Chemical And Physical Stability Flashcards

1
Q

Admixture

A

Combined Parenteral dosage forms for administration, including SVPs and LVPs

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2
Q

Incompatibility

A

Medication error of dosage dorms from compounding, dispensing, or administration

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3
Q

Chemical incompatibility

A

More rapid degradation
Hydrolysis
Oxidation
Photolysis
Increased storage temperature
Packaging

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4
Q

Hydrolysis

A

Ph catalyzes hydrolysis

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5
Q

Order of liability to hydrolysis:

A

B-lactams, esters, imines, and amides

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6
Q

Oxidation

A

Free radical react with oxygen or loss of electrons, often catalyzed by trace metals

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7
Q

Oxidation signs

A

Coloring on the drug

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8
Q

Oxidation effects

A

fats and natural oils

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9
Q

Antioxidants

A

Tocopherol
EDTA
Sulfites
Nitrogen blanket

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10
Q

Photolysis

A

Decomposition of drug by light

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11
Q

Avoiding photolysis

A

Amber vials
Aluminum foil

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12
Q

Photolysis affects

A

Tryptophan

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13
Q

Chemical incompatibility

A

Increases over time
Depends on vehicle

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14
Q

Physical incompatibility

A

Interactions of two or more substances
Change in appearance
Change in color
Chang in clarity
Evolution of gas
Combining anions and cations can lead to precipitation

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15
Q

Salting out

A

High levels of salts lead to precipitation
Dehydrate nonelectrolytes (neutral) and electrolytes (ion pairs)

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16
Q

Isoelectric point

A

PH where molecule has no net charge. Protein has lowest solubility and highest adsorption at isoelectric point.

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17
Q

albumin isoelectric point

A

4.9

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18
Q

Adsorption

A

Lipophilic drugs partition into plastic and rubber at container surfaces

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19
Q

Freeze drying

A

Reduced water content, enhanced drug stability
High storage stability for biologics

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20
Q

Drug solubilization

A

Removal of molecule from crystal lattice
Creating a void in solvent
Release of solvation energy

21
Q

nonpolar drugs and solubility

A

Poor water solubility due to hydrophobic effect
Water forms a highly ordered shell reducing mobility

22
Q

Hydrophobic effect

A

Adsorption
Assembly
Particle aggregation
Embolization

23
Q

Ionizable drug and solubility

A

PH adjustment can increase water solubility
Weak acids increased at pH>5
Weak bases increased at pH <7

24
Q

To maintain pH in solution

A

Use buffers

25
Q

Account for >90% of cations

A

Sodium salts of weak acids

26
Q

Most common salts

A

Hydrochloride salts of weak bases

27
Q

IV dilution in salts

A

Rapid and neutralizing

28
Q

IM salt dilution

A

Reduced

29
Q

SC salt dilution

A

Further reduced, more potential for irritation

30
Q

Cosolvent solubility

A

Reduces polarity
Usually diluted with normal saline and infused as diluted solution
Use of final filter recommended

31
Q

Cosolvents

A

Propylene glycol
Ethanol
Glycerol
Polyethylene glycol
Dimethylacetamide

32
Q

Rapid IV of propylene glycol

A

Hypotension
Arrhythmias
Thombophlebitis

33
Q

Cosolvents for IM

A

Precipitation may occur in cosolvent formulation after IM injection
Slow and erratic drug absorption

34
Q

Nonionic surfactant

A

Molecule that has water-loving and water hating parts
Surface active
Reduce surface tension of water
Potentially adsorb the surface
Forms a micelle at higher concentrations

35
Q

Micelle vs liposomes

A

Liposomes have a hole in the center

36
Q

Taxol

A

Surfactant
Solution is diluted prior to infusion and forms a super-saturated solution which may precipitate

37
Q

Cremophor-EL

A

Widely used nonionic surfactant
Enhances leeching of additives from PVC
Allergic reactions in later doses
Pgp responsible for multi-drug resistance
Influences PK of paclitaxel

38
Q

Increase solubilization

A

PH adjustments
Co-solvents
Micelles
Complexes
Prodrugs
Nanoparticles
Emulsions

39
Q

drug solubilization

A

pH adjustments/salts
cosolvents
micelles
complexes
prodrugs
nanoparticles
oils/emulsions

40
Q

solubility of drug complexes

A

=solubility of complexed drug + concentration of drug in complexed drug

41
Q

cyclodextrans

A

relatively nontoxic cyclic oligomers of dextrose that form complexes with drugs

42
Q

Prodrugs for injection

A

–Prodrug containing a hydroxyl, carboxyl, or amine form hydrophilic prodrugs to enhance solubility
–After IV pro-moiety is removed by hydrolysis or esterase
–may alter the PK of parent drug depending on rate of prodrug conversion to parent drug

43
Q

Etopophos

A

Prodrug: water solubility of etoposide phosphate lessens potential for precipitation after dilution during IV infusion

44
Q

Nanoparticles for injection

A

reduced particle size–> increased SA/dissolution
solid state: increased drug loading and chemical stability
IM, IV, SC

45
Q

nanoparticles

A

ideal when they are further apart for lower potential energy

46
Q

nanoparticle albumin-bound (abraxane-nab-paclitaxel)

A

active drug nanoparticle is in non-crystalline, amorphous, readily bioavailable state

47
Q

Long-acting HIV prevention

A

also uses nanoparticles

48
Q

oil-in-water emulsion

A

10-20% soybean/sunflower oil
2% glycerol
1% lecithin
for oil-soluble drugs