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 easy adhesion and aggregation, difficulty in mass production, and large particle distribution range

Inactive Publication Date: 2010-11-24
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 Piperacillin Sodium-Tazobactam Sodium Pharmaceutical Composition Microsphere Injection

[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] making process:

[0082] (1) 40g of piperacillin sodium, 10g of tazobactam sodium, 60g of PEG600 and 20g of mannitol were dissolved in 800ml of water for injection to obtain an aqueous phase;

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

[0084] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, stir for 10 minutes after dropping, 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 c...

Embodiment 2

[0101] Example 2 Preparation of Piperacillin Sodium-Tazobactam Sodium Pharmaceutical Composition Microsphere Injection

[0102] Prescription: (100 bottles)

[0103] Piperacillin Sodium 80g

[0104] Tazobactam Sodium 10g

[0105] PLA-PEG 55g

[0106] PEG60070g

[0107] Polysorbate 80 15g

[0108] Mannitol 20g

[0109] making process:

[0110] (1) Dissolve 80g of piperacillin sodium, 10g of tazobactam sodium, 70g of PEG600 and 20g of mannitol in 1000ml of water for injection to obtain an aqueous phase;

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

[0112] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, stir for 10 minutes after dropping, 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 (inl...

Embodiment 3

[0129] Example 3 Preparation of Piperacillin Sodium-Tazobactam Sodium Pharmaceutical Composition Microsphere Injection

[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] making process:

[0138] (1) Dissolve 80g of piperacillin sodium, 10g of tazobactam sodium, 65g of PEG600 and 30g of mannitol in 1200ml of water for injection to obtain an aqueous phase;

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

[0140] (3) Slowly drop the water phase obtained above into the oil phase under stirring conditions, stir for 10 minutes after dropping, 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 (in...

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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 microsphere injection of a pharmaceutical composition of piperacillin sodium and tazobactam sodium, which belongs to the technical field of medicine. Background technique [0002] Piperacillin is a spectrum semi-synthetic penicillin antibiotic, which has been widely used in clinic. Due to the long-term use and improper use of piperacillin, the therapeutic effect of piperacillin is declining, which affects the application of piperacillin to a large extent. Tazobactam sodium is a lactamase inhibitor and belongs to the third-generation antibacterial potent synergist. Combining it with 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 produces a significant synergistic effect, and is widely used in the treatment of severe systemic and local infections, abdominal infection, lower respiratory tract infection, soft...

Claims

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Application Information

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