The effect of polyvinyl pyrrolidone (PVP) K30 and/or L-arginine on etoricoxib-HPbetaCD complex was investigated. The phase solubility profiles were classified as A(L)-type, both in absence or presence of auxiliary substances used. The apparent stability constant (K(c)) of binary complex obtained at room temperature, 371.80 +/- 2.61 M(-1), was decreased with the addition of PVP and arginine indicating no benefit of addition of auxiliary substances to promote higher complexation efficiency. Therefore, solid etoricoxib-HPbetaCD binary systems were prepared and characterized by proton nuclear magnetic resonance spectroscopy (1HNMR), X-ray powder diffractometry, Fourier transformation-infrared spectroscopy, and dissolution studies. Among all binary systems, a lyophilized product showed superior performance in enhancing dissolution of etoricoxib.
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http://dx.doi.org/10.1080/03639040802220292 | DOI Listing |
Chem Pharm Bull (Tokyo)
December 2024
School of Traditional Chinese Medicines, Shenyang Pharmaceutical University.
Enteric-coated microcapsules can protect roxithromycin (ROX) from acid hydrolysis enhancing efficacy, solubility, and dissolution rate, representing a promising oral formulation for children and patients with swallowing difficulties. ROX-layered core particles were obtained with polyvinylpyrrolidone (PVP) K30 as the binder and Eudragit L30 D-55 as the coating material using the Wurster process in a fluidized bed processor. The enteric-coated microcapsules were characterized using powder X-ray diffraction, differential scanning calorimetry, and polarized optical microscopy.
View Article and Find Full Text PDFAAPS PharmSciTech
December 2024
Hebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, 067000, Hebei, China.
Glycyrrhetinic acid (GA) possesses various pharmacological effects, including anti-inflammatory, anti-tumor, and anti-viral properties. However, its clinical application is limited by poor solubility and low oral bioavailability. Polymers play a crucial role in pharmaceutical formulations, particularly as matrices in excipients to enhance the solubility, bioavailability, and stability of active pharmaceutical ingredients.
View Article and Find Full Text PDFMol Pharm
January 2025
State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Metastable polymorphs of active pharmaceutical ingredients can occasionally be used to enhance bioavailability or make processing more convenient. However, the thermodynamic instability of metastable polymorphs poses a severe threat to the quality and performance of the drug products. In this study, we used hot-stage microscopy and powder X-ray diffraction to quantitatively analyze the kinetics of the solid-solid phase transition of piracetam (PCM) polymorphs in the absence and presence of several polymeric excipients.
View Article and Find Full Text PDFInt J Pharm
January 2025
Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab 160062, India. Electronic address:
Dasatinib (DASA), a potent second-generation multitarget kinase inhibitor marketed as Sprycel® (Tablet), is limited by poor oral bioavailability (14-24 %) and dose-related gastrointestinal side effects. A supersaturable self-nanoemulsifying drug delivery system (su-SNEDDS) designed to enhance DASA's solubility, sustain supersaturation, and improve oral bioavailability. The su-SNEDDS formulation comprises DASA, an oil, surfactant, co-surfactant, and polyvinylpyrrolidone (PVP) K30 as a precipitation inhibitor (PI).
View Article and Find Full Text PDFEur J Pharm Biopharm
November 2024
Department of Pharmacognosy and Phytochemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia in Katowice, Jagiellonska 4 41-200, Sosnowiec, Poland. Electronic address:
This paper presents an innovative approach that utilizes self-synthesized homopolymers of polyvinylpyrrolidone (PVP) with different architectures as effective matrices for inhibiting the crystallization of naproxen (NAP). We have thoroughly investigated amorphous solid dispersions containing NAP and (i) self-synthesized linear PVP, (ii) self-synthesized three-armed star-shaped PVP, and (iii) self-synthesized linear PVP with a mass (M) corresponding to the length of one arm of the star polymer, as well as (iv) commercial linear PVP K30 as a reference. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and infrared spectroscopy (FTIR) studies, as well as molecular dynamics simulations were conducted to gain comprehensive insights into the thermal and structural properties, as well as intermolecular interactions in the NAP-PVP systems.
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