Pharmaceutics III - Tablets Quiz

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Questions and Answers

What percentage of all other dosage forms do tablets represent?

56%

36%

46% (correct)

66%

Which of the following is NOT an advantage of tablets?

They enable more accurate dosing.

They can easily mask bitter and unpleasant taste.

They are simple to identify.

They require extensive refrigeration. (correct)

Which of the following types of drugs presents the most challenges for tablet formulation?

Stable drugs

Poorly water-soluble drugs (correct)

Highly soluble drugs

Non-compressible substances (correct)

What is one of the reasons why tablets are considered more stable than liquid dosage forms?

They do not contain any solvents. Signup and view all the answers

What type of tablets can be used for sustained release of medication?

Sustained release tablets Signup and view all the answers

Which of the following statements about the disadvantages of tablets is true?

They may cause local irritant effects. Signup and view all the answers

What is a reason that tablets enable more accurate dosing compared to some other forms?

They are less variable in volume. Signup and view all the answers

Which manufacturing challenge is associated with certain drugs when creating tablets?

Resistance to compression into tablet form. Signup and view all the answers

Which sugar alcohol is hygroscopic at humidity above 65%?

Sorbitol Signup and view all the answers

What is a key advantage of cellulose as a filler in tablet formulation?

Biocompatibility Signup and view all the answers

Which type of binder is less likely to remain effective when applied as a dry powder?

Solution binders Signup and view all the answers

Microcrystalline cellulose is primarily used in tablet formulation for which purpose?

As a filler and disintegrant Signup and view all the answers

What property of mannitol makes it unique compared to other sugars?

It has a negative heat of solution Signup and view all the answers

Which of the following is NOT a type of binder used in tablet formulation?

Sorbitol Signup and view all the answers

What is the role of binders in tablet formulation?

To ensure mechanical strength Signup and view all the answers

Which of the following properties describes starch 1500?

Free flowing and directly compressible Signup and view all the answers

Which property is NOT required for a good filler used in tablet formulation?

High reactivity Signup and view all the answers

Which of the following attributes is NOT considered essential for the quality of tablets?

Tablets must always dissolve in less than 5 minutes. Signup and view all the answers

What aspect of tablets does not pertain to their physical stability?

The elegant appearance of the tablet Signup and view all the answers

Which of the following substances is considered a common diluent for tablets?

Dicalcium phosphate dihydrate Signup and view all the answers

What is a potential disadvantage of using lactose as a tablet diluent?

It may cause lactose intolerance in some individuals. Signup and view all the answers

Which statement regarding tablet excipients is FALSE?

All excipients have therapeutic effects. Signup and view all the answers

Which statement best describes the properties of a good filler for tablet formation?

It should be chemically inert and have good biopharmaceutical properties. Signup and view all the answers

Which of the following statements regarding the release of the drug from tablets is accurate?

Release should be controlled and reproducible. Signup and view all the answers

What is the primary role of a disintegrant in tablet formulation?

To ensure the tablet breaks up into small fragments when in contact with liquid. Signup and view all the answers

Which mechanism of action of disintegrants involves the swelling of materials in the presence of fluids?

Swelling in aqueous fluids. Signup and view all the answers

What is the common method of incorporating a disintegrant mixed with other ingredients before granulation called?

Intragranular addition. Signup and view all the answers

Which of the following is an example of a sugar alcohol?

Xylitol. Signup and view all the answers

What is the most commonly used disintegrant in tablet formulations?

Starch. Signup and view all the answers

What occurs when a tablet disintegrates in the presence of aqueous fluids through gas production?

This is known as effervescent disintegration. Signup and view all the answers

What is a negative consequence of inadequate lubrication during tablet formation?

Pitted surface of tablets. Signup and view all the answers

What is the recommended concentration of lubricants in tablet formulations?

Less than 1%. Signup and view all the answers

What is the primary role of a lubricant in the granulation process?

To reduce adhesion between powder and punch faces Signup and view all the answers

Which of the following is a commonly used hydrophilic lubricant?

Sodium Lauryl Sulfate Signup and view all the answers

Which substance acts as both a lubricant and an antiadherent?

Talc Signup and view all the answers

What is the typical concentration range for talc when used as a glidant?

1-2 % Signup and view all the answers

In tablet formulation, how are flavoring agents typically added?

Dissolved in the granulation liquid or as an alcohol solution Signup and view all the answers

What is the purpose of a sorbent in tablet formulation?

To absorb moisture and incorporate liquids or semisolids Signup and view all the answers

Which sweetener is known to be significantly sweeter than sucrose?

Saccharin Signup and view all the answers

What is the main function of colorants in tablet formulation?

To aid in patient identification and compliance Signup and view all the answers

Study Notes

Pharmaceutics III/Pharmaceutical Dosage Forms III - PT 316/PTC 316 - Tablets - Fall 2024

Course instructor: Prof. Dr. Amal Saber Mohammed Abu El-Enin, Head of Pharmaceutics Department
Course grading: 100 marks total
- Midterm: 15 marks
- Practical: 25 marks
- Final Exam: 50 marks
- Oral Exam: 10 marks

Introduction to Tablets and Tablet Excipients: 2 hours
Tablet Types: 2 hours
Manufacturing of Tablets: 2 hours
Tablet Coating and Tablet Defects: 2 hours

Introduction to Tablets

Tablets are solid pharmaceutical preparations holding a single or multiple active ingredients, formed by compressing uniform particle volumes.
Used for local and systemic effects.
Most commonly used for oral administration.
Account for approximately 46% of all other dosage forms.

Advantages of Tablets

Convenient and safe drug administration
More physically and chemically stable than liquid dosage forms
Easier to package and ship than liquids
Enable more accurate dosing
Mask bitter or unpleasant tastes
Comparatively lower manufacturing costs
Simple to identify

Disadvantages of Tablets

Not suitable for poorly water-soluble or poorly absorbable drugs (poor bioavailability).
Some drugs can cause gastrointestinal irritation or harm to the mucous membranes.
Some drugs resist compression into tablets due to their nature
Difficulty in swallowing for some patients.

Quality Attributes of Tablets

Correct drug dose
Elegant appearance, and consistent weight & size
Controlled and reproducible drug release
Biocompatible (no harmful excipients or contaminants)
Enough hardness to withstand handling and prevent erosion

Tablet Components

Active therapeutic agent (drug)
Inactive materials (excipients)

Tablet Excipients

Inert materials added to ensure quality and preparation.
Help create satisfactory compression characteristics:
- Diluents
- Lubricants
- Glidants
Help to create additional physical characteristics:
- Disintegrators
- Colors
- Flavors
- Sweeteners

Fillers/Diluents

Role: Increase the bulk volume of the powder to make it an acceptable size.
- Not needed if the medication dose per tablet is high.
Common Fillers:
- Lactose
- Sugar or sugar alcohols
- Starch
- Cellulose
- Dicalciumphosphate dihydrate

Requirements for a Good Filler

Chemically inert and biocompatible
Non-hygroscopic
Good biopharmaceutical properties (e.g., water-soluble or hydrophilic)
Good technical properties (e.g., good compression properties)
Acceptable taste
Inexpensive

Lactose

Advantages: Water-soluble, pleasant taste, non-hygroscopic, non-reactive, and low cost.
Disadvantages: Some people have lactose intolerance, existing in hydrous, anhydrous, and spray-dried forms.

Other Sugars or Sugar Alcohols

Used in lozenges or chewable tablets due to pleasant taste.
Mannitol: Negative heat of solution = cooling sensation
Sorbitol: Optical isomer of mannitol, hygroscopic above 65% humidity

Starch

Derived from rice, wheat, or potatoes
Free-flowing, directly compressible form; multifunctional (diluent, binder, disintegrant)

Cellulose

Widely used filler
Biocompatible, chemically inert, good tablet-forming and disintegrating properties
Hygroscopic
Often used as dry binder or disintegrant
Microcrystalline cellulose (Avicel) is a common type

Binders/Adhesives

Role: Ensure that granules and tablets have the required mechanical strength (glue that holds particles together).

Different Ways to Add a Binder

Dry binder: Mixed with other ingredients before compaction
Solution binder: Used as a solution (granulating fluid) in wet granulation.

Example of Commonly Used Binders

Dry binders: Microcrystalline cellulose and cross-linked PVP
Solution binders: Starch, sucrose, and gelatin

Types of Binders

Sugars
Natural polymers (starches, gums, gelatin)
Synthetic polymers (methyl, ethyl, hydroxypropyl cellulose, PVP)

Disintegrant

Role: Ensures the tablet breaks into small fragments when it contacts liquid, promoting rapid drug dissolution.
Mechanisms:
- Increase porosity and wettability of the compressed tablet matrix
- Swelling in the presence of aqueous fluids leads to increased internal pressure
- Production of gas when the tablet contacts aqueous fluids (effervescent tablets)

Methods of Disintegrant Addition

Intragranular addition: Mixed with other ingredients prior to granulation, and thus incorporated within the granules
Extragranular addition: Mixed with dry granules before compaction

Commonly Used Disintegrants

Starch
Modified Starch (e.g., Explotab - sodium starch glycolate)
Modified cellulose (e.g., Ac-di-Sol - cross-linked form of sodium carboxymethyl cellulose)
Alginic acid and its salts (high cost)

Lubricants

Role: Ensure tablet formation and ejection with low friction between solid and die wall, facilitating ejection from die cavity
Poor lubrication leads to pitted tablet surfaces
Concentration is less than 1%
Added in the last step before granulation

Common Lubricants

Hydrophobic (water-insoluble):
- Magnesium stearate
- Stearic acid
Hydrophilic (water-soluble):
- Sodium lauryl sulfate
- Polyethylene glycol (PEG)

Antiadherent

Role: Reduces adhesion between powder and punch faces, preventing particles from sticking to punches
Common examples include magnesium stearate, talc, and starch

Glidant

Role: Improves powder flowability by reducing friction between particles
Common examples include talc, colloidal silicon dioxide, and magnesium stearate

Sorbent

Definition: Substances that absorb fluids while remaining in a solid, dry state.
- Moisture absorption
- Incorporating liquid or semi-solid components (oily drugs, flavors) into tablets

Examples of Sorbents

Microcrystalline cellulose
Silica

Flavour

Role: Providing the tablet with a more pleasant taste or masking an unpleasant one
Often added as a solution to the granulation liquid, or mixed with the granules. Flavoring agents are often thermolabile avoiding heat-related degradation
Added after granulation, avoids heat degradation.

Colorant

Role: Aid in identification and patient compliance.
Added during coating or prior to compaction as an insoluble powder or dissolved in the granulation liquid

Sweetener

Role: Used in lozenges, orodispersible, and chewable tablets to replace or limit sugar use
Examples: Mannitol, Saccharin, Aspartame

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Description

Test your knowledge on Pharmaceutics III focusing on tablet formulations and manufacturing processes. This quiz covers the types of tablets, excipients, coatings, and common defects. Prepare to demonstrate your understanding of this essential pharmaceutical dosage form.