Week 1/2 Flashcards
Based on the description provided, “Inhaled Albuterol Sulfate Suspension,” answer the following questions:
The drug is?
The dosage form is?
The route of administration is?
albuterol sulfate
suspension
pulmonary
Based on your understating of dosage forms, categorize the following dosage forms/ formulations as solid, liquid, or semi-solid.
- Emulsions
- Pastes
- Granules
liquids
semisolids
solids
Excipients which control the rate of drug release impact the drug’s
rate of absorption
Which type of excipient is critical for an orally administered acid-sensitive drug?
Buffering agent
How quickly to effervescent tablets dissolve compared to regular tablets?
faster
Based on your understanding of dosage forms which of the excipients would you expect in a liquid dosage form? {Select all that apply} Emulsifying agent Lubricant Vehicle Sweeting agent
Emulsifying agent
Vehicle
Sweeting agent
Based on your understanding of dosage forms, which excipients would you expect in a semisolid dosage form? {Select all that apply} Levigating agent Lubricants Vehicle Ointment base
Levigating agent
Ointment base
Based on your understanding of dosage forms, which excipients would you expect in a solid dosage form? {Select all that apply} Glidant Lubricants Vehicle Film coating
Glidant
Lubricants
Film coating
T/F Excipients listed in the Inactive Ingredients Database can be incorporated into all dosage forms without any additional considerations
False
T/F Excipients that can increase the rate of absorption aid with the disintegration of solid dosage forms.
True
The major pathway of absorption for small hydrophilic molecules (MW <300 Da) is?
passive paracellular diffusion.
The major pathway of absorption for small lipophilic drugs (<1000 Da) is
passive transcellular diffusion.
The major pathway for most drug absorption is passive ______ transport.
transcellular
T/F Drugs which are slightly hydrophobic will have higher drug absorption than very hydrophilic or very hydrophobic drugs
True
As the molecular weight of a molecule increases its diffusion coefficient, _____
decreases
As the radius of a molecule decreases its diffusion coefficient, _____
increases
As the viscosity of a medium increases, the diffusion coefficient of a molecule in that medium, _____
decreases
As the temperature increases the, diffusion coefficient of a molecule, ______
increases
As the molecular weight increases the, molecular size, _____
increases
If a drug has a high partition coefficient, it is lipophobic or liphophilic?
Lipophilic
For an API absorption, the ideal range for log Ko/w or log Po/w is between?
1 to 3
A drug has a partition coefficient of 0.333. Its log partition coefficient value is?
-0.478 (figure out how to calculate)
A log Ko/w or log Po/w value of 2 indicates that the drug molecule is?
lipophilic
A log Ko/w or log Po/w value of -3 indicates that the drug molecule is?
hydrophilic
A log Ko/w or log Po/w value of 0 indicates that the drug molecule is?
equally lipohilic and hydrophilic
A drug has log Po/w value of 2.699 indicating that; (select that all apply)
the solubility ratio of the drug in oli/water is ≈ 500.
the solubility ratio of the drug in oil/water is ≈ 0.431.
the drug is lipophilic.
the drug is hydrophilic.
the solubility ratio of the drug in oli/water is ≈ 500.
the drug is lipophilic.
What happens to the permeability of a molecule if the MW of the compound increases?
Permeability decreases
What happens to the permeability of a molecule if the partition coefficient increases?
Permeability increases
What happens to the flux of a molecule across biological membrane if its permeability decreases?
Flux decreases
What happens to the flux of a molecule across the biological membrane if the molecule concentrations C0 and Ci are equal?
Flux stops
define Molecular dispersion
homogenous, dispersant size less than 1nm
define Colloidal dispersion
non-homogwnous, dispersant size 1nm to 1um
define Coarse dispersion
non-homogwnous, dispersant size greater than 1um
Components of a solution include a ____ completely ____ in a _____
key: solvent, solute, dissolved
solute, dissolved, solvent
Increasing the dissolution rate:
- increases solubility
- decreases solubility
- dose not affect solubility
dose not affect solubility
A compound that is sparingly soluble has an approximate solubility of:
- 33 – 100 mg/mL
- 10 – 33 mg/mL
- 1 – 10 mg/mL
10 – 33 mg/mL
Ionized forms of the drug have ____ aqueous solubility compared to the unionized form of the drug molecule.
higher
Salt forms of the drug have ____ aqueous solubility compared to the weak electrolyte form of the drug molecule.
higher
Different salt forms of the drug have _____ aqueous solubility compared to the weak electrolyte form of the drug molecules.
different
Neutral molecules need co-solvents, surfactants, or non-aqueous formulations due to their ____ aqueous solubility
lower
The crystalline form of the drug will have ____ solubility compared to the amorphous form of the drug.
lower
Typically, solubility of solid solutes in liquid solvents _____ with increasing temperature.
increases
Aqueous water-based solutions can be administered by __ routes of administration.
all
Aqueous syrups contain:
- 100% water and up to 100% sugar
- 100% water and up to 85% sugar
- 100% alcohol and up to 85% sugar
- 100% alcohol and up to 100% sugar
100% water and up to 85% sugar
Elixirs contain:
- 60-95% water & 5 - 40% alcohol
- 60-95% alcohol & 5 - 40% water
- 60-95% oil & 5 - 40% alcohol
- 60-95% alcohol & 5 - 40% oil
60-95% water & 5 - 40% alcohol
Elixirs can be administered by ________ route(s) of administration.
oral & topical
Oil solutions contain ___ oil.
100%
Oil solutions can be administered by what route(s) of administration?
IM, topical & ophthalmic
Which of the following vehicles can be used by all routes of administration?
- Collodion
- Water
- Tincture
- Syrup
water
Drug X is available in two forms with the following aqueous solubilities: slightly soluble WA or a soluble Na salt of the WA.
Which form of the drug is most appropriate for an aqueous solution dosage form?
Na salt of WA
Drug X is available in two forms with the following aqueous solubilities: slightly soluble WA or a soluble Na salt of the WA.
Which form of the drug is most appropriate for an oil based solution dosage form?
WA
Drug X is very slightly soluble with a log Ko/w 2.2 and a MW of 420 Da. No salt forms of Drug X are available. Based on its solubility each dose will require 8 tablespoons. What option(s) should you consider if Drug X needs to be formulated as an aqueous solution? [Select all that apply.] Use a co-solvent Use a surfactant Use a complexing agent Use an oil vehicle
Use a surfactant
Use a complexing agent
Which of the following excipients will you expect in a topical solution? [Select all that apply.]
- Vehicle
- Surfactants/complexing agents/ co-solvents
- Preservatives
- Sweeteners
Vehicle
Surfactants/complexing agents/ co-solvents
Preservatives
The chemical stability of drugs in solution dosage forms can be improved by making?
- aqueous solutions
- powders for reconstitution
- hydro-alcoholic solutions
powders for reconstitution
Drug S is available as an aqueous solution. Drug S has a MW of 420 Da and a log Ko/w of -3.5. What will be the rate limiting step for Drug S in this dosage form?
- Diffusion coefficient
- Partition coefficient
- Both diffusion coefficient & partition coefficient
- Neither diffusion coefficient & partition coefficient
Partition coefficient