CN1931133A - Total arasaponin precursor liposome and its prepn process - Google Patents
Total arasaponin precursor liposome and its prepn process Download PDFInfo
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- CN1931133A CN1931133A CN 200610048618 CN200610048618A CN1931133A CN 1931133 A CN1931133 A CN 1931133A CN 200610048618 CN200610048618 CN 200610048618 CN 200610048618 A CN200610048618 A CN 200610048618A CN 1931133 A CN1931133 A CN 1931133A
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Abstract
The present invention is total arasaponin precursor liposome and its preparation process. The total arasaponin precursor liposome consists of total arasaponin, phospholipid and cholesterol in the weight ratio of 1 to 0.5-20 to 0-10 as well as water soluble carrier in the weight ratio to phospholipid of 1-10 to 0.5-10. It is prepared through one simple process, and may be prepared into liquid or solid.
Description
Technical field
The invention belongs to medical technical field, be specifically related to total arasaponin precursor liposome and the pharmaceutical preparation that contains total arasaponin precursor liposome.
Background technology
Radix Notoginseng total arasaponins is the active component in the araliaceae ginseng plant Radix Notoginseng (panax notoginseng), it can increase blood flow volume, blood vessel dilating, reduction arteriotony and myocardial oxygen consumption, improve body immune function and to anoxia tolerance three years ago, and anticoagulant is arranged, reduce effects such as blood viscosity.But the Radix Notoginseng total arasaponins water solublity is very big, and at gastrointestinal tract mucous permeability extreme difference, the bioavailability of oral formulations is very low, and eliminates very fast in blood.Radix Notoginseng total arasaponins is enclosed in the liposome, can reduce the toxicity of medicine, strengthens pharmacological action, and can reduce the elimination speed of Radix Notoginseng total arasaponins, prolongs the effect of Radix Notoginseng total arasaponins, increases the inside and outside stability of Radix Notoginseng total arasaponins, improves the compliance of patient's medication.But total notoginseng saponin liposome is less owing to granule, separation difficulty in preparation process, and assemble easily, mobile poor.Total notoginseng saponin liposome mobile relatively poor needs to add in being prepared into processes such as tablet, capsule increases mobile adjuvant, increases operation, has brought inconvenience being prepared into to the preparation processing process.
Patent of invention total notoginseng saponin liposome and preparation thereof (zl03135782.2) and total notoginseng saponin liposome and preparation method thereof (zl0310108690.4) is to the preparation and the preparation of total notoginseng saponin liposome, but Radix Notoginseng total arasaponins is made not appearing in the newspapers of pro-liposome.Total arasaponin precursor liposome is liquid or dry, as to have good flow performance solid granulates shape material; except that can accomplishing scale production; a large amount of total arasaponin precursor liposomes is convenient to store before aquation; overcome the phase inter coagulation between the liposome, be easy to again during suspendible again disperse.Good fluidity is convenient, assurance product quality in processes such as preparation tablet, capsule.
Summary of the invention
The objective of the invention is provides a kind of total arasaponin precursor liposome and preparation method thereof at the deficiencies in the prior art part.
Purpose of the present invention can be achieved by subordinate's technical scheme.
Total arasaponin precursor liposome of the present invention is made up of Radix Notoginseng total arasaponins, phospholipid, cholesterol and water-solubility carrier, the weight ratio of Radix Notoginseng total arasaponins, phospholipid, cholesterol is a Radix Notoginseng total arasaponins: phospholipid: cholesterol is 1: 0.5～20: 0～10, and the weight ratio of water-solubility carrier and phospholipid is 1-10: 0.5-10.
Wherein said water-solubility carrier is a kind of in intoxicated of sorbitol, mannitol, sodium chloride, monosaccharide, disaccharidase, polysaccharide, dextrose.
The preparation method of above-mentioned total arasaponin precursor liposome is:
(1) described water-solubility carrier, phospholipid, cholesterol, Radix Notoginseng total arasaponins are made solution, mixing filters;
(2) drying is sieved, and promptly gets total arasaponin precursor liposome;
Perhaps:
(1) with behind water-solubility carrier and the Radix Notoginseng total arasaponins mix homogeneously, put at the bottom of the garden in the flask, load onto rotary evaporator, flask is immersed preheating in the water-bath;
(2) get phospholipid, cholesterol, be dissolved in the dehydrated alcohol, make solution; Gradation adds in the powder bed that rotates, and continues the vacuum decompression evaporation;
(3) all adding back continuation reduction vaporization to solvent at ethanol liquid is evaporated completely substantially;
(4) the powder taking-up is placed the vacuum desiccator drying under reduced pressure, sieve, promptly get total arasaponin precursor liposome.
Perhaps:
(1) the water intaking solubleness carrier is put in the flask, loads onto rotary evaporator, and rotary flask is immersed in the 30-70 ℃ of water-bath;
(2) get Radix Notoginseng total arasaponins, phospholipid, cholesterol, make solution, be added in the powder bed of rotation, continue the vacuum decompression evaporation, add solution gradually, solution adds back continuation evaporation and is evaporated completely substantially until solvent;
(3) take out content, sieve, put drying under reduced pressure in the vacuum desiccator, sieve after the drying, promptly get total arasaponin precursor liposome.
Perhaps:
(1) water intaking solubleness carrier water dissolution is standby;
(2) get in Radix Notoginseng total arasaponins, phospholipid, the cholesterol adding dehydrated alcohol, the heating in water bath dissolving is made into liposome solutions;
(3) the water-solubility carrier aqueous solution is poured in the liposome solutions, in ultraemulsifier ultrasonic 5-20 minute, under nitrogen current in packing ampoule or the cillin bottle, lyophilization 18-48 hour, seal or inflated with nitrogen seals, promptly get total arasaponin precursor liposome.
Phospholipid described in the present invention is a kind of in the solid acyl acetyl fat of fabaceous lecithin, lecithin, cephalin, phosphatidyl ethamine alcohol, gallbladder, cupreol, β-sitoesterol, natrii tauroglycocholas, sphingo, Yolk lecithin, sphingomyelin, two whale vinegar phosphoric acid fat, phosphatidyl alcohol, phosphatidylinositols, cholic acid, phosphatidic acid Phosphatidylserine cardiolipin, two myristoyl lecithin, stearmide or other synthetic phospholipid, or their mixture.
Total arasaponin precursor liposome of the present invention can be made capsule, tablet, granule, injection, transfusion, freeze-dried powder, oral liquid, preparation capable of permeating skin, aerosol, spray, ophthalmic preparation, ointment and emulsifiable paste.
Total arasaponin precursor liposome of the present invention; preparation easily; except that can accomplishing scale production; total arasaponin precursor liposome is liquid or dry, as to have good flow performance solid granulates shape material; before aquation, be convenient to store; overcome the phase inter coagulation between the liposome, be easy to dispersive shortcoming again during suspendible again.Be prepared into tablet, capsule of good fluidity etc., guaranteed the quality of product better.
Total arasaponin precursor liposome adds water or buffer before use and forms liposome by jolting, stirring, ultrasound wave aquation, when digestive tract contacts with water, and lipid swelling and carrier dissolves rapidly, the formation multilamellar liposome.The stabilizing agent of multilamellar liposome is more higher than the envelop rate of unilamellar liposome, and stability better.
The specific embodiment:
Below with embodiment the present invention is described in detail, but the invention is not restricted to following examples.
Embodiment 1:
Getting soybean phospholipid 1.15g, cholesterol 0.7g adds dehydrated alcohol 50ml dissolving back and adds and contain among the aqueous solution 10ml of Radix Notoginseng total arasaponins 0.2g, the constant temperature high-speed stirred is mixed, filtering with microporous membrane, promptly get total notoginseng saponin liposome, add sorbitol 5g, emulsifying is even, spray drying, sieve, promptly get Powdered total arasaponin precursor liposome.
Embodiment 2:
In containing the aqueous solution 10ml of Radix Notoginseng total arasaponins 0.5g, add lactose 0.1g, and make dissolve A liquid; Other gets lecithin 2.1g, and cholesterol 1.8g, phosphatidic acid 0.1g are dissolved in and get B liquid among the dehydrated alcohol 50ml; B liquid is under agitation slowly added in the A liquid, and mixing filters, and spray drying is sieved, and promptly gets Powdered total arasaponin precursor liposome.
Embodiment 3:
Get Radix Notoginseng total arasaponins 1.5g be dissolved in the 30ml water A liquid; Other gets phosphatidylinositols 3g, and cholesterol 1.5g is dissolved in and gets B liquid among the dehydrated alcohol 50ml, under agitation slowly adds B liquid in the A liquid, be sprayed in the fluid bed that contains 13g sodium chloride, by fluid bed boiling one-step palletizing, drying, sieve, promptly get the graininess total arasaponin precursor liposome.
Embodiment 4
Get Radix Notoginseng total arasaponins 2g be dissolved in the 30ml water A liquid; Other gets phosphatidylinositols 3g, and cholesterol 1.5g is dissolved in and gets B liquid among the dehydrated alcohol 50ml; B liquid is under agitation slowly added in the A liquid, be sprayed in the fluid bed that contains lactose 13g,, sieve, promptly get the graininess total arasaponin precursor liposome by fluid bed boiling one-step palletizing, drying.
Embodiment 5
Get sorbitol 0.5g and Radix Notoginseng total arasaponins 0.8g mix homogeneously is placed in the eggplant-shape bottle, load onto rotary evaporator, flask is immersed in the water-bath rotation preheating 30 minutes, get phosphatidyl ethamine alcohol 2.0g, cholesterol 0.5g, vitamin E 0.2g is dissolved among the dehydrated alcohol 100ml, add in the powder bed that rotates in batches, continue the vacuum decompression evaporation; All add back continuation reduction vaporization to solvent at ethanol liquid and be evaporated completely substantially, powder is taken out place the vacuum desiccator drying under reduced pressure, sieve, promptly get Powdered total arasaponin precursor liposome;
Embodiment 6:
Getting sorbitol 10g puts at the bottom of eggplant shape or the garden in the flask, load onto rotary evaporator, rotary flask is immersed in the 35-45 ℃ of water-bath, get Radix Notoginseng total arasaponins 1.5g, cephalin 2.5g, cholesterol 1g, be dissolved among the dehydrated alcohol 100ml, be added to again in the powder bed of rotation, continue the vacuum decompression evaporation, add solution gradually, note being sure not to make powder bed wet excessively, solution adds back continuation evaporation and is evaporated completely substantially until solvent; Take out content, sieve, put drying under reduced pressure in the vacuum desiccator, sieve after the drying, promptly get Powdered total arasaponin precursor liposome.
Embodiment 7:
Get among Radix Notoginseng total arasaponins 1g, phosphatidase 11 g, the cholesterol 0.5g adding dehydrated alcohol 20ml, heating in water bath 50-90 ℃ dissolving is made into liposome solutions; Mannitol 3g, glucose 2g are dissolved in the 25ml water, mixing, and pour in the liposome solutions, in ultraemulsifier ultrasonic 5-20 minute, under nitrogen current, divide in the ampoule of packing into lyophilization 24-36 hour, inflated with nitrogen seals, and promptly gets total arasaponin precursor liposome.Get 1 total arasaponin precursor liposome, add the abundant mixing of an amount of water for injection, promptly get total notoginseng saponin liposome.
Total arasaponin precursor liposome of the present invention can be made into tablet, capsule, injection etc.
Claims (7)
1, a kind of total arasaponin precursor liposome, it is characterized in that forming by Radix Notoginseng total arasaponins, phospholipid, cholesterol and water-solubility carrier, the weight ratio of Radix Notoginseng total arasaponins, phospholipid, cholesterol is a Radix Notoginseng total arasaponins: phospholipid: cholesterol is 1: 0.5～20: 0～10, and the weight ratio of water-solubility carrier and phospholipid is 1-10: 0.5-10.
2, total arasaponin precursor liposome according to claim 1 is characterized in that described water-solubility carrier is a kind of in intoxicated of sorbitol, mannitol, sodium chloride, monosaccharide, disaccharidase, polysaccharide, dextrose.
3,, it is characterized in that included sequential steps is according to the preparation method of the described total arasaponin precursor liposome of claim 1:
(1) described water-solubility carrier, phospholipid, cholesterol, Radix Notoginseng total arasaponins are made solution, mixing filters;
(2) drying is sieved, and promptly gets total arasaponin precursor liposome;
4,, it is characterized in that included sequential steps is according to the preparation method of the described total arasaponin precursor liposome of claim 1:
(1) with behind water-solubility carrier and the Radix Notoginseng total arasaponins mix homogeneously, places flask, load onto rotary evaporator, flask is immersed in the 30-70 ℃ of water-bath;
(2) get phospholipid, cholesterol, be dissolved in the dehydrated alcohol, make solution; Add gradually in the powder bed that rotates, continue the vacuum decompression evaporation;
(3) all adding back continuation reduction vaporization to solvent at ethanol liquid is evaporated completely substantially;
(4) with powder for drying, sieve, promptly get total arasaponin precursor liposome.
5,, it is characterized in that included sequential steps is according to the preparation method of the described total arasaponin precursor liposome of claim 1:
(1) the water intaking solubleness carrier is put in the flask, loads onto rotary evaporator, and rotary flask is immersed in the 30-70 ℃ of water-bath;
(2) get Radix Notoginseng total arasaponins, phospholipid, cholesterol, make solution, be added in the powder bed of rotation, continue the vacuum decompression evaporation, add solution gradually, solution adds back continuation evaporation and is evaporated completely substantially until solvent;
(3) take out content, drying is sieved, and promptly gets total arasaponin precursor liposome.
6,, it is characterized in that included sequential steps is according to the preparation method of the described total arasaponin precursor liposome of claim 1:
(1) water intaking solubleness carrier water dissolution is standby;
(2) get in Radix Notoginseng total arasaponins, phospholipid, the cholesterol adding dehydrated alcohol, the heating in water bath dissolving is made into liposome solutions;
(3) the water-solubility carrier aqueous solution is poured in the liposome solutions, in ultraemulsifier ultrasonic 5-20 minute, in packing ampoule or the cillin bottle, lyophilization was sealed or inflated with nitrogen seals, and promptly gets total arasaponin precursor liposome under nitrogen current.
7,, it is characterized in that included sequential steps is according to the preparation method of the described total arasaponin precursor liposome of claim 1:
(1) the water intaking solubleness carrier is in fluid bed;
(2) get Radix Notoginseng total arasaponins, phospholipid, cholesterol and make solution, be sprayed in the water-solubility carrier in the fluid bed,, sieve, promptly get total arasaponin precursor liposome by fluid bed boiling one-step palletizing, drying.
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| Application Number | Priority Date | Filing Date | Title |
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| CNB2006100486180A CN100460017C (en) | 2006-08-14 | 2006-08-14 | Total arasaponin precursor liposome and its prepn process |
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| CNB2006100486180A CN100460017C (en) | 2006-08-14 | 2006-08-14 | Total arasaponin precursor liposome and its prepn process |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103585466A (en) * | 2013-11-21 | 2014-02-19 | 吉林大学 | Sapodilla saponin composite precursor liposome and preparation method thereof |
| CN118140999A (en) * | 2024-05-09 | 2024-06-07 | 长春中医药大学 | Instant coffee containing ginseng glycoprotein liposome and preparation method thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1212122C (en) * | 2003-09-05 | 2005-07-27 | 云南植物药业有限公司 | Notiginseng total saponin liposome and its preparation |
| CN1256949C (en) * | 2003-11-19 | 2006-05-24 | 复旦大学 | Notoginsen triterpenes liposome and prepartion thereof |
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2006
- 2006-08-14 CN CNB2006100486180A patent/CN100460017C/en active Active
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103585466A (en) * | 2013-11-21 | 2014-02-19 | 吉林大学 | Sapodilla saponin composite precursor liposome and preparation method thereof |
| CN103585466B (en) * | 2013-11-21 | 2016-04-06 | 吉林大学 | Herba Herminii saponin's composite precursor liposome and preparation method |
| CN118140999A (en) * | 2024-05-09 | 2024-06-07 | 长春中医药大学 | Instant coffee containing ginseng glycoprotein liposome and preparation method thereof |
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| Publication number | Publication date |
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| CN100460017C (en) | 2009-02-11 |
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