ABSTRACT

Drugs must be present in a solution form to cross biologic barriers such as the gastrointestinal

mucosa. Thus the process of dissolution becomes an integral part of the various rate-limiting

steps leading to a clinical response. However, dissolution alone is not sufficient to provide the

absorption of drugs. The drug molecules must have the characteristics required for

crossing the various lipoid layers or membranes in order to reach the general circulation.

Lack of sufficient aqueous solubility is usually the rate-limiting step in the dissolution

process, and lack of sufficient lipophilic properties is the usual rate-limiting step in the

penetration of the lipoid barriers. Attempts to rectify dissolution problems can therefore

lead to problems in membrane transport, and vice versa. A fine balance between the

hydrophilic and lipophilic properties is needed to provide optimum delivery of drugs to

the site of action.