aescinate A, B as active component lipidosome gel and
Its preparation method.
Background technology
Otoginsenoside be also known as otoginsenoside acid, be from Hippocastanaceae buckeye seed extract obtain total saposins,
The general name of β-otoginsenoside or different otoginsenoside etc., belongs to triterpene saponin.The water solubility of otoginsenoside is poor, to increase it
Solubility, is often made into sodium salt, and research has shown that, the higher composition of content is Aescinate A, B, C, D in Sodium Aescinate.Seven
Leaf saponin(e sodium can reduce pathologic capillary permeability and increase, and increase intravenous tension, reduce Inflammatory substances and ooze out, with anti-
The effects such as inflammation, detumescence, analgesic, improvement blood circulation, the recovery of promotion acute and closed soft tissue injury.
Sodium Aescinate oral administration biaavailability is not high, injects larger to blood vessel irritation, and topical administration leads to medicine
The osmosis for crossing skin reaches internal body, has the following advantages that：1. the first pass effect and medicine of liver can be avoided in stomach and intestine
Degraded in road, drug absorption is not influenceed by gastrointestinal factors, reduces the individual difference of medication；2. when single administration can be long
Between medicine is entered internal with constant speed, reduce administration number of times, extend dosing interval；3. avoid caused by oral administration
Blood concentration peak valley phenomenon, reduces toxicity.
Have the exterior-applied formulations such as Sodium Aescinate ointment, aerosol, liniment at present to come out, existing Sodium Aescinate external application system
Agent has the disadvantages that：1. very well, Determination of oil-water partition coefficient is very low, and Transdermal absorption effect is poor for Sodium Aescinate water-soluble；2. seven
Leaf saponin(e sodium complicated component, property is unstable, the exterior-applied formulation less stable being made；3. Sodium Aescinate external preparation is to skin
Skin excitant is larger.
The content of the invention
The purpose of the present invention is poor for existing Sodium Aescinate external preparation Transdermal absorption effect, and skin irritation is big etc.
Problem is there is provided a kind of using Aescinate A, B as lipidosome gel of active component and preparation method thereof.
Aescinate A that the present invention is provided, B lipidosome gels, it is made up of the composition of following weight proportion：
Preferably, described Aescinate B lipidosome gel, it is made up of the composition of following weight proportion：
The preparation method that the present invention is provided comprises the following steps：
1) preparation of liposome：Aescinate A, Aescinate B, soybean lecithin and cholesterol are taken, absolute ethyl alcohol, 55 is added
~65 DEG C are stirred to dissolve, by the ethanol solution of gained by peristaltic pump with 5-30ml/min speed be injected into constant temperature to 55
In~65 DEG C of purified water, 10~30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is placed in liposome
In mini-extruder extrusion instrument, sequentially pass through the PC filter membranes that aperture is 200nm and 100nm and respectively extrude 2~4 times；The method finally dialysed using film,
Extrusion liquid plus purified water are diluted, dialysed 2~3 times, the ethanol in extrusion liquid is removed, obtains the liposome containing Aescinate A, B；
2) preparation of lipidosome gel：Take carbomer to add purifying water-swellable, obtain the carbomer that weight concentration is 1~3%
Solution, then adds triethanolamine, menthol, EDTA2Na, stirs, and Blank gel matrix is made；Seven leaves will finally be contained
Saponin A, B liposome are added in Blank gel agent matrix, stirring while adding until uniform mixing, produces Aescinate A, B
Lipidosome gel.
The beneficial effects of the invention are as follows：
1) lipidosome gel that the present invention is provided has total transmitance of more preferable Transdermal absorption effect, Aescinate A and B
Apparently higher than Aescinate A, B gels, and with slow-releasing and controlled-releasing action, can slowly it be discharged with given pace, so that in skin
It is interior to form constant blood concentration, be conducive to extending the treatment time of medicine.
2) lipidosome gel that the present invention is provided has preferable quality stability.
3) lipidosome gel that the present invention is provided has more preferable security, can reduce the generation of skin wound repair
Rate.
4) lipidosome gel that provides of the present invention have more preferable anti-inflammatory, it is impervious go out effect.
Embodiment
The present invention is described in detail by the following examples.
Embodiment 1
Raw material prescription：
Preparation technology：
1) preparation of liposome：Aescinate A 6.8g, Aescinate B 4.3g, soybean lecithin 20g and cholesterol 5g are taken,
Absolute ethyl alcohol 50g is added, 60 DEG C are stirred to dissolve, the ethanol solution of gained is injected by peristaltic pump with 15ml/min speed
Into the 250g purified waters of constant temperature to 60 DEG C, 30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is put
In liposome mini-extruder extrusion instrument, sequentially pass through the PC filter membranes that aperture is 200nm and 100nm and respectively extrude 4 times, obtain extrusion liquid 305g；
The method finally dialysed using film, first adds the dilution of 200g purified waters into extrusion liquid, then dialyses 3 times, to remove in extrusion liquid
Ethanol, obtain Aescinate A, B liposomes 414g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 87%, and average grain diameter is 310nm.
2) preparation of gel：Carbomer 8g is taken, stirring makes fully to be swelled under the conditions of adding 400g purified waters, 40 DEG C, obtains
To the carbomer solution that concentration is 2%, triethanolamine 8g, menthol 20g, EDTA2Na are then added into carbomer solution
0.1g, stirs, and Blank gel matrix 436g is made；The liposome 414g containing Aescinate A, B is finally added to blank
It is stirring while adding until uniform mixing, produces Aescinate A, B lipidosome gels 850g in gel substrate 436g.
It is computed, in the Aescinate A, B lipidosome gels, the theoretical content of each composition is：
Embodiment 2
Raw material prescription：
Preparation technology：
1) preparation of liposome：Aescinate A 14g, Aescinate B 4g, soybean lecithin 25g and cholesterol 10g are taken, plus
Enter absolute ethyl alcohol 100g, 60 DEG C are stirred to dissolve, the ethanol solution of gained is injected by peristaltic pump with 25ml/min speed
Into the 300g purified waters of constant temperature to 60 DEG C, 30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is put
In liposome mini-extruder extrusion instrument, sequentially pass through the PC filter membranes that aperture is 200nm and 100nm and respectively extrude 4 times, obtain extrusion liquid 370g；
The method finally dialysed using film, first adds the dilution of 300g purified waters into extrusion liquid, then dialyses 3 times, to remove in extrusion liquid
Ethanol, obtain Aescinate A, B liposomes 505g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 83%, and average grain diameter is 390nm.
2) preparation of gel：Carbomer 5g is taken, stirring makes fully to be swelled under the conditions of adding 400g purified waters, 40 DEG C, obtains
To the carbomer solution that concentration is 1.25%, triethanolamine 5g, menthol 15g, EDTA are then added into carbomer solution
2Na 0.2g, stir, and Blank gel matrix 425g is made；Finally the liposome 505g containing Aescinate A, B is added to
It is stirring while adding until uniform mixing, produces Aescinate A, B lipidosome gels 930g in Blank gel agent matrix 425g.
It is computed, in the Aescinate A, B lipidosome gels, the theoretical content of each composition is：
Embodiment 3
Raw material prescription：
Preparation technology：
1) preparation of liposome：Aescinate A 3.2g, Aescinate B 5.2g, soybean lecithin 15g and cholesterol 4g are taken,
Absolute ethyl alcohol 30g is added, 60 DEG C are stirred to dissolve, the ethanol solution of gained is injected by peristaltic pump with 5ml/min speed
Into the 180g purified waters of constant temperature to 60 DEG C, 30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is put
In liposome mini-extruder extrusion instrument, sequentially pass through the PC filter membranes that aperture is 200nm and 100nm and respectively extrude 4 times, obtain extrusion liquid 195g；
The method finally dialysed using film, first adds the dilution of 150g purified waters into extrusion liquid, then dialyses 3 times, to remove in extrusion liquid
Ethanol, obtain Aescinate A, B liposomes 320g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 85%, and average grain diameter is 430nm.
2) preparation of gel：Carbomer 7.5g is taken, stirring makes fully to be swelled under the conditions of adding 300g purified waters, 40 DEG C,
The carbomer solution that concentration is 2.5% is obtained, triethanolamine 6g, menthol 10g, EDTA are then added into carbomer solution
2Na 0.1g, stir, and Blank gel matrix 323g is made；Finally the liposome 320g containing Aescinate A, B is added to
It is stirring while adding until uniform mixing, produces Aescinate A, B lipidosome gels 643g in Blank gel agent matrix 323g.
It is computed, in the Aescinate A, B lipidosome gels, the theoretical content of each composition is：
Embodiment 4
Raw material prescription：
Preparation technology：
1) preparation of liposome：Take Aescinate A 9.3g, Aescinate B 4.6g, soybean lecithin 16g and cholesterol
9.6g, adds absolute ethyl alcohol 80g, 60 DEG C are stirred to dissolve, by the ethanol solution of gained by peristaltic pump with 15ml/min speed
Degree is injected into the 250g purified waters of constant temperature to 60 DEG C, stirs 30min, liposome turbid liquor is made；Then liposome is mixed
Suspension is placed in liposome mini-extruder extrusion instrument, is sequentially passed through the PC filter membranes that aperture is 200nm and 100nm and is respectively extruded 4 times, obtains extrusion liquid
315g；The method finally dialysed using film, first adds the dilution of 180g purified waters into extrusion liquid, then dialyses 3 times, to remove extrusion
Ethanol in liquid, obtains Aescinate A, B liposomes 380g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 86%, and average grain diameter is 340nm.
2) preparation of gel：Carbomer 6.4g is taken, stirring makes fully to be swelled under the conditions of adding 360g purified waters, 40 DEG C,
Obtain the carbomer solution that concentration is 1.8%, then added into carbomer solution triethanolamine 6.4g, menthol 24g,
EDTA2Na 0.16g, stir, and Blank gel matrix 396g is made；Finally by the liposome 380g containing Aescinate A, B
It is added in Blank gel agent matrix 396g, it is stirring while adding until uniform mixing, produces Aescinate A, B lipidosome gels
776g。
It is computed, in the Aescinate A, B lipidosome gels, the theoretical content of each composition is：
Test example
1. Transdermal absorption is tested
SD rats are taken, using 10%Na2The S aqueous solution is taken off except back wool, and next day, disconnected neck was put to death, and skin of back is cut immediately,
Hypodermis and fat are rejected, after physiological saline is rinsed well repeatedly, appropriately sized, inspection skin integrity is cut into.Using changing
(effective area is 2.9cm to good Franz vertical double-chambers diffusion cell2), the rat skin handled well is fixed on to two Room of diffusion cell
Between, stratum corneum side is to supply chamber.Aescinate A B lipidosome gels and comparison medicine prepared by embodiment 1~4 is (routinely square
Aescinate A B gels made from method) precision takes 0.5mL to be placed in supply chamber, and 7mL reception liquids are added into receiving chamber, and reception liquid is
PBS (0.01M, pH7.4).Water bath with thermostatic control is set as 32 DEG C, with 150r/min magnetic agitations.Respectively at 0.5,1,2,4,
6th, 8,12,24h takes 0.5mL reception liquids, while supplementing 0.5mL PBSs, after 0.45 μm of membrane filtration, takes 20 μ L sample introductions
Aescinate A, B peak areas are determined, drug concentration is calculated.
HPLC chromatogram condition is as follows：Stationary phase is Ultimate C18 (5 μm, 4.6 × 250mm), and mobile phase is acetonitrile：
0.55% phosphate aqueous solution (38：62), Detection wavelength 220nm, flow velocity 1mL/min, 35 DEG C of column temperature, the μ L of sample size 20.
Percutaneous penetration is shown：
Aescinate A, B ordinary gels are respectively A 31%, B 27% in the accumulation transmitance of 4 hours, and with when
Between extension A, B transmitance change it is little, the accumulation transmitance of 12 hours is respectively A 34%, B 32%；
The lipidosome gel of embodiment 1 is respectively A 27%, B 24% in the accumulation transmitance of 4 hours, is then gradually increased
Plus, the accumulation transmitance of 12 hours is respectively A 43%, B 39%；
The lipidosome gel of embodiment 2 is respectively A 29%, B 25% in the accumulation transmitance of 4 hours, is then gradually increased
Plus, the accumulation transmitance of 12 hours is respectively A 38%, B 34%；
The lipidosome gel of embodiment 3 is respectively A 25%, B 22% in the accumulation transmitance of 4 hours, is then gradually increased
Plus, the accumulation transmitance of 12 hours is respectively A 36%, B 34%；
The lipidosome gel of embodiment 4 is respectively A 30%, B 25% in the accumulation transmitance of 4 hours, is then gradually increased
Plus, the accumulation transmitance of 12 hours is respectively A 41%, B 36%.
As can be seen from the above results, the present invention can not only improve Aescinate A, B Transdermal absorption effect, total to pass through
Rate can slowly be discharged obviously higher than Aescinate A B ordinary gels, and with slow-releasing and controlled-releasing action with given pace, so that
Constant blood concentration is formed in skin, is conducive to extending the treatment time of medicine.
2. stability test
Reference drug stability test guideline, medicine is put in measuring cup, is spread out into≤thick 5mm thin layer, is carried out
The high temperature of the present invention, the stability test of high humidity and strong light are studied, and are below specific experimental result.
(1) hot test test sample is put in sealing clean container, is placed 10 days under the conditions of 60 DEG C, in 0, sampling in 5,10 days
Detection.
The hot test measurement result of table 1
(2) high wet test test sample is put in constant humidity equipment, is placed 10 days under the conditions of 25 DEG C, RH92.5% ± 5%, 0,
5th, sampling detection in 10 days.
The high wet test measurement result of table 2
(3) strong illumination experiment test sample is put in lighting box or other suitable illumination containers equipped with fluorescent lamp, Yu Zhao
Spend to be placed 10 days under the conditions of 4500lx ± 500lx, 0, sampling detection in 5,10 days.
The highlight test measurement result of table 3
3. skin irritation test
Healthy rabbits (2.0 ± 0.2kg) 20 are taken, 5 groups are randomly divided into, every group of male and female half and half are investigated embodiment 1~4 and made
Standby lipidosome gel and the Aescinate A prepared according to a conventional method, the skin irritation of B ordinary gels.In 24h before administration,
Animal backbone diamond wool is taken off with 10% sodium sulfide solution, per side unhairing scope about 3cm × 3cm, epidermis can not be damaged.Experiment
Using consubstantiality left and right sides Self-control method.Lipidosome gel and water are given respectively in left and right side unhairing area.2 times a day, successive administration
One week, residual test medicine was washed away with warm water in the 8th day.Respectively at remove medicine after 1,6,12,24h observation medicine-feeding part whether there is
Erythema and oedema situation, no erythema or oedema are set to 0 grade, have erythema or oedema then by being set to 1-4 grades from light to heavy.
The rabbit skin irritation test result (n=5) of table 4
As can be seen from the above tests, skin wound repair incidence of the present invention is relatively low, and only slight erythema or oedema go out
It is existing, and can be completely eliminated in 24 hours after being discontinued, do not influence treatment, and Aescinate A, the skin irritatin of B ordinary gels are anti-
Answer incidence higher, and symptom is even more serious, takes a turn for the better slower, still respectively having 1 within 24 hours has slight erythema and oedema, illustrates this hair
Bright security is more preferable than ordinary gel.
4. anti-swelling/it is impervious go out experiment
Using mice ear model, if blank group, Aescinate A B lipidosome gels group, Aescinate A B ordinary gels
Swelling is determined after group, Sodium Aescinate ordinary gel group, every group of 10 animals, coating, 5 are the results are shown in Table.
The anti-swelling Experiment on Function result of table 5
By 3,4 groups be compared, as a result show, Aescinate A B and Sodium Aescinate can reduce mice ear model
Swelling, two groups of results do not have significant difference, show to carry out the concept feasible of anti-inflammatory treatment using Aescinate A B.
By 2,3 groups be compared, as a result show, the anti-swelling ability of Aescinate A B lipidosome gels is substantially better than seven leaves
Saponin A B ordinary gels, the two there were significant differences (P<0.05).
Using the animal model on the granulomatous influence of rat acute croton oil, if blank group, Aescinate A B liposomes
Determine and ooze out after gel group, Aescinate A B ordinary gels group, Sodium Aescinate ordinary gel group, every group of 10 animals, coating
Amount, the results are shown in Table 6.
Table 6 it is impervious go out Experiment on Function result
| Group | Dosage | Acute seepage discharge (ml) | |
| 1 | Negative control group | / | 6.69±3.52 |
| 2 | Aescinate A B lipidosome gel groups | 5mg/kg | 3.56±2.10 |
| 3 | Aescinate A B ordinary gel groups | 5mg/kg | 4.86±2.21 |
| 4 | Sodium Aescinate ordinary gel group | 5mg/kg | 4.31±2.14 |
As a result show, Aescinate A B and Sodium Aescinate can reduce the seepage discharge of mice ear model and the two does not have
There were significant differences；The impervious output capacity of Aescinate A B lipidosome gels is substantially better than Aescinate A B ordinary gels, and the two has
Significant difference (P<0.05).
Claims (3)
1. a kind of Aescinate A, B lipidosome gels, it is characterised in that be made up of the composition of following weight proportion：
2. Aescinate A as claimed in claim 1, B lipidosome gels, it is characterised in that by following weight proportion into packet
Into：
3. a kind of prepare Aescinate A described in claim 1 or 2, the method for B lipidosome gels, it is characterised in that including following
Step：
1) preparation of liposome：Aescinate A, Aescinate B, soybean lecithin and cholesterol are taken, absolute ethyl alcohol, 55~65 is added
DEG C be stirred to dissolve, by the ethanol solution of gained by peristaltic pump with 5-30ml/min speed be injected into constant temperature to 55~65
DEG C purified water in, stir 10~30min, liposome turbid liquor is made；Then liposome turbid liquor is placed in liposome extrusion
In instrument, sequentially pass through the PC filter membranes that aperture is 200nm and 100nm and respectively extrude 2~4 times；The method finally dialysed using film, will be squeezed
Go out liquid plus purified water dilution, dialyse 2~3 times, remove the ethanol in extrusion liquid, obtain the liposome containing Aescinate A, B；
2) preparation of lipidosome gel：Take carbomer to add purifying water-swellable, obtain the carbomer solution that weight concentration is 1~3%,
Then triethanolamine, menthol, EDTA2Na are added, is stirred, Blank gel matrix is made；Otoginsenoside will finally be contained
A, B liposome are added in Blank gel agent matrix, stirring while adding until uniform mixing, produces Aescinate A, B lipids
Body gel.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116115566A (en) * | 2021-11-15 | 2023-05-16 | 上海维洱生物医药科技有限公司 | Aescin sodium liposome and preparation method thereof |
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2017
- 2017-04-01 CN CN201710212709.1A patent/CN107157921A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| 徐白: "复方三七总皂苷脂质体凝胶皮肤给药剂型的研究", 《中国优秀硕士学位论文全文数据库 医药卫生科技辑》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116115566A (en) * | 2021-11-15 | 2023-05-16 | 上海维洱生物医药科技有限公司 | Aescin sodium liposome and preparation method thereof |
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