Towards improved solubility of poorly water-soluble drugs: cryogenic co-grinding of piroxicam with carrier polymers
| Autor: | Jouko Yliruusi, Sirpa Vuorinen, Jaan Aruväli, Peep Veski, Karin Kogermann, Maija Hakola, Jyrki Heinämäki, Anna Penkina, Kristian Semjonov, Timo Repo |
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| Rok vydání: | 2015 |
| Předmět: |
Materials science
Polymers Scanning electron microscope Chemistry Pharmaceutical Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy law.invention Piroxicam 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Differential scanning calorimetry X-Ray Diffraction law Spectroscopy Fourier Transform Infrared Drug Discovery Polymer chemistry medicine Fourier transform infrared spectroscopy Crystallization Cellulose Dissolution Cryopreservation Pharmacology chemistry.chemical_classification Drug Carriers Polyvinylpyrrolidone Organic Chemistry Water Polymer 021001 nanoscience & nanotechnology Solubility chemistry Chemical engineering 0210 nano-technology medicine.drug |
| Zdroj: | Drug Development and Industrial Pharmacy. 42:378-388 |
| ISSN: | 1520-5762 0363-9045 |
| DOI: | 10.3109/03639045.2015.1054400 |
| Popis: | Amorphous solid dispersions (SDs) open up exciting opportunities in formulating poorly water-soluble active pharmaceutical ingredients (APIs). In the present study, novel catalytic pretreated softwood cellulose (CPSC) and polyvinylpyrrolidone (PVP) were investigated as carrier polymers for preparing and stabilizing cryogenic co-ground SDs of poorly water-soluble piroxicam (PRX). CPSC was isolated from pine wood (Pinus sylvestris). Raman and Fourier transform infrared (FTIR) spectroscopy, X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) were used for characterizing the solid-state changes and drug-polymer interactions. High-resolution scanning electron microscope (SEM) was used to analyze the particle size and surface morphology of starting materials and final cryogenic co-ground SDs. In addition, the molecular aspects of drug-polymer interactions and stabilization mechanisms are presented. The results showed that the carrier polymer influenced both the degree of amorphization of PRX and stabilization against crystallization. The cryogenic co-ground SDs prepared from PVP showed an enhanced dissolution rate of PRX, while the corresponding SDs prepared from CPSC exhibited a clear sustained release behavior. In conclusion, cryogenic co-grinding provides a versatile method for preparing amorphous SDs of poorly water-soluble APIs. The solid-state stability and dissolution behavior of such co-ground SDs are to a great extent dependent on the carrier polymer used. |
| Databáze: | OpenAIRE |
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