1. solute molecules solid -> solute

2. molecules migrate through boundry layer to bulk solution. (think diffusion)

bigg SA, more soluble

bigger SA, smaller molecule

viscosity

molecular characteristics, size

thickness of boundry layer

oral

suspension

aerosol

topical

poor water soluble

dissolution rate limiting stepin absorption process

(eg) grisofulvin

passing thrugh gut wall

NOT lumen

what makes more amorphous?

ball milled or microniser?

Humulin L

Humulin U

L : crystaline 70% amorphous 30%

U: all crystaline (ER)

solvent

temperature

rate of cooling

Sieve number for a particle dictates into

small number = coarser

bigger number = finer

comminution

trituration

hammer mill

pebble ball mill

fluid energy mill

using extra chemical to help break up

chemical easily removed later (eg) alcohol, acetone because evaporation

best for hard crystaline powders, gummy substances

rate of diffusion

K = Cu/CL

lipophylic

greater pass through bio membranes.

preservatives

flavors

want it in the water system

want flavors in highest concentration external phase.

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

Ca

Na

K

HCL

sulfate

nitrate

easier to crystalize for stability

disolve in water

easy handle for processing

lower degredation

better comfort/compliance

more efficient

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%

miscible in water, alcohol, sorbitol, propyleme glycol

humectant, levigating agent, suppository base, preservative

miscible in water, alcohol, glycerin, propylene glycol

emulsifying agent, humectant

laxative if > 20g/day

miscible in alcohol, water, glycerin, and sorbitol

preservative, humectant, levigating agent

substitute for glycerin

doesn't depress CNS, not volatile

preservtive

low solubility in water,

stable PH 4-8

longer the chain, better preservative

agitation with heat: Fast, risk of breaking down sugars

agitation withut heat: safer

Percolation: extraction of drug, preparation of syrup

metronidazole

chlorpropamide

glyburide

glipizide

volatile

saturated but not verry water soluble

made using talc/distilation

Pyroxilen aka nitrocellulose 4% w/v

alcohol to ether 1:3

apply to skin for cuts

flamable, uncomfortable

flexible add camphor and castor oil

5-40%

bad if patient has drousyness or anibuse

vegetable drugs

high OH as solvent

1g/ml

not self administered by patient

percolation

volatile

62-85%

theraputic aromatic solute

simple solution or extraction

if aquious solution added, cloudy

non volatile

15-80%
bad taste

plant or animal source

"extracts dont contain just a single constituent"

percolation, maceration

suspensions:

zeta

particle repulsion. 

higher zeta = more stable suspension

interaction between liquid and vapor

"unbalanced molecular cohesive forces at surface"

net atractive force towards bulk of liquid

hydrophilic part is -

body shampoos

topical only

sodium laural sulfate

cation provides emulsifying property

disinfect/preservative

only topical/opthalmic

incompatible with anionic surfactants

combined with non ionic surfactants

benzylkonium chloride

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

hydrophilic part no charge

non electrolyte

tween, span, peg

bile salts, phospholipids

batch variability, bacterial growth

beeswax, wool

made in liver

highly surface active

poorly water soluble drugs.  bile salts raise absorption and bioavailability

alveolar lining of lungs, tears

mix of phospholipids, neutral lipids, proteins

0 = lipophilic

50 = hydrophilic

HLB 1-3

dissapates foam by draining liquid

HLB 7-9

lowers contact angle when in water

bile salt

HLB 13-16

lower surface tension, wets surface being cleaned.

sodium laural sulfate

HLB 16-18

raise solubility

CMC "crucial micelle concentration"

HLB 3-6, 8-18

reduce tension oil to water

loose agregation of suspended particles

increases sedementation volume

prevents caking

electrolites, polymers and clays, surfactants

store in refrigerator

dispensed phase = internal phase (liquid)

dispersion phase = external continuous phase

topical, oral, and parenteral

non newtonian flow of matter

effected by:

viscosity of continuous phase

phase volume ratio

emulsifier

droplet size and size distribution

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

large swolen microcells containing internal phase

between thermodinamically stable, and normal emulsion

10-200 nm diamater

more rapid absorption, topical.

similar to gels

suspension of inorganic acids like clay in water

"thexotropic rheological behavior"

1. solute molecules solid -> solute

2. molecules migrate through boundry layer to bulk solution. (think diffusion)

bigg SA, more soluble

bigger SA, smaller molecule

viscosity

molecular characteristics, size

thickness of boundry layer

Sieve number for a particle dictates into

small number = coarser

bigger number = finer

comminution

trituration

hammer mill

pebble ball mill

fluid energy mill

using extra chemical to help break up

chemical easily removed later (eg) alcohol, acetone because evaporation

best for hard crystaline powders, gummy substances

rate of diffusion

K = Cu/CL

lipophylic

greater pass through bio membranes.

preservatives

flavors

want it in the water system

want flavors in highest concentration external phase.

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

Ca

Na

K

HCL

sulfate

nitrate

easier to crystalize for stability

disolve in water

easy handle for processing

lower degredation

better comfort/compliance

more efficient

parabens

benzoic acid

edetate disodium

sorbic acid

benzokonium chloride

BHA

BHT

ascorbic acid

tocopherol

sodium metabisulfate

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

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%

miscible in water, alcohol, sorbitol, propyleme glycol

humectant, levigating agent, suppository base, preservative

miscible in water, alcohol, glycerin, propylene glycol

emulsifying agent, humectant

laxative if > 20g/day

miscible in alcohol, water, glycerin, and sorbitol

preservative, humectant, levigating agent

substitute for glycerin

doesn't depress CNS, not volatile

preservtive

low solubility in water,

stable PH 4-8

longer the chain, better preservative

agitation with heat: Fast, risk of breaking down sugars

agitation withut heat: safer

Percolation: extraction of drug, preparation of syrup

metronidazole

chlorpropamide

glyburide

glipizide

volatile

saturated but not verry water soluble

made using talc/distilation

Pyroxilen aka nitrocellulose 4% w/v

alcohol to ether 1:3

apply to skin for cuts

flamable, uncomfortable

flexible add camphor and castor oil

5-40%

bad if patient has drousyness or anibuse

vegetable drugs

high OH as solvent

1g/ml

not self administered by patient

percolation

volatile

62-85%

theraputic aromatic solute

simple solution or extraction

if aquious solution added, cloudy

non volatile

15-80%
bad taste

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

interaction between liquid and vapor

"unbalanced molecular cohesive forces at surface"

net atractive force towards bulk of liquid

hydrophilic part is -

body shampoos

topical only

sodium laural sulfate

cation provides emulsifying property

disinfect/preservative

only topical/opthalmic

incompatible with anionic surfactants

combined with non ionic surfactants

benzylkonium chloride

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

hydrophilic part no charge

non electrolyte

tween, span, peg

bile salts, phospholipids

batch variability, bacterial growth

beeswax, wool

made in liver

highly surface active

poorly water soluble drugs.  bile salts raise absorption and bioavailability

alveolar lining of lungs, tears

mix of phospholipids, neutral lipids, proteins

0 = lipophilic

50 = hydrophilic

HLB 1-3

dissapates foam by draining liquid

HLB 7-9

lowers contact angle when in water

bile salt

HLB 13-16

lower surface tension, wets surface being cleaned.

sodium laural sulfate

HLB 16-18

raise solubility

CMC "crucial micelle concentration"

HLB 3-6, 8-18

reduce tension oil to water

loose agregation of suspended particles

increases sedementation volume

prevents caking

electrolites, polymers and clays, surfactants

store in refrigerator

dispensed phase = internal phase (liquid)

dispersion phase = external continuous phase

topical, oral, and parenteral

non newtonian flow of matter

effected by:

viscosity of continuous phase

phase volume ratio

emulsifier

droplet size and size distribution

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

large swolen microcells containing internal phase

between thermodinamically stable, and normal emulsion

10-200 nm diamater

more rapid absorption, topical.

similar to gels

suspension of inorganic acids like clay in water

"thexotropic rheological behavior"

oral

suspension

aerosol

topical

poor water soluble

dissolution rate limiting stepin absorption process

(eg) grisofulvin

passing thrugh gut wall

NOT lumen

what makes more amorphous?

ball milled or microniser?

Humulin L

Humulin U

L : crystaline 70% amorphous 30%

U: all crystaline (ER)

solvent

temperature

rate of cooling