Piperacillin sodium and sulbactam sodium drug composite microsphere injection

A technology of piperacillin sodium sulbactam sodium and cillin sodium sulbactam sodium, which is applied in the field of medicine and can solve problems such as easy adhesion and aggregation, difficulty in mass production, and large particle distribution range

Inactive Publication Date: 2012-01-11
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, microcapsules and microspheres generally have many problems such as large particle distribution range, easy adhesion and aggregation, poor drug stability, large burst release, solvent residue, difficulty in large-scale preparation, and poor process reproducibility. Sustained-release properties and stability of microcapsules and microspheres are no easy feat, and those skilled in the pharmaceutical field are well aware of the various difficulties faced in the preparation of pharmaceutical microsphere formulations, all of which are far from simple theory that can be expected to solve Yes, in fact the same material has different or even opposite effects on drug release in different microspheres

Method used

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  • Piperacillin sodium and sulbactam sodium drug composite microsphere injection
  • Piperacillin sodium and sulbactam sodium drug composite microsphere injection
  • Piperacillin sodium and sulbactam sodium drug composite microsphere injection

Examples

Experimental program
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Effect test

Embodiment 1

[0063] The preparation of embodiment 1 piperacillin sodium sulbactam sodium pharmaceutical composition microsphere injection

[0064] Prescription: (100 bottles)

[0065] Piperacillin Sodium 40g

[0066] Sulbactam Sodium 10g

[0067] Albumin 60g

[0068] Poloxamer 188 30g

[0069] PEG600 50g

[0070] Mannitol 20g

[0071] making process:

[0072] (1) 40g piperacillin sodium, 10g sulbactam sodium, 50g PEG600, 20g mannitol, 30g poloxamer 188 and 60g albumin were dissolved in 1000ml water for injection, filtered to obtain a clear solution;

[0073] (2) Pour the above solution into the spray dryer, adjust the spray conditions: the inlet temperature is 70°C, the outlet temperature is about 35°C, the nozzle size is 0.5mm, the spray flow rate is 6ml / min, the compressed air velocity is 10L / min, spray dry , to obtain white microspheres with uniform shape;

[0074] (3) The obtained microspheres were finally heated and solidified at a temperature of 100° C. for 8 hours, and distr...

Embodiment 2

[0077] The preparation of embodiment 2 piperacillin sodium sulbactam sodium pharmaceutical composition microsphere injection

[0078] Prescription: (100 bottles)

[0079] Piperacillin Sodium 20g

[0080] Sulbactam Sodium 10g

[0081] Albumin 80g

[0082] Poloxamer 188 40g

[0083] PEG600 60g

[0084] Mannitol 40g

[0085] making process:

[0086] (1) Dissolve 20g of piperacillin sodium, 10g of sulbactam sodium, 60g of PEG600, 40g of mannitol, 80g of albumin and 40g of poloxamer 188 in 2000ml of water for injection, and filter to obtain a clear solution;

[0087](2) Pour the above solution into a spray dryer and adjust the spray conditions: the inlet temperature is 80°C, the outlet temperature is about 40°C, the size of the nozzle is 1mm, the spray flow rate is 15ml / min, the compressed air velocity is 20L / min, spray dry, Obtain white microspheres with uniform shape;

[0088] (3) The obtained microspheres were finally heated and solidified at a temperature of 80° C. for ...

Embodiment 3

[0091] The preparation of embodiment 3 piperacillin sodium sulbactam sodium pharmaceutical composition microspheres

[0092] Prescription: (100 bottles)

[0093] Piperacillin Sodium 40g

[0094] Sulbactam Sodium 10g

[0095] Albumin 100g

[0096] Poloxamer 188 50g

[0097] PEG60070g

[0098] Mannitol 50g

[0099] making process:

[0100] (1) Dissolve 40g of piperacillin sodium, 10g of sulbactam sodium, 70g of PEG600, 50g of mannitol, 100g of albumin and 50g of poloxamer 188 in 2000ml of water for injection, and filter to obtain a clear solution;

[0101] (2) Pour the above solution into the spray dryer, adjust the spray conditions: the inlet temperature is 70°C, the outlet temperature is about 45°C, the nozzle size is 0.8mm, the spray flow rate is 12ml / min, the compressed air velocity is 15L / min, spray dry , to obtain white microspheres with uniform shape;

[0102] (3) The obtained microspheres were finally heated and solidified at a temperature of 120° C. for 4 hours,...

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Abstract

The invention discloses a piperacillin sodium and sulbactam sodium drug composite microsphere injection which is characterized by comprising the following components in parts by weight: 2-4 parts of piperacillin sodium, 1 part of sulbactam sodium, 6-10 parts of albumin, 3-5 parts of poloxamer 188, 5-7 parts of polyethylene glycol 600 (PEG600) and 2-5 parts of trehalose. Compared with the prior art, the piperacillin sodium and sulbactam sodium drug composite microsphere injection prepared by the invention has the characteristics of good stability, high entrapment rate, good reproducibility of preparation technology, even particle distribution, small dissolvent residue, good injectability and excellent slow-release property, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a piperacillin sodium sulbactam sodium pharmaceutical composition microsphere injection, which belongs to the technical field of medicine. Background technique [0002] Piperacillin is a penicillin-like broad-spectrum antibiotic, which mainly plays a bactericidal effect by interfering with the synthesis of bacterial cell walls. It is mainly used for infections caused by Pseudomonas aeruginosa and various Gram-negative bacilli but is easily produced by bacteria. Drug resistance due to amidase hydrolysis; sulbactam has no antibacterial activity against other bacteria except Neisseriaceae and Acinetobacter, but sulbactam is important for most of the bacteria produced by β-lactam antibiotic resistant strains β-lactamases are irreversibly inhibited. Sulbactam can prevent drug-resistant bacteria from destroying penicillins and cephalosporins, and sulbactam has obvious synergistic effects with penicillins and cephalosporins. [0003...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K31/43A61K9/16A61P31/04
Inventor 胡建荣
Owner HAINAN MEILAN SMITH KLINE PHARMA
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