Liposome injection of amoxicillin sodium sulbactam sodium medicinal composition

Abstract

The invention provides liposome injection of an amoxicillin sodium sulbactam sodium medicinal composition. The liposome injection consists of amoxicillin sodium, sulbactam sodium, liposome carriers, freeze-drying supporting agents and optional antioxidant, wherein the liposome carriers are dipalmitoyl phosphatidyl choline and deoxysodium cholate. The liposome injection has high stability; in the freeze-drying process, a phenomenon of breaking liposome caused by dehydration, fusion, ice crystal generation and the like does not occur; and the liposome can remain good encapsulation ratio after being hydrated and redissolved.

Description

technical field

[0001] The invention relates to an antibiotic liposome preparation, in particular to an amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique

[0002] Amoxicillin sodium is a bactericidal broad-spectrum antibiotic, and sulbactam sodium is an irreversible broad-spectrum β-lactamase inhibitor, which can effectively inhibit the β-lactamase produced by drug-resistant bacteria. Many gram-positive and gram-negative bacteria clinically produce β-lactamase, which can make amoxicillin lose its antibacterial activity. Due to the presence of sulbactam sodium, amoxicillin can be protected from the destruction of β-lactamase, so that the bacteria that have been resistant to amoxicillin and produce β-lactamase are still sensitive to amoxicillin. This product is a bactericidal antibiotic, which can kill a variety of Gram-positive and Gram-negativ...

Examples

Embodiment 1

[0038] Example 1 Preparation of amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection

[0039] Prescription (specification 1.5g)

[0040] Amoxicillin Sodium 100g

[0041] Sulbactam Sodium 50g

[0042] Dipalmitoyl Phosphatidylcholine 150g

[0043] Sodium deoxycholate 50g

[0044] Mannitol 150g

[0045] Lactose 50g

[0046] Ascorbyl Palmitate 2.5g

[0047] making process

[0048] (1) 150g of dipalmitoylphosphatidylcholine and 50g of sodium deoxycholate are dissolved in 800ml of a mixed solvent of ethanol and chloroform at a volume ratio of 1:1, and placed on a rotary thin film evaporator to remove the organic solvent under reduced pressure , to obtain a phospholipid film, add pH 6.0 phosphoric acid-dipotassium hydrogen phosphate buffer solution 500ml and stir to dissolve, to obtain a blank liposome solution;

[0049](2) 100g of amoxicillin sodium and 50g of sulbactam sodium were dissolved in 400ml of water for injection, mixed evenly with the ...

Embodiment 2

[0051] Example 2 Amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection preparation

[0052] Prescription (specification 0.75g)

[0053] Amoxicillin Sodium 50g

[0054] Sulbactam Sodium 25g

[0055] Dipalmitoylphosphatidylcholine 175g

[0056] Sodium deoxycholate 100g

[0057] Mannitol 225g

[0058] Lactose 75g

[0059] Ascorbyl Palmitate 1.25g

[0060] making process

[0061] (1) 175g of dipalmitoylphosphatidylcholine and 100g of sodium deoxycholate are dissolved in 1200ml of a mixed solvent of ethanol and chloroform with a volume ratio of 1:1, and placed on a rotary thin film evaporator to remove the organic solvent under reduced pressure , to obtain a phospholipid film, add pH 6.0 phosphoric acid-dipotassium hydrogen phosphate buffer solution 600ml and stir to dissolve, to obtain a blank liposome solution;

[0062] (2) 50g of amoxicillin sodium and 25g of sulbactam sodium were dissolved in 300ml of water for injection, mixed evenly with th...

Embodiment 3

[0064] Example 3 Preparation of Amoxicillin Sodium Sulbactam Sodium Pharmaceutical Composition Liposome Injection

[0065] Prescription (specification 0.375g)

[0066] Amoxicillin Sodium 25g

[0067] Sulbactam Sodium 12.5g

[0068] Dipalmitoylphosphatidylcholine 62.5g

[0069] Sodium deoxycholate 25g

[0070] Mannitol 75g

[0071] Lactose 25g

[0072] Ascorbyl Palmitate 0.25g

[0073] The preparation process was the same as that in Example 2, and amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection was prepared. The components of each prescription and parts by weight of comparative examples 1-3 are as in Table 1.

[0074] Table 1 comparative ratio prescription composition

[0075] components

[0076] components

[0077] Amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection was prepared according to the above prescription components, and the preparation method was the same as in Example 1.

technical field

[0001] The invention relates to an antibiotic liposome preparation, in particular to an amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique

[0002] Amoxicillin sodium is a bactericidal broad-spectrum antibiotic, and sulbactam sodium is an irreversible broad-spectrum β-lactamase inhibitor, which can effectively inhibit the β-lactamase produced by drug-resistant bacteria. Many gram-positive and gram-negative bacteria clinically produce β-lactamase, which can make amoxicillin lose its antibacterial activity. Due to the presence of sulbactam sodium, amoxicillin can be protected from the destruction of β-lactamase, so that the bacteria that have been resistant to amoxicillin and produce β-lactamase are still sensitive to amoxicillin. This product is a bactericidal antibiotic, which can kill a variety of Gram-positive and Gram-negativ...

Examples

Embodiment 1

[0038] Example 1 Preparation of amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection

[0039] Prescription (specification 1.5g)

[0040] Amoxicillin Sodium 100g

[0041] Sulbactam Sodium 50g

[0042] Dipalmitoyl Phosphatidylcholine 150g

[0043] Sodium deoxycholate 50g

[0044] Mannitol 150g

[0045] Lactose 50g

[0046] Ascorbyl Palmitate 2.5g

[0047] making process

[0048] (1) 150g of dipalmitoylphosphatidylcholine and 50g of sodium deoxycholate are dissolved in 800ml of a mixed solvent of ethanol and chloroform at a volume ratio of 1:1, and placed on a rotary thin film evaporator to remove the organic solvent under reduced pressure , to obtain a phospholipid film, add pH 6.0 phosphoric acid-dipotassium hydrogen phosphate buffer solution 500ml and stir to dissolve, to obtain a blank liposome solution;

[0049](2) 100g of amoxicillin sodium and 50g of sulbactam sodium were dissolved in 400ml of water for injection, mixed evenly with the ...

Embodiment 2

[0051] Example 2 Amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection preparation

[0052] Prescription (specification 0.75g)

[0053] Amoxicillin Sodium 50g

[0054] Sulbactam Sodium 25g

[0055] Dipalmitoylphosphatidylcholine 175g

[0056] Sodium deoxycholate 100g

[0057] Mannitol 225g

[0058] Lactose 75g

[0059] Ascorbyl Palmitate 1.25g

[0060] making process

[0061] (1) 175g of dipalmitoylphosphatidylcholine and 100g of sodium deoxycholate are dissolved in 1200ml of a mixed solvent of ethanol and chloroform with a volume ratio of 1:1, and placed on a rotary thin film evaporator to remove the organic solvent under reduced pressure , to obtain a phospholipid film, add pH 6.0 phosphoric acid-dipotassium hydrogen phosphate buffer solution 600ml and stir to dissolve, to obtain a blank liposome solution;

[0062] (2) 50g of amoxicillin sodium and 25g of sulbactam sodium were dissolved in 300ml of water for injection, mixed evenly with th...

Embodiment 3

[0064] Example 3 Preparation of Amoxicillin Sodium Sulbactam Sodium Pharmaceutical Composition Liposome Injection

[0065] Prescription (specification 0.375g)

[0066] Amoxicillin Sodium 25g

[0067] Sulbactam Sodium 12.5g

[0068] Dipalmitoylphosphatidylcholine 62.5g

[0069] Sodium deoxycholate 25g

[0070] Mannitol 75g

[0071] Lactose 25g

[0072] Ascorbyl Palmitate 0.25g

[0073] The preparation process was the same as that in Example 2, and amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection was prepared. The components of each prescription and parts by weight of comparative examples 1-3 are as in Table 1.

[0074] Table 1 comparative ratio prescription composition

[0075] components

[0076] components

[0077] Amoxicillin sodium sulbactam sodium pharmaceutical composition liposome injection was prepared according to the above prescription components, and the preparation method was the same as in Example 1.