Parenteral dosage forms for poorly water-soluble drugs

Question 1

propylene glycol

Answer 1

cosolvent

Question 2

ethanol (absolute alcohol)

Answer 2

cosolvent

Question 3

glycerol

Answer 3

cosolvent

Question 4

polyethylene glycol

Answer 4

cosolvent

Question 5

dimethylacetamide

Answer 5

cosolvent

Question 6

Tween 80

Answer 6

nonionic surfactant (forms micelles above CMC)

Question 7

Cremophor-EL

Answer 7

nonionic surfactant (forms micelles above CMC)

Question 8

bile salts (sodium deoxycholate)

Answer 8

anionic surfactant (for amphotericin-B/”ampho-terrible”), (forms micelles above CMC)

Question 9

cyclodextrin

Answer 9

nontoxic cyclic oligomers of dextrose, forms complexes w/ hydrophobic drugs

Question 10

propofol

Answer 10

only o/w emulsion marketed, 10mg/mL for anesthetic practice

Question 11

prodrug

Answer 11

inactive form of drug, hydrolysis by enzymes/esterases releases parent drug (active form)

pro moiety can be hydrophilic or hydrophobic (opp from the parent drug)

Question 12

NAB (nanoparticle albumin-bound)

Answer 12

nano particle of hydrophobic drug (amorphous form), coated w/ serum albumin – gets solubilized in the blood and drug gets released fast

avoids using cremophor and ethanol in formulation

Question 13

primary driving force for water solubilization (of drug)

Answer 13

hydrophobic effect

Question 14

benzylalcohol

Answer 14

preservative