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ER Oral DF FINAL
ER Oral DF FINAL
Characteristics of Extended-Release
Products:
Exhibit neither very slow nor very fast rates
Characteristics of Extended-Release
Products:
Uniformly absorbed from g.i.t
Drug must have:
Good aqueous solubility
Maintain adequate residence time in g.i.t
Poor candidates:
Poorly absorbed drugs
Drugs at varying & unpredictable rates
Characteristics of Extended-Release
Products:
Administered in relatively small doses
Not suitable:
Drugs w/ large single doses
Characteristics of Extended-Release
Products:
Posses a good margin of safety
Therapeutic Index
most widely used measure of the margin
TD50/ED50
Very potent drugs = narrow/very small
therapeutic index
Larger therapeutic index = Safer drug
Poor candidate:
Drugs administered in small doses/
possess very narrow therapeutic
indices
Characteristics of Extended-Release
Products:
Used in the treatment of chronic rather than
acute condition
Cause:
Drugs for acute condition = greater adjustment of the
dosage by physician
EXTENDED-RELEASE TECHNOLOGY
FOR ORAL DOSAGE FORMS
Extended drug action achieved by:
Affecting the rate (drug release from dosage form)
EXTENDED-RELEASE TECHNOLOGY
FOR ORAL DOSAGE FORMS
Technologies
systems
Commercial Examples
Toprol-XL (metoprolol succinate) tabs. (Astra);
Indocin SR
- a solution of drug
substance is placed on small inert
nonpareil seeds/ beads made of
sugar & starch or on microcrystalline
cellulose spheres
Nonpareil seeds 425 to 850 um
Microcrystalline cellulose spheres
- 170-600 um
- more durable during
production than
sugar-based cores
thicknesses
Provide desired drug-released characteristics
MULTITABLET SYSTEM
Preparation of small spheroid compressed tablets 3-4mm
in diameter
To have varying drug release characteristics
MICROENCAPSULATED DRUG
Microencapsulation
- A process by which solids, liquids, or even gases may be
MICROENCAPSULATED DRUG
Gelatin
Common wall forming material, and synthetic polymer such as:
Polyvinyl alcohol
Ethylcellulose
Polyvinyl chloride
MICROENCAPSULATED DRUG
Typical encapsulation process:
1.
Dissolve the wall material
2.
3.
4.
Gelatin in water
Usually Acacia
Additive material concentrates the gelatin (polymer) into tiny
liquid droplets
Droplets(coacervate)
- Form a film/coat around the particles of the substance to be
encapsulated
- Consequence of low interfacial tension of residual water/solvent in the
wall material
- To have continuous tight film coating
MICROENCAPSULATED DRUG
Final Dry Microcapsules:
Free flowing discrete particles of coated material
Wall material 2% to 20% of total particle weight
To obtain different rates of drug release:
Change ratio of core to wall, the polymer used for coating, and
method of microencapsulation
MICROENCAPSULATED DRUG
Advantage:
Administered dose of drug is subdivided into small units that are
spread over a large area of the g.i.t