Method for preparing aztreonam powder aerosol

A technology of powder aerosol and aztreonam, which is applied in the field of preparation of aztreonam powder aerosol, can solve the problems of uneasy control of dosage, limited use, inconvenience of carrying, etc., and achieve the effect of high efficiency of transpulmonary delivery and good dispersibility

Inactive Publication Date: 2015-07-22
SUZHOU HUIREN BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the pulmonary inhalation efficiency of the lung inhalation spray is low, the dose is not easy to control and it is inconvenient to carry, which is very limited in use.

Method used

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  • Method for preparing aztreonam powder aerosol
  • Method for preparing aztreonam powder aerosol
  • Method for preparing aztreonam powder aerosol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Put AZT, or AZT and amino acid, into deionized water, fully stir until all the solutes are dissolved to obtain the basic solution, and then spray-dry the basic solution to prepare the corresponding dry powder particles, and determine the in vitro lung deposition efficiency.

[0018] The amino acid is selected from leucine (LEU), isoleucine (ILE), histidine (HIS), arginine (ARG), phenylalanine (PHE), tryptophan (TRP), tyrosine One or more of tyrosine (TYR), proline (PRO), and methionine (MET).

[0019] The pulmonary delivery efficiency of the above dry powder particles is shown in Table 1.

[0020] Table 1 Transpulmonary delivery efficiency of AZT and its dry powder particles with amino acids

[0021]

[0022]

[0023] In the preparation technology: A is spray drying; B is nano spray drying; C is freeze spray drying; D is freeze nano spray drying.

Embodiment 2

[0025] Put AZT, or AZT and absorption enhancer, into deionized water (add a certain amount of organic solvents such as ethanol and acetone to promote dissolution if necessary), stir well until all the solutes are dissolved to obtain a basic solution, and then spray the basic solution After drying, the corresponding dry powder particles were prepared, and the lung deposition efficiency in vitro was determined.

[0026] The absorption enhancer is selected from α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), dimethyl-β-cyclodextrin (DMC), hydroxypropyl-β-cyclodextrin High molecular weight chitosan (HPC), γ-cyclodextrin (γ-CD), low molecular weight chitosan (CLMW), medium molecular weight chitosan (CMMW), high molecular weight chitosan (CHMW), trimethyl chitosan ( TMC), sodium taurocholate (STC), sodium glycocholate (SGC), sodium oleate (SOA), carboxymethyl cellulose (CMC), sodium salicylate (PAS), glycyrrhetinic acid (GCA) , Sodium caprate (SCA), Distearoylphosphatidylcholine (DSPC),...

Embodiment 3

[0033] Put AZT, or AZT, amino acid, and absorption enhancer into deionized water (if necessary, add a certain amount of organic solvents such as ethanol, acetone, etc. to promote dissolution), stir well until all the solutes are dissolved to obtain the basic solution, and then add the basic solution After spray drying, the corresponding dry powder particles were prepared, and the lung deposition efficiency in vitro was determined.

[0034] The pulmonary delivery efficiency of the above dry powder particles is shown in Table 3.

[0035] Table 3 Transpulmonary delivery efficiency of AZT and its dry powder particles with amino acids and absorption enhancers

[0036]

[0037]

[0038] In the preparation technology: A is spray drying; B is nano spray drying; C is freeze spray drying; D is freeze nano spray drying.

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Abstract

The invention discloses a method for preparing an aztreonam (AZT) powder aerosol. The method comprises the following steps: accurately weighing a certain quantity of AZT or AZT and auxiliary materials; dissolving the weighed AZT or AZT and auxiliary materials in an appropriate solvent to obtain a basic solution; spray-drying the basic solution to manufacture corresponding dry powder particles, wherein the auxiliary material is amino acid and/or an absorption enhancing agent. According to the method, the particle diameters of the prepared AZT dry powder particles are within the inhalable range, so that favorable dispersity and efficient lung delivery efficiency are achieved.

Description

Technical field [0001] The invention relates to a preparation method of aztreonam powder spray. Background technique [0002] Inflammation of the respiratory tract caused by infection with Pseudomonas aeruginosa is a common disease in patients with cystic fibrosis, and antibiotic therapy is often used clinically. Lung inhalation of antibiotics is the most direct way to treat pulmonary infections. The drugs can avoid the first pass effect of the liver and the gas-liquid barrier to reach the diseased part. It has the characteristics of fast onset, low dosage, and small side effects. Antibiotics used to treat respiratory inflammation include tobramycin, polymyxin, aztreonam, ciprofloxacin, and amphotericin B. Among them, aztreonam (AZT) is a monocyclic β-lactam antibiotic widely used in clinical practice, and has its unique effect on the treatment of respiratory infections caused by Pseudomonas aeruginosa infection. In European countries AZT is also used to treat diseases caused b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/427A61K47/18A61K47/36A61K47/26A61K47/20A61P11/00A61P31/04
Inventor 李浩莹
Owner SUZHOU HUIREN BIOLOGICAL SCI & TECH
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