Optimization of a novel wax matrix system using aminoalkyl methacrylate copolymer E and ethylcellulose to suppress the bitter taste of acetaminophen

Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

“…The most common equipment in the industry used for melt processing are the extruder, the high shear mixer, the fluid bed, the pan coater and the spray dryer, which all allow for upscaling. Depending on the desired solid dosage form, a great number of different downstream processes are addressed in the literature, such as spheronization ( 49 , 69 , 109 , 209 ), molding ( 74 , 95 , 133 , 183 , 237 , 238 ), capsule filling ( 87 , 88 , 91 , 98 , 100 , 102 , 139 , 239 – 246 ), injection moulding ( 247 , 248 ), freeze pelletization ( 121 , 249 ), pastilation ( 250 ), milling ( 122 , 196 ) or tableting ( 92 , 156 , 251 ). Nevertheless, it should be obvious, that manufacturing costs will rise with the addition of further process steps and, therefore, should be considered thoroughly in advance.…”

Evaluation of coat uniformity and taste-masking efficiency of irregular-shaped drug particles coated in a modified tangential spray fluidized bed processor

“…The drug release study for examining the taste-masking efficiency of the coated particles followed the methodology reported by Shiino et al [16]. Dissolution tests were conducted in a USP dissolution apparatus 1 (2100 C, Distek, USA) with 900 mL dissolution medium maintained at 37 ± 0.5 C and baskets rotated at 100 rpm.…”

“…In the case of particle coating for taste masking, an optimum coat thickness is desirable to allow for fast dissolution in the soluble pH range of the polymer coat while maintaining sufficient sealant properties in the polymer insoluble pH range. Paracetamol has been widely used as a model drug for the development of taste-masking formulations and the in vitro dissolution profile of the developed dosage forms has been commonly used to evaluate their taste-masking efficiency [16,[22][23][24]. The percentage drug release within an early time point (e.g., £ 5 min) has been recommended by FIP/AAPS (Federation International Pharmaceutique/American Association of Pharmaceutical Scientists) guidelines as an approximation of the bitter taste for ODTs [25,26].…”

“…The percentage drug release within an early time point (e.g., £ 5 min) has been recommended by FIP/AAPS (Federation International Pharmaceutique/American Association of Pharmaceutical Scientists) guidelines as an approximation of the bitter taste for ODTs [25,26]. The study by Shiino et al found the human threshold for identifying the bitterness of paracetamol to be 35 µg/mL when the dissolution tests were carried out using the paddle method listed in the Japanese Pharmacopoeia (15th edition) with a dissolution medium volume of 900 mL [16]. Therefore, taste-masking efficiency could be evaluated by whether the drug substance is released or the released amount is below the human threshold for identifying its bitter taste within an early time point in the dissolution profile.…”

Recent advances in bitterness evaluation methods

“…Many foods elicit a bitter flavor naturally (e.g., grapefruit juice, beer) 5 and many active pharmaceutical ingredients (APIs), such as acetaminophen, macrolide antibiotics and alkaloids are too bitter to be administrated orally. [6][7][8] Therefore, bitterness is one of the greatest challenges for food and drug commercialization due to lack of patient compliance, especially in pediatric patients. [9][10][11] Thus a suitable bitter masking method is necessary to ensure the acceptability and commercialization of APIs, and many bitter evaluation methods have also been developed for evaluating the efficiency of bitter masking.…”