文档介绍：1Form Selection of poundsAnn W. Newman and G. Patrick StahlySSCI, Inc., West Lafayette, IndianaI. INTRODUCTIONThe drug development process involves a number of activities which are carriedout simultaneously, as shown by the oversimpli?ed depiction in Fig. 1. Once amolecule is discovered that has desirable biological activity, the process of creat-ing a pharmaceutical drug product from this molecule begins. As toxicology andef?cacy studies are undertaken, methods for manufacture of the active moleculeand for its delivery in therapeutic doses are sought. Critical to the latter effort is?nding a form of the active molecule which exhibits appropriate physical proper-ties. The form ultimately selected, called the active pharmaceutical ingredient(API), or drug substance, must be stable and bioavailable enough to be formulatedinto a drug product, such as a tablet or suspension. This formulation must beeffective at delivering the active molecule to the targeted chapter describes methodology useful in selection of the appropriatesolid form of a drug substance for inclusion in a drug product. Form monly considered among the primary goals of a preformulation , the investigative techniques discussed herein also have application inearly drug substance and drug product development activities (shown by the cir-cled area in Fig. 1).Solid form selection involves the preparation and property evaluation ofmany derivatives of an active molecule. Drug substance properties of importancein the drug development process may be categorized as shown in Table depend on the nature of the drug substance and the ?nal anic molecules contain ionizable groups such as opyright 2002 by Marcel Dekker. All Rights . 1The drug development or amino groups. Reaction of pounds with acids or bases producesalts, which have much different physical properties than the neutral parents. Asingle molecular entity, be it a salt o