Amorphization is widely used as an effective method of increasing the solubility of insoluble drugs. However, some amorphous drugs exhibit a much lower dissolution rate than their corresponding crystalline form due to their gelation. In this study, we reported the gels formed from amorphous acemetacin (ACM) for the first time. Gelation was promoted at conditions of lower pH, higher temperature and lower ionic strength. Solid-state characterizations suggested that ACM gels may be formed by recrystallization. This mechanism provides a new direction in facilitating the elimination of gelation for amorphous drugs. Moreover, it also provides the basis for the development of sustained-release formulations using the gelation properties.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9860709 | PMC |
| http://dx.doi.org/10.3390/pharmaceutics15010219 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Using the Radial Distribution Function to Analyze Atomic Force Microscopy Images of Colloidal Systems.
Int J Mol Sci
December 2024
Institute of Biomedical Chemistry, Pogodinskaya Str., 10, Moscow 119121, Russia.
Biomacromolecules generally exist and function in aqueous media. Is it possible to estimate the state and properties of molecules in an initial three-dimensional colloidal solution based on the structure properties of biomolecules adsorbed on the two-dimensional surface? Using atomic force microscopy to study nanosized objects requires their immobilization on a surface. Particles undergoing Brownian motion in a solution significantly reduce their velocity near the surface and become completely immobilized upon drying.
View Article and Find Full Text PDFNew Ionic Liquid Forms of Antituberculosis Drug Combinations for Optimized Stability and Dissolution.
AAPS PharmSciTech
January 2025
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Isoniazid (INH) and rifampicin (RIF) are the two main drugs used for the management of tuberculosis. They are often used as a fixed drug combination, but their delivery is challenged by suboptimal solubility and physical instability. This study explores the potential of active pharmaceutical ingredient-ionic liquids (API-ILs) to improve the physicochemical and pharmaceutical properties of INH and RIF.
View Article and Find Full Text PDFTwin Screw Melt Granulation of Simvastatin: Drug Solubility and Dissolution Rate Enhancement Using Polymer Blends.
Pharmaceutics
December 2024
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA.
This study evaluates the efficacy of twin screw melt granulation (TSMG), and hot-melt extrusion (HME) techniques in enhancing the solubility and dissolution of simvastatin (SIM), a poorly water-soluble drug with low bioavailability. Additionally, the study explores the impact of binary polymer blends on the drug's miscibility, solubility, and in vitro release profile. SIM was processed with various polymeric combinations at a 30% / drug load, and a 1:1 ratio of binary polymer blends, including Soluplus (SOP), Kollidon K12 (K12), Kollidon VA64 (KVA), and Kollicoat IR (KIR).
View Article and Find Full Text PDFDrug-Phospholipid Co-Amorphous Formulations: The Role of Preparation Methods and Phospholipid Selection.
Pharmaceutics
December 2024
Department of Pharmacy, Faculty of Health and Medical Science, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
: This study aims to broaden the knowledge on co-amorphous phospholipid systems (CAPSs) by exploring the formation of CAPSs with a broader range of poorly water-soluble drugs, celecoxib (CCX), furosemide (FUR), nilotinib (NIL), and ritonavir (RIT), combined with amphiphilic phospholipids (PLs), including soybean phosphatidylcholine (SPC), hydrogenated phosphatidylcholine (HPC), and mono-acyl phosphatidylcholine (MAPC). : The CAPSs were initially prepared at equimolar drug-to-phospholipid (PL) ratios by mechano-chemical activation-based, melt-based, and solvent-based preparation methods, i.e.
View Article and Find Full Text PDFEffect of Process Parameters on Nano-Microparticle Formation During Supercritical Antisolvent Process Using Mixed Solvent: Application for Enhanced Dissolution and Oral Bioavailability of Telmisartan Through Particle-Size Control Based on Experimental Design.
Pharmaceutics
November 2024
College of Pharmacy and Research Institute for Drug Development, Pusan National University, 63 Busandaehak-ro, Geumjeong-gu, Busan 46241, Republic of Korea.
This study investigates the impact of supercritical antisolvent (SAS) process parameters on the particle formation of telmisartan, a poorly water-soluble drug. A fractional factorial design was employed to examine the influence of the SAS process parameters, including solvent ratio, drug solution concentration, temperature, pressure, injection rate of drug solution, and CO₂ flow rate, on particle formation. Solid-state characterizations of the SAS process particles using XRD and FT-IR confirmed their amorphous nature.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!