New Aspects in the Formulation of Drugs Based on Three Case Studies.

The improvement of pharmaceutical dosage forms, such as tablets, towards drug delivery control and cost efficiency is of great importance in formulation technologies. Here, three examples: in situ coating, freeze casting and protein-based biocomposites are presented that address the above mentioned issues and contribute to further developments in formulation technologies. The in situ coating increases the economic efficiency by saving process steps in comparison to a conventional tableting process and provides a crystalline coating for a tailorable drug delivery rate.

Novel mineralized heparin-gelatin nanoparticles for potential application in tissue engineering of bone.

Nanoparticles (NPs) were prepared from succinylated gelatin (s-GL) cross-linked with aldehyde heparin (a-HEP) and used subsequently as a nano-template for the mineralization of hydroxyapatite (HAP). Gelatin was functionalized with succinyl groups that made it soluble at room temperature. Heparin was oxidized to generate aldehyde groups and then used as a cross-linker that can react with s-GL to form NPs via Schiff's base linkage.

From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor.

The solid-state development for the low dose drug molecule SAR114137, a selective and reversible inhibitor of cysteine cathepsin S/K, is reported. Six polymorphic forms as well as various solvate phases were discovered by an extensive polymorphism screening. The solid phase characterizations revealed that phase 1, from which a single crystal structure could be obtained, is the thermodynamically most stable form and therefore it was chosen for pharmaceutical development.

Effect of additives on isothermal crystallization kinetics and physical characteristics of coconut oil.

The effect of lauric acid and low-HLB sucrose esters (L-195, S170) on the isothermal crystallization of coconut oil was investigated by differential scanning calorimetry. The fundamental crystallization parameters, such as induction time of nucleation and crystallization rate, were obtained by using the Gompertz equation. The Gibb's free energy of nucleation was calculated via the Fisher-Turnbull equation based on the equilibrium melting temperature.

Impurity distribution in a solid-liquid interface during static layer crystallization.

The impurity distribution inside crystalline layers in static layer crystallizations was explored theoretically and experimentally for a binary eutectic mixture of caprolactam and water. The impurity distribution in the layer is modeled by a mass balance equation coupled with an energy balance equation. The mass balance equation is established with a combination of the growth of the layer and the diffusional movement of impurity.

Microwave processing of natural biopolymers--studies on the properties of different starches.

In this study, the influence of microwave irradiation on some physico-chemical properties and several pharmaceutical technological parameters of potato and maize starches was investigated. Changes in their habits were observed and decrease in moisture contents caused by the electromagnetic irradiation was determined. The crystalline structures and the micromorphological parameters of the starches were affected by microwave irradiation in different ways depending on the botanical origin of the samples.

Investigation of entrapped pore in the pastilles by a mercury porosimetery technique.

The pore in pastilles was investigated which are produced by a pastillation technology. Mercury intrusion porosimeter and scanning electron microscopy (SEM) techniques were used for the investigation. The formation of micro-pores and cracks were in dependence of the manufacturing conditions of the pastilles (final impacting velocity, degree of subcooling and surface roughness of cooled substrate).

Prediction of degree of deformation and crystallization time of molten droplets in pastillation process.

The direct solidification process of a melt into a particulate solid is studied to achieve the desired size and shape of the product and to predict the required crystallization time. For an example, a Bisacodyl melt is chosen. The role of the contact angle of the droplet is investigated as a function of Reynolds number, degree of subcooling and characteristic of used cooled surface (substrate).