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