A kind of meropenem liposome injection

A technology of meropenem and liposome, which is applied in the directions of non-active ingredients medical preparations, organic active ingredients, powder delivery, etc., can solve the problems of low bioavailability of meropenem, and improve the quality of preparation products and the encapsulation efficiency. The effect of high and improved therapeutic index

Inactive Publication Date: 2011-11-30
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The currently marketed meropenem drug products are mainly injections, which simply freeze-dry meropenem, and the bioavailability of meropenem in this dosage form is low

Method used

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  • A kind of meropenem liposome injection
  • A kind of meropenem liposome injection
  • A kind of meropenem liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Meropenem liposome injection

[0036] Prescription (1000 bottles):

[0037]

[0038] Production Process:

[0039] (1) Add 25g of meropenem, 100g of phosphatidylethanolamine, 125g of cholesterol, 5g of tert-butyl-p-hydroxyanisole and 25g of polyether 188 into 800ml of a mixed solvent of ethanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly , remove ethanol and acetone under reduced pressure on a rotary evaporator to prepare a phospholipid film;

[0040] (2) Add 800ml of carbonate buffer solution with a pH of 5.6, shake and stir to completely hydrate the phospholipid membrane, high-speed homogeneously emulsify, and filter through a microporous membrane to prepare a meropenem liposome suspension;

[0041] (3) Add 250 g of PVP to the above liposome suspension, keep warm at 40-50°C and stir for 20-30 minutes to dissolve, then cool to room temperature to obtain a meropenem liposome solution;

[0042] (4) The above solution was freeze...

Embodiment 2

[0043] Example 2 Preparation of meropenem liposome injection

[0044] Prescription (1000 bottles):

[0045]

[0046] Preparation Process:

[0047] (1) Add 50g of meropenem, 300g of phosphatidylethanolamine, 150g of cholesterol, 10g of tert-butyl-p-hydroxyanisole and 40g of polyether 188 into 1000ml of a mixed solvent of ethanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly , remove ethanol and acetone under reduced pressure on a rotary evaporator to prepare a phospholipid film;

[0048] (2) Add 1000ml of carbonate buffer solution with a pH of 5.6, shake and stir to completely hydrate the phospholipid membrane, high-speed homogeneously emulsify, and filter through a microporous membrane to prepare a meropenem liposome suspension;

[0049] (3) Add 300 g of PVP to the above liposome suspension, keep warm at 40-50°C and stir for 20-30 minutes to dissolve it, then cool to room temperature to obtain a meropenem liposome solution;

[0050] (4) The above...

Embodiment 3

[0051] Example 3 Preparation of meropenem liposome injection

[0052] Prescription (1000 bottles):

[0053]

[0054] Preparation Process:

[0055] (1) Add 100g of meropenem, 200g of phosphatidylethanolamine, 100g of cholesterol, 10g of tert-butyl-p-hydroxyanisole and 20g of polyether 188 into 800ml of a mixed solvent of ethanol and acetone with a volume ratio of 3:1, heat and stir to disperse evenly , remove ethanol and acetone under reduced pressure on a rotary evaporator to prepare a phospholipid film;

[0056] (2) Add 800ml of carbonate buffer solution with a pH of 5.6, shake and stir to completely hydrate the phospholipid membrane, high-speed homogeneously emulsify, and filter through a microporous membrane to prepare a meropenem liposome suspension;

[0057] (3) Add 500 g of PVP to the above liposome suspension, keep warm at 40-50°C and stir for 20-30 minutes to dissolve, then cool to room temperature to obtain a meropenem liposome solution;

[0058] (4) The above s...

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Abstract

The invention discloses a meropenem liposome injection, which is characterized by mainly comprising the following components of: by weight, one part of meropenem, 2-8 parts of phosphatidylethanolamine, 1-5 parts of cholesterol, 0.2-1 part of polyether 188, 0.1-0.4 part of an antioxidant, and 5-10 parts of a supporting agent. The liposome injection prepared in the invention has good redissolving performance, good stability, high entrapment rate and little side-effect, can be used to raise the preparation product quality, minimize toxic and side effects and improve the bioavailability, and has remarkable curative effects.

Description

technical field [0001] The invention relates to a preparation method of meropenem liposome injection, belonging to the field of pharmaceutical preparations. Background technique [0002] Meropenem (Biapenem), belonging to penem antibiotics, is a white to slightly yellow crystalline powder, and its chemical name is: (-)6-[[(4R,5S,6S)-2-carboxy-6[(1R) -1-Hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-en-3-yl]thio]-6,7-dihydro-5H- Pyrazol[1,2-a][1,2,4]triazol-4-ium inner salt, the molecular formula is: C 15 h 18 N 4 o 4 S, molecular weight: 350.40, structural formula: [0003] [0004] Meropenem produces antibacterial effects by inhibiting the synthesis of bacterial cell walls. Meropenem easily penetrates the cell walls of most Gram-positive and negative bacteria and reaches its target penicillin-binding protein. [0005] Meropenem is sensitive to both Gram-positive and Gram-negative bacteria, and has strong antibacterial activity especially against Gram-negati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/407A61K47/34A61P31/04
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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