Formulation design and development

Akers, M.J., Fites, A.L., and Robinson, R.L., Formulation design and development of parenteral suspensions, Bull. Parent Drug Assoc., 41, 88, 1987. 

Merging solid form discovery, with the formulation design and development, and with FIH manufacturing into the same cohesive team. 

Oral dmg product formulation and manufacturing process development can use a hierarchical approach to meeting three conditions based on, in order of importance, bioavailability, stability, and manufacturability. The bioavailability of a drug product is the most critical condition and must meet established criteria or the product is not viable. Dmg substance properties such as salt form, solubility, and particle size can significantly affect pharmacokinetic and pharmacodynamic performance of a product. The dosage form platform, formulation design, and manufacturing process can also affect the PK/PD profile of a product. Therefore, all selections must maintain the required pharmacokinetic/pharmacodynamic outcome and work within these confines to achieve a stable and robust product/process. 

Figure 6.3 Formulation flow chart for designing and developing drug products.

Computers are now used in the design and development of new chemicals, and their employment in toxicity prediction could lead to improved products that present a reduced hazard to humans. Although computers are useful for performing routine calculations, they do not usually possess insight or rationalization. Therefore, they should represent only one of a number of test procedures used to formulate a full safety evaluation in a given chemical. Where they are used, their results should be interpreted by a panel of expert toxicologists capable of providing an overall view of the likely toxic risk in the human environment. 

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