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Pharmaceutical compositions for treating bacterial infections

A composition and drug technology, applied in the directions of antibacterial drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of affecting the pulverization efficiency, difficult to remove the bonded drugs, and the pulverization work has to be terminated, etc.

Active Publication Date: 2015-10-28
SHANGHAI MICURX LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] When the solid powder of insoluble oxazolidinone compounds such as MRX-I is directly micronized and pulverized by jet pulverization, it is found that the drug is very easy to stick in the pulverization chamber, which is very hard and will block the pulverization chamber and high pressure in a short time. The air flow channel seriously affects the crushing efficiency, and even the crushing work has to be terminated
It is a complicated and time-consuming process to disassemble the jet mill for cleaning. The bonded drugs are difficult to remove and need to be cleaned with water or organic solvents and then dried
Continue to micronize and pulverize after thorough cleaning, there is also the problem of sticking and clogging
Therefore, there is no satisfactory method for micronizing the solid powders of insoluble oxazolidinones such as MRX-I

Method used

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  • Pharmaceutical compositions for treating bacterial infections
  • Pharmaceutical compositions for treating bacterial infections
  • Pharmaceutical compositions for treating bacterial infections

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0167] Embodiment 1: co-micronizing and pulverizing with sodium lauryl sulfate and MRX-I (small batch)

[0168] Mix 38.9g MRX-I bulk drug (D(50)=78 micron, D(90)=307 micron) with 1.9g sodium lauryl sulfate (the ratio of drug to excipient is about 100:5) and pass through 30 mesh Sieve 3 times, carry out micronization with airflow mill (JGM-H100 type airflow mill of Huali Company), pulverization pressure is about 8bar, feed rate is about 15g / min, micronization treatment once. After micronization and pulverization, 40.0 g of the micronized drug was obtained with a yield of 98.0%.

[0169] The particle size distribution of the micronized material was measured with a Malvern particle size analyzer, and the results showed that D(50) was 2.3 μm and D(90) was 5.0 μm.

[0170] Co-micronizing the drug and sodium lauryl sulfate, the drug yield is high, the micronization effect is good, and no clogging phenomenon is seen.

Embodiment 2

[0171] Embodiment 2: use sodium lauryl sulfate and MRX-I co-micronized pulverization (bigger batch)

[0172] Mix 422.4g MRX-I bulk drug (D(50)=20 microns, D(90)=185 microns) with 21.1g sodium lauryl sulfate (the ratio of drug to auxiliary material is about 100:5), and pass 16 Mesh sieve 3 times, then carry out micronization with airflow mill (JGM-H200 type airflow mill of Huali Company), pulverization pressure 8 ± 0.5bar, feed rate about 75 ± 25g / min, micronization treatment 2 times. After the crushing was completed, a total of 436.5 g of micronized materials were recovered, with very little loss and a recovery rate of 98.4%.

[0173] The particle size distribution of the micronized material was measured with a Malvern particle size analyzer, and D(50) was 2.9 μm, and D(90) was 6.2 μm.

[0174]After continuous micronization of two larger batches of mixed materials, no sticking or clogging was observed in the jet mill cavity. There is little loss of medicine. The particle si...

Embodiment 3

[0175] Example 3: Co-micronizing and pulverizing with silica and MRX-I

[0176] Mix 40.1g compound MRX-I (D(50)=78 micron, D(90)=307 micron) with 0.3g silicon dioxide (the ratio of drug to excipient is about 100:0.75), and pass through a 30-mesh sieve 3 For the second time, micronize with a jet mill (JGM-H100 type jet mill of Huali Company), the pulverizing pressure is about 8bar, the feed rate is about 15g / min, and the micronization process is performed once. After micronization and pulverization, 38.5 g of micronized drug was obtained, with a yield of 95.3%.

[0177] The particle size distribution of the micronized material was measured with a Malvern particle size analyzer, and the results showed that D(50) was 3.8 μm and D(90) was 8.3 μm. After micronization, there is no sticking phenomenon in the jet mill cavity.

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Abstract

The invention provides a pharmaceutical composition used for treating bacteria infection, concretely provides medicament particles of micronized compound as a formula II and its preparation method. The invention also provides a pharmaceutical composition containing the medicament particles. The micronization method is capable of greatly minimizing phenomena of bonding and obstruction during crushing, and substantially raising the solubility, yield and crushing efficiency of micronized medicaments. The prepared pharmaceutical composition can increase the dissolution in vitro and absorption in vivo of the medicament, and can be used as single medicament or combined with other treatment agent for treating bacteria infection.

Description

technical field [0001] The present invention relates to the field of medicine, and more particularly to a pharmaceutical composition for treating bacterial infection. The invention also relates to a method for preparing micronized oxazolidinone drugs and a micronized pharmaceutical composition. The micronization method of the present invention can greatly reduce the phenomenon of cohesion and blockage in pulverization, and improve the solubility, yield and pulverization efficiency of the micronized medicine. The prepared composition can improve drug dissolution in vitro and absorption in vivo. Background technique [0002] Due to the gradual increase of antimicrobial resistance, the treatment of bacterial infections urgently needs new antibacterial drugs with novel modes of action. Among the newer antibacterial drugs, oxazolidinones are a new class of synthetic compounds with anti-infection of various pathogenic bacteria including drug-resistant bacterial infection. [00...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4439A61P31/04B01J13/02
Inventor 刘春傅崇东
Owner SHANGHAI MICURX LTD
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