dosage form exam 2 – Flashcards
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Unlock answers| 2 steps in dissolution |
1. solute molecules solid -> solute 2. molecules migrate through boundry layer to bulk solution. (think diffusion) |
| how do you change thickness of boundry layer? |
| agitation |
| Surface area and solubility |
bigg SA, more soluble bigger SA, smaller molecule |
| effect diffusion coeficient of solute in media |
viscosity molecular characteristics, size |
| effect dissolution rate constant |
thickness of boundry layer
|
| dosage forms effected by particle size |
oral suspension aerosol topical |
| when is drug better fine than coarse? |
poor water soluble dissolution rate limiting stepin absorption process (eg) grisofulvin |
| whats the rate limiting step |
passing thrugh gut wall NOT lumen |
what makes more amorphous? ball milled or microniser? |
| microniser |
| is insulin-zink suspension amorphous or crystaline? |
| can be either |
Humulin L Humulin U |
L : crystaline 70% amorphous 30% U: all crystaline (ER) |
| what factors effect polymorphism when forming? |
solvent temperature rate of cooling
|
| type of polymorph with greatest disolution rate |
| metastable |
| Hydrate |
| molecule crystalized while in water latice |
| Solvate |
| material crystalized in latice other than water |
| Monohydrate |
| 1 molecule of water per molecule of crystalized material. |
Sieve number for a particle dictates into
|
small number = coarser bigger number = finer |
| decreasing particle size |
comminution trituration
|
| decrease particle size in industry |
hammer mill pebble ball mill fluid energy mill |
| pulverization by intervention |
using extra chemical to help break up chemical easily removed later (eg) alcohol, acetone because evaporation
best for hard crystaline powders, gummy substances
|
| partition coefficient |
rate of diffusion
K = Cu/CL |
| miscibility |
| dependent on polarity of two solvents |
| high K for partition coefficient |
lipophylic greater pass through bio membranes. |
preservatives flavors |
want it in the water system want flavors in highest concentration external phase. |
| biopharmaceutics |
| absorption, distribution |
weak acids: PKA: PH |
ph 2 helow PKA: unionized PH 2 above PKA: ionized |
weak base PH: PKA |
PH 2 above PKA = unionized PH 2 below PKA = ionized |
| salts of weak acids |
Ca Na K |
| salts of weak base |
HCL sulfate nitrate |
| why are salt forms prefered? |
easier to crystalize for stability disolve in water easy handle for processing |
| why buffer dosage formulations? |
lower degredation better comfort/compliance more efficient |
| primary buffer system of the body? |
| proteins |
| tablet lubricant |
| prevent tablets from sticking to die walls |
| tablet anti adherant |
| prevent tablet powder from sticking to punches and dies. |
| Tablet glident |
| improves flow properties of powder mixtures during tablet/capsule processing |
| tablet coating agent |
| coat for usage |
| Plasticizer |
| tablet film coating to make it more pliable, enhancing spreading of coating |
| Lake Dye |
| fat soluble |
| Candurin |
2007 harder to counterfit because pearlescent effect |
ETOH ALcohol USP Dehydrated Alcohol methyl/isopropyl |
Alcohol USP: 96%, used as solvent with water, glycerin Dehydrated alcohol: 99.5%, water free OH, must state OH content on lable, Methyl/isopropyl: cant be used orally |
ETOH age <6 years 6-12 years >12 years |
< 6 years: 0.5% 6-12 years: 5% >12 years: 10% |
| Glycerin |
miscible in water, alcohol, sorbitol, propyleme glycol humectant, levigating agent, suppository base, preservative |
| Tween (sorbitol) |
miscible in water, alcohol, glycerin, propylene glycol emulsifying agent, humectant laxative if > 20g/day |
| Propylene glycol |
miscible in alcohol, water, glycerin, and sorbitol
preservative, humectant, levigating agent
substitute for glycerin
doesn't depress CNS, not volatile |
| Parabens |
preservtive low solubility in water, stable PH 4-8 longer the chain, better preservative |
| Making syrups |
agitation with heat: Fast, risk of breaking down sugars agitation withut heat: safer Percolation: extraction of drug, preparation of syrup |
| Antibue |
metronidazole chlorpropamide glyburide glipizide |
| Aromatic Water |
volatile saturated but not verry water soluble made using talc/distilation |
| Collodions |
Pyroxilen aka nitrocellulose 4% w/v alcohol to ether 1:3 apply to skin for cuts flamable, uncomfortable flexible add camphor and castor oil |
| Elixer |
5-40% bad if patient has drousyness or anibuse ; |
| fluidextracts |
vegetable drugs high OH as solvent 1g/ml not self administered by patient percolation |
| spirits |
volatile 62-85% theraputic aromatic solute simple solution or extraction if aquious solution added, cloudy |
| Tincture |
non volatile 15-80% plant or animal source "extracts dont contain just a single constituent" percolation, maceration |
suspensions: zeta |
particle repulsion.; higher zeta = more stable suspension |
| surface tension |
interaction between liquid and vapor "unbalanced molecular cohesive forces at surface" net atractive force towards bulk of liquid |
| anionic surfactant |
hydrophilic part is - body shampoos topical only sodium laural sulfate |
| cationic surfactant |
cation provides emulsifying property disinfect/preservative only topical/opthalmic incompatible with anionic surfactants combined with non ionic surfactants benzylkonium chloride |
| amphoteric surfactant |
hydrophylic has a + and a - can act as anionic, cationic, nonionic depends on PH of solution rarely the only surfactant N-dodecyl-N-N-dimethyl betaine |
| non ionic surfactant |
hydrophilic part no charge non electrolyte tween, span, peg |
| naturally occuring compounds |
bile salts, phospholipids batch variability, bacterial growth beeswax, wool |
| Bile salt |
made in liver highly surface active ; poorly water soluble drugs.; bile salts raise absorption and bioavailability |
| Phospholipids |
alveolar lining of lungs, tears mix of phospholipids, neutral lipids, proteins ; |
| HLB |
0 = lipophilic 50 = hydrophilic |
| anti foaming agents |
HLB 1-3 dissapates foam by draining liquid |
| wetting agents |
HLB 7-9 lowers contact angle when in water bile salt |
| detergents |
HLB 13-16 lower surface tension, wets surface being cleaned. sodium laural sulfate |
| solubilizing agents |
HLB 16-18 raise solubility CMC "crucial micelle concentration" |
| emulsifying agents |
HLB 3-6, 8-18 reduce tension oil to water |
| flocculating agents |
loose agregation of suspended particles increases sedementation volume prevents caking electrolites, polymers and clays, surfactants store in refrigerator |
| emulsions |
dispensed phase = internal phase (liquid) dispersion phase = external continuous phase topical, oral, and parenteral ; |
| rheology |
non newtonian flow of matter effected by: viscosity of continuous phase phase volume ratio emulsifier droplet size and size distribution |
| types of emulsifiers |
1 surfactants ; 2 hydrophilic colloids: water soluble polymer.; O/W, doesn't lower surface tension, raises viscosity. carbs and geletins
3 Finely divided solid particles: adsorbed at interface, W/O, O/W. magnesium hydroxide. aluminum hydroxide |
emulsion problems Creaming |
separation into two regios, rich, poot less likely if both phases similar less likely if external phase is viscous prevent by storing in refrigerator reverseable eg globules rising to top of product |
emulsion problems coalescence/cracking/breaking |
irreversible film of emulsifying agent surounding droplets broken |
emulsion problems phase inversion |
convert to oposite emulsion type prevented by protecting emulsion from extreme hot/cold |
| microemulsions |
large swolen microcells containing internal phase
between thermodinamically stable, and normal emulsion
10-200 nm diamater
more rapid absorption, topical. |
| magma |
similar to gels suspension of inorganic acids like clay in water "thexotropic rheological behavior" |
| milk |
| suspension in aquious vehicle intended for oral. |
| 2 steps in dissolution |
1. solute molecules solid -> solute 2. molecules migrate through boundry layer to bulk solution. (think diffusion) |
| theory of cavity creation |
| solute makes a cavity for solvent to fit into. (boundry layer) |
| how do you change thickness of boundry layer? |
| agitation |
| Surface area and solubility |
bigg SA, more soluble bigger SA, smaller molecule |
| effect diffusion coeficient of solute in media |
viscosity molecular characteristics, size |
| effect dissolution rate constant |
thickness of boundry layer
|
Sieve number for a particle dictates into
|
small number = coarser bigger number = finer |
| decreasing particle size |
comminution trituration
|
| decrease particle size in industry |
hammer mill pebble ball mill fluid energy mill |
| pulverization by intervention |
using extra chemical to help break up chemical easily removed later (eg) alcohol, acetone because evaporation
best for hard crystaline powders, gummy substances
|
| partition coefficient |
rate of diffusion
K = Cu/CL |
| miscibility |
| dependent on polarity of two solvents |
| high K for partition coefficient |
lipophylic greater pass through bio membranes. |
preservatives flavors |
want it in the water system want flavors in highest concentration external phase. |
| biopharmaceutics |
| absorption, distribution |
non electrolyte
strong electrolyte
weak electrolyte
|
non: doesnt ionize strong: completely ionized, and dissociated weak: ionized, not fully dissociated. |
weak acids: PKA: PH |
ph 2 helow PKA: unionized PH 2 above PKA: ionized |
weak base PH: PKA |
PH 2 above PKA = unionized PH 2 below PKA = ionized |
| salts of weak acids |
Ca Na K |
| salts of weak base |
HCL sulfate nitrate |
| why are salt forms prefered? |
easier to crystalize for stability disolve in water easy handle for processing |
| why buffer dosage formulations? |
lower degredation better comfort/compliance more efficient |
| primary buffer system of the body? |
| proteins |
| Excipient preservatives |
parabens benzoic acid edetate disodium sorbic acid benzokonium chloride |
| Excipient anti-oxidents |
BHA BHT ascorbic acid tocopherol sodium metabisulfate |
| tablet lubricant |
| prevent tablets from sticking to die walls |
| tablet anti adherant |
| prevent tablet powder from sticking to punches and dies. |
| Tablet glident |
| improves flow properties of powder mixtures during tablet/capsule processing |
| tablet coating agent |
| coat for usage |
| Plasticizer |
| tablet film coating to make it more pliable, enhancing spreading of coating |
color FD&C D&C external D&C |
FD&C: food, drugs, cosmetics D&C: drugs & cosmetics external D&C: only used in topical preparations |
| Lake Dye |
| fat soluble |
| Candurin |
2007 harder to counterfit because pearlescent effect |
ETOH ALcohol USP Dehydrated Alcohol methyl/isopropyl |
Alcohol USP: 96%, used as solvent with water, glycerin Dehydrated alcohol: 99.5%, water free OH, must state OH content on lable, Methyl/isopropyl: cant be used orally |
ETOH age <6 years 6-12 years >12 years |
< 6 years: 0.5% 6-12 years: 5% >12 years: 10% |
| Glycerin |
miscible in water, alcohol, sorbitol, propyleme glycol humectant, levigating agent, suppository base, preservative |
| Tween (sorbitol) |
miscible in water, alcohol, glycerin, propylene glycol emulsifying agent, humectant laxative if > 20g/day |
| Propylene glycol |
miscible in alcohol, water, glycerin, and sorbitol
preservative, humectant, levigating agent
substitute for glycerin
doesn't depress CNS, not volatile |
| Parabens |
preservtive low solubility in water, stable PH 4-8 longer the chain, better preservative |
| Making syrups |
agitation with heat: Fast, risk of breaking down sugars agitation withut heat: safer Percolation: extraction of drug, preparation of syrup |
| Antibue |
metronidazole chlorpropamide glyburide glipizide |
| Aromatic Water |
volatile saturated but not verry water soluble made using talc/distilation |
| Collodions |
Pyroxilen aka nitrocellulose 4% w/v alcohol to ether 1:3 apply to skin for cuts flamable, uncomfortable flexible add camphor and castor oil |
| Elixer |
5-40% bad if patient has drousyness or anibuse ; |
| fluidextracts |
vegetable drugs high OH as solvent 1g/ml not self administered by patient percolation |
| spirits |
volatile 62-85% theraputic aromatic solute simple solution or extraction if aquious solution added, cloudy |
| Tincture |
non volatile 15-80% plant or animal source "extracts dont contain just a single constituent" percolation, maceration |
contact angle completely wetted readily wetted poorly wetted completely unwetted |
completely: 0 readily: ;90 poorly: 90-180 unwet: 180 |
suspensions: zeta |
particle repulsion.; higher zeta = more stable suspension |
| surface tension |
interaction between liquid and vapor "unbalanced molecular cohesive forces at surface" net atractive force towards bulk of liquid |
| anionic surfactant |
hydrophilic part is - body shampoos topical only sodium laural sulfate |
| cationic surfactant |
cation provides emulsifying property disinfect/preservative only topical/opthalmic incompatible with anionic surfactants combined with non ionic surfactants benzylkonium chloride |
| amphoteric surfactant |
hydrophylic has a + and a - can act as anionic, cationic, nonionic depends on PH of solution rarely the only surfactant N-dodecyl-N-N-dimethyl betaine |
| non ionic surfactant |
hydrophilic part no charge non electrolyte tween, span, peg |
| naturally occuring compounds |
bile salts, phospholipids batch variability, bacterial growth beeswax, wool |
| Bile salt |
made in liver highly surface active ; poorly water soluble drugs.; bile salts raise absorption and bioavailability |
| Phospholipids |
alveolar lining of lungs, tears mix of phospholipids, neutral lipids, proteins ; |
| HLB |
0 = lipophilic 50 = hydrophilic |
| anti foaming agents |
HLB 1-3 dissapates foam by draining liquid |
| wetting agents |
HLB 7-9 lowers contact angle when in water bile salt |
| detergents |
HLB 13-16 lower surface tension, wets surface being cleaned. sodium laural sulfate |
| solubilizing agents |
HLB 16-18 raise solubility CMC "crucial micelle concentration" |
| emulsifying agents |
HLB 3-6, 8-18 reduce tension oil to water |
| flocculating agents |
loose agregation of suspended particles increases sedementation volume prevents caking electrolites, polymers and clays, surfactants store in refrigerator |
| emulsions |
dispensed phase = internal phase (liquid) dispersion phase = external continuous phase topical, oral, and parenteral ; |
| rheology |
non newtonian flow of matter effected by: viscosity of continuous phase phase volume ratio emulsifier droplet size and size distribution |
| types of emulsifiers |
1 surfactants ; 2 hydrophilic colloids: water soluble polymer.; O/W, doesn't lower surface tension, raises viscosity. carbs and geletins
3 Finely divided solid particles: adsorbed at interface, W/O, O/W. magnesium hydroxide. aluminum hydroxide |
emulsion problems Creaming |
separation into two regios, rich, poot less likely if both phases similar less likely if external phase is viscous prevent by storing in refrigerator reverseable eg globules rising to top of product |
emulsion problems coalescence/cracking/breaking |
irreversible film of emulsifying agent surounding droplets broken |
emulsion problems phase inversion |
convert to oposite emulsion type prevented by protecting emulsion from extreme hot/cold |
| microemulsions |
large swolen microcells containing internal phase
between thermodinamically stable, and normal emulsion
10-200 nm diamater
more rapid absorption, topical. |
| magma |
similar to gels suspension of inorganic acids like clay in water "thexotropic rheological behavior" |
| milk |
| suspension in aquious vehicle intended for oral. |
| dosage forms effected by particle size |
oral suspension aerosol topical |
| when is drug better fine than coarse? |
poor water soluble dissolution rate limiting stepin absorption process (eg) grisofulvin |
| whats the rate limiting step |
passing thrugh gut wall NOT lumen |
what makes more amorphous? ball milled or microniser? |
| microniser |
| is insulin-zink suspension amorphous or crystaline? |
| can be either |
Humulin L Humulin U |
L : crystaline 70% amorphous 30% U: all crystaline (ER) |
| what factors effect polymorphism when forming? |
solvent temperature rate of cooling
|
| type of polymorph with greatest disolution rate |
| metastable |
| Hydrate |
| molecule crystalized while in water latice |
| Solvate |
| material crystalized in latice other than water |
| Monohydrate |
| 1 molecule of water per molecule of crystalized material. |
