Lyophilized powder kit for preparing 99mTc-GSA and preparation method and application thereof
A technology of 99mtc-gsa and freeze-dried powder, which is applied in chemical instruments and methods, esterified saccharides, sugar derivatives, etc., can solve the problems of not getting the labeling rate GSA kit, the synthesis method is not stable enough, and is too simple
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Embodiment 1
[0133] one for preparing 99m The lyophilized powder kit of Tc-GSA is prepared by the following method:
[0134] 1) Preparation of 2-imino-2-methoxyethyl-1-thio-β-D-galactopyranoside
[0135] The synthetic route of this step is as follows:
[0136]
[0137] Among them, a stands for Ac 2 O, HClO 4 , 30~40℃ / Br 2 , P;
[0138] b stands for: thiourea, acetone;
[0139] c stands for: Chloroacetonitrile, K 2 CO 3 , NaHSO 3 ;
[0140] d stands for: CH 3 ONa, CH 3 OH;
[0141] 1.1) Preparation of 1-bromo-2,3,4,6-tetra-O-acetyl-α-D-galactose:
[0142] In a 250mL four-necked flask, add 32mL of acetic anhydride and 0.16mL of perchloric acid. Under stirring at room temperature, add 8 g of galactose in batches and keep the temperature at 30~40°C. The galactose gradually dissolves, and the solution becomes darker in color. After it is completely dissolved, heat and control the temperature at 30-40°C for half an hour. Heating was stopped and 2.4 g of red phosphorus was add...
Embodiment 2
[0160] Patient Y, male, 60 years old, was admitted to the hospital on March 20, 2009, for more than 1 year due to the discovery of a liver mass.
[0161] The patient's physical examination in December 2007 found a space occupying about 1 cm in the right liver. Hemangioma was considered locally and was not treated. In June 2008, the re-examination of the tumor increased to 4cm. Considering liver cancer, radiofrequency treatment was performed twice in July and August 2008, and the tumor did not shrink significantly. In November 2008, re-examination CT showed a mass of 5×4cm in segment VIII of the second hepatic hilum, which was closely related to the right hepatic vein and the middle hepatic vein. After three interventional embolizations in our hospital, he was admitted for surgery. Past: HBsAg (+) 26 years, diabetes for half a year. Physical examination: a 3×3cm mass was palpable in the right 6th and 7th intercostal space, with medium quality, poor mobility, no tenderness, and...
Embodiment 3
[0184] Healthy subject T, female, 27 years old, liver function, blood coagulation and other indicators were normal.
[0185] Detect liver GSA uptake index according to the method identical with embodiment 1, obtain UI=0.248min -1 .
[0186] The curve diagram or scatter diagram involved in the whole detection process, such as Figure 7 shown.
[0187] Using the technetium-99m labeled GSA complex prepared by the kit of the present invention as the drug for detection, the liver GSA uptake index was detected for 64 patients with the same detection method as in Example 2, and the results were all effective. Used to evaluate liver function.
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