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Ceutics > Exam 1 Definitions and Concepts 5-7 > Flashcards

Exam 1 Definitions and Concepts 5-7 Flashcards

1
Q

drugs can be in many different ionized forms

A

weak organic acids
weak bases
salts
nonelectrolytes
quaternary ammonium salts

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2
Q

ionization affects

A

absorption, distribution, elimination of drugs
*not metabolism

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3
Q

pH partition hypothesis

A

partitioning into lipophilic membrane is greatly inhibited by ionic charges
*ionized will not partition, unionized will
*pH can be altered to increase excretion or absorption

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4
Q

3 acid base theories

A

Arrhenius
Lowry-Bronsted
Lewis

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5
Q

Arrhenius acid and base

A

acid= any species that can increase the concentration of H+ in an aqueous solution
base= any species that can increase the concentration of OH- in an aqueous solution
*limiting because may not always have H+ and OH-

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6
Q

Lowry-Bronsted acid and base

A

acid donates proton
base accepts proton
water is amphiprotic

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7
Q

Lewis acid and base

A

acid= electron donating
base= electron accepting
*won’t really use because mostly applies to inorganic molecules

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8
Q

amphiprotic

A

substance that can both accept and donate a proton (acts as an acid and a base)
*ex. water and amino acids
*amphoteric substances are called ampholytes

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9
Q

equilibrium

A

established when the rate of the forward reaction equals the rate of the reverse reaction

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10
Q

pH

A

negative logarithm of the hydrogen ion concentration

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11
Q

pH + pOH =

A

14 (pKw)

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12
Q

mole fraction

A

always part over total
*for HA = Ka/([H3O+]+Ka)
*for BH+ = [H3O+]/(Ka+[H3)+])

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13
Q

salts of weak acids and bases

A

weak acid + strong base or strong acid + weak base
dissociate fully to equilibrium

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14
Q

ionization of ordinary ampholytes

A

pKa of acid group > pKa of basic group

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15
Q

Zwitter ionic ampholytes

A

pKa of acid group < pKa of basic group

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16
Q

rules of ionization

A

like dissolves (dissociates) like
*acid drugs become more NON ionized in acidic pH (will absorb in stomach)
*basic drugs become more NON ionized in basic pH (will absorb in intestine)

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17
Q

buffer solution

A

solution that changes pH only slightly when small amounts of a strong acid or strong base are added
*resists changes in pH
*contains significant concentrations of both a weak acid and its conjugate base or a weak base and its conjugate acid

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18
Q

blood buffer system

A

pH of blood is 7.35-7.45
maintained by H2CO3/HCO3

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19
Q

buffer capacity, B = dC/d(pH) where dC is

A

number of moles of alkali needed to change the pH of 1 liter of solution by an amount d(pH)

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20
Q

hydrogen bonding

A

intra or inter molecular interactions between H and an electronegative atom (O,N)

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21
Q

polymorph

A

crystalline vs. amorphous

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22
Q

bioavailability

A

amount that gets to blood/organ after first pass if applicable

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23
Q

important pharmaceutical buffer

A

PBS (phosphate buffered saline)
*NaCl and Na2PO4 or KCl and KH2PO4 or CaCl2 or CaCl2 or MgSO4

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24
Q

acidic buffer

A

combination of weak acid and its salt with a strong base
*ex. HCOOH/HCOONa (formic acid and sodium formate)

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25
Q

basic buffer

A

combination of weak base and its salt with a strong acid

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26
Q

buffers with 2 salts

A

monobasic potassium phosphate (KH2PO4)
dibasic potassium phosphate (K2HPO4)

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27
Q

buffer action

A

resistance of a buffer solution to a change in pH

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28
Q

MOA of acidic buffers when an acid is added ex. HCl and CH3COONa/CH3COOH

A

hydrogen ion yielded by HCl are quickly made into acetic acid (CH3COOH), so hydrogen ion concentration does not change
*strong electrolytes (CH3COONa and HCl) dissociate quickly

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29
Q

MOA of acidic buffers when a base is added Ex. NaOH and CH3COOH/CH3COONa

A

hydroxyl ions yielded by NaOH are removed as water
*CH3COOH dissociates to H+ and NaOH to OH-

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30
Q

MOA of basic buffers when an acid is added

A

makes water, same as MOA of acidic buffers when base is added

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31
Q

MOA of basic buffers when base is added ex. NH4OH/NH4CL and NaOH

A

hydroxyl ions quickly removed as ammonium hydroxide. NH4OH
water is also made

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32
Q

MOA of phosphate buffers KH2PO4/K2HPO4

A

H2PO4- is weak acid, HPO42- is conjugate base
water is made whether acid or base is added

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33
Q

common ion effect

A

shift in equilibrium potential that occurs because of addition of ion already involved in equilibrium reaction

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34
Q

a solution of HCN and NaCN is more/less acidic than HCN alone

A

less

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35
Q

buffer capacity

A

measure of a buffer’s magnitude of resistance to change in pH
*buffer index, buffer value, buffer efficiency, buffer coefficient
*B= delta A or B / delta pH (approximate)
*solution has a buffer capacity of 1 when 1 liter of it requires 1 g equivalent of a strong acid or base to change the pH by one unit

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36
Q

secondary buffers in erythrocytes

A

oxy-hemoglobin/hemoglobin and acid/alkali potassium salts of phosphoric acid
*primary is blood
*erythrocytes + RBCs
*carbon monoxide poisoning changes blood pH

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37
Q

common ophthalmic buffers

A

borate, carbonate, phosphate

38
Q

common ointment and cream buffers

A

citric acid/ its salts and phosphoric acid/ its salts

39
Q

use of buffers in pharmaceutical systems

A
  • adjust pH for stability
  • very important for injections (want it to be 7.4)
  • acetate, phosphate, citrate, glutamate often used
40
Q

effect of pH on drug solubility

A

weak acids best absorbed in acidic stomach
weak bases best absorbed in more basic intestine

41
Q

drug classifications by solubility and permeability (BCS= biopharmaceutics classification system)

A

Class I- high solubility and permeability
Class II- low solubility, high permeability
Class III- high solubility, low permeability
Class IV- low solubility and permeability

42
Q

pHp

A

for a weakly acidic drug, the pH below which the drug precipitates
for a weakly basic drug, the pH above which the drug precipitates

43
Q

addition of H3O+ will increase/decrease the solubility of a salt that contains the anion of a weak acid

A

increase

44
Q

crenation

A

cell shrinks, hypertonic solution

45
Q

hemolysis

A

cell bursts, hypotonic solution

46
Q

solution

A

mixture of 2 or more components that form a homogeneous mixture

47
Q

solute

A

dissolved agent, less abundant in solution

48
Q

solvent

A

component in which solute is dissolved, more abundant part of solution

49
Q

unsaturated solution

A

contains dissolved solute in a concentration below that necessary for complete saturation at a definite temp

50
Q

saturated solution

A

one in which an equilibrium is established between dissolved and undissolved solute at a definite temperature

51
Q

supersaturated solution

A

contains more of the dissolved solute than it would normally contain in a saturated state at a definite temperature

52
Q

solubility quantitatively vs. qualitatively

A

quant- concentration of solute in a saturated solution at a certain temperature
qual- spontaneous interaction of 2 or more substances to form a homogeneous molecular dispersion

53
Q

degree of saturation

A

how much solute can be dissolved in a certain amount of water at a given temp

54
Q

solubility curve

A

any solution can be made more saturated, unsaturated, or supersaturated by changing the temperature

55
Q

thermodynamic solubility of a drug in a solvent

A

max amount of the most stable crystalline form that remains in solution in a given volume of the solvent at a given temp and pressure under equilibrium conditions
*balance of solvent with solvent, solute with solute, solvent with solute

56
Q

solubility process

A

mechanistic perspective of solubilization process for organic solute in water involving these steps
1. break up of solute-solute bonds
2. break up of solvent-solvent bonds
3. formation of cavity in solvent phase that can accommodate solute molecule
4. transfer of solute into the cavity
5. formation of solute-solvent intermolecular bonds

57
Q

3 types of interaction in solution process

A

solvent-solvent, solute-solute, solvent-solute
delta Hsol = delta H1 + delta H2 + delta H3

58
Q

enthalpy

A

overall amount of heat released or absorbed during dissolving process at constant pressure
*can be positive or negative, endothermic or exothrmic

59
Q

molarity

A

M,c
moles of solute in 1 L of solution

60
Q

molality

A

m
moles of solute in 1000g of solvent

61
Q

normality

A

N
gram equivalent weights of solute in 1 L solution

62
Q

mole fraction

A

x
ratio of moles of solute to total moles solute + solvent

63
Q

percentage by weight

A

%w/w
g solute in 100g solution

64
Q

percentage by volume

A

%v/v
mL solute in 100mL of solution

65
Q

percentage weight in volume

A

%w/v
g solute in 100mL solution

66
Q

USP solubility

A

number of mL of solvent in which 1g of solute will dissolve

67
Q

polar solvents

A

polarity measured as dipole moment
ability to form hydrogen bonds is generally more important (and will be reflected by high dipole moment)
water dissolves phenols, alcohols, other nitrogen and oxygen containing compounds

68
Q

as length of non-polar chain of an aliphatic alcohol increases

A

solubility in water decreases

69
Q

branching increases/decreases solubility in water

A

increases

70
Q

non-polar solvents

A

unable to form hydrogen bonds
dissolve non-polar solutes through weak van der Waals forces

71
Q

semi-polar solvents

A

ex. ketones, propylene glycol
can induce a certain degree of polarity in non-polar solvents
intermediate solvents- bring about miscibility of polar and non-polar liquids

72
Q

solubility product principle

A

Ksp, mathematical product of its dissolved ion concentrations raised to the power of their stoichiometric coefficients

73
Q

barium sulfate

A

radiopaque contrast media
coats the esophagus, stomach, intestine with material not absorbed by body so it can be seen on an x-ray

74
Q

dielectric constant

A

property of solvent relating to the amount of energy required to separate 2 oppositely charged bodies in a solvent as compared with the energy required to separate the same 2 oppositely charged bodies in a vacuum
*highest: water then glycols
*drugs can be polar, non-polar, semipolar

75
Q

solubility of gases in liquids

A

when pressure above solution is released, solubility of gas decreases
as temperature increases, solubility of gas decreases

76
Q

2 types of liquid-liquid systems

A

ones with complete miscibility (alcohol and water)
ones with partial miscibility (phenol and water)

77
Q

miscibility

A

mutual solubility of components in liquid-liquid systems

78
Q

complete miscibility

A

adhesive forces between different molecules (A-B) > cohesive forces between like molecules (A-A or B-B)

79
Q

partial miscibility

A

cohesive forces of constituents of a mixture are different
ex. water (A) and hexane (B), A-A > B-B
*think oil and water

80
Q

decreasing particle size _ surface area and _ solubility

A

increases, increases

81
Q

molecular size effect on solubility of solids in liquids

A

larger molecules more difficult to solvate
*carbon branching increases solubility

82
Q

boiling point of liquids and melting point of solids effect on solubility

A

aqueous solubility decreases with increasing boiling and melting point

83
Q

influence of substituents on solubility

A

polar groups capable of H bonding impart high solubility
non-polar groups impart low solubility
ionization of substituent increases solubility

84
Q

influence of temperature on solubility

A

if solution process absorbs energy, solubility will increase as temperature increases
if solution process releases energy, solubility will decrease with increasing temperature

85
Q

influence of crystal properties on solubility

A

polymorphs- same chemical structure but different physical properties
amorphous- noncrystalline form
amorphous dissolves more rapidly than same drug in crystalline form

86
Q

influence of pH on solubility

A

very important
solubility depends on degree of ionization, and this changes with pH

87
Q

carboxylic acids with more than _ carbons are insoluble in water

A

5
*react with sodium hydroxide, carbonates, bicarbonates to form salts

88
Q

fatty acids

A

carboxylic acids with 12-20 carbons
*soluble in solvents with low dielectric constants

89
Q

benzoic acid soluble in

A

sodium hydroxide solution

90
Q

phenol soluble in

A

NaOH (not water, weak acid)

91
Q

most weak electrolytes not very soluble in water, but are soluble in

A

dilute solutions of acids

Ceutics (2 decks)

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