Term
| Describe therapeutic window |
|
Definition
area between MINIMUM EFFECTIVE CONCENTRATION and MINIMUM TOXIC CONCENTRATION
blood concentration of drug that is safe AND effective |
|
|
Term
| describe graph of controlled release |
|
Definition
prolonged and flat curve
drug is released independent of amount of drug in the formulation
not a function of how much drug is in delivery system |
|
|
Term
| describe graph of sustained release |
|
Definition
prolonged curve (like a hill)
releases drug as a function of amount of drug |
|
|
Term
| What is better: small or large therapeutic window? |
|
Definition
|
|
Term
| how do you classify a small therapeutic window? |
|
Definition
|
|
Term
| Describe concentration constant of immediate release |
|
Definition
| K release>>>>>K absorption |
|
|
Term
| 2 kinds of formulations of sustained release |
|
Definition
1) Barrier/Reservoir (polymer coating)
2)Matrix (drug is mixed in with polymer) |
|
|
Term
|
Definition
| Crushing a sustained release tablet with a barrier formulation: all drug is released at once DANGER |
|
|
Term
| What are ghosts in the stool |
|
Definition
| polymer leftovers in sustain released tablet that are in matrix formulation |
|
|
Term
| Which sustained release tablet causes dose dumping when crushed? |
|
Definition
|
|
Term
|
Definition
Control Released Tablet
Tablet consists of active ingredient, osmotic agents (salts), and a film coat (which is semi permeable) |
|
|
Term
| Mechanism of Controlled Release tablet? |
|
Definition
semi permeable film coat is permeable to water, but not drug
laser cuts hole
water flows thru membrane (bc of salts)
osmotic pressure increases, and drug flows out |
|
|
Term
| 2 types of chemical drug delivery design approaches |
|
Definition
Make drugs as salt form
Make drug as prodrug |
|
|
Term
|
Definition
| Active ingredient + Chemical structure |
|
|
Term
| 3 reasons why we use ProDrugs? |
|
Definition
1) increases active drug bioavailability
2) Increases stability of active ingredient
3) Targeted Delivery |
|
|
Term
| What does prodrug epinephrine (for glaucoma) do? |
|
Definition
| allows 100% bioavailability |
|
|
Term
| What does Prodrug Erythromycin do? |
|
Definition
| increases stability of active ingredient |
|
|
Term
| What does Sulfasalazine do? |
|
Definition
Aids in targeted delivery of 5-ASA to surface of small intestine tissue
(prevents absorption through stomach) |
|
|
Term
| How does epinephrine become more bioavailable? |
|
Definition
| esterification>>>lipophilic |
|
|
Term
| 2 examples of biological drug delivery design approaches? |
|
Definition
1) Normal physiology (insulin)
2) Immune response (monoclonal Antibodies) |
|
|
Term
| 4 diffusion-based variables |
|
Definition
viscosity
temperature
size of particle
charges |
|
|
Term
| What is the Nernst equation for Dissolution? |
|
Definition
Rate of Dissolution (dM/dt) = A (Kd) (Cs - CB)
=Surface area x Diffusional term x (concentration at surface - concentration in bulk) |
|
|
Term
| What is the diffusional term in the Nernst Equation? |
|
Definition
| Diffusion coefficient/diffusion layer thickness |
|
|
Term
| what results from stirring? |
|
Definition
| strips away diffusion layer (decreases thickness) and increases rate of dissolution |
|
|
Term
| Explain what happens in a depot injection |
|
Definition
| Into muscle>>>slow blood flow>>>drug isn't being removed by blood>>>Cs = CB >>>Cs-Cb=0>>>Release of drug stops |
|
|
Term
|
Definition
| made really big particles to minimize number of particles and slow the release of the drug to minimize nausea |
|
|
Term
|
Definition
Puts a coating on Aspirin that is not soluble in the stomach
It becomes soluble in the small intestine (bc of the pH difference) so aspirin dissolves |
|
|
Term
|
Definition
characterizing physical and chemical propeerties of the drug
(ie site of delivery/dosage form) |
|
|
Term
|
Definition
developing the dosage form, small scale
like a recipe |
|
|
Term
| hard capsule: wall thickness? |
|
Definition
|
|
Term
| soft capsule: wall thickness? |
|
Definition
|
|
Term
| which has more water: hard or soft capsule? |
|
Definition
|
|
Term
| which has a plasticizer: hard or soft capsules? |
|
Definition
|
|
Term
| method for tamper-proofing of hard capsules? |
|
Definition
|
|
Term
| what does oooo mean? (four circles) |
|
Definition
| high number = small capsule |
|
|
Term
| 2 Manual methods for capsule filling? |
|
Definition
1) Punch and Weight
2) Hand Press |
|
|
Term
| What is the automatic process for capsule filling? |
|
Definition
Zanazi Capsule Filling Machine
dosator |
|
|
Term
| Name formulations of hard capsules: |
|
Definition
| immediate, sustained, and delayed/enteric release |
|
|
Term
| 3 reasons to use soft gelatin capsules? |
|
Definition
1) Mask taste/smell
2) Stability (light/water)
3) Bioavailability |
|
|
Term
|
Definition
| soft gelatin capsule to improve bioavailability of Digoxin |
|
|
Term
| what is the mechanism of release of a soft gelatin capsule |
|
Definition
| Hydrostatic pressure increases and the seal ruptures>>>immediate release |
|
|
Term
| side effect of soft-gelatin capsule |
|
Definition
|
|
Term
| what is the range of volume that a soft gelatin capsule will hold |
|
Definition
|
|
Term
| why are soft gelatin capsules expensive? |
|
Definition
| it's a specialized process |
|
|
Term
| 4 solvents used in soft gelatin capsules: |
|
Definition
1) oils
2) glycol (PEG)
3) alochols (isopropyl)
4) w/o emulsion |
|
|
Term
| 2 solvents that cannot be used in soft gelatin capsules? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| what dosage forms are microcapsules? |
|
Definition
| injectable and dermatology |
|
|
Term
| example of cosmetic use of microcapsule: |
|
Definition
| RetinA micro (moisturizer) |
|
|
Term
| example of oral microcapsule |
|
Definition
|
|
Term
|
Definition
| attraction of hydrophilic polymers of opposite charge and phase separation occurs |
|
|
Term
| how do you make microcapsules? |
|
Definition
Have 2 different gelatins with different pKI's
put one gelatin in water with the drug
add the other gelatin with water and acid
Stir
Gelatin Sheet forms>>>cross-links of aldehydes makes shells rigid |
|
|
Term
| 3 disadvantages of tablets |
|
Definition
poor compression
poor bioavailability
tough to mask odor |
|
|
Term
| how is size and shape of tablet achieved? |
|
Definition
|
|
Term
|
Definition
measure of degree to which a tablet chips/loses particles
high friability = chips easily |
|
|
Term
| describe the breakdown of an immediate release tablet |
|
Definition
tablet disintegrates into granules
granules deaggregate into small particles>>>dissolution into drug in solution and become bioavailable |
|
|
Term
| what does a diluent/filler do? |
|
Definition
|
|
Term
|
Definition
| promotes cohesion for granules/slugs |
|
|
Term
|
Definition
| prevent ssticking to die walls |
|
|
Term
|
Definition
| prevent sticking to punch faces |
|
|
Term
|
Definition
| improve powder flowability |
|
|
Term
|
Definition
| facilitate disintegration in presence of moisture |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
| how long does wet granulation take |
|
Definition
|
|
Term
| what is the most time consuming and most commoonly used method of tableting |
|
Definition
|
|
Term
| what is dry granulation used for |
|
Definition
| drugs that are not good for direct compression and are hydrolyzed in water |
|
|
Term
| which compresses better: powder or granules? |
|
Definition
|
|
Term
| which granulation uses ribbons (roller compactor) |
|
Definition
|
|
Term
| how long does direct compression take |
|
Definition
|
|
Term
|
Definition
1) aesthetics (taste, odor)
2) Functional (logo, number) |
|
|
Term
| 2 types of tablet coating |
|
Definition
| sugar coating and film coating |
|
|
Term
|
Definition
| very thick-adds weight to tablet |
|
|
Term
|
Definition
|
|
Term
| what is film coat made of |
|
Definition
latex
polymer dispersed in solvent |
|
|
Term
| when is a plasticizer used in tablet coating? |
|
Definition
| in film coating to keep from breaking |
|
|
Term
| what is purpose of surfactant in film coating? |
|
Definition
|
|
Term
| what is a Wurster coater? |
|
Definition
fluidized bed
tablets are suspended (air pressure) and coated by a spray, then they fall back down |
|
|
Term
| 2 advantages of using Wurster coater? |
|
Definition
1) no attrition/sticking
2) coat more tablets at a time |
|
|
Term
|
Definition
| when top comes off of tablet |
|
|
Term
|
Definition
| striations through tablet |
|
|
Term
|
Definition
| when the surface isn't completely smooth |
|
|
Term
|
Definition
| variation in color of tablet |
|
|
Term
| If mottling of an IR tablet occurs... |
|
Definition
|
|
Term
| Mottling of functional coat... |
|
Definition
|
|
Term
| what is orange peel effect? |
|
Definition
when coating was dried too quickly
if it's a functional coat, don't fill it |
|
|
Term
| characteristic of buccal/sublingual |
|
Definition
| no disintegrants bc we don't want to swallow the drug in the saliva |
|
|
Term
| characterisitc of troches and lozenges |
|
Definition
| no disintegrants (local anestheticK) |
|
|
Term
| characteristic of effervescent tablet |
|
Definition
| > H2O>>>degrades (gives off CO2) |
|
|
Term
| what effects do organic salts cause |
|
Definition
| make it less soluble and therefore slows drug dissolution |
|
|
Term
|
Definition
|
|
Term
| mechanism of hard gelatin capsule release: |
|
Definition
| dissolution of capsule shell |
|
|
Term
| 3 examples of enteric coating |
|
Definition
cellulose acetate phthalate (CAP)
polyvinyl acetate phthalate (PVAP)
hydroxypropyl methylcellulose phthalate (HPMC-P) |
|
|
Term
| 2 examples of sugar-coated tablets |
|
Definition
multii-vitamines
sudafed tabs |
|
|
Term
| how long does it take to sugar coat a tablet |
|
Definition
|
|
Term
| describe composition of film-coat |
|
Definition
| polymer, plasticizer, surfactant |
|
|
Term
| how long does it take to make film coat |
|
Definition
|
|
Term
| what is used as the solvent for film coats |
|
Definition
|
|
Term
| How does a tablet qualify as being enteric-coated? |
|
Definition
| 6 enteric-coated tablets placed in separate compartments remain intact after 30 miniutes of exporsure to gastric fluid |
|
|
Term
| of film-coated and sugar coated, which has stronger, more elastic, more fleixble coat? |
|
Definition
|
|
Term
| increase type of coat increases the tablet weight by a lot |
|
Definition
|
|
Term
| which coat has a thick coat |
|
Definition
|
|
Term
| disadvantage of film-coat? |
|
Definition
|
|
Term
| purpose of chewable tablet? |
|
Definition
| administered to children or elderly |
|
|
Term
| buccal/sublingual tablets: what kind of effect? |
|
Definition
|
|
Term
| sublingual/buccal tabs: faster or slower onset of action? |
|
Definition
|
|
Term
| troches and lozenges: what kind of effect? |
|
Definition
|
|
Term
| purpose of implantation tablets: |
|
Definition
| provide prolonged drug effects |
|
|
Term
| describe composition of effervescent tabs |
|
Definition
| active ingredients plus organic acid |
|
|
Term
| what are tablet triturates |
|
Definition
|
|
Term
| what are dispensing tablets used for? |
|
Definition
| incorporated (through compounding) into powders or liquids |
|
|
