Disintegrating Agents: Ensuring Efficient
Drug Delivery
Dr. T. B. Barot
particularly in oral solid dosage forms
like tablets and capsules. These agents,
also known as disintegrants or
superdisintegrants, are seemingly simple
ingredients, but their function is vital for
ensuring the effectiveness of a
medication. This document delves into
the world of disintegrating agents,
exploring their types, mechanisms of
1. Definition and Function
defines disintegrants as "agents added
to tablet or capsule formulations to
facilitate the breakup or disintegration of
the tablet or capsule into smaller
particles that dissolve more rapidly in the
gastrointestinal fluids" [1]. Essentially,
disintegrants disrupt the tablet's
structure, allowing it to break down into
smaller particles once it reaches the
Enhanced Dissolution: Disintegration
exposes a larger surface area of the
drug to the digestive fluids. This
facilitates faster dissolution of the
medication, leading to quicker absorption
into the bloodstream and onset of action.
Improved Bioavailability: Faster
dissolution translates to improved
bioavailability, which is the proportion of
the drug that reaches the bloodstream in
its active form. This ensures the
medication can achieve its intended
therapeutic effect.
2. Types of Disintegrating Agents
Disintegrants can be broadly classified
into two categories:
Traditional Disintegrants: These agents
work primarily through a wicking
mechanism. They absorb water from the
surrounding fluids, causing them to swell
and exert a disruptive force within the
tablet matrix, leading to its breakdown.
Examples include:
Starch: A natural and inexpensive option,
but its water-sensitivity can lead to
variability in disintegration time.
Cellulose: Microcrystalline cellulose
(MCC) is a popular choice due to its
good flowability and compressibility.
Superdisintegrants: These are highly
effective disintegrants that achieve rapid
disintegration at low concentrations.
They employ various mechanisms,
including wicking, swelling, and gas
generation:
Sodium Starch Glycolate (SSG): A
widely used superdisintegrant that wicks
water rapidly and swells, causing the
tablet to break apart.
Croscarmellose Sodium (CCS): Another
popular option with excellent water-
wicking and disintegration properties.
Crospovidone: This superdisintegrant
works through a combination of wicking,
swelling, and gas generation due to the
presence of carbon dioxide.
3. Mechanisms of Action
Disintegrants achieve their function
through various mechanisms, depending
on their type:
Wicking: This is the primary mechanism
for traditional disintegrants. The agent
absorbs water from the surrounding
fluids, causing it to swell and put
pressure on the tablet matrix. This
exerted force leads to cracks and breaks
in the tablet, facilitating its disintegration.
Swelling: Some disintegrants, particularly
superdisintegrants, have a high swelling
capacity. As they absorb water, they
swell significantly, disrupting the internal
structure of the tablet and causing it to
break apart.
Gas Generation: Certain
superdisintegrants, like crospovidone,
contain specific components that react
with water to generate carbon dioxide
gas. This gas creates internal pressure
within the tablet, forcing it to disintegrate
rapidly.
4. Applications of Disintegrating Agents
Disintegrating agents are essential
components in various oral solid dosage
forms, including:
Tablets: Both conventional and fast-
disintegrating tablets (ODTs) rely on
disintegrants to ensure proper
breakdown and drug release.
Capsules: Though capsules themselves
dissolve readily, some formulations may
also include disintegrants to aid in the
disintegration of the contained powder or
pellets.
Chewable Tablets: Disintegrants can
improve the mouthfeel and ease of
disintegration for chewable medications.
5. Factors to Consider When Selecting
Disintegrants
The choice of disintegrating agent
depends on several factors:
Desired Disintegration Time: The
formulation might require immediate
disintegration (ODTs) or a more
controlled release profile.
Compatibility with Other Excipients: The
disintegrant should be compatible with
other ingredients in the formulation to
avoid interactions that could affect drug
stability or performance.
Dosage Form: The type of dosage form
(tablet, capsule) and its desired
properties (chewability, taste) can
influence the selection.
Cost and Availability: Traditional
disintegrants are generally less
expensive, while superdisintegrants
often come at a higher cost.
6. Conclusion
Disintegrating agents are seemingly
simple ingredients, but their role in
ensuring efficient drug delivery is
significant. By facilitating rapid
disintegration and promoting faster drug
dissolution, they contribute to improved
bioavailability and a quicker onset

Disintegrating Agents Ensuring Efficient Drug Delivery.pptx

  • 1.
    Disintegrating Agents: EnsuringEfficient Drug Delivery Dr. T. B. Barot
  • 2.
    particularly in oralsolid dosage forms like tablets and capsules. These agents, also known as disintegrants or superdisintegrants, are seemingly simple ingredients, but their function is vital for ensuring the effectiveness of a medication. This document delves into the world of disintegrating agents, exploring their types, mechanisms of
  • 3.
  • 4.
    defines disintegrants as"agents added to tablet or capsule formulations to facilitate the breakup or disintegration of the tablet or capsule into smaller particles that dissolve more rapidly in the gastrointestinal fluids" [1]. Essentially, disintegrants disrupt the tablet's structure, allowing it to break down into smaller particles once it reaches the
  • 5.
    Enhanced Dissolution: Disintegration exposesa larger surface area of the drug to the digestive fluids. This facilitates faster dissolution of the medication, leading to quicker absorption into the bloodstream and onset of action.
  • 6.
    Improved Bioavailability: Faster dissolutiontranslates to improved bioavailability, which is the proportion of the drug that reaches the bloodstream in its active form. This ensures the medication can achieve its intended therapeutic effect.
  • 7.
    2. Types ofDisintegrating Agents
  • 8.
    Disintegrants can bebroadly classified into two categories:
  • 9.
    Traditional Disintegrants: Theseagents work primarily through a wicking mechanism. They absorb water from the surrounding fluids, causing them to swell and exert a disruptive force within the tablet matrix, leading to its breakdown. Examples include:
  • 10.
    Starch: A naturaland inexpensive option, but its water-sensitivity can lead to variability in disintegration time.
  • 11.
    Cellulose: Microcrystalline cellulose (MCC)is a popular choice due to its good flowability and compressibility.
  • 12.
    Superdisintegrants: These arehighly effective disintegrants that achieve rapid disintegration at low concentrations. They employ various mechanisms, including wicking, swelling, and gas generation:
  • 13.
    Sodium Starch Glycolate(SSG): A widely used superdisintegrant that wicks water rapidly and swells, causing the tablet to break apart.
  • 14.
    Croscarmellose Sodium (CCS):Another popular option with excellent water- wicking and disintegration properties.
  • 15.
    Crospovidone: This superdisintegrant worksthrough a combination of wicking, swelling, and gas generation due to the presence of carbon dioxide.
  • 16.
  • 17.
    Disintegrants achieve theirfunction through various mechanisms, depending on their type:
  • 18.
    Wicking: This isthe primary mechanism for traditional disintegrants. The agent absorbs water from the surrounding fluids, causing it to swell and put pressure on the tablet matrix. This exerted force leads to cracks and breaks in the tablet, facilitating its disintegration.
  • 19.
    Swelling: Some disintegrants,particularly superdisintegrants, have a high swelling capacity. As they absorb water, they swell significantly, disrupting the internal structure of the tablet and causing it to break apart.
  • 20.
    Gas Generation: Certain superdisintegrants,like crospovidone, contain specific components that react with water to generate carbon dioxide gas. This gas creates internal pressure within the tablet, forcing it to disintegrate rapidly.
  • 21.
    4. Applications ofDisintegrating Agents
  • 22.
    Disintegrating agents areessential components in various oral solid dosage forms, including:
  • 23.
    Tablets: Both conventionaland fast- disintegrating tablets (ODTs) rely on disintegrants to ensure proper breakdown and drug release.
  • 24.
    Capsules: Though capsulesthemselves dissolve readily, some formulations may also include disintegrants to aid in the disintegration of the contained powder or pellets.
  • 25.
    Chewable Tablets: Disintegrantscan improve the mouthfeel and ease of disintegration for chewable medications.
  • 26.
    5. Factors toConsider When Selecting Disintegrants
  • 27.
    The choice ofdisintegrating agent depends on several factors:
  • 28.
    Desired Disintegration Time:The formulation might require immediate disintegration (ODTs) or a more controlled release profile.
  • 29.
    Compatibility with OtherExcipients: The disintegrant should be compatible with other ingredients in the formulation to avoid interactions that could affect drug stability or performance.
  • 30.
    Dosage Form: Thetype of dosage form (tablet, capsule) and its desired properties (chewability, taste) can influence the selection.
  • 31.
    Cost and Availability:Traditional disintegrants are generally less expensive, while superdisintegrants often come at a higher cost.
  • 32.
  • 33.
    Disintegrating agents areseemingly simple ingredients, but their role in ensuring efficient drug delivery is significant. By facilitating rapid disintegration and promoting faster drug dissolution, they contribute to improved bioavailability and a quicker onset