Hot melt coating with lipid excipients for user-friendly solid oral dosage forms
1Diogo Gomes Lopes, 2Karin becker, 3Detlev Haack, 4Michael Stehr, 2Andreas Zimmer, 1Sharareh Salar-Behzadi*
1- Research Center Pharmaceutical Engineering (RCPE) GmbH, Graz, Austria
2- Institute of Pharmaceutical Science, Department of Pharmaceutical Technology, University of Graz, 8010 Graz, Austria
3- HERMES ARZNEIMITTEL GmbH, Großhesselohe, Germany
4- CREMER OLEO GmbH & Co. KG, Witten, Germany
The simple and effective orally delivery of an active pharmaceutical ingredient (API) is an important factor influencing treatment efficacy, tolerability and patient compliance. To further improve the user-friendliness and acceptance of solid oral dosage forms, multiparticulate systems are becoming more common. As they have proven especially popular with patients requiring regular doses or those that find it difficult to swallow solid tablets, such as children, the elderly or individuals suffering from esophagitis. However, for this method to prove effective, most APIs must be effectively coated. Traditional methods to coat solid oral dosage forms mostly use solvents, an approach that suffers from a range of drawbacks including environmental concerns, lengthy processing times and the risk of dissolving drug. Hot melt coating (HMC) is an innovative and effective alternative that is reliable, cheap and fast, while simultaneously offering an opportunity to better manipulate and control characteristics such as taste, stability and release rate.
In this work, multiparticulate systems of different APIs are coated with lipid formulations via HMC. Drug release profiles and the solid state of triacylglycerides (TAGs) based excipients are monitored over storage. Small angle X-ray scattering, scanning electron microscopy and differential scanning calorimetry are used to characterize polymorphism, surface disruption (blooming) and complex networks of crystallites.
Our results show that surface blooming does not play a critical role in the drug release from TAGs coatings, but that the apparent diffusion coefficient of drugs can be dramatically reduced by increasing TAGs crystallite size and resulting tortuosity. This work brings new insights on the drug release from solid lipid dosage forms being an important step towards avoiding conventional complex formulations and preventing the overuse of excipients with unknown toxicity.
See more of this Group/Topical: Pharmaceutical Discovery, Development and Manufacturing Forum