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Use of dspe-peg polymers as oral and pulmonary absorption enhancers

A technology of DSPE-PEG-SH and absorption enhancer, which is applied in the application field of DSPE-PEG polymer as an oral and pulmonary absorption enhancer, and can solve the problems that drug absorption cannot be generalized

Active Publication Date: 2021-04-20
XI AN JIAOTONG UNIV
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  • Claims
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Problems solved by technology

The sulfhydryl group in the polymer structure can form a disulfide bond with the cysteine-rich region in the tissue mucus layer glycoprotein, tightly bind to the mucosa with a covalent bond, prolong the residence time of the loaded drug, and increase the local drug concentration, but The function of the thiol group is also affected by the overall structure of the polymer, whether it can promote drug absorption cannot be generalized

Method used

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  • Use of dspe-peg polymers as oral and pulmonary absorption enhancers
  • Use of dspe-peg polymers as oral and pulmonary absorption enhancers
  • Use of dspe-peg polymers as oral and pulmonary absorption enhancers

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Embodiment Construction

[0029] The following combines different end-capped DSPE-PEG polymers (DSPE-PEG-SH and DSPE-PEG-OH, the structure is as follows figure 1 Shown, PEG specifically is PEG2000) promote intestinal absorption, promote the embodiment of pulmonary absorption to illustrate the effect of DSPE-PEG polymer as the absorption enhancer of drug through oral administration and lung absorption.

[0030] 1. DSPE-PEG-SH promotes intestinal absorption in rats

[0031]Male SD rats (body weight 230-250 grams) aged 8-10 weeks were selected to construct an experimental model of intestinal absorption in vivo. Fasting for 16 hours before the experiment, free to drink water, intraperitoneal injection of pentobarbital sodium anesthesia (40mg / kg), the rats were placed supine on a fixed board, cut along the midline of the abdomen, first ligated the common bile duct, from the Intubate the upper end of the intestinal segment, flush the intestinal tract with PBS (pH7.4) solution, insert the other end from the ...

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Abstract

The invention discloses the application of DSPE-PEG polymer as oral and pulmonary absorption enhancer. As an absorption enhancer, DSPE-PEG polymer can significantly improve the oral and pulmonary absorption of water-soluble macromolecular refractory drugs; at the same time, the toxicity test results show that DSPE-PEG polymer has no obvious damage to the mucosa at the oral and pulmonary absorption sites, so DSPE‑PEG polymer is a safe absorption enhancer, which can be used in the oral and pulmonary absorption preparations of macromolecular drugs to improve the refractory absorption of water-soluble macromolecular drugs, especially the oral and pulmonary absorption of protein peptide drugs. Utilization.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to the application of DSPE-PEG polymers as oral and pulmonary absorption accelerators. Background technique [0002] In recent years, with the rapid development of biotechnology and gene technology, a large number of biomacromolecular drugs have been produced, mainly including proteins, polypeptides, nucleic acids, vaccines, antibodies, etc., which are mostly used to treat tumors, hepatitis, neurodegenerative diseases, heart disease, etc. Major diseases such as cerebrovascular disease and immune disease. Compared with chemical drugs, this type of drug has the characteristics of single-target action, strong specificity, less adverse reactions, and strong drug efficacy. It is more and more widely used in the prevention and treatment of diseases. However, these drugs also have limitations while having good activity. Protein and polypeptide drugs are generally unst...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/24A61K9/00
CPCA61K9/0053A61K9/007A61K47/24
Inventor 高阳张海龙孙娅孙建梅
Owner XI AN JIAOTONG UNIV
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