Amorphous solid dispersion formation via solvent granulation - A case study with ritonavir and lopinavir.
Amorphous
Lopinavir
Ritonavir
Solvent granulation
Journal
International journal of pharmaceutics: X
ISSN: 2590-1567
Titre abrégé: Int J Pharm X
Pays: Netherlands
ID NLM: 101753452
Informations de publication
Date de publication:
Dec 2019
Dec 2019
Historique:
received:
31
05
2019
revised:
28
08
2019
accepted:
21
09
2019
entrez:
3
12
2019
pubmed:
4
12
2019
medline:
4
12
2019
Statut:
epublish
Résumé
Herein, we evaluate the potential of using a simple solvent granulation process to prepare a binary drug amorphous solid dispersion (ASD) containing two anti-HIV drugs, ritonavir and lopinavir. The drugs were granulated onto a mixture of lactose and microcrystalline cellulose, followed by drying to remove the solvent. The resultant granules were characterized and each drug was found to be X-ray amorphous. No crystallization was observed following storage for 1 month under accelerated stability conditions (40 °C and 75% relative humidity). The dissolution behavior of the compacted granules was compared with the marketed formulation. The dissolution rate of ritonavir was found to be significantly retarded relative to the commercial product when the two drugs were co-granulated. However, comparable release could be achieved when each drug was individually granulated, followed by combination and compaction. The solvent granulation approach may be a viable method to make ASDs of low dose drugs with low crystallization tendencies.
Identifiants
pubmed: 31788669
doi: 10.1016/j.ijpx.2019.100035
pii: S2590-1567(19)30049-0
pii: 100035
pmc: PMC6880113
doi:
Types de publication
Journal Article
Langues
eng
Pagination
100035Informations de copyright
© 2019 The Author(s).
Déclaration de conflit d'intérêts
The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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