Strategies to address low drug solubility in discovery and development

HD Williams, NL Trevaskis, SA Charman… - Pharmacological …, 2013 - ASPET
Drugs with low water solubility are predisposed to low and variable oral bioavailability and,
therefore, to variability in clinical response. Despite significant efforts to “design in” …

Amorphous drug delivery systems: molecular aspects, design, and performance

AM Kaushal, P Gupta, AK Bansal - Critical Reviews™ in …, 2004 - dl.begellhouse.com
The biopharmaceutical properties—especially the solubility and permeability—of a molecule
contribute to its overall therapeutic efficacy. The newer tools of drug discovery have caused …

Dissolution and precipitation behavior of amorphous solid dispersions

DE Alonzo, YI Gao, D Zhou, H Mo, GGZ Zhang… - Journal of …, 2011 - Elsevier
Amorphous solid dispersions (ASDs) are widely utilized in the pharmaceutical industry for
bioavailability enhancement of low solubility drugs. The important factors governing the …

Thermal analysis of cyclodextrins and their inclusion compounds

F Giordano, C Novak, JR Moyano - Thermochimica Acta, 2001 - Elsevier
This review examines the literature concerning the thermal properties of natural and
semisynthetic cyclodextrins and their inclusion compounds. Particular emphasis is given to …

Role of cyclodextrins in improving oral drug delivery

T Loftsson, ME Brewster, M Masson - American Journal of Drug Delivery, 2004 - Springer
The use of high-throughput screening and similar techniques in drug discovery has put a
number of evolutionary pressures on drug candidates such that over time there is a …

Cyclodextrins in the pharmaceutical field

O Bekers, EV Uijtendaal, JH Beijnen… - Drug development …, 1991 - Taylor & Francis
Cyclodextrins (CyDs) are cyclic oligosaccharides, containing a minimum of six D-(+)-
glycopyranose units attached by α-1, 4-linkages produced by the action of the cyclodextrin …

Studies of cyclodextrin inclusion complexes. I. The salbutamol-cyclodextrin complex as studied by phase solubility and DSC

HMC Marques, J Hadgraft, IW Kellaway - International Journal of …, 1990 - Elsevier
Cyclodextrins (CYDs) are cyclic non-reducing oligosaccharides built up from six, seven or
eight glucopyranose units (α-, β-or γ-CYD, respectively). Many drugs are able to form an …

Mechanisms of dissolution of fast release solid dispersions

OI Corrigan - Drug development and industrial pharmacy, 1985 - Taylor & Francis
Drug dissolution from a solid dispersion is dependent on the technology employed to
prepare the dispersion and on the proportion and properties of the carrier used. The …

Improvement of the in vitro dissolution of praziquantel by complexation with α-, β-and γ-cyclodextrins

G Becket, LJ Schep, MY Tan - International journal of pharmaceutics, 1999 - Elsevier
Although praziquantel (PZQ) is the primary drug of choice in the treatment of
schistosomiasis, its poor solubility has restricted its delivery via the oral route. In spite of its …

Interactions of ketoprofen and ibuprofen with β-cyclodextrins in solution and in the solid state

P Mura, GP Bettinetti, A Manderioli, MT Faucci… - International journal of …, 1998 - Elsevier
The complexing, solubilizing and amorphizing abilities towards ketoprofen and ibuprofen of
native β-cyclodextrin and some randomly substituted amorphous derivatives (methyl …