Assessment of hot-melt coating methods for multiparticulate substrates: mortar-coating vs. pan-coating
Abstract
Hot-melt coating (HMC) is an alternative, solvent-free coating method generally used to modify substrate release rate and/or mask its unpleasant taste. The aim of this study was to assess two HMC methods (pan-coating and mortar-coating) by assaying functional properties of the coated material. The selected substrates included highly soluble sodium chloride (model substance) and caffeine (bitter drug), and the coating agent was glycerol distearate without/with the addition of liquid paraffin. Experiments with sodium chloride revealed that pan-coating yielded particles of more regular shape, while mortar-coating yielded samples of more uniform coating layer. The flowability of the coated material depended on the particle size. Sustained sodium chloride release was achieved for all mortar-coated and some pan-coated samples. The analysis of the results indicated mortar-coating as a preferable HMC method for caffeine coating. The resulting caffeine yield in the coated samples was high (99%), the material showed satisfactory mechanical properties and drug release from the coated particles was sustained. Overall, the obtained results suggest that both pan- and mortar-coating can be used to sustain the release of drugs with unpleasant taste, but mortar-coating can be considered as a more simple and practical method that can be potentially used in compounding pharmacies.
References
Bose S, Bogner RH. Solventless pharmaceutical coating processes. Pharm Dev Techn. 2007;12:115-31.
Kim KH, Jun M, Lee MK. Bioavailability of the common cold medicines in jellies for oral administration. Pharmaceutics. 2020;12(11):1073.
Sohi H, Sultana Y, Khar RK. Taste masking technologies in oral pharmaceuticals: recent developments and approaches. Drug Dev Ind Pharm. 2004;30(5):429-48.
Douroumis D. Practical approaches of taste masking technologies in oral solid forms. Expert Opin Drug Deliv. 2007;4:417-26.
Basu A, De A, Dey S. Techniques of tablet coating: concepts and advancements. A comprehensive review. RRJPPS. 2013;2(4):1-6.
Foroughi-Dahr M, Mostoufi N, Sotudeh-Gharebagh R, Chaouki J. Particle Coating in Fluidized Beds, Reference Module in Chemistry, Molecular Sciences and Chemical Engineering, Elsevier; 2017; p. 6-8.
Thies C, Dos Santos IR, Richard J, VandeVelde V, Rolland H, Benoit JP. A supercritical fluid-based coating technology 1: Process considerations. Journal Microencapsul. 2003;20(1):87-96.
Becker K, Salar-Behzadi S, Zimmer A. Solvent-free melting techniques for the preparation of lipid-based solid oral formulations. Pharm Res. 2015;32:1519-45.
Sudke SG, Sakarakar DM. Lipids - An instrumental excipient in pharmaceutical hot-melt coating. Int J Pharm Tech Res. 2013;5(2):607-21.
Milanović A, Aleksić I, Ibrić S, Parojčić J, Cvijić S. Hot-melt coating with Precirol ATO 5 in a fluidized-bed apparatus: Application of experimental design in the optimization of process parameters. J Drug Deliv Sci Technol. 2018;46:274-84.
Disch T, Haala J, Koeberle M. Hot-melt coated immediate-release taste-masked paracetamol and caffeine orally-disintegrating granules. Pullach: Hermes Pharma. 2016.
Patil A, Chafle S, Khobragade D, Umathe S, Avari J. Evaluation of hot melt coating as taste masking tool. Int Res J Pharm. 2011;2(8):169-72.
Becker K, Haack D, Salar-Behzadi S, Zimmer A. Oral pharmaceutical composition comprising taste-masked N-acetylcystein. United States patent US 9,636,307. 2017.
Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’drug delivery systems. Eur J Pharm Sci. 2000;11:S93-8.
Jannin V, Cuppok Y. Hot-melt coating with lipid excipients. Int J Pharm. 2013;457:480-7.
Lopes DG, Salar-Behzadi S, Zimmer A. Designing optimal formulations for hot-melt coating. Int J Pharm. 2017;533(2):357-63.
Becker K, Saurugger EM, Kienberger D, Lopes D, Haack D, Köberle M, Stehr M, Lochmann D, Zimmer A, Salar-Behzadi S. Advanced stable lipid-based formulations for a patient-centric product design. Int J Pharm. 2016;497(1-2):136-49.
Kraahs P, Bold S, Fahsel L. Melt-coated pharmaceutical composition with fast release. United States patent US 8,481,060. 2013.
Freund M, Csikos R, Keszthelyi S, Mózes GY. Applications of paraffin waxes and liquid paraffins. In: Mózes GY, editor. Paraffin products: properties, technologies, applications. Elsevier Scientific; 1982; p. 240-329.
Szewczyk E, Karlowicz–Bodalska K, Han S, Musial W. Influence of liquid paraffin, white soft paraffin and initial hydration on viscosity of corticosteroid cream. Trop J Pharm Res. 2014;13(8):1233-8.
European Pharmacopoeia, 10th ed, Strasbourg: Council of Europe, 2019.
Kolafa J. Solubility of NaCl in water and its melting point by molecular dynamics in the slab geometry and a new BK3-compatible force field. J Chem Phys. 2016;145(20):204509.
Schneider CA, Rasband WS, Eliceiri KW. NIH Image to ImageJ: 25 years of image analysis. Nat Methods. 2012;9(7):671-75.
The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. 15th ed. O'Neil MJ, editor. Cambridge, UK: Royal Society of Chemistry; 2013; p. 1596.
Drašković M, Medarević D, Aleksić I, Parojčić J. In vitro and in vivo investigation of taste-masking effectiveness of Eudragit E PO as drug particle coating agent in orally disintegrating tablets. Drug Dev Ind Pharm. 2017;43(5):723-31.
Moore JW, Flanner HH. Mathematical comparison of curves with an emphasis on in vitro release profiles. Pharm Tech. 1996;20(6):64-74.
Szumilo M, Belniak P, Swiader K, Holody E, Poleszak E. Assessment of physical properties of granules with paracetamol and caffeine. Saudi Pharm J. 2017;25(6):900-5.