Orodispersible dosage forms are promising new approaches for drug delivery. They enable an easy application, as there is no need to drink high amounts of liquids or swallow large solid dosage forms. The aim of the study was to develop an orodispersible film (ODF) as an alternative to tablets, syrups or suppositories for the treatment of vomiting and nausea, especially for the pediatric population. Formulations were investigated by X-ray diffraction, scanning electron and polarized light microscopy. Additionally, two commercially available electronic taste sensing systems were used to investigate the applied taste-masking strategies. Results obtained from X-ray-diffraction and polarized light microscopy showed no recrystallization of dimenhydrinate in the formulation when cyclodextrin or maltodextrin were used as solubilizing and complexing agent. All ODFs showed fast disintegration depending on the characterization method. In order to get taste information, the dimenhydrinate formulations were analytically compared to pure drug and drug-free formulations by electronic tongues. Results obtained from both systems are comparable and were used together for the first time. It was possible to develop an ODF of dimenhydrinate that is fast disintegrating even in small volumes of liquid. Furthermore, in vitro taste assessment by two electronic tongues revealed taste-masking effects by the excipients. Full article

One “Quality by Design” approach is the focus on the variability of the properties of the active substance. This is crucially important for active substances that are obtained from natural resources such as herbal plant material and extracts. In this paper, we present various strategies for the development of herbal products especially taking into account the natural batch-to-batch variability (mainly of the dry mass) of tablets that contain a fixed amount of tincture. The following steps in the development have been evaluated for the outcome of the physico-chemical properties of the resulting tablets and intermediates: concentration of the tincture extracted from Echinacea fresh plant, loading of the concentrate onto an inert carrier, the respective wet granulation and drying step, including milling, and the adjuvant excipients for the tablet compression step. The responses that were investigated are the mean particle size of the dried and milled granulates, compaction properties and disintegration time of the tablets. Increased particle size showed a significant increase of the disintegration time and a decrease of the compaction properties. In addition, our results showed that the particle size has a great dependency on the ratio of liquid to carrier during the wet granulation process. Thus, the variability of the respective parameters tested was influenced by the performed strategies, which is how the tincture correlated to its dry mass and the relation of the amount of carrier used. In order to optimize these parameters, a strategy considering the above-mentioned points has to be chosen. Full article

The suitability of the new isomalt grade galenIQ™ 801 for dry granulation and following tableting is evaluated in this study. Isomalt alone, as well as a blend of equal parts with dibasic calcium phosphate, is roll compacted and tableted. Particle size distribution and flowability of the granules and friability and disintegration time of the tablets are determined. Tensile strength of tablets is related to the specific compaction force during roll compaction and the tableting force. In all cases, the tensile strength increases with raising tableting forces. The specific compaction force has a different influence. For isomalt alone the tensile strength is highest for tablets made from granules prepared at 2 kN/cm and 6 kN/cm and decreases at higher values, i.e., >10 kN/cm. Tensile strength of the blend tablets is almost one third lower compared to the strongest tablets of pure isomalt. Friability of pure isomalt tablets is above the limit. Disintegration time is longest when the tensile strength is at its maximum and decreases with higher porosity and lower tensile strengths. Isomalt proves to be suitable for tableting after roll compaction. Even though the capacity as a binder might not be as high as of other excipients, it is a further alternative for the formulation scientist. Full article