CN101129329A - Injection containing huperzine for sulci venosi and method of preparing the same - Google Patents
Injection containing huperzine for sulci venosi and method of preparing the same Download PDFInfo
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- CN101129329A CN101129329A CNA200710145475XA CN200710145475A CN101129329A CN 101129329 A CN101129329 A CN 101129329A CN A200710145475X A CNA200710145475X A CN A200710145475XA CN 200710145475 A CN200710145475 A CN 200710145475A CN 101129329 A CN101129329 A CN 101129329A
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- huperzine
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Abstract
The invention provides intravenous injections of Huperzine and process for preparation, which include the dose forms of injections, fluid infusions and freeze dried injections.
Description
Technical field
The invention belongs to medical technical field, specifically relate to a kind of used for intravenous injection medicine preparation and preparation method thereof, specifically huperzine A and with its can be salifiable acid injection, transfusion, freeze-dried powder and the manufacture method thereof formed.
Background technology
Huperzine A is extract from China's Chinese herbal medicine Herba Lycopodii serrati a kind of efficient, the maincenter acetylcholinesteraseinhibitors inhibitors of high selectivity, true acetylcholine esterase had selective inhibitory, easily by blood brain barrier, long action time has the promotion memory represents, the effect that hypermnesis keeps, the domestic injection of at first developing was applied to myasthenia gravis in 1985, afterwards in clinical treatment senile dementia, the diseases such as benign memory deficits of also being used in.Be used to improve memory through the FDA approval as nutrient and healthcare products in the U.S. at present.And finished the III clinical trial phase.Clinical evaluation shows with similar medicine to be compared, and huperzine A has rapid-action, easily sees through blood brain barrier, long action time, and pharmaceutical properties is stable, is better than similar other medicines.Existing market is sold and is mainly contained the huperzine A tablet, capsule, and injection, wherein injection has only intramuscular injection, is not developed to intravenous fluid.
We discover, because the huperzine A water solublity is very poor, very unstable after the little liquid drugs injection dilution that conventional method is made, be difficult to carry out intravenous injection, we are through a large amount of huperzine A hydrochlorates that earlier huperzine A is converted into stable performance of discovering, and then being diluted to the injection of desired concn, the injection of making stability and dilution property are all fine, can be used for intravenously administrable.
Our research also find the first huperzine A clinically can with the medicine (rivastigmine-hydrogentartrate of the recovery that promotes the cholinergic nerve function, ginkalide A, benzhexol, levodopa, carbidopa etc.) or Chinese medicine blood-activating stasis-removing kind extract (Radix Salviae Miltiorrhizae extract, Flos Carthami extract, Folium Ginkgo extract, Herba Erigerontis extract and Radix Notoginseng extract etc.) drug combination with strengthen its treatment senile dementia, the effect of benign memory deficits and myasthenia gravis, and the huperzine A injection of selling in the market has only the muscle medication and does not have the intravenous drip medication, limited the use clinically of this medicine greatly, we have passed through big quantity research, disperse the salify technology to succeed in developing vein huperzine A injection finally by solvent-applied, provide great convenience to elderly patients, improved the compliance of medication greatly.
Summary of the invention
The present invention relates to a kind of vein injection that contains huperzine A, it is characterized in that this injection is used for intravenous injection, comprise huperzine A and can acid salifiable in this injection with it, concrete preparation comprises huperzine A and the injection, freeze-dried powder and the transfusion that become with the salifiable processed with acid of its energy, and water for injection is 1000 with the ratio of the weight of huperzine A in the injection: 1-500000: 1.
Huperzine A, its molecular formula are C
15H
18N
2O, molecular weight are 242.32, and huperzine A purity is greater than 98%, and acid salifiable with it is a kind of in hydrochloric acid, acetic acid, sulphuric acid, lactic acid and the citric acid.
Vein of the present invention is earlier huperzine A to be converted into the huperzine A hydrochlorate of stable performance or to use ethanol with the huperzine A injection, glycerol, propylene glycol dissolving back redilution becomes the injection of desired concn, and wherein water for injection is 1000 with the ratio of the weight of huperzine A: 1-500000: 1.
The vein injection of huperzine A of the present invention, its preparation method is as follows:
(1) huperzine A is added an amount of diluted acid and make salt, add in an amount of water for injection by the method for disperseing to drip, stir, add an amount of pin activated carbon, by the requirement of injection medicinal liquid, regulate pH value, filter decarburization, qualified to clarity, with liquid medicine filling, 100 ℃ of pressure sterilizings promptly get the huperzine A injection.
(2) huperzine A is added an amount of diluted acid and make salt, add an amount of proppant and fully dissolve, add an amount of pin activated carbon, by the requirement of injection medicinal liquid with an amount of water for injection, regulate pH value, filter decarburization, qualified to clarity, sterile filling, place the freezer dryer lyophilization, gland promptly gets the injection huperzine A, and wherein proppant comprises a kind of in glucose, mannitol, sorbitol and the Nulomoline.
(3) huperzine A is added an amount of diluted acid and make salt, add a spot of ethanol again, glycerol, behind a kind of dissolved dilution in the propylene glycol, join in the solution of preparing the proper amount of water for injection composition in advance by the method for disperseing to drip, the adding proper amount of sodium chloride is fully dissolved and is stirred, add an amount of pin activated carbon,, regulate pH value by the requirement of injection medicinal liquid, filter decarburization, qualified to clarity, fill, 115-121 ℃ of pressure sterilizing, be prepared into the huperzine A transfusion of hyperosmosis or isosmoticity
Vein of the present invention huperzine A injection, clinically can with the medicine of the recovery that promotes the cholinergic nerve function or Chinese medicine blood-activating stasis-removing kind injection drug combination to improve curative effect; Promote the medicine of the recovery of cholinergic nerve function to refer to specifically in rivastigmine-hydrogentartrate, ginkalide A, benzhexol, levodopa, the carbidopa that Chinese medicine blood-activating stasis-removing kind injection comprises one or more in Radix Salviae Miltiorrhizae Injection, Flos Carthami injection, YINXINGYE ZHUSHEYE, ginkgetin lactone injection, Herba Erigerontis injection, XUESHUANTONG ZHUSHEYE and the XUESAITONG ZHUSHEYE.
Specific implementation method
One, embodiment 1
Prescription:
Huperzine A 100mg
Dilute hydrochloric acid is an amount of
Water for injection is an amount of
Make 1000ml
Method for making: huperzine A is dissolved in fully dissolving in dilute hydrochloric acid, the ethanol, become huperzine A and disperse ethanol liquid, add water for injection to full dose, be stirred well to evenly, add an amount of activated carbon, stir, be filtered to clear and bright, embedding, 100 ℃ following 30 minutes the sterilization, passed examination is the huperzine A injection.
Two, embodiment 2
Prescription:
Huperzine A 200mg
Dilute hydrochloric acid is an amount of
Ethanol 10ml
Mannitol 50g
Make 1000ml
Method for making: huperzine A is dissolved in fully dissolving in an amount of dilute hydrochloric acid, the ethanol, become huperzine A and disperse ethanol liquid, add capacity ethanol, add an amount of activated carbon and stir, be filtered to clear and bright, sterile filling, place the freeze dryer lyophilization, gland, passed examination is the injection huperzine A.
Three, embodiment 3
Prescription:
Huperzine A 50mg
Dilute hydrochloric acid is an amount of
Ethanol 1ml
Sodium chloride 450g
Water for injection is an amount of
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of dilute hydrochloric acid, and fully dissolving in the ethanol becomes huperzine A and disperses ethanol liquid, add in the dissolved sodium chloride solution, stir, add an amount of activated carbon, stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in 30 minutes, passed examination, promptly get the huperzine A injection, wherein the 50ml/ bag.
Four, embodiment 4
Prescription:
Huperzine A 1g
Dilute hydrochloric acid is an amount of
Sodium chloride 450g
Glycerol 10ml
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of dilute hydrochloric acid makes salt, reuse glycerol fully dissolves, and becomes huperzine A and disperses ethanol liquid, adds in the mannitol solution of heating for dissolving, stir, add activated carbon and stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in following 30 minutes, after the passed examination, promptly get compound recipe huperzine A injection, wherein the 50ml/ bag.
Five, embodiment 5
Prescription:
Huperzine A 100mg
Dilute hydrochloric acid is an amount of
Sodium chloride 450g
Propylene glycol 8ml
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of dilute hydrochloric acid, fully dissolving in the ethanol becomes huperzine A and disperses ethanol liquid, adds in the sorbitol solution of heating for dissolving, stir, add activated carbon and stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in following 30 minutes, after the passed examination, promptly get the huperzine A transfusion, wherein the 50ml/ bag.
Six, embodiment 6
Prescription:
Huperzine A 500mg
Acetic acid is an amount of
Ethanol 1ml
Sodium chloride 450g
Water for injection is an amount of
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of spirit of vinegar, and fully dissolving in the ethanol becomes huperzine A and disperses ethanol liquid, add in the dissolved sodium chloride solution, stir, add an amount of activated carbon, stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in 30 minutes, passed examination, promptly get the huperzine A transfusion, wherein the 50ml/ bag.
Seven, embodiment 7
Prescription:
Huperzine A 2mg
Sulphuric acid is an amount of
Sodium chloride 450g
Glycerol 8ml
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of spirit of vinegar, fully dissolving in the ethanol becomes huperzine A and disperses ethanol liquid, adds in the sorbitol solution of heating for dissolving, stir, add activated carbon and stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in following 30 minutes, after the passed examination, promptly get the huperzine A transfusion, wherein the 50ml/ bag.
Eight, embodiment 8
Prescription:
Huperzine A 20mg
Lactic acid is an amount of
Sodium chloride 450g
Propylene glycol 8ml
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of rare lactic acid, fully dissolving in the ethanol becomes huperzine A and disperses ethanol liquid, adds in the sorbitol solution of heating for dissolving, stir, add activated carbon and stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in following 30 minutes, after the passed examination, promptly get the huperzine A transfusion, wherein the 50ml/ bag.
Nine, embodiment 9
Prescription:
Huperzine A 100mg
Citric acid is an amount of
Sodium chloride 450g
Make 1000 bags
Method for making: huperzine A is dissolved in an amount of rare citric acid, add ethanol an amount of in fully dissolving, become huperzine A and disperse ethanol liquid, add in the sorbitol solution of heating for dissolving, stir, add activated carbon and stir, be filtered to clear and bright, fill, 121 ℃ of sterilizations in following 30 minutes, after the passed examination, promptly get the huperzine A transfusion, wherein the 50ml/ bag.
Claims (8)
1. a vein injection that contains huperzine A is characterized in that this injection is used for intravenous injection, comprise in this injection huperzine A and with its can salifiable acid.
2. intravenous fluid huperzine A according to claim 1 is characterized in that concrete preparation comprises huperzine A and the injection, freeze-dried powder and the transfusion that become with the salifiable processed with acid of its energy.
3. huperzine A according to claim 1, its molecular formula are C
15H
18N
2O, molecular weight are 242.32, and huperzine A purity is greater than 98%, and acid salifiable with it is a kind of in hydrochloric acid, acetic acid, sulphuric acid, lactic acid and the citric acid.
4. according to the described vein injection that contains huperzine A of claim 1-3, it is characterized in that earlier huperzine A being converted into the injection that redilution after the huperzine A salt of stable performance becomes desired concn, injection, freeze-dried powder and the transfusion of making huperzine A or its salt then according to conventional method.
5. huperzine A injection according to claim 1 is characterized in that the water for injection and the ratio of the weight of huperzine A are 1000: 1～500000: 1.
6. according to the described vein injection that contains huperzine A of claim 1-4, wherein also comprise proppant in the freeze-dried powder, be specially a kind of in glucose, mannitol, sorbitol and the Nulomoline.
7. according to the described vein injection that contains huperzine A of claim 1-4, wherein can also comprise solubilizing agent in the transfusion, be specially ethanol, glycerol, a kind of in the propylene glycol.
8. according to the vein huperzine A injection described in the claim 1-4, clinically can with the medicine of the recovery that promotes the cholinergic nerve function or Chinese medicine blood-activating stasis-removing kind injection drug combination to improve curative effect; Promote the medicine of the recovery of cholinergic nerve function specifically to refer to a kind of in rivastigmine-hydrogentartrate, ginkalide A, benzhexol, levodopa, the carbidopa; Chinese medicine activating blood circulation to dissipate blood stasis class injection comprises one or more in Radix Salviae Miltiorrhizae Injection, Flos Carthami injection, YINXINGYE ZHUSHEYE, bilobalide injection, Herba Erigerontis injection and the XUESHUANTONG ZHUSHEYE.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200710145475XA CN101129329A (en) | 2007-09-19 | 2007-09-19 | Injection containing huperzine for sulci venosi and method of preparing the same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200710145475XA CN101129329A (en) | 2007-09-19 | 2007-09-19 | Injection containing huperzine for sulci venosi and method of preparing the same |
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|---|---|
| CN101129329A true CN101129329A (en) | 2008-02-27 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200710145475XA Pending CN101129329A (en) | 2007-09-19 | 2007-09-19 | Injection containing huperzine for sulci venosi and method of preparing the same |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102514755A (en) * | 2011-11-04 | 2012-06-27 | 蚌埠丰原涂山制药有限公司 | Preparation method of xantinol nicotinate and sodium chloride injection packaged by using soft bag |
| CN105796582A (en) * | 2016-04-07 | 2016-07-27 | 于昉 | Tablet for treating senile dementia |
| CN114796132A (en) * | 2022-05-13 | 2022-07-29 | 海南灵康制药有限公司 | Lyophilized powder injection of huperzine A and its preparation method |
-
2007
- 2007-09-19 CN CNA200710145475XA patent/CN101129329A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102514755A (en) * | 2011-11-04 | 2012-06-27 | 蚌埠丰原涂山制药有限公司 | Preparation method of xantinol nicotinate and sodium chloride injection packaged by using soft bag |
| CN105796582A (en) * | 2016-04-07 | 2016-07-27 | 于昉 | Tablet for treating senile dementia |
| CN114796132A (en) * | 2022-05-13 | 2022-07-29 | 海南灵康制药有限公司 | Lyophilized powder injection of huperzine A and its preparation method |
| CN114796132B (en) * | 2022-05-13 | 2023-08-22 | 海南灵康制药有限公司 | Huperzine A freeze-dried powder injection and preparation method thereof |
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Open date: 20080227 |