Pulsatile drug delivery aims to release drugs on a programmed pattern i.e.: at appropriate time and/or at appropriate site of action. Currently, it is gaining increasing attention as it offers a more sophisticated approach to the traditional sustained drug delivery i.e: a constant amount of drug released per unit time or constant blood levels. Technically, pulsatile drug delivery systems administered via the oral route could be divided into two distinct types, the time controlled delivery systems and the site-specific delivery systems. The simplest pulsatile formulation is a two layer press coated tablet consisted of polymers with different dissolution rates. Homogenicity of the coated barrier is mandatory in order to assure the predictability of the lag time. The disadvantage of such formulation is that the rupture time cannot be always adequately manipulated as it is strongly correlated with the physicochemical properties of the polymer. Gastric retentive systems, systems where the drug is released following a programmed lag phase, chronopharmaceutical drug delivery systems matching human circadian rhythms, multiunit or multilayer systems with various combinations of immediate and sustained-release preparation, are all classified under pulsatile drug delivery systems. On the other hand, site-controlled release is usually controlled by factors such as the pH of the target site, the enzymes present in the intestinal tract and the transit time/pressure of various parts of the intestine. In this review, recent patents on pulsatile drug delivery of oral dosage forms are summarized and discussed.
Nowadays, pharmaceutical technology and research for new drugs and formulations is of great importance, as scientists attempt to discover even more revolutionary and efficient methods to treat various diseases. At the same time the correct dosing and site targeting are equally important for clinical success. Research in sustained drug release systems is very promising towards such a direction, while it offers advantages and potential rewards contrary to traditional therapy. The drug plasma concentrations remain inside the therapeutic range for a longer time period compared to the conventional formulations. In addition, sustained release formulations may increase the likelihood for the patient to respond to the therapy, since drug formulations are generally characterized by one daily given dose. The rate at which a drug is released from a sustained-release formulation depends upon many factors, while excipients play the most important role. Most sustained release formulations are based on biodegradable polymers in the form of a drug-encapsulating matrix or membrane. Examples range from monolithic devices, polymer-coated capsules and implant devices, hydrogels, to injectable systems based on suspensions of micro-, nanospheres or polymer solutions. The advantages and disadvantages of these different formulation systems are being extensively discussed in the present review.
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