Formulations medicinal chemistry

In the last few years, optimization techniques have become more widely used in the pharmaceutical industry. Some of these have appeared in the literature, but a far greater number remain as in-house information, using the same techniques indicated in this chapter, but with modifications and computer programs specific to the particular company. An excellent review of the application of optimization techniques in the pharmaceutical sciences was published in 1981 [20]. This covers not only formulation and processing, but also analysis, clinical chemistry, and medicinal chemistry. 

Gareth Kilian completed his undergraduate B.Pharm. degree at the University of Port Elizabeth in 1999. In 2002 he completed his M.Sc. degree in medicinal chemistry Cum Laude, also at the University of Port Elizabeth, were his work was directed on the medicinal chemistry of aromatic cyclic dipeptides. He has since worked as a community service pharmacist in 2002 at Butterworth Hospital in the Eastern Cape, after which he was employed as a lecturer in Pharmaceutics at the NMMU, where he currently works. He is a Ph.D. candidate at the NMMU under Professor Pieter Milne, also working on cyclic dipeptides. He has coauthored several peer-reviewed manuscripts in international journals as well as supervising and cosupervising a number of M.Sc. candidates over the past 6 years in the fields of medicinal chemistry and pharmaceutical formulation. 

Sultan, M., Stecher, G., Stoggl, W. M., Bakry, R., Zahorski, P, Huck, C. W., El Kousy, N. M., and Bonn, G. K., Sample pretreatment and determination of non steroidal anti-inflammatory drugs (NSAIDs) in pharmaceutical formulations and biological samples (blood, plasma, erythrocytes) by HPLC-UV-MS and micro-HPLC, Current Medicinal Chemistry 12(5), 573-588, 2005. 

The medicinal chemistry of fluorosteroids is of course dominated by the fluoro-corticoids. Research in fluorocorticoids is now essentially devoted to the search for new formulation of registered drugs. Elsewhere, there is currently a renewal of interest for fluorosteroids in medicinal chemistry mainly in view to develop drugs for hormonal disorders. 

The synthesis of fluorinated aliphatic compounds is the main topic of this chapter. Indeed, numerous aromatic fluorinated products are available commercially. Moreover, in contrast to aliphatic molecules, their synthesis has not undergone significant evolution in the last few years. The synthesis of highly fluorinated compounds is also not considered here, since these compounds are much more involved in the formulation sciences than in medicinal chemistry. In this chapter, the synthesis of fluorinated compounds is dealt with in the following order monofluorinated, then difluoro-methylated, and finally trifluoromethylated molecules. 

It is clear that if these aspirational E factor targets are to be met, then improvements are desirable in many areas of chemistry, including waste minimization in medicinal chemistry, greener synthetic methods in primary manufacture, increased use of chemo and biocatalysis, and more collaborative efforts between pharmaceutical companies. These areas are aU discussed in the remainder of this chapter. Although Sheldon focused on primary manufacture, it is also important to think about secondary manufacture (formulating tablets, capsules, or other dosage forms), which is also covered in this chapter. 

Isis Pharmaceuticals Chemistry/Formulations, http // www.isispharm.com/Antisense-Technology/ Antisense-Drug-Discovery-Platform/Medicinal-Chemistry. htm (accessed August 2012). 

The objectives of medicinal chemistry are as easily formulated as they are difficult to achieve Find, develop and improve drug substances that cure or alleviate diseases (see below Section l.C.) and understand the causative and accompanying chemical processes (see below Section HI. A.). 

---