Sulbenicillin sodium liposome injection

Abstract

The invention discloses a sulbenicillin sodium liposome injection, which is characterized by comprising the following components in part by weight preferably: 1 part of sulbenicillin sodium, 3 to 5 parts of soya bean lecithin, 0.8 to 2 parts of cholesterol, 0.2 to 1 part of dipalmitoyl phosphatidylethanolamine, 0.1 to 0.5 part of antioxygen and 5 to 10 parts of excipient. The liposome injection prepared by the invention has the advantages of obvious technical effect, high dissolvability and stability, high encapsulating rates, small side effect, high bioavailability and obvious curative effect.

Description

technical field

[0001] The invention relates to a liposome injection, in particular to a liposome injection of sulbenicillin sodium, which belongs to the technical field of medicine. Background technique

[0002] Sulbenicillin Sodium, its chemical name is (2S,5R,6R)-3,3-Dimethyl-6-(2-phenyl-2-sulfoacetamido)-7-oxo-4-thia -1-Azabicyclo[3.2.0]heptane-2-carboxylic acid disodium salt, molecular formula C 16 h 16 N 2 Na 2 o 7 S 2 , molecular weight 458.42, structural formula:

[0003]

[0004] Sulbenicillin sodium is a broad-spectrum semi-synthetic penicillin antibiotic, which is effective against Enterobacteriaceae such as Escherichia coli, Proteus, Enterobacter, Citrobacter, Salmonella and Shigella, as well as Pseudomonas aeruginosa Bacteria, Haemophilus influenzae, Neisseria and other Gram-negative bacteria have antibacterial activity; it also has antibacterial activity against hemolytic streptococcus, Streptococcus pneumoniae and staphylococcus that does not produce...

Examples

Embodiment 1

[0053] The preparation of embodiment 1 sulbenicillin sodium liposome injection

[0054] Prescription (100 bottles):

[0055] Sulbenicillin Sodium 100g

[0056] Soy Lecithin 300g

[0057] Cholesterol 80g

[0058] Dipalmitoyl Phosphatidylethanolamine 20g

[0059] Vitamin E 10g

[0060] Mannitol 250g

[0061] Trehalose 250g

[0062] Preparation Process

[0063] (1) Add 300g of soybean lecithin, 80g of cholesterol, 20g of dipalmitoylphosphatidylethanolamine, and 10g of vitamin E into 1000ml of a mixed solvent of isopropanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly, and evaporate in a rotary thin film The mixed solvent was removed under reduced pressure on the apparatus to obtain a phospholipid film;

[0064] (2) Add 500ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane at 55-60°C for 1 hour, high-speed homogeneous emulsific...

Embodiment 1

[0067] The preparation of comparative example 1 sulbenicillin sodium liposome injection

[0068] Prescription (100 bottles):

[0069] Sulbenicillin Sodium 100g

[0070] Soy Lecithin 300g

[0071] Cholesterol 80g

[0072] Vitamin E 10g

[0073] Mannitol 250g

[0074] Trehalose 250g

[0075] The preparation process was the same as in Example 1, and the sulfbenicillin sodium liposome injection not containing dipalmitoylphosphatidylethanolamine was prepared.

Embodiment 2

[0076] The preparation of embodiment 2 sulbenicillin sodium liposome injection

[0077] Prescription (100 bottles):

[0078] Sulbenicillin Sodium 200g

[0079] Soy Lecithin 1000g

[0080] Cholesterol 400g

[0081] Dipalmitoyl Phosphatidylethanolamine 200g

[0082] Vitamin E 100g

[0083] Mannitol 1000g

[0084] Trehalose 1000g

[0085] Preparation Process

[0086] (1) Add 1000g of soybean lecithin, 400g of cholesterol, 200g of dipalmitoylphosphatidylethanolamine, and 100g of vitamin E into 5000ml of a mixed solvent of isopropanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly, and evaporate in a rotary film evaporation The mixed solvent was removed under reduced pressure on the apparatus to obtain a phospholipid film;

[0087] (2) Add 3000ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane at 55-60°C for 1 hour, high-speed hom...

technical field

[0001] The invention relates to a liposome injection, in particular to a liposome injection of sulbenicillin sodium, which belongs to the technical field of medicine. Background technique

[0002] Sulbenicillin Sodium, its chemical name is (2S,5R,6R)-3,3-Dimethyl-6-(2-phenyl-2-sulfoacetamido)-7-oxo-4-thia -1-Azabicyclo[3.2.0]heptane-2-carboxylic acid disodium salt, molecular formula C 16 h 16 N 2 Na 2 o 7 S 2 , molecular weight 458.42, structural formula:

[0003]

[0004] Sulbenicillin sodium is a broad-spectrum semi-synthetic penicillin antibiotic, which is effective against Enterobacteriaceae such as Escherichia coli, Proteus, Enterobacter, Citrobacter, Salmonella and Shigella, as well as Pseudomonas aeruginosa Bacteria, Haemophilus influenzae, Neisseria and other Gram-negative bacteria have antibacterial activity; it also has antibacterial activity against hemolytic streptococcus, Streptococcus pneumoniae and staphylococcus that does not produce...

Examples

Embodiment 1

[0053] The preparation of embodiment 1 sulbenicillin sodium liposome injection

[0054] Prescription (100 bottles):

[0055] Sulbenicillin Sodium 100g

[0056] Soy Lecithin 300g

[0057] Cholesterol 80g

[0058] Dipalmitoyl Phosphatidylethanolamine 20g

[0059] Vitamin E 10g

[0060] Mannitol 250g

[0061] Trehalose 250g

[0062] Preparation Process

[0063] (1) Add 300g of soybean lecithin, 80g of cholesterol, 20g of dipalmitoylphosphatidylethanolamine, and 10g of vitamin E into 1000ml of a mixed solvent of isopropanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly, and evaporate in a rotary thin film The mixed solvent was removed under reduced pressure on the apparatus to obtain a phospholipid film;

[0064] (2) Add 500ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane at 55-60°C for 1 hour, high-speed homogeneous emulsific...

Embodiment 1

[0067] The preparation of comparative example 1 sulbenicillin sodium liposome injection

[0068] Prescription (100 bottles):

[0069] Sulbenicillin Sodium 100g

[0070] Soy Lecithin 300g

[0071] Cholesterol 80g

[0072] Vitamin E 10g

[0073] Mannitol 250g

[0074] Trehalose 250g

[0075] The preparation process was the same as in Example 1, and the sulfbenicillin sodium liposome injection not containing dipalmitoylphosphatidylethanolamine was prepared.

Embodiment 2

[0076] The preparation of embodiment 2 sulbenicillin sodium liposome injection

[0077] Prescription (100 bottles):

[0078] Sulbenicillin Sodium 200g

[0079] Soy Lecithin 1000g

[0080] Cholesterol 400g

[0081] Dipalmitoyl Phosphatidylethanolamine 200g

[0082] Vitamin E 100g

[0083] Mannitol 1000g

[0084] Trehalose 1000g

[0085] Preparation Process

[0086] (1) Add 1000g of soybean lecithin, 400g of cholesterol, 200g of dipalmitoylphosphatidylethanolamine, and 100g of vitamin E into 5000ml of a mixed solvent of isopropanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly, and evaporate in a rotary film evaporation The mixed solvent was removed under reduced pressure on the apparatus to obtain a phospholipid film;

[0087] (2) Add 3000ml of potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with a pH value of 5.8, shake and stir to completely hydrate the phospholipid membrane at 55-60°C for 1 hour, high-speed hom...

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