CN1602878A - Preparation process of polyene phosphatidylcholine injection - Google Patents
Preparation process of polyene phosphatidylcholine injection Download PDFInfo
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- CN1602878A CN1602878A CN 200410056865 CN200410056865A CN1602878A CN 1602878 A CN1602878 A CN 1602878A CN 200410056865 CN200410056865 CN 200410056865 CN 200410056865 A CN200410056865 A CN 200410056865A CN 1602878 A CN1602878 A CN 1602878A
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- polyene phosphatidylcholine
- injection
- polyene
- benzyl alcohol
- activated carbon
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Abstract
The invention discloses a method for preparing polyene phosphatidyl choline injection, including mixing polyene phosphatidyl choline, solubilizer, and injection water in proportion, stirring them into a colloidal dispersive system, adding in activated carbon to absorb, and adding proper antiseptic. It is a low-cost, simple-technique preparing method.
Description
Technical field
The present invention relates to a kind of preparation method of Polyene Phosphatidylcholine injection liquid, belong to the technical field of medicament preparation.
Technical background
Polyene Phosphatidylcholine injection liquid is a kind of liver plasma membrane protective agent, treats multiple hepatic disease.Its main component is natural polyene phosphatidylcholine, contains a large amount of unsaturated fatty acids, is mainly linoleic acid (accounting for 70%), linolenic acid and oleic acid.Various hepatopathys all exist liver plasma membrane and the damage of cell mitochondrial ultrastructure and companion's phospholipid to lose, Cellular respiration and energy are synthetic not enough, take supplemented with exogenous phospholipid, how unsaturated phospholipid is introduced in the liver plasma membrane structure, substitute the endogenous saturated phospholipid, membrane fluidity and transmembrane transport system activity are strengthened, and impaired membrane structure is therefore recovered.This medicine is a most sure hepatic of present curative effect.Liposome with the preparation of its hypotoxicity, phase commute, can avoid the degraded of medicine and can realize advantage such as targeting administration, often extensively used as pharmaceutical carrier, be a kind of common medicinal supplementary material.But as principal agent, required dissolved concentration is higher, and relative difficulty is also big, and domestic Polyene Phosphatidylcholine injection liquid mainly relies on import at present, and cost is higher, costs an arm and a leg.
Summary of the invention
The present invention is directed to above problem, it is low to have studied a kind of cost, and technology simply prepares the method for Polyene Phosphatidylcholine injection liquid.
Insoluble in water among the present invention owing to polyene phosphatidylcholine, it is higher again to make the injection desired concn, therefore to select appropriate solubilizing agent, and both to be added by a certain percentage the injection water stir, until becoming uniform translucent colloidal dispersion, selected solubilizing agent is a kind of in sodium cholate, NaTDC, the sodium dehydrocholate, and the ratio of solubilizing agent and principal agent is 1.8-2.5.Add the 0.05-0.2% active carbon and adsorb 15-25min, according to the physicochemical property of preparation component and the performance of filter material, select for use sintered glass filter to remove by filter and be suspended in the mechanical admixture (white point, color dot, fiber etc.) of solution and the antibacterial that in preparation, falls into then.Again because natural polyene phosphatidylcholine, easily oxidation, so must add antiseptic in preparation, selected antiseptic is a benzyl alcohol, its final concentration is 95-105%.In addition, benzyl alcohol also can play the effect of the agent that relieves the pain.
Key step of the present invention is with polyene phosphatidylcholine, solubilizing agent, 3/5 water for injection, stirs under nitrogen current until becoming uniform translucent colloidal dispersion.Add activated carbon adsorption, under nitrogen current with No. 3 incipient fusion filter coarse filtration.Add antiseptic and remaining water for injection then, the circulation homogenize is mended and is added water to capacity for several times, and the circulation homogenize is even.With the microporous filter membrane of 0.45 μ m filter (taking a sample to check) qualified after, fill in the peace of 5ml is cutd open, towards nitrogen, sealing by fusing, 121 ℃, sterilization in 15 minutes.
The present invention and finished product thereof have been carried out necessary detection, and the result is as follows
1, the Polyene Phosphatidylcholine injection liquid that the present invention is prepared carries out clarity test, loading quantity inspection, related substance inspection, sterility test, bacterial endotoxin inspection, assay, and the result all meets standards of pharmacopoeia.
2, get polyene phosphatidylcholine, the NaTDC of recipe quantity, be configured to 200ml polyene phosphatidylcholine colloidal dispersion, detection adds activated carbon adsorption front and back character, pH value, related substance and assay.
After adsorbing before the test item absorption
The yellow clear liquid of the yellow clear liquid of character
PH value 8.80 8.82
Related substance 1.01 1.00
Assay 97.29 97.22
Active carbon does not all have obvious absorption to benzyl alcohol and polyene phosphatidylcholine among proof the present invention.
3, investigate the influence of embedding sterilization to pH value, clarity and change color.Sterilizing methods routinely (121 ℃ of 15min) is surveyed sterilization front and back character, pH value, related substance and assay.
After sterilizing before the test item sterilization
Character colourless clear liquid colourless clear liquid
PH value 8.74 8.07
Relevant PC (%) 0.96 0.98
Material benzyl alcohol (%) 0.09 0.12
Content PC (%) 97.41 97.36
Measure benzyl alcohol (%) 98.82 98.70
The Polyene Phosphatidylcholine injection liquid that proof is prepared with the present invention uses conventional sterilizing methods to get final product.
4, light stability is investigated
Press the Polyene Phosphatidylcholine injection liquid that the present invention prepares,, detect, and compare with 0 o'clock sample by stable high spot reviews project placing 10 days under the intensity of illumination of illumination 4500lx ± 500lx and under 40 ℃ of conditions of high temperature in sampling in the 5th, 10 day.
Proof is degraded not obvious under illumination and high temperature (40 ℃) condition with the Polyene Phosphatidylcholine injection liquid that the present invention prepares.
The specific embodiment
Following specific embodiment will further specify the present invention.
Embodiment 1
With preparation 5000ml Polyene Phosphatidylcholine injection liquid is example, with 232.5g polyene phosphatidylcholine, 500g NaTDC and 3/5 water for injection, stirs under nitrogen current until becoming uniform translucent colloidal dispersion.Add 5g activated carbon adsorption 20min, under nitrogen current with No. 3 incipient fusion filter coarse filtration.Add 45g benzyl alcohol and remaining water for injection then, the circulation homogenize is mended and is added water to capacity for several times, and the circulation homogenize is even.With the microporous filter membrane of 0.45 μ m filter (taking a sample to check) qualified after, fill in the peace of 5ml is cutd open, towards nitrogen, sealing by fusing, 121 ℃, sterilization in 15 minutes.
Embodiment 2
With preparation 5000ml Polyene Phosphatidylcholine injection liquid is example, with 232.5g polyene phosphatidylcholine, 420g sodium dehydrocholate and 3/5 water for injection, stirs under nitrogen current until becoming uniform translucent colloidal dispersion.Add 2.5g activated carbon adsorption 15min, under nitrogen current with No. 3 incipient fusion filter coarse filtration.Add 40g benzyl alcohol and remaining water for injection then, the circulation homogenize is mended and is added water to capacity for several times, and the circulation homogenize is even.With the microporous filter membrane of 0.45 μ m filter (taking a sample to check) qualified after, fill in the peace of 5ml is cutd open, towards nitrogen, sealing by fusing, 121 ℃, sterilization in 15 minutes.
Embodiment 3
With preparation 5000ml Polyene Phosphatidylcholine injection liquid is example, with 232.5g polyene phosphatidylcholine, 580g sodium cholate and 3/5 water for injection, stirs under nitrogen current until becoming uniform translucent colloidal dispersion.Add 10g activated carbon adsorption 25min, under nitrogen current with No. 3 incipient fusion filter coarse filtration.Add 47.5g benzyl alcohol and remaining water for injection then, the circulation homogenize is mended and is added water to capacity for several times, and the circulation homogenize is even.With the microporous filter membrane of 0.45 μ m filter (taking a sample to check) qualified after, fill in the peace of 5ml is cutd open, towards nitrogen, sealing by fusing, 121 ℃, sterilization in 15 minutes.
Although described the present invention by specific embodiment, some is revised and equivalence is obvious for the technical staff who is proficient in this field, and these variations are believed to comprise within the scope of the present invention.
Claims (7)
1, a kind of preparation method of Polyene Phosphatidylcholine injection liquid comprises polyene phosphatidylcholine, solubilizing agent, water for injection are stirred to the colloidal dispersion, adds activated carbon adsorption, adds suitable antiseptic.
2, the method for claim 1, wherein said solubilizing agent is selected from sodium cholate, NaTDC, sodium dehydrocholate.
3, the method for claim 1, the ratio of wherein said solubilizing agent and polyene phosphatidylcholine are 1.8-2.5: 1.
4, the method for claim 1, its final concentration of wherein said active carbon is 0.05-0.2%.
5, the method for claim 1,15-25min is carried out in wherein said activated carbon adsorption.
6, the method for claim 1, wherein said antiseptic are benzyl alcohol.
7, benzyl alcohol as claimed in claim 6, its final concentration are 95-105%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410056865 CN1602878A (en) | 2004-08-26 | 2004-08-26 | Preparation process of polyene phosphatidylcholine injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410056865 CN1602878A (en) | 2004-08-26 | 2004-08-26 | Preparation process of polyene phosphatidylcholine injection |
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|---|---|
| CN1602878A true CN1602878A (en) | 2005-04-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CN 200410056865 Pending CN1602878A (en) | 2004-08-26 | 2004-08-26 | Preparation process of polyene phosphatidylcholine injection |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1314401C (en) * | 2005-09-08 | 2007-05-09 | 四川科伦药业股份有限公司 | Polyenic phosphatide acylcholine freeze-dried powder injecta medicine |
| CN100366238C (en) * | 2005-10-25 | 2008-02-06 | 江苏正大天晴药业股份有限公司 | Freeze dried polyene lecithin powder for injection and its prepn |
| CN100393317C (en) * | 2005-10-08 | 2008-06-11 | 北京国仁堂医药科技发展有限公司 | Polyene phosphatidyl choline infusion solution and its preparing method |
| 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 |
| CN103705446A (en) * | 2012-10-08 | 2014-04-09 | 正大天晴药业集团股份有限公司 | Polyene phosphatidyl choline injection, and preparation method thereof |
-
2004
- 2004-08-26 CN CN 200410056865 patent/CN1602878A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1314401C (en) * | 2005-09-08 | 2007-05-09 | 四川科伦药业股份有限公司 | Polyenic phosphatide acylcholine freeze-dried powder injecta medicine |
| CN100393317C (en) * | 2005-10-08 | 2008-06-11 | 北京国仁堂医药科技发展有限公司 | Polyene phosphatidyl choline infusion solution and its preparing method |
| CN100366238C (en) * | 2005-10-25 | 2008-02-06 | 江苏正大天晴药业股份有限公司 | Freeze dried polyene lecithin powder for injection and its prepn |
| 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 |
| CN103705446A (en) * | 2012-10-08 | 2014-04-09 | 正大天晴药业集团股份有限公司 | Polyene phosphatidyl choline injection, and preparation method thereof |
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