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Drug Delivery Systems Exam 2
DDS
61
Pharmacology
Graduate
10/21/2012

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Cards

Term
ETA (ethylene diamine tetraacetic acid)
Definition
This is a chelating agent- part of methods to enhance permeability: it scavanges for free metals
Term
Magnesium Stearate
Definition
Used as a lubricant (part of ingredients in typical tablet formulation)
Term
Corn starch
Definition
This is a a type organic dilutent. It is also a diluent, a binder (paste, hydrolyzed), and a type of disintegrator
Term
Colloidal silicon dioxide
Definition
This is a type of glidant- this is called Cab-O-Sil by Cabot
Term
gelatin
Definition
This is what capsules are contained in. This gelatin is usually derived from animals. Used for improved bioavailability. There is both hard and soft gelatin capsules. in order to prepare hard gelatin capsules, there are metallic pins that are removed and dried, there are shells (cap and base) that are stripped from the pins. They are then cut to proper length for given capsule size and then the pins for caps. Basic steps: 1. calculate the amount of drug and other ingredients required to make a given number of capsules. 2. mix all ingredients 3. Fill the capsule base 4. place the cap on base 5. clean the filled capsules. With soft gelatin capsules- there is sufficient plasticizer (glycerin or sorbitol) to retain flexibility.
Term
Talc
Definition
This is a type of lubricant
Term
Surcrose
Definition
You can include surcrose into a formulation in order to received effects of sustained release. This is also involved with Klucel, a type of binder. Also note that micro-organisms cannot grow in hypertonic solutions (67% sucrose in syrups)
Term
Calcium stearate
Definition
This is a type of lubricant
Term
Stearic Acid
Definition
This is a type of lubricant
Term
HPMC
Definition
This can be used as an alternative material to gelatin. this is a water soluble polymer (example is capsugel-VCAP)
Term
Sodium Lauryl Sulfate
Definition
Surfactant (part of industrial manufacture of hard gelatin capsules)
Term
PVP (polvidone)
Definition
This is a type of binder, an ingredient typically used in tablet formulation
Term
Croscarmellose sodium (by avedbe)
Definition
This is a type of superdisintegrant
Term
propyl paraben
Definition
?
Term
Benzalkonium Bromide
Definition
? antimicrobial?
Term
xanthan gum
Definition
?
Term
Sorbitol
Definition
a type of plasticizer to retain flexibility in soft gelatin capsules (these are like fish oils or vitamin E)
Term
Microcrystakkube cellulose
Definition
This is used for film coating( used in lustreClear (FMC))- helps in an advantage for a patient
Term
Dicalcium phosphate
Definition
This is used as an inorganic diluent
Term
Sodium starch glycolate
Definition
This is a type of super disintegrant that is in primojel by Avebe
Term
Mannitol
Definition
This is an organic diluent. This is also used for soluble chewable tablets
Term
tween 80/polysorbate 80
Definition
this is a nonionic surfactant
Term
Sodium bicarbonate
Definition
This is for effervescent tablets (granules)- used as a base
Term
Important physiochemical properities of a drug
Definition
aqueous solubility
dissolution rate
partition coefficient
permeability
ionization constant
polymorphism
crystallinity
particle size
particle morphology
surface area
hygroscopicity
and chemical stability!
Term
Why is the oral route so popular?
Definition
*most convenient form of admin for ambulatory and conscious patients
*most cost effective from perspective of manufacturing, storage, and handling
*offers great flexibility in dosage regimen
Term
Oral route: compartments of the G.I tract
Definition
Mouth: good for various routes

Esophagus: very short transit time

Stomach: Major barrier

Small intestine: Main target

Colon: potentially useful target
Term
Buccal
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
Definition
PH:about 7
Membrane:thin
Blood Supply:good, fast, absorption w/ low dose
Surface Area:small
Transit Time: short unless controlled
Bypass Liver:yes
Term
esophagus
give:
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
Definition
PH:5-6
Membrane: very thick, no absorption
Blood Supply: -
Surface Area: small
Transit Time: short
Bypass Liver:-
Term
Stomach:
give:
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
Definition
PH:1-3 decomposition, weak acid unionized
Membrane:normal
Blood Supply: good
Surface Area: small
Transit Time: 30-40 minutes- reduced absorption
Bypass Liver:no
Term
Duodenum
give:
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
Definition
PH:6-6.5 bile duct, surfactant properties
Membrane:normal
Blood Supply: good
Surface Area: very large
Transit Time: very short (6" long window effect)
Bypass Liver:no
Term
Small intestine
give
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
Definition
PH:7-8
Membrane:normal
Blood Supply: good
Surface Area: very large (10-14 ft 80 cm^2/cm)
Transit Time: about 3 hrs
Bypass Liver:NO
Term
Large intestine
give
PH:
Membrane:
Blood Supply:
Surface Area:
Transit Time:
Bypass Liver:
Definition
PH:5.5-7
Membrane:-
Blood Supply: good
Surface Area: not very large (4-5ft)
Transit Time: long, up to 24 hour
Bypass Liver:lower colon, rectum, yes
Term
ml of the GI:
stomach
duodenum
SI
LI
Definition
Stomach: 1,500ml
Duodenum: 2,000ml
SI: 5,500ml
LI: 1,300ml
Term
difference between buccal and SL delivery?
Definition
*some drugs are taken as smaller tablets which are held in the mouth or under the tongue (these are buccal/sl)
*buccal tablets are often harder tablets (4hr disintegration time) designed to dissolve slowly
*nitroglycerin- softer Sl tablet(2min disintegration time) may be used for the rapid relief of angina
Term
Advantages of buccal delivery
Definition
*the mucosa is well supplied with both vascular and lymphatic drainage
*first-pass metabolism and presystemic elmination of the GI tract are avoided
* the are is well suited for retentice device and appears acceptable to patients
*the permeability and the local environment of the mucosa can be controlled and manipulated to accommodate drug permeation
*promising area for systemic delivery of orally inefficient drugs as well as an attractive alternative for noninvasive delivery of potent peptide and perhaps protein drug molecules
*the need for safe and effective buccal permeations and absorptions enhancers is crucial component for a promising future in the area of buccal drug delivery.
Term
disadvangtages of buccal drug delivery
Definition
*holding the dose in the mouth is inconvenient
*if any swallowed- oral and first pass affected
*small doses only can be accommodated easily.
Term
Why would someone oppose to gelatin in their capsules?
Definition
They are religious, vegan, worried about mad cow disease
Term
Hard gelatin advantages
Definition
versatile
conceal odor/mask taste
flexible
easily administered
easily filled
placeboes
very few ingredients (f)
elegant
Term
Drum
give:
Mixing mech:
Segregation:
axial mixing:
ease of emptying:
segregation on emptying:
Definition
Mixing mech: diffusive
Segregation:bad
axial mixing:bad
ease of emptying:bad
segregation on emptying: bad
Term
V-mixer

give:
Mixing mech:
Segregation:
axial mixing:
ease of emptying:
segregation on emptying:
Definition
Mixing mech: diffusive
Segregation:bad
axial mixing:bad
ease of emptying:good
segregation on emptying:bad
Term
Cone

give
Mixing mech:
Segregation:
axial mixing:
ease of emptying:
segregation on emptying:
Definition
Mixing mech: Diffusive
Segregation:Bad
axial mixing:Bad
ease of emptying:good
segregation on emptying:bad
Term
Ribbon
give:
Mixing mech:
Segregation:
axial mixing:
ease of emptying:
segregation on emptying:
Definition
Mixing mech: Convective
Segregation: Good
axial mixing:Slow
ease of emptying:Good
segregation on emptying:Fair
Term
Fluidize
give:
Mixing mech:
Segregation:
axial mixing:
ease of emptying:
segregation on emptying:
Definition
Mixing mech: Convective
Segregation:fair
axial mixing:good
ease of emptying:good
segregation on emptying: good
Term
Screw
Give:
Mixing mech:
Segregation:
axial mixing:
ease of emptying:
segregation on emptying:
Definition
Mixing mech: Shear
Segregation:Bad
axial mixing:good
ease of emptying:good
segregation on emptying: bad
Term
Why hard gelatin capsules are made to lock one the cap is firmly placed on the body of the capsule
Definition
There was poisonings that were going on because someone was able to open up the manufacturer's capsules and split inside bad things such as poison
Term
Advantages of a compressed tablet as an oral drug delivery system
Definition
*great variety in size and shape for different dosage
high speed equipment for timely large scale manufacturing at minimal cost per dose compared to liquid and capsules
*Various options for controlling release characteristics
Term
Advantages of compressed tablets for the patient
Definition
*accuracy of dosing
*blandness of taste
*sugar coating
*enteric coating
*film coating
*scored (grooved)
*formulated- chewable/soluble dosage forms
*formulated to have variable/DR rates
*elegant
*efficient, versitile, practical
Term
Tablet disadvantage
Definition
*inflexible dosage form
*not prepared extemporaneously
*large # of ingredients
*dissolution of drug
*drug sensitive to moisture, oxygen, light
Term
What is the difference between compressed and molded tablets?
Definition
*molded tablets requires heat?????
Term
Three method to tablet manufacturing
Definition
direct compression
*for drugs with:
*have large doses
*are free flowing crystalline substances
*have cohesive properties
advantages
-simplicity and time
-no prior granulation
avoid:
+moisture
+heat
+both
wet granulation
Procedure-
*mix
*add binding solution
*wet screening
*drying
*dry screening
*add remaining ingrediant
*press tablets
*coat tablets
dry granulation
*mix
*make slugs
*form granules
*dry screen
*add remaining ingrediants
*pressed into tablets
Term
CT
SCT
FCT
ECT

What is the difference?
Definition
CT: Compressed tablet

Sct: Sugar coated tablet

FCT: Film coated tablet

ECT: Enteric Coated tablet
Term
Common flow problems
Definition
*non-uniform flow causing unacceptable tablet weight uniformity
*uneven flow causing segregation of ingredients
*need for force feeders,vibrators, custom hoppers
*non reproducible manufacturing operations

*low process yields due to inefficient material handling and high reject levels
Term
What is the purpose of tablet coating?
Definition
used to mask unpleasant taste, protect tablet ingredients during storage, or improve the tablet appearance
Term
What are the two most commonest tablet coatings and how are they different?
Definition
sugar vs film

film coating
may or may not have enteric coating properties
Term
Why dissolution testing is done on solid oral doseage form as part of quality control process and as predictor of in vivo drug performance
Definition
It is done for quality control in order to assess process control, batch-to-batch quality, and batch release??????
Term
What is the difference between dissolution and solubility
Definition
noyes-whitney equation shows that aqueous solubility of drug determines the dissolution rate

dissolution is a process in which a solid substance solubilizes in a given solvent ie mass transfer from the solid surface to the liquid phase.

the rate of dissolution is the amount of drug substances that goes in solution per unit time under standardized conditions of liquid/solid interface, temperature and solvent composition
Term
How can the factors in the noyes and whitney equation be manipulated to increase or decrease the drug dissolution from tablets?
Definition
*diffusion coeff- decrease in presence of substance that increase viscosity (negative)
* area of exposed solvent (increased by micronization) +

Thickness of disffusion layer: decreased by increased agitation in gut/flask (+)

Solubility in diffusion layer: changing crystal form, PH, salt form, or adding buffer component
* concentration in bulk- decreased by intake of fluic, by rapid removal of drug or absorption (+)

*thickness diffusion layer (decreased by increased agitation in gut/flask)

*solubility in diffusion layer (changing crystal form, PH, Salt form, or adding buffer component) (-/+)
Term
Difference between the paddle and Basket method?
Definition
Term
BCS
Definition
*Class 1= High Sol, High Perm
IVIVC= no
When disolution rate>gastric emptying, dissolution is not likely to be rate limiting.

*Class II- Low Sol, High Perm
IVIVC= yes

Class III-high solubility, Low permeability
IVIVC= no

*Class IV= Low solubility, Low permeability
RLS:various factors
in vitro dissolution may not be reliable
IVIVC: maybe
Term
What are the properties of a drugs measure in order to determine the BCS class of a drug?
Definition
Solubulity, permeability????
Term
What is IVIVC?
Definition
mathematical model describing the relationship between in vitro and in vivo properties of a drug

in vitro- in vivo correlation can be achieved using
pharmalogical correlation
semi-quantitative correlation
quantitative correlation
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