CN1562147A - Radix scutellariae extract freeze-dried powder injection and its preparing method - Google Patents
Radix scutellariae extract freeze-dried powder injection and its preparing method Download PDFInfo
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- CN1562147A CN1562147A CN 200410017147 CN200410017147A CN1562147A CN 1562147 A CN1562147 A CN 1562147A CN 200410017147 CN200410017147 CN 200410017147 CN 200410017147 A CN200410017147 A CN 200410017147A CN 1562147 A CN1562147 A CN 1562147A
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- baicalin
- radix scutellariae
- powder injection
- lyophilized powder
- extract
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Abstract
A freeze-dried powder injection of the mixture of scutellarin and scutelloside extracted from scutellaria root features high stability. Its preparing process is also disclosed.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, lyophilized powder injection of baikal skullcap root extract that specifically from Radix Scutellariae, extracts and preparation method thereof.
Background technology
Baikal skullcap root (Scutellaria baicalensis Georgi) is the root of labiate Radix Scutellariae, has heat clearing and damp drying, effects such as eliminating fire and detoxication, arresting bleeding and miscarriage prevention.
Baicalin (Baicalein), baicalin (Baicalin) are the extracts that extracts from the Radix Scutellariae dried roots, have definite chemical constitution, and its structural formula is:
Discovering in recent years, effects, particularly baicalin such as that these two Radix Scutellariae extracts have is antibiotic, antiviral have more the hepatic cholagogic diuresis, remove free radical and antioxidation, anticoagulation and antithrombotic form, suppress the pancreatin activity, to the pharmacological actions such as expression of biomembranous effect, anticancer, dual regulation effect, hypotensive activity, inhibition adhesion molecule to smooth muscle.
Baicalin is used for clinical with the dosage form of tablet and aqueous injection for many years.But baicalin because of water insoluble or in alkaline solution reason such as instability, never a sophisticated dosage form is used clinically.
As everyone knows, need onset after gastrointestinal absorbs after tablet is oral, onset time is long, absorbs also incomplete, can not be used for emergent treatment, and the Chinese medicine aqueous injection, because Chinese medicine is purified and is restricted complicated component, when depositing, be prone to degradation quality problems under oxidation precipitation and color change, the pH value, more seriously influence the safety of medicine, thereby the influence treatment also can cause some malpracticees sometimes.
Summary of the invention
The objective of the invention is to overcome the deficiency that exists in the existing Chinese medicine preparation technology, solved the problem that Radix Scutellariae extract can't be made injection.
But the invention provides the direct administration of a kind of vein, steady quality, safety, drug effect pharmaceutical dosage form rapidly, i.e. the lyophilized injectable powder of Radix Scutellariae extract, also provide simultaneously a kind of can be in the preparation technology of industrial production in enormous quantities.
The invention discloses a kind of lyophilized powder injection of baikal skullcap root extract, form (percentage by weight) by following component:
Radix Scutellariae extract 22-80%
Alkalescence lytic agent 11-75%
Antioxidant, chelating agent 1-12%
Filler 1-30%
Wherein said Radix Scutellariae extract is baicalin monomer, baicalin monomer or both mixture.Said baicalin monomer, the monomeric purity of baicalin are all more than 85%, and the component total content of the two mixture also should be more than 85%.
The percentage by weight of wherein said baicalin and baicalin mixture is 1: 0.6-1.8 was good with 1: 1.
Wherein said alkaline lytic agent is the acceptable inorganic bases of all pharmacy, as NaOH, NH
3Organic base is as the citric acid trisodium; Basic amino acid is as arginine; Strong base-weak acid salt is as Na
2CO
3Deng.
Wherein antioxidant is organic antioxidant, as sodium ascorbate, arginine or inorganic antioxidant such as sodium thiosulfate etc., and preferred arginine; Chelating agent is EDTA disodium, EDTA four sodium, arginine etc.
Wherein filler is mannitol, lactose, glucosan, inositol, meglumine and glucose.Preferred mannitol is as filler.
Above-mentioned alkaline lytic agent, antioxidant, chelating agent, more than one mix use but filler all can be selected for use also separately.
Though baicalin has extraordinary pharmacological action, because it is water insoluble, and unstable in alkaline solution, brought very big obstacle to clinical application.The inventor is through test of many times, under MIN alkali condition, rationally select one or more for use or have the adjuvant of alkalescence dissolving, antioxygen Stabilization concurrently, and utilize the similar principle that mixes dexterously, promptly utilize baicalin easily molten characteristic in water, further increase the dissolubility of baicalin, and be equipped with antioxidant stabilizer, fine solved baicalin in water insoluble and in alkaline aqueous solution problem of unstable, make the problem be difficult to make injection baicalin, injection baicalin baicalin mixture freeze-dried powder be able to perfect the solution.
The invention provides a kind of method for preparing lyophilized powder injection of baikal skullcap root extract, may further comprise the steps:
A) in alkaline lytic agent solution, add antioxidant, raw material respectively after ultrasound wave or the heating deoxygenation, stir, heat, dissolve, regulate pH then
B) add filler, chelating agent
C) depyrogenation
D) aseptic filtration, fill
E) vacuum lyophilization
F) gland, packing
Below describe preparation method of the present invention in detail:
Radix Scutellariae extract dissolubility under alkali condition is better, can not add other cosolvents.In water for injection, add alkaline lytic agent, after ultrasonic Treatment or heating deoxygenation, add antioxidant such as sodium ascorbate, arginine or sodium thiosulfate, and an amount of injection Radix Scutellariae extract, agitating heating, heating-up temperature is 60-80 ℃, and the time is 10-30 minute, makes it whole dissolvings, transfer pH to 8.0-11.0, if alkalescence is strong excessively, vial there is infection, influential to Radix Scutellariae extract active ingredient structure.Adding filler commonly used then, as mannitol, lactose, glucosan, meglumine, inositol and glucose etc., but is good with mannitol.Add chelating agent, as EDTA disodium, EDTA four sodium, arginine etc. are used for the metal ion of complex solution.More than one mix use but the above pin that reaches can be selected for use also respectively separately with filler, antioxidant, chelating agent.Add to the full amount of water for injection.Add solution weight 0.05-1.0% pin activated carbon, under 50-90 ℃ temperature, heated while stirring 10-50 minute, adopting activated carbon to adsorb pyrogen is effective method, but activated carbon has adsorption to Radix Scutellariae extract, therefore to control certain ratio, measure low absorption pyrogen and do not reach requirement, measure too high too high Radix Scutellariae extract absorption, through test of many times, it is proper that the use amount of activated carbon is controlled at 0.05-1.0%.Be 0.22 micron filtering with microporous membrane then with the aperture.Remove thermal source and molecule, fill is in 10-20 milliliter bottle under aseptic condition for filtrate, and every loading amount is the 2.0-4.0 milliliter, the vacuum freeze drier vacuum freeze-drying, and the gland packing promptly obtains lyophilized powder injection of baikal skullcap root extract.Through check, every index of the lyophilized powder injection of baikal skullcap root extract for preparing with preparation technology of the present invention all meets the requirements.
Lyophilized powder injection of baikal skullcap root extract active ingredient purity height provided by the present invention, determined curative effect can be used for intravenously administrable.And have good stability, and steady quality, its pH value, color, clarity do not change, and are convenient to keeping, deposit and advantage such as transportation.
The specific embodiment
Embodiment 1:
Make 10% aqueous solution with medicinal L-arginine and water for injection, after the ultrasound wave deoxygenation, get 1000ml, add injection baicalin 33g, agitating heating makes it dissolving for 60 ℃, continue to add filler mannitol 6g, it is an amount of to add needle-use activated carbon then, and 60 ℃ were stirred 30 minutes, after the filtration of No. 4 core rods, there is not Mycoderma pressure filtration with 0.22 μ ф 300mm, after prediction content and pyrogen are qualified, aseptic subpackaged in the 10ml cillin bottle, every bottle of about 2ml of packing, carry out lyophilization then, make 500 bottles of finished products, every bottle of specification is for containing the 60mg baicalin.
Embodiment 2:
Make 0.6% aqueous solution with analytical pure sodium hydroxide and water for injection, get 1000ml through the ultrasound wave deoxygenation, add sodium ascorbate 5g, add injection baicalin 16.5g and scutelloside for injection 16.5g then, agitating heating makes it dissolving for 80 ℃, it is an amount of to add needle-use activated carbon then, 80 ℃ were stirred 20 minutes, after filtering with No. 4 core rods, did not have Mycoderma pressure filtration with 0.22 μ ф 300mm, after prediction content and pyrogen are qualified, aseptic subpackaged in the 10ml cillin bottle, every bottle of about 2ml of packing carries out lyophilization then, make 500 bottles of finished products, every bottle of specification is for containing 60mg Radix Scutellariae extract (each 30mg of baicalin and baicalin).
Embodiment 3:
Make 15% aqueous solution with medicinal arginine and water for injection, get 1000ml through the ultrasound wave deoxygenation, add sodium ascorbate 5g, after the EDTA disodium 0.5g dissolving, add injection baicalin 33g and scutelloside for injection 33g then, agitating heating makes it dissolving for 70 ℃, it is an amount of to add needle-use activated carbon then, 90 ℃ were stirred 10 minutes, after filtering with No. 4 core rods, did not have Mycoderma pressure filtration with 0.22 μ ф 300mm, after prediction content and pyrogen are qualified, aseptic subpackaged in the 20ml cillin bottle, every bottle of about 4ml of packing carries out lyophilization then, make 500 bottles of finished products, every bottle of specification is for containing 120mg Radix Scutellariae extract (each 60mg of baicalin and baicalin).
Embodiment 4:
Make 1% aqueous solution with analytical pure sodium carbonate and water for injection, get 1000ml through the heating deoxygenation, add sodium thiosulfate 5g, after the EDTA disodium 0.5g dissolving, add scutelloside for injection 66g then, agitating heating makes it dissolving for 60 ℃, add filler lactose 6 grams, it is an amount of to add needle-use activated carbon then, and 50 ℃ were stirred 50 minutes, after the filtration of No. 4 core rods, there is not Mycoderma pressure filtration with 0.22 μ ф 300mm, after prediction content and pyrogen are qualified, aseptic subpackaged in the 20ml cillin bottle, every bottle of about 4ml of packing, carry out lyophilization then, make 500 bottles of finished products, every bottle of specification is for containing the 120mg baicalin.
Claims (9)
1. lyophilized powder injection of baikal skullcap root extract, form (percentage by weight) by following component:
Radix Scutellariae extract 22-80%;
Alkalescence lytic agent 11-75%;
Antioxidant, chelating agent 1-12%;
Filler 1-30%.
2. lyophilized powder injection of baikal skullcap root extract as claimed in claim 1 is characterized in that described Radix Scutellariae extract is a baicalin.
3. lyophilized powder injection of baikal skullcap root extract as claimed in claim 1 is characterized in that described Radix Scutellariae extract is a baicalin.
4. lyophilized powder injection of baikal skullcap root extract as claimed in claim 1 is characterized in that described Radix Scutellariae extract is the mixture of baicalin and baicalin.
5. lyophilized powder injection of baikal skullcap root extract as claimed in claim 4, the percentage by weight that it is characterized in that described baicalin and baicalin is 1: 0.6-1.8.
6. as claim 4 or 5 described lyophilized powder injection of baikal skullcap root extract, the percentage by weight that it is characterized in that described baicalin and baicalin is 1: 1.
7. Radix Scutellariae extract freeze-dried powder as claimed in claim 1 is characterized in that described alkaline lytic agent arginine, NaOH, Na
2CO
3, NH
3, the citric acid trisodium; Described antioxidant is sodium ascorbate, arginine, sodium thiosulfate; Described chelating agent is EDTA disodium, EDTA four sodium, arginine; Described filler is mannitol, lactose, glucosan, inositol, meglumine and glucose.
8. as claim 1 or 7 described Radix Scutellariae extract freeze-dried powders, it is characterized in that described alkaline lytic agent is an arginine.
9. method for preparing lyophilized powder injection of baikal skullcap root extract may further comprise the steps:
A) in alkaline lytic agent solution, add antioxidant, raw material after ultrasound wave or the heating deoxygenation, stir, heat, dissolve, regulate pH then
B) add filler, chelating agent
C) depyrogenation
D) aseptic filtration, fill
E) vacuum lyophilization
F) gland, packing
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410017147 CN1562147A (en) | 2004-03-24 | 2004-03-24 | Radix scutellariae extract freeze-dried powder injection and its preparing method |
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|---|---|---|---|
| CN 200410017147 CN1562147A (en) | 2004-03-24 | 2004-03-24 | Radix scutellariae extract freeze-dried powder injection and its preparing method |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1330312C (en) * | 2005-06-27 | 2007-08-08 | 宛六一 | Baicalin soft capsule and preparation method thereof |
| CN102247329A (en) * | 2010-05-19 | 2011-11-23 | 昆明制药集团股份有限公司 | 5,6,7,4'-tetrahydroxyflavone powder injection and preparation method thereof |
| CN101088523B (en) * | 2006-06-12 | 2012-08-22 | 北京五和博澳医药科技发展有限公司 | Nanometer solid lipid particle of active skullcap components and its prepn process and prepn |
| CN104258402B (en) * | 2014-09-28 | 2017-01-11 | 青岛橡胶谷知识产权有限公司 | Wogonin composition and preparation method thereof |
| CN108992672A (en) * | 2017-06-07 | 2018-12-14 | 山东丹红制药有限公司 | A kind of wogonin pharmaceutical composition for treating neoplastic disease |
-
2004
- 2004-03-24 CN CN 200410017147 patent/CN1562147A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1330312C (en) * | 2005-06-27 | 2007-08-08 | 宛六一 | Baicalin soft capsule and preparation method thereof |
| CN101088523B (en) * | 2006-06-12 | 2012-08-22 | 北京五和博澳医药科技发展有限公司 | Nanometer solid lipid particle of active skullcap components and its prepn process and prepn |
| CN102247329A (en) * | 2010-05-19 | 2011-11-23 | 昆明制药集团股份有限公司 | 5,6,7,4'-tetrahydroxyflavone powder injection and preparation method thereof |
| CN102247329B (en) * | 2010-05-19 | 2014-02-05 | 昆明制药集团股份有限公司 | 5,6,7,4'-tetrahydroxyflavone powder injection and preparation method thereof |
| CN104258402B (en) * | 2014-09-28 | 2017-01-11 | 青岛橡胶谷知识产权有限公司 | Wogonin composition and preparation method thereof |
| CN108992672A (en) * | 2017-06-07 | 2018-12-14 | 山东丹红制药有限公司 | A kind of wogonin pharmaceutical composition for treating neoplastic disease |
| CN108992672B (en) * | 2017-06-07 | 2022-08-09 | 山东丹红制药有限公司 | Wogonin pharmaceutical composition for treating tumor |
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