MODIFIED RELEASE Flashcards
Used to describe dosage forms having drug release features based on; time, course, location that are designed to accomplish therapeutic
MODIFIED RELEASE
- Dosage form allows a reduction in dosing frequency
- drug is released slowly
EXTENDED RELEASE
- Release the drug from the dosage form at a time other than promptly after administration
- enteric coated
DELAYED RELEASE
Contain two doses of medication, one for immediate release and the second for delayed release
repeat action
The release of a drug from an oral dosage form may be intentionally delayed until it reaches the intestines for several reasons
- protect drug from gastric fluids
- reduce gastric distress
- facilitate GI transit
use for coating enteric coated tablets (5)
fats
fatty acids
waxes
shellac
cellulose acetate phthalate
breaking down in the less acidic environment of the intestine
pH dependent
eroding by moisture over time during gastrointestinal transit
time dependent
deteriorating as a result of the hydrolysis-catalyzing action of intestinal enzymes
enzyme dependent
tablet’s outer shell or coating
immediate release
tablet’s inner core separated by a slowly permeable barrier coating
second release
Drug from the inner core is exposed to body fluids and release ____ hours after administration
4 - 6 hours
Repeat action dosage forms are best suited for the treatment of ____ conditions requiring repeated dosing
chronic
The drugs utilized should have ____ dosage and fairly rapid rates of ____ and ____.
low
absorption
excretion
Drug release directed toward isolating or concentrating a drug in a body region, tissue, or site for absorption or for drug action
targeted release
The drug is distributed into beads, pellets, granules or other particulate system
coated beads, granules, and microspheres
COATED BEADS, GRANULES AND MICROSPHERES
Drug is coated onto inert beads (____, ____ or -
____)
starch
sugar
microcrystalline cellulose
COATED BEADS, GRANULES AND MICROSPHERES
Then, the beads are coated with a lipid material (____, ____, ____ or ____)
beeswax
carnauba wax
glyceryl monostearate
cetyl alcohol
COATED BEADS, GRANULES AND MICROSPHERES
Then, the beads are coated with a cellulosic material like ____
ethylcellulose
COATED BEADS, GRANULES AND MICROSPHERES
Granules will be placed in ____ or ____
capsules or tablets
COATED BEADS, GRANULES AND MICROSPHERES
are also used as coating material such as ethyl cellulose and plasticizer
aqueous coating systems
COATED BEADS, GRANULES AND MICROSPHERES
The thicker the coat the more ____ top penetration more delay on drug release and dissolution
more resistant
- Small spheroid compressing tablets 3 to 4 mm in diameter
- Placed in gelatin capsule shell to provide the desired pattern of drug release
- Each capsule contain 8 to 10 mini tablets
- Uncoated for immediate release and other coated for extended release
multitablet system
MULTITABLET SYSTEM
size in diameter
3 to 4 mm
MULTITABLET SYSTEM
each capsule contain ____ to ____ mini tablets
8 - 10
MULTITABLET SYSTEM
____ fro immediate release
uncoated
MULTITABLET SYSTEM
____ for extended release
other coated
MULTITABLET SYSTEM
____ does not have coating
first two tablets
in 8-10 minitabs
Solids, liquids, or even gases may be ENCLOSED into MICROSCOPIC-SIZE PARTICLES, through the formation of thin coatings of “wall” materials around the substance .
* Advantage
The administered drug dose is subdivided into small units spread over a large area of the GIT, enhance absorption by diminishing local drug concentration)
microencapsulation
MICROENCAPSULATION
example of wall forming materials
gelatin
polyvinyl alcohol
ethylcellulose
polyvinyl chloride
MICROENCAPSULATION
The “wall” material (e.g. gelatin) is ____
first dissolved in water
MICROENCAPSULATION
To this is added the material to be encapsulated, and then a second material, usually ____, is added to concentrate the gelatin into tiny liquid droplets
acacia
tablet that comes out of tableting machine
compressed tab
Drug granules are made with a material (lipid or cellulosic) which slowly erodes in body fluids, thus resulting in granules which progressively release the drug for absorption.
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
Combination of drug granules and drug-excipient granules provide ____ action.
EXTENDED RELEASE
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
The granules may be ____ or formulated as a ____.
TABLETED, CAPSULE
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
commonly used as the excipient base in tablet matrix system
HYDROPHILIC CELLULOSE POLYMERS
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
In the body, the tablet (or capsule material) is wetted and the polymer forms a ____ around the tablet.
GEL LAYER
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
the drug ____ through the gel layer
diffuses
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
the ____ gel layer becomes completely hydrated
outer
EMBEDDING DRUG IN SLOWLY ERODING OR HYDROPHILIC MATRIX SYSTEM
the outer gel layer erodes and a ____ will form with any polymer still remaining in the tablet
new gel layer
Embedding drug in an INERT PLASTIC MATRIX such as ____, ____, or ____
polyethylene
polyvinyl acetate
polymethacrylate
- Drug is slowly released from the plastic matrix by leaching into the body fluids
- The granulation is compressed into tablet, the immediate release portion at the surface of the tablet.
- Examples: Ferro-Gradumet iron supplement
EMBEDDING DRUG IN INERT PLASTIC MATRIX
EMBEDDING DRUG IN INERT PLASTIC MATRIX
The granulation is compressed into
TABELT
EMBEDDING DRUG IN INERT PLASTIC MATRIX
the immediate release portion at the ____ of the tablet
surface
- Drug substances are combined with other chemical agent to form complexes that may be only slowly soluble in body fluids
- The slow dissolution provides the extended release of the drug
- liquid preparations only
- Example: Rynatan (Chlorpheniramine and phenylephrine) antihistamine
COMPLEX FORMATION
Ferro-Gradumet iron supplement
EMBEDDING DRUG IN INERT PLASTIC MATRIX
Rynatan (Chlorpheniramine and phenylephrine) antihistamine
COMPLEX FORMATION
- A complex of resin-drug is formed; tabletted, encapsulated or suspended in an aqueous vehicle
- The release of the drug is dependent upon the pH and the electrolyte concentration in the GIT
- Examples:
Hydrocodone polistirex and chlorpheniramine polistirie suspension (Tussionex
Pennkinetic Extended Release Suspension) cough preparation
Phentermine Resin Capsules (Ionamine) weight loss
ION EXCHANGE RESINS
RYNATAN
ANTIHISTAMINE
FERRO GRADUMET
IRON SUPPLEMENT
Hydrocodone polistirex and chlorpheniramine polistirie suspension (Tussionex
Pennkinetic Extended Release Suspension) cough preparation
Phentermine Resin Capsules (Ionamine) weight loss
ION EXCHANGE RESIN
Pennkinetic Extended Release Suspension
cough
Phentermine Resin Capsules (Ionamine)
weight loss
pioneer oral osmotic pump delivery system
OROS SYSTEM
Composed of a core tablet surrounded by a semi-permeable membrane coating having a ”hole.”
* Core tablet:
(1) “ACTIVE” layer – containing the drug
(2) “PUSH” layer – containing the polymeric osmotic agent
OSMOTICALLY CONTROLLED SYSTEMS
OSMOTICALLY CONTROLLED SYSTEMS
containing the drug
ACTIVE LAYER
OSMOTICALLY CONTROLLED SYSTEMS
containing the polymeric osmotic agent
PUSH LAYER
OSMOTICALLY CONTROLLED SYSTEMS
the hole is produced by
laser beam
Ocular Pilocarpine therapeutic system which releases medication over a 7-day period in the treatment of glaucoma
common in diabetic patients
ocusert
Inserts for for the treatment of dry eyes
lacrisert
inserts that contains dinoprostone for the induction of labor
cervidil vaginal insert
Inserts that contains progesterone used to assist reproduction
crinone gel
Vaginal ring containing estradiol for the treatment of urogenital symptoms associated with postmenopausal atrophy of the vagina
estring
Solid dosage form designed to be inserted under the skin by special injectors or by** surgical incisions**
implants
Implants that contains goserelin acetate for the treatment of advanced prostatic cancer
zoladex
Implants that contains levonorgestrel that provides up to 5 years contraception
norplant system
long lasting effect preparations
depo