Tablets Flashcards by Sofia Gross

two types of solid dosage forms

disintegrating type

non-disintegrating type

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Oral Tablets for Ingestion

Compressed tablets
Multiple compressed tablets
Chewable tablets
Fast dissolving tablets
Delayed action and enteric coat tablets
Sugar and chocolate coated tablets
Gelatin coated tablets
Molded tablets

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Advantages of Tablets

Accurate dosage 
Convenient
Can be scored or coated
Easy to administer
Control release of active
Economical to manufacture

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Disadvantages of Tablets

Mistaken as candy
Formulation sometimes limited
Not useful of vomiting/unconscious patients
Difficulty swallowing

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Components of a Tablet

Active ingredient

Excipients

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Excipients used for tablet

Diluents/ fillers
Binders
Lubricants
Gildants
Anti-adherents
Disintegrants

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Provide bulk to a tablet formulation
Good compaction properties
Flow properties

Diluents or Fillers

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Examples of Diluents or Fillers

Lactose USP
Microcrystalline cellulose
Modified dextrose

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Factors Influencing Choice of Fillers

Compressibility
Flowability
Particle size and distribution
Moisture content
Bulk density
Compatibility with active
Solubility 
Stability
Cost/availability
Inertness
Governmental acceptability

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Promote adhesion of powder particles
Its concentration affects hardness and friability of tablet
Dry or liquid state

Binders

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examples of binders

Starch
Polyvinylpyrrolidone (PVP)*

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Promotes break-up of tablet into smaller pieces after it has been swallowed

Disintegrating Agents

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Disintegrating Agents Mechanism

absorb water and swell

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______ affects rate of disintegration in Disintegrating Agents

Concentration

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Prevent the formulation and formed tablet

from sticking to machinery

Lubricants

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more efficient lubricants are water _____

insoluble

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Improves flowability of powders/granulation.
Allows formulation to flow easily through tableting
machine

Glidants

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In Glidants, flowability is measured using angle of ___ or

____

repose

Flowdex

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Flavors and Sweeteners

Sprayed dried and other flavors
Natural sweeteners
Artificial sweeteners

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Primary reason for using colors: ______

Marketing

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Colors used

FD&C dyes
FD&C lakes
Iron oxides

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Methods of Tablet Preparation

Direct compression
Wet granulation
Lugging (dry granulation)
Novel methods

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the following are examples of novel method:

Fluid bed processing

Hot melt extrusion

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Must be a free-flowing and compressible

formulation

direct compression

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Improve compressibility, flowability, and | content uniformity of powder blend

Wet Granulation

Direct Compression may require ___ to improve flowability. Problems with high dose drugs: ____ Problems with low dose drugs: ____

glidant Compressibility Uniformity

Improves compressibility, flowability, and content uniformity of powder blend

Wet granulation

Stainless steel chamber Airflow causes continual movement More efficient drying Use apparatus to wet granulate and dry

Fluidized bed dryer

characteristics of Wet Granulation

``` Good for poor compressible powders Excellent flow Good content uniformity Stability problems Possible problems with disintegration Less sensitive to over-blended lubrication ```

What are the things in common between Wet granulation and direct compression

blending premix compression

Comparison of the Two Processes: wet granulation and direct compression

Direct Compression - Faster dissolution - Lower levels of disintegrants needed - Increased cost of raw materials Wet Granulation - Produce harder tablets - Slower dissolution - Cost of equipment, time, labor, and energy

Which method does the following: Compacts large masses of powder mixture Crush and size pieces into smaller granules

Dry Granulation Method | Slugging

Properties of Good Tablets

- Physical Stability - Chemical Stability - Esthetic Appearance - Bioavailability - Weight and Content Uniformity

What is meant by Esthetic Appearance

Free of chips/cracks, contamination, uneven coloration

What is meant by Physical Stability

Remain whole during manufacture/transport/ dispensing

Problems in Tableting

``` Capping Improper fill Picking or sticking Crumbling Mottled tablets Non-disintegrating tablets ```

In-Vitro Tests of Finished Tablets

``` Content uniformity Weight uniformity Tablet density and or diameter Hardness Friability Disintegration Dissolution ```

this type of testing does the following: Operates by reciprocating action A basket-rack device Records time for disintegration

USP Disintegration Testing

Factors Affecting Disintegration

Addition of disintegrants Manufacturing method Pressure used for compression Tablet hardness

A Round bottom flasks containing dissolution | media at 37C

USP Apparatus I (Basket) and II (Paddle)

In order to Pass the Dissolution Test, All six tablets dissolved at a value that is some % of the total dose, this is called

Q-value

Other Official Dissolution | Methods

USP method III, IV, V-VII,

Factors Affecting Dissolution

``` Particle size Solubility of drug in solvent Ph of solvent Rate of mixing temperature of media Excipients in formulation ```

Reasons for multiple compression tablets?

Separate incompatible components Make each layer release at a different rate Make each layer different color

Compressed tablets designed to be chewed. Critical considerations in formulation- Organoleptic properties

Chewable Tablets

Tablets designed to dissolve or disintegrate in | mouth in second

Fast-Dissolving Tablets

advantages of Fast-Dissolving Tablets

Good for people who have difficulty swallowing

disadvantages of Fast-Dissolving Tablets

Tablet is generally weak | Moisture sensitive

Reasons for using Buccal and Sublingual Tablets as delivery route?

drug destroyed by gastric fluid drug poorly absorbed from GI tract achieve rapid absorption (SL Nitroglycerin)

____ Used to produce | ‘chocolate’ color

iron-oxides

Used to deliver anti-infective agents or hormones Inserts Dispensed with applicator Compressed tablets

Vaginal tablets

Effervescent Tablets advantages

Rapid disintegration No dissolution problems Mask taste

Effervescent Tablets disadvantages

Expensive High sodium conc Packaged in hermetically sealed containers Special production facility

Tablet Triturates

- rapidly dissolved in water - contain a small amount of potent drug, lactose or sucrose as filler - fragile tablets

____ Tablets are Compress effervescent salts

Effervescent

some excipients required for effervescent tablets

Binders Lubricants Flavors/sweeteners

Acids used in effervescent tablets

citric acid | tartaric acid

salt used in effervescent tablets

bicarbonate

Official dissolution methods: Reciprocating cylinder apparatus- Flow through cell- Transdermal patches-

USP method III IV V-VII

Examples of disintegrating agents

Starch and starch derivatives - croscarmellose starch and sodium starch glycolate

Examples of lubricants

Magnesium stearate* | Talc

Examples of glidants

Silica derivatives | Talc