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Degrees of order: A comparison of nanocrystal and amorphous solids for poorly soluble drugs.
Metadata
Journalinternational journal of pharmaceutics4.845Date
2020 Jun 04
4 months ago
Type
Journal Article
Volume
2020-Aug-30 / 586 : 119492
Author
Peltonen L 1, Strachan CJ 2
Affiliation
  • 2. Drug Research Program, Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56, Viikinkaari 5 E, FI-00014, Finland.
Doi
PMIDMESH
Abstract
Poor aqueous solubility is currently a prevalent issue in the development of small molecule pharmaceuticals. Several methods are possible for improving the solubility, dissolution rate and bioavailability of Biopharmaceutics Classification System (BCS) class II and class IV drugs. Two solid state approaches, which rely on reductions in order, and can theoretically be applied to all molecules without any specific chemical prerequisites (compared with e.g. ionizable or co-former groups, or sufficient lipophilicity), are the use of the amorphous form and nanocrystals. Research involving these two approaches is relatively extensive and commercial products are now available based on these technologies. Nevertheless, their formulation remains more challenging than with conventional dosage forms. This article describes these two technologies from both theoretical and practical perspectives by briefly discussing the physicochemical backgrounds behind these approaches, as well as the resulting practical implications, both positive and negative. Case studies demonstrating the benefits and challenges of these two techniques are presented.
Keywords: Amorphous Crystallinity Nanocrystals Poor solubility Solubility enhancement Supersaturation
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4.8
Int J Pharminternational journal of pharmaceutics
Metadata
LocationNetherlands
FromELSEVIER

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