The global demand for phytopharmaceutical products is on the upward trend and will probably continue to rise in the next few decades. This demand is fuelled by the growing acceptability, availability and affordability and the growing scientific evidence of efficacy. However, while great progress is being made in research and development of these products in the developed world, very little progress has been made in research, development and documentation of possible leads/products in developing countries of Africa. The challenges range from dearth of capacity to develop implement appropriate research protocols and tools. This article is an attempt toward providing a guide to the chemical and biologiocal screening approaches in the research and development of phytopharmaceuticals. Approaches towards achieving quality products that meets basic regulatory requirements are discussed.