Cyclosporin A pulmonary inhaled macroporous microspheres and preparation method thereof

A technology of macroporous microspheres and cyclosporine, which is applied in the fields of cyclic peptide components, respiratory system diseases, inactive components of polymer compounds, etc. problems such as large differences, to achieve the effect of good biocompatibility, good biocompatibility and smooth surface

Active Publication Date: 2013-05-15
WEIFANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]However, cyclosporin A oral preparations have low bioavailability and large individual differences. Severe side effects such as toxicity and gastrointestinal reactions limit the application
Atomized inhalation of CsA can solve the shortcomings of less drug distribution in the blood of the systemic drug and great side effects on the liver and kidney. However, the airway mucosa is irritating and the absorption is not complete due to its fat solubility. The development of long-acting lung inhalation dosage forms has become a challenge to overcome this problem. the crux of the matter

Method used

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  • Cyclosporin A pulmonary inhaled macroporous microspheres and preparation method thereof
  • Cyclosporin A pulmonary inhaled macroporous microspheres and preparation method thereof
  • Cyclosporin A pulmonary inhaled macroporous microspheres and preparation method thereof

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Embodiment 1

[0039] A cyclosporin A macroporous microsphere for pulmonary inhalation, prepared from the following components:

[0040] Cyclosporin A 1g;

[0041] Chitosan derivative 1g;

[0042] β-cyclodextrin 0.5g;

[0043] Porogen 0.5g;

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

[0045] The porogen is ammonium bicarbonate.

[0046] The preparation method of the cyclosporin A lung inhalation macroporous microspheres comprises the following steps:

[0047] (1) Prepare a mixed solution of each component according to the above ratio requirements, weigh vacuum-dried β-cyclodextrin, dissolve it in 200 mL of HTCC (molecular weight: 1.3 million) distilled water, and dissolve ammonium bicarbonate in the sample solution ;

[0048] (2) After filtering through a 0.45 μm microporous membrane, adjust the mass concentration of the mixed filtrate to 0.5-1.5%;

...

Embodiment 2

[0053] A cyclosporin A macroporous microsphere for pulmonary inhalation, prepared from the following components:

[0054] Cyclosporine A 2g;

[0055] Chitosan derivative 5 g;

[0056] β-cyclodextrin 2.5 g;

[0057] Porogen 2.5 g;

[0058] Described chitosan derivative is chitosan quaternary ammonium salt;

[0059] The chitosan quaternary ammonium salt is a high molecular weight chitosan quaternary ammonium salt with a molecular weight of 1100kDa, and the substitution degree is 90%.

[0060] The porogen is propylene glycol block polyether (F68).

[0061] The preparation method of the cyclosporin A lung inhalation macroporous microspheres comprises the following steps:

[0062] (1) Prepare a mixed solution of each component according to the above ratio requirements, weigh vacuum-dried β-cyclodextrin, dissolve it in 200 mL of HTCC (molecular weight: 1.3 million) distilled water, and dissolve F68 in the above-prepared mixed solution. in solution;

[0063] (2) After filtering ...

Embodiment 3

[0068] A cyclosporin A macroporous microsphere for pulmonary inhalation, prepared from the following components:

[0069] Cyclosporin A 3g;

[0070] Chitosan derivative 10g;

[0071] β-cyclodextrin derivative 5g;

[0072] Porogen 5g;

[0073] Described chitosan derivative is chitosan quaternary ammonium salt;

[0074] The chitosan quaternary ammonium salt is a chitosan quaternary ammonium salt with a molecular weight of 450kDa and a substitution degree of 85%.

[0075] The β-cyclodextrin derivative is 2-hydroxypropyl-β-cyclodextrin (Hp-β-CD);

[0076] The porogen is polyethylene glycol.

[0077] The preparation method of the cyclosporin A lung inhalation macroporous microspheres comprises the following steps:

[0078] (1) Prepare the mixed solution of each component according to the above 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 the polyethylene glycol in the above prep...

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Abstract

The invention discloses cyclosporin A pulmonary inhaled macroporous microspheres and a preparation method thereof. The cyclosporin A pulmonary inhaled macroporous microspheres consist of the following components in part by weight: 1 to 3 parts of cyclosporin A, 1 to 10 parts of chitosan derivative, 0.5 to 5 parts of beta-cyclodextrin or a derivative thereof and 0.5 to 5 parts of porogen, and havethe particle size of 1 to 10mu m. The preparation method mainly comprises the steps of filtering and spray-drying. The invention has the advantages that: the pulmonary inhaled microspheres have a macroporous structure, can be used for pulmonary administration, have the particle size of 1 to 10mu m, the medicine loading capacity of 5.28 to 7.28 percent, the encapsulating rate of 0.85 to 1.19 percent, and high biocompatibility, can reduce irritation of a respiratory mucosa, and is particularly suitable for a dry powder inhalant to fulfill the aim of pulmonary administration, the medicine is sustained-release, the using amount and side effects of the medicine can be reduced, the preparation method is easy and convenient to operate, the process is stable, and industrial production is easy to implement.

Description

technical field [0001] The invention relates to a drug preparation for sustained and controlled release in the lungs, in particular to cyclosporine A macroporous microspheres for pulmonary inhalation and a preparation method thereof, belonging to the field of drug delivery for the sustained and controlled release of the lungs. 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 must have good powder characteristics, effective lung depositio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K38/13A61K47/40A61P11/00
Inventor 张维芬郑增娟李志坚崔娟娟
Owner WEIFANG MEDICAL UNIV
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