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Cefathiamidine prosoma liposome preparation

The technology of cefathiamidine and prolipid, which is applied in the field of medicine, can solve the problems of increased cost of organic solvents, high requirements on environmental equipment, unsecured safety and the like, and achieves low cost, reduced drug toxicity, and improved drug performance. The effect of therapeutic index

Inactive Publication Date: 2010-04-14
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The methods of the above two patents both use organic solvents to dissolve and purify cefathiamidine, and then carry out aseptic subpackaging. A large amount of organic solvents increase the cost and safety cannot be guaranteed, and aseptic subpackaging requires high environmental equipment. Not conducive to operation

Method used

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  • Cefathiamidine prosoma liposome preparation
  • Cefathiamidine prosoma liposome preparation
  • Cefathiamidine prosoma liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation of embodiment 1 cefathiamidine proliposome

[0054] prescription:

[0055] Component Dosage

[0056] Cefathiamidine 50g

[0057] Hydrogenated Soy Lecithin 300g

[0058] Poloxamer 188 220g

[0059] Sodium deoxycholate 125g

[0060] Mannitol 300g

[0061] Trehalose 150g

[0062] Preparation

[0063] (1) 300g of hydrogenated soybean lecithin, 220g of poloxamer 188 and 125g of sodium deoxycholate were dissolved in 2600ml of ethanol and tert-butanol in a mixed solvent with a volume ratio of 4:1, mixed evenly, and placed in a rotary thin film evaporator Ethanol and tert-butanol were removed under reduced pressure to obtain a phospholipid film;

[0064] (2) Add 1500ml of phosphoric acid-dipotassium hydrogen phosphate buffer solution with a pH value of 5.5, shake, stir for 30min, and rotate at a speed of 400r / min to completely hydrate the phospholipid membrane. , and then filtered with a 0.45 μm microporous membrane to obtain a blank liposome suspension...

Embodiment 2

[0067] The preparation of embodiment 2 cefathiamidine proliposome

[0068] prescription:

[0069] Component Dosage

[0070] Cefathiamidine 100g

[0071] Hydrogenated Soy Lecithin 400g

[0072] Poloxamer 188 200g

[0073] Sodium deoxycholate 80g

[0074] Glucose 75g

[0075] Sorbitol 225g

[0076] Preparation

[0077] (1) 400g of hydrogenated soybean lecithin, 200g of poloxamer 188 and 80g of sodium deoxycholate were dissolved in 2100ml of isopropanol and acetone in a mixed solvent with a volume ratio of 3:1, mixed evenly, and placed on a rotary thin film evaporator Isopropanol and acetone were removed under reduced pressure to obtain a phospholipid film;

[0078] (2) Add 1050ml of acetic acid-sodium acetate buffer solution with a pH value of 5.0, shake, stir for 20min, and rotate at a speed of 600r / min to completely hydrate the phospholipid membrane. Filter with a 0.45 μm microporous membrane to obtain a blank liposome suspension;

[0079] (3) Dissolve 100g of cefath...

Embodiment 3

[0081] The preparation of embodiment 3 cefathiamidine proliposome

[0082] prescription:

[0083] Component Content

[0084] Cefathiamidine 200g

[0085] Hydrogenated Soy Lecithin 2000g

[0086] Poloxamer 188 1600g

[0087] Sodium deoxycholate 1000g

[0088] Lactose 1500g

[0089] Dextran 1500g

[0090] Preparation

[0091] (1) 2000g hydrogenated soybean lecithin, 1600g poloxamer 188 and 1000g sodium deoxycholate are dissolved in 23000ml n-hexane and methanol volume ratio 1: 2 mixed solvent, mix well, reduce on rotary film evaporator Remove n-hexane and methanol under pressure to obtain a phospholipid film;

[0092] (2) Add 18000ml of citric acid-sodium citrate buffer solution with a pH value of 6.0, shake, stir for 40min, and rotate at a speed of 200r / min to completely hydrate the phospholipid membrane. / min, then filter with a 0.3 μm microporous membrane to obtain a blank liposome suspension;

[0093] (3) Dissolve 200g of cefathiamidine in 10,000ml of water, filter...

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Abstract

The invention provides a cefathiamidine prosoma liposome preparation, which comprises the following ingredients by shares: 1 share of cefathiamidine, 3-20 shares of hydrogenated soya bean lecithin, 2-12 shares of poloxamer 188-, 0.5-10 shares of deoxysodium cholate and 1-30 shares of proppants. The invention further provides a preparation method and usage of prosoma liposome. The prosoma liposome of the invention has the advantages of high stability, high entrapping efficiency, even grain diameters, small side effects and the like.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a cefathiamidine proliposome preparation and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Cefathiamidine, also known as cephalosporin-18, cephalosporin pyramidine, cephalosporin thioamidine, its chemical name is: (6R, 7R)-3[(acetyl)methyl]-7-[α-(N , N'-diisopropylamidinothio)-acetylamino]-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylate betaine salt, formula C 19 h 28 N 4 o 6 S 2 , molecular weight 472.59, structural formula: [0003] [0004] It is a β-lactam antibiotic, the first-generation cephalosporin, and its antibacterial spectrum is similar to that of cephalothin. It has strong antibacterial effect on G+ bacteria, especially has a unique effect on G+ enterococci. A cephalosporin exclusive to cocci. It is mainly used for respiratory tract infection, biliary tract, urinary tract, gynecological diseases...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/14A61K9/19A61K31/545A61K47/34A61K47/28A61K47/24A61K47/36A61P31/04A61P11/00A61P1/16A61P13/02A61P15/00A61P7/00A61P25/00A61K47/10
Inventor 邱民
Owner HAINAN LINGKANG PHARMA CO LTD
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