Amorphous Drug Solubility And Absorption Enhancement
Marzena Rams-Baron, R. Jachowicz, E. Boldyreva, Deliang Zhou, Witold Jamróz, M. Paluch
Published 2018 · Chemistry
Download PDFAnalyze on Scholarcy
The poor oral bioavailability of many active pharmaceutical ingredients (APIs) resulting from low solubility is one of the important challenges in pharmaceutical technology. Over the last two decades the number of relatively insoluble drugs has grown steadily. Nowadays it is estimated that approximately 70% of new drug candidates are characterized by poor solubility. In order to ensure the optimum therapeutic efficacy, the selection of the drug substance and formulation is crucial in drug design. The development and approval of new, innovative and safe drugs is tremendously complex and requires extensive knowledge of materials, current technological processes and regulations. Bearing in mind that the form of drug should be suitable for the administration route and safe to apply, understanding of manufacturing process is of key importance to successful dosage form development.
This paper references
What is the True Solubility Advantage for Amorphous Pharmaceuticals?
Bruno C. Hancock (2004)
Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications.
Y. Kawabata (2011)
Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs.
Teófilo Vasconcelos (2007)
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.
C. Lipinski (1997)
Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process.
J. Park (2013)
Hot-melt extrusion for enhanced delivery of drug particles.
D. Miller (2007)
Amorphous is not always better-A dissolution study on solid state forms of carbamazepine.
Linda G. Jensen (2017)
Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs.
S. Baghel (2016)
Unexpected solvent impact in the crystallinity of praziquantel/poly(vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study.
Emanuel D. Costa (2016)
The Mean Dissolution Time Depends on the Dose/Solubility Ratio
E. Rinaki (2004)
Optimizing the physical form - opportunities and limitations.
S. Byrn (2012)
In vitro and in vivo evaluation of carbamazepine-PEG 6000 solid dispersions.
N. Zerrouk (2001)
Correlation of Inhibitory Effects of Polymers on Indomethacin Precipitation in Solution and Amorphous Solid Crystallization Based on Molecular Interaction
Harsh Raj Chauhan (2013)
Poloxamer-based solid dispersions for oral delivery of docetaxel: Differential effects of F68 and P85 on oral docetaxel bioavailability.
Chung Kil Song (2016)
The mechanisms of drug release from solid dispersions in water-soluble polymers.
D. Craig (2002)
Effect of polymer type and drug dose on the in vitro and in vivo behavior of amorphous solid dispersions.
Matthias Manne Knopp (2016)
Supersaturation Produces High Bioavailability of Amorphous Danazol Particles Formed by Evaporative Precipitation into Aqueous Solution and Spray Freezing into Liquid Technologies
J. M. Vaughn (2006)
Dissolution behavior of co‐amorphous amino acid‐indomethacin mixtures: The ability of amino acids to stabilize the supersaturated state of indomethacin
Rami Ojarinta (2017)
Development and in-vivo assessment of the bioavailability of oridonin solid dispersions by the gas anti-solvent technique.
Songming Li (2011)
Amorphous solid dispersions: Rational selection of a manufacturing process.
Teófilo Vasconcelos (2016)
Supersaturation, nucleation, and crystal growth during single- and biphasic dissolution of amorphous solid dispersions: polymer effects and implications for oral bioavailability enhancement of poorly water soluble drugs.
Ashish L. Sarode (2014)
PHYSICOCHEMICAL CHARACTERIZATION OF SPRAY DRIED FORMULATION CONTAINING AMORPHOUS DRUG
Glorybel L Pastrano (2012)
Development of an oral solid dispersion formulation for use in low-dose metronomic chemotherapy of paclitaxel.
J. Moes (2013)
Development of hot melt co-formulated antimalarial solid dispersion system in fixed dose form (ARLUMELT): Evaluating amorphous state and in vivo performance.
Ritesh Fule (2015)
Aqueous solubility: simple predictive methods (in silico, in vitro and bio-relevant approaches).
David Paul Elder (2013)
Oral hesperidin-Amorphization and improved dissolution properties by controlled loading onto porous silica.
Q. Wei (2017)
The role of polymers in oral bioavailability enhancement; a review
Haoyu Liu (2015)
Dissolution Performance of High Drug Loading Celecoxib Amorphous Solid Dispersions Formulated with Polymer Combinations
Tian Xie (2015)
The influence of amorphization methods on the apparent solubility and dissolution rate of tadalafil.
Krzysztof Wlodarski (2014)
Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs.
Chau Le-Ngoc Vo (2013)
Dissolution enhancement of the poorly soluble drug nifedipine by co-spray drying with microporous zeolite beta
Christina Karavasili (2016)
Anomalous dissolution behaviour of tablets prepared from sugar glass-based solid dispersions.
D. V. van Drooge (2004)
Amorphous solid dispersions and nano-crystal technologies for poorly water-soluble drug delivery.
C. Brough (2013)
Amorphous compositions using concentration enhancing polymers for improved bioavailability of itraconazole.
James C Dinunzio (2008)
Establishment of new preparation method for solid dispersion formulation of tacrolimus.
K. Yamashita (2003)
Understanding the Behavior of Amorphous Pharmaceutical Systems during Dissolution
David E. Alonzo (2009)
Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188.
Madhuri Newa (2007)
Part I: Characterization of Solid Dispersions of Nimodipine Prepared by Hot-melt Extrusion
X. Zheng (2007)
Investigation and correlation of drug polymer miscibility and molecular interactions by various approaches for the preparation of amorphous solid dispersions.
Fan Meng (2015)
Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems.
Zsombor K. Nagy (2013)
Use of polymer combinations in the preparation of solid dispersions of a thermally unstable drug by hot-melt extrusion
Jia Liu (2013)
Increasing Dissolution Rates and Gastrointestinal Absorption of Drugs via Solid Solutions and Eutectic mixtures III: Experimental Evaluation of Griseofulvin—succinic Acid Solid Solution
A. H. Goldberg (1966)
The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate.
G. Mooter (2012)
Enhancement of solubility, dissolution and bioavailability of ibuprofen in solid dispersion systems.
Madhuri Newa (2008)
Effect of hydroxypropylcellulose and Tween 80 on physicochemical properties and bioavailability of ezetimibe-loaded solid dispersion.
Rehmana Rashid (2015)
Albendazole Generics—A Comparative In Vitro Study
E. Galia (2004)
Part II: Bioavailability in Beagle Dogs of Nimodipine Solid Dispersions Prepared by Hot-Melt Extrusion
X. Zheng (2007)
Studies on Absorption of Eutectic Mixture. I. A Comparison of the Behavior of Eutectic Mixture of Sulfathiazole and that of Ordinary Sulfathiazole in Man.
K. Sekiguchi (1961)
Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability?
J. Brouwers (2009)
Characterization and Dissolution Properties of Ketoprofen in Binary and Ternary Solid Dispersions with Polyethylene Glycol and Surfactants
P. Mura (2005)
Hot melt extrusion based solid solution approach: Exploring polymer comparison, physicochemical characterization and in-vivo evaluation.
Ritesh Fule (2016)
Improved dissolution and pharmacokinetic behavior of cyclosporine A using high-energy amorphous solid dispersion approach.
S. Onoue (2010)
Preparation of amorphous cefuroxime axetil nanoparticles by sonoprecipitation for enhancement of bioavailability.
R. Dhumal (2008)
Haste Makes Waste: The Interplay Between Dissolution and Precipitation of Supersaturating Formulations
Dajun D. Sun (2015)
Review: physical chemistry of solid dispersions
Sandrien Janssens (2009)
Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract
D. Hörter (1997)
Ritonavir-PEG 8000 amorphous solid dispersions: in vitro and in vivo evaluations.
D. Law (2004)
Solubility and dissolution enhancement strategies: current understanding and recent trends*
S. Jain (2015)
Dissolution and Absorption of Nipedipine from Nifedipine-Polyvinylpyrrolidone Coprecipitate
Isao Sugimoto (1980)
Solid dispersion: A promising technique to enhance solubility of poorly water soluble drug
A. Sharma (2011)
The developability classification system: application of biopharmaceutics concepts to formulation development.
J. Butler (2010)
Impact of solid state properties on developability assessment of drug candidates.
L. Huang (2004)
Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract.
D. Hörter (2001)
Pharmaceutical applications of solid dispersion systems.
W. Chiou (1971)
Estimating drug solubility in the gastrointestinal tract.
J. Dressman (2007)
Mucoadhesive amorphous solid dispersions for sustained release of poorly water soluble drugs
Justin S. Lafountaine (2017)
Effect of amorphization method on telmisartan solubility and the tableting process.
P. Lepek (2013)
Effects of Temperature and Solvent on the Solid-State Transformations of Pranlukast During Mechanical Milling.
Xinnuo Xiong (2017)
Solid dispersions of efonidipine hydrochloride ethanolate with improved physicochemical and pharmacokinetic properties prepared with microwave treatment.
M. Otsuka (2016)
Improving drug solubility for oral delivery using solid dispersions.
C. Leuner (2000)