Supercritical CO2 utilization in preparation of poorly soluble drugs solid dispersions
Апстракт
Formulation of solid dispersions is one of the most feasible strategies for overcoming the poor
drugs’ solubility – one of the major issues affecting drug bioavailability and therapeutic outcomes.
Since traditional methods used for preparation of solid dispersions often require usage of organic
solvents, it is of great importance to seek for more environment-friendly methods. It has been
demonstrated that supercritical (sc) CO2 may be effectively utilized for dispersion of drugs into the
suitable carrier (polymer), thus obtaining solid dispersions with the improved drug dissolution rate.
The aim of the presented study was to investigate the potential of scCO2 for preparation of poorly
soluble antihypertensive drugs (carvedilol and valsartan) solid dispersions in the conventional
pharmaceutical polymers (polyvinilypyrolidone-PVP and hypromellose-HPMC). Prepared solid
dispersions were characterized by scanning electron microscopy, differential scanning calorimetry
and Fourier-t...ransform infrared spectroscopy; their porosity and density were determined and drug
dissolution rate was assessed and compared to the results obtained from solid dispersions prepared
by the traditional solvent casting method. Selected samples were tested for their tableting properties
as well. It has been demonstrated that scCO2 may be successfully applied for preparation of
carvedilol or valsartan solid dispersions with the improved drug dissolution rate. Further
characterization revealed the nature of interactions between the drugs and selected polymers. Due
to the low density (and high porosity), some of the prepared solid dispersions may be used for
further development of the floating dosage forms. It has also been demonstrated that some of the
prepared dispersions have excellent compressibility and compactibility, which is of great
importance for further development of solid dosage forms. The obtained results provide framework
for further development of environment-friendly methods in pharmaceutical development and
production.
Извор:
Twenty-first Annual Conference YUCOMAT 2019 & Eleventh World Round Table Conference on Sintering WRTCS 2019, September 2-6, 2019, Herceg Novi, Montenegro, 2019, 71-71Издавач:
- Materials Research Society of Serbia
- International Institute for the Science of Sintering
Финансирање / пројекти:
- Развој производа и технологија које обезбеђују жељено ослобађање лековитих супстанци из чврстих фармацеутских облика (RS-MESTD-Technological Development (TD or TR)-34007)
- Функционални физиолошки активни биљни материјали са додатом вредношћу за примену у фармацеутској и прехрамбеној индустрији (RS-MESTD-Integrated and Interdisciplinary Research (IIR or III)-45017)
Институција/група
PharmacyTY - CONF AU - Đuriš, Jelena AU - Milovanović, Stoja AU - Medarević, Đorđe AU - Dobričić, Vladimir AU - Ibrić, Svetlana PY - 2019 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/5483 AB - Formulation of solid dispersions is one of the most feasible strategies for overcoming the poor drugs’ solubility – one of the major issues affecting drug bioavailability and therapeutic outcomes. Since traditional methods used for preparation of solid dispersions often require usage of organic solvents, it is of great importance to seek for more environment-friendly methods. It has been demonstrated that supercritical (sc) CO2 may be effectively utilized for dispersion of drugs into the suitable carrier (polymer), thus obtaining solid dispersions with the improved drug dissolution rate. The aim of the presented study was to investigate the potential of scCO2 for preparation of poorly soluble antihypertensive drugs (carvedilol and valsartan) solid dispersions in the conventional pharmaceutical polymers (polyvinilypyrolidone-PVP and hypromellose-HPMC). Prepared solid dispersions were characterized by scanning electron microscopy, differential scanning calorimetry and Fourier-transform infrared spectroscopy; their porosity and density were determined and drug dissolution rate was assessed and compared to the results obtained from solid dispersions prepared by the traditional solvent casting method. Selected samples were tested for their tableting properties as well. It has been demonstrated that scCO2 may be successfully applied for preparation of carvedilol or valsartan solid dispersions with the improved drug dissolution rate. Further characterization revealed the nature of interactions between the drugs and selected polymers. Due to the low density (and high porosity), some of the prepared solid dispersions may be used for further development of the floating dosage forms. It has also been demonstrated that some of the prepared dispersions have excellent compressibility and compactibility, which is of great importance for further development of solid dosage forms. The obtained results provide framework for further development of environment-friendly methods in pharmaceutical development and production. PB - Materials Research Society of Serbia PB - International Institute for the Science of Sintering C3 - Twenty-first Annual Conference YUCOMAT 2019 & Eleventh World Round Table Conference on Sintering WRTCS 2019, September 2-6, 2019, Herceg Novi, Montenegro T1 - Supercritical CO2 utilization in preparation of poorly soluble drugs solid dispersions SP - 71 EP - 71 UR - https://hdl.handle.net/21.15107/rcub_farfar_5483 ER -
@conference{ author = "Đuriš, Jelena and Milovanović, Stoja and Medarević, Đorđe and Dobričić, Vladimir and Ibrić, Svetlana", year = "2019", abstract = "Formulation of solid dispersions is one of the most feasible strategies for overcoming the poor drugs’ solubility – one of the major issues affecting drug bioavailability and therapeutic outcomes. Since traditional methods used for preparation of solid dispersions often require usage of organic solvents, it is of great importance to seek for more environment-friendly methods. It has been demonstrated that supercritical (sc) CO2 may be effectively utilized for dispersion of drugs into the suitable carrier (polymer), thus obtaining solid dispersions with the improved drug dissolution rate. The aim of the presented study was to investigate the potential of scCO2 for preparation of poorly soluble antihypertensive drugs (carvedilol and valsartan) solid dispersions in the conventional pharmaceutical polymers (polyvinilypyrolidone-PVP and hypromellose-HPMC). Prepared solid dispersions were characterized by scanning electron microscopy, differential scanning calorimetry and Fourier-transform infrared spectroscopy; their porosity and density were determined and drug dissolution rate was assessed and compared to the results obtained from solid dispersions prepared by the traditional solvent casting method. Selected samples were tested for their tableting properties as well. It has been demonstrated that scCO2 may be successfully applied for preparation of carvedilol or valsartan solid dispersions with the improved drug dissolution rate. Further characterization revealed the nature of interactions between the drugs and selected polymers. Due to the low density (and high porosity), some of the prepared solid dispersions may be used for further development of the floating dosage forms. It has also been demonstrated that some of the prepared dispersions have excellent compressibility and compactibility, which is of great importance for further development of solid dosage forms. The obtained results provide framework for further development of environment-friendly methods in pharmaceutical development and production.", publisher = "Materials Research Society of Serbia, International Institute for the Science of Sintering", journal = "Twenty-first Annual Conference YUCOMAT 2019 & Eleventh World Round Table Conference on Sintering WRTCS 2019, September 2-6, 2019, Herceg Novi, Montenegro", title = "Supercritical CO2 utilization in preparation of poorly soluble drugs solid dispersions", pages = "71-71", url = "https://hdl.handle.net/21.15107/rcub_farfar_5483" }
Đuriš, J., Milovanović, S., Medarević, Đ., Dobričić, V.,& Ibrić, S.. (2019). Supercritical CO2 utilization in preparation of poorly soluble drugs solid dispersions. in Twenty-first Annual Conference YUCOMAT 2019 & Eleventh World Round Table Conference on Sintering WRTCS 2019, September 2-6, 2019, Herceg Novi, Montenegro Materials Research Society of Serbia., 71-71. https://hdl.handle.net/21.15107/rcub_farfar_5483
Đuriš J, Milovanović S, Medarević Đ, Dobričić V, Ibrić S. Supercritical CO2 utilization in preparation of poorly soluble drugs solid dispersions. in Twenty-first Annual Conference YUCOMAT 2019 & Eleventh World Round Table Conference on Sintering WRTCS 2019, September 2-6, 2019, Herceg Novi, Montenegro. 2019;:71-71. https://hdl.handle.net/21.15107/rcub_farfar_5483 .
Đuriš, Jelena, Milovanović, Stoja, Medarević, Đorđe, Dobričić, Vladimir, Ibrić, Svetlana, "Supercritical CO2 utilization in preparation of poorly soluble drugs solid dispersions" in Twenty-first Annual Conference YUCOMAT 2019 & Eleventh World Round Table Conference on Sintering WRTCS 2019, September 2-6, 2019, Herceg Novi, Montenegro (2019):71-71, https://hdl.handle.net/21.15107/rcub_farfar_5483 .