CN102232931A - Formula of asarone for injection and preparation method thereof - Google Patents
Formula of asarone for injection and preparation method thereof Download PDFInfo
- Publication number
- CN102232931A CN102232931A CN 201010166759 CN201010166759A CN102232931A CN 102232931 A CN102232931 A CN 102232931A CN 201010166759 CN201010166759 CN 201010166759 CN 201010166759 A CN201010166759 A CN 201010166759A CN 102232931 A CN102232931 A CN 102232931A
- Authority
- CN
- China
- Prior art keywords
- injection
- asarone
- medicinal liquid
- preparation
- recipe quantity
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention provides a formula of asarone for injection and a preparation method thereof. In the invention, an injection is prepared by using asarone as a main ingredient, Tween-80 and polyethylene glycol (PEG)-400 as solubilizer and mannitol as an excipient, and the solubility of the asarone is improved effectively; and thus, the medicine carrying capacity of the injection is increased. The injection prepared by the invention has high re-solubility and product stability, and the preparation process is simple.
Description
Technical field:
The present invention relates to a kind of drug injection, particularly relate to a kind of preparation method of injection asarone.
Background technology:
Asarone has another name called a-asarone or a-asaricin, mainly is present in the volatile oil of plants such as acorus gramineus araceae plant, has calmness, convulsion, and spasmolytic is relievingd asthma, blood fat reducing, function of gallbladder promoting, multiple pharmacological effect such as anticancer.Diplococcus pneumoniae, staphylococcus aureus and colibacillary growth also there are in various degree inhibitory action, are mainly used in pneumonia, bronchial asthma, chronic obstructive pulmonary disease companion pulmonary acute inflammation etc. clinically.
The asarone oral absorption is rapid, can reach the blood concentration peak in 15 minutes, plasma protein binding rate 61%, and be distributed in internal organs such as liver, kidney, bile and the heart, brain, lung, spleen rapidly, and wherein Liver and kidney concentration is near plasma concentration, and all the other successively decrease successively.Aarin preparation dosage form on the market has tablet, capsule, injection at present.Asarone and the chemical compound of hydrophilic extreme difference extremely strong as lipotropy, its tablet and capsule, oral back is difficult for disperseing and stripping, and effective ratio area is little when contacting with body fluid, can't realize therapeutic effect.Now a lot of technology adopt the injection of prepared in various methods asarone, but have number of drawbacks, for example, adopt water and organic solvent dissolution asarone, make to redissolve weak effect behind the lyophilized formulations, easily produce muddyly, and influence is used; People can add surfactant medicine is carried out solubilising in addition, but then can there be serious potential safety hazard in simple adding surfactant, and a large amount of surfactant of single adding, can cause the product lyophilizing incomplete, outward appearance is not good, and the effect of redissolving is also bad, is unfavorable for practical clinical.
For addressing the above problem, the invention provides a kind of Asarone injection, said preparation adopts PEG-400, tween 80 is done solubilizing agent, selects for use mannitol as excipient simultaneously, the lyophilized injectable powder of making, redissolve respond well, the solution clear, clinical ill effect has also reduced.
Summary of the invention
The present invention is in order to solve multiple security risk and the preparation defective that Aarin preparation exists in the prior art, a kind of employing Polyethylene Glycol-400 is provided, tween 80 is as the injection of the asarone of solubilizing agent, can add pharmaceutically acceptable excipient according to reality in the described preparation, PH regulator etc.
A kind of injection asarone preparation method provided by the invention, its prescription is composed as follows:
Asarone 8.0～16.0g
Mannitol 200.0～500.0g
PEG-400 111.0～225.0g
Tween 80 65.0～130.0g
Citric acid is an amount of
Water for injection is an amount of
0.15% of Actidose total amount
Make 1000 bottles after the lyophilizing altogether
Solubilizing agent is Polyethylene Glycol-400, tween 80 in the prescription that the present invention proposes;
Excipient is a mannitol in the prescription that the present invention proposes;
The PH regulator is a citric acid in the prescription that the present invention proposes.
The preparation method that the present invention proposes is " A " medicinal liquid in the PEG-400 that the asarone of recipe quantity is dissolved in fully recipe quantity, the tween 80; The mannitol of recipe quantity is dissolved in an amount of water for injection fully, stand-by; Citric acid adds water for injection in right amount makes into citric acid soln; In mannitol solution, add citric acid soln 70ml, survey the solution pH value and should be 4.6; Add recipe quantity active carbon stirring and adsorbing 30 minutes,, be " B " medicinal liquid with the carbon removal of 0.45um filter membrane coarse filtration; " B " medicinal liquid is added in " A " medicinal liquid, and mend to full dose, stirred 10 minutes, making the medicinal liquid mix homogeneously regulate pH value is 5.0～5.2, and further degerming fill lyophilizing gets final product.Aarin preparation by this law preparation has improved the asarone meltage effectively, thereby has increased the drug loading of injection.The injection solubility of the present invention's preparation is good, and goods are stable, and preparation technology is simple.
The specific embodiment
The invention will be further described with by way of example more below, provides implementation detail of the present invention, but be not to be intended to limit protection scope of the present invention.
Embodiment 1:
Asarone 8.0g
Mannitol 400.0
PEG-400 225.0
Tween 80 130.0
Citric acid 1.5g
Water for injection 2.0kg
0.15% of Actidose total amount
Make 1000 bottles after the lyophilizing altogether
Take by weighing the recipe quantity supplementary material, asarone is dissolved in PEG-400, the tween 80 fully, be " A " medicinal liquid; The mannitol of recipe quantity is dissolved in the proper amount of water for injection, stand-by; The recipe quantity citric acid is added water for injection make into citric acid soln; In mannitol solution, add citric acid soln 70ml, survey the solution pH value and should be 4.6; Add recipe quantity active carbon stirring and adsorbing 30 minutes,, be " B " medicinal liquid with the carbon removal of 0.45um filter membrane coarse filtration; " B " medicinal liquid is added in " A " medicinal liquid, and mend to full dose, stirred 10 minutes, making the medicinal liquid mix homogeneously regulate pH value is 5.0～5.2; Through the degerming of 0.22um membrane filtration, filtrate fill, lyophilizing get final product.
Embodiment 2:
Asarone 8.0g
Mannitol 452.0
PEG-400 225.0
Tween 80 125.0
Citric acid 1.5g
Water for injection 3.0kg
0.15% of Actidose total amount
Make 1000 bottles after the lyophilizing altogether
Take by weighing the recipe quantity supplementary material, asarone is dissolved in PEG-400, the tween 80 fully, be " A " medicinal liquid; The mannitol of recipe quantity is dissolved in the proper amount of water for injection, stand-by; Citric acid 1.5g adds water for injection makes into the 72ml citric acid soln; In mannitol solution, add citric acid soln 70ml, survey the solution pH value and should be 4.6; Add recipe quantity active carbon stirring and adsorbing 30 minutes,, be " B " medicinal liquid with the carbon removal of 0.45um filter membrane coarse filtration; " B " medicinal liquid is added in " A " medicinal liquid, and mend to full dose, stirred 10 minutes, making the medicinal liquid mix homogeneously regulate pH value is 5.0～5.2; Through the degerming of 0.22um membrane filtration, filtrate fill, lyophilizing get final product.
Embodiment 3:
Asarone 16.0g
Mannitol 500.0
PEG-400 225.0
Tween 80 120.0
Citric acid 1.50g
Water for injection 4.0kg
0.15% of Actidose total amount
Make 1000 bottles after the lyophilizing altogether
Take by weighing the recipe quantity supplementary material, asarone is dissolved in PEG-400, the tween 80 fully, be " A " medicinal liquid; The mannitol of recipe quantity is dissolved in the proper amount of water for injection, stand-by; Citric acid 1.5g adds water for injection makes into the 80ml citric acid soln; In mannitol solution, add citric acid soln 70ml, survey the solution pH value and should be 4.6; Add recipe quantity active carbon stirring and adsorbing 30 minutes,, be " B " medicinal liquid with the carbon removal of 0.45um filter membrane coarse filtration; " B " medicinal liquid is added in " A " medicinal liquid, and mend to full dose, stirred 10 minutes, making the medicinal liquid mix homogeneously regulate pH value is 5.0～5.2; Through the degerming of 0.22um membrane filtration, filtrate fill, lyophilizing get final product.
Claims (3)
1. an injection asarone is write out a prescription and preparation method, and the dosage form that it is characterized in that said preparation is a lyophilized injectable powder.
2. the preparation method of injection asarone as claimed in claim 1 is characterized in that, the prescription of this injection consists of:
Asarone 8.0～16.0g
Mannitol 200.0～500.0g
PEG-400 111.0～225.0g
Tween 80 65.0～130.0g
Citric acid is an amount of
Water for injection is an amount of
0.15% of Actidose total amount
Make 1000 bottles after the lyophilizing altogether.
3. the preparation method of injection asarone as claimed in claim 1 is characterized in that, may further comprise the steps:
3.1 vial is removed through outer package, cleaning machine cleans, and clean compressed air dries up, after 350 ℃ of dry heat sterilizations 5 minutes, and cooling, standby;
3.2 butyl rubber bung is removed through outer package, washes the plug machine and cleans, and is in 121 ℃ of dry heat sterilizations 120 minutes, cooling, standby;
3.3 aluminium-plastic cap is removed through outer package, baking is 120 minutes in 110 ℃ of baking ovens, and cooling is standby;
3.4 take by weighing supplementary material by recipe quantity, the asarone of recipe quantity is dissolved in fully among the PEG-400, tween 80 of recipe quantity, be " A " medicinal liquid;
3.5 the mannitol of recipe quantity is dissolved in the proper amount of water for injection fully, stand-by; Citric acid adds water for injection in right amount makes into citric acid soln; In mannitol solution, add citric acid soln 70ml, survey the solution pH value and should be 4.6; Add recipe quantity active carbon stirring and adsorbing 30 minutes,, be " B " medicinal liquid with the carbon removal of 0.45um filter membrane coarse filtration;
3.6 " B " medicinal liquid is added in " A " medicinal liquid, and mends to full dose, stirred 10 minutes, making the medicinal liquid mix homogeneously regulate pH value is 5.0～5.2;
3.7 through the degerming of 0.22u m membrane filtration, filtrate for later use;
3.8 intermediate detects qualified back fill, tamponade after the lyophilizing, packs after rolling lid, lamp inspection, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010166759 CN102232931A (en) | 2010-04-23 | 2010-04-23 | Formula of asarone for injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010166759 CN102232931A (en) | 2010-04-23 | 2010-04-23 | Formula of asarone for injection and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102232931A true CN102232931A (en) | 2011-11-09 |
Family
ID=44884357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201010166759 Pending CN102232931A (en) | 2010-04-23 | 2010-04-23 | Formula of asarone for injection and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102232931A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104857516A (en) * | 2015-05-12 | 2015-08-26 | 张蕊 | Asarone injection and preparation process thereof |
| CN106619498A (en) * | 2016-12-19 | 2017-05-10 | 宜昌三峡制药有限公司 | Production method of asarone sodium chloride injection |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1657071A (en) * | 2004-02-03 | 2005-08-24 | 深圳市康瑞医药有限公司 | Asarone injection and its preparation method |
| CN1698590A (en) * | 2005-05-30 | 2005-11-23 | 许群 | Aarin preparation for injection and preparing process thereof |
| CN1720907A (en) * | 2005-06-13 | 2006-01-18 | 广州中医药大学第一附属医院 | The agent of treatment stroke injection |
-
2010
- 2010-04-23 CN CN 201010166759 patent/CN102232931A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1657071A (en) * | 2004-02-03 | 2005-08-24 | 深圳市康瑞医药有限公司 | Asarone injection and its preparation method |
| CN1698590A (en) * | 2005-05-30 | 2005-11-23 | 许群 | Aarin preparation for injection and preparing process thereof |
| CN1720907A (en) * | 2005-06-13 | 2006-01-18 | 广州中医药大学第一附属医院 | The agent of treatment stroke injection |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104857516A (en) * | 2015-05-12 | 2015-08-26 | 张蕊 | Asarone injection and preparation process thereof |
| CN104857516B (en) * | 2015-05-12 | 2017-11-10 | 张蕊 | A kind of Asarone Injectin and its preparation technology |
| CN106619498A (en) * | 2016-12-19 | 2017-05-10 | 宜昌三峡制药有限公司 | Production method of asarone sodium chloride injection |
| CN106619498B (en) * | 2016-12-19 | 2019-08-06 | 宜昌三峡制药有限公司 | A kind of production method of asarone sodium chloride injection |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102670527B (en) | Freeze-dried powder injection of L-oxiracetam and process for preparing freeze-dried powder injection | |
| CN107789340B (en) | Solution preparation for andrographis paniculata aerosol inhalation and preparation method thereof | |
| US11491138B2 (en) | Injectable psychoactive alkaloid composition and preparation thereof | |
| CN102247579A (en) | Formula, preparation method and application of Xingnaojing lipidosome combined drug | |
| CN1813782B (en) | Composition of ginkgo leaf extract and dipyridamole, medicine containing same and preparing method thereof | |
| CN102058593A (en) | Combination medicament of ilaprazole sodium and preparation process thereof | |
| CN101129368A (en) | Freeze-dried powder needle containing lansoprazole | |
| CN102283808A (en) | Azithromycin liposome combined medicament and preparation method thereof | |
| CN101744815B (en) | Composite medicament of omeprazole sodium | |
| CN102232931A (en) | Formula of asarone for injection and preparation method thereof | |
| CN101874789B (en) | Lansoprazole-contained freeze-dried powder injection | |
| CN108524453A (en) | A kind of pharmaceutical composition of aspartic acid ornithine | |
| CN103961322A (en) | Freeze-dried dexlansoprazole composition for injection and preparation method thereof | |
| CN105726495B (en) | A kind of short-acting benzodiazepine salt pharmaceutical composition of injection and preparation method thereof | |
| CN100453072C (en) | Isatis root drops and preparation thereof | |
| CN102091070A (en) | Rabeprazole sodium combined medicament and preparation process thereof | |
| CN104490800B (en) | A kind of good fortune department Fluconazole freezes compound powder and preparation method thereof | |
| CN107397722B (en) | (S) -4-hydroxy-2-oxo-1-pyrrolidine acetamide freeze-dried powder for injection and preparation method thereof | |
| CN107281121B (en) | (S) -4-hydroxy-2 oxo-1-pyrrolidine acetamide freeze-dried powder for injection and preparation method thereof | |
| CN106692077A (en) | Levo oxiracetam lyophilized powder for injection and preparation method thereof | |
| CN107281114A (en) | A kind of injection levo-oxiracetam freeze-dried powder and preparation method thereof | |
| CN107432862A (en) | Injection (S)-Esomeprazole freeze-dried powder and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20111109 |