Pharmaceuticals screening methods

Ishihama et al. [147] have describe a rapid screening method for determining pK values of pharmaceutical samples by pressure-assisted CE, coupled with a photodiode array detector. Each CE run was completed in less than 1 min, so a 96-well microtiter plate could be measured in one day. Determinations of the pKa values of 82 drugs illustrated this interesting new method. 

Yazbeck D, Tao J, Martinez C, Kline B, Hu S (2003) Automated enzyme screening methods for the preparation of enantiopure pharmaceutical intermediates. Adv Syn Cat 4 524-532... 

Pulsed ultrafiltration MS (PUF-MS) represents an inline high throughput affinity screening method with a variety of potential uses in the discovery and development of pharmaceuticals [22]. The in-line combination of solution-phase equilibration, ultrafiltration, and electrospray liquid chromatography mass spectrometry (LC-ESI-MS) facilitates the identification of high affinity target-specific... 

Lienert J, Gudel K, Escher BI (2007) Screening method for ecotoxicological hazard assessment of 42 pharmaceuticals considering human metabolism and excretory routes. Environ Sci Technol 41 4471 78... 

Of course, not all methods of cocrystal production require the use of auxiliary solvents. Thermal microscopy was used to determine if a particular carboxylic acid could cocrystallize with 2-[4-(4-chloro-2-fluorophe-noxy)phenyl]pyrimidine-4-carboxamide, with positive interactions being detected as crystalline material being produced at the binary interface [35]. Once identified, authentic cocrystal systems were prepared on a larger scale using solution-phase methods. In a similar study, hot-state microscopy was used to screen the possible interactions of nicotinamide with seven compounds of pharmaceutical interest that contained carboxylic acid groups [36]. A screening method for cocrystal formation based on differential scanning calorimetry has also been described, and used to demonstrate cocrystal formation in 16 out of 20 tested binary systems [37],... 

The screening method described here was originally developed in the pharmaceutical industry to examine samples positioned on so-called titer-plates with up to... 

JU Bowie, AA Pakula. Screening method for identifying ligands for target proteins. U.S. Patent 5,585,277, Scriptgen Pharmaceuticals, 1996. 

There are examples in the literature for the application of LC-MS-NMR in the pharmaceutical industry. In the area of natural products, this technique has been applied as a rapid screening method of searching unknown marine natural products in chromatographic fractions [108] and for the separation and characterization of natural products from plant origin [109, 110]. Another application is in the area of combinatorial chemistry [111]. In the field of drug metabolism, LC-MS-NMR has been extensively applied for the identification of metabolites [112-120]. And finally, LC-MS-NMR has been used for areas such pharmaceutical research [35,121,122], drug discovery [123], degradation products [101], and food analysis [124,125]. 

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