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Drug-film affinity measuring method based on polydiacetylene sensor

A polydiacetylene and affinity technology, which is applied in the field of drug-membrane affinity determination, can solve the problems of complex analysis process, poor inter-column reproducibility, tedious chromatographic column preparation, etc., and achieves good inter-batch reproducibility, low detection cost, Combining simple effects

Inactive Publication Date: 2012-05-02
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Phospholipid membrane chromatography (IAM) and immobilized liposome chromatography (ILC) are earlier methods used to determine drug-membrane affinity, such methods use phospholipid monolayer (IAM) or liposome (ILC) as chromatographic Stationary phase, the distribution ratio of the drug between the mobile phase and the stationary phase is obtained by measuring the chromatographic retention time, and then reflects the size of the drug-membrane affinity; however, the preparation of the chromatographic column is cumbersome and the reproducibility between columns is poor, so the application is limited. certain limit
There are also foreign researchers using surface plasmon resonance sensing technology (SPR) to measure drug-membrane affinity, but this technology requires advanced equipment and high detection costs, which are unaffordable for most domestic drug research and development institutions.
Some other methods such as stent model support technology (SSLM) and pH titration method are not suitable for rapid screening of drug-membrane affinity due to the complex analysis process

Method used

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  • Drug-film affinity measuring method based on polydiacetylene sensor
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  • Drug-film affinity measuring method based on polydiacetylene sensor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Changes in absorption spectra of polydiacetylene / phospholipid color-changing vesicles before and after they interact with drugs

[0040] Prepare the following three samples, and scan the absorption spectrum at a wavelength of 500 to 700 nm on a SHIMADZU UV2401 ultraviolet-visible spectrophotometer:

[0041] (1) Dissolve phospholipids and diacetylene structural monomers (3:2 in molar ratio) in organic solvents respectively, and after mixing, remove the organic solvents by rotary evaporation under reduced pressure in a warm water bath, then add an appropriate amount of deionized water, and ultrasonically Mix well, take it out after standing at 4°C for 12 hours, it is a diacetylenic acid / phospholipid mixed solution assembled without ultraviolet light irradiation;

[0042] (2) Dissolve phospholipids and diacetylene structural monomers (3:2 in molar ratio) in organic solvents respectively, and after mixing, remove the organic solvents by rotary evaporation under red...

Embodiment 2

[0045] Embodiment 2: the reproducibility of CR value

[0046] Dissolve phospholipids and diacetylene structural monomers (3:2 in molar ratio) in organic solvents respectively, and after mixing, remove the organic solvents by rotary evaporation in a warm water bath under reduced pressure, then add an appropriate amount of deionized water, and mix them evenly with ultrasound. Take it out after standing at 4°C for 12 hours, and irradiate it while stirring under a UV lamp (wavelength: 254nm), to form a blue polydiacetylene / phospholipid color-changing vesicle suspension, and prepare 5 batches continuously according to the above method. The CR value of each batch of samples is determined according to the following method: take 0.2ml of the color-changing vesicle suspension, add 2ml of Tris-HCl (pH7.4) buffer solution, add different concentrations of amlodipine besylate solution respectively, vortex and place in Incubate at 25°C for 15 minutes, calculate the color change response val...

Embodiment 3

[0050] Example 3: K b Value reproducibility

[0051] Prepare polydiacetylene / phospholipid color-changing vesicles according to the method in "Example 2", and measure the K of procaine hydrochloride, metoprolol tartrate and amlodipine besylate three kinds of drugs respectively according to the linear fitting method b value( figure 2 ), the vesicles prepared from the same batch were tested three times, and the K b The intra-batch reproducibility of the value; the vesicles prepared in three consecutive batches were measured three times, and the K b Inter-assay reproducibility of values. As can be seen from the measurement results in Table 2, after the polydiacetylene / phospholipid color-changing vesicles prepared by the preparation method described in the present invention react with different types of drugs, the K obtained by measuring according to the linear fitting method b Values ​​are very reproducible.

[0052] Table 2: K b Value reproducibility

[0053]

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Abstract

The invention discloses a drug-film affinity measuring method based on a polydiacetylene sensor, which comprises the following steps of: inserting phospholipid into a diacetylene vesicle sensor so as to form biofilm like polydiacetylene / phospholipid color change vesicles; and measuring color change levels before and after the color change vesicles interact with drug molecules, and calculating affinity of the drug molecules and the color change vesicles by using a certain model and a mathematical treatment method. The method is simple, convenient, quick, good in repeatability, and the like; the requirements on the analysis conditions are not high, so that the method can be realized by utilizing a general visible spectrophotometer only in a general test lab; and the method can be compatiblewith a high-throughput micropore plate mode, so that the method is suitable for high-throughput screening of the drug-film affinity.

Description

technical field [0001] The invention relates to a method for measuring drug-membrane affinity based on a polydiacetylene photochemical sensor, belonging to the technical field of drug analysis. Background technique [0002] The cell membrane is an important target of drug action, and it is also a physiological barrier for drugs to enter cells. The activity and transport of drugs in the human body are closely related to drug-membrane affinity. A very important research content. [0003] n-octanol / water is the earliest in vitro system used to determine drug-membrane affinity. The system uses organic solvent-n-octanol to simulate the cell membrane, and the partition coefficient (K oct ) to reflect the membrane affinity of the drug. However, the cell membrane is an anisotropic lipid bilayer structure, so the correlation between n-octanol / water partition coefficient and drug-membrane affinity is not ideal, and it cannot accurately simulate certain interactions between drugs and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N21/33G01N21/35G01N21/3563G01N21/78
Inventor 郑枫陈夷花
Owner CHINA PHARM UNIV
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