By Jens T. Carstensen

FROM THE PREFACE This ebook addresses difficulties and ideas of formula and preformulation with which i've got involved myself for 34 years. whilst i used to be hired within the pharmaceutical I labored at features, within the 1960's, which have been the precursors of preformulation, and my early courses handled such concerns. within the following a long time advances were made in technique and the world of preformulation has grown. thought and how during which difficulties are seen have additionally passed through swap. The textual content offers with the pharmaceutical elements of preformulation, no longer the factitious nor the analytical facets. It takes its vantage aspect on the time limit while the pharmaceutical preformulator first obtains a pattern of the drug substance, and it explores the actual, chemical and technological features which are wanted for an entire exploration of the aptitude merits and drawbacks of the drug substance. it's only during the knowing of underlying rules that sufficient exploration could be conducted.

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54:1334. , Sokoloski, T. , (1996), J. Pharm. , 84: 1236. , Sokoloski, T. , (1996), J. Pharm. , 85: 381. 64. , Zografi, G. , (1980), Int. J. , 5:1. 1 Definition of pH pH is defined as the negative of the logarithm of the hydronium ion activity, but in this text we shall simply substitute concentrations for activities, since they are almost equal in dilute solution. Hence, pH is (Brønsted, 1943a): or Some authors employ activity rather than concentration in the definition of pH. The ion [H3O+] is usually referred to as the hydronium ion.

6 Macroscopic Property Determination in Later Phases In the development of a product, after it has been determined in early clinical, phases that the drug substance is a potential market candidate, thoughts of scale-up come up, eventually leading to pivotal and pilot batches. g. compression) of the substance. A great deal can be learned by model experimentation on the drug substance itself to abort problems in later stages, so that when adequate amounts of drug substance become available several mechanical and thermodynamic determinations are in order.

A thermal activation monitor is a highly sensitive (microwatt range) instrument that is capable of monitoring heat events that are exceedingly small. , adsorption, heat of solution, dissolution, crystallization) may be investigated at a high level of precision and with small samples. Page 13 Chapter 2 Solubility In order to assess properties of solutions it is necessary first to be able to produce them. For this reason, it is of importance to determine the solubility of a compound in aqueous media.

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