Hydrophilic and lipophilic radiopharmaceuticals as tracers in pharmaceutical development : in vitro in vivo studies.

Dublin Core

Título

Hydrophilic and lipophilic radiopharmaceuticals as tracers in pharmaceutical development : in vitro in vivo studies.

Tema

RECURSO ELECTRÓNICO
RADIOFARMACIA
PRODUCTOS FARMACEUTICOS
BIBLIOGRAFIA NACIONAL QUIMICA
2005

Abstract

Background: Scintigraphic studies have been performed to assess the release, both in vitro and in vivo, of radiotracers from tablet formulations. Four different tracers with differing physicochemical characteristics have been evaluated to assess their suitability as models for drug delivery. Methods: In-vitro disintegration and dissolution studies have been performed at pH 1, 4 and 7. Invivo studies have been performed by scintigraphic imaging in healthy volunteers. Two hydrophilic tracers, (99mTc-DTPA) and (99mTc-MDP), and two lipophilic tracers, (99mTc-ECD) and (99mTc-MIBI), were used as drug models. Results: Dissolution and disintegration profiles, differed depending on the drug model chosen. In vitro dissolution velocity constants indicated a probable retention of the radiotracer in the formulation. In vivo disintegration velocity constants showed important variability for each radiopharmaceutical. Pearson statistical test showed no correlation between in vitro drug release, and in vivo behaviour, for 99mTc-DTPA, 99mTc-ECD and 99mTc-MIBI. High correlation coefficients were found for 99mTc-MDP not only for in vitro dissolution and disintegration studies but also for in vivo scintigraphic studies. Conclusion: Scintigraphic studies have made a significant contribution to the development of drug delivery systems. It is essential, however, to choose the appropriate radiotracers as models of drug behaviour. This study has demonstrated significant differences in release patterns, depending on the model chosen. It is likely that each formulation would require the development of a specific model, rather than being able to use a generic drug model on the basis of its physicochemical characteristics.

Autor

Paolino, Andrea
Frier, Malcolm

Fuente

BMC Nuc. Med. v. 55, 2005

Editor

BioMed Central

Fecha

2005

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PDF

Idioma

Inglés

Tipo

Artículo

Identificador

doi:10.1186/1471-2385-5-5

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Original Format

PDF
Fecha de agregación
April 7, 2015
Colección
Bibliografía Nacional Química
Tipo de Elemento
Document
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Citación
Terán, Mariella, “Hydrophilic and lipophilic radiopharmaceuticals as tracers in pharmaceutical development : in vitro in vivo studies.,” RIQUIM - Repositorio Institucional de la Facultad de Química - UdelaR, accessed June 24, 2022, http://riquim.fq.edu.uy/items/show/2659.
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