Abstract：
:Developing amorphous solid dispersions of water-insoluble molecules using polymeric materials is a well-defined approach to improve the dissolution rate and bioavailability. While the selected polymer plays a vital role in stabilizing the amorphous solid dispersion physically, it is equally important to improve the dissolution profile by inhibiting crystallization from the supersaturated solution generated by dissolution of the amorphous material. Furthermore, understanding the mechanism of dissolution rate enhancement is of vital importance. In this work, wetting kinetics was taken up as an alternative approach for understanding the enhanced dissolution rate for amorphous solid dispersion of a poorly soluble drug. While cilostazol (CIL) was selected as the model drug, povidone (PVP), copovidone, and hypromellose (HPMC) were the polymers of choice. The concentrations against time profiles were evaluated for the supersaturated solutions of CIL in the presence and absence of the selected polymers. The degree of supersaturation increased significantly with increase in polymer content within the solid dispersion. While povidone was found to maintain the highest level of supersaturation for the greatest length of time both in dissolution and solution crystallization experiments, copovidone and hypromellose were found to be the less effective as crystallization inhibitor. The ability of polymers to generate and maintain supersaturated drug solutions was assessed by dissolution studies. The wetting kinetics was compared against the solid dispersion composition to establish a correlation with enhanced dissolution rate.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Verma S,Rudraraju VSdoi
10.1208/s12249-014-0281-xsubject
Has Abstractpub_date
2015-10-01 00:00:00pages
1079-90issue
5issn
1530-9932pii
10.1208/s12249-014-0281-xjournal_volume
16pub_type
杂志文章abstract：:The present work embarks upon increasing the dissolution rate and the bioavailability of model anti-diabetic drug, gliquidone, a sulfonylurea class drug used for treating diabetes mellitus type 2. The gliquidone nanoparticles were prepared by using anti-solvent precipitation technique in which, gliquidone solution in ...
journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-017-0751-z
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1565-y
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章,评审
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-019-1600-z
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01741-w
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0078-y
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
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pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
pub_type： 已发布勘误
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pub_type： 杂志文章
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