[MODIFIED RELEASE DOSAGE FORMS] TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS

1. Coated Beads, Granules, and Microspheres

2. Microencapsulation

3. Matrix Tablets

4. Osmotic Systems

5. Ion-Exchange Resins

6. Complex Formation

Technologies Used in Extended-Release Dosage Forms

Coated Beads, Granules, and Microspheres

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

The drug is distributed into beads, pellets, granules, or other particulate systems.

● Lipid materials

● Cellulosic materials

● Commercial aqueous coating systems

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

Beads, granules, or microspheres are coated with varying thicknesses using:

● Beeswax

● Carnauba wax

● Glyceryl monostearate

● Cetyl alcohol

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

LIPID materials used in coating beads, granules, or microspheres:

Ethylcellulose

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

CELLULOSIC materials used in coating beads, granules, or microspheres:

Ethylcellulose with plasticizer

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

COMMERICAL AQUEOUS COATING SYSTEMS used in coating beads, granules, or microspheres:

● Placed in CAPSULES

● Compressed in TABLETS

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

Coated beads, granules, or microspheres may be placed in:

Microencapsulation

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This involves enclosing solids, liquids, or gases within microscopic size particles by forming a thin coating of "wall" material around the substance.

Microencapsulation

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This process uses WALL-FORMING materials.

● Gelatin

● Polyvinyl alcohol

● Ethylcellulose

● Polyvinyl chloride

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

WALL-FORMING materials used in MICROENCAPSULATION

Matrix Tablets

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This approach involves embedding drug in an INERT PLASTIC MATRIX such as polyethylene, polyvinyl acetate, or polymethacrylate

● Polyethylene

● Polyvinyl acetate

● Polymethacrylate

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

Inert polymeric matrix used in MATRIX tablets include:

Matrix Tablets

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

In _____, drugs are slowly released from the plastic matrix by DIFFUSION.

Diffusion

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

In MATRIX TABLETS, drugs are slowly released from the plastic matrix by ____.

TRUE

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

TRUE OR FALSE:

After the drug is completely released, the inert tablet matrix is excreted UNCHANGED in the feces.

Osmotic Systems

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

These systems use osmotic pressure to control drug release.

OROS (Osmotic Release Oral System)

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This is a pioneering oral osmotic pump system.

OROS (Osmotic Release Oral System)

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This system is composed of a core tablet surrounded by a semi-permeable membrane coating having a 0.4-mm diameter "hole" produced by a laser beam.

0.4-mm diameter "hole"

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

OROS (Osmotic Release Oral System) is composed of a core tablet surrounded by a semi-permeable membrane coating having a ____-mm diameter "hole" produced by a laser beam.

laser beam

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

OROS (Osmotic Release Oral System) is composed of a core tablet surrounded by a semi-permeable membrane coating having a 0.4-mm diameter "hole" produced by a ____.

Active layer

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

The core tablet layer of OROS (Osmotic Release Oral System) which contains the DRUG.

Push layer

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

The core tablet layer of OROS (Osmotic Release Oral System) which contains the polymeric osmotic agent.

● GITS (Gastrointestinal Therapeutic System)

● COER (Controller-Onset Extended Release)

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

Other osmotic systems include:

GITS (Gastrointestinal Therapeutic System)

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This is a type of PUSH-PULL osmotic system.

COER (Controller-Onset Extended Release)

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This type of osmotic system releases drug 4-5 hours after ingestion via a SLOWLY SOLUBILIZING COATING between the drug core and semipermeable membrane.

4-5 hours

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

COER (Controller-Onset Extended Release) releases drug ___ hours after ingestion via a SLOWLY SOLUBILIZING COATING between the drug core and semipermeable membrane.

Ion-Exchange Resins

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

A solution of a CATIONIC drug may be passed through a column containing an ion-exchange resin, forming a complex by the replacement of HYDROGEN atoms.

● Tableted

● Encapsulated

● Suspended in an aqueous vehicle

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

The RESIN-DRUG complex formed by ion-exchanged resins can be:

Ion-Exchange Resins

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

In _____, the release of the drug is dependent upon the pH and the ELECTROLYTE concentration in the GIT.

● pH in the GIT

● Electrolyte concentration in the GIT

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

In Ion-Exchange Resins, the release of the drug is dependent upon the___ and ____

Complex Formation

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

This approach involves drug substances combined with other chemical agent to form COMLEXES that may be only SLOWLY SOLUBLE in body fluids.

Complex Formation

[TECHNOLOGIES USED IN EXTENDED-RELEASE DOSAGE FORMS]

In _____, the SLOW dissolution provides the extended release of the drug.

● Patients should be advised of the dose and dosing frequency of modified drug-release products and instructed not to use them interchangeably or concomitantly with immediate-release forms of the same drug.

● Patients should be advised that modified-release tablets and capsules should not be crushed or chewed, since such action would compromise their drug release feature.

● Patients and caregivers should be advised that nonerodible plastic matrix shells and osmotic tablets remain intact throughout gastrointestinal transit and the empty shells or ghosts from osmotic tablets may be seen in the stool

[CLINICAL CONSIDERATIONS]

Clinical considerations in using modified release dosage forms

TRUE

[CLINICAL CONSIDERATIONS]

TRUE OR FALSE:

Patients should be advised of the dose and dosing frequency of modified drug-release products and instructed NOT TO use them interchangeably or concomitantly with immediate-release forms of the same drug.

TRUE

[CLINICAL CONSIDERATIONS]

TRUE OR FALSE:

Patients should be advised that modified- release tablets and capsules should NOT BE crushed or chewed, since such action would compromise their drug release feature.

TRUE

[CLINICAL CONSIDERATIONS]

TRUE OR FALSE:

Patients and caregivers should be advised that NON-ERODIBLE plastic matrix shells and osmotic tablets remain intact throughout gastrointestinal transit and the empty shells or ghosts from osmotic tablets may be seen in the stool.

● Well-closed and tight container

● Light-resistant container

PACKAGING used for modified release dosage forms