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Piperacillin sodium-tazobactam sodium medicinal composition microsphere injection

A technology of tazobactam sodium and piperacillin sodium, which is applied in the field of medicine and can solve problems such as large burst release, difficulty in large-scale preparation, and poor process reproducibility

Inactive Publication Date: 2011-10-26
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-tazobactam sodium medicinal composition microsphere injection
  • Piperacillin sodium-tazobactam sodium medicinal composition microsphere injection
  • Piperacillin sodium-tazobactam sodium medicinal composition microsphere injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 Preparation of microsphere injection of pharmaceutical composition of piperacillin sodium and tazobactam sodium

[0074] Prescription: (100 bottles)

[0075] Piperacillin Sodium 40g

[0076] Tazobactam Sodium 10g

[0077] PLA-PEG 40g

[0078] PEG600 60g

[0079] Polysorbate 80 10g

[0080] Mannitol 20g

[0081] Preparation Process:

[0082] (1) Dissolve 40g piperacillin sodium, 10g tazobactam sodium, 60gPEG600 and 20g mannitol in 800ml water for injection to obtain an aqueous phase;

[0083] (2) Dissolve 40g PLA-PEG and 10g polysorbate 80 in 200ml dichloromethane to obtain an oil phase;

[0084] (3) Slowly drip the water phase obtained above into the oil phase under stirring conditions, stir for 10 minutes after dripping, and then transfer to a high-speed homogenizer and stir at high speed for 3 times, each time for 10 minutes, to obtain a uniform white emulsion ;

[0085] (4) Put the white emulsion into the spray dryer, adjust the spray conditions (inlet temperature 65°C, ou...

Embodiment 2

[0101] Example 2 Preparation of microsphere injection of pharmaceutical composition of piperacillin sodium and tazobactam sodium

[0102] Prescription: (100 bottles)

[0103] Piperacillin Sodium 80g

[0104] Tazobactam Sodium 10g

[0105] PLA-PEG 55g

[0106] PEG600 70g

[0107] Polysorbate 80 15g

[0108] Mannitol 20g

[0109] Preparation Process:

[0110] (1) Dissolve 80g piperacillin sodium, 10g tazobactam sodium, 70gPEG600 and 20g mannitol in 1000ml water for injection to obtain an aqueous phase;

[0111] (2) Dissolve 55g PLA-PEG and 15g Polysorbate 80 in 300ml of toluene to obtain an oil phase;

[0112] (3) Slowly drip the water phase obtained above into the oil phase under stirring conditions, stir for 10 minutes after dripping, and then transfer to a high-speed homogenizer and stir at high speed for 3 times, each time for 10 minutes, to obtain a uniform white emulsion ;

[0113] (4) Put the white emulsion into the spray dryer, adjust the spray conditions (inlet temperature 70°C, outlet...

Embodiment 3

[0129] Example 3 Preparation of microsphere injection of pharmaceutical composition of piperacillin sodium and tazobactam sodium

[0130] Prescription: (100 bottles)

[0131] Piperacillin Sodium 80g

[0132] Tazobactam Sodium 10g

[0133] PLA-PEG 60g

[0134] PEG600 65g

[0135] Polysorbate 80 22g

[0136] Mannitol 30g

[0137] Preparation Process:

[0138] (1) Dissolve 80g piperacillin sodium, 10g tazobactam sodium, 65gPEG600 and 30g mannitol in 1200ml water for injection to obtain an aqueous phase;

[0139] (2) Dissolve 60g PLA-PEG and 22g polysorbate 80 in 400ml acetone to obtain an oil phase;

[0140] (3) Slowly drip the water phase obtained above into the oil phase under stirring conditions, stir for 10 minutes after dripping, and then transfer to a high-speed homogenizer and stir at high speed for 5 times, each time for 10 minutes, to obtain a uniform white emulsion ;

[0141] (4) Put the white emulsion into the spray dryer, adjust the spray conditions (inlet temperature 75°C, outlet te...

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Abstract

The invention discloses piperacillin sodium-tazobactam sodium medicinal composition microsphere injection. The injection is characterized by consisting of piperacillin sodium, tazobactam sodium, polylactic acid-polyethylene glycol (PLA-PEG), PEG600, polysorbate 80 and mannitol and particularly consisting of 4 to 8 parts of piperacillin sodium, 1 part of tazobactam sodium, 4 to 9 parts of PLA-PEG,6 to 10 parts of PEG600, 1 to 3 parts of polysorbate 80 and 2 to 4 parts of mannitol. Compared with the prior art, the piperacillin sodium-tazobactam sodium medicinal composition microsphere injection prepared by the invention has the characteristics of good stability, high entrapment rate, high preparation technology repeatability, suitability for industrial production, uniform particle distribution, few solvent residue, good injectability and excellent sustained release property.

Description

Technical field [0001] The invention relates to a chemical drug piperacillin sodium tazobactam sodium pharmaceutical composition microsphere injection, which belongs to the technical field of medicine. Background technique [0002] Piperacillin is a spectral semi-synthetic penicillin antibiotic, which has been widely used in clinical practice. Due to the long-term use and improper use of piperacillin, the therapeutic effect of piperacillin is declining, which largely affects the application of piperacillin. Tazobactam sodium is a lactamase inhibitor and belongs to the third generation of antibacterial potent synergist. The combination of piperacillin or cefoperazone can enhance the efficacy and prolong the action time of the two. When tazobactam sodium is used in combination with piperacillin sodium, it has a significant synergistic effect. It is widely used in the treatment of severe systemic and local infections, abdominal cavity infections, lower respiratory tract infections,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K31/431A61K9/16A61P31/04
Inventor 郝志艳
Owner HAINAN MEILAN SMITH KLINE PHARMA
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