Oral Bioavailability Enhancement of Poorly Soluble Drug by Amorphous Solid Dispersion Using Sucrose Acetate Isobutyrate
- PMID: 39237685
- DOI: 10.1208/s12249-024-02924-5
Oral Bioavailability Enhancement of Poorly Soluble Drug by Amorphous Solid Dispersion Using Sucrose Acetate Isobutyrate
Abstract
The focus of the present work was to develop amorphous solid dispersion (ASD) formulation of aprepitant (APT) using sucrose acetate isobutyrate (SAIB) excipient, evaluate for physicochemical attributes, stability, and bioavailability, and compared with hydroxypropyl methylcellulose (HPMC) based formulation. Various formulations of APT were prepared by solvent evaporation method and characterized for physiochemical and in-vivo performance attributes such as dissolution, drug phase, stability, and bioavailability. X-ray powder diffraction indicated crystalline drug conversion into amorphous phase. Dissolution varied as a function of drug:SAIB:excipient proportion. The dissolution was more than 80% in the optimized formulation (F10) and comparable to HPMC based formulation (F13). Stability of F10 and F13 formulations stored at 25 C/60% and 40°C/75% RH for three months were comparable. Both ASD formulations (F10 and F13) were bioequivalent as indicated by the pharmacokinetic parameters Cmax and AUC0-∞. Cmax and AUC0-∞ of F10 and F13 formulations were 2.52 ± 0.39, and 2.74 ± 0.32 μg/ml, and 26.59 ± 0.39, and 24.79 ± 6.02 μg/ml.h, respectively. Furthermore, the bioavailability of ASD formulation was more than twofold of the formulation containing crystalline phase of the drug. In conclusion, stability and oral bioavailability of SAIB based ASD formulation is comparable to HPMC-based formulation of poorly soluble drugs.
Keywords: amorphous solid dispersion; aprepitants; pharmacokinetic; stability; sucrose acetate isobutyrate.
© 2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.
Similar articles
-
Application of Sucrose Acetate Isobutyrate in Development of Co-Amorphous Formulations of Tacrolimus for Bioavailability Enhancement.Pharmaceutics. 2023 May 9;15(5):1442. doi: 10.3390/pharmaceutics15051442. Pharmaceutics. 2023. PMID: 37242683 Free PMC article.
-
Preparation and Characterization of Stable Amorphous Glassy Solution of BCS II and IV Drugs.AAPS PharmSciTech. 2021 Dec 23;23(1):35. doi: 10.1208/s12249-021-02198-1. AAPS PharmSciTech. 2021. PMID: 34950995
-
Formulation performance and processability window for manufacturing a dual-polymer amorphous solid dispersion via hot-melt extrusion and strand pelletization.Int J Pharm. 2018 Dec 20;553(1-2):408-421. doi: 10.1016/j.ijpharm.2018.10.035. Epub 2018 Oct 14. Int J Pharm. 2018. PMID: 30326284
-
Hypromellose - A traditional pharmaceutical excipient with modern applications in oral and oromucosal drug delivery.J Control Release. 2020 Aug 10;324:695-727. doi: 10.1016/j.jconrel.2020.05.045. Epub 2020 May 29. J Control Release. 2020. PMID: 32479845 Review.
-
Navigating the Solution to Drug Formulation Problems at Research and Development Stages by Amorphous Solid Dispersion Technology.Recent Adv Drug Deliv Formul. 2024;18(2):79-99. doi: 10.2174/0126673878271641231201065151. Recent Adv Drug Deliv Formul. 2024. PMID: 38062659 Review.
References
-
- Emend® FDA label. https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/21549_Emend_lb... . Accessed on May 15, 2024.
-
- Abouhussein DMN. Enhnaced transdermal permeation of BCS class IV aprepitant using binary ethosome: Optimization, characterization and ex vivo permeation. J Drug Del Sci Technol. 2021;61:20285.
-
- Abdellatif AAH, Alsowinea AF. Approved and marketed nanoparticles for disease targeting and applications in COVID-19. Nanotech Rev. 2021;10:1941–77. - DOI
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Miscellaneous
