CN1634099A - Swerianmarin injectio, its preparation process and application - Google Patents
Swerianmarin injectio, its preparation process and application Download PDFInfo
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- CN1634099A CN1634099A CN 200310121024 CN200310121024A CN1634099A CN 1634099 A CN1634099 A CN 1634099A CN 200310121024 CN200310121024 CN 200310121024 CN 200310121024 A CN200310121024 A CN 200310121024A CN 1634099 A CN1634099 A CN 1634099A
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- injection
- swertiamarin
- pharmaceutic adjuvant
- hepatitis
- filtering
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Abstract
The invention discloses a Swerianmarin injection, its preparation process and application, wherein the preparing process comprises using Gentianaceae, Scrophulariaceae or Oleaceae plants as raw material, employing conventional phytochemical method for extraction, segregation and purification, thus obtaining swertiamarin, weighing swertiamarin and medicinal adjuvant, charging water for injection, thermal insulating 10-20 minutes at 30-60 deg. C, cooling down, filtering, dispensing the filter liquor 1-48 hours at 0-5 deg. C, filtering, encapsulating, drying in frozen, sterilizing, and packaging.
Description
Technical field
The present invention relates to pharmaceutical preparation and its production and application.
Background technology
Hepatitis is a kind of self-limited disease, gets suitable treatment and recuperation is provided after being ill, and the most applications lower body can obtain immunity and fully recover.But, acute attack stage in the acute stage or the chronic hepatitis of seizure of disease, malpractice or other reasons cause that sb.'s illness took a turn for the worse or delay, can make the immune antibody of virus tolerance body, hide body to the removing of virus or slow down the removing speed of virus, increase the incidence rate of chronic hepatitis, thereby cause diseases such as liver cirrhosis, hepatocarcinoma, bring lifelong misery to the patient.So hepatitis is viral hepatitis particularly, the early treatment is very crucial, important.
China's hepatitis has 2,800 ten thousand chronic hepatitis patients, account for 50% of whole world sum, simultaneously China 100,000,000 people that have an appointment are hepatitis B virus or other types infectious hepatitis virus carrier, and only the baby of infective virus hepatitis just has an appointment 800,000 every year by mother-to-baby transmission.Therefore, China is the severely afflicated area of hepatitis, and viral hepatitis is the pernicious infectious disease that seriously jeopardizes China people health and lives, and its sickness rate occupy the 3rd in Notifiable disease, is only second to flu and diarrhoea.At present, for chronic hepatitis particularly the compound hepatitis of chronic hepatitis B and multiple cross infection still do not have specific drug.
Summary of the invention
The objective of the invention is at the deficiencies in the prior art, a kind of swertiamarin (swertiamarin) injection is provided.
Another object of the present invention provides the preparation method of described swertiamarin injection.
Simultaneously, the present invention also aims to the application of described swertiamarin injection in pharmacy.
Purpose of the present invention is achieved by following technical proposals.
The invention provides a kind of swertiamarin (having another name called swertiamarin, swertiamarin, swertiamarin) injection, this injection contains following composition by weight percentage: swertiamarin 50%～100% has reached the pharmaceutic adjuvant 0～50% of hydrotropy effect (or having antioxidant effect or the effect of skeleton proppant).Used its content of swertiamarin raw material of related injection should be greater than 90% among the present invention, and other impurity should be less than 10%.
Wherein, the described adjuvant that has played hydrotropy effect or skeleton proppant is selected from a kind of in mannitol, glucose, polyvidon, lactose or the glycine or their mixture.
The adjuvant of described Stabilization (or antioxidation) is selected from a kind of of vitamin C, sodium sulfite, sodium sulfite, sodium pyrosulfate or sodium thiosulfate, or their mixture.
Described injection is the above injection, an injection powder injection dosage form of any pharmaceutics.
Swertiamarin injection provided by the invention causes the application in the medicine of pain as preparation treatment or prevention viral hepatitis, the damaging hepatitis of medicine (chemistry), cholecystitis and cramps of gastrointestinal tract.Its effective dosage scope is 0.5mg to 50mg for per kilogram of body weight every day.Its medication preferred dose per kilogram of body weight every day is 15 ± 10mg.
The invention provides a kind of preparation method of swertiamarin injection, this method adopts the step of following order:
(1) take by weighing swertiamarin and pharmaceutic adjuvant, and add water for injection, be incubated 10～20 minutes down at 30 ℃～60 ℃, cooling is filtered;
(2) filtrate was placed 1～48 hour down at 0 ℃～5 ℃, filter, and embedding or embedding lyophilization, sterilization, packing is required swertiamarin injection.
Wherein, described filtration is based on the microporous filter membrane (molecular cut off is greater than 100,000), ultrafilter membrane (molecular cut off 5000 to 100,000), NF membrane (molecular cut off 500-5000) of molecular sieve principle design to remove thermal source and contaminant particles.
The present invention has carried out following pharmacodynamics test to described swertiamarin injection.
A. function for protecting liver and reducing enzyme activity
1. the swertiamarin injection is to the protective effect of hepatic injury due to the D-Gal amine (D-GalN)
(1) pharmacological model commonly used is that heavy dose of D-Gal amine (D-GalN) can cause serious acute hepatocyte injury in the present hepatitis medicament research of principle, and its liver histopathology feature is very similar to human virus's hepatitis.Serum aminotransferase activity is the sensitive indicator of hepatocellular damage, and is proportionate with the hepatocyte injury degree.The protective effect of this experiment test D-Gal amine (D-GalN) induced mice acute liver damage.
(2) method acute liver damage: mice (18-22g) lumbar injection D-GalN (600mg/kg)/LPS (10 μ g/kg).Normal control group (10): respectively at experiment preceding 18 hours and intravenous injection in 2 hours and intraperitoneal injection of saline.Poisoning group (10): respectively at experiment preceding 18 hours and 2 hours intravenous injection normal saline, lumbar injection D-GalN (700mg/kg)/LPS during experiment (10 μ g/kg).
Low dose of administration group (10,10mg/kg): respectively at experiment preceding 18 hours and 2 hours intravenous drug samples, lumbar injection D-GalN (700mg/kg)/LPS during experiment (10 μ g/kg).
Middle dosed administration group (10,20mg/kg): respectively at experiment preceding 18 hours and 2 hours intravenous drug samples, lumbar injection D-GalN (700mg/kg)/LPS during experiment (10 μ g/kg).
Heavy dose of administration group (10,40mg/kg): respectively at experiment preceding 18 hours and 2 hours intravenous drug samples, lumbar injection D-GalN (700mg/kg)/LPS during experiment (10 μ g/kg).
The mensuration of ALT: lumbar injection D-GalN (700mg/kg)/LPS (10 μ g/kg) measured mice ALT level in back 8 hours.Result of the test sees Table 1.
Table 1.
| Group | Dosage (mg/kg) | ALT level (U/1) | The ALT level reduces (%) |
| The normal control group | ????-- | ????58±21 | ????-- |
| The poisoning group | ????-- | ????2351±820 | ????-- |
| Swertiamarin | ????10 ????20 ????40 | ????1025±230 ????1352±320 ????1512±280 | ????62 ????48 ????35 |
Result of the test shown in the table 1 shows that hepatic injury has significant protective effect to the swertiamarin injection to the D-GalN/LPS induced mice, and medicine and therapeutic effect are dependence.
B. the swertiamarin injection is to the protective effect of digitophyllin poisoning mice liver detoxification function
4 groups of mices, 10 every group, gave mouse mainline swertiamarin injection 15mg/kg/ days, for three days on end, gave and digitalin 20mg/kg in the 4th day, give for three days on end then and swertiamarin injection 15mg/kg/ days.The result: matched group (injecting normal saline) mice 20 has 12 death, and 20 mices of administration group have 5 death.This injection of test explanation can be strengthened the mouse liver function of detoxification.
C. toxicity test
1. acute toxicity
3 groups of mices (18-22g), 10 every group, swertiamarin injection 1000mg/kg intravenously administrable does not have dead the generation in three days, and mice is movable normal, does not have obvious poisoning symptom.
2. long term toxicity
5 groups of rats (120-150g), 10 every group, swertiamarin injection 50mg/kg/ days, connect continuous 30 days of intraperitoneal administration, rat does not have dead the generation, and is movable normal, there is not obvious poisoning symptom, internal organs and body weight change and matched group zero differences such as the rat heart, lung, liver yet.
In sum, the present invention has following beneficial effect:
1. be raw material with the natural plants, medicine resource is abundant, and toxic and side effects is little, and is safe in utilization.
2. drug administration by injection, the bioavailability height.Treat at the acute stage of the state of an illness or the acute attack stage of chronic disease, the hepatitis of substance metabolism imbalance is particularly important for this.
Obviously transaminase lowering, resist hepatic injury, improve the liver microcirculation disturbance, promote liver cell regeneration, recover the hepatic tissue normal configuration, strengthen immunity of organism and rebuild.Point out it that virus, hepatitis that medicine, chemicals caused are all had therapeutical effect.This poisonous side effect of medicine is little, and is safe in utilization.Can be used for the symptomatic treatment that various acute and chronic viral hepatitis, medicine and chemicals cause hepatitis clinically.Simultaneously, it can also increase bile secretion, treatment cholecystitis and alleviation cramps of gastrointestinal tract.
The specific embodiment
By specific embodiment given below, can further be well understood to the present invention.But they are not limitation of the invention.
Embodiment 1
Take by weighing swertiamarin 100g, mannitol 50g adds water for injection 3000ml, make dissolving, be incubated 20 minutes down, be cooled to room temperature at 40 ℃～45 ℃, add injection and be diluted with water to 5000ml, filtrate was placed 0.45 μ m filtering with microporous membrane 12 hours down at 0 ℃～5 ℃; Water for injection is diluted to 10000ml, 0.2 μ m filtering with microporous membrane, and embedding (5ml/ bottle), lyophilization, radiation sterilization, packing gets final product.
Embodiment 2
Take by weighing swertiamarin 100g, each 20g of mannitol and vitamin C adds water for injection 5000ml, makes dissolving, is incubated 20 minutes down at 45 ℃～50 ℃, cooling, 0.45 μ m filtering with microporous membrane; Filtrate was placed 24 hours down at 0 ℃～5 ℃, and water for injection is diluted to 10000ml, 0.2 μ m filtering with microporous membrane, and ultrafiltration membrance filter (molecular cut off 10,000), embedding (5ml/ bottle), lyophilization, packing gets final product.
Embodiment 3
Take by weighing swertiamarin 100g, mannitol 100g adds water for injection 5000ml, make dissolving, be incubated 20 minutes down, cooling at 40 ℃～45 ℃, 0.45 μ m filtering with microporous membrane, 0.2 μ m filtering with microporous membrane, filtrate was placed 24 hours down at 0 ℃～5 ℃, water for injection is diluted to 10000ml, 0.1 μ m filtering with microporous membrane, ultrafiltration membrance filter (molecular cut off 6000), embedding (5ml/ bottle), lyophilization, packing gets final product.
Embodiment 4
Take by weighing swertiamarin 100g, glucose 50g adds water for injection 3000ml, make dissolving, be incubated 20 minutes down, be cooled to room temperature at 40 ℃～45 ℃, add injection and be diluted with water to 5000ml, filtrate was placed 0.45 μ m filtering with microporous membrane 12 hours down at 0 ℃～5 ℃; Water for injection is diluted to 10000ml, 0.2 μ m filtering with microporous membrane, and embedding (5ml/ bottle), radiation sterilization, packing gets final product.
Embodiment 5
Take by weighing swertiamarin 100g, dextran 50g adds water for injection 3000ml, make dissolving, insulation is 20 minutes under 40 ℃～45 ℃ temperature, is cooled to room temperature, add injection and be diluted with water to 5000ml, filtrate was placed 0.45 μ m filtering with microporous membrane 12 hours down at 0-5 ℃; Water for injection is diluted to 10000ml, 0.2 μ m filtering with microporous membrane, and embedding (5ml/ bottle), lyophilization, radiation sterilization, packing gets final product.
Embodiment 6
Take by weighing swertiamarin 100g, each 20g of polyvidon and glycine adds water for injection 5000ml, makes dissolving, and insulation is 20 minutes under 45 ℃～50 ℃ temperature, cooling, 0.45 μ m filtering with microporous membrane; Filtrate was placed 24 hours down at 0 ℃～5 ℃, and water for injection is diluted to 10000ml, 0.2 μ m filtering with microporous membrane, and ultrafiltration membrance filter (molecular cut off 10,000), embedding (5ml/ bottle), lyophilization, packing gets final product.
Embodiment 7
Take by weighing swertiamarin 100g, carbamide 10g, glucose 20g, add water for injection 5000ml, make dissolving, insulation is 20 minutes under 40 ℃～45 ℃ temperature, cooling, 0.45 μ m filtering with microporous membrane, 0.2 μ m filtering with microporous membrane, filtrate was placed 24 hours down at 0 ℃～5 ℃, and water for injection is diluted to 10000ml, 0.1 μ m filtering with microporous membrane, ultrafiltration membrance filter (molecular cut off 6000), embedding (5ml/ bottle), lyophilization, packing gets final product.
Embodiment 8
Take by weighing swertiamarin 100g, the 1g vitamin C, 0.5g sodium sulfite, the 20g glucose adds water for injection 3000ml, make dissolving, insulation is 20 minutes under 40 ℃～45 ℃ temperature, is cooled to room temperature, adds injection and is diluted with water to 5000ml, filtrate was placed 12 hours down at 0 ℃～5 ℃, 0.45 μ m filtering with microporous membrane; Water for injection is diluted to 10000ml, 0.2 μ m filtering with microporous membrane, and embedding (5ml/ bottle), radiation sterilization, packing gets final product.
Claims (10)
1. a swertiamarin injection is characterized in that, contains following composition in this injection of dry product by weight percentage: swertiamarin raw material 50%～100%, pharmaceutic adjuvant 0～50%.
2. swertiamarin injection according to claim 1, greater than 90%, other impurity are less than 10% by its content of dry product for wherein said swertiamarin raw material.
3. swertiamarin injection according to claim 1, wherein said injection are the above injection, injection powder injection dosage forms of any pharmaceutics.
4. swertiamarin injection according to claim 1, wherein said pharmaceutic adjuvant comprise cosolvent and/or skeleton proppant, antioxidant.
5. swertiamarin injection pharmaceutic adjuvant according to claim 4, wherein said cosolvent or skeleton proppant are selected from a kind of in mannitol, lactose, glucose, dextran, polyvidon, glycine or the carbamide or their mixture.
6. swertiamarin injection pharmaceutic adjuvant according to claim 4, wherein said antioxidant are selected from a kind of in vitamin C, sodium sulfite, sodium sulfite, sodium pyrosulfate or the sodium thiosulfate or their mixture.
7. the preparation method of a swertiamarin injection, this method adopts the step of following order:
(1) is raw material with Gentianaceae, Scrophulariaceae or Oleaceae plant, adopts the extraction of phytochemistry conventional method, separation, purification, make swertiamarin;
(2) take by weighing swertiamarin and pharmaceutic adjuvant, and add water for injection, be incubated 10～20 minutes down at 30 ℃～60 ℃, cooling is filtered;
(3) filtrate was placed 1～48 hour down at 0 ℃～5 ℃, filter, and embedding or embedding lyophilization, sterilization, packing is required swertiamarin injection
8. the preparation method of swertiamarin injection according to claim 7, microporous filter membrane, ultrafilter membrane or NF membrane are adopted in wherein said filtration.
9. the swertiamarin injection is as the application in the medicine of preparation treatment or prevention liver and gall diseases, viral hepatitis or the damaging hepatitis of chemicals.
10. the application in the medicine of the pain that causes as preparation treatment or prevention cholecystitis and cramps of gastrointestinal tract of swertiamarin injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310121024 CN1634099A (en) | 2003-12-31 | 2003-12-31 | Swerianmarin injectio, its preparation process and application |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310121024 CN1634099A (en) | 2003-12-31 | 2003-12-31 | Swerianmarin injectio, its preparation process and application |
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| CN1634099A true CN1634099A (en) | 2005-07-06 |
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| CN 200310121024 Pending CN1634099A (en) | 2003-12-31 | 2003-12-31 | Swerianmarin injectio, its preparation process and application |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579564A (en) * | 2012-03-15 | 2012-07-18 | 中国科学院西北高原生物研究所 | Preparing method of Tibetan capillaris effective part extractives |
| CN104188994A (en) * | 2014-08-22 | 2014-12-10 | 中国人民解放军第三军医大学第一附属医院 | Application of swertiamarin serving as drug for treating cholestasis |
| CN110123744A (en) * | 2019-06-03 | 2019-08-16 | 齐齐哈尔医学院 | A kind of method and its application preparing erythricine injection using rough gentian as raw material |
-
2003
- 2003-12-31 CN CN 200310121024 patent/CN1634099A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579564A (en) * | 2012-03-15 | 2012-07-18 | 中国科学院西北高原生物研究所 | Preparing method of Tibetan capillaris effective part extractives |
| CN102579564B (en) * | 2012-03-15 | 2013-07-31 | 中国科学院西北高原生物研究所 | Preparing method of Tibetan capillaris effective part extractives |
| CN104188994A (en) * | 2014-08-22 | 2014-12-10 | 中国人民解放军第三军医大学第一附属医院 | Application of swertiamarin serving as drug for treating cholestasis |
| CN110123744A (en) * | 2019-06-03 | 2019-08-16 | 齐齐哈尔医学院 | A kind of method and its application preparing erythricine injection using rough gentian as raw material |
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