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Pharm Sci
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Ionized forms are?
More water soluble
Less lipid soluble
Non-ionized forms are?
More lipid soluble
Less water soluble
Acids are?
Species that can donate a proton
Bases are?
Species that can accept a proton
When acid is added to water?
H3O will increase and OH will decrease to maintain equilibrium pH<7
When a base is added to water?
OH will increase and H3O will decrease to maintain equilibrium ph>7
Strong acids and strong bases do what in water?
Will completely dissociate, = large Ka
Non-electrolytes?
Have no acid or base functionality
Monoprotics?
Can either donate/accept 1 proton/molecule
Polyprotics?
Can either donate/accept 1+ proton/molecule
Ampholytes?
Have both acid and base functionality
Salts of acids are?
Are made with a strong base
like sodium or potassium hydroxide
Will act as conj. base
Salts of bases?
Are made with strong acids
will act as conj. acid
What is expected of fraction ionized of salt forms?
That it will be 100% ionized
ALSO CALCULATED IN RESPECT TO FREE FORM
Excipients?
Inactive ingredients that enable product quality and performance
What are the two classifications of stability?
Physical - molecules remaining the same
Chemical - molecules changed, no longer deal with the same molecule
How might physical instability arise?
Changes in phase, soluble components into insoluble components
What might happen when physical instability occurs?
Precipitation, changes in ph can change drug solubility leading to precipitation
Buffers?
Are a form of excipient, designed to maintain the solution at a consent pH
Why is pH selection in a formulation important?
It is selected to maintain solubility and minimize potential chemical degradation
Buffer capacity?
Is a measure of how well buffers maintain solution pH
What is beta in the Van Slyke mean?
The larger the beta, the more effective a buffer is, and the smaller the change in solution pH upon addition of a strong acid/base
Carbonates?
Biological buffers that maintain stable blood pH and renal function
Phosphates?
Biological buffers, H2PO4- and HPO4-
Proteins?
Biological buffers, Hemoglobin and albumin
Why are strong acids and base not used in buffers?
They are used to adjust the pH of a solution, only at extreme pHs would their buffer capacity be available
What is intrinsic solubility?
So, moles/L of unionized acid/base that dissolves in solution
So???
Is the BASELINEE, not a function of a pH
Total solubility?
St, is all compound in solution=concentration of unionized compound + ionized form
Precipitation may occur when?
Increases as % unionized increases
Precipitation begins when concentration of HA=So
What determines the chance of a drug precipitating out of a solution?
So, pH of solution, pKa/pkb of acid/base
In weak acids, precipitation at risk when?
pH is below calculated pHp
In weak bases, precipitation at risk when?
pH is above calculated pHp
Rank weak acids from strongest to weakest
Sulfonic acids
Carboxylic acids
Aryl sulfonamides
Phenols
Imides
Thiols
Rank weak bases from strongest to weakest
Guanidines
Aliphatic nitrogens
Amidines
Ar-NH2
Aromatic Nitrogens
Strong Bases
LiOH Lithium hydroxide
NaOH Sodium hydroxide
KOH Potassium hydroxide
Ca(OH)2 Calcium hydroxide
Mg(OH)2 Magnesium hydroxide
Ba(OH)2 Barium Hydroxide
Strong acids
HCl Hydrochloric acid
H2SO4 Sulfuric Acid
HI Hydroiodic Acid
HClO4 Perchloric Acid
HNO3 Nitric Acid
HBr Hydrobromic acid