Identifying the stable polymorph early in the drug discovery-development process.
Pharm Dev Technol
; 10(2): 291-7, 2005.
Article
em En
| MEDLINE
| ID: mdl-15926678
ABSTRACT
The thermodynamically most stable polymorph under ambient conditions is almost without exception the most desirable crystalline form for development by a pharmaceutical company. It is, therefore, beneficial to discover and to characterize this polymorph at the earliest possible stage of development. A screen for discovering the stable polymorph of a pharmaceutical compound early in the drug discovery-development process is developed and described. In this screen, a small amount of compound is suspended in a diverse group of solvents for two weeks in an effort to crystallize the most stable polymorph. The solubility of the compound in each solvent utilized in the stable polymorph screen is also simultaneously determined using a simple gravimetric method. Ritonavir and an early development candidate (Pfizer compound A) are used as model compounds to demonstrate the utility of the screen for finding the stable polymorph early in the drug discovery-development process.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Preparações Farmacêuticas
/
Desenho de Fármacos
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Pharm Dev Technol
Assunto da revista:
FARMACIA
Ano de publicação:
2005
Tipo de documento:
Article
País de afiliação:
Estados Unidos