Fast Dissolving Tablets

Novel Drug Delivery

Systems
Presented to : Mam Nabeela
Presented by : Group 1
Bilal Bin Shoukat
Ehtisham Naqvi
Ateeb Mazhar
Kaleem Talib
Adeel Rafiq
 CONTENTS
● Introduction
● Design of FDTs
● Mechanism of Superdisintegrants
● Salient Features of FDDDs
● Desired Characteristics & Development challenges of
FDTs
● Formulation Processes for making FDTs
● Drugs eligible for FDTs
● Limitations of FDTs
● Evaluation Parameters
● Future Research Trends in FDTs
 INTRODUCTION

● The concept of mouth dissolving tablets known as MDTs or Fast dissolving/disintegrating tablets
FDTs or Orodispersible tablets as ODTs or Rapidly disintegrating tablets RDTs has emerged with an
objective to improve patient’s compliance, which is convenient in administration and easy
manufacturing, should free from side effects and should exhibit immediate release with better patient
compliance and enhanced bioavailability.

● These are novel dosage forms which dissolve in saliva within a few seconds, when put on tongue.
● are ideal for people who have swallowing difficulties, paediatric, geriatric, and bedridden patients.

● Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the
safest, most convenient and most economical method of drug delivery.
Fast Dissolving Tablets (FDTs)

Definition
“A solid dosage form containing medicinal substances which disintegrates rapidly, usually
within a matter of seconds when placed upon the tongue.”

Orodispersible tablets are uncoated tablets intended to be placed in the mouth where they
disperse rapidly before being swallowed.
Design of Fast dissolving drug delivery system
Mechanism of Super disintegrants (FDTs):
There are four major mechanisms for tablets disintegration as follows:

Swelling Porosity and Capillary Action (Wicking)

Superdisintegrants which act by this mechanism This mechanism suggests that primarily all the particles
work on the fundamental of “swell” and “burst” of the tablet are surface wetted in the given aqueous
media. Water then penetrates into the core of the tablet,
reducing the inter-particle bond thus aiding in breaking
of the tablet. Thus it is termed as capillary action or
wicking

Particle/Particle Repulsive Forces Deformation

This theory states the swelling via tablet made of
“non-swellable” disintegrants. This works on the During tablet compression, disintegrated particles get
principle of electric repulsive force of particles. It is deformed and these deformed particles get into their
mandatory for the tablet to come in contact with normal structure when they come in contact with
water thus generating repulsive force, making aqueous media or water.
particles repel each other and thus the tablet
disintegrates.
Salient Features of FDDDs
FDT products in global Markets
DESIRED CHARACTERISTICS AND DEVELOPMENT CHALLENGES OF
FAST DISINTEGRATING TABLETS:
1. Fast Disintegration
2. Taste of Active Ingredients
3. Drug Properties
4. Tablet Strength and Porosity
5. Moisture Sensitivity
6. Criteria for Fast dissolving Drug Delivery System:

Fast Disintegration
A fast-dissolving drug delivery system is a tablet that dissolves or disintegrates quickly in the oral cavity upon the contact
with saliva, resulting in solution or suspension of the administered medicine also commonly known as fast melt, quick melt,
orally disintegrating tablets, and orodispersible systems.

Taste of Active Ingredients

Exposure of solubilized drug to the oral cavity can be prevented by encapsulation in polymer system or complexation or
more efficient techniques such as coating, microencapsulation, and granulation have been used in combination with the
sweeteners.
Drug Properties

the drugs with poor solubility and high permeability are best suitable moieties for FDTs in a dose of 125 and 250 mg. The
FDT technology should be versatile enough to accommodate unique properties of each drug.

Tablet Strength and Porosity

The FDTs comprise of two component frameworks of lyophilized matrix system that work together to ensure the
development of a successful formulation. The first component is water-soluble polymers such as gelatin, dextran, alginate,and
maltodextrin.This component maintains the shape and provides mechanical strength to the tablets (binder). The second
constituent is matrix-supporting/disintegration-enhancing agents such as sucrose and mannitol, which acts by cementing
the porous framework, provided by the water-soluble polymer and accelerates the disintegration of the FDT.

Moisture Sensitivity

Hygroscopicity is related to its solubility. FDTs should have low sensitivity to humidity. Many highly water-soluble excipients
are used in formulation to enhance fast-dissolving properties as well as to create good mouth feel. Those highly water-soluble
excipients are susceptible to moisture; A good package design or other strategy should be created to protect FDTs from
various environmental conditions.
Criteria for Fast dissolving Drug Delivery System:
Drugs Eligible for Fast Dissolving Tablets
 FORMULATION PROCESSES FOR MAKING FAST-DISSOLVING TABLETS

Many techniques have been reported for the formulation of Fast dissolving tablets or Orodispersible tablets. Here we have
discussed the six major techniques which are widely used for the formulation of these tablets.

1. Freeze drying/ Lyophilisation

2. Tablet moulding
3. Spray drying
4. Direct Compression
5. Sublimation
6. Mass Extrusion

1.Freeze Drying or Lyophilisation

Freeze drying is the process in which water is sublimed from the product after it is frozen. This technique creates an
amorphous porous structure that can dissolve rapidly. Freeze-drying technique is used in order to improve the dissolution
rate and oral bioavailability of drugs with poor solubility and high permeability.

This technique is used in some patented technologies like Zydis, Quicksolv, and Lyoc technologies, which are used to
manufacture RDTs or Rapidly disintegrating tabs.
Zydis® process
Quicksolv Process
In Quicksolv porous solid dosage forms are obtained by freezing an aqueous dispersion/solution of the drug-containing
matrix and then drying it by removing the water using excess of alcohol by solvent extraction.The ideal drug
characteristics required for this technology are relative low aqueous solubility, fine particle size <50 μm, and good
aqueous stability in the suspension.
Advantages
The tablets produced by this technology have very low disintegration time and
Tablets having great mouth feel due to fast melting effect.

Lyoc Process
Lyoc is a porous and solid galenic form obtained by lyophilization of an oil-in-water emulsion placed directly in the blister
alveolus.The method of preparation involves freezing a thickened (paste-like) emulsion containing the active as bulk or as
coated microparticles. This product is capable of accommodating high dose and disintegrates rapidly but possesses poor
mechanical strength.
2. Tablet Molding
3. Spray Drying

Flow chart for spray-

dry process of coating
liquid or solid particles

● In this technique, gelatin is used as a matrix and a supporting agent, mannitol as bulking agent, and
superdisintegrants like croscarmellose or sodium starch glycolate or crospovidone.
● This spray-dried powder, compressed into tablets showed quick disintegration and improved dissolution.
4. Direct Compression
● A direct compression method uses conventional equipment, commonly available excipients, and a limited number of
process steps.
● This process may involve granulation prior to final blend.
● The direct compression tablet's disintegration and solubilization are based on the single or combined action of super
disintegrants, water-soluble excipients, and effervescent agents.
● Tizanidine HCl, Oxybutynin HCl, Rofecoxib are some examples of model drugs that have been formulated as FDT by
direct compression method.

Sugar Based Excipients:

This is another route to approach the direct compression technique. The use of sugar based excipients especially bulking
agents like lacitilol, dextrose,fructose,maltose, mannitol, sorbitol, display high aqueous solubility and sweetness, and hence
impart taste masking property and a pleasant mouth feel. sugar-based excipients are categorized into two types on the basis
of molding and dissolution rate.

● Type 1 saccharides (mannitol and lactose) exhibit low mould-ability but high dissolution rate.
● Type 2 saccharides (maltitol and maltose) exhibit high mould-ability and low dissolution rate
5. Sublimation

● Incorporation of volatile ingredients to generate a porous mixture is subjected to a process of sublimation.

Highly volatile ingredients like benzoic acid, ammonium bicarbonate, ammonium carbonate, camphor may
be compressed along with other excipients into a tablet. By process of sublimation this volatile material is
then removed, leaving behind a highly porous matrix.
6. Mass extrusion
● In this technology the active blend is soften using the solvent mixture of water-soluble methanol
and polyethylene glycol.
● Subsequent expulsion of softened mass through the extruder or syringe to get a cylinder product
and is divided into even segments using heated blade to form tablet.
● The dried cylinder can also be used to coat granules for bitter drugs and thereby achieve taste
masking
7. Cotton candy process

This process is so named as it utilizes a unique spinning mechanism to produce flosslike crystalline structure,
which mimic cotton candy. Cotton candy process involves formation of matrix of polysaccharides or
sacharides by simultaneous action of flash melting and spinning. The matrix formed is partially recrystallized
to have improved flow properties and compressibility. This candy floss matrix is then milled and blended with
active ingredients and excipients and subsequently compressed to FDT. This process can accommodate larger
drug doses and offers improved mechanical strength. However, high-process temperature limits the use of
this process.
 Limitation of Mouth Dissolving Tablets

● The tablets have insufficient mechanical strength. So,careful handling is required.

● The tablets may leave unpleasant taste in mouth if not formulate properly.
● Drugs which are in larger doses are difficult to formulate into Mouth dissolving tablets
e.g.antibiotics like ampicillin about 500mg of the drug.
● Patients who take anticholinergic medications may not be the good candidates for MDT. Same
patients with Sjögren‟s syndrome or dryness of the mouth due to decreased saliva production
may not be good candidates for these tablet formulations.

Disadvantage
● Mouth dissolving tablet is hygroscopic in nature so must be keep in dry place.
● Some time it possesses mouth feeling.
● MDT requires special packaging for properly stabilization & safety of stable product.
Evaluation Parameters
FUTURE RESEARCH TRENDS IN FAST DISINTEGRATING TABLETS

❏ Although FDT technology and products face many challenges as they are fairly new in the
marketplace, these technologies are rapidly evolving and continue to undergo improvement
which will address the future challenges and changing patient and healthcare needs.

❏ Several technologies are used to achieve quick dispersion and drug delivery to the oral cavity.
The four FDT technologies reviewed in this chapter include WOWTAB®, Zydis®, OraSolv®,
and Shearform™.

❏ FDT products have enormous commercial potential, which will be realized in the next decade
as more effective FDT products are being developed to address the unmet needs of the patients.
 References:

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administered drugs on the world health organization model list of essential medicines according
to the biopharmaceutical classification system. Eur J Pharm Biopharm. 2004;58:265–278. [
PubMed] [Google Scholar]: 2005. European Pharmacopoeia 5.0; p. 628.

2. Omaima SA, Mohammed HA, Nagia MA, Ahmed SZ. Formulation and optimization of
mouth dissolve tablets containing rofecoxib solid dispersion. AAPS Pharm Sci Tech. 2006;7:E1–
9. [PMC free article] [PubMed]

3. International Journal of Pharmaceutical Research & Allied Sciences, 2016, 5(2):311-322

Review Article ISSN : 2277-3657 CODEN(USA) : IJPRPM
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