CN106943339A - Aescinate A lipidosome gel and preparation method thereof - Google Patents
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- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
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Abstract
The invention discloses a kind of Aescinate A lipidosome gel, it is made up of compositions such as Aescinate A, 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 a kind of Aescinate A lipidosome gel and preparation method thereof.
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.
There is provided a kind of lipidosome gel using Aescinate A as active component and preparation method thereof for problem.
The Aescinate A lipidosome gel that the present invention is provided, it is made up of the composition of following weight proportion：
Preferably, described Aescinate A 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, soybean lecithin and cholesterol are taken, absolute ethyl alcohol, 55~65 DEG C of stirrings is added
Make dissolving, it is pure to 55~65 DEG C that by peristaltic pump the ethanol solution of gained is injected into constant temperature with 5-30ml/min speed
Change in water, stir 10~30min, liposome turbid liquor is made；Then liposome turbid liquor is placed in liposome mini-extruder extrusion instrument, according to
It is secondary respectively to be extruded 2~4 times for 200nm and 100nm PC filter membranes by aperture；The method finally dialysed using film, by extrusion liquid plus
Purified water dilutes, and dialyses 2~3 times, removes the ethanol in extrusion liquid, obtains the liposome containing Aescinate A；
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
The liposome of saponin A is added in Blank gel agent matrix, stirring while adding until uniform mixing, produces Aescinate A lipid
Body gel.
The beneficial effects of the invention are as follows：
1) lipidosome gel that the present invention is provided has more preferable Transdermal absorption effect, and the total transmitance of Aescinate A is obvious
Higher than Aescinate A gel, and with slow-releasing and controlled-releasing action, can slowly it be discharged with given pace, so as to be formed in skin
Constant blood concentration, is 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 5g, soybean lecithin 20g and cholesterol 5g are taken, absolute ethyl alcohol 50g is added,
60 DEG C are stirred to dissolve, by the ethanol solution of gained by peristaltic pump with 15ml/min speed be injected into constant temperature to 60 DEG C
In 250g purified waters, 30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is placed in liposome mini-extruder extrusion instrument,
Sequentially pass through the PC filter membranes that aperture is 200nm and 100nm respectively to extrude 4 times, obtain extrusion liquid 285g；The side finally dialysed using film
Method, first adds the dilution of 200g purified waters into extrusion liquid, then dialyses 3 times, to remove the ethanol in extrusion liquid, obtains Aescinate A
Liposome 420g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 89%, and average grain diameter is 350nm.
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 420g containing Aescinate A finally is added into blank to coagulate
It is stirring while adding until uniform mixing, produces Aescinate A lipidosome gel 856g in jelly matrix 436g.
It is computed, in the Aescinate A lipidosome gel, the theoretical content of each composition is：
Embodiment 2
Raw material prescription：
Preparation technology：
1) preparation of liposome：Aescinate A 3g, soybean lecithin 25g and cholesterol 10g are taken, absolute ethyl alcohol is added
100g, 60 DEG C are stirred to dissolve, and the ethanol solution of gained is injected into constant temperature is extremely by peristaltic pump with 25ml/min speed
In 60 DEG C of 300g purified waters, 30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is placed in into liposome to squeeze
Go out in instrument, sequentially pass through the PC filter membranes that aperture is 200nm and 100nm and respectively extrude 4 times, obtain extrusion liquid 350g；Finally use film
The method of dialysis, first adds the dilution of 300g purified waters into extrusion liquid, then dialyses 3 times, to remove the ethanol in extrusion liquid, obtains seven
Leaf saponin A liposome 490g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 82%, and average grain diameter is 500nm.
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；The liposome 490g containing Aescinate A is finally added to sky
It is stirring while adding until uniform mixing, produces Aescinate A lipidosome gel 915g in white gel agent matrix 425g.
It is computed, in the Aescinate A lipidosome gel, the theoretical content of each composition is：
Embodiment 3
Raw material prescription：
Preparation technology：
1) preparation of liposome：Aescinate A 8g, soybean lecithin 15g and cholesterol 4g are taken, absolute ethyl alcohol 30g is added,
60 DEG C are stirred to dissolve, by the ethanol solution of gained by peristaltic pump with 5ml/min speed be injected into constant temperature to 60 DEG C
In 150g purified waters, 30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is placed in liposome mini-extruder extrusion instrument,
Sequentially pass through the PC filter membranes that aperture is 200nm and 100nm respectively to extrude 4 times, obtain extrusion liquid 175g；The side finally dialysed using film
Method, first adds the dilution of 150g purified waters into extrusion liquid, then dialyses 3 times, to remove the ethanol in extrusion liquid, obtains Aescinate A
Liposome 290g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 86%, and average grain diameter is 420nm.
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；The liposome 290g containing Aescinate A is finally added to sky
It is stirring while adding until uniform mixing, produces Aescinate A lipidosome gel 613g in white gel agent matrix 323g.
It is computed, in the Aescinate A lipidosome gel, the theoretical content of each composition is：
Embodiment 4
Raw material prescription：
Preparation technology：
1) preparation of liposome：Aescinate A 2.4g, soybean lecithin 16g and cholesterol 9.6g are taken, absolute ethyl alcohol is added
80g, 60 DEG C are stirred to dissolve, by the ethanol solution of gained by peristaltic pump with 15ml/min speed be injected into constant temperature to 60
DEG C 250g purified waters in, stir 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 4 times, obtain extrusion liquid 310g；It is finally saturating using film
The method of analysis, first adds the dilution of 210g purified waters into extrusion liquid, then dialyses 3 times, to remove the ethanol in extrusion liquid, obtains seven leaves
Saponin A liposome 404g；
The envelop rate and particle diameter of liposome are detected according to literature method, envelop rate is 87%, and average grain diameter is 400nm.
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 the liposome 404g containing Aescinate A is added
Enter into Blank gel agent matrix 396g, it is stirring while adding until uniform mixing, produces Aescinate A lipidosome gel 800g.
It is computed, in the Aescinate A lipidosome gel, 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 lipidosome gel and comparison medicine prepared by embodiment 1~4 is (routinely square
Aescinate A ordinary gel made from method) precision takes 0.5mL to be placed in supply chamber, and 7mL reception liquids are added into receiving chamber, receive
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,
2nd, 4,6,8,12,24h takes 0.5mL reception liquids, while supplementing 0.5mL PBSs, after 0.45 μm of membrane filtration, takes 20 μ L
Sample introduction determines Aescinate A peak area, calculates drug concentration.
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 gel reached 32% in the accumulation transmitance of 4 hours, and transmitance changes as time went on
Less, the accumulation transmitance of 12 hours is 36%；
The lipidosome gel of embodiment 1 is 25% in the accumulation transmitance of 4 hours, is then gradually increased, 12 hours tired
Product transmitance reaches 45%；
The lipidosome gel of embodiment 2 is 22% in the accumulation transmitance of 4 hours, is then gradually increased, 12 hours tired
Product transmitance reaches 37%；
The lipidosome gel of embodiment 3 is 24% in the accumulation transmitance of 4 hours, is then gradually increased, 12 hours tired
Product transmitance reaches 38%；
The lipidosome gel of embodiment 4 is 27% in the accumulation transmitance of 4 hours, is then gradually increased, 12 hours tired
Product transmitance reaches 41%.
As can be seen from the above results, the present invention can not only improve the Transdermal absorption effect of Aescinate A, total transmitance
Apparently higher than Aescinate A gel, and with slow-releasing and controlled-releasing action, can slowly it be discharged with given pace, so that in skin
Constant blood concentration is formed, 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 high 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
The skin irritation of standby lipidosome gel and the Aescinate A ordinary gel prepared according to a conventional method.In 24h before administration, use
10% sodium sulfide solution takes off animal backbone diamond wool, per side unhairing scope about 3cm × 3cm, can not damage epidermis.Experiment is adopted
With 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
In 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 it is red
Spot 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 after drug withdrawal in 24 hours, do not influence to treat, and the skin wound repair of Aescinate A ordinary gel
Incidence is higher, and symptom is even more serious, takes a turn for the better relatively slow, still respectively having 1 within 24 hours has slight erythema and oedema, illustrates the present invention
Security it is more preferable than ordinary gel.
4. anti-swelling/it is impervious go out experiment
Using mice ear model, if blank group, Aescinate A lipidosome gel group, Aescinate A ordinary gel
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 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 single Aescinate A.
By 2,3 groups be compared, as a result show, the anti-swelling ability of Aescinate A lipidosome gel is substantially better than seven leaves
Saponin A ordinary gel, 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 liposome are solidifying
Seepage discharge is determined after glue group, Aescinate A ordinary gel group, Sodium Aescinate ordinary gel group, every group of 10 animals, coating,
It 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 | / | 6.17±3.50 |
| 2 | Aescinate A lipidosome gel group | 5mg/kg | 3.78±2.02 |
| 3 | Aescinate A ordinary gel group | 5mg/kg | 4.78±2.02 |
| 4 | Sodium Aescinate ordinary gel group | 5mg/kg | 4.26±2.07 |
As a result show, Aescinate A 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 lipidosome gel is substantially better than Aescinate A ordinary gel, and the two has aobvious
Write difference (P<0.05).
Claims (3)
1. a kind of Aescinate A lipidosome gel, it is characterised in that be made up of the composition of following weight proportion：
2. Aescinate A lipidosome gel as claimed in claim 1, it is characterised in that by following weight proportion into packet
Into：
3. a kind of method for preparing Aescinate A lipidosome gel described in claim 1 or 2, it is characterised in that including following step
Suddenly：
1) preparation of liposome：Aescinate A, soybean lecithin and cholesterol are taken, absolute ethyl alcohol is added, 55~65 DEG C of stirrings make molten
Solution, the ethanol solution of gained is injected into by peristaltic pump with 5-30ml/min speed the purified water of constant temperature to 55~65 DEG C
In, 10~30min is stirred, liposome turbid liquor is made；Then liposome turbid liquor is placed in liposome mini-extruder extrusion instrument, passed through successively
The PC filter membranes that aperture is 200nm and 100nm are crossed respectively to extrude 2~4 times；The method finally dialysed using film, by extrusion liquid plus purifying
Water dilutes, and dialyses 2~3 times, removes the ethanol in extrusion liquid, obtains the liposome containing Aescinate A；
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；Aescinate A will finally be contained
Liposome be added in Blank gel agent matrix, it is stirring while adding until uniform mixing, produces Aescinate A liposome and coagulate
Glue.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111249226A (en) * | 2020-03-24 | 2020-06-09 | 中南大学 | Aescin injectable hydrogel and preparation method and application thereof |
-
2017
- 2017-04-01 CN CN201710212793.7A patent/CN106943339A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| 张慧慧: "三七叶总皂苷脂质体凝胶剂的研究", 《中国优秀硕士学位论文全文数据库工程科技Ⅰ辑》 * |
| 戴德银 等: "《实用新药特药手册》", 31 May 2015, 人民军医出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111249226A (en) * | 2020-03-24 | 2020-06-09 | 中南大学 | Aescin injectable hydrogel and preparation method and application thereof |
| CN111249226B (en) * | 2020-03-24 | 2021-06-15 | 中南大学 | Aescin injectable hydrogel and preparation method and application thereof |
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