Medicament box of 2beta-[N,N'-di(2-mercaptoethyl) ethylene diamine] methyl-3 beta-(4- chlorphenyl) tropane

A technology of ethylenediamine and chlorophenyl, which is applied in the field of single photon emission computed tomography imaging agents, can solve the problems of increasing operation steps, complicated operation process, and increased cost, and achieves simple marking process, convenient promotion and application, and marking The effect of rate stabilization

Inactive Publication Date: 2006-04-26
JIANGSU INST OF NUCLEAR MEDICINE
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  • Description
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Problems solved by technology

However, this method increases the operation steps, the operation process is co

Method used

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  • Medicament box of 2beta-[N,N'-di(2-mercaptoethyl) ethylene diamine] methyl-3 beta-(4- chlorphenyl) tropane
  • Medicament box of 2beta-[N,N'-di(2-mercaptoethyl) ethylene diamine] methyl-3 beta-(4- chlorphenyl) tropane
  • Medicament box of 2beta-[N,N'-di(2-mercaptoethyl) ethylene diamine] methyl-3 beta-(4- chlorphenyl) tropane

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Experimental program
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Effect test

Embodiment 1

[0021] Preparation of TRODAT-1 kit:

[0022] The preparation method of 100 bottles of TRODAT-1 kit is as follows: Weigh 2 mmol of potassium dihydrogen phosphate and 5 mmol of disodium hydrogen phosphate, dissolve them in 88 mL of distilled water, then add 1.00 g of sodium glucoheptonate and 100 mg of ethylenediaminetetraacetic acid Disodium, add 7.00mL of 1.00mg / mL stannous chloride dilute hydrochloric acid (0.05mol / L) solution, and finally add 5.00mL of 1.00mg / mL TRODAT-1 dilute hydrochloric acid (0.05mol / L) solution, mix well Sterile filtration, and then divided into 10m1 vials at 1.00mL / bottle, and freeze-dried to obtain the TRODAT-1 kit. Each kit contains 50.0 μg of TRODAT-1, 70.0 μg of stannous chloride, 1.00 mg of disodium EDTA and 10.0 mg of sodium glucoheptonate, and the pH value after adding 1 ml of water to the kit For: 4.0-8.5.

Embodiment 2

[0024] Labeling method of TRODAT-1 kit:

[0025] Take 1 piece of TRODAT-1 kit, add the newly rinsed Na 99m TcO 4 Solution 1.0mL, placed in a boiling water bath and heated for 30min, after cooling.

Embodiment 3

[0027] Marking rate measurement method:

[0028] Upstream thin layer chromatography (TLC) method.

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Abstract

The technetium [99m Tc] cachet pharmaceutical case for the 2beta- [N, N'-(2-mercapto ethyl) ethylenediamine] methyl-3beta-(4- chlorphenyl) tropane (in the following, using TRODAT-1 as abbreviation), relating to technique field of single photon emission computer tomography (SPECT) imaging agent. The invention provides a medicine case formulation for the TRODAT-1, the operation is simple and the marking rate is stable and larger than 90% when the medicine case is used for the mark of [99mTc]. The medicine is prepared through a certain composition of TRODAT-1, stannous salt, gluceplate, edetate and pH buffering agent. There is no identical report of the medicine case raised in this invention in the international.

Description

technical field [0001] Technetium [ 99m Tc] labeling kit involving Tc[ 99m The invention relates to the formulation and preparation technology of a Tc] labeling kit, belonging to the technical field of single photon emission computed tomography (SPECT) imaging agents. Background technique [0002] Technetium [ 99m Tc]-2β-[N, N'-bis(2-mercaptoethyl)ethylenediamine]methyl-3β-(4-chlorophenyl)tropane ( 99m Tc-TRODAT-1) is the first technetium[ 99m Tc] labeled dopamine transporter imaging agent successfully used in human body, it can specifically combine with dopamine transporter in the brain and concentrate in the striatum, provide clear images, prompt the change information of the dopaminergic system, and provide information on the changes of the dopaminergic system It has great potential for clinical application especially in the early diagnosis of Parkinson's disease. Since the first report by Kung H.F. in 1996, a large number of pharmacological and clinical studies have...

Claims

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Application Information

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IPC IPC(8): A61K51/00A61K103/10
Inventor 陈正平李晓敏王颂佩唐婕
Owner JIANGSU INST OF NUCLEAR MEDICINE
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