CN101244070A - Polyene phosphatidylcholine high-capacity injection - Google Patents

Polyene phosphatidylcholine high-capacity injection Download PDF

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Publication number
CN101244070A
CN101244070A CNA2007100049535A CN200710004953A CN101244070A CN 101244070 A CN101244070 A CN 101244070A CN A2007100049535 A CNA2007100049535 A CN A2007100049535A CN 200710004953 A CN200710004953 A CN 200710004953A CN 101244070 A CN101244070 A CN 101244070A
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polyene phosphatidylcholine
injection
preparation
add
polyene
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CNA2007100049535A
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Chinese (zh)
Inventor
桂勇
袁振
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Individual
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Individual
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Abstract

The invention discloses a polyene phosphatidylcholine large volume injection which is prepared by the mixture of polyene phosphatidylcholine or soybean phospholipid as the active component and the pharmaceutical carrier; the content proportion of the active component in the injection is 0.0465% to 0.93%. The large volume injection is characterized in that the polyene phosphatidylcholine injection can be used for intravenous infusion directly. The polyene phosphatidylcholine large volume injection has the advantage of omitting the diluting process in the present medication condition, avoiding cross infection, improving the clinical application level and safety, and facilating the convenient use.

Description

A kind of polyene phosphatidylcholine high-capacity injection
Technical field
The present invention relates to a kind of polyene phosphatidylcholine high-capacity injection.
Background technology
Polyene phosphatidylcholine is a digestive system drug commonly used both at home and abroad.Be reported to be the liver and gall diseases curative in National Drug Administration's standard " Polyene Phosphatidylcholine injection liquid ".Be used for various types of hepatopathys, as hepatitis, chronic hepatitis, hepatic necrosis, liver cirrhosis, hepatic coma (comprising forerunner's hepatic coma), fatty liver, cholestasis, poisoning, the recurrence of prevention cholelithiasis, perioperative treatment, especially hepatobiliary surgery, gestosis, psoriasis, neurodermatitis, the radiation syndrome.Intravenous injection, but also intravenous drip are used with not containing electrolytical glucose injection dilution back during intravenous drip.Because the liquid of getting before the intravenous injection mixes, and has brought some shortcomings, not only formality is loaded down with trivial details, and be subjected to the pollution of environment, apparatus easily, make the patient produce infusion reaction, as have a fever, feel sick, feel cold, tachycardia or slow excessively etc., can jeopardize patient's life when serious.
Summary of the invention
The technical issues that need to address of the present invention just are to overcome the defective of prior art, and a kind of polyene phosphatidylcholine high-capacity injection is provided, and it is a kind of Polyene Phosphatidylcholine injection liquid that is directly used in venoclysis.
For addressing the above problem, the present invention adopts following technical scheme:
A kind of polyene phosphatidylcholine high-capacity injection of the present invention, described polyene phosphatidylcholine high-capacity injection is prepared from as active component and pharmaceutical carrier by polyene phosphatidylcholine or soybean phospholipid, and the content that contains active component in the injection is 0.0465%~0.93%.
Pharmaceutical carrier of the present invention is antioxidant, buffer agent, cosolvent and water for injection.
Antioxidant of the present invention is vitamin E, vitamin C, sodium sulfite and other sulphite or citric acid; Described buffer agent is a riboflavin; Described cosolvent is deoxycholic acid, sodium hydroxide or dehydrated alcohol.
Deoxycholic acid of the present invention is hyodeoxycholic acid, ursodeoxycholic acid or chenodeoxy cholic acid.
Also contain isotonic agent in the injection of the present invention; Described isotonic agent is glucose, xylitol, mannitol, sorbitol or dextran.
The present invention provides a kind of preparation method of described polyene phosphatidylcholine high-capacity injection simultaneously, and described preparation method comprises the following steps:
A, to get dehydrated alcohol an amount of, adds polyene phosphatidylcholine or soybean phospholipid, antioxidant, stirs and make dissolving;
B, get sodium hydroxide and add injection water dissolving, add deoxycholic acid, stirring and dissolving, adjust pH to 8.0, heated and boiled;
C, the solution that steps A is prepared join in the solution of step B preparation, stir, and add buffer agent, add water, add active carbon, continue heated and stirred 15 minutes; Decarbonization filtering adds buffer agent, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
The preparation method of polyene phosphatidylcholine high-capacity injection of the present invention, the step that also comprises preparation isotonic agent concentrated wiring liquid: get the water for injection that isotonic agent adds 3 times of amounts, stirring and dissolving, add water, adding 0.3% active carbon boiled 15 minutes, through sand filtration rod filtering decarbonization,, get the isotonic agent concentrated wiring liquid through 0.22 μ m filtering with microporous membrane.
Preparation polyene phosphatidylcholine high-capacity injection finished product of the present invention, isotonic agent concentrated wiring liquid and polyene phosphatidylcholine concentrated wiring liquid are filled into respectively in the different chamber of the soft bag in the two chambers of non-PVC, the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid is 4: 1, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, make it fully mixed, get the polyene phosphatidylcholine high-capacity injection finished product.
The high energy polyene phosphatidylcholine that polyene phosphatidylcholine high-capacity injection of the present invention provides high dose to absorb easily has by the direct membrane structure that influences and makes impaired liver function and enzyme activity recover normal; Regulate the energy balance of liver; Promote hepatic tissue regeneration; Neutral fat and cholesterol are changed into easy metabolic form, stablize physiological functions such as bile.Be applicable to various types of hepatopathys, as hepatitis, chronic hepatitis, hepatic necrosis, liver cirrhosis, hepatic coma (comprising forerunner's hepatic coma), fatty liver, cholestasis, poisoning, the recurrence of prevention cholelithiasis, perioperative treatment, especially hepatobiliary surgery, gestosis, psoriasis, neurodermatitis, the radiation syndrome.
Polyene phosphatidylcholine high-capacity injection of the present invention is applicable to the infusion solutions of all size.
Injection of the present invention can be directly used in venoclysis, has reduced the dilution in the existing medicining condition, avoids cross infection, and improves clinical practice level and safety, and is easy to use.
The specific embodiment
Example 1: preparation polyene phosphatidyl gallbladder glucose injection
Prescription:
Polyene phosphatidyl gallbladder (soybean phospholipid) 4.65g
Deoxycholic acid 3.88g
Sodium hydroxide 0.388g
Vitamin E 0.2g
Dehydrated alcohol 5.47ml
Riboflavin 0.01g
Glucose 50g
Water for injection adds to 1000ml
Preparation method
(1) preparation isotonic agent concentrated wiring liquid
Get glucose 50g, add the water for injection of 150ml, stirring and dissolving adds 0.3% active carbon and boiled 15 minutes, through sand filtration rod filtering decarbonization, adds water to 800ml, through 0.22 μ m filtering with microporous membrane, gets the isotonic agent concentrated wiring liquid.
(2) preparation polyene phosphatidylcholine concentrated wiring liquid
1, gets dehydrated alcohol 5.47ml, add polyene phosphatidylcholine (or soybean phospholipid) 4.65g, vitamin E 0.2g, stir and make dissolving;
2, get sodium hydroxide 0.388g and add the dissolving of injection water, add deoxycholic acid 3.88g, stirring and dissolving, adjust pH to 8.0, heated and boiled;
The solution of step 1 preparation is joined in the solution of step 2 preparation, stir, add water, add active carbon, continued heated and stirred 15 minutes to 200ml; Decarbonization filtering adds buffer agent and comprises riboflavin 0.01g, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
(3) preparation polyene phosphatidylcholine high-capacity injection
With the solution of above-mentioned steps () and step (two) preparation respectively liquid drug go in the different chamber of the soft bag in the two chambers of non-PVC, it in the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid 4: 1 ratio fill, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, makes it fully mixed, lamp inspection makes polyene phosphatidylcholine high-capacity injection after the quality inspection.
Example 2: preparation polyene phosphatidyl gallbladder glucose injection
Prescription:
Polyene phosphatidyl gallbladder (soybean phospholipid) 9.3g
Deoxycholic acid 7.76g
Sodium hydroxide 0.776g
Vitamin E 0.4g
Dehydrated alcohol 10.94ml
Riboflavin 0.02g
Glucose 50g
Water for injection adds to 1000ml
Preparation method
(1) preparation isotonic agent concentrated wiring liquid
Get glucose 50g, add the water for injection of 150ml, stirring and dissolving adds 0.3% active carbon and boiled 15 minutes, through sand filtration rod filtering decarbonization, adds water to 800ml, through 0.22 μ m filtering with microporous membrane, gets the isotonic agent concentrated wiring liquid.
(2) preparation polyene phosphatidylcholine concentrated wiring liquid
1, gets dehydrated alcohol 10.94ml, add polyene phosphatidylcholine 9.3g (or soybean phospholipid), vitamin E 0.4g, stir and make dissolving;
2, get sodium hydroxide 0.776g and add the dissolving of injection water, add deoxycholic acid 7.76g, stirring and dissolving, adjust pH to 8.0, heated and boiled;
The solution of above-mentioned steps 1 preparation is joined in the solution of step 2 preparation, stir, add water, add active carbon, continued heated and stirred 15 minutes to 200ml; Decarbonization filtering adds buffer agent and comprises riboflavin 0.02g, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
(3) preparation polyene phosphatidylcholine high-capacity injection
With two solution of above-mentioned steps () and step (two) preparation respectively liquid drug go in the different chamber of the soft bag in the two chambers of non-PVC, it in the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid 4: 1 ratio fill, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, makes it fully mixed, lamp inspection makes polyene phosphatidylcholine high-capacity injection after the quality inspection.
Example 3: preparation polyene phosphatidyl gallbladder glucose injection
Prescription:
Polyene phosphatidyl gallbladder (soybean phospholipid) 0.465g
Deoxycholic acid 0.388g
Sodium hydroxide 0.039g
Vitamin E 0.02g
Dehydrated alcohol 0.547ml
Riboflavin 0.001g
Glucose 50g
Water for injection adds to 1000ml
Preparation method
(1) preparation isotonic agent concentrated wiring liquid
Get glucose 50g, add the water for injection of 150ml, stirring and dissolving adds 0.3% active carbon and boiled 15 minutes, through sand filtration rod filtering decarbonization, adds water to 800ml, through 0.22 μ m filtering with microporous membrane, gets the isotonic agent concentrated wiring liquid.
(2) preparation polyene phosphatidylcholine concentrated wiring liquid
1, gets dehydrated alcohol 0.547ml, add polyene phosphatidylcholine (soybean phospholipid) 0.465g, vitamin E 0.02g, stir and make dissolving;
2, get sodium hydroxide 0.039g and add the dissolving of injection water, add deoxycholic acid 0.388g, stirring and dissolving, adjust pH to 8.0, heated and boiled;
The solution of above-mentioned steps 1 preparation is joined in the solution of step 2 preparation, stir, add water, add active carbon, continued heated and stirred 15 minutes to 200ml; Decarbonization filtering adds buffer agent and comprises riboflavin 0.001g, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
(3) preparation polyene phosphatidylcholine high-capacity injection
With two solution of above-mentioned steps () and step (two) preparation respectively liquid drug go in the different chamber of the soft bag in the two chambers of non-PVC, it in the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid 4: 1 ratio fill, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, makes it fully mixed, lamp inspection makes polyene phosphatidylcholine high-capacity injection after the quality inspection.
Example 4: preparation contains the polyene phosphatidylcholine high-capacity injection of sorbitol
Press the method for example 1, replace glucose to make as raw material with sorbitol.
Example 5: preparation contains the polyene phosphatidylcholine high-capacity injection of xylitol
Press the method for example 1, replace glucose to make as raw material with xylitol.
Example 6: preparation contains the dextran polyene phosphatidylcholine high-capacity injection of (comprising big or middle or small-molecular weight dextran)
Press the method for example 1, replace glucose to make as raw material with dextran.
Example 7: preparation polyene phosphatidyl gallbladder glucose injection
Prescription:
Polyene phosphatidyl gallbladder (soybean phospholipid) 4.65g
Deoxycholic acid 3.88g
Sodium hydroxide 0.388g
Vitamin C 0.2g
Dehydrated alcohol 5.47ml
Riboflavin 0.01g
Glucose 50g
Water for injection adds to 1000ml
Preparation method
(1) preparation isotonic agent concentrated wiring liquid
Get glucose 50g, add the water for injection of 150ml, stirring and dissolving adds the .0.3% active carbon and boiled 15 minutes, through sand filtration rod filtering decarbonization, adds water to 800ml, through 0.22 μ m filtering with microporous membrane, gets the isotonic agent concentrated wiring liquid.
(2) preparation polyene phosphatidylcholine concentrated wiring liquid
1, gets dehydrated alcohol 5.47ml, add polyene phosphatidylcholine (or soybean phospholipid) 4.65g, vitamin C 0.2g, stir and make dissolving;
2, get sodium hydroxide 0.388g and add the dissolving of injection water, add deoxycholic acid 3.88g, stirring and dissolving, adjust pH to 8.0, heated and boiled;
The solution of above-mentioned steps 1 preparation is joined in the solution of step 2 preparation, stir, add water, add active carbon, continued heated and stirred 15 minutes to 200ml; Decarbonization filtering adds buffer agent and comprises riboflavin 0.01g, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
(3) preparation polyene phosphatidylcholine high-capacity injection
With two solution of above-mentioned steps () and step (two) preparation respectively liquid drug go in the different chamber of the soft bag in the two chambers of non-PVC, it in the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid 4: 1 ratio fill, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, makes it fully mixed, lamp inspection makes polyene phosphatidylcholine high-capacity injection after the quality inspection.
Example 8: preparation polyene phosphatidyl gallbladder glucose injection
Prescription:
Polyene phosphatidyl gallbladder (soybean phospholipid) 4.65g
Deoxycholic acid 3.88g
Sodium hydroxide 0.388g
Sodium sulfite 0.5g
Dehydrated alcohol 5.47ml
Riboflavin 0.01g
Glucose 50g
Water for injection adds to 1000ml
Preparation method
(1) preparation isotonic agent concentrated wiring liquid
Get glucose 50g, add the water for injection of 150ml, stirring and dissolving adds 0.3% active carbon and boiled 15 minutes, through sand filtration rod filtering decarbonization, adds water to 800ml, through 0.22 μ m filtering with microporous membrane, gets the isotonic agent concentrated wiring liquid.
(2) preparation polyene phosphatidylcholine concentrated wiring liquid
1, gets dehydrated alcohol 5.47ml, add polyene phosphatidylcholine (or soybean phospholipid) 4.65g, vitamin sodium sulfite 0.5g, stir and make dissolving;
2, get sodium hydroxide 0.388g and add the dissolving of injection water, add deoxycholic acid 3.88g, stirring and dissolving, adjust pH to 8.0, heated and boiled;
The solution of above-mentioned steps 1 preparation is joined in the solution of step 2 preparation, stir, add water, add active carbon, continued heated and stirred 15 minutes to 200ml; Decarbonization filtering adds buffer agent and comprises riboflavin 0.01g, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
(3) preparation polyene phosphatidylcholine high-capacity injection
With two solution of above-mentioned steps () and step (two) preparation respectively liquid drug go in the different chamber of the soft bag in the two chambers of non-PVC, it in the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid 4: 1 ratio fill, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, makes it fully mixed, lamp inspection makes polyene phosphatidylcholine high-capacity injection after the quality inspection.
Example 9: preparation polyene phosphatidyl gallbladder glucose injection
Prescription:
Polyene phosphatidyl gallbladder (soybean phospholipid) 4.65g
Deoxycholic acid 3.88g
Sodium hydroxide 0.388g
Citric acid 0.5g
Dehydrated alcohol 5.47ml
Riboflavin 0.01g
Glucose 50g
Water for injection adds to 1000ml
Preparation method
(1) preparation isotonic agent concentrated wiring liquid
Get glucose 50g, add the water for injection of 150ml, stirring and dissolving adds 0.3% active carbon and boiled 15 minutes, through sand filtration rod filtering decarbonization, adds water to 800ml, through 0.22 μ m filtering with microporous membrane, gets the isotonic agent concentrated wiring liquid.
(2) preparation polyene phosphatidylcholine concentrated wiring liquid
1, gets dehydrated alcohol 5.47ml, add polyene phosphatidylcholine (or soybean phospholipid) 4.65g, citric acid 0.5g, stir and make dissolving;
2, get sodium hydroxide 0.388g and add the dissolving of injection water, add deoxycholic acid 3.88g, stirring and dissolving, adjust pH to 8.0, heated and boiled;
The solution of above-mentioned steps 1 preparation is joined in the solution of step 2 preparation, stir, add water, add active carbon, continued heated and stirred 15 minutes to 200ml; Decarbonization filtering adds buffer agent and comprises riboflavin 0.01g, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
(3) preparation polyene phosphatidylcholine high-capacity injection
With two solution of above-mentioned steps () and step (two) preparation respectively liquid drug go in the different chamber of the soft bag in the two chambers of non-PVC, it in the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid 4: 1 ratio fill, seal, high temperature sterilize, lucifuge is cooled to room temperature, gets through two chambers bag sealing coat, makes it fully mixed, lamp inspection makes polyene phosphatidylcholine high-capacity injection after the quality inspection.
The survey report of the polyene phosphatidylcholine high-capacity injection that the inventive method makes is as follows:
The name of an article: polyene phosphatidylcholine high-capacity injection
Character: this product is yellow clear liquid
Differentiate: be positive reaction
PH value: 8.6
5 hydroxymethyl furfural:<12.5 μ g/ml
Sterility test: up to specification
Particulate matter: up to specification
Bacterial endotoxin: up to specification
Other: meet requirement under the injection item
Polyene phosphatidylcholine content is labelled amount %:100.9%
Glucose content is labelled amount %:99.1%
The present invention is not limited to above-mentioned preferred forms, and other any identical with the present invention or akin products that anyone draws under enlightenment of the present invention all drop within protection scope of the present invention.

Claims (8)

1. polyene phosphatidylcholine high-capacity injection, it is characterized in that described polyene phosphatidylcholine high-capacity injection is prepared from as active component and pharmaceutical carrier by polyene phosphatidylcholine or soybean phospholipid, the content of contained active component is 0.0465%~0.93% in the injection.
2. polyene phosphatidylcholine high-capacity injection according to claim 1 is characterized in that described pharmaceutical carrier is antioxidant, buffer agent, cosolvent and water for injection.
3. polyene phosphatidylcholine high-capacity injection according to claim 2, described antioxidant are vitamin E, vitamin C, sodium sulfite and other sulphite or citric acid; Described buffer agent is a riboflavin; Described cosolvent is deoxycholic acid, sodium hydroxide or dehydrated alcohol.
4. polyene phosphatidylcholine high-capacity injection according to claim 3 is characterized in that described deoxycholic acid is hyodeoxycholic acid, ursodeoxycholic acid or chenodeoxy cholic acid.
5. according to the arbitrary described polyene phosphatidylcholine high-capacity injection of claim 1-4, it is characterized in that also containing in the described polyene phosphatidylcholine high-capacity injection isotonic agent; Described isotonic agent is glucose or xylitol or mannitol or sorbitol or dextran.
6. the described preparation method of polyene phosphatidylcholine high-capacity injection as claimed in claim 1 comprises the following steps:
A, to get dehydrated alcohol an amount of, adds polyene phosphatidylcholine or soybean phospholipid, antioxidant, stirs and make dissolving;
B, get sodium hydroxide and add injection water dissolving, add deoxycholic acid, stirring and dissolving, adjust pH to 8.0, heated and boiled;
C, the solution that steps A is prepared join in the solution of step B preparation, stir, and add buffer agent, add the injection water, add active carbon, continue heated and stirred 15 minutes; Decarbonization filtering adds buffer agent, and stirring and dissolving through 0.22 μ m filtering with microporous membrane, gets the polyene phosphatidylcholine concentrated wiring liquid.
7. the preparation method of polyene phosphatidylcholine high-capacity injection as claimed in claim 6, the manufacture method that it is characterized in that described isotonic agent concentrated wiring liquid is to get the water for injection that isotonic agent adds 3 times of amounts, stirring and dissolving, add water, adding 0.3% active carbon boiled 15 minutes, through sand filtration rod filtering decarbonization,, get the isotonic agent concentrated wiring liquid through 0.22 μ m filtering with microporous membrane.
8. as the preparation method of claim 6 and 7 described polyene phosphatidylcholine high-capacity injections, it is characterized in that: preparation polyene phosphatidylcholine high-capacity injection finished product, isotonic agent concentrated wiring liquid and polyene phosphatidylcholine concentrated wiring liquid are filled into respectively in the different chamber of the soft bag in the two chambers of non-PVC, the fill amount of polyene phosphatidylcholine concentrated wiring liquid and isotonic agent concentrated wiring liquid is 4: 1, seal, high temperature sterilize, lucifuge is cooled to room temperature, get through two chambers bag sealing coat, make it fully mixed, get the polyene phosphatidylcholine high-capacity injection finished product.
CNA2007100049535A 2007-02-13 2007-02-13 Polyene phosphatidylcholine high-capacity injection Pending CN101244070A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
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Application Number Priority Date Filing Date Title
CNA2007100049535A CN101244070A (en) 2007-02-13 2007-02-13 Polyene phosphatidylcholine high-capacity injection

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CN101244070A true CN101244070A (en) 2008-08-20

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101756895B (en) * 2009-03-13 2012-05-16 北京瑞伊人科技发展有限公司 Polyene phosphatidyl choline intravenous preparation and preparation method thereof
CN102631313A (en) * 2011-11-10 2012-08-15 上海天氏利医药科技有限公司 Polyene phosphatidyl choline intravenous administration preparation and preparation method thereof
CN103816118A (en) * 2014-02-14 2014-05-28 西藏海思科药业集团股份有限公司 Polyene phosphatidyl choline composition for injection and preparation method thereof

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101756895B (en) * 2009-03-13 2012-05-16 北京瑞伊人科技发展有限公司 Polyene phosphatidyl choline intravenous preparation and preparation method thereof
CN102631313A (en) * 2011-11-10 2012-08-15 上海天氏利医药科技有限公司 Polyene phosphatidyl choline intravenous administration preparation and preparation method thereof
CN103816118A (en) * 2014-02-14 2014-05-28 西藏海思科药业集团股份有限公司 Polyene phosphatidyl choline composition for injection and preparation method thereof

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Open date: 20080820