Therapeutic188Re-lanreotide: determination of radiopharmacokinetic parameters in rats
| Autor: | Helgi Jung-Cook, Guadalupe Vertiz Serrano, Eva María Molina-Trinidad, Consuelo Arteaga de Murphy, José Luis Morales‐Marquez, Eduardo Murphy Stack, Martha Pedraza-López |
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| Rok vydání: | 2010 |
| Předmět: |
Male
188Re-lanreotide medicine.medical_specialty Carcinoma Hepatocellular Metastatic lesions Urology Pharmaceutical Science High resolution Antineoplastic Agents Peptides Cyclic Bone and Bones Reference Values Internal medicine medicine Animals Tissue Distribution In patient Rats Wistar Radionuclide Imaging Radioisotopes Pharmacology Volume of distribution business.industry Muscles Liver Neoplasms Cancer Tail vein medicine.disease Rats Rhenium Endocrinology Liver Hepatocellular carcinoma Radiopharmaceuticals Somatostatin business Half-Life |
| Zdroj: | Journal of Pharmacy and Pharmacology. 62:456-461 |
| ISSN: | 2042-7158 0022-3573 |
| DOI: | 10.1211/jpp.62.04.0007 |
| Popis: | Objectives The radiopharmacokinetic parameters of the therapeutic radiopharmaceutical 188Re-lanreotide were compared in rats implanted with hepatocarcinoma tumours (n= 18) and healthy rats (n= 18). Methods Rats were injected with approximately 1.8 MBq 188Re-lanreotide (0.1 ml) via the tail vein and blood samples were obtained. The activity per gram of tissue (%IA/g) was calculated and the radiopharmacokinetic parameters determined. Data were fitted using a two-compartment model. Key findings Significant differences were found between healthy and hepatoma rats for beta elimination half-life (22.56 vs 48.14 h); transference constants K10 (ke) (6.44 vs 3.05 h-1) and K12 (2.76 vs 7.09 h-1); volume of distribution (2.06 vs 5.45 ml); mean residence time (66.58 vs 95.50 h) and apparent volume of distribution at steady state (131.30 vs 810.37 ml). The tumour/organ ratios after 24 h were 11.20 for tumour/muscle, 8.00 for tumour/liver and 7.72 for tumour/bone. The scintigraphic images obtained therefore had high resolution. Conclusions188Re-lanreotide had a prolonged beta elimination half-life and increased volume of distribution in rats with hepatocellular carcinoma. This may be beneficial in the diagnosis and therapy of metastatic lesions in patients with cancer. |
| Databáze: | OpenAIRE |
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