A facile way to continuously coat drug crystals with a polymer is needed in controlled drug release. Conventional polymer coating methods have disadvantages: high energy consumption, low productivity, batch processing. A novel method for continuous polymer coating of drug crystals based on solid hollow fiber cooling crystallization (SHFCC) is introduced here. The drug acting as the host particle and the polymer for coating are Griseofulvin (GF) and Eudragit RL100, respectively. The polymer's cloud point temperature in its acetone solution was determined by UV spectrophotometry. An acetone solution of the polymer containing the drug in solution as well as undissolved drug crystals in suspension were pumped through the tube side of the SHFCC device; a cold liquid was circulated in the shell side to rapidly cool down the feed solution-suspension in the hollow-fiber lumen. The polymer precipitated from the solution and coated the suspended crystals due to rapid temperature reduction and heterogeneous nucleation; crystals formed from the solution were also coated by the polymer. Characterizations by scanning electron microscopy, thermogravimetric analysis, laser diffraction spectroscopy, X-ray diffraction, Raman spectroscopy, and dissolution tests show that a uniformly coated, free-flowing drug/product can be obtained under appropriate operating conditions without losing the drug's pharmaceutical properties and controlled release characteristics.
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http://dx.doi.org/10.1016/j.ijpharm.2016.01.008 | DOI Listing |
Acta Pharm Sin B
December 2024
State Key Laboratory of Cellular Stress Biology and Fujian Provincial Key Laboratory of Innovative Drug Target Research, School of Pharmaceutical Science, Xiamen University, Xiamen 361102, China.
The orphan nuclear receptor Nur77 is emerging as an attractive target for cancer therapy, and activating Nur77's non-genotypic anticancer function has demonstrated strong therapeutic potential. However, few Nur77 site B ligands have been identified as excellent anticancer compounds. There are no co-crystal structures of effective anticancer agents at Nur77 site B, which greatly limits the development of novel Nur77 site B ligands.
View Article and Find Full Text PDFCurr Org Synth
January 2025
Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Hyderabad, Telangana, 502329, India.
Introduction: The origin, synthesis, characterization and docking studies of (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((R,1E,4E)-3-hydroxy-5-phenylpenta-1,4-dien-1-yl)cyclopentyl)-N-ethylhept-5-enamide, an impurity generated in the preparation of an anti-glaucoma agent-Bimatoprost has been described.
Methods: This impurity was controlled by employing 30% Pd/C, and the impurity level was brought to the permissible level, i.e.
ACS Appl Bio Mater
January 2025
Department of Chemistry, National Institute of Technology, Rourkela, Odisha 769008, India.
The idea of coordinating biologically active ligand systems to metal centers to exploit their synergistic effects has gained momentum. Therefore, in this report, three Ru complexes - of morpholine-derived thiosemicarbazone ligands have been prepared and characterized by spectroscopy and HRMS along with the structure of through a single-crystal X-ray diffraction study. The solution stability of - was tested using conventional techniques such as UV-vis and HRMS.
View Article and Find Full Text PDFChemMedChem
January 2025
Crystals First GmbH, -, GERMANY.
Protonation states serve as an essential molecular recognition motif for biological processes. Their correct consideration is key to successful drug design campaigns, since chemoinformatic tools usually deal with default protonation states of ligands and proteins and miss atypical protonation states. The protonation pattern for the Endothiapepsin/PepstatinA (EP/pepA) complex is investigated using different dry lab and wet lab techniques.
View Article and Find Full Text PDFArch Biochem Biophys
January 2025
Department of Biotechnology, Maharaja Sriram Chandra Bhanjadeo University, (Erstwhile: North Orissa University), Baripada, Odisha 757003, India. Electronic address:
Our previous study revealed that lipid flip-flop inducing phytochemicals from Gymnema sylvestre increase membrane permeability of antimicrobials in S. aureus. However, their lipid flipping and membrane permeabilizing effect on methicillin resistant S.
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