New methodology for pancreatic scintiscanning imaging using 125I-L-3 Iodo-alpha-Methyl Tyrosine.

The difficulty of a reliable diagnosis of pancreatic diseases by scintiscanning, is mainly derived from the lack of adequate radiopharmaceuticals. With this purpose 125I-L-3 Iodo-a-Methyl Tyrosine (125I-IMT) has been studied, which has also been used for the diagnosis of different kind of brain tumors. The purpose of this work is the development of a quick and easy method for the synthesis and purification of the 125I-IMT in order to be used in a Nuclear Medicine Service. The L-alpha-Methyl Tyrosine was labeled with 125I using I-/I03 and afterwards purified by an anionic exchange resin. The labeling yield obtained was (96.0 +/- 0.5)% when the incubation time was 15 minutes. No significant statistical differences were observed when the incubation time was extended to 1 hour. Biodistribution studies in mice show that the percentage of activity concentration in pancreas is (34.24 +/- 14.03)% at 15 minutes post injection, remaining constant for 30 minutes. The pancreas/liver ratio 15 minutes after the injection of the labeled product was (12.22 +/- 3.59) and it remained constant for 45 minutes more. These results show that 125I-IMT can be used as a diagnostic agent for pancreatic diseases. Since 123I was not available at the moment, this new methodology was developed with 125I.

New methodology for pancreatic scintiscanning imaging using 125I-L-3 iodo-alpha-methyl tyrosine

The difficulty of a reliable diagnosis of pancreatic diseases by scintiscanning, is mainly derived from the lack of adequate radiopharmaceuticals. With this purpose (125) I-L(-3) Iodo-a-Methyl Tyrosine ((125) I-IMT) has been studied, which has also been used for the diagnosis of different kind of brain tumors. The purpose of this work is the development of a quick and easy method for the synthesis and purification of the (125) I-IMT in order to be used in a Nuclear Medicine Service. The L-(-Methly Tyrosine was labeled with (125) I using I-/I03 and afterwards purified by an aniomic exchange resin. The labeling yield obtained was (96.0+0.5) per cent when the incubation time was 15 minutes. No significant statistical differences were observed when the incubation time was extended to 1 hour. Biodistribution studies in mice show that the percentage of activity concentration in pancreas is (34.24+14.03) per cent at 15 minutes post injection, remaining constant for 30 minutes. The pancreas/liver ratio 15 minutes after the injection of the labeled product was (12.22+3.59) and it remained constant for 45 minutes more. These results show that (125) I-IMT cab be used as a diagnostic agent for pancreatic diseases. Since (123) I was not avilable at the moment, this new methodology was developed with (125) I. (AU)

New methodology for pancreatic scintiscanning imaging using 125I-L-3 iodo-alpha-methyl tyrosine

The difficulty of a reliable diagnosis of pancreatic diseases by scintiscanning, is mainly derived from the lack of adequate radiopharmaceuticals. With this purpose (125) I-L(-3) Iodo-a-Methyl Tyrosine ((125) I-IMT) has been studied, which has also been used for the diagnosis of different kind of brain tumors. The purpose of this work is the development of a quick and easy method for the synthesis and purification of the (125) I-IMT in order to be used in a Nuclear Medicine Service. The L-(-Methly Tyrosine was labeled with (125) I using I-/I03 and afterwards purified by an aniomic exchange resin. The labeling yield obtained was (96.0+0.5) per cent when the incubation time was 15 minutes. No significant statistical differences were observed when the incubation time was extended to 1 hour. Biodistribution studies in mice show that the percentage of activity concentration in pancreas is (34.24+14.03) per cent at 15 minutes post injection, remaining constant for 30 minutes. The pancreas/liver ratio 15 minutes after the injection of the labeled product was (12.22+3.59) and it remained constant for 45 minutes more. These results show that (125) I-IMT cab be used as a diagnostic agent for pancreatic diseases. Since (123) I was not avilable at the moment, this new methodology was developed with (125) I.

Marcación, control y estudios de estabilidad y distribución biológica del Acido Condroitin Sulfato.Tc-99m / Labelling, control, stability and biological distribution of condroitin

Se ajustó a la técnica de preparación del ACS.Tc-99m descrita por Dupuy y col., encontrándose el pH óptimo para su estabilidad. Se estudió la distribución biológica en ratones, determinando el porcentaje de dosis inyectada en distintos órganos, a diferentes tiempos

Marcación, control y estudios de estabilidad y distribución biológica del Acido Condroitin Sulfato.Tc-99m / Labelling, control, stability and biological distribution of condroitin

Se ajustó a la técnica de preparación del ACS.Tc-99m descrita por Dupuy y col., encontrándose el pH óptimo para su estabilidad. Se estudió la distribución biológica en ratones, determinando el porcentaje de dosis inyectada en distintos órganos, a diferentes tiempos

Síntesis y control del MAG3 99mTc. Estudios comparativos con el hipurán 131I en seres humanos / Syntesis and control of Tc99m MAG3: comparative study with 131I hippuran in humans

La benzoilmercaptoacetiltriglicina (MAG,) se sintetizó de acuerdo con el método de A.R.Fritzberg y colaboradores. Se comprobó su pureza por punto de fusión, composición centesimal, cromatografía líquida de alta presión y resonancia magnética nuclear. Se realizaron estudios farmacológicos, esterilidad, apirogenicidad, toxicidad aguda y distribución biológica en animales. El producto (MAG,) marcado con tecnecio 99m, según la técnica de J.R.Coveney y M.S.Roblins, se controló por cromatografía en papel. Posteriormente, se inyectó en seres humanos (2,5-3 ,Ci) en normales y con patología renal (39 casos totales) realizándose el estudio comparativo con hipurán

Síntesis y control del MAG3 99mTc. Estudios comparativos con el hipurán 131I en seres humanos / Syntesis and control of Tc99m MAG3: comparative study with 131I hippuran in humans

La benzoilmercaptoacetiltriglicina (MAG,) se sintetizó de acuerdo con el método de A.R.Fritzberg y colaboradores. Se comprobó su pureza por punto de fusión, composición centesimal, cromatografía líquida de alta presión y resonancia magnética nuclear. Se realizaron estudios farmacológicos, esterilidad, apirogenicidad, toxicidad aguda y distribución biológica en animales. El producto (MAG,) marcado con tecnecio 99m, según la técnica de J.R.Coveney y M.S.Roblins, se controló por cromatografía en papel. Posteriormente, se inyectó en seres humanos (2,5-3 ,Ci) en normales y con patología renal (39 casos totales) realizándose el estudio comparativo con hipurán

Myocardial imaging with technetium-99m CPI: initial experience in the human.

The hexakis(isonitrile)technetium(I) analog [99mTc]carbomethoxyisopropyl isonitrile (CPI) has high myocardial uptake and rapid lung and liver clearance in most animal species. To evaluate [99mTc]CPI as a myocardial imaging agent in the human, we evaluated this tracer in three normals and in six patients with coronary artery disease (CAD). In normals, [99mTc]CPI cleared quickly from the lungs and accumulated in the liver and heart. The liver activity peaked at 10-15 min and cleared through the hepatobiliary system. Planar images were of excellent technical quality with high myocardial to background ratios as early as 10 min after injection. Myocardial activity fell gradually to 76.1 +/- 2.9 (s.d.)% of initial activity by 60 min after injection. In six patients with CAD, myocardial defects were present on planar images up to 2 hr after exercise and injection. In one out of six patients, the defect was not seen 3 hr after injection. In five of the six patients, normal perfusion patterns were observed 1 hr after reinjection of CPI at rest (4 hr after the initial injection). In one patient who developed spontaneous angina prior to reinjection, the perfusion defects persisted. The repeat study 3 days later with injection of [99mTc]CPI at rest was normal. Technetium-99m CPI appears to have excellent physical and biologic properties for use in association with myocardial imaging with exercise.

Pharmacokinetic study of 2-(2'-methyl-3'-chloro-anilino)-lysine nicotinate (L-104).

The pharmacokinetic study of a new analgesic-antiinflammatory agent, 2-(2'-methyl-3'-chloro-anilino)lysine nicotinate (L-104), was preformed in the rat and the dog. When administered p.o. in rats at a dose of 40 mg/kg, the serum peak was 131.3 microgram/ml +/- 10.3 at 15 min post application, and the elimination t 1/2 was 1.20 h. For the same dose, given i.v., the biological t 1/2 was 1.38 h, the AUC 337.18 microgram/ml/h and the Vdss 0.232 l/kg. When administered i.v. in dogs of 10 mg/kg, the biological t 1/2 was 0.96 h +/- 0.14, the AUC 73,066 microgram/ml/h and the Vdss 0.178 l/kg. In the rat, for a dose of 40 mg/kg given p.o., 79.1% of tritium-labelled L-104 were excreted within 72 h, 56.0% of them through the kidneys. In the dog, at an i.v. dose of 10 mg/kg, the whole of the drug was excreted at the end of 72 h, corresponding 52.6% urinary excretion. The main metabolite in the rat was 2-(2'-methyl-3'-chloro-4'-hydroxy-anilino)-nicotinic acid (72.2%), whereas in the dog it was 2-(2'-methyl-3'-chloro-anilino)-5-hydroxy-nicotinic acid (35.2%).