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DSF Exam 1 Preformulation part 2
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Examples of salts that improve drug solubility
Phytoin sodium for injection
Ampicillin sodium in oral suspension/injection
Intrinsic solubility
Solubility of unionized drug
Intrinsic solubilty must be below ___ for a need to be salt form
Less than 1 mg/ml
Salts from weak bases yield more ____ solutions.
Salts from Weak acids yield more ____ solution.s
Acidic
alkaline
Minocylcline HCl IV solution has a pH of
2 to 2.8
Salt form has a ______ percent of active drug compared to non-salt form.
Lower
Prodrug
Synthetic derivative of a drug that is transformed in vivo to liberate an active drug molecule.
Purpose of prodrug
Biostability/prolonged action
Targeting
Solubility
Erythromycin ethylsuccinate is less soluble than
Erythromycin for better taste (suspension), Bypass gastric degradation (degrade in stomach), and better absorption (more lipophilic).
Phosphate is added to
Increase water solubility, added to create a phosphate-ester derivative.
T/F phosphate ester is the same as a phosphate salt
True
False
FALSE Example is disopyramide phosphate
Rate limiting step for absorption
Drug dissolution rate for oral bioavailability
Dissolution of solid in liquid occurs in 2 phases
Interfacial reaction liberates molecules from solid phase
Diffusion of liberated molecules away from solid into the bulk liquid.
Noyes whitney equation dissolution rate
dm/dt= kA(Cs-C)
k-D/h
Terms for dissolution equation
dm/dt= mass dissolved in time
A is surface area
Cs is drug solubility
C is concentration
k is dissolution rate constant
D is diffusion coefficient of solute in medium
h is thickness of static boundary layer
Dissolution equation affected by
Size, Solubility in water, volume of dissolution medium, and thickness of static boundary.
Partition
to move from one phase to another (polar and nonpolar phases)
Partition is important to
Traverse lipid bilayers
Partition coefficient
Oil over water
partition phenomena
Into fat
Into microorganisms
Into plastic
between oil and water
Most common organic solvent used
Octanol because it mimics membrane
Butanol mimics ______
Chloroform mimics _____
Buccal membrane
Blood brain barrier
Unionized drug has higher partition coefficient and is
less polar
Drug absorption most likely found in regions with pHs
favoring unionized form
Author
swynocker
ID
45359
Card Set
DSF Exam 1 Preformulation part 2
Description
Preformulation part 2
Updated
2010-10-27T04:42:19Z
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