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compressed tablets
compressing granules formed from powder particles into definite shape, made of AI and II, inactive ingredients usually take up most space
what excipients do compressed tablets have
diluents (fillers) to add bulk for shape, binders (adhesives) to keep integrity of tablet shape, disintegrators to promote breakup after administration, glidants to enhance flow before compression, lubricants to prevent sticking (also gives sheen), flavorants and colorants
tablet diluent examples
dicalcium phosphate, calcium sulfate, lactose, cellulose, kaolin, mannitol, starch, glucose
tablet binder examples
starch, gelatin, sugars (sucrose, lactose, maltose, dextrose), gums like acacia, sodium alginate, carboxymethylcellulose (CMC), methylcellulose, polyvinylpyrrolidone, veegum, waxes
tablet lubricant examples
sodium benzoate, leucine, carbowax 4000, magnesium lauryl sulfate
tablet glidant examples
silica, colloidal silicon dioxide, talc sometimes
tablet disintegrant examples
starches, clays, celluloses, algins, gums, corn, potato starch
tablet flavorant examples
aspartame
coated tablets
sugar-coated tablets, film-coated tablets, enteric-coated tablets
sugar-coated tablets
mask taste, if too objectionable will be made into capsule, enhance appearance, increase size by 50%, Advil
film-coated tablets
more durable and less bulky, polymers (poly vinyls and celluloses) that will disintegrate in gastric juices, Viagra
enteric-coated tablets
resists acidic pH of stomach, popular for acidic or caustic medications that may irritate sensitive stomach, Ecotrin
sublingual tablets
flat and oval, dissolve under tongue or buccal pouch, useful for medications destroyed by gastric juices and medications that need quick onset (nausea), Nitrostat, Suboxone film
chewable tablets
people who cannot swallow tablets, palatable, not compacted so easy to chew, effervescent tablets
effervescent tablets
citric acid gives fruity taste, easier to drink, Theraflu, Prilosec packets, usually OTC
tablet triturates
not used as much, basically sublingual, closest compounded pellet tablet, Nitrostat is closest example
what do inactive ingredients do in a tablet?
hold the tablet together until swallowed, absorb gastric juices, disintegrate tablet, help with dissolving of particles in gastric solution
wet granulation
blend AI with disintegrants and fillers, add liquid binder, screen into granules (pellets), spread gloop on trays for drying, dry the granules, add lubricants and blend, compress tablet
dry granulation
blend AI and additives together, roll crush and sieve powders, lubricant is blended, resultant powder compressed into tablet
direct compression
materials have free flowing characteristics and cohesive properties, no need to make granules
what is the purpose of granules?
make powdered drug ingredients easier to handle and manufacture into a dosage form
friability test
test for tablet hardness, friability is tendency of tablet to break under stress, hardness = USP 1216
hard gelatin capsules
gelatin, sugar, water, and colorant, similar lubricants to those in tablet compression, no need for adherents, comes from collagen of white connective tissue and bones of animals, soluble in hot water, in gastric fluids the gelatin is digested and absorbed, for size a higher number = smaller capsule, has banding for tamper proof, long body and short cap
soft gelatin capsules
hard gelatin formula but with glycerin or sorbitol, flexible, usually contains suspensions or liquids, not compounded in pharmacies, requires elaborate equipment, vitamin d3, OTC docusate sodium
what is the Noyes Whitney principle of dissolution?
the rate of dissolution of solids depends on the rate of diffusion of a very thin layer of saturated solution that forms around each solid particle
what is sink condition?
a drug is instantaneously absorbed as soon as it dissolves
what factors influence drug dissolution?
particle size and surface area, unionized and ionized, drug formulation, gastric emptying and intestinal transit times
what is the relationship between surface area and dissolution?
direct, as particle size decreases surface area increases
compare solubilities of salt forms and “free” acids or bases
salt forms (N+, Cl-) of weak bases or acids are more water soluble than the unionized form
compare and contrast increasing pH or decreasing pH on degree of ionization and unionization for acids and bases
acids = when pH decreases, ratio moves tenfold in favor of unionized, 1 molecule of ionized : 10 molecules unionized
bases = when pH decreases, ratio moves tenfold in favor of ionized, 1 molecule unionized : 10 molecules ionized
distinguish the role of gastric emptying time on drug dissolution
time is inversely proportional to rate, gastric emptying time is shorter when fasting vs with food
what is liberation of drug from a dosage form?
liberation happens prior to absorption, drug must be “liberated” from dosage forms, then particles must dissolve in body fluids
what is molarity?
moles of solute per 1000 mL of solvent
what is molality?
moles of solute in 1000g of solvent
what is normality?
the gram equivalent weight of solute in 1000 mL of solvent
what is osmotic pressure?
movement of pure solvent into solution in an attempt to dilute the solute in the solvent and raise the vapor pressure back to its original value, the pressure needed to push against the pure solvent to prevent movement of pure solvent into the solution
vapor pressure vs particles
the presence of particles in solution causes vapor pressure to decrease
what does isosmotic mean?
when two solutions have the same osmotic pressure
what is the Van’t Hoff (i) factor and how is it used?
solutions of electrolytes produce more osmotic pressure, i accounts for the contributions of ions in solution
how does the knowledge of freezing point depression help in calculating isotonicity?
you can test freezing point of medicine, if it freezes below what is expected (-0.52) then it is NOT isotonic
what is the utility of the sodium chloride equivalent (E value)?
most medicinal salts approximate the extend of dissociation of sodium chloride in weak solutions, E is the factor that relates the needed weight of NaCl that would have the same freezing point depression as 1 gram of drug in 1000 mL, E is an evaluation of the relative ionic strength of the API compared to NaCl
sodium chloride (E) equation
(MW NaCl / (i NaCl) x (i of API / MW substance)
if the E value of 1 g of atropine sulfate in a 100 mL solution is 0.12, what does that mean?
the osmotic pressure generated by 1 gram of atropine is the same osmotic pressure generated by 0.12 g of NaCl
what is osmolarity?
the concentration of a solution expressed as number of particles per liter, molar concentration and osmotic pressure
how is tonicity a function osmolarity?
as mOsmol increases, more tone is exerted, range is 240-340
what is a “mol”?
6.02 × 10²³ particles, the molecular weight of a substance in g
what is a milliequivalent?
the concentration of electrolytes in a solution, VALENCE
what terms of this section are influenced by charge?
mEq, valence, electrolytes
what terms of this section are influenced by species?
Osmol, Van’t Hoff, i, osmotic pressure
what terms of this section are influenced by mass?
normality, equivalent weight
intraarticular
into/between articulating joints
intraspinal/intrathecal
directly into cerebral spinal fluid
intravenous
into veins
thrombus
blood clot formed in vessel due to slowing of bloow flow
embolus
circulating thrombus
embolism
an embolus obstructs a vessel which creates a blockage
pulmonary embolism
obstruction in microvasculature of lungs
intramuscular
into muscle, vaccines, most common route for pharmacists, deltoid/quadricep/gluts
subcutaneous
under the skin, insulin products, usually self-administered
6 solvents
sterile water for injection, bacteriostatic water for injection, sodium chloride for injection, bacteriostatic sodium chloride, ringer’s solution, lactated ringer’s solution
sterile water for injection
less than 1-L package (50, 100, 250, 500 mL), used topically for rinsing
bacteriostatic water for injection
antimicrobial, less than 30mL, do not give to baby, multi-dose vials
sodium chloride for injection
sterile, isotonic solution of NaCl, no antimicrobials
bacteriostatic sodium chloride for injection
NaCl with added antimicrobial, less than 30mL, multi-dose vials, do not give baby
ringer’s injection
sterile solution of sodium chloride, potassium chloride, and calcium chloride, vehicle for injection or fluid replenisher (no drug)
lactated ringer’s injection
sterile solution of sodium chloride, potassium chloride, calcium chloride, sodium lactate, vehicle for injection, fluid replenisher (no drug)
what parentals do pharmacists administer
intramuscular
what parentals do patients administer
subcutaneous (insulin)
what is SNAC in semaglutide and how does it function?
a penetration enhancer that increases pH in stomach (protects semaglutide from acid), affects transcellular pathways that allow HUGE molecule to be absorbed in stomach
radiopharmaceuticals decay at what rate order? what does that mean?
first order rate, rate of decay is dependent on concentration, high concentration = rate increase
2 examples of radiopharmaceuticals discussed in class
Technetium-99 (99Tc) and sodium iodide 123
what are the time limitations of compounding radiopharmaceuticals?
around 30 hours
importance of isotonicity in ophthalmic
isotonicity is required to prevent tissue damage
general technique of instilling ophthalmic drops
wash hands, pull eyelid down, drop medication inside lower eyelid while looking up, slowly close eye, use tissue to wipe away liquid, wait 10 minutes before next administration
general technique of instilling ophthalmic ointment
wash hands, lower eyelid, look up, squeeze ¼ inch ribbon into lower eyelid, close eye and rotate eyelid, wait 10 minutes before next administration
tan cap
anti-infective
gray cap
nonsteroidal anti-inflammatory
pink cap
steroid anti-inflammatory
dark blue cap
beta blocker/combo
yellow cap
beta blockers
orange cap
carbonic anhydrase inhibitors
dark green cap
miotic (shrink pupil)
red cap
mydriatics (dilate pupil)
turquoise cap
prostaglandin analog
purple cap
adrenergic agonist, treats glaucoma
gel-forming – reasons to use
stay in eye longer, ER
nasal – technique and use of gels to increase contact time
insert into nose and tilt to the side, gels stick to inner nares and increase contact of medication
compare and contrast sterility and pH and tonicity between ophthalmic and otic
ophthalmic has to be sterile and otic does not, otic has lower pH and ophthalmic has close to 7, want isotonicity in eye and ear
what are the factors affecting percutaneous absorption?
drug concentration, surface area, attraction of the drug to the skin over the vehicle, molecular weight, hydration of skin, skin thickness, contact time, penetration enhancers manipulation of TDDS
how do skin penetration enhancers function?
encourage skin to take up more drug, chemicals help move large molecular weight drugs across skin
what are the differences between the reservoir patch and the matrix patch?
reservoir - four layer system with backing, reservoir of drug, membrane, and adhesive with usually some drug, large excess of drug, dose dumping, gel patches, transderm scop, fentanyl
matrix - no reservoir, drug dispersed in adhesive, tape patch
what is compounding?
what is NOT compounding?
mixing or altering and existing drug form to create new medication by tailored to individual needs, regulated by state board pharmacy, not large scale, 20 or more to be compounding in 30-day period, cannot be existing drug with adding a couple things to it
USP involvement in compounding
USP 797, 795, 800
SC Board of Pharmacy checklists and requirements
make 20 or less within 30 days = not compounding, reconstituting is not compounding
arguments against compounding
less oversight than FDA, does not need GMP, do not need to be tested for safety and efficacy, do not need to report ADE, may act as manufacturers
quality control
use professional judgement
documentation of compounding
keep for two years
compounding examples and rationale (reason to compound)
aliquot for estradiol, cannot swallow stuff make lollipop, rectal rocket, allergies, cannot use existing dosage, sugar or dye free, do not meet needs
know the classes of Recalls
class I = death
class II = medically reversible effects
class III = labelling/packaging issues
SC Board of pharmacy requirements on recalls
PIC is responsible