Modified Release Dosage Form 6cn12
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MODIFIED RELEASE DOSAGE FORM by A. S. Adebayo, PhD
Monday, August 26, 2013
1
Introduction
Modified release dosage forms are drug delivery systems (DDS) which, by virtue of formulation and product design, provide drug release in a modified form distinct from that of the conventional dosage forms. Drug release can either be delayed or extended in nature.
Monday, August 26, 2013
2
Delayed-release products
Usually enteric coated tablets or capsules designed to through the stomach unaltered to release their medication within the intestinal tract.
Monday, August 26, 2013
3
Extended-release products
Designed to release their medication in controlled manner, at pre-determined rate, duration and location in the body to achieve and maintain optimum therapeutic blood levels of drug.
Monday, August 26, 2013
4
Rationale for extended release pharmaceuticals
Drugs that are not inherently long lasting require multiple daily dosing to achieve the desired therapeutic effects.
Multiple daily dosing is often inconvenient and can result in missed doses, made-up doses and patient non-compliant with therapeutic regimen.
Blood levels of drugs from conventional immediaterelease dosage forms taken more than once daily following definite schedule usually demonstrate sequential peaks and troughs (valleys) associated with each dose.
Monday, August 26, 2013
5
Rationale for extended release pharmaceuticals
Extended release tablets or capsules are commonly taken only once or twice daily compared with the conventional dosing of 2 to 4 times daily
Products are designed to provide an immediate release of drug which promptly produces the desired therapy, followed by gradual and continual release of additional amounts of drug to maintain this effect over a predetermined period of time.
The need for night dosing of drugs may be eliminated Monday, August 26, 2013
6
Advantages of Extended-release Dosage Forms over Conventional Forms
Reduction in drug blood level fluctuations
Reduction in frequency of dosing
Enhanced patient compliance
Reduction in incidence of adverse side effects
Reduction in overall healthcare costs.
Monday, August 26, 2013
7
Terminology
The following have been applied to “extended” or “sustained” drug delivery systems:
Controlled-release Extended release (ER) Sustained-release (SR) Timed-release (TR) Long-acting (LA) Prolonged-action (PA), and Sustained-action (SA)
Monday, August 26, 2013
8
Extended-release dosage forms The US FDA defines ER dosage form as: one that allows a reduction in dosing frequency to that presented by a conventional dosage form such as a solution or an immediate release dosage forms.
Monday, August 26, 2013
9
Delayed-release
These are dosage forms designed to release the drug at a time other than promptly after istration.
The delay may be time-based or based on the influence of environmental conditions such as g.i. pH, enzyme, pressure, etc
Monday, August 26, 2013
10
Repeat action
These are dosage forms usually containing 2 single doses of medication, one for immediate and the second for delayed release e.g. bilayered tablets.
Monday, August 26, 2013
11
Targeted release
Drug release that is directed towards isolating or concentrating a drug in a body region, tissue, or site for absorption or drug action
Monday, August 26, 2013
12
Extended-release Oral Dosage Forms The general properties of drugs best suited for ER product design are: They exhibit neither very slow nor very fast rates of absorption and excretion
They are uniformly absorbed from the g.i.t.
They are istered in relatively small doses.
They possess a good margin of safety i.e. Therapeutic Index (TI) Monday, August 26, 2013
13
Technology of ER Dosage Forms ER Coated Beads, Granules or Microspheres – Granules of drug may be coated with lipid materials such as beeswax, carnuba wax, glyceryl monostearate, cetyl alcohol, etc.
Careful blending of coated and uncoated granules and with coatings of different thicknesses will provide drug release of desired characteristics.
Monday, August 26, 2013
14
COMMERCIAL EXAMPLES
Toprol-XL® (metoprolol succinate) tabs. (Astra);
Indocin SR ® (indomethacin capsules (Merck);
Compazine ® (prochloperazine) Spansule Capsules (SmithKline Beecham)
Monday, August 26, 2013
15
Technology of ER Dosage Forms Multitablet system
Monday, August 26, 2013
16
Technology of ER Dosage Forms
Embedding drug in slowly eroding or hydrophilic matrix system – The design comprises of the drug substance plus excipient material that slowly erodes in body fluids thereby progressively releasing the drug for absorption
E.g. Quinidex® Quinine SO4 tablets (Robins); Oramorph ® SR Morphine SO4 tabs. Roxane ®
Monday, August 26, 2013
17
Technology of ER Dosage Forms: ER Microencapsulated Drug
–Microencapsulation is a process by which solids, liquid and semi-solid substances may be encapsulated into microscopic size particles through the formation of thin coating of “wall” material around the substance.
Different rate of drug release can be obtained by changing the core to wall ratio, the type of polymer coat and the method of microencapsulation. E.g. K-Dur ®Microburst Release System (KCl) tabs. (Key)
Monday, August 26, 2013
18
Technology of ER Dosage Forms: Osmotic pump device
This consists of a core tablet surrounded by a semi-permeable membrane coating with a 0.4 mm diameter hole produced by laser beam.
The core tablet has 2 layers, one containing the drug (the “active” layer) and the other containing the polymeric osmotic agent (the “push” layer).
E.g. Glucotrol ® XL (glipizide) tablets (Pfizer) Covera – HS ® (verapamil HCl) tabs. (Searle)
Monday, August 26, 2013
19
Other methods
Embedding drug in an inert plastic matrix – e.g. Desoxyn® (methamphetamine HCl) tabs (Abbott); Procanbid ® (procainamide HCl tabs. (Parke-Davis)
Complex formation
Ion exchange resins
Monday, August 26, 2013
20
Kinetics of Drug release
Drug release from conventional dosage forms, like the other processes of E, are governed by the first-order kinetics model.
In First-order model, drug release is dependent on the amount of drug available for release and therefore the rate of release declines exponentially with time.
Monday, August 26, 2013
21
Kinetics of Drug release…
Extended release dosage forms are governed by zero-order kinetics in which the rate of release is independent of amount of drug remaining in the dosage form.
Therefore a constant amount of drug will be released over time from extended release dosage forms
Monday, August 26, 2013
22
Assignments (Due Feb. 4, 2010)
Identify 3 controlled release formulation excipients, giving chemical and commercial names
What is the kinetic mechanism of drug release followed by Osmotic controlled delivery devices?
Using a suitable graph, illustrate the profile that would be observed in the following scenarios:
Burst release at peal plasma level Design failure leading to “Dose dumping” Design failure leading to drug being withheld
Monday, August 26, 2013
23
MODIFIED RELEASE DOSAGE FORM
THANK YOU FOR YOUR ATTENTION Monday, August 26, 2013
24
Monday, August 26, 2013
1
Introduction
Modified release dosage forms are drug delivery systems (DDS) which, by virtue of formulation and product design, provide drug release in a modified form distinct from that of the conventional dosage forms. Drug release can either be delayed or extended in nature.
Monday, August 26, 2013
2
Delayed-release products
Usually enteric coated tablets or capsules designed to through the stomach unaltered to release their medication within the intestinal tract.
Monday, August 26, 2013
3
Extended-release products
Designed to release their medication in controlled manner, at pre-determined rate, duration and location in the body to achieve and maintain optimum therapeutic blood levels of drug.
Monday, August 26, 2013
4
Rationale for extended release pharmaceuticals
Drugs that are not inherently long lasting require multiple daily dosing to achieve the desired therapeutic effects.
Multiple daily dosing is often inconvenient and can result in missed doses, made-up doses and patient non-compliant with therapeutic regimen.
Blood levels of drugs from conventional immediaterelease dosage forms taken more than once daily following definite schedule usually demonstrate sequential peaks and troughs (valleys) associated with each dose.
Monday, August 26, 2013
5
Rationale for extended release pharmaceuticals
Extended release tablets or capsules are commonly taken only once or twice daily compared with the conventional dosing of 2 to 4 times daily
Products are designed to provide an immediate release of drug which promptly produces the desired therapy, followed by gradual and continual release of additional amounts of drug to maintain this effect over a predetermined period of time.
The need for night dosing of drugs may be eliminated Monday, August 26, 2013
6
Advantages of Extended-release Dosage Forms over Conventional Forms
Reduction in drug blood level fluctuations
Reduction in frequency of dosing
Enhanced patient compliance
Reduction in incidence of adverse side effects
Reduction in overall healthcare costs.
Monday, August 26, 2013
7
Terminology
The following have been applied to “extended” or “sustained” drug delivery systems:
Controlled-release Extended release (ER) Sustained-release (SR) Timed-release (TR) Long-acting (LA) Prolonged-action (PA), and Sustained-action (SA)
Monday, August 26, 2013
8
Extended-release dosage forms The US FDA defines ER dosage form as: one that allows a reduction in dosing frequency to that presented by a conventional dosage form such as a solution or an immediate release dosage forms.
Monday, August 26, 2013
9
Delayed-release
These are dosage forms designed to release the drug at a time other than promptly after istration.
The delay may be time-based or based on the influence of environmental conditions such as g.i. pH, enzyme, pressure, etc
Monday, August 26, 2013
10
Repeat action
These are dosage forms usually containing 2 single doses of medication, one for immediate and the second for delayed release e.g. bilayered tablets.
Monday, August 26, 2013
11
Targeted release
Drug release that is directed towards isolating or concentrating a drug in a body region, tissue, or site for absorption or drug action
Monday, August 26, 2013
12
Extended-release Oral Dosage Forms The general properties of drugs best suited for ER product design are: They exhibit neither very slow nor very fast rates of absorption and excretion
They are uniformly absorbed from the g.i.t.
They are istered in relatively small doses.
They possess a good margin of safety i.e. Therapeutic Index (TI) Monday, August 26, 2013
13
Technology of ER Dosage Forms ER Coated Beads, Granules or Microspheres – Granules of drug may be coated with lipid materials such as beeswax, carnuba wax, glyceryl monostearate, cetyl alcohol, etc.
Careful blending of coated and uncoated granules and with coatings of different thicknesses will provide drug release of desired characteristics.
Monday, August 26, 2013
14
COMMERCIAL EXAMPLES
Toprol-XL® (metoprolol succinate) tabs. (Astra);
Indocin SR ® (indomethacin capsules (Merck);
Compazine ® (prochloperazine) Spansule Capsules (SmithKline Beecham)
Monday, August 26, 2013
15
Technology of ER Dosage Forms Multitablet system
Monday, August 26, 2013
16
Technology of ER Dosage Forms
Embedding drug in slowly eroding or hydrophilic matrix system – The design comprises of the drug substance plus excipient material that slowly erodes in body fluids thereby progressively releasing the drug for absorption
E.g. Quinidex® Quinine SO4 tablets (Robins); Oramorph ® SR Morphine SO4 tabs. Roxane ®
Monday, August 26, 2013
17
Technology of ER Dosage Forms: ER Microencapsulated Drug
–Microencapsulation is a process by which solids, liquid and semi-solid substances may be encapsulated into microscopic size particles through the formation of thin coating of “wall” material around the substance.
Different rate of drug release can be obtained by changing the core to wall ratio, the type of polymer coat and the method of microencapsulation. E.g. K-Dur ®Microburst Release System (KCl) tabs. (Key)
Monday, August 26, 2013
18
Technology of ER Dosage Forms: Osmotic pump device
This consists of a core tablet surrounded by a semi-permeable membrane coating with a 0.4 mm diameter hole produced by laser beam.
The core tablet has 2 layers, one containing the drug (the “active” layer) and the other containing the polymeric osmotic agent (the “push” layer).
E.g. Glucotrol ® XL (glipizide) tablets (Pfizer) Covera – HS ® (verapamil HCl) tabs. (Searle)
Monday, August 26, 2013
19
Other methods
Embedding drug in an inert plastic matrix – e.g. Desoxyn® (methamphetamine HCl) tabs (Abbott); Procanbid ® (procainamide HCl tabs. (Parke-Davis)
Complex formation
Ion exchange resins
Monday, August 26, 2013
20
Kinetics of Drug release
Drug release from conventional dosage forms, like the other processes of E, are governed by the first-order kinetics model.
In First-order model, drug release is dependent on the amount of drug available for release and therefore the rate of release declines exponentially with time.
Monday, August 26, 2013
21
Kinetics of Drug release…
Extended release dosage forms are governed by zero-order kinetics in which the rate of release is independent of amount of drug remaining in the dosage form.
Therefore a constant amount of drug will be released over time from extended release dosage forms
Monday, August 26, 2013
22
Assignments (Due Feb. 4, 2010)
Identify 3 controlled release formulation excipients, giving chemical and commercial names
What is the kinetic mechanism of drug release followed by Osmotic controlled delivery devices?
Using a suitable graph, illustrate the profile that would be observed in the following scenarios:
Burst release at peal plasma level Design failure leading to “Dose dumping” Design failure leading to drug being withheld
Monday, August 26, 2013
23
MODIFIED RELEASE DOSAGE FORM
THANK YOU FOR YOUR ATTENTION Monday, August 26, 2013
24
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