Radiochemical and radiopharmacological properties of pirocarbotrat and other labeled charcoal dispersions: comparative studies in rats with NMU-induced mammary tumors.

The purpose of this work is to study the physicochemical properties of Pirocarbotrat to explain its radiopharmacological behavior. We also studied a mixture of charcoal plus chromic [32P]phosphate and charcoal plus sodium [32P]orthophosphate only for comparative purposes. The results show that the mean diameter of the Pirocarbotrat particles was 2.5 microm with an homogeneous distribution, while the other products show an heterogeneous distribution of the particle sizes, with a mean size diameter between 0.5 and 0.9 microm. Hydrolysis studies with a solution of 0.1 N HCl and with sulfochromic mixture revealed that in Pirocarbotrat the 32P is strongly bound to the charcoal particles. Bioelimination studies of Pirocarbotrat show that the total eliminated activity was 12.70 +/- 3.90%, with a higher amount in urine (8.30 +/- 1.80%) than in feces (4.40 +/- 3.50%). When biodistribution studies of Pirocarbotrat were carried out, we found that the 84.50 +/- 2.60% of the activity remained in the tumor with almost null irradiation of the other organs under study. When therapeutic action was evaluated, we observed that the percentage of tumor regression was 78.3% for the tumors injected with Pirocarbotrat. The other dispersions under study showed different behaviors with high activity percentages distributed throughout the organism. These studies demonstrate that Pirocarbotrat has the best radiopharmacological properties to ensure irradiation of the tumor with the least concomitant irradiation of surroundings or other organs or tissues.

Pirocarbotrat: a new radiopharmaceutical for the treatment of solid tumors--comparative studies in N-nitrosomethylurea-induced rat mammary tumors.

To evaluate the effectiveness of a single intratumoral dose of Pirocarbotrat, a gelatin-protected charcoal suspension labeled with chromic [32P]pyrophosphate, studies of bioelimination, biodistribution and therapeutic action were carried out in rats, and the results obtained were compared with those of other 32P dispersions. We found that 78.3% of the treated tumors reduced size after 32 days of treatment. At that time, the total eliminated activity was 12.70 +/- 3.90% distributed in urine (8.30 +/- 1.80%) and feces (4.40 +/- 3.50%). Biodistribution studies demonstrate that 84.50 +/- 2.60% of the injected activity remained in the tumor, with no significant concentration in the rest of the organism. We conclude that Pirocarbotrat can be used as a safe agent for brachytherapy of solid tumors with beta particles.

Use of colloids of chromic [32P] phosphate in treatment of solid tumors.

In order to evaluate the effectiveness of an intratumorally single dose of chromic [32P] phosphate for the treatment of solid tumors, studies of bioelimination, biodistribution, and therapeutic action were carried out. Only for comparative purposes were similar studies undertaken using a solution of sodium [32P] orthophosphate-gelatin. Results show that when sodium [32P] orthophosphate-gelatin was intratumorally injected, the percentage of total elimination, after 32 days of treatment, was equal to 85.90 +/- 8.70%, with a higher percentage in urine (64.50 +/- 13.70%) than in feces (21.40 +/- 4.50%). In biodistribution studies, the greater percentage was found in bone (15.54 +/- 2.21%), whereas only 2.51 +/- 0.39% remained in the tumor. When chromic [32P] phosphate was intratumorally injected, we found that the total elimination was equal to 51.70 +/- 6.90%, with a higher amount in feces (32.70 +/- 4.80%) than in urine (19.00 +/- 3.60%). Biodistribution studies demonstrated that 28.93 +/- 1.30% was still in the tumor and 19.01 +/- 1.30% of the injected activity was found in the liver. On the other hand, when therapeutic action was evaluated, no tumoral regression was observed. These results demonstrate that the colloid of chromic [32P] phosphate cannot be used in the treatment of solid tumors as it mobilizes from the injection point, delivering a high dose to the entire organism.

Great particles [32P]chromic phosphate for treatment of solid tumors.

With the purpose of studying the effectivity of an intratumoral single dose of chromic [32P] phosphate with great particles for the treatment of solid tumors, studies of bioelimination, biodistribution and therapeutic action were carried out. Only for comparative purposes, similar studies were undertaken using a solution of sodium -32P- orthophosphate-gelatine. The results show that when sodium [32P] orthophosphate-gelatine is used, the percentage of total elimination is (85.90 +/- 8.70)% with a higher percentage in urine (64.50 +/- 13.70)% than in faeces (21.40 +/- 4.50)%. In biodistribution studies, the greater percentage is found in bone (15.54 +/- 2.21)% while only a (2.51 +/- 0.39)% remains in the tumor. When great particles chromic [32P]phosphate was intratumorally injected, we determined that the total elimination is equal (36.28 +/- 6.27)%, finding a higher amount in faeces (29.44 +/- 5.26)% than in urine (6.84 +/- 2.21)%. Biodistribution studies demonstrated that (49.82 +/- 5.41)% remains in the tumor and (9.63 +/- 4.89)% of the injected activity is found in the liver. On the other hand, when therapeutic action was evaluated, we observed that the percentage of tumor regression (P.T.R.) is 52.0% for the tumors injected with chromic [32P]phosphate and 0.0% for those injected with sodium [32P]orthophosphate-gelatine. These results show that the great particles colloid of chromic [32P]phosphate is not safe enough for the treatment of solid tumors, since it is mobilized from the injection point, delivering a high dose to the whole organism.

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.

Great particles (32P) chromic phosphate for treatment of solid tumors

With the purpose studying the effectivity of an intratumoral single dose of chromic [(32)P] phosphate with great particles for the treatment of solid tumors, studies of biolimination, biodistribution and therapeutic action were carried out. Only for comparative purpose, similar studies were undertaken using a solution of sodium [(32)P] orthophosphategelatine. The results show that when sodium [(32)P] orthophosphategelatine is used, the percentage of total elimination is (85.90+8,70) per cent with a higler percentage in urine (64.50+13.70) per cent than in faeces (21.40+4.50) per cent. In biodistribution studies, the greater percentage is found in bone (15.54+2.21) per cent while only a (2.51+0.39) per cent remains in the tumor. When great particles chromic [(32)P] phosphate was intratumorally injected, we determined that the total elimination is equal (36.28+6.27) per cent, finding a higler amount in faeces (29.44+5.26) per cent than in urine (6.84+2.21) per cent. Biodistribution studies demonstrated that (49.82+5.41) per cent remains in the tumor and (9.63+4.89) per cent of the injected activity is found in the liver. On the other hand, when therapeutic action was evoluted, we observed that the percentage of tumor regression (P.T.R) is 52.0 per cent for the tumors injected with chromic [(32)P] phosphate and 0.0 per cent for those injected with sodium [(32)P] orthophosphate-gelatine. These results show that the great particles colloid of chromic [(32)P] phosphate is not safe enough for the tratment of solid tumors, since it is mobilezed from the injection point, delivering a high dose to the whole organism.

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)

Great particles (32P) chromic phosphate for treatment of solid tumors

With the purpose studying the effectivity of an intratumoral single dose of chromic [(32)P] phosphate with great particles for the treatment of solid tumors, studies of biolimination, biodistribution and therapeutic action were carried out. Only for comparative purpose, similar studies were undertaken using a solution of sodium [(32)P] orthophosphategelatine. The results show that when sodium [(32)P] orthophosphategelatine is used, the percentage of total elimination is (85.90+8,70) per cent with a higler percentage in urine (64.50+13.70) per cent than in faeces (21.40+4.50) per cent. In biodistribution studies, the greater percentage is found in bone (15.54+2.21) per cent while only a (2.51+0.39) per cent remains in the tumor. When great particles chromic [(32)P] phosphate was intratumorally injected, we determined that the total elimination is equal (36.28+6.27) per cent, finding a higler amount in faeces (29.44+5.26) per cent than in urine (6.84+2.21) per cent. Biodistribution studies demonstrated that (49.82+5.41) per cent remains in the tumor and (9.63+4.89) per cent of the injected activity is found in the liver. On the other hand, when therapeutic action was evoluted, we observed that the percentage of tumor regression (P.T.R) is 52.0 per cent for the tumors injected with chromic [(32)P] phosphate and 0.0 per cent for those injected with sodium [(32)P] orthophosphate-gelatine. These results show that the great particles colloid of chromic [(32)P] phosphate is not safe enough for the tratment of solid tumors, since it is mobilezed from the injection point, delivering a high dose to the whole organism. (AU)