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Cefsulodin sodium liposome injection

A technology of cefsulodin sodium and sulfsulodin sodium lipid, applied in the field of medicine, can solve problems such as leakage of encapsulated drugs, easy aggregation and fusion of liposomes, and achieve enhanced stability, excellent stability, and wide storage conditions. Effect

Inactive Publication Date: 2010-12-08
HAINAN YONGTIAN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The stability of liposomes has long been an important problem that has limited the wide application of liposomes. Liposomes are generally prone to aggregation and fusion, resulting in leakage of encapsulated drugs. Therefore, the industrial preparation of pharmaceutical liposomes that meet the stability requirements It is not easy, and those skilled in the field of pharmaceuticals with general experience clearly know that they face various difficulties in the preparation of pharmaceutical liposomes, all of which are by no means expected to be solved by simple theory, and many difficulties need to be overcome

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  • Cefsulodin sodium liposome injection
  • Cefsulodin sodium liposome injection
  • Cefsulodin sodium liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The preparation of embodiment 1 cefsulodin sodium liposome injection

[0053] Prescription (100 bottles):

[0054] Cefsulodin sodium 10g

[0055] Egg yolk lecithin 50g

[0056] Sodium Glycocholate 27g

[0057] Tween 8016g

[0058] Sodium bisulfite 5g

[0059] Glucose 20g

[0060] Mannitol 60g

[0061] Preparation Process

[0062] (1) Add 50g egg yolk lecithin, 27g sodium glycocholate, and 16g Tween 80 into 800ml of a mixed solvent of dichloromethane and acetone at a volume ratio of 4:1, heat and stir to disperse evenly, and place on a rotary thin film evaporator Remove the organic solvent under reduced pressure to obtain a phospholipid film;

[0063] (2) Add 400ml of acetic acid-sodium acetate buffer solution with a pH value of 5.6, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and microporous membrane filtration to obtain a blank liposome suspension;

[0064] (3) Dissolve 10 g of cefsulodin sodium in 200 ml of...

Embodiment 1

[0066] The preparation of comparative example 1 cefsulodin sodium liposome injection

[0067] Prescription (100 bottles):

[0068] Cefsulodin sodium 10g

[0069] Egg yolk lecithin 50g

[0070] Tween 8016g

[0071] Sodium bisulfite 5g

[0072] Glucose 20g

[0073] Mannitol 60g

[0074] The preparation process was the same as in Example 1, and cefsulodin sodium liposome injection without sodium glycocholate was prepared.

Embodiment 2

[0075] The preparation of embodiment 2 cefsulodin sodium liposome injection

[0076] Prescription (100 bottles):

[0077] Cefsulodin sodium 20g

[0078] Egg yolk lecithin 44g

[0079] Sodium Glycocholate 12g

[0080] Tween 806g

[0081] Sodium sulfite 1.2g

[0082] Glucose 17.5g

[0083] Mannitol 52.5g

[0084] Preparation Process

[0085] (1) Add 44g egg yolk lecithin, 12g sodium glycocholate, and 6g Tween 80 into 800ml of a mixed solvent of dichloromethane and acetone at a volume ratio of 4:1, heat and stir to disperse evenly, and place on a rotary film evaporator Remove the organic solvent under reduced pressure to obtain a phospholipid film;

[0086] (2) Add 500ml of citric acid-sodium citrate buffer solution with a pH value of 5.6, shake and stir to make the phospholipid membrane completely hydrated, high-speed homogeneously emulsified, and filtered through a microporous membrane to prepare a blank liposome mixture suspension;

[0087] (3) Dissolve 20 g of cefsu...

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Abstract

The invention provides a cefsulodin sodium liposome injection, which is characterized by consisting of the following components in part by weight: 1 part of cefsulodin sodium, 1.8 to 13 parts of yolk lecithin, 0.3 to 7 parts of sodium glycyl-cholate, 0.1 to 5 parts of Tween 80, 0.02 to 3 parts of antioxidant and 2 to 20 parts of excipient. The cefsulodin sodium liposome injection prepared by the invention has the advantages of better solubility, better stability, high entrapment efficiency, lower side effect, higher bioavailability and more obvious treatment effect.

Description

technical field [0001] The invention relates to a liposome injection, in particular to a cefsulodin sodium liposome injection, which belongs to the technical field of medicine. Background technique [0002] Cefsulodin sodium, its chemical name is [6R-[6R,7β(R*)]]-4(carbamoyl)-1-[3-[2-carboxy-8-oxidation-7-[(phenyl Sulfoacetamide)]-5-thia-1-azabicyclo[4,2,0]oct-2-ene]methyl]pyridinium inner salt sodium salt, the molecular formula is C 22 h 19 N 4 NaO 8 S 2 , the molecular weight is: 554.52, and the structural formula is: [0003] [0004] Cefsulodine sodium belongs to the third generation of cephalosporin antibiotics. Cephalosporin antibiotics for Pseudomonas aeruginosa injection. Clinically, it is mainly used for various secondary infections of sepsis, pneumonia, bronchitis, bronchiectasis complications, pyelonephritis, cystitis, peritonitis, trauma or burn caused by Pseudomonas aeruginosa. [0005] Chinese patent CN1732948A discloses a preparation process of cefs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/546A61K47/34A61K47/24A61K47/28A61P31/04A61P11/00A61P13/12A61P13/10A61P17/02A61K47/26
Inventor 王明
Owner HAINAN YONGTIAN PHARMA INST
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