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V farmacevtski industriji pri izdelavi tablet, kot pomožne snovi pri direktnem stiskanju, pogosto uporabljamo različne poliole, različne oblike laktoze, škroba ter celuloze. Te pri tableti predstavljajo znaten delež, zato je, v povezavi z direktnim stiskanjem, poznavanje njihovih pretočnih lastnosti in stisljivosti, zelo pomembno. Vse te lastnosti vplivajo na ponovljivost stiskanja, enakomernost mase tablet in mehansko odpornost končnega produkta ter omogočajo optimizacijo procesa stiskanja. Naš namen v tej magistrski nalogi je bil preučevanje enajstih pogosto uporabljenih pomožnih snovi za direktno stiskanje v farmacevtski industriji. To so Vivapur® 200, Emcompress®, Neosorb® 300 DC, Pearlitol® 300 DC, Xylisorb® 100 DC, ksilitol, Tablettose® 70, FlowLac® 100, GalenIQTM 721, Starch 1500® in Pearlitol® 100 DC. Najprej smo preučevali pretočne lastnosti čistih pomožnih snovi in pomožnih snovi po dodatku veziva (Kollidon® VA 64) in antiadheziva (Mg stearat). Za njihovo vrednotenje smo uporabili metodo merjenja masnega pretoka, Carrovega indeksa in nasipnega kota. Stisljivost smo vrednotili s primerjavo kompresibilnosti in kompaktibilnosti. Kompresibilnost smo vrednotili s Heckelovim, Walkerjevim in Kuentz-Leuenbergovim modelom, kompaktibilnost s pomočjo kompaktibilnostnega profila, ki prikazuje odvisnost natezne trdnosti tablete od tlaka stiskanja. Vrednotili smo tudi elastičnost posamezne pomožne snovi z merjenjem elastične relaksacije. Vse izbrane pomožne snovi so izkazovale ustrezne pretočne lastnosti za direktno tabletiranje, le-te pa so se jim ob dodatku antiadheziva in suhega veziva v večini primerov tudi izboljšale. Glede stisljivosti so se vse pomožne snovi izkazale kot ustrezne za direktno tabletiranje. Najboljšo kompresibilnost in kompaktibilnost sta izkazovala Vivapur® 200 in Neosorb® 300 DC, ki sta zaradi tega tudi najbolj primerna za direktno tabletiranje, najslabšo Emcompress®. Najboljšo elastičnost so izkazovali Neosorb® 300 DC, Xsylisorb® 100DC in Pearlitol® 100DC. Slabše lastnosti stisljivosti posameznih pomožnih snovi gre pripisati deloma velikosti, deloma obliki delcev ter njihovi hrapavosti. In the pharmaceutical industry, various polyols, various forms of lactose, starch and cellulose are often used in the tablets manufacturing process as excipients in direct compression. These represent an important part of composition, so, in conjunction with direct compression, knowing their flow and compact properties, is very important. All these affect the repeatability of compaction, the uniformity of the mass of the tablet and the mechanical resistance of the final product and allow optimization of the compaction process. The purpose of this Master's Thesis was to study eleven frequently used excipients for direct compression in the pharmaceutical industry. These are Vivapur® 200, Emcompress®, Neosorb® 300 DC, Pearlitol® 300 DC, Xylisorb® 100 DC, xylitol, Tablettose® 70, FlowLac® 100, GalenIQ TM 721, Starch 1500® in Pearlitol® 100 DC. First, we studied the flow properties of pure excipients and excipients after the addition of a binder (Kollidon® VA 64) and an antiadhesive agent (Mg stearate). To evaluate them, we used the methodology of measuring mass flow, Carr's index and angle of repose. Compaction properties were evaluated by measuring compressibility and compactibility. Compressibility was evaluated by Heckel's, Walker's in the Kuentz-Leuenberg model, compactibility by means of a compactibility profile, which shows the dependence of the tensile strength of the tablet versus compression pressure. We also evaluated the elasticity of individual excipients by measuring index of elastic relaxation. All selected excipients exhibited appropriate flow properties for direct compression and after the addition of antiadhesive and dry binder, they were also improved in most cases. In terms of good compaction properties, all excipints proved to be suitable for direct tableting. Vivapur® 200 and Neosorb® 300 DC showed the best compressibility and compactibility, so they are the best for direct commpression, while Emcompress® was the worst. The best elasticity showed Neosorb® 300 DC, Xsylisorb® 100DC and Pearlitol® 100DC. Poorer compaction properties of individual excipients can be attributed partly to size, partly to particle shape and their roughness. |
