CN1686155A - Astragalus glycoside fatty emulsion and its preparation technology - Google Patents
Astragalus glycoside fatty emulsion and its preparation technology Download PDFInfo
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- CN1686155A CN1686155A CN 200510038651 CN200510038651A CN1686155A CN 1686155 A CN1686155 A CN 1686155A CN 200510038651 CN200510038651 CN 200510038651 CN 200510038651 A CN200510038651 A CN 200510038651A CN 1686155 A CN1686155 A CN 1686155A
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Abstract
A lipid emulsion of astragaloside A is proportional prepared from astragaloside A, oil, surfactant, isotonic regulator, cosolvent and water for injection. Its preparing process is also disclosed.
Description
Technical field:
The present invention relates to a kind of astragalus glycoside fatty emulsion and preparation technology thereof.
Background technology:
Astragaloside is one of Radix Astragali monomer, except antiinflammatory, blood pressure lowering being arranged, improving the effect such as myocardial ischemia, Recent study shows that it has following pharmacological action: can suppress the rising of cerebral tissue content of MDA after the cerebral ischemia, and improve the activity of glutathione peroxidase; Have tangible anti-liver injury (hepatitis, hepatic fibrosis, liver tumor), treatment rheumatoid arthritis and anti-aging effects; Rats with renal ischemic reperfusion injury had protective effect; The early diabetic nephropathy rat had protective effect.The astragaloside activity is extremely strong, and especially it has strong active at diabetic nephropathy and anti-tumor aspect.
Astragaloside is insoluble in water, and purity highly dissoluble more is poor more, and cosolvent is not basic yet to take on a new look even add, and places a period of time and promptly separates out crystallization, cause the astragaloside injection poor stability clinical application problem of safety inadequately, limited astragaloside application clinically greatly.
Summary of the invention:
The object of the present invention is to provide a kind of main active that can make to be dispersed in the oil phase, redispersion forms astragalus glycoside fatty emulsion to aqueous phase.Because principal agent is wrapped in the oil, this dosage form has good stability, and toxicity is little, and zest is little, and untoward reaction is few, and has certain slow-releasing, has not only solved the problem that poorly water-soluble is easily separated out, and has guaranteed clinical drug safety and effectiveness.Owing to the passive targeting of Emulsion, also provide a kind of route of administration of relative high-efficiency low-toxicity simultaneously for the patient.
Another object of the present invention is to provide a kind of technology for preparing astragalus glycoside fatty emulsion.
Purpose of the present invention can reach by following measure:
The invention provides a kind of astragalus glycoside fatty emulsion, it is characterized in that: the principal agent astragaloside adds adjuvant and makes astragalus glycoside fatty emulsion, described adjuvant has oil, surfactant, isoosmotic adjusting agent and suitable cosolvent, its each component percentages (g/ml) is respectively astragaloside 0.0001～2%, oil 3～50%, surfactant 0.5～5%, isoosmotic adjusting agent 0.05～5%, cosolvent 0～5%, and surplus is a water for injection.
Above-mentioned astragalus glycoside fatty emulsion, its preparation technology is: under inert gas shielding, take by weighing oil for injection, be heated to 30～100 ℃, under high-speed stirred surfactant, astragaloside are added in the oil for injection, stir as oil phase; In addition isoosmotic adjusting agent is added in the proper amount of water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water; Under high-speed stirred, oil phase is mixed with water and continue high-speed stirred and make colostrum, add to the full amount of water for injection, mixing is regulated pH to 2.5～10.5 after the high pressure homogenize breast is even, makes white emulsion liquid, filters, and fill, seals, sterilizes, promptly.
Above-mentioned astragalus glycoside fatty emulsion, its preparation technology also can be: under inert gas shielding, take by weighing oil for injection, be heated to 30～100 ℃, under high-speed stirred, surfactant, astragaloside and cosolvent are added in the oil for injection, stir as oil phase; In addition isoosmotic adjusting agent is added in the proper amount of water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water; Under high-speed stirred, oil phase is mixed with water and continue high-speed stirred and make colostrum, add to the full amount of water for injection, mixing is regulated pH to 2.5～10.5 after the high pressure homogenize breast is even, makes white emulsion liquid, filters, and fill, seals, sterilizes, promptly.
Above-mentioned astragalus glycoside fatty emulsion, wherein said astragaloside is 50%～100% extract for extract the purified astragaloside that contains in the Radix Astragali.
Above-mentioned astragalus glycoside fatty emulsion, wherein said grease separation is from soybean oil, Oleum Gossypii semen, safflower oil, fish oil, Oleum sesami, olive oil or MCT Oil, short-chain fatty acid triglyceride, or with the mixture of the aforementioned multiple oil for injection of any mixed.
Described astragalus glycoside fatty emulsion, wherein said oil is soybean oil.
Above-mentioned astragalus glycoside fatty emulsion, wherein said surfactant are phospholipid or non-ionic surface active agent Planck Buddhist nun 188F
68, or it is with the mixture of any mixed.
Described astragalus glycoside fatty emulsion, wherein said phospholipid is lecithin.
Described astragalus glycoside fatty emulsion, wherein said lecithin are Ovum Gallus domesticus Flavus lecithin or soybean lecithin.
Above-mentioned astragalus glycoside fatty emulsion, wherein said suitable cosolvent is to be selected from methanol, ethanol, 1,2-propylene glycol, glycerol, Polyethylene Glycol, benzyl alcohol, ethyl lactate, ethyl oleate or benzyl benzoate, or with the mixture of the aforementioned multiple cosolvent of any mixed.
Above-mentioned astragalus glycoside fatty emulsion, described isoosmotic adjusting agent are glycerol, mannitol, xylitol, sorbitol or glucose, or with the mixture of the aforementioned multiple isoosmotic adjusting agent of any mixed.
Described astragalus glycoside fatty emulsion, wherein said isoosmotic adjusting agent is a glycerol.
The invention has the advantages that:
1. astragalus glycoside fatty emulsion of the present invention, its raw material astragaloside are that the patent No. that the applicant has authorized is the patented product of " 0213798.3 ", and the release of novel formulation provides a kind of brand-new route of administration for the clinical application of astragaloside.
2. astragalus glycoside fatty emulsion of the present invention is a kind of oil-in-water emulsion, and astragaloside is dispersed in the oil phase, and divided dose is accurate, slowly discharges in blood behind the intravasation, so alleviated zest to blood vessel greatly.
3. the present invention is directed to astragaloside and be insoluble in water, in water, easily separate out crystalline characteristics, it is scattered in the oil, make oil-in-water emulsion, improved product stability greatly, guaranteed clinical application safety and effectiveness.
4. the preparation technology advanced person of this product, reliable, breast grain particle diameter is 0.05～10um in the medicament, drug loading is bigger, and the particle diameter of may command Emulsion and particle size distribution rheological properties, the character that can change the electrochemical properties control Emulsion on Emulsion surface to a certain extent adapts to clinical needs, and the change size makes it bring into play its targeting to improve clinical efficacy at different focuses.
5. this product has characteristics such as preparation technology is simple, ripe, suitable suitability for industrialized production.
The specific embodiment:
Embodiment one
Under nitrogen protection, take by weighing soybean oil 30g, be heated to 40 ℃, under high-speed stirred, add Ovum Gallus domesticus Flavus lecithin 1g, astragaloside 0.001g, stir as oil phase.Glycerol for injection 1g is added in the 600ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 3.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment two
Under nitrogen protection, take by weighing soybean oil 50g, be heated to 60 ℃, under high-speed stirred, add Ovum Gallus domesticus Flavus lecithin 10g, astragaloside 1g, stir as oil phase.Glycerol for injection 20g is added in the 600ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 5.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment three
Under nitrogen protection, take by weighing Oleum sesami 100g, be heated to 50 ℃, under high-speed stirred, add Ovum Gallus domesticus Flavus lecithin 12.5g, astragaloside 0.5g, stir as oil phase.Glycerol for injection 22.5g is added in the 500ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 8.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment four
Under nitrogen protection, take by weighing fish oil 200g, be heated to 80 ℃, under high-speed stirred, add Planck Buddhist nun 188F
685g, astragaloside 2g stir as oil phase.Glucose 50g is added in the 550ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 4.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment five
Under nitrogen protection, take by weighing Oleum Gossypii semen 300g, be heated to 80 ℃, under high-speed stirred, add lecithin 3g, Planck Buddhist nun 188F
685g, astragaloside 20g, ethanol 50g stir as oil phase.Mannitol 30g is added in the 500ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 7.5, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment six
Under nitrogen protection, take by weighing safflower oil 500g, be heated to 30 ℃, under high-speed stirred, add soybean lecithin 10g, Planck Buddhist nun 188F
681g, astragaloside 15g, propylene glycol 10g stir as oil phase.Xylitol 100g is added in the 300ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 9.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment seven
Under nitrogen protection, take by weighing short-chain fatty acid triglyceride 100g, be heated to 35 ℃, under high-speed stirred, add Ovum Gallus domesticus Flavus lecithin 12g, astragaloside 0.5g, stir as oil phase.Glycerol 22.5g is added in the 600ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 7.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment eight
Under nitrogen protection, take by weighing MCT Oil 50g, be heated to 55 ℃, under high-speed stirred, add Ovum Gallus domesticus Flavus lecithin 45g, astragaloside 5g, stir as oil phase.Sorbitol 25g is added in the 700ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 10.5, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment nine
Under nitrogen protection, take by weighing soybean oil 50g, safflower oil 50g, mixing is heated to 90 ℃, under high-speed stirred, adds soybean lecithin 15g, astragaloside 1g, stirs as oil phase.Glucose 100g is added in the 500ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 4.5, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment ten
Under nitrogen protection, take by weighing olive oil 450g, be heated to 60 ℃, under high-speed stirred, add phosphatidase 15 0g, astragaloside 15g, ethyl oleate 5g, stir as oil phase.Glucose 50g, glycerol 15g are added in the 300ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 6.5, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Embodiment 11
Under nitrogen protection, take by weighing soybean oil 100g, be heated to 50 ℃, under high-speed stirred, add phosphatidase 11 5g, astragaloside 2.5g, benzyl benzoate 3g, ethanol 12g, stir as oil phase.Glycerol 20g is added in the 500ml water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water.Under high-speed stirred, oil phase is added aqueous phase and make colostrum.Add the injection water to 1000ml, regulate pH to 7.0, even through the high pressure homogenizer breast, make white emulsion liquid, filter, fill, seal, sterilize, promptly.
Claims (12)
1. astragalus glycoside fatty emulsion, it is characterized in that: the principal agent astragaloside adds adjuvant and makes astragalus glycoside fatty emulsion, described adjuvant has oil, surfactant, isoosmotic adjusting agent and suitable cosolvent, its each component percentages (g/ml) is respectively astragaloside 0.0001～2%, oil 3～50%, surfactant 0.5～5%, isoosmotic adjusting agent 0.05～5%, cosolvent 0～5%, and surplus is a water for injection.
2. astragalus glycoside fatty emulsion according to claim 1, wherein said astragaloside is 50%～100% extract for extract the purified astragaloside that contains in the Radix Astragali.
3. astragalus glycoside fatty emulsion according to claim 1, wherein said grease separation is from soybean oil, Oleum Gossypii semen, safflower oil, fish oil, Oleum sesami, olive oil or MCT Oil, short-chain fatty acid triglyceride, or with the mixture of the aforementioned multiple oil for injection of any mixed.
4. astragalus glycoside fatty emulsion according to claim 3, wherein said oil is soybean oil.
5. astragalus glycoside fatty emulsion according to claim 1, wherein said surfactant are phospholipid or non-ionic surface active agent Planck Buddhist nun 188F
68, or it is with the mixture of any mixed.
6. astragalus glycoside fatty emulsion according to claim 5, wherein said phospholipid is lecithin.
7. astragalus glycoside fatty emulsion according to claim 6, wherein said lecithin are Ovum Gallus domesticus Flavus lecithin or soybean lecithin.
8. astragalus glycoside fatty emulsion according to claim 1, wherein said suitable cosolvent is to be selected from methanol, ethanol, 1,2-propylene glycol, glycerol, Polyethylene Glycol, benzyl alcohol, ethyl lactate, ethyl oleate or benzyl benzoate, or with the mixture of the aforementioned multiple cosolvent of any mixed.
9. astragalus glycoside fatty emulsion according to claim 1, wherein said isoosmotic adjusting agent are glycerol, mannitol, xylitol, sorbitol or glucose, or with the mixture of the aforementioned multiple isoosmotic adjusting agent of any mixed.
10. astragalus glycoside fatty emulsion according to claim 9, wherein said isoosmotic adjusting agent is a glycerol.
11. the preparation technology of astragalus glycoside fatty emulsion according to claim 1, it is characterized in that: under inert gas shielding, take by weighing oil for injection, be heated to 30～100 ℃, under high-speed stirred, surfactant and astragaloside are added in the oil for injection, stir as oil phase; In addition isoosmotic adjusting agent is added in the proper amount of water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water; Under high-speed stirred, oil phase is mixed with water and continue high-speed stirred and make colostrum, add to the full amount of water for injection, mixing is regulated pH to 2.5～10.5 after the high pressure homogenize breast is even, makes white emulsion liquid, filters, and fill, seals, sterilizes, promptly.
12. the preparation technology of astragalus glycoside fatty emulsion according to claim 11, it is characterized in that: under inert gas shielding, take by weighing oil for injection, be heated to 30～100 ℃, under high-speed stirred, surfactant, astragaloside and cosolvent are added in the oil for injection, stir as oil phase; In addition isoosmotic adjusting agent is added in the proper amount of water for injection, behind the mixing with the membrane filtration of 0.45 μ m as water; Under high-speed stirred, oil phase is mixed with water and continue high-speed stirred and make colostrum, add to the full amount of water for injection, mixing is regulated pH to 2.5～10.5 after the high pressure homogenize breast is even, makes white emulsion liquid, filters, and fill, seals, sterilizes, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CNB2005100386510A CN100366260C (en) | 2005-04-01 | 2005-04-01 | Astragalus glycoside fatty emulsion and its preparation technology |
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| Application Number | Priority Date | Filing Date | Title |
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| CNB2005100386510A CN100366260C (en) | 2005-04-01 | 2005-04-01 | Astragalus glycoside fatty emulsion and its preparation technology |
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| CN1686155A true CN1686155A (en) | 2005-10-26 |
| CN100366260C CN100366260C (en) | 2008-02-06 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102793730A (en) * | 2012-08-31 | 2012-11-28 | 山西普德药业股份有限公司 | Ginkgo-damole medicinal composition and preparation method thereof |
| CN108478525A (en) * | 2018-04-02 | 2018-09-04 | 青岛科技大学 | One kind having highly-water-soluble and high stable type Astragaloside IV eye drops and preparation method thereof |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4104817A1 (en) * | 2021-06-17 | 2022-12-21 | Skeye Pharma GbR | Ophthalmic composition comprising astragaloside iv |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1543976A (en) * | 2003-11-27 | 2004-11-10 | 上海博泰医药科技有限公司 | Astragaloside injection preparation and its preparing process |
-
2005
- 2005-04-01 CN CNB2005100386510A patent/CN100366260C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102793730A (en) * | 2012-08-31 | 2012-11-28 | 山西普德药业股份有限公司 | Ginkgo-damole medicinal composition and preparation method thereof |
| CN102793730B (en) * | 2012-08-31 | 2013-11-06 | 山西普德药业股份有限公司 | Ginkgo-damole medicinal composition and preparation method thereof |
| CN108478525A (en) * | 2018-04-02 | 2018-09-04 | 青岛科技大学 | One kind having highly-water-soluble and high stable type Astragaloside IV eye drops and preparation method thereof |
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| CN100366260C (en) | 2008-02-06 |
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Owner name: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. Free format text: FORMER NAME: JIANGSU ZHENGDA TIANQING PHARMACEUTICAL CO., LTD. |
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Address after: 222006 Sinpo City, Lianyungang Province, North Road, No. 8, No. Patentee after: Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Address before: 222006 Sinpo City, Lianyungang Province, North Road, No. 8, No. Patentee before: Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd. |
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Effective date of registration: 20160304 Address after: 223001 No. 9 HANKOOK North Road, Jiangsu, Huaian Patentee after: Jiangsu Chiatai Qingjiang Pharmaceutical Co., Ltd. Address before: 222006 Sinpo City, Lianyungang Province, North Road, No. 8, No. Patentee before: Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
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Granted publication date: 20080206 Termination date: 20180401 |