Effects of polymer and surfactant on the dissolution and transformation profiles of cocrystals in aqueous media

  title={Effects of polymer and surfactant on the dissolution and transformation profiles of cocrystals in aqueous media},
  author={Amjad Alhalaweh and Hassan Refat H. Ali and Sitaram Velaga},
  journal={Crystal Growth \& Design},
Capturing solubility advantages of cocrystals is of great interest, and thus to understand the mechanism by which different excipients could maintain the supersaturation generated by cocrystals at the course of absorption in aqueous media is essential. To achieve this aim, the impact of different excipients on dissolution behavior of indomethacin–saccharin (IND–SAC) were monitored by measuring the concentrations of cocrystal components in the absence and presence of various concentration of… 
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Influence of Drug-Polymer Interactions on Dissolution of Thermodynamically Highly Unstable Cocrystal.
The study highlighted that, despite no influence of the polymers on the cocrystal SMPT, dissolution enhancement was achieved, attributed to small-sized drug crystals generated from the supersaturation-mediated crystallization and improved solvation due to drug-polymer interactions.
Cocrystal solubility advantage diagrams as a means to control dissolution, drug supersaturation and precipitation.
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Dissolution Advantage of Nitazoxanide Cocrystals in the Presence of Cellulosic Polymers
The study demonstrates that the incorporation of an appropriate excipient in adequate concentration can be a key factor for inducing and maintaining the solubilization of poorly soluble drugs starting from co-crystallized solid forms.
Formation of Indomethacin-Saccharin Cocrystals during Wet Granulation: Role of Polymeric Excipients.
The objectives were to evaluate the influence of polymers on cocrystal formation kinetics during wet granulation, and mechanistically understand the role ofPolyvinylpyrrolidone (PVP), hydroxypropyl cellulose (HPC), and polyethylene oxide (PEO) were chosen to investigate the Influence of soluble polymers.
Role of polymers in solution and tablet-based carbamazepine cocrystal formulations
The aim of this study was to evaluate the influence of three chemically diverse polymers, namely hydroxypropylmethylcellulose acetate succinate (HPMCAS), polyvinylpyrrolidone (PVP) and polyethylene


Solubility Behavior and Solution Chemistry of Indomethacin Cocrystals in Organic Solvents
The main objective of this study was to investigate the solubility behavior and solution chemistry of indomethacin–saccharin (IND–SAC) cocrystals in organic media. We also evaluated previously
Dissolution Improvement and the Mechanism of the Improvement from Cocrystallization of Poorly Water-soluble Compounds
Cocrystallizations of exemestane and megestrol acetate from cocrystallization using various particle sizes improved initial dissolution rates compared to the respective original crystals.
Phase solubility diagrams of cocrystals are explained by solubility product and solution complexation
The purpose of this work was to develop a mathematical model that describes the solubility of cocrystals by taking into consideration the equilibria between cocrystal, cocrystal components, and
Dependence of cocrystal formation and thermodynamic stability on moisture sorption by amorphous polymer
The purpose of this study was to determine the influence of water vapor sorbed by and dissolved in an amorphous polymer on the formation and thermodynamic stability of cocrystals that are
Influence of different polymers on the crystallization tendency of molecularly dispersed amorphous felodipine.
It was found that each polymer was able to significantly decrease the nucleation rate of amorphous felodipine even at low concentrations (3-25% w/w), and hydrogen bonding interactions were formed between felodIPine and each of the polymers.
Stability and Solubility of Celecoxib-PVP Amorphous Dispersions: A Molecular Perspective
The solubility enhancement and enthalpy relaxation studies with respect to PVP concentration helped in a better prediction of role of carrier and optimization of concentration in the use of solid dispersions or amorphous systems.
Improving the Chemical Stability of Amorphous Solid Dispersion with Cocrystal Technique by Hot Melt Extrusion
By in-situ forming cocrystal, chemically stable amorphous solid dispersions were prepared by MM and HME at a depressed processing temperature, which provides an attractive opportunity for HME of heat-sensitive drugs.
Indomethacin–Saccharin Cocrystal: Design, Synthesis and Preliminary Pharmaceutical Characterization
Physical characterization showed that the IND–SAC cocrystal is unique vis-à-vis thermal, spectroscopic and X-ray diffraction properties, and were associated with a significantly faster dissolution rate than indomethacin (γ-form).
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Pharmaceutical cocrystals are of great interest because of their potential to enhance solubility and bioavailability of poorly water-soluble drugs. Cocrystal development is however limited by their
Formulation of a danazol cocrystal with controlled supersaturation plays an essential role in improving bioavailability.
In the case of the danazol:vanillin cocystal, using a combination of cocrystal, solubilizer, and precipitation inhibitor in a designed supersaturating drug delivery system resulted in a dramatic improvement in the bioavailability.