1. Priprava i karakterizacija čvrstih disperzija etorikoksiba s polietilenglikolom 4000 i polivinilpirolidonom K30
- Author
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BHANUBHAI N. SUHAGIA, HARESH M. PATEL, SHAILESH A. SHAH, ISHWARSINH RATHOD, and VIJAY K. PARMAR
- Subjects
etoricoxib ,solid dispersions ,dissolution ,polyethylene glycol ,polyvinylpyrrolidone ,factorial design ,technology, industry, and agriculture ,etorikoksib ,čvrsta disperzija ,oslobađanje ,polietilenglikol ,polivinilpirolidon ,faktorijalni dizajn - Abstract
The objective of the present investigation was to study the influence of polyethylene glycol 4000 (PEG) and polyvinylpyrrolidone K30 (PVP) on in vitro dissolution of etoricoxib from solid dispersions. The preliminary studies were carried out using physical mixture of drug and carriers. The solid dispersions were prepared using the solvent evaporation method. A 32 factorial design was adopted in the solvent evaporation method using the concentration of PEG and PVP as independent variables. Full and reduced models were evolved for dependant variables, such as the percentage of drug release in 10 min (Q10), percentage of drug release in 30 min (Q30), percentage of drug release in 45 min (Q45) and percent dissolution efficiency (DE). The reduced models were validated using two check points. Q10 > 65%, Q30 > 75%, Q45 > 85% and DE > 80% were used as constraints for the selection of an optimized batch. Contour plots are presented for the selected dependant variables. PEG was found to be more effective in increasing the drug dissolution compared to PVP. Wettability study was carried out for pure drug and optimized batch. FT-IR spectroscopy, microscopic study, differential scanning calorimetry and X-ray diffraction study were carried out in order to characterize drug in the solid dispersions. Improved dissolution was attributed to decreased crystallinity of the drug, improved wetting and solubilizing effects of carriers such as PEG and PVP from the solid dispersion of etoricoxib. In conclusion, dissolution of etoricoxib can be modulated using appropriate levels of hydrophilic carriers., U radu je proučavan utjecaj polietilenglikola 4000 (PEG) i polivinilpirolidona K30 (PVP) na in vitro oslobađanje etorikoksiba iz čvrstih disperzija. Preliminarni pokusi provedeni su sa smjesom ljekovite tvari i polimernih nosača. Čvrste disperzije pripravljene su metodom uparavanja otapala. Za ovu metodu razvijen je 32 faktorijalni dizajn koristeći koncentraciju PEG i PVP kao nezavisne varijable. Za zavisne varijable razvijeni su potpuni i reducirani modeli, kao što su postotak oslobođene ljekovite tvari u 10 (Q10), 30 (Q30) ili 45 minuta (Q45) i postotak učinkovitosti oslobađanja (DE). Reducirani modeli su validirani pomoću dviju kontrolnih točaka. Q10 > 65%, Q30 > 80%, Q45 > 85% i DE > 80% su upotrebljeni kao ograničenja za izbor optimirane serije. Prikazane su konturne linije za pojedine zavisne varijable. Oslobađanje lijeka bilo je učinkovitije iz pripravaka s PEG-om. Vlaženje je proučavano za čistu ljekovitu supstanciju i omptimiranu seriju. Za karakterizaciju ljekovite tvari u čvrstim disperzijama korištene su FT-IR spektroskopija, mikroskopske studije, diferencijalna pretražna kalorimetrija i difrakcija rentgenskim zrakama. Povećano oslobađanje posljedica je smanjene kristaliničnosti ljekovite tvari, pojačanog vlaženja i solubilizacijskog učinka polimernih nosača u disperzijama. Može se zaključiti da se oslobađanje etorikoksiba može modulirati promjenom količine hidrofilnih nosača.
- Published
- 2006