Solubility and dissolution rate enhancement of ibuprofen by co-milling with polymeric excipients.

The aim of this study was to enhance the kinetic solubility and dissolution rate of ibuprofen by co-milling with different excipients and to establish the underlying mechanism(s) for such enhancement. In the first-part, two excipients (HPMC and soluplus) were selected from seven, and the optimal ball-milling parameters of speed and time (18 Hz, 15 min) were determined based on solubility-enhancement and flow-ability criteria. In the second-part, co-milling of different weight-ratios of ibuprofen-to-excipient was carried out and solubility and dissolution rates were determined.

Enhancing crystalline properties of a cardiovascular active pharmaceutical ingredient using a process analytical technology based crystallization feedback control strategy.

Pharmaceutical regulatory bodies require minimal presence of solvent in an active pharmaceutical ingredient (API) after crystallization. From a processing point of view bigger crystals with minimal agglomeration and uniform size distribution are preferred to avoid solvent inclusion and for improved downstream processing. The current work addresses these issues encountered during the production of the potential anti-arrhythmic cardiovascular drug, AZD7009.

Combining self-modeling curve resolution methods and partial least squares to develop a quantitative reaction monitoring method with minimal reference data.

An example of combining self-modeling curve resolution (SMCR) methods and partial least squares (PLS) to construct a quantitative model using minimal reference data is presented. The objective was to construct a quantitative calibration model to allow real-time in situ ultraviolet-attenuated total reflection (UV/ATR) measurements to determine the end-point during a chlorination reaction. Time restrictions for development combined with difficult reaction sampling conditions required the method to be developed using only a few key reference measurements.