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Degrees of order : A comparison of nanocrystal and amorphous solids for poorly soluble drugs
- Publication Year :
- 2020
-
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.
- Subjects :
- DISSOLUTION BEHAVIOR
Materials science
DISPERSIONS
IMPACT
BIOAVAILABILITY
Chemistry, Pharmaceutical
Biological Availability
Pharmaceutical Science
02 engineering and technology
SOLUBILITY
030226 pharmacology & pharmacy
Dosage form
Biopharmaceutics
03 medical and health sciences
0302 clinical medicine
NANOPARTICLES
Technology, Pharmaceutical
Solubility
Solubility enhancement
Dissolution
Crystallinity
FORMULATION
Poor solubility
021001 nanoscience & nanotechnology
Biopharmaceutics Classification System
Small molecule
PARTICLE-SIZE
Amorphous solid
Nanocrystals
Supersaturation
Order (biology)
Pharmaceutical Preparations
Nanocrystal
317 Pharmacy
Amorphous
PROCESS PARAMETERS
Biochemical engineering
0210 nano-technology
PRECIPITATION INHIBITORS
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....641b696d1c7e903437bb741fe6996d73