No abstract

Drug powders containing micron-size drug particles are used in several pharmaceutical dosage forms. Many drugs, especially newly developed substances, are poorly water soluble, which limits their oral bioavailability. The dissolution rate can be enhanced by using micronized drugs. Small drug particles are also required in administration forms, which require the drug in micron-size size due to geometric reasons in the organ to be targeted (e.g., drugs for pulmonary use). The common technique for the preparation of micron-size drugs is the mechanical comminution (e.g., by crushing, grinding, and milling) of previously formed larger particles. In spite of the widespread use of this technique, the milling process does not represent the ideal way for the production of small particles because drug substance properties and surface properties are altered in a mainly uncontrolled manner. Thus, techniques that prepare the drug directly in the required particle size are of interest. Because physicochemical drug powder properties are decisive for the manufacturing of a dosage form and for therapeutic success, the characterization of the particle surface and powder properties plays an important role. This article summarizes common and novel techniques for the production of a drug in small particle size. The properties of the resulting products that are obtained by different techniques are characterized and compared.

No abstract

No abstract

No abstract

Different crystal forms of the analgesic drug ibuprofen were prepared and characterized in this study. Various conditions were used for the crystallization: crystallization was carried out using the solvent change method, the temperature change method, and the solvent evaporation method. Crystals were grown from different solvents. Different crystal forms with different properties were observed: cubic, needle-shaped, and plate-shaped crystals were obtained. Spherical agglomeration occurs when crystallization is carried out in acetonitrile or methanol. Flowability of these spherical crystals is increased. All crystals were determined as isomorphic by differential scanning calorimetry and x-ray analysis--which queries doubtful results of recent publications. Properties like dissolution behavior and properties influencing the manufacturing of dosage forms--like flowability--differ. Thus the choice of the optimal preparation method influencing the crystal habit is important in manufacturing the drug ibuprofen.

In situ micronization is a suitable method for the production of micro-sized drugs. This technique can be performed continuously or discontinuously and uses only common technical equipment. Compared to milled products drug properties are optimized as all particle surfaces are naturally grown, the particle size is more uniformly distributed and the powder is less cohesive.

No abstract