24. February 2018

To investigate the nature of drug-excipient interactions between indomethacin (IMC) and methacrylate copolymer Eudragit® E (EE) in the amorphous state, and evaluate the effects on formulation and stability of these amorphous systems. Methods Amorphous solid dispersions containing IMC and EE were spray dried with drug loadings from 20% to 90%. PXRD was used to confirm the amorphous nature of the dispersions, and DSC was used to measure glass transition temperatures (Tg). 13C and 15N solid-state...

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...

21. December 2016

Abstract Synergetic role of polymer blending on dissolution of amorphous solid dispersion was investigated. Dissolution rates of hypromellose (HPMC) and methacrylic acid copolymer (EUD) from the HPMC/EUD spray-dried sample (SPD) were improved compared to those of each single polymer SPD. Differential scanning calorimetry measurements revealed that the structural change in HPMC following heating was inhibited by co-spray-drying with EUD, suggesting an intermolecular interaction between the...

15. August 2016

Abstract The saturation solubility of PVP:PZQ physical mixtures (PMs) and solid dispersions (SDs) prepared from ethanol (E/E) or ethanol/water (E/W) by the solvent evaporation method at 1:1, 2:1 and 3:1 ratio (w/w) was determined. The presence of PVP improves the solubility of PZQ (0.31 ± 0.01 mg/mL). A maximum of 1.29 ± 0.03 mg/mL of PZQ in solution was achieved for the 3:1 SD (E/E). The amount of PZQ in solution depends on the amount of polymer and on the preparation method. Solid-state NMR...

27. July 2016

Granules with release-sustaining properties were developed by twin screw hot melt granulation (HMG) using a combination of stearic acid (SA) and high molecular weight polyethylene oxide (PEO) as matrix for a highly water soluble model drug, metoprolol tartrate (MPT). Earlier studies demonstrated that mixing molten SA and PEO resulted in hydrogen bond formation between hydroxyl groups of fatty acid molecules and ether groups in PEO chains. These molecular interactions might be beneficial in...

20. June 2016

Abstract Since the discovery about 30 years ago (2-hydroxypropyl) beta-cyclodextrin, a highly soluble derivative of beta-cyclodextrin, has become an approved excipient of drug formulations included both in the United States and European Pharmacopoeias. It is recommended to use as solubilizer and stabilizer for oral and parenteral formulations. Recently, its pharmacological activity has been recognized in various diseases. The increasing applications require a closer look to the...

22. January 2016

Excipients used in the solid drug formulations differ in their NMR relaxation and 13C cross-polarization (CP) kinetics parameters.Therefore, experimental parameters like contact time of crosspolarizationand repetition time have a major impact on the registeredsolid state NMR spectra and in consequence on the results of the NMRanalysis. In this work the CP kinetics and relaxation of the most common pharmaceutical excipients: anhydrous α-lactose, α-lactose monohydrate, mannitol, sucrose,...

02. March 2015

Mol. Pharmaceutics, 2015, 12 (3), pp 857–866 DOI: 10.1021/mp500692a Publication Date (Web): January 13, 2015 Copyright © 2015 American Chemical Society *E-mail: lubach.joseph@gene.com This study investigated the presence of specific drug–excipient interactions in amorphous solid dispersions of lapatinib (LB) and four commonly used pharmaceutical polymers, including Soluplus, polyvinylpyrrolidone vinyl acetate (PVPVA), hydroxypropylmethylcellulose acetate succinate (HPMCAS), and...

15. January 2015

Yang Song , Xinghao Yang , Xin Chen , Haichen Nie , Stephen Byrn , and Joseph W. Lubach Mol. Pharmaceutics, Just Accepted ManuscriptDOI: 10.1021/mp500692aPublication Date (Web): January 13, 2015Copyright © 2015 American Chemical Society http://pubs.acs.org/doi/abs/10.1021/mp500692a