Application of Tumbling Melt Granulation Method to Prepare Controlled-Release Beads by Coating with Mixture of Functional Non-meltable and Meltable Materials.

Granulation techniques and technologies: recent progresses

“…Cooling of the agglomerated powder and the consequent solidification of the molten or soften binder complete the granulation process. 31,32 Low melting binders can be added to the granulation process either in the form of solid particles that melt during the process (melt-in procedure or in situ melt granulation) or in the form of molten liquid, optionally containing the dispersed drug (spray-on or pump-on procedure), which displays a variety of options to design final granular properties. More specifically, the melt-in procedure of melt granulation process includes heating a mixture of drug, binder and other excipients to a temperature within or above the melting range of the binder.…”

“…36 Moreover, in comparison with the conventional wet granulation process, it proposes several advantages. 31,32,34,37,38 Generally, organic or aqueous solvents are not demanded for the melt granulation process, hence the environmental requirements of organic solvent capture and recycling are eliminated, while the absence of water excludes the wetting and drying phases, making the entire process less energy- and time-consuming. Melt granulation method could be efficiently applied in order to enhance the stability of moisture sensitive drug and further to improve the poor physical properties of the drug substance.…”

Application of melt granulation technology to enhance stability of a moisture sensitive immediate-release drug product

“…Thomsen et al (1994) proposed that materials melting in the range of 45-100 • C are suitable binders for melt granulation. The method is gaining increased popularity as an alternative to conventional granulation methods, such as wet granulation, roller compaction, fluid-bed granulation, etc., and there are numerous reports in the literature on the application of melt granulation in drug product development as well as on different granulating agents used and various techniques applied during the process (Kidokoro et al, 2002(Kidokoro et al, , 2003Passerini et al, 2002;Perissutti et al, 2003;Royce et al, 1996;Tan et al, 2006;Walker et al, 2005;Young et al, 2002) Furthermore, by selecting suitable binders, the melt granulation may be used to prepare controlled release granules (Grassi et al, 2003;Hamdani et al, 2002;Maejima et al, 1998;Theis and Kleinebudde, 1999;Zhang and Schwartz, 2003;Voinovich et al, 2000). Many different hydrophobic excipients (e.g., stearic acid, mono-, di-and tri-glycerides, glyceryl behenate, hydrogenated castor oil, etc.)…”