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8/11/2019 SolidOralModified-releaseDosageFormsandDrugDelivery1
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Solid Oral Modified-releaseDosage Forms and Drug
Delivery SystemsSan Pedro, BlessingSantos, Zelica Trina
So, Liza MarieTan, Alexis Vianca
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Modified Release
In recent years: use to describe dosage forms havingdrug release features based on time, course, and/orlocation that are designed to accomplish therapeutic orconvenience objectives not offered by conventional or
immediate-release forms USP differentiates modified-release forms as extended
release and delayed release.
Modified Release
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Delayed-release products
Enteric coated tablets or capsules
Designed to pass through the stomach unaltered, laterto release their medication within the intestinal tract
** enteric coatings- protect a subs. from destruction bygastric fluids or to reduce stomach distress caused byirritating drugs
Delayed-release and Extended-release Products
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Extended-release products
Designed to release their medication in a controlledmanner of a predetermined rate, duration and locationto achieve and maintain optimum therapeutic bloodlevels of drug
Delayed-release and Extended-release Products
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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
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Drugs that are not inherently long lasting and require
multiple daily dosing to achieve the desired therapeuticresults.
Multiple daily dosing is inconvenient for the patient andcan result in missed doses, madeup doses, andnoncompliance with the regimen.
When conventional immediate-release dosage forms aretaken on schedule and more than once daily, they causesequential therapeutic blood level peaks and valleysassociated with the taking of each dose.
The Rationale for Extended-releasePharmaceuticals
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When doses are not administered on schedule, the
resulting peaks and valleys reflect less than the optimumdrug therapy
If doses are administered too frequently, minimum toxicconcentrations of drug may be reached with toxic sideeffects resulting.
If doses are missed, periods of sub therapeutic drug bloodlevels or those below the minimum effective concentrationmay result, with no benefit to the patients.
The Rationale for Extended-releasePharmaceuticals
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Extended-release tablets and capsule
Commonly taken only once or twice daily
Provide an immediate release of drug that promptlyproduces the desired therapeutic effect, followed bygradual 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-releasePharmaceuticals
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Non-oral rate-controlled drug delivery systems
Drug release patterno 24 hrs for most transdermal patches to 3 months for the
estradiol vaginal insert
The Rationale for Extended-releasePharmaceuticals
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Less fluctuation in drug blood levels
-Controlling rate of release eliminates peaks and valleys of bloodlevels
Frequency reduction in dosing-extended release products frequently deliver more than asingle dose, hence may be taken less often than conventionalforms
Enhanced convenience and compliance- With less frequency of dosing a patient is less apt to neglecttaking a dose; also greater convenience with day and nightadministration
Advantages of Extended-ReleaseDosage Forms Over Conventional
Forms
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Reduction in adverse side effects
-Because of fewer blood level peaks outside therapeutic rangeand into toxic range, adverse side effects are less frequent
Reduction in overall health care costs
- Although initial cost of extended-release dosage forms may begreater than for conventional forms, overall cost of treatmentmay be less because of enhanced therapeutic benefit, fewerside effects, reduced time for healthcare personnel to dispenseand administer drugs and monitor patients
Advantages of Extended-ReleaseDosage Forms Over Conventional
Forms
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Loss of flexibility in adjusting the drug dose and/or
dosage regimen Sudden and total drug release
Dose dumping (failure to technology)
Disadvantages
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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
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Sustained-release (SR)
- Designed to slowly release a drug in the body over anextended period of time
* Timed-release (TR)
- Consisting of a drug that is released in small amounts overtime usually in the gastrointestinal tract
* Sustained Action (SA)
- A drug product formulation that provides the required dosageinitially and then maintains or repeats it at desired intervals
Terminology
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Prolonged Action (PA)
- Designed to release drug slow and provide a backup drugcontinuously over a long interval of time, preventing rapidabsorption
* 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 effectsover a long period of time, being slowly absorbed and persistingin the tissues before being excreted
Terminology
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* Rate-controlled delivery
Applied to certain types of drug delivery systems inwhich the rate of delivery is controlled by features ofthe device rather than by physiologic or environmentalconditions
Like gastrointestinal pH or drug transit through thegastrointestinal tract
Terminology
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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 thatnecessitated by a conventional dosage form such as a solutionor an immediate-release dosage form
* Delayed Release- designed to release the drug at a timeother than promptly after administration The delayed may be time based or based on the influence of
environmental conditions, like gastrointestinal pH
Terminology
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Repeat Action
usually contain two single doses of medication, one forimmediate 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 forabsorption or for drug action
Terminology
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Examples of Extended-release
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Examples of Extended-release
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