Determination method of radioactive ligand N2S2-Memantine and brain receptor imaging agent 99mTc-Memantine oil-water distribution coefficient
A technology of oil-water partition coefficient and determination method, applied in the field of nuclear medicine analysis and detection
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Embodiment 1N2
[0029] Example 1N 2 S 2 -Determination of oil-water partition coefficient of Memantine
[0030] (1) Solution preparation
[0031] Accurately weigh N 2 S 2 -Memantine 1.0g, put in a 100mL measuring bottle, add an appropriate amount of methanol to dissolve, add methanol to the mark, shake well, and obtain a stock solution with a concentration of 10mg / mL.
[0032] (2) Linear relationship
[0033] Precisely measure an appropriate amount of stock solution, place it in a 10mL measuring bottle, add mobile phase to dilute to the mark, shake well, and obtain mass concentrations of 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0mg / mL of standard solutions, respectively, accurately draw 20 μL of each series of standard solutions and inject them into the high-performance liquid chromatograph, and record the peak area. to N 2 S 2 -Memantine mass concentration ρ (mg / mL) is the abscissa, and the peak area A is the ordinate to carry out linear regression to get N 2 S 2 -Memantine'...
Embodiment 2
[0043] The selection of embodiment 2 mobile phase
[0044] The effect of different mobile phases on the separation conditions of water phase and oil phase was investigated. Different proportions of methanol-water systems were selected, and the retention time of the main peak was about 6.5 minutes, but the main components of the oil phase were seriously interfered by impurity peaks, and could not be effectively separated; the separation effect was greatly improved by using acetonitrile-water system, When the ratio of acetonitrile and water is selected to be 2:1, the degree of separation is greater than 1.5; adding a certain proportion of trifluoroacetic acid, the peak shape is better and has a suitable retention time. The chromatograms of the oil phase and the water phase are shown in image 3 , Figure 4 .
Embodiment 3
[0045] Embodiment 3 pH is to the influence of partition coefficient
[0046] Change the water used in step (5) method among the embodiment 1 into 0.1mol / L pH value and be respectively the phosphate buffer saline solution of 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 7.4, 8.0 and 9.0, measure with the same method N in different pH buffers 2 S 2 -Memantine partition coefficient, see Table 2. Results The partition coefficient of n-octanol-phosphate buffer system was not significantly affected by the pH value of the buffer.
[0047] Table 2 Determination of partition coefficient
[0048]
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