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Application of spermine NONOate as an absorption enhancer for macromolecular poorly absorbed drugs administered through the lungs

A technology of absorption enhancer and water-soluble macromolecules, which is used in pharmaceutical combinations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc.

Active Publication Date: 2021-02-05
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The mechanism of different nitric oxide donors in promoting drug absorption is affected by internal and external factors such as their own structural characteristics and the environment of the route of administration, and there is no unified and clear explanation

Method used

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  • Application of spermine NONOate as an absorption enhancer for macromolecular poorly absorbed drugs administered through the lungs
  • Application of spermine NONOate as an absorption enhancer for macromolecular poorly absorbed drugs administered through the lungs
  • Application of spermine NONOate as an absorption enhancer for macromolecular poorly absorbed drugs administered through the lungs

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Experimental program
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Embodiment Construction

[0022] The present invention will be described in further detail below in conjunction with the accompanying drawings and embodiments.

[0023] The present invention proposes Spermine NONOate as a lung absorption accelerator for improving the bioavailability of water-soluble macromolecular refractory drugs. The experimental process and results are as follows:

[0024] 1. Spermine NONOate promotes lung absorption experiment in rats

[0025] Healthy male SD rats (body weight 220-250g) were used to construct an in vivo lung absorption model. Fasting for 12 hours before the experiment, free to drink water. After intraperitoneal injection of pentobarbital sodium (32mg / kg) to anesthetize the rat, fix it supine on the mouse board, then strip off its trachea and perform tracheal intubation, use silk thread to fix the trachea, and finally use a micro-syringe to draw accurately 100 μL of liquid medicine (water as the solvent) was injected into the lungs through the cannula. The jugula...

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Abstract

The present invention discloses application of Spermine NONOate used as an absorption enhancer of macromolecular indigestible drugs administered by the lung. Spermine NONOate can be used as an absorption enhancer to improve pulmonary absorption of macromolecular indigestible drugs. Meanwhile, the results of toxicity investigation show that Spermine NONOate has no obvious damage to the mucosa of the pulmonary absorption site. It can be known that Spermine NONOate is a safe and reliable absorption enhancer, can improve the absorption of macromolecular indigestible drugs, especially the bioavailability of protein peptide drugs of pulmonary absorption, and can be applied in the preparation of a pulmonary absorption preparation for the macromolecular indigestible drugs.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to Spermine NONOate for improving the bioavailability of macromolecular difficult-to-absorb drugs through pulmonary administration. Background technique [0002] As a non-invasive drug delivery method that has attracted more and more attention, transpulmonary drug delivery has its unique advantages: the drug delivery method is easily accepted by patients, and the patient's compliance is good; it avoids the first-pass effect and improves the bioavailability of drugs degree; avoid the influence of gastrointestinal environment, less metabolic reaction in the lungs, can reduce its degradation. [0003] Drugs with poor absorption of macromolecules are generally characterized by strong hydrophilicity, large molecular weight, and weak ability to penetrate the biomembrane barrier, which usually leads to poor permeability of such drugs through epithelial cells. In partic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04A61K38/28A61K38/23A61P3/10A61P19/10
CPCA61K38/23A61K38/28A61K47/02A61P3/10A61P19/10
Inventor 高阳张海龙
Owner XI AN JIAOTONG UNIV
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