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Application of HP-beta-CD-GMA-PEI as oral and transpulmonary absorption accelerant

A technology of -CD-GMA-PEI, -CD-GMA-PEI10000, which is applied in the field of oral and pulmonary absorption enhancers, can solve the problems of limited application and increased mucosal damage

Inactive Publication Date: 2013-11-27
XI AN JIAOTONG UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

Numerous research results have shown that the above-mentioned absorption enhancers can significantly improve the absorption of poorly absorbed drugs at each administration site, but with the enhancement of their absorption-promoting effect, these absorption enhancers will gradually increase the damage to the mucosa of the absorption site, thus Limits the application of these absorption enhancers in pharmaceutical formulations

Method used

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  • Application of HP-beta-CD-GMA-PEI as oral and transpulmonary absorption accelerant
  • Application of HP-beta-CD-GMA-PEI as oral and transpulmonary absorption accelerant
  • Application of HP-beta-CD-GMA-PEI as oral and transpulmonary absorption accelerant

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Embodiment Construction

[0030] The present invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the present invention rather than limitations.

[0031] Accelerated absorption agent HP-β-CD-GMA-PEI of the present invention (its structural formula is as figure 1 As shown), polyethyleneimine is connected to hydroxypropyl β-cyclodextrin through glycidyl methacrylate, in which hydroxypropyl β-cyclodextrin is the basic skeleton, and glycidyl methacrylate is the branched chain , polyethyleneimine is the adhesive functional group.

[0032] Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a derivative formed by condensation of β-cyclodextrin and 1,2-propylene oxide. Compared with β-cyclodextrin, its water solubility is significantly improved; it is stable to heat and light, and when HP-β-CD is used in peptide drugs, it can inhibit proteases on peptide drugs The decomposition of peptide drugs improves the stability of peptide drugs; HP-β-CD is basic...

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Abstract

The invention discloses an application of HP-beta-CD-GMA-PEI as an oral and transpulmonary absorption accelerant. The HP-beta-CD-GMA-PEI can obviously promote the oral and transpulmonary absorption of water-soluble macro-molecular difficult-to-absorb drugs as an absorption accelerant; and toxicity investigation results show that the HP-beta-CD-GMA-PEI has no obvious damages to the oral and pulmonary absorption positions, so the HP-beta-CD-GMA-PEI is a safe absorption accelerant, can be applied in the oral and transpulmonary absorption preparations of the macro-molecular drugs, is used for improving the water-soluble macro-molecular difficult-to-absorb drugs, and is especially used for improving the oral and transpulmonary absorption bioavailability of protein peptide drugs.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, and relates to the application of HP-β-CD-GMA-PEI as an oral and pulmonary absorption accelerator. Background technique [0002] In recent years, with the development of biotechnology, the application of combinatorial chemistry and the improvement of high-throughput drug screening technology, more and more drugs with physiological activity have been gradually developed. Among them, water-soluble macromolecular drugs such as proteins and polypeptides Drugs are one of them. However, these drugs also have limitations while having good activity. Protein and polypeptide drugs are generally unstable in the body and are easily hydrolyzed and degraded by acid and protease in the body; low fat solubility, high molecular weight, and weak ability to penetrate the biomembrane barrier, etc., ultimately make it difficult for these drugs to be absorbed after administration. Therefore, the ...

Claims

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Application Information

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IPC IPC(8): A61K47/40
Inventor 高阳王珂张海龙邢建峰
Owner XI AN JIAOTONG UNIV
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