33 KB288 KB30 KB199820252011Burjak, MatejaDreu, RokGašperlin, MirjanaHomar, MihaKerč, JanezSrčič, Stankoštevilka:2letnik:58str. 318-325ISSN:1318-0207COBISSID:3052657URN:URN:NBN:SI:doc-EHBS2ENZenSlovenian Chemical SocietySlovensko kemijsko društvoActa chimica slovenicafarmacevtske oblikeklaritromicinpolietilen glikolsferični mikrodelcisproščanje učinkovinStudy of immediate release spherical microparticles containing clarithromycin using a hot-melt fluid bed technique|The aim of the study was to evaluate a hot-melt technique for preparation of immediate release spherical microparticles containing clarithromycin with acceptable characteristics and process yield. A modified fluid bed apparatus with rotor insert was used to prepare spherical microparticles in the size range of 125-355 im. Poloxamer 188, PEG-32 glyceryl laurate (Gelucire 44/14) and a mixture of polyethylene glycol (PEG) 4000 with PEG 400 were used as meltable binders. Key process parameters were identified and optimized and their influence on process yield and microparticles characteristics was determined. Microparticles with poloxamer 188 and PEG exhibited relatively good mechanical properties. Process yield was around 70% and 60% in the case of PEG and poloxamer 188 respectively. Microparticles prepared with PEG-32 glyceryl laurate exhibited poor mechanical properties and process yield compared to other microparticles. The process was shown to be limited by the bed temperature, exhibiting the best process stability with poloxamer 188 followed by PEG and PEG-32 glyceryl laurate. Dissolution rate and equilibrium concentration of clarithromycin released from prepared microparticles was improved compared to similar particles prepared by wet granulationNamen raziskovalnega dela je bil razviti postopek na osnovi talin za izdelavo sferičnih mikrodelcev klaritromicina s takojšnjim sproščanjem. Za izdelavo mikrodelcev v velikostnem razredu 125-355 mikrom smo priredili aparaturo na principu zvrtinčenih plasti z rotorskim nastavkom. Kot veziva smo preskusili PEG-32 gliceril laurat (Gelucire 44/14r), poloksamer 188 in zmes dveh polietilenglikolov (PEG). Določili smo ključne procesne spremenljivke procesa in jih optimirali v smislu izkoristka procesa in mehanskih lastnosti mikrodelcev. Mikrodelci, pripravljeni s poloksamerom 188 in PEG so v splošnem izkazovali dobre mehanske lastnosti, izkoristek procesa pa je bil okoli 70 % vprimeru PEG in okoli 60 % v primeru poloksamera 188. Mikrodelci izdelani s PEG-32 gliceril lauratom so izkazovali slab{e mehanske lastnosti in nižji izkoristek procesa v primerjavi z mikrodelci izdelanimi z ostalima vezivoma. Stabilnost procesa je bila odvisna predvsem od temperature produkta v komori in je bila najboljša v primeru poloksamera 188 in najslabša v primeru PEG-32 gliceril laurata. Hitrost raztapljanja in nasičena topnost klaritromicina, sproščenega iz mikrodelcev izdelanih s talinami, je bila večja v primerjavi z mikrodelci izdelanimi s klasično mokro granulacijoTEXTznanstveno časopisjejournalsSlovenian National E-content AggregatorNational and University Library of SloveniaSlovensko kemijsko društvo