This document provides objectives and content for a chapter on tablet dosage forms. It begins by listing 7 learning objectives for students related to different tablet types, ingredients, and modified release forms. It then covers various topics on tablet dosage forms including definitions of immediate and modified release tablets, important ingredients like fillers, binders, and disintegrants, factors that influence powder compaction, and mechanisms of drug release from tablets. The document aims to educate students on the development, formulation, and performance of oral tablet dosage forms.
University Institute of Pharmaceutical Sciences is a flag bearer of excellence in Pharmaceutical education and research in the country. Here is another initiative to make study material available to everyone worldwide. Based on the new PCI guidelines and syllabus here we have a presentation dealing with the tablets and its excipients and Ideal properties of tablet and the methods and equipment for there for manufacturing.
Thank you for reading.
Hope it was of help to you.
UIPS,PU team
It includes the detail information about the different dosage form along with its example and the factors affecting the choice of different dosage form.
University Institute of Pharmaceutical Sciences is a flag bearer of excellence in Pharmaceutical education and research in the country. Here is another initiative to make study material available to everyone worldwide. Based on the new PCI guidelines and syllabus here we have a presentation dealing with the tablets and its excipients and Ideal properties of tablet and the methods and equipment for there for manufacturing.
Thank you for reading.
Hope it was of help to you.
UIPS,PU team
It includes the detail information about the different dosage form along with its example and the factors affecting the choice of different dosage form.
This presentation involves the information about Modified-Release Drug Products, Targeted Drug Delivery Systems and Biotechnological Products in Pharmaceutics
Oral drug delivery is one of the most preferred routes for administering medications due to its convenience, patient compliance, and non-invasiveness. Over the years, significant advancements have been made in oral drug delivery systems to enhance drug bioavailability, control release kinetics, and overcome various physiological barriers. This article provides a comprehensive review of the current state of oral drug delivery systems, including their principles, components, and recent advancements. Moreover, it highlights the challenges associated with oral drug delivery and discusses potential future directions for improving therapeutic outcomes.
BCS Guideline for solubility and Dissolution.pptxImdad H. Mukeri
Briefly explanation of The Biopharmaceutics Classification System (BCS) of drug substance
and its solubility in the pH range of 1–7.5, absorption or intestinal membrane permeability
PillPower The Art and Science of Pharmaceutical Tablets. pptx.Whahidul Hasan
"PillPower: The Art and Science of Pharmaceutical Tablets" is an engaging and informative presentation that delves into the world of tablet formulation, manufacturing, and usage. This visually captivating slide deck explores the intricate blend of art and science involved in creating pharmaceutical tablets that deliver optimal therapeutic outcomes.
From the history of tablet dosage forms to emerging trends in tablet development, this presentation provides a comprehensive overview of the subject. It covers various types of tablets, including compressed tablets, layered tablets, and coated tablets, highlighting their unique features and benefits. The importance of tablets in healthcare and their role in oral ingestion are also emphasized.
With a focus on quality control and regulatory compliance, the presentation sheds light on the rigorous processes involved in tablet formulation development and manufacturing. It explores key concepts such as granulation, compression, and coating, unraveling the intricate steps and techniques that contribute to producing high-quality tablets.
Whether you are a healthcare professional, pharmaceutical enthusiast, or simply curious about the world of tablets, "PillPower: The Art and Science of Pharmaceutical Tablets" offers valuable insights and a visually captivating experience. Discover the fascinating journey from formulation to ingestion and gain a deeper understanding of the complexities behind one of the most common and essential dosage forms in medicine.
This presentation involves the information about Modified-Release Drug Products, Targeted Drug Delivery Systems and Biotechnological Products in Pharmaceutics
Oral drug delivery is one of the most preferred routes for administering medications due to its convenience, patient compliance, and non-invasiveness. Over the years, significant advancements have been made in oral drug delivery systems to enhance drug bioavailability, control release kinetics, and overcome various physiological barriers. This article provides a comprehensive review of the current state of oral drug delivery systems, including their principles, components, and recent advancements. Moreover, it highlights the challenges associated with oral drug delivery and discusses potential future directions for improving therapeutic outcomes.
BCS Guideline for solubility and Dissolution.pptxImdad H. Mukeri
Briefly explanation of The Biopharmaceutics Classification System (BCS) of drug substance
and its solubility in the pH range of 1–7.5, absorption or intestinal membrane permeability
PillPower The Art and Science of Pharmaceutical Tablets. pptx.Whahidul Hasan
"PillPower: The Art and Science of Pharmaceutical Tablets" is an engaging and informative presentation that delves into the world of tablet formulation, manufacturing, and usage. This visually captivating slide deck explores the intricate blend of art and science involved in creating pharmaceutical tablets that deliver optimal therapeutic outcomes.
From the history of tablet dosage forms to emerging trends in tablet development, this presentation provides a comprehensive overview of the subject. It covers various types of tablets, including compressed tablets, layered tablets, and coated tablets, highlighting their unique features and benefits. The importance of tablets in healthcare and their role in oral ingestion are also emphasized.
With a focus on quality control and regulatory compliance, the presentation sheds light on the rigorous processes involved in tablet formulation development and manufacturing. It explores key concepts such as granulation, compression, and coating, unraveling the intricate steps and techniques that contribute to producing high-quality tablets.
Whether you are a healthcare professional, pharmaceutical enthusiast, or simply curious about the world of tablets, "PillPower: The Art and Science of Pharmaceutical Tablets" offers valuable insights and a visually captivating experience. Discover the fascinating journey from formulation to ingestion and gain a deeper understanding of the complexities behind one of the most common and essential dosage forms in medicine.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Francesca Gottschalk - How can education support child empowerment.pptxEduSkills OECD
Francesca Gottschalk from the OECD’s Centre for Educational Research and Innovation presents at the Ask an Expert Webinar: How can education support child empowerment?
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
The Roman Empire A Historical Colossus.pdfkaushalkr1407
The Roman Empire, a vast and enduring power, stands as one of history's most remarkable civilizations, leaving an indelible imprint on the world. It emerged from the Roman Republic, transitioning into an imperial powerhouse under the leadership of Augustus Caesar in 27 BCE. This transformation marked the beginning of an era defined by unprecedented territorial expansion, architectural marvels, and profound cultural influence.
The empire's roots lie in the city of Rome, founded, according to legend, by Romulus in 753 BCE. Over centuries, Rome evolved from a small settlement to a formidable republic, characterized by a complex political system with elected officials and checks on power. However, internal strife, class conflicts, and military ambitions paved the way for the end of the Republic. Julius Caesar’s dictatorship and subsequent assassination in 44 BCE created a power vacuum, leading to a civil war. Octavian, later Augustus, emerged victorious, heralding the Roman Empire’s birth.
Under Augustus, the empire experienced the Pax Romana, a 200-year period of relative peace and stability. Augustus reformed the military, established efficient administrative systems, and initiated grand construction projects. The empire's borders expanded, encompassing territories from Britain to Egypt and from Spain to the Euphrates. Roman legions, renowned for their discipline and engineering prowess, secured and maintained these vast territories, building roads, fortifications, and cities that facilitated control and integration.
The Roman Empire’s society was hierarchical, with a rigid class system. At the top were the patricians, wealthy elites who held significant political power. Below them were the plebeians, free citizens with limited political influence, and the vast numbers of slaves who formed the backbone of the economy. The family unit was central, governed by the paterfamilias, the male head who held absolute authority.
Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
Palestine last event orientationfvgnh .pptxRaedMohamed3
An EFL lesson about the current events in Palestine. It is intended to be for intermediate students who wish to increase their listening skills through a short lesson in power point.
Instructions for Submissions thorugh G- Classroom.pptxJheel Barad
This presentation provides a briefing on how to upload submissions and documents in Google Classroom. It was prepared as part of an orientation for new Sainik School in-service teacher trainees. As a training officer, my goal is to ensure that you are comfortable and proficient with this essential tool for managing assignments and fostering student engagement.
The French Revolution, which began in 1789, was a period of radical social and political upheaval in France. It marked the decline of absolute monarchies, the rise of secular and democratic republics, and the eventual rise of Napoleon Bonaparte. This revolutionary period is crucial in understanding the transition from feudalism to modernity in Europe.
For more information, visit-www.vavaclasses.com
A Strategic Approach: GenAI in EducationPeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
BÀI TẬP BỔ TRỢ TIẾNG ANH GLOBAL SUCCESS LỚP 3 - CẢ NĂM (CÓ FILE NGHE VÀ ĐÁP Á...
tablets_part_1.pdf
1.
2. O6U, FACULTY OF PHARMACY, PHARMACEUTICS 3, DR.OSAMA ELNAHAS
By:
DR. Osama Elnahas
PHD of pharmaceutics and industrial pharmacy
o6u, Faculty of Pharmacy
Egypt
3.
4. objectives
• After reading this chapter, the student will be able to:
• 1. Differentiate between the various types of tablet dosage forms.
• 2. Compare and contrast advantages and disadvantages of the various types of
tablet dosage forms.
• 3. List categories of inert ingredients, with examples, which are employed in
the manufacture of compressed tablets.
• 4. State quality standards and USP compendial requirements for tablets.
• 5. Differentiate between the various types of modified-release dosage forms.
• 6. Compare and contrast advantages and disadvantages of the various types of
modified-release dosage forms.
• 7. List physical-chemical characteristics of drugs that make them candidates
for an extended-release dosage form.
• 8. Explain microencapsulation, embedding, ion exchange, and osmotic pump
as these apply to modified-release dosage forms.
6. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Systemic effect Local effect
Tablet should be (Quality attributes):
Accurate dose Elegant (weight, size, appearance)
Biocompatible
Drug release in a controlled & reproducible way
Hard to resist fracture and erosion during handling
Chemically, physically, microbiologically stable)
7. Critical Quality Attributes
•CQA determination helps the formulator to
concentrate on most critical elements in formulation
Q Attribute Criteria
Content uniformity If API represents < 25% of final mass
Assay If the API is poor stable
Related substances If API is poor stable
Disintegration In case of BCS I or III
Dissolution In case of BCS II or IV
Loss on drying/ Water If API is hygroscopic
Hardness
If dosage form is coated, and API has poor
compaction properties
Friability
If dosage form is coated, and API has poor
compaction properties
8. •Tablets are popular for several reasons:
The oral route represents a
convenient and safe
way of drug administration.
Compared to liquid dosage forms, tablets (and
other solid dosage forms) have general
advantages in terms of the chemical, physical
and microbiological stability of the dosage form.
The preparation procedure
enables accurate
dosing of the drug.
O6u, Faculty of pharmacy, Pharmaceutics 3,
Dr.osama elnahas
Tablets are convenient to handle and can be
prepared in a versatile way with respect to their
use and the delivery of the drug.
Finally, tablets can be relatively cheaply mass produced, with robust and
quality-controlled production procedures giving an elegant preparation of
consistent quality.
9. O6u, Faculty of pharmacy, Pharmaceutics 3,
Dr.osama elnahas
The main disadvantage of tablets as a dosage form is
the problem of poor bioavailability of drugs due to
unfavorable drug properties, e.g. poor solubility, poor
absorption properties and instability in the
gastrointestinal tract.
In addition, some drugs may cause local irritant effects
or otherwise cause harm to the gastrointestinal mucosa
10. O6u, Faculty of pharmacy, Pharmaceutics 3, Dr.osama elnahas
A common means of
classifying tablets is
based on the drug
release pattern from
the tablets.
Immediate
release
Modified-
release tablets.
the drug is intended to be
released rapidly after
administration, or the
tablet is dissolved in liquid
before intake and thus
administered as a solution.
Prolonged release.
Pulsatile release.
Delayed release.
Immediate-release tablets
are the most common type
of tablet and include
disintegrating, chewable,
effervescent, sublingual and
buccal tablets.
11. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Modified-
release tablets.
Modified-release tablets should
normally be swallowed intact.
The term prolonged-release (controlled
release) tablet is used to indicate that the
drug is released slowly at a nearly
constant rate.
If the rate of release is constant during a
substantial period of time, a zero-order
type of release is obtained, i.e. M = kt
(where M is the cumulative amount of
drug released and t is the release time).
12. Modified-
release tablets.
For delayed-release tablets the drug is
liberated from the tablet some time after
administration.
After this period has elapsed, the release is
normally rapid.
The most common type of delayed-release
tablet is a gastro-resistant (also known as
enteric coated) tablet, for which the drug is
released in the upper part of the small
intestine after the preparation has passed the
stomach.
O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
13. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
14. Modified-
release tablets.
O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
A pulsatile release is another means to
increase the time period for drug absorption
after a single administration and is
accomplished by releasing the drug in two
or more pulses.
17. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Their role is to ensure that the tableting operation can run
satisfactorily and that tablets of specified quality are
prepared.
Depending on the intended main function, excipients to be
used in tablets are subcategorized into different groups.
One excipient can affect the properties of a powder or the
tablet in a series of ways and many substances used in tablet
formulations can thus be described as multifunctional.
18. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
19. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
20. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Filler
diluent
Disintegrant Solution binder Dry binder
Glidiant Lubricant Antiadherent
21. Powder
compaction
characteristics
If API represents more than 20% of final mass, so its
compactability may affect the tableting properties.
Compactability can be defined by various
techniques (Heckel plot, Kawakita analysis),
however the simplest way is determination of
deformation mechanism.
Materials may be classified according to their
deformation mechanism; Plastic, elastic,
fragmentation
Understanding deformation mechanism help in
understanding compression cycle and reworkability
of the formulation.
24. Powder compaction characteristics
• Simple way to measure deformation
mechanism:
• Mix Drug with 1% Magnesium
stearate for 5 minutes (Blend I)
• Mix Drug with 1% Magnesium
stearate for 15 minutes (Blend II).
• Use 13 mm flat punch to compress
the powder at 1 ton
• Compress (Blend I), hold for 1
second prior to release (sample A).
• Compress (Blend I), hold for 30
second prior to release (Sample B).
• Compress (Blend II), hold for 1
second prior to release (Sample C).
• Store the compressed tablets
overnight to allow equilibrium
• Measure hardness
• A<B Plastic
• A>C Plastic
• C<A<B Plastic
• A=B or C Fragmentation
• A=B=C Fragmentation
• If powder is not compressed, so it
is elastic
25. Significance of deformation mechanism
•Material with fragmentation pattern: Tablet hardness
is not sensitive to lubricant conc., mixing time,
compression force nor dwell time. However this
material show lower hardness upon rework.
•Materials with plastic pattern: Increase dwell time
results in increase tablet hardness.
•Materials with elastic pattern: Material will rebound
on release of compression force. If bonding is weak,
capping or lamination will occur. Such materials need
plastic filler or wet granulation.
26. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Filler (or diluent)
Tablets normally weigh at least 50
mg.
Therefore, a low dose of a potent drug requires the
incorporation of a substance into the formulation to increase the
bulk volume of the powder and hence the size of the tablet.
Filler is not necessary if the dose of the drug per tablet is high.
possess good technical properties (such as compactability and dilution capacity)
have an acceptable taste cheap
chemically inert non-hygroscopic biocompatible
possess good biopharmaceutical properties (e.g. water soluble or hydrophilic)
27. Filler (or diluent)
Diluent shall be
chosen based on:
• Final tablet weight
• API characteristics
(solubility,
hygroscopicity,
stability,
compactability)
Soluble diluents are
used to improve
solubility of poorly
soluble API.
Insoluble diluents
shall be used for
soluble API.
28. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Lactose
Is the most common filler in tablets.
Dissolves readily in water
has a pleasant taste, is non-hygroscopic
is fairly non-reactive
shows good compatibility.
Its main limitation
Some people have an intolerance to lactose
29. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
30. lactose
Lactose is a soluble diluent that is
available in different physical forms;
powder, spray dried, agglomerates
prepared by roller compactor.
Lactose undergoes fragmentation
deformation under compression, so
its rework is bit difficult.
Compactability of anhydrous lactose
is higher than lactose monohydrate
31. lactos
e
Lactose monohydrate is alpha type, where lactose anhydrous
is Beta type.
The molecular structures of α- and β -lactose differ in the
orientation of a hydrogen- and a hydroxyl group on carbon
atom no.1 in the glucose moiety.
β –lactose dissolves faster than α- type.
Spray dried lactose is a mixture of crystalline/ amorphous
lactose 85/15. Amorphous lactose (Mix of & ) is very
hygroscopic, plastic deformable and lack brittleness of
crystalline lactose.
Roller dried lactose is less hygroscopic.
Amorphous lactose is unstable, and may be converted upon
storage (under high RH) to crystalline lactose. This result in
loss of compressability of lactose spray dried.
32. Maillard reaction (1ry amine API with B lactose):
High temperature,
humidity and alkaline pH
promote the reaction.
The result is yellow,
brown or black polymer.
33.
34. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Other sugars or sugar alcohols, such as
glucose, sucrose, sorbitol and mannitol, have
been used as alternative fillers to lactose,
primarily in lozenges or chewable tablets
because of their pleasant taste.
Mannitol has a negative heat of solution and
imparts a cooling sensation when sucked or
chewed.
35. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Apart from the sugars, perhaps the most widely used fillers
are powdered celluloses of different types.
biocompatible
Chemically inert
have good tablet-forming Disintegrating properties
They are therefore also used as dry binders and disintegrants
in tablets.
hygroscopicity, may be incompatible with drugs prone to
chemical degradation in the solid state.
36. Microcrystalline cellulose (Avicel).
•Microcrystalline Cellulose
One of the most famous diluents that was
introduced by FMC in 1960s to overcome
problems associated with lactose. It is available in
several grades that differs according to particle
size and moisture content. MCC is insoluble
hydrophilic diluent that is undergo plastic
deformation by compression.
prepared by hydrolysis of cellulose followed by spray drying.
37.
38. Final important example of a common filler is
Inorganic substance
dicalcium phosphate dihydrate.
insoluble in water non-hygroscopic
hydrophilic, i.e. easily wetted by water
mainly used in granulation
possesses good flowability
tablet production by direct compaction.
O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
39. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Calcium phosphate
slightly alkaline
May thus be incompatible with drugs
sensitive to alkaline conditions.
42. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Binder adhesive
Added to a drug- filler mixture to
ensure that granules and tablets
can be formed with the required
mechanical strength.
43. Binder
•Binders are added to tablet formulations to add cohesiveness
to powders, to improve bonding to form granules.
•Binders may be used in dried form in DC techniques, or in
solution in wet granulation.
•Binder in solution is more efficient than dry binders.
44. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Binders can be added to a powder in different ways:
As a dry powder which is mixed
with the other ingredients before
wet agglomeration.
During the agglomeration
procedure, the binder might thus
dissolve partly or completely in
the agglomeration liquid
As a solution which is used as
agglomeration liquid during wet
agglomeration. The binder is here
often referred to as a solution
binder
As a dry powder which is mixed
with the other ingredients before
compaction (slugging or
tableting). The binder is here
often referred to as a dry binder.
Both solution binders and
dry binders are included in
the formulation at relatively
low concentrations, typically
2–10% by weight.
45.
46. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Common traditional solution binders
are starch, sucrose and gelatin.
More commonly used binders today, with
improved adhesive properties, are polymers such
as polyvinylpyrrolidone and cellulose derivatives
(in particular hydroxypropyl methylcellulose).
Dry binders are microcrystalline
cellulose and crosslinked
polyvinylpyrrolidone.(Kollidon)
47. Binder in formulation of tablets
• Binder solution may be prepared using aqueous or non-aqueous
solvents.
• Aqueous binders provide higher binding than organics.
• Addition of surfactants improve powder wetting and ease granulation
process.
• Binder solution quantity varies 10-35% based on solubility of
fillers/API. Less aqueous binder solution is required for water soluble
fillers/API blend.
• Non-aqueous solvents are used for moisture-sensitive materials or
low-melting point API.
• Non-aqueous solvents include ethanol, methanol, acetone and
Isopropyl alcohol.
• Adequate precautions shall be taken upon usage organic solvents
(usage of explosion-proof drying systems)
48. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
Disintegrant
is included in the formulation to ensure that the tablet, when in
contact with a liquid, breaks up into small fragments, which
promotes rapid drug dissolution.
Ideally, the tablet should break up into individual drug particles
in order to obtain the largest possible effective surface area
during dissolution.
49. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
50. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
The disintegration process for a tablet occurs in two steps.
First, the liquid wets the
solid and penetrates the
pores of the tablet.
Thereafter, the tablet
breaks into smaller
fragments.
De-aggregation directly into
primary powder particles will
set up conditions for the
fastest possible dissolution of
the drug.
Several mechanisms of action of disintegrants have been
suggested, such as swelling of particles, exothermic wetting
reaction, particle repulsion and particle deformation recovery.
51. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
1. Disintegrants that facilitate water uptake.
These disintegrants act by facilitating the transport of liquids
into the pores of the tablet, with the consequence that the tablet
may break into fragments..
One obvious type of substance that can promote liquid
penetration is surface-active agents.
It has also been suggested that other substances can promote the
liquid penetration, using capillary forces to suck water into the
pores of the tablet.
52. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
2. Disintegrants that will rupture the tablet.
Rupturing of tablets can be caused by swelling of the disintegrant
particles during sorption of water.
However, it has also been suggested that non-swelling disintegrants
can break the tablet and different mechanisms have been suggested.
- recovery of deformed particles to their original shape in contact
with water, i.e. particles which have been deformed during
compaction..
53. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
3.Disintegrants by gas production:
A third group of disintegrants functions by producing
gas, normally carbon dioxide
Such disintegrants are used in effervescent tablets and normally
not in tablets that should be swallowed as a solid.
54. O6U, Faculty of pharmacy, Pharmaceutics 3, Dr. Osama Elnahas
The disintegrant most traditionally used in conventional tablets
is starch, among which potato, maize and corn starches are
commonly used.
The typical concentration range of starch in a tablet formulation
is up to 10%. Starch particles swell in contact with water and
this swelling can subsequently disrupt the tablet.
High-swelling disintegrants are included in the formulation
at relatively low concentrations, typically 1–5% by weight.
55. Disintegrant Type Common Conc.
Common
Croscamellose sodium Super-disintegrant 0.5-5%
Crospovidone Super-disintegrant 2-5%
Sodium Starch glycolate Super-disintegrant 2-8%
Starch Disintegrant 3-25%
Pre-gelatinized starch Disintegrant 5-10%
Less Common
Alginic acid Disintegrant 1-5%
Calcium alginate Disintegrant < 10%
Hydroxypropyl cellulose-
low substituted
Disintegrant
Magnesium aluminum
silicate
Disintegrant