Taste Masking of Griseofulvin and Caffeine Anhydrous Using Kleptose Linecaps DE17 by Hot Melt Extrusion

Abstract

Abstract. The objective of this project was to investigate the potential of Kleptose Linecaps DE17 (KLD) in masking the unpleasant/bitter taste of therapeutic agents by hot melt extrusion (HME). Griseofulvin (GRI) and caffeine anhydrous (CA) were used as a bitter active pharmaceutical ingredient (API) model drugs. Thermogravimetric studies confirmed the stability of GRI, CA, and KLD at the employed extrusion temperatures. The differential scanning calorimetry (DSC) studies revealed a characteristic melting endotherm of GRI at 218-220°C and CA at 230-232°C in the physical mixtures as well as in all extrudates over the period of study, indicating the crystalline nature of drug. HME of KLD was achieved only in the presence of plasticizer. Among the several plasticizers investigated, xylitol showed improved processability of KLD at 15% w/w concentration. Dissolution studies of HME extrudates using simulated salivary medium exhibited ∼threefold less release compared to physical mixture at the end of 5 min (the lesser drug release, better the taste masking efficiency). Furthermore, the results from the sensory evaluation of products in human panel demonstrated strong bitter taste in the case of physical mixture compared to the HME formulation, suggesting the potential of Kleptose Linecaps DE17 as taste masking polymer in melt extruded form.

Development and evaluation of an oral fast disintegrating anti-allergic film using hot-melt extrusion technology

“…This study is also in accordance with the Code of Ethics of the World Medical Association (Declaration of Helsinki). The experimental procedure for this study was as per our previously published work [10, 32]. …”

Engineering Size and Structure of Particles in Novel Modified-Release Delivery Systems

“…In another study, HME of Kleptose Linecaps DE17 was achieved only in the presence of xylitol as plasticizer at 15% w/w level. And as for the select of a pore former, formulations with inorganic salts showed slightly better taste masking efficiency (80).…”

Therapies Available for the Treatment of Fungal Nail Infection

“…Nail avulsion or the removal of the nail plate is mainly carried out to determine the spread of infection in the nail bed, separate the infected nail plate from adjacent tissue and treat a fungal infection that has spread to nearby tissue areas. As surgical treatment is the most invasive treatment for onychomycosis, it leads to some severe complications such as hematoma and nail warping/distortion [14][15][16][17][18]. Two types of avulsion are prevalent in clinical treatment today: chemical avulsion and surgical avulsion.…”