Solid drugs taken orally are mixtures of active pharmaceutical ingredients (hereinafter referred to as “API”); agents such as excipients added as binders or diluents; and lubricants added to enhance flow properties of particles. In general, active pharmaceutical ingredients are solid organic substances. In many cases, a substance of the same chemical...
In the early stages of new drug discovery, the structure of small molecule hits resulting from compound screening is modified to derive leads (putative drug molecules) and then the leads are optimized intensely to achieve a molecule with a higher affinity to the target protein. The atomic resolution protein structure...
The phenomenon whereby a single substance exhibits multiple different crystal structures is known as crystal polymorphism; the structures are known as polymorphic forms. Many active pharmaceutical ingredients (hereinafter referred to as “API”) of pharmaceutical drugs exhibit polymorphism. Differences in crystal type attributable to hydration may sometimes be referred to as...
Many Japanese pharmaceutical companies are now intensively investigating methods for inspection of starting materials. One of the reasons is the PIC/S (Pharmaceutical Inspection Convention and Pharmaceutical Inspection Co-operation Scheme) accession of Japan in the near future. Since samples taken from all containers must be tested, speed of identification is strongly...
The analysis of metal impurities for pharmaceutical products such as harmful elements contained in the raw materials and residual catalysts in the manufacturing process is important for the risk assessment in actual large scale production.
Various guidelines and criteria of harmful elements in pharmaceutical products have been established. According to...
Data collection and processing have a significant impact on the structure analysis step. Considering the power of current direct method programs, quality data are nearly equal in importance to obtaining the initial structure when crystallographic difficulties such as an ambiguous space group and twining are not involved.
For the expert small molecule crystallographer, where a flexible configuration is required, Rigaku offers the XtaLAB P200 chemical crystallography system. The XtaLAB P200 represents a state-of-the-art chemical crystallography system with its incorporation of the DECTRIS PILATUS 200K hybrid pixel array detector (HPAD). The XtaLAB P200 can be configured with molybdenum...
We have improved the conventional micro area stress measurement system (AutoMATE) by replacing the gas flowing detector Position Sensitive Proportional Counter (PSPC) with a semiconductor detector, the D/teX Ultra 1000. This new AutoMATE II provides the user with new functions, high sensitivity, high counting rate and good energy resolution. Maintenance...
