Chitosan quaternary ammonium salt macroporous microspheres for pulmonary inhalation and preparation method thereof

A technology of chitosan quaternary ammonium salt and macroporous microspheres, which can be used in the preparation of microspheres, microcapsule preparations, medical preparations of non-active ingredients, etc., and can solve the problem of limiting the wider application of drug carriers and loss of positive charge. problems, achieve good biocompatibility and degradability, easy operation and stable process

Active Publication Date: 2012-04-18
WEIFANG MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, chitosan is acid-soluble, and chitosan will lose its positive charge under neu

Method used

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  • Chitosan quaternary ammonium salt macroporous microspheres for pulmonary inhalation and preparation method thereof
  • Chitosan quaternary ammonium salt macroporous microspheres for pulmonary inhalation and preparation method thereof
  • Chitosan quaternary ammonium salt macroporous microspheres for pulmonary inhalation and preparation method thereof

Examples

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Example Embodiment

[0039] Example 1

[0040] A chitosan quaternary ammonium salt macroporous microsphere for lung inhalation, prepared from the following ingredients:

[0041] Chitosan quaternary ammonium salt 1g;

[0042] β-cyclodextrin derivative 0.5 g;

[0043] Pore ​​forming agent 0.5g;

[0044] The chitosan quaternary ammonium salt is a high molecular weight chitosan quaternary ammonium salt with a molecular weight of 1360 kDa, and the degree of substitution is 90%.

[0045] The β-cyclodextrin derivative is 2-hydroxypropyl-β-cyclodextrin (Hp-β-CD);

[0046] The porogen is propylene glycol block polyether (F68).

[0047] The method for preparing the above-mentioned chitosan quaternary ammonium salt macroporous microspheres includes the following steps:

[0048] (1) Prepare a mixed solution of each component according to the above-mentioned ratio requirements, weigh the vacuum-dried Hp-β-CD, dissolve it in 200 mL of HTCC (molecular weight 1.3 million) distilled water, and dissolve F68 in the above-prepare...

Example Embodiment

[0053] Example 2

[0054] A chitosan quaternary ammonium salt macroporous microsphere for lung inhalation, prepared from the following ingredients:

[0055] Chitosan quaternary ammonium salt 10 g;

[0056] β-cyclodextrin 5g;

[0057] Pore-forming agent 5g;

[0058] The chitosan quaternary ammonium salt is a high molecular weight chitosan quaternary ammonium salt with a molecular weight of 1100 kDa, and the degree of substitution is 90%.

[0059] The porogen is ammonium bicarbonate.

[0060] The method for preparing the above-mentioned chitosan quaternary ammonium salt macroporous microspheres includes the following steps:

[0061] (1) Prepare a mixed solution of each component according to the above-mentioned ratio requirements, weigh the vacuum-dried β-cyclodextrin, dissolve it in 200 mL of HTCC (molecular weight 1.3 million) distilled water, and dissolve ammonium bicarbonate in the above-mentioned preparation. In the mixed solution;

[0062] (2) Filter through a 0.45 μm microporous memb...

Example Embodiment

[0066] Example 3

[0067] A chitosan quaternary ammonium salt macroporous microsphere for lung inhalation, prepared from the following ingredients:

[0068] Chitosan quaternary ammonium salt 5 g;

[0069] β-cyclodextrin derivative 2.5 g;

[0070] Pore-forming agent 2.5 g;

[0071] The chitosan quaternary ammonium salt is a mid-molecular-weight chitosan quaternary ammonium salt with a molecular weight of 450 kDa, and the degree of substitution is 85%.

[0072] The β-cyclodextrin derivative is 2-hydroxypropyl-β-cyclodextrin;

[0073] The porogen is polyethylene glycol (PEG).

[0074] The method for preparing the above-mentioned chitosan quaternary ammonium salt macroporous microspheres includes the following steps:

[0075] (1) Prepare the mixed solution of each component according to the above-mentioned ratio requirements, weigh the vacuum-dried Hp-β-CD, dissolve it in 200 mL of HTCC (molecular weight 1.3 million) distilled water, and dissolve polyethylene glycol in the above-mentioned prep...

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Abstract

The invention discloses chitosan quaternary ammonium salt macroporous microspheres for pulmonary inhalation and a preparation method thereof. The chitosan quaternary ammonium salt macroporous microspheres comprise the following components in part by weight: 1 to 10 parts of chitosan quaternary ammonium salt, 0.5 to 5 parts of beta-cyclodextrin or derivatives thereof and 0.5 to 5 parts of pore forming agent. The particle size of the chitosan quaternary ammonium salt macroporous microspheres is 0.5 to 10 mu m. The preparation method mainly comprises filtering and spray-drying. The invention hasthe advantages that: the use of chitosan quaternary ammonium salt overcomes the drawback that chitosan may lose the electropositivity of the chitosan under a neutral or physical condition; the microspheres for pulmonary inhalation have an obvious sustained-release function and also have high biocompatibility and degradability, so the range of the application of the microspheres as medicine carriers can be enlarged; and the preparation method has the advantages of simple operation, stable process and easy industrial production.

Description

technical field [0001] The invention relates to a macroporous microsphere for lung inhalation, in particular to a chitosan quaternary ammonium salt macroporous microsphere for lung inhalation and a preparation method thereof, which belongs to the field of pulmonary sustained and controlled release drug delivery . Background technique [0002] Pulmonary sustained and controlled release drug delivery is a new drug delivery system developed in recent years. Microspheres deposited in the lungs can delay the release of drugs, increase drug efficacy and protect drugs from enzymatic hydrolysis; wrap drugs inside the preparation, It increases the stability of the drug; it can effectively reduce the irritation and toxicity of the drug to the respiratory tract and lungs, and has become a hot spot in the study of the drug carrier for controlled release of the lung. However, pulmonary inhalation administration requires good powder characteristics, effective lung deposition rate, good s...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/40A61K47/36B01J13/02A61P11/00
Inventor 张维芬刘冬梅郑增娟李志坚崔娟娟
Owner WEIFANG MEDICAL UNIVERSITY
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