04. October 2018
Praziquantel is an antiparasitic drug used for decades. Currently, the praziquantel commercial preparation is a racemic mixture, inwhich only the levo-enantiomer possesses anthelmintic activity. The knowledge of its properties in the solid state and other chemical-physical properties is necessary for improving its efficacy andapplications. Drug solid dispersions were prepared with calcium carbonate at 1:5 drug to excipient weight ratio by solventevaporation method. Then, the modification of the...
18. August 2018
The development of oral dosage forms for poorly water-soluble active pharmaceutical ingredients (APIs) is a persistent challenge. A range of methods has been explored to address this issue, and amorphous solid dispersions (ASDs) have received increasing attention. ASDs are typically prepared by starting with a liquid precursor (a solution or melt) and applying energy for solidification. Many techniques can be used, with the emergence of electrospinning as a potent option in recent years. This...
16. April 2018
Surfactants are common stabilizers, often added to biopharmaceuticals formulations, but the mechanisms at the basis of their activity are unclear. The aim of this work is to provide insight into the molecular factors underlying surfactant effectiveness as protectants. Methods Molecular Dynamics simulations of human growth hormone (hGH) in the presence of Tween 20 were performed. The effect of Tween 20 was compared with the activity of commonly used protectants, such as the disaccharides....
26. March 2017
Abstract A quantitative structure-property relationship (QSPR) between protein stability and the physicochemical properties of excipients was investigated to enable a more rational choice of stabilizing excipients than prior knowledge. The thermal transition temperature and aggregation time were determined for lysozyme in combination with 13 different amino acids using high throughput fluorescence spectroscopy and kinetic static light scattering measurements. On the theoretical side, around 200...
24. March 2017
ABSTRACT Introduction: For almost two decades there has been intense debate about whether the amorphous solid state form could resolve the solubility problems and subsequent bioavailability issues of many small molecule drugs. Since the amorphous form is a high energy and unstable state of solid matter, any material in that form requires stabilization. Areas covered: This review examines the technologies being exploited to stabilize the amorphous state in co-amorphous formulations. The review...
20. March 2017
Abstract In recent years, the demand and interest for functionalized polymers have increased for drug delivery purposes. Because of the increased interest, methods that can be used to predict physical and chemical properties of polymers prior to synthesis would be of high value for the design and development of novel polymer structures. Through use of molecular descriptors and Principal Component Analysis, this study explores the possibilities of using in silico methods for polymer design and...
10. January 2017
Abstract The purpose of this study was to determine the drug-polymer miscibility of GENE-A, a Genentech molecule, and Hydroxypropyl methylcellulose-acetate succinate (HPMC-AS), a polymer, using computational and experimental approaches. The Flory-Huggins interaction parameter,χ, was obtained by calculating the solubility parameters for GENE-A and HPMC-AS over the temperature range of 25–100 °C to obtain the free energy of mixing at different drug loadings (0-100%) using the Materials Studio...
23. December 2016
Abstract This research study aimed to develop a new strategy for using a polymer blend in solid dispersion (SD) for dissolution enhancement of poorly water-soluble drugs. SDs with different blends of hydrophilic-hydrophobic polymers (zein/hydroxypropyl methylcellulose – zein/HPMC) were prepared using spray drying to modulate the drug crystal and polymer-drug interactions in SDs. Physicochemical characterizations, including power X-ray diffraction and Fourier transform infrared spectroscopy,...
14. September 2016
Abstract This research study aimed to develop a new strategy for using a polymer blend in solid dispersion (SD) for dissolution enhancement of poorly water-soluble drugs. SDs with different blends of hydrophilic-hydrophobic polymers (zein/hydroxypropyl methylcellulose – zein/HPMC) were prepared using spray drying to modulate the drug crystal and polymer-drug interactions in SDs. Physicochemical characterizations, including power X-ray diffraction and Fourier transform infrared spectroscopy,...
22. August 2016
Abstract During the formulation of solid dosage forms coating, plasticizers are added to the film forming polymer to improve the mechanical properties of the coating shell of the drug product. For the coating formulation to be successful and in order to produce flexible continuous film, the plasticizer should be compatible with the film forming polymer (i.e. high plasticizer-polymer miscibility in solid dispersion) (McGinity and Felton, 2008). This paper proposes and compares different...