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Solid Oral Modified-release

Dosage Forms and Drug


Delivery Systems
San Pedro, Blessing
Santos, Zelica Trina
So, Liza Marie
Tan, Alexis Vianca
Modified Release
In recent years: use to describe dosage forms having
drug release features based on time, course, and/or
location that are designed to accomplish therapeutic or
convenience objectives not offered by conventional or
immediate-release forms
USP differentiates modified-release forms as extended
release and delayed release.

Modified Release
Delayed-release products
Enteric coated tablets or capsules
Designed to pass through the stomach unaltered, later
to release their medication within the intestinal tract

** enteric coatings- protect a subs. from destruction by
gastric fluids or to reduce stomach distress caused by
irritating drugs
Delayed-release and Extended-
release Products
Extended-release products
Designed to release their medication in a controlled
manner of a predetermined rate, duration and location
to achieve and maintain optimum therapeutic blood
levels of drug
Delayed-release and Extended-
release Products
Most modified-release products are administered
orally (capsules and tablets).
Some modified-release dosage forms and drug
delivery systems are described including:
Ocular
Parenteral
Subdermal (transdermal patches)
Vaginal products
Drugs that are not inherently long lasting and require
multiple daily dosing to achieve the desired therapeutic
results.
Multiple daily dosing is inconvenient for the patient and
can result in missed doses, madeup doses, and
noncompliance with the regimen.
When conventional immediate-release dosage forms are
taken on schedule and more than once daily, they cause
sequential therapeutic blood level peaks and valleys
associated with the taking of each dose.
The Rationale for Extended-release
Pharmaceuticals
When doses are not administered on schedule, the
resulting peaks and valleys reflect less than the optimum
drug therapy
If doses are administered too frequently, minimum toxic
concentrations of drug may be reached with toxic side
effects resulting.
If doses are missed, periods of sub therapeutic drug blood
levels or those below the minimum effective concentration
may result, with no benefit to the patients.
The Rationale for Extended-release
Pharmaceuticals
Extended-release tablets and capsule
Commonly taken only once or twice daily
Provide an immediate release of drug that promptly
produces the desired therapeutic effect, followed by
gradual release of additional amount of drug to maintain
this effect over a predetermined period
* Sustained plasma drug levels
Eliminate the need for night dosing


The Rationale for Extended-release
Pharmaceuticals
Non-oral rate-controlled drug delivery systems
Drug release pattern
o 24 hrs for most transdermal patches to 3 months for the
estradiol vaginal insert
The Rationale for Extended-release
Pharmaceuticals
Less fluctuation in drug blood levels
-Controlling rate of release eliminates peaks and valleys of blood
levels
Frequency reduction in dosing
-extended release products frequently deliver more than a
single dose, hence may be taken less often than conventional
forms
Enhanced convenience and compliance
- With less frequency of dosing a patient is less apt to neglect
taking a dose; also greater convenience with day and night
administration
Advantages of Extended-Release
Dosage Forms Over Conventional
Forms
Reduction in adverse side effects
- Because of fewer blood level peaks outside therapeutic range
and into toxic range, adverse side effects are less frequent
Reduction in overall health care costs
- Although initial cost of extended-release dosage forms may be
greater than for conventional forms, overall cost of treatment
may be less because of enhanced therapeutic benefit, fewer
side effects, reduced time for healthcare personnel to dispense
and administer drugs and monitor patients

Advantages of Extended-Release
Dosage Forms Over Conventional
Forms
Loss of flexibility in adjusting the drug dose and/or
dosage regimen
Sudden and total drug release
Dose dumping (failure to technology)
Disadvantages
Many terms has been used by manufacturers to describe
product types and function.
-Used to describe orally administered dosage forms
Sustained Release (SR)
Sustained Action (SA)
Prolonged Action (PA)
Controlled Release (CR)
Extended Release (ER)
Timed Release (TR)
Long Acting (LA)
Terminology
Sustained-release (SR)
- Designed to slowly release a drug in the body over an
extended period of time
* Timed-release (TR)
- Consisting of a drug that is released in small amounts over
time usually in the gastrointestinal tract
* Sustained Action (SA)
- A drug product formulation that provides the required dosage
initially and then maintains or repeats it at desired intervals
Terminology
Prolonged Action (PA)
- Designed to release drug slow and provide a backup drug
continuously over a long interval of time, preventing rapid
absorption
* Controlled Release (CR)
- Dosage forms of a drug that are released or are activated
over a period of time by controlled-release process or
technology
* Long Acting (LA)
- Slowly effective after initial dosage but maintaining its effects
over a long period of time, being slowly absorbed and persisting
in the tissues before being excreted
Terminology
* Rate-controlled delivery
Applied to certain types of drug delivery systems in
which the rate of delivery is controlled by features of
the device rather than by physiologic or environmental
conditions
Like gastrointestinal pH or drug transit through the
gastrointestinal tract

Terminology
Extended-release (ER) designed to provide prolonged
release of the medication
According to the U.S Food and Drug Administration:
- One that allows a reduction in dosing frequency from that
necessitated by a conventional dosage form such as a solution
or an immediate-release dosage form
* Delayed Release- designed to release the drug at a time
other than promptly after administration
The delayed may be time based or based on the influence of
environmental conditions, like gastrointestinal pH

Terminology
Repeat Action
usually contain two single doses of medication, one for
immediate release and the second for delayed release.
Targeted Release
describes drug directed toward isolating or
concentrating a drug in a body region, tissue, or site for
absorption or for drug action
Terminology
Examples of Delayed-release
Examples of Extended-release
Examples of Extended-release