Comparison of Different Liquid and Semisolid Vehicles Selected for Oral Administration of Pellets and Minitablets with Diazepam: In Vitro Investigation

Abstract

The acceptability and palatability of a dosage form are extremely important to improve patient compliance. Mixing oral solid dosage forms with food carriers is often necessary to ease swallowing and provide the taste-masking effect. The present research investigated how a liquid or semisolid carrier influences the disintegration time and drug dissolution rate of pellets and minitablets with diazepam. The disintegration of pellets and minitablets in liquid carriers (water, milk and apple juice) was determined using a texture analyser. Dissolution tests were performed for the dosage forms dispersed in gel vehicles (2% carmellose and 0.5% carbomer gels) or applesauce. The disintegration of minitablets in water and apple juice was fast (1 min), but it slowed to 3 and 5 min in milk and gel vehicles, respectively. The pellets disintegrated in liquid carriers within 3 min. The drug dissolution rate in 0.1 M HCl depended on the gel viscosity in this medium. The preserved high viscosity of a carmellose gel inhibited the dissolution of diazepam. On the other hand, the viscosity of the carbomer gel decreased rapidly, and in effect, the dissolution rate of diazepam from the incorporated pellets or minitablets was comparable to the dissolution from loose pellets or minitablets.

The Use of Calcium Phosphate-Based Starter Pellets for the Preparation of Sprinkle IR MUPS Formulation of Rosuvastatin Calcium

“…This way of taking medicines facilitates swallowing and helps to mask their unpleasant taste, leading to better patient compliance. Furthermore, studies have shown that sprinkle formulations are more acceptable to children than liquid forms such as traditionally used syrups [ 4 , 5 ]. In recent years, numerous types of sprinkled drug products have begun to emerge and are now available in the form of immediate-release (IR), delayed-release (DR), extended-release (XR), or multiparticulate drug delivery systems (MDDS), including multiple-unit pellet systems (MUPS) [ 6 ].…”

“…It should also be noted that sprinkle formulations are solid dosage forms and have enhanced stability during storage compared to liquids. In addition, they make it possible to give the drug product the required release characteristics (immediate or modified) [ 4 , 6 ]. With this respect, sprinkle formulations in the form of multiparticulate pellet system (multiple-unit pellet system, MUPS) appear to be the most beneficial, as all the critical quality characteristics can be easily achieved by applying the appropriate coating layers [ 9 , 10 , 11 ].…”