Pharmaceutics II Exam 1: Introduction, Ophthalmic Preparations, Pharmaceutical Solutions, Solid Dosage Forms
Ophthalmic suspensions should have a microfine size of ____
10 um or less.
Mannitol can be used for what? Select all that applies A) Osmotic Agents B) Lyophilization C) Powder ophthalmic drug D) Liquid ophthalmic drug
A) Osmotic Agents B) Lyophilization C) Powder ophthalmic drug
Which of the following properties of a solid therapeutic agents are influenced by the particle size reduction? A) Porosity B) Angle of repose C) Specific Surface D) Melting point E) Partition Coefficient
A, B, C
Which of the following parameters are dimensionless (i.e. no unit?) a) porosity b) Tortuosity C) Specific Surface D) Diffusion coefficient E) Molar absorptivity F) Absorbance
A, B, F
Select all that applies: Particle size can affect which physical property? A) Bulk Density B) Surface Area C) Specific Surface Area D) Powder Flow E) Porosity
ALL :)
Which of the following are disadvantages of solution topical eye ointments? (select all that applies) A) short time to stay on eye surface B) Retention of the solution is influenced by instilled volume C) Poor Availability D) insability E) preservatives
ALL :)
When the ophthalmic solution is susceptible to deterioration through heat, how should it be sterilized?
Add ophthalmic solution to heat-resistant packaging like Amber glass
How should ophthalmic drugs become sterile?
Autoclaving (121ºC for 20-30 mins)
Which of the following pharmacokinetic parameter(s) reflect the lipophilicity of a therapeutic agent? A) Elimination half-life B) Apparently volume distribution C) Creatine Clearance D) Angle of repose E) Elimination rate constant
B) Apparent Volume distribution
Which inactive agent(s) are not added to topical drops: Select all that applies A) Solubility Enhancers B) Preservative C) Flavoring agent D) Color
C - flavoring agent D - Color
Of the 3 common ophthalmic dosage forms, which is the MOST common? A) Solutions B) Suspensions C) Ointments D) A , B E) A, B, C
C) ointments
What is the unit for rate?
Change in something/time
What are two things that heavily impact solubility?
Chemical structure Particle size
Ophthalmic solutions, suspensions, elixirs, tinctures, and lotions are what kind of dosage forms?
Liquid
Surface/interfacial tension is important to which drug forms?
Liquid Dosage forms
What drug form can be classified as both a liquid and a semi-solid liquid dosage form?
Lotion
Which excipient is used to help the irregular flow of a powder particle?
Lubricant
What can be used to perform lyophilization?
Mannitol Potassium Acetate
Which drug delivery system specifies its rate of release?
Transdermal Patch
T/F: Absence of an inactive ingredient will cause a dosage form to not become effective.
True
T/F: Inactive ingredients can be used for multiple things
True
T/F: Preservatives are used for topical eye drops
True -preservatives are used for topical eye drops
Explain what happens to each powder physical property when you decrease the particle size
When you decrease the particle size, Bulk density will increase Surface area and specific surface area will increase Porosity will increase Powder flow will become more irregular thus use a lubricant
Transdermal patches follow which chemical kinetic order?
Zero order because degradation is not affected by initial dose
What are the 3 most common ophthalmic dosage forms?
👁Solutions 👁Suspension 👁Ointments
What are the three kinds of ophthalmic preparations?
👁topical (external surface) 👁 intraocular (administered inside) 👁periocular (adjacent)
Which dosage forms are heavily impacted by viscosity (η)?
Liquid, Suspensions, Semi-Solid, Lotion
Polymeric materials can be used for what?
Modifying release of a drug and viscosity
How can gel-forming ophthalmic solutions be made?
-temperature increases -pH changes -Ion sensitivity -contact with Lysozymes
Retention of solution eye drops is influenced by....
-viscosity -hydrogen ion -concentration instilled volume
One of the most common tonicity adjusting agents for osmotic agents is NaCl. What is the NaCl range that does not cause a pain response?
0.5-2%
What is the range of NaCl used in most persons?
0.7-1.5%
What steroid salts should be used in ophthalmic suspensions?
1) Predisolone acetate 2) dexamethason 3) fluorometholone 4) rimexolone
What are the 4 formulations used to create topical eye drops?
1) Solutions 2) Suspensions 3) Powder for reconstitution 4) Gel-forming solutions
When choosing a delivery system for ophthalmic drugs, what should be considered?
1) good corneal penetration 2) prolong time with corneal tissue 3) Easy instillation for the patient 4) not irritative & comfy 5) appropriate rheological properties
When choosing a salt to create a topical eye drop, what factors must you consider?
1) solubility 2) ocular toxicity 3) pH 4) Tonicity 5) buffer capacity 6) compatibility 7) irritation
Every dosage form must contain what two things?
1. Active ingredient/active pharmaceutical ingredient (API)/Therapeutic agent 2. Inactive ingredients/excipient/adjuvant (these are all the same name for each thing)
What are the two categories of solid dosage forms?
1. Conventional 2. Modified release/controlled release
What are the two types of viscosity?
1. Non-newtonian 2. Newtonian
What are three subgroups of conventional solid dosage forms?
1. Powder 2. Immediate release (conventional tablet) 3. Hard/Soft gelatin capsule
Why are Excipients/Inactive ingredients/Additives necessary for drug formation?
1. Provide properties to make drugs safe, effective, and stable 2. Protect active ingredients from undergoing degradation or microbial growth
Which two factors influences the properties of a non-disintegrating tablet/Modified release dosage form?
1. Tortuosity (τ) 2. Porosity (ε)
A drug has an ability to absorb moisture in the air (hygroscopic). What inactive ingredient can counteract this affect?
A Desiccator
What excipient can be added to prevent bacterial growth on Keppra?
A preservative
What is a gel-forming solution?
A solution that is liquid in a container but gel on contact with the tear fluid
Which of the following therapeutic agents belong to the class of weak acidic compounds? A) Indomethacin B) Penicillin VK C) Aspirin D) All of the above E) A and B F) A and C
D
You are combining powder particles into water in a lab. You notice the particles are mixing with the water. Which statement(s) is/are true? A)Add inactive ingredients to create a suspension B)Add inactive ingredients to create a solution C) The contact angle is at least 90 degrees or greater D) A & C E) A,B,C
D b is wrong because the powder particles will not dissolve in the aqueous environment. Recall, contact angle is hydrophobicity. You are not changing the dissolving properties of the powder particles.
Which of the following will influence the lipophilicity of a therapeutic agent? A) Substituent groups B) Molecular weight C) The volume of drug distribution D) A and B E) A, B, C
D) substituent groups and molecular weight
Contact angle is important for which dosage forms? A) Liquid B) Solid C) Semi-Solid D) A, B E) A, B, C
D: Liquid and Solid
What are osmotic agents used for?
Decrease irritation
Which of the following approaches may be utilized to improve the aqueous solubility of a poorly soluble drug? A) Use of a suitable co-solvent B) Prepare a suitable salt C) Adjust the pH of a solution D) A, B E) A, B, C
E
Which of the following is true about the class of weak acidic drugs? A) They are available as sodium or potassium salt B) They are available as hydrochloride or sulfate salt C) They are more soluble at higher pH D) A, B E) A, C
E
Which of the following is true about the class of weak acidic drugs? A) They are available in an unionized form at a low pH B) They are available as hydrochloride salt C) They are better absorbed t the region of a low pH D) A, B E) A, B, C
E
Which of the following will exhibit inverse relationship when plotted on R.L paper? A) Absorbance against concentration B) True volume against the weight of the powder C) True volume against true density for different powders of an identical weight D) Bulk volume against Bulk density E) Bulk density against particle size
E
Timolol maleate is an example of what ophthalmic drug form? A) Solution B) Suspension C) Powder E) Gel Form
E - Timolol maleate is a gel-forming solution
What is the advantage of gel-forming solutions?
Enhanced contact time which increases bioavailability
T/F: You can use an ear drop for ophthalmic use
False! It is not isotonic
T/F: the eye tolerates hypotonic solutions better than hypertonic
False! The eye tolerates hypertonic solutions better
T/F: Rate's unit for a zero order and first order process are different.
False! They're the same
T/F: Modified release dosage drugs are comprised of solutions
False, made of fine sized particles thus a suspension
T/F: most ophthalmic drugs are sterilized by autoclaving
False. Only a few.
T/F: Ophthalmic preparations used during eye surgeries should be packaged in multi-dose containers.
False. Surgeries utilize single dose and preservatives can irritate the nerves in the open eye.
T/F: The drugs in topical eye solutions always have better bioavailability than those in ophthalmic suspensions.
False; suspensions have a better availability because the drug stays on the surface longer.
T/F: All types of viscosity follows linear kinetics.
False; Non-newtonian follows non-linear kinetics
Which process (es) is/are used to describe elimination, absorption, drug degradation, and drug dissolution?
First and Second Order Process
A graph with the unit 1/T on its x-axis follows which order process?
First order process
Explain a hard vs soft capsule
Hard capsules contain powder inside Soft capsules contain liquid inside. (still considered a solid because of the capsule)
Increasing solubility leads to an increase of dissolution. How does this impact drug absorbance?
High absorbance Increase solubility, Increase dissolution, increase absorbance, and drug availability isn't an issue
What are the most common salt forms used for topical eye drops?
Hydrochloride Sulfate Nitrate Phosphate P.N.S.H
Contact angle measures what?
Hydrophobicity
Colligative properties are important which dosage form?
IV, Ophthalmic solutions
When should preservatives be used for ophthalmic solutions?
In multiple dose eye solutions
Why are viscosity enhancements added to topical drops?
Increase dispersion of the drug in suspensions
What is the pro of creating ophthalmic solutions via lyophilization?
Increases solubility
How does corneal permeability affect availability?
It decreases it which affects the bioavailability.
What are common tonicity adjusting ingredients used in osmotic agents?
NaCl KCl Dextrose Glycerin propylene glycol Mannitol Buffer Salts
Which two equations explains solubility of a drug?
Noise-Whitney Hixson-Crowell
Powder ophthalmic solutions are manufactured by lyophilization. What does this mean?
Ophthalmic solutions are frozen then added to a vacuum to remove the water.
What excipient is used to decrease irritation in topical drops?
Osmotic agents
The most important factor in ophthalmic solutions is?
Particle size
Drugs with limited stability in liquid should be made into what kind of ophthalmic dosage form?
Powder
What is powder as a solid dosage form used for and explain ny Nystatin is an example.
Powder is used for topical or oral use. Nystatin is an example because it contains fine particles and used for topical use. The particles must be small enough to not damage the skin and small particles provide a faster absorption (fast acting)
Which salts are preferred when creating topical eye drops? select all that apply A) Nitrate B) Phosphate C) Salicylate D) Hydrobromide
Preferred Salts: A, B
If hydrochloride, sulfate, nitrate, and phosphate aren't available to use, what salts can you use to prepare topical eye drops?
Salicylate Hydrobromide Bitartrate
Anything that is used topically for local and systemic effects is which drug dosage form?
Semi-Solid
Lotions Ointments Creams Pastes Suppositories Transdermal Products Injectable Inhales or aerosols are examples of which dosage form?
Semi-solid
Which liquid dosage form is a one phase system?
Solution (clear & transparent liquids)
Which liquid dosage form(s) is/are a two phase system?
Suspensions (powders dispersed in liquid medium) Emulsions (two immiscible phages)
Why shouldn't preservatives be used in ophthalmic drugs utilized for surgery?
The eye is open and can irritate the nerves.
Define: Semi-Solid Dosage Forms
These dosage forms are between solid and liquid states
What is true about Psuedomonas aeruginosa? A) most common organism that can affect the eye B) Causes Loss of Vision C) Causes Pink eye D) Grows in the cornea E) A,B,D F)A,B,C,D
What is true about Psuedomonas aeruginosa? A,B,D
When should ophthalmic suspensions drugs be created?
When the drug has... -Insufficient Solubility -Bad stability in solution -Low Bioavailability
Acacia and tragacanth are used for what?
binding agents and emulsifying agents
A delivery system is know as?
dosage form
Tween and Span are used for what?
emulsion and solubility
T/F: Gel forming ophthalmic drugs should have particles of a microfine size
false; suspensions not gel-forming
Equilibrium or saturated solubility is important for which dosage form(s)?
injectable, solution, and suspension dosage forms
Explain the two forms of emulsions: o/w w/o
o/w: oil is dispersed in water w/o: water is dispersed in oil
What are some examples of colligative properties?
vapor pressure, freezing point, osmotic pressure
Which drugs should you make into powder form?
α-chymotrypsin acetylcholine
