A kind of imipenem cilastatin sodium pharmaceutical composition liposome injection

A technology of imipenem cilastatin sodium and cilastatin sodium, which is applied in the field of medicine, can solve problems such as unsolved oxidative decomposition of components, accurate proportioning of content, and impact on the quality of final products, so as to avoid organic Solvent toxicity, small particle size, and the effect of improving encapsulation efficiency

Inactive Publication Date: 2011-12-07
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long exposure in complex production process (mixing, sub-packaging), difficulty in hypoxic or anaerobic environment in infusion bottles will affect the quality of the final product
[0012] Patent document CN1568975A discloses a method for preparing a pharmaceutical composition using a mixture of imipenem and cilastatin sodium as an active ingredient, which includes two technical solutions: first, combining imipenem and cilastatin sodium After decibels of butyl sodium are made into freeze-dried powders, they are mixed; secondly, imipenem and cilastatin sodium are made into freeze-dried powders together. Compared to technical problems

Method used

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  • A kind of imipenem cilastatin sodium pharmaceutical composition liposome injection
  • A kind of imipenem cilastatin sodium pharmaceutical composition liposome injection
  • A kind of imipenem cilastatin sodium pharmaceutical composition liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Imipenem cilastatin sodium pharmaceutical composition liposome injection

[0039] Prescription (1000 bottles):

[0040]

[0041] Preparation Process:

[0042] (1) 150g sphingomyelin, 50g cholesterol, 50g Pluronic F-68 are dissolved in the phosphate buffered saline solution of pH6.5 of 600ml, make blank heterogeneous liposome;

[0043] (2) Dissolve 100g of imipenem and 100g of cilastatin sodium in 400ml of pH 6.5 phosphate buffer solution, stir to dissolve completely;

[0044] (3) After the blank liposome prepared in step (1) and the imipenem cilastatin sodium buffered phosphate solution in step (2) are sterilized by circulating steam, the sterilized solution is treated twice by ultrasonic method , 10 minutes each time;

[0045](4) Under sterile conditions, add imipenem cilastatin sodium buffer solution to the blank liposomes in a molten state at 60°C, stir, then add 150g trehalose and 50g PVP, continue stirring to dissolve it, and obtain Imipenem cilast...

Embodiment 2

[0047] Example 2 Imipenem cilastatin sodium pharmaceutical composition liposome injection

[0048] Prescription (1000 bottles):

[0049]

[0050] Preparation Process:

[0051] (1) 175g sphingomyelin, 100g cholesterol, 75g Pluronic F-68 are dissolved in the phosphate buffered saline solution of pH6.5 of 800ml, make the multiphase liposome of blank;

[0052] (2) Dissolve 50g of imipenem and 50g of cilastatin sodium in 200ml of pH 6.5 phosphate buffer solution, and stir to make it completely dissolved;

[0053] (3) After the blank liposome prepared in step (1) and the imipenem cilastatin sodium buffered phosphate solution in step (2) are sterilized by circulating steam, the sterilized solution is treated twice by ultrasonic method , 10 minutes each time;

[0054] (4) Under sterile conditions, add imipenem cilastatin sodium buffer solution to the blank liposomes in a molten state at 60°C, stir, then add 200g trehalose and 100g PVP, continue stirring to dissolve it, and obtai...

Embodiment 3

[0056] Example 3 Imipenem cilastatin sodium pharmaceutical composition liposome injection

[0057] Prescription (1000 bottles):

[0058]

[0059] Preparation Process:

[0060] (1) 62.5g sphingomyelin, 25g cholesterol, 50g Pluronic F-68 are dissolved in the phosphate buffered saline solution of pH6.5 of 400ml, make the multiphase liposome of blank;

[0061] (2) Dissolve 25g of imipenem and 25g of cilastatin sodium in 100ml of pH6.5 phosphate buffer solution, stir to make it completely dissolve;

[0062] (3) After the blank liposome prepared in step (1) and the imipenem cilastatin sodium buffered phosphate solution in step (2) are sterilized by circulating steam, the sterilized solution is treated twice by ultrasonic method , 10 minutes each time;

[0063] (4) Under sterile conditions, add imipenem cilastatin sodium buffer solution to the blank liposomes in the molten state at 60°C, stir, then add 75g trehalose and 25g PVP, continue stirring to dissolve it, and obtain Imi...

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PUM

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Abstract

The invention provides an imipenem and cilastatin sodium pharmaceutical composition liposome injection, comprising imipenem, cilastatin sodium, sphingomyelin, cholesterol, an emulsifier and a cryoprotectant. The imipenem and cilastatin sodium injection prepared by using the method provided by the invention improves the quality of the preparation product, reduces toxic and adverse effects, increases bioavailability of medicinal components, and has good preparation stability. During the lyopilization process, liposomes do not break due to dehydration, fusion, ice crystals, and so on, and after hydration redissolution, liposomes also remain good encapsulation rate.

Description

technical field [0001] The invention relates to an antibiotic liposome preparation, in particular to an imipenem cilastatin sodium pharmaceutical composition liposome injection, which belongs to the technical field of medicine. Background technique [0002] Imipenem (Imipenem), the chemical name is (5R,6S)-6-[(1R)-1-hydroxyethyl]-3-[[2-[(iminomethyl)amino]ethyl]sulfur Generation]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid monohydrate, molecular formula C 12 h 17 N 3 o 4 S·H 2 O, molecular weight 317.4, structural formula: [0003] [0004] Imipenem is a carbapenem antibiotic, which has antibacterial effect on Gram-positive and negative aerobic and anaerobic bacteria. The antibacterial spectrum includes Streptococcus, Staphylococcus aureus, E. coli, Klebsiella, and Part of the strains of Actinobacillus, Haemophilus influenzae, Proteus, Serratia, Pseudomonas aeruginosa, etc. Imipenem is especially suitable for mixed infections caused by various pathogens a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/407A61K31/198A61K9/127A61K47/24A61K47/28A61K47/34A61K47/36A61K47/32A61P31/04
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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