How Does the Addition of Kollidon
amorphization
contact angle
dissolution
ezetimibe
solid dispersion
Journal
Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003
Informations de publication
Date de publication:
23 Jan 2021
23 Jan 2021
Historique:
received:
30
12
2020
revised:
15
01
2021
accepted:
20
01
2021
entrez:
27
1
2021
pubmed:
28
1
2021
medline:
28
1
2021
Statut:
epublish
Résumé
Amorphization serves as a strategy for the improvement of poor dissolution characteristics of many drug compounds. However, in many formulations the content of polymeric stabilizer is high, which is undesirable from the perspective of future applications. Thus, studying the composition-dependent stability of amorphous solid dispersions seems to be demanded. In this paper, we describe the amorphization of ezetimibe, a lipid-lowering drug, in the spray drying process and investigate the effect of polyvinylpyrrolidone-co-poly(vinyl acetate) (PVP/VA) content on the physical stability and dissolution characteristics of the drug. Fully amorphous systems were obtained when the concentration of the polymer in solid dispersion was as low as 20%. The amorphization led to the dissolution enhancement by even 70%, with a noticeable sudden increase at around 40% of PVP/VA content and very small variations for systems having 66-90% PVP/VA. It was also correlated to wettability characteristics of solid dispersions, which may suggest that in the vicinity of 40% of the polymer content, the behavior of the system becomes independent of the PVP/VA content.
Identifiants
pubmed: 33498609
pii: pharmaceutics13020147
doi: 10.3390/pharmaceutics13020147
pmc: PMC7912050
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Narodowe Centrum Nauki
ID : 2015/16/W/NZ7/00404
Références
Eur J Pharm Sci. 2010 Jan 31;39(1-3):125-33
pubmed: 19932176
Saudi Pharm J. 2018 Jul;26(5):725-732
pubmed: 29991917
Mol Pharm. 2009 Sep-Oct;6(5):1492-505
pubmed: 19634917
Curr Atheroscler Rep. 2018 Mar 7;20(4):19
pubmed: 29516190
Int J Pharm. 2015 Oct 15;494(1):23-30
pubmed: 26241751
Int J Pharm. 2013 Aug 30;453(1):253-84
pubmed: 22820134
Lancet. 2018 Nov 10;392(10159):1789-1858
pubmed: 30496104
J Pharm Sci. 2010 Feb;99(2):575-86
pubmed: 19774644
Mol Pharm. 2015 Oct 5;12(10):3610-9
pubmed: 26301858
Eur J Pharm Biopharm. 2006 Jun;63(2):103-14
pubmed: 16675209
AAPS PharmSciTech. 2020 Sep 4;21(7):254
pubmed: 32888102
Pharmacol Rev. 2013 Jan;65(1):315-499
pubmed: 23383426
Circulation. 2019 Jun 18;139(25):e1082-e1143
pubmed: 30586774
Int J Pharm. 2015 Dec 30;496(2):382-91
pubmed: 26468038
Pharmaceutics. 2018 Oct 18;10(4):
pubmed: 30340413
Eur J Pharm Biopharm. 2017 Nov;120:43-51
pubmed: 28822874
J Pharm Sci. 2006 Dec;95(12):2692-705
pubmed: 16892209
JAMA. 2019 Feb 26;321(8):800-801
pubmed: 30715135
Clin Pharmacokinet. 2005;44(5):467-94
pubmed: 15871634
J Pharm Sci. 2016 Sep;105(9):2527-2544
pubmed: 26886314
Mol Pharm. 2014 Nov 3;11(11):4280-90
pubmed: 25310722
Chem Pharm Bull (Tokyo). 2011;59(1):41-5
pubmed: 21212545
Eur J Pharm Sci. 2010 May 12;40(2):84-93
pubmed: 20230893
Pharmacotherapy. 2003 Nov;23(11):1463-74
pubmed: 14620392
Eur J Pharm Biopharm. 2015 Oct;96:237-46
pubmed: 26247119
Eur J Pharm Biopharm. 2008 May;69(1):303-11
pubmed: 18053697
J Pharm Sci. 2012 Apr;101(4):1355-77
pubmed: 22213468
Adv Drug Deliv Rev. 2016 Jun 1;101:122-142
pubmed: 27013254
Pharm Res. 2009 Nov;26(11):2523-34
pubmed: 19771495
Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):799-813
pubmed: 24056053
Eur J Pharm Biopharm. 2013 May;84(1):208-18
pubmed: 23246797
J Pharm Sci. 2018 Jan;107(1):24-33
pubmed: 29031973
Curr Top Med Chem. 2005;5(3):243-56
pubmed: 15857308
Pharmaceutics. 2020 May 09;12(5):
pubmed: 32397432
J Pharm Sci. 2010 Sep;99(9):4005-12
pubmed: 20533553
J Pharm Sci. 2017 Jan;106(1):5-27
pubmed: 27372552
Pharm Res. 2006 Oct;23(10):2417-26
pubmed: 16933098
Adv Drug Deliv Rev. 2016 May 1;100:27-50
pubmed: 26705850