Multivariate analysis in the development of bioequivalent tablets containing bicalutamide.
Pharm Dev Technol
; 26(1): 48-59, 2021 Jan.
Article
em En
| MEDLINE
| ID: mdl-33121318
ABSTRACT
The pharmaceutical industry has to tackle the explosion of high amounts of poorly soluble APIs. This phenomenon leads to numerous sophisticated solutions. These include the use of multifactorial data analysis identifying correlations between the components and dosage form properties, laboratory and production process parameters with respect to the API liberation Example of such API is bicalutamide. Improved liberation is achieved by particle size reduction. Laboratory batches, with different PSD of API, were filled into gelatinous capsules and consequently granulated for tablet compression. Comparative dissolution profiles with Casodex 150 mg (Astra Zeneca) were performed. The component analysis was used for the statistical evaluation of f1 and f2 factors and D(v,0.9) and D[4,3] parameters of PSD to identify optimal PSD values. Suitable PSD limits for API were statistically confirmed in laboratory and in commercial scale with respect to optimized tablet properties. The tablets were bioequivalent with originator (n = 20; 90% CI for ln AUC0-120 99.8-111.9%; 90% CI for ln cmax 101.1-112.9%). In conclusion, the micronisation of the API is still an efficient and inexpensive method improving the bioavailability, although there are more complicated and expensive methods available. Statistical multifactorial methods improved the safety and reproducibility of production.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Tosil
/
Química Farmacêutica
/
Anilidas
/
Nitrilas
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Pharm Dev Technol
Assunto da revista:
FARMACIA
Ano de publicação:
2021
Tipo de documento:
Article