In recent years, many research efforts have been spent in the achievement of selective delivery of drugs into the colon following oral administration. Indeed, colonic release is regarded as a beneficial approach to the pharmacological treatment or prevention of widespread large bowel pathologies, such as inflammatory bowel disease and adenocarcinoma. In addition, it is extensively explored as a potential means of enhancing the oral bioavailability of peptides, proteins and other biotechnological molecules, which are known to be less prone to enzymatic degradation in the large, rather than in the small, intestine. Based on these premises, several formulation strategies have been attempted in pursuit of colonic release, chiefly including microflora-, pH-, pressure- and time-dependent delivery technologies. In particular, this review is focused on the main design features and release performances of time-controlled devices, which rely on the relative constancy that is observed in the small intestinal transit time of dosage forms.
The swelling and dissolution behavior of pharmaceutical systems containing a drug and a polymer can be analyzed by a mathematical model which predicts the drug released and the gel layer thickness as a function of time. It is possible to approximate the values of several of the physicochemical parameters of this model in order to obtain an order-of-magnitude analysis of the tablet dissolution process. Selected experimental results of tablet dissolution and drug release are analyzed and conclusions are made about the importance of the drug and polymer content and solubility in the release behavior.
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