1. Effect of drug content and agglomerate size on tabletability and drug release characteristics of bromhexine hydrochloride-talc agglomerates prepared by crystallo-co-agglomeration
- Author
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NAMDEO JADHAV, ATMARAM PAWAR, and ANANT PARADKAR
- Subjects
crystallo-co-agglomeration ,agglomerate size ,drug content ,compression ,extended release ,kristalokoaglomeracija ,veličina aglomerata ,sadržaj ljekovite tvari ,kompresija ,produljeno oslobađanje - Abstract
The objective of the investigation was to study the effect of bromhexine hydrochloride (BXH) content and agglomerate size on mechanical, compressional and drug release properties of agglomerates prepared by crystallo-co-agglomeration (CCA). Studies on optimized batches of agglomerates (BXT1 and BXT2) prepared by CCA have showed adequate sphericity and strength required for efficient tabletting. Trend of strength reduction with a decrease in the size of agglomerates was noted for both batches, irrespective of drug loading. However, an increase in mean yield pressure (14.189 to 19.481) with an increase in size was observed for BXT2 having BXH-talc (1:15.7). Surprisingly, improvement in tensile strength was demonstrated by compacts prepared from BXT2, due to high BXH load, whereas BXT1, having a low amount of BXH (BXH-talc, 1:24), showed low tensile strength. Consequently, increased tensile strength was reflected in extended drug release from BXT2 compacts (Higuchi model, R2 = 0.9506 to 0.9981). Thus, it can be concluded that interparticulate bridges formed by BXH and agglomerate size affect their mechanical, compressional and drug release properties., Cilj rada bio je praćenje utjecaja sadržaja bromheksidin hidroklorida (BXH) i veličine aglomerata na mehanička svojstva, kompresivnost i oslobađanje ljekovite tvari iz aglomerata pripravljenih kristalokoaglomeracijom (CCA). Optimizirani pripravci aglomerata (BXT1 i BXT2) pripravljeni CCA metodom pokazuju adekvatnu sferičnost i čvrstoću potrebnu za učinkovito tabletiranje. U oba pripravka se smanjenjem veličine aglomerata smanjivala i čvrstoća, neovisno o količini ljekovite tvari. Međutim, povećanje prosječnog tlaka s povećanjem veličine čestica primijećeno je u pripravku BXT2 s omjerom BXH-talk 1:15,7. Iznenađuje da su kompakti pripravljeni iz BXT2, s visokim sadržajem BXH, imali veću vlačnu čvrstoću, dok su BXT1 s niskim sadržajem BXH (BXH-talk, 1:24) imali manju čvrstoću. Veća vlačna čvrstoća imala je za posljedicu produljeno oslobađanje ljekovite tvari iz BXT2 (Higuchijev model, R2 = 0,9506 do 0,9981). Može se zaključiti da mostovi među česticama BXH i veličina aglomerata utječu na njihova mehanička i kompresivna svojstva te na oslobađanje ljekovite tvari.
- Published
- 2010