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INTRODUCTION
Sustained released
Before initiating a discussion of sustained release dosage forms, it is necessary to
provide a short explanation of terminology used because there is considerable
confusion in this area. The general consensus is that controlled release denotes
systems, which can provide some control, whether this is of a temporal or spatial
nature, or both, of drug release in the body. In other words, the systems attempts to
control drug concentration in the target tissue or cells. Thus, prolonged release or
sustained release systems, which only prolong therapeutic blood or tissue levels of
the drug for an extended period of time, cannot be considered as controlled release
systems by this definition. They are distinguished from rate-controlled drug
delivery systems, which are able to specify the release rate and duration in vivo
precisely, on the basis of simple in vitro tests. Drug targeting, on the other hand,
can be considered as a form of controlled release in that it exercises spatial control
of drug release within the body.
Sustained release describes the release of drug substance from a dosage form or
delivery system over an extended period of time. 1 The basic goal of this system is
to achieve a steady state blood level that is therapeutically effective and non-toxic
for an extended period of time. The design of proper dosage regimens is an
important element in accomplishing this goal. Sustained release, sustained action,
controlled release, extended action, timed release, depot and repository dosage
forms are terms used to identify drug therapy systems that are designed to achieve
a prolonged therapeutic effect by continuously releasing medication over an
extended period of time after administration of single dose. In the case of
injectable dosage forms, this period is measured in hours and critically depends on
the residence time of the dosage form in the gastrointestinal tract. The term
controlled release has become associated with those systems from which
therapeutic agents may be automatically delivered at predetermined rates over a
long period of time. Products of this type have been formulated for oral, injectable
and topical use and inserts for placement in body cavities.2 Controlled release
systems also denotes systems which can provide some control whether this be of a
temporal or spatial nature or both, of drug release in the body. The system attempts
to control drug concentrations in the target tissues or cells.
Prolonged or sustained release systems only prolong therapeutic blood or tissue
levels of the drug for an extended period of time.
Sustained release
Sustained release
and devices, and the allocation to one or the other category is decided on a case by
case basis. Sustained release (SR) preparations are not new but several new
modifications are being introduced. They are also referred to as long acting or
delayed release when compared to rapid or conventional release
preparations. The term sometimes overlaps with controlled release, which
implies more sophisticated control of release and not just confined to the time
dimension.Now a days conventional dosage forms of drugs are rapidly being
replaced by the new and the novel drug delivery systems. Amongst, these the
controlled release/sustained release dosage forms have become extremely popular
in modern therapeutics. Matrix system is the release system which prolongs and
controls the release of the drug, which is dissolved or dispersed. A matrix is
defined as a well-mixed composite of one or more drugs with gelling agent i.e.
hydrophilic polymers. Introduction of matrix tablet as sustained release (SR) has
given a new breakthrough for novel drug delivery system in the field of
Pharmaceutical technology [1]. Sustained release constitutes any dosage form that
provides medication over an extended time or denotes that the system is able to
provide some actual therapeutic control whether this is of a temporal nature, spatial
nature or both. Sustained release system generally do not attain zero order type
release and usually try to mimic zero order release by providing drug in a slow first
order. Repeat action tablet are an alternative method of sustained release in which
multiple doses of drug are an alternative method of Sustained release, in which,
multiple doses are contained within a dosage form and each dose is released at a
periodic interval. Oral drug delivery has been known for decades as the most
widely utilized route of administration among all the routes that has been explored
for the systemic delivery of drugs via various pharmaceutical products of different
dosage form. Nowadays most of the pharmaceutical scientists are involved in
developing an ideal DDS. This ideal system should have advantage of single dose
for whole duration of the treatment and it should deliver the drug directly at
specific site. Scientists have succeeded to develop a system that can be as near to
an ideal system and it encourages the scientists to develop controlled release
system. The design of oral sustain drug delivery system (DDS) should be primarily
aimed to achieve the more predictability and reproducibility to control the drug
release, drug concentration in the target tissue and optimization of the therapeutic
effect of a drug by controlling its release in the body with lower and less frequent
dose. Conventional drug therapy typically involves the periodic dosing of a
therapeutic agent that has been formulated in a manner to ensure its stability,
activity and bioavailability. For most of the drugs, conventional methods of
formulation are quite effective. However some drugs are unstable and toxic and
have a narrow therapeutic range, exhibit extreme solubility problems, require
localization to a particular site in the body or require strict compliance or long-term
Sustained release
Sustained release
Sustained release
Sustained release
Both high and low doses of API present a challenge in this respect. Most APIs tend
to have poor compressibility, which affects the quality of tablets if the formulation
calls for a large proportion of API. At the same time, there can also be problems
when low amounts of actives need to be incorporated into tablets because it is
difficult to accurately blend a small amount of active in a large amount of excipient
to achieve the desired uniformity and homogeneity.
For instance, segregation of the different components can occur. This means there
is not a uniform distribution of tablet ingredients being fed to the press, and thus
batch to batch consistency of the manufactured tablet cannot be assured.
One of the principal risk factors for segregation is the wide particle size
distribution in direct compression formulations, in which active ingredients tend to
be at the fine end of the range. Where there is a wide range of particle sizes, there
is an increased likelihood of sifting, where the smaller particles 'slip through' the
bigger ones.
Other bulk powder properties are also important for successful tabletting, such as
good flow ability, and all of these factors combine to place a high requirement on
the excipients used for direct compression.
Sustained release