Application of venenum bufonis polypeptide as medicine penetration enhancer

A technology of toad venom polypeptide and penetration enhancer, which is applied in the field of medicine, and can solve problems such as unclear efficacy of polypeptide substances, and achieve the effects of enhancing anti-inflammatory and analgesic effects, promoting penetration, and improving anti-inflammatory and analgesic capabilities

Active Publication Date: 2019-12-13
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

At present, the main experiments are focused on the study of bufadienolactone, and the ...

Method used

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  • Application of venenum bufonis polypeptide as medicine penetration enhancer
  • Application of venenum bufonis polypeptide as medicine penetration enhancer
  • Application of venenum bufonis polypeptide as medicine penetration enhancer

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Experimental program
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Embodiment 1

[0021] 1. Materials and methods

[0022] 1.1 Reagents and instruments

[0023] Acetonitrile (HPLC grade) and methanol (HPLC grade) were purchased from Merck, Germany; formic acid was purchased from Sigma-Aldrich, USA. Standard compounds, bufafalin (118981–201501, ≥99.2%), bufafagenin (110718-201809, ≥99.6%), cinobufagin (110803-201408, ≥99.6%) were purchased from China Food and Drug General Administration of Supervision and Administration (Beijing, China), Sand Bufalin (180427, ≥98%), and Bufatalin (180118, ≥98%), Cinobufafeline (180318, ≥98%), Bufatalin (180419, ≥98%), and Yuanhuabufenjing (180427, ≥98%) were purchased from Beijing Putian Tongchuang Biotechnology Co., Ltd. (China, Beijing). Deionized water was purified by a milliq water system from Millipore.

[0024] Agilent 1290 high-performance liquid chromatography, 1290 variable wavelength detector (VWD), Agilent Corporation of the United States; AB SCIEX triple quadrupole mass spectrometer 5500 liquid mass spectromet...

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Abstract

The invention discloses a new application of venenum bufonis polypeptide as medicine penetration enhancers, including bufadienolide and the like. An in vitro Franz diffusion cell and an in vivo transdermal experiment test the penetration enhancement effect of the venenum bufonis polypeptide on the bufadienolide. An LC-MS/MS (Liquid Chromatogram-Mass Spectrometry/Mass Spectrometry) method carries out detection to discover that the penetration of six types of main bufadienolide in cavia procellus skins is increased by 36.99-91.13% after the venenum bufonis polypeptide is added. A von Frey filament stimulation method verifies that the venenum bufonis polypeptide can improve the anti-inflammatory and analgesic capability of the bufadienolide. After the venenum bufonis polypeptide is applied, 2% formalin is injected on the right rear foot of the cavia procellus, a test result indicates that the mechanical withdrawal threshold of the right rear foot of the cavia procellus added with the bufadienolide of the venenum bufonis polypeptide is obviously improved, and the mechanical withdrawal threshold is improved by 2-3 times after the formalin is injected for 30min. The venenum bufonis polypeptide can accelerate the penetration of sterene in the skin of the cavia procellus so as to enhance the anti-inflammatory and analgesic effect of the venenum bufonis polypeptide.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to the application of Bufonnin polypeptide isolated from Bufonime as a drug penetration enhancer. Background technique [0002] In recent years, many studies have been carried out on the percutaneous penetration of drugs. Compared with other drug delivery routes, the transdermal drug delivery system has the advantages of avoiding first-pass metabolism in the liver, reducing potential adverse side effects, and improving bioavailability. [0003] However, drug penetration needs to pass through the skin barrier, and the stratum corneum, the outermost layer of the skin, is the main obstacle hindering drug transdermal absorption. Only a few compounds with low molecular weight and moderate lipophilicity can partially pass through the stratum corneum, but their penetration efficiency still needs to be improved. In order to facilitate the transdermal penetration of drugs, various method...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K31/585A61P29/00
CPCA61K47/42A61K31/585A61K9/0014A61P29/00Y02A50/30
Inventor 马宏跃
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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