Abstract: The present invention relates to an automatic system for synthesizing iodine-123 meta-iodobenzylguanidine (123I-MIBG), which comprises a first reactor for subjecting radioactive iodine-containing sodium iodide and meta-iodobenzylguanidine (MIBG) sulfate to an iodine-iodine exchange reaction to obtain radioactive iodine labeled MIBG; a purification unit for purifying the iodine labeled MIBG; and a second reactor for substituting a solvent used in purification with a phosphate buffer to obtain a phosphate solution containing 123I-MIBG. The present invention also relates to an automatic device for dispensing 123I-MIBG, which comprises the automatic system for synthesizing 123I-MIBG, a radioactivity measuring unit, and a dispensing and packing unit.

Abstract: A radiocontrast agent for tau protein is provided. The agent is selectively and strongly bound to tau protein and its tangle found in brain diseases like Alzheimer's disease (AD). The agent is especially suitable to be used in PET imaging for brain diseases. Or, the agent can be used to inhibit tau protein overexpressive and, thus, stop the proceeding of brain disease.

Abstract: The present invention establishes a fast and simple [F-18] FLT synthesis process. Solid extraction units are used for purification to achieve an equally high and constant radiochemical yield and purity in a short period of time. By using a separation method, the impurities are reduced successfully while the total synthesis time is shortened. The radiochemical purity and the corrected radiochemical yield are both high.

Abstract: The present invention is related to a radiolabeled active targeting pharmaceutical composition, including: a bioconjugate and a radionuclide, wherein the bioconjugate includes a biomolecule and a metal nanoparticle, wherein the biomolecule has an affinity for receptors on the surface of a cell membrane and is selected from the group consisting of a peptide and a protein. The present invention further provides a method for evaluating a thermal adjuvant therapy for tumors and a kit thereof. The above-mentioned pharmaceutical composition is applied to evaluate a tumor accumulation time, so as to establish the optimal policy for a radiofrequency- or laser-induced thermal adjuvant therapy for tumors.

Abstract: A method for preparing a precursor used to label hepatocyte receptors is revealed. The precursor contains a bifunctional structure including trisaccharide and DTPA ligand. During synthesis processes of the precursor, silica gel columns and Reverse phase-18 (RP-18) columns are used for purification. Thus both the purification times and cost of each purification are reduced. Moreover, use diethyl ether to facilitate precipitation of products and remove a part of coupling reagent. Removing the coupling reagent helps purification of products. Furthermore, N?,N?-bis(carboxymethyl)-L-lysine hydrate and benzyl chloroformate are coupled to form a trisaccharide skeleton so as to ensure the yield rate of trisaccharide structure.

Abstract: The present invention is related to a pharmaceutical composition for a liver-receptor imaging injection, the pharmaceutical composition including a bi-functional compound which has a ASGPR specificity, wherein the bi-functional compound includes a backbone of alpha-amino acid (or the derivatives thereof) and a poly-galactosamine chain (or a poly-lactose chain) connected to the alpha-amino acid. Thereby, the pharmaceutical composition can quantify potential of liver storage ability and evaluate severity of the course of liver disease. A liver-receptor imaging injection using the same and the one-step dispensing method thereof are also provided to improve defects of iodine-labeled and overcome disadvantages of the reduced labeling-yield and the instability after autoclave sterilization.

Abstract: The present invention provides a method of preparing [123I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/?mol and radiochemical purity of 95%. The present invention further provides a method of applying [123I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.

Abstract: The present invention relates to an automatic system for synthesizing iodine-123 meta-iodobenzylguanidine (123I-MIBG), which comprises a first reactor for subjecting radioactive iodine-containing sodium iodide and meta-iodobenzylguanidine (MIBG) sulfate to an iodine-iodine exchange reaction to obtain radioactive iodine labeled MIBG; a purification unit for purifying the iodine labeled MIBG; and a second reactor for substituting a solvent used in purification with a phosphate buffer to obtain a phosphate solution containing 123I-MIBG. The present invention also relates to an automatic device for dispensing 123I-MIBG, which comprises the automatic system for synthesizing 123I-MIBG, a radioactivity measuring unit, and a dispensing and packing unit.

Abstract: A 18F-labeled monomeric galactose derivative is provided as a tomography probe. The derivative is a positron emission tomography (PET) probe. The derivative has high affinity and good stability in animal's body. The derivative can be an alternative glucose metabolism imaging agent used in clinic examination and quantification.

Abstract: A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.

Abstract: A novel gall bladder image agent which includes a radio-labelled MAG3-tri-galactosamine, and its preparation method, which includes reacting mercaptoacetyltriglycine (MAG3)-tri-galactosamine, SnF2 and Tc-99m in the presence of a phosphate buffer solution (at pH of from 10.0˜12.0) to obtain Tc-99m-MAG3-tri-galactosamine, when the MAG3-tri-galactosamine is MAG3-DCM-Lys(Gah-GalNAc)3 (where DCM represents a dicarboxymethyl group, and Gah represents a glycine-aminohexyl group), it obtains a labelling yield of at least 90%, and its specific radioactivity is at least 7.0×109 Bq/mg.

Abstract: A tumor radiation probe of iodine-123 marker thymidine (FLT) analogue [123I]-IaraU is disclosed. Commercial available uridine is used as the raw material for the synthesis of the precursor. A radioactive iodine-123 is marked on an alkaline group of uridine to obtain [123I]-IaraU, which is distinguishable from [18F]-FLT marking 18F on a glycosyl group to obtain a novel tumor radiation probe. The marking procedures include mixing the marker precursor with Na [123I] solution, acetic acid and hydrogen peroxide solution, and the solution of chloroform and sodium hydroxide. The sonication time increases from 1 minute to 10 minutes, so that [123I]-IaraU has radiologically chemical purity of higher than 98% and radiological specific activity of not less than 0.196 GBq/umole, and the yield can increase from 8% to 40%. Its radioactive specific activity, yield and purity reach to the degree for the use in biological experiments, while reducing production cost.

Abstract: The present invention provides a method of preparing [123I]Iodooctyl fenbufen amide with a radiochemical yield of 15%, a specific activity of 37 GBq/?mol and radiochemical purity of 95%. The present invention further provides a method of applying [123I]Iodooctyl fenbufen amide as tracer of single photon emission computer tomography (SPECT) to estimate the distribution of cyclooxygenase. By the binding characteristics of the iodine isotope-labeled compounds and the positive correlation of inflammation to tumor lesion, the present invention can estimate the tumor development and metastasis.

Abstract: A tumor radiation probe of iodine-123 marker thymidine (FLT) analogue [123I]-IaraU is disclosed. Commercial available uridine is used as the raw material for the synthesis of the precursor. A radioactive iodine-123 is marked on an alkaline group of uridine to obtain [123I]-IaraU, which is distinguishable from [18F]-FLT marking 18F on a glycosyl group to obtain a novel tumor radiation probe. The marking procedures include mixing the marker precursor with Na [123I] solution, acetic acid and hydrogen peroxide solution, and the solution of chloroform and sodium hydroxide. The sonication time increases from 1 minute to 10 minutes, so that [123I]-IaraU has radiologically chemical purity of higher than 98% and radiological specific activity of not less than 0.196 GBq/umole, and the yield can increase from 8% to 40%. Its radioactive specific activity, yield and purity reach to the degree for the use in biological experiments, while reducing production cost.

Abstract: A novel synthesis method of Glyco-drug radiotracer precursor is revealed. After completing synthesis of Z-Gly-ah (main structure), galactosamine GalNAc(OAc)4 is added to have coupling reaction. Then a product is separated directly from dichloromethane. Thus loss of galactosamine during extraction with liquid chromatography is reduced. Moreover, instead of trifluoroacetyl group, carbobenzoxy (abbreviated as Cbz or Z) is used as a protecting group to ensure uniformity of the phase. The cost and synthesis time are also dramatically reduced.

Abstract: A method for preparing a precursor used to label hepatocyte receptors is revealed. The precursor contains a bifunctional structure including trisaccharide and DTPA ligand. During synthesis processes of the precursor, silica gel columns and Reverse phase-18 (RP-18) columns are used for purification. Thus both the purification times and cost of each purification are reduced. Moreover, use diethyl ether to facilitate precipitation of products and remove a part of coupling reagent. Removing the coupling reagent helps purification of products. Furthermore, N?,N?-bis(carboxymethyl)-L-lysine hydrate and benzyl chloroformate are coupled to form a trisaccharide skeleton so as to ensure the yield rate of trisaccharide structure.

Abstract: The present invention provides a method for fabricating an indium(In)-111 radioactive isotope. A target of cadmium(Cd)-112 is processed through steps of dissolving with heat, absorbing, washing, desorbing and drying for obtaining the In-111 radioactive isotope. Thus, chemical separation is coordinated with the target for fabricating the In-111 radioactive isotope with high efficiency and low cost for production procedure.

Abstract: This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilotriacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in N?-benzyloxycarbonyl-N?-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 molecules of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.

Abstract: A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.

Abstract: The present invention provides a method for fabricating an indium(In)-111 radioactive isotope. A target of cadmium(Cd)-112 is processed through steps of dissolving with heat, absorbing, washing, desorbing and drying for obtaining the In-111 radioactive isotope. Thus, chemical separation is coordinated with the target for fabricating the In-111 radioactive isotope with high efficiency and low cost for production procedure.