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

Exam 1 Definitions and Concepts 5-7 Flashcards

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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
basic buffer
combination of weak base and its salt with a strong acid
26
buffers with 2 salts
monobasic potassium phosphate (KH2PO4) dibasic potassium phosphate (K2HPO4)
27
buffer action
resistance of a buffer solution to a change in pH
28
MOA of acidic buffers when an acid is added ex. HCl and CH3COONa/CH3COOH
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
29
MOA of acidic buffers when a base is added Ex. NaOH and CH3COOH/CH3COONa
hydroxyl ions yielded by NaOH are removed as water *CH3COOH dissociates to H+ and NaOH to OH-
30
MOA of basic buffers when an acid is added
makes water, same as MOA of acidic buffers when base is added
31
MOA of basic buffers when base is added ex. NH4OH/NH4CL and NaOH
hydroxyl ions quickly removed as ammonium hydroxide. NH4OH water is also made
32
MOA of phosphate buffers KH2PO4/K2HPO4
H2PO4- is weak acid, HPO42- is conjugate base water is made whether acid or base is added
33
common ion effect
shift in equilibrium potential that occurs because of addition of ion already involved in equilibrium reaction
34
a solution of HCN and NaCN is more/less acidic than HCN alone
less
35
buffer capacity
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
36
secondary buffers in erythrocytes
oxy-hemoglobin/hemoglobin and acid/alkali potassium salts of phosphoric acid *primary is blood *erythrocytes + RBCs *carbon monoxide poisoning changes blood pH
37
common ophthalmic buffers
borate, carbonate, phosphate
38
common ointment and cream buffers
citric acid/ its salts and phosphoric acid/ its salts
39
use of buffers in pharmaceutical systems
- adjust pH for stability - very important for injections (want it to be 7.4) - acetate, phosphate, citrate, glutamate often used
40
effect of pH on drug solubility
weak acids best absorbed in acidic stomach weak bases best absorbed in more basic intestine
41
drug classifications by solubility and permeability (BCS= biopharmaceutics classification system)
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
pHp
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
addition of H3O+ will increase/decrease the solubility of a salt that contains the anion of a weak acid
increase
44
crenation
cell shrinks, hypertonic solution
45
hemolysis
cell bursts, hypotonic solution
46
solution
mixture of 2 or more components that form a homogeneous mixture
47
solute
dissolved agent, less abundant in solution
48
solvent
component in which solute is dissolved, more abundant part of solution
49
unsaturated solution
contains dissolved solute in a concentration below that necessary for complete saturation at a definite temp
50
saturated solution
one in which an equilibrium is established between dissolved and undissolved solute at a definite temperature
51
supersaturated solution
contains more of the dissolved solute than it would normally contain in a saturated state at a definite temperature
52
solubility quantitatively vs. qualitatively
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
degree of saturation
how much solute can be dissolved in a certain amount of water at a given temp
54
solubility curve
any solution can be made more saturated, unsaturated, or supersaturated by changing the temperature
55
thermodynamic solubility of a drug in a solvent
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
solubility process
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
3 types of interaction in solution process
solvent-solvent, solute-solute, solvent-solute delta Hsol = delta H1 + delta H2 + delta H3
58
enthalpy
overall amount of heat released or absorbed during dissolving process at constant pressure *can be positive or negative, endothermic or exothrmic
59
molarity
M,c moles of solute in 1 L of solution
60
molality
m moles of solute in 1000g of solvent
61
normality
N gram equivalent weights of solute in 1 L solution
62
mole fraction
x ratio of moles of solute to total moles solute + solvent
63
percentage by weight
%w/w g solute in 100g solution
64
percentage by volume
%v/v mL solute in 100mL of solution
65
percentage weight in volume
%w/v g solute in 100mL solution
66
USP solubility
number of mL of solvent in which 1g of solute will dissolve
67
polar solvents
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
as length of non-polar chain of an aliphatic alcohol increases
solubility in water decreases
69
branching increases/decreases solubility in water
increases
70
non-polar solvents
unable to form hydrogen bonds dissolve non-polar solutes through weak van der Waals forces
71
semi-polar solvents
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
solubility product principle
Ksp, mathematical product of its dissolved ion concentrations raised to the power of their stoichiometric coefficients
73
barium sulfate
radiopaque contrast media coats the esophagus, stomach, intestine with material not absorbed by body so it can be seen on an x-ray
74
dielectric constant
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
solubility of gases in liquids
when pressure above solution is released, solubility of gas decreases as temperature increases, solubility of gas decreases
76
2 types of liquid-liquid systems
ones with complete miscibility (alcohol and water) ones with partial miscibility (phenol and water)
77
miscibility
mutual solubility of components in liquid-liquid systems
78
complete miscibility
adhesive forces between different molecules (A-B) > cohesive forces between like molecules (A-A or B-B)
79
partial miscibility
cohesive forces of constituents of a mixture are different ex. water (A) and hexane (B), A-A > B-B *think oil and water
80
decreasing particle size _ surface area and _ solubility
increases, increases
81
molecular size effect on solubility of solids in liquids
larger molecules more difficult to solvate *carbon branching increases solubility
82
boiling point of liquids and melting point of solids effect on solubility
aqueous solubility decreases with increasing boiling and melting point
83
influence of substituents on solubility
polar groups capable of H bonding impart high solubility non-polar groups impart low solubility ionization of substituent increases solubility
84
influence of temperature on solubility
if solution process absorbs energy, solubility will increase as temperature increases if solution process releases energy, solubility will decrease with increasing temperature
85
influence of crystal properties on solubility
polymorphs- same chemical structure but different physical properties amorphous- noncrystalline form amorphous dissolves more rapidly than same drug in crystalline form
86
influence of pH on solubility
very important solubility depends on degree of ionization, and this changes with pH
87
carboxylic acids with more than _ carbons are insoluble in water
5 *react with sodium hydroxide, carbonates, bicarbonates to form salts
88
fatty acids
carboxylic acids with 12-20 carbons *soluble in solvents with low dielectric constants
89
benzoic acid soluble in
sodium hydroxide solution
90
phenol soluble in
NaOH (not water, weak acid)
91
most weak electrolytes not very soluble in water, but are soluble in
dilute solutions of acids

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