Review:
On Mouth Dissolving Tablet
Presented By
S. B. THOKE [M. PHARM]
[DEPT OF PHARMACEUTICS]
Content’s  Definition
 Significance
 Requirements of ODTs
 Formulation Methodologies
 Patented Technologies
 Superdi...
Definition

Fast Dissolving Tablets (FDTs) or “mouth dissolving
tablets” (MDTs) which disintegrates or dissolves
rapidly w...
According to European pharmacopoeia, these MDTs
should dissolve/disintegrate in less than three minutes.

US FDA defined O...
Mouth dissolving tablets are also called as
 Orodispersible tablets (ODTs),
 Fast disintegrating tablets,
 Orally disin...
Significance
 It offer all advantages of solid dosage forms
and liquid dosage forms along with special
advantages, includ...
 Pre-gastric absorption of drug avoids hepatic
metabolism, which reduces the dose and
increase the bioavailability.
 The...
Requirements of ODTs
An ideal FDT should
I. Dissolve / disintegrate in the mouth in matter
of seconds without water.
II. H...
Formulation Methodologies
1.
2.
3.
4.
5.
6.
7.
8.
a)
b)
c)

Freeze drying or lyophilization
Molding
Cotton candy process
S...
9. Conventional methods
a)Dry granulation
b)Wet granulation
c)Direct compression

10
1. Freeze drying or lyophilization
This process includes the removal of solvent from a
frozen suspension or solution of dr...
2. Molding
Molded tablets are prepared by using water-soluble
ingredients.
The powder blend is
hydroalcoholic solvent.

mo...
3. Cotton candy process
This process involves formation of matrix of
polysaccharides or saccharides by simultaneous
action...
4. Spray drying
In this method hydrolyzed and nonhydrolyzed
gelatin were used as supporting matrix.
Mannitol as bulking ag...
This technology produces highly porous and fine
powders as processing solvent is evaporated during
process.
Disintegration...
5. Mass extrusion
Involves softening the active blend using the
solvent mixture of water-soluble polyethylene
glycol and m...
6. Nanonization
Nanomelt technology involves reduction in the
particle size of drug by proprietary wet-milling
technique.
...
7. Three-dimensional Printing (3DP)
It is a rapid prototyping (RP) technology.
Prototyping involves constructing specific ...
8. Compaction
a) Melt granulation
Powders are efficiently agglomerated by a melt able
binder.
Advantages:- No water or org...
It involves the use of a hydrophilic waxy binder
(Superpolystate©, PEG-6-stearate).
Superpolystate© having melting point 3...
b) Phase transition process
In this compress powder containing erythritol
(melting point: 122 °C) and xylitol (melting poi...
c) Sublimation
When inert volatile solid ingredients like
ammonium bicarbonate, ammonium carbonate,
benzoic acid, camphor,...
Figure:- Steps Involved in sublimation

23
9. Conventional methods
a) Direct compression
Easiest way to manufacture tablets.
Conventional equipment, commonly availab...
Below critical concentration, tablet disintegration
time is inversely proportional to disintegrants
concentration.
Above
t...
Which are having high aqueous solubility and
sweetness.
It impart taste masking and a pleasing mouthfeel.
Microcrystalline...
b) Wet granulation
Acid component of the effervescent couple
presented in the tablet with lower than 5%, quick
disintegrat...
which consisted of 1–10% of the final weight of
the granule in a fluid bed.
Granules with high porosity and low apparent
d...
c) Dry granulation
Low-density alkali earth metal salts or watersoluble carbohydrates were precompacted, and the
resulting...
Patented Technologies
1. OraSolv technology
OraSolv technology (Cima Labs) produces tablets
by low compression pressure
It...
The carbon dioxide evolved from the reaction may
provide some “fizzing” sensation, which is a
positive organoleptic sensat...
2. DuraSolv Technology
Developed by Ciba, second-generation technology.
To Produce stronger tablets for packaging in
blist...
Key ingredients Non-direct compression filler and lubricant.
Non-direct compression filler particle size 20-65 μm.
e.g. de...
Higher amounts (1–2.5%) of hydrophobic
lubricants, such as magnesium stearate, can be
added.
lubricant blending times can ...
3. WOWTAB Technology
Patented by "Yamanouchi Pharmaceutical Co. "
WOW means "Without Water ".
In this process, API is mixe...
Low moldability saccharides
e.g. lactose, mannitol, glucose, sucrose, and
xylitol.
Tablets with hardness 0-2 kg, when 150 ...
4. Flashtab Technology
Prographarm laboratories
Flashtab technology.

have

patented

the

Drug micro granules may be prep...
2] Swelling agents- carboxymethylcellulose,
starch, modified starch, carboxymethylated
starch, microcrystalline cellulose,...
5. AdvaTab Technology
Patented by Kyowa Hakko Kogyo
Lubrication is dispensed onto each tablet by using
a spray.
10–30 time...
6. Dispersible Tablet Technology
Lek in Yugoslavia was issued patents for
dispersible tablets of dihydroergotoxine and
cim...
Cimetidine formulated with one of disintegrating
agent. It provides rapid swelling and/or good
wetting capability to the t...
7. Pharmaburst Technology
Process involves a dry blend of a drug, flavor, and
lubricant that are compressed into tablets o...
8. OraQuick technology
It utilizes a patented taste masking technology.
KV Pharmaceutical claims its microsphere
technolog...
Tablets can be compressed to achieve significant
mechanical strength without disrupting taste
masking.
KV Pharmaceutical h...
9. Quick –Dis technology
Lavipharm Laboratories Inc. (Lavipharm) invented
this ideal intraoral FDDS.
Thin, flexible, and q...
10. Zydis technology
Zydis is a unique freeze dried oral solid dosage
form.
Dissolves in less than 3 seconds.
Drug is phys...
Matrix contain excipients like
1] Polymers (e.g., gelatine, alginates, and dextrin)
to provide strength and rigidity to ta...
6] Permeation enhancers (e.g., sodium lauryl
sulphate)
to improve transmucosal permeability;
7] pH adjusters (e.g, citric ...
11. Frosta technology
Patented by Akina.
It utilizes core concept of formulating plastic
granules and compressing at low p...
Superdisintegrants employed in ODT
Super
Commercially
disintegrants available grades
Crosslinked
Crosscarmellose®
Cellulos...
Crosslinked
starch

Explotab®
Primogel®

Swells 7-12 folds in
< 30 seconds.

Swells in three
dimensions
and high level
ser...
Marketed product of MDTs
Brand name
Claritin®
RediTabs®
Feldene Melt®
Maxalt® -MLT®
Pepeid® ODT
Zyperxa®
Zofran® ODT
Respe...
Preformulation Studies
1. Bulk Density
Formula
Where :
ρb - Bulk density, M- Weight of powder, and
V- Volume of powder.
2....
3. Compressibility Index
Simplest way for measurement of flow of powder.
Formula
% C.I. = ρt – ρb/ρt x100
4. Hausner ratio...
Flow property

% C.I.

Hosner ratio

Excellent
Good
Fair
Passable
Poor
Very poor
Very, very
poor

≤10
11-15
16-20
21-25
26...
5. Porosity
Formula

ε = ( 1 - ρapp / ρtrue) X 100

Where,
ε- Porosity, ρapp- Apparent density, and
ρtrue- True density.
6...
7. Angle of repose
Formula
ϴ = Tan-1 ( h / r )
Where,
ϴ- Angle of repose, h- Hight of the heap, and
r- Radius of the heap....
Evaluation of Mouth dissolving
1. Thickness
Measured using Vernier calipers.
2. Hardness
Force required to break a tablet ...
3. Uniformity of weight
20 tablets randomly take from lot and weighted
individually to check for weight variation.
Weight ...
4. In-vitro dispersion time test
Drop a tablet in a beaker containing 50ml of
sorrenson’s buffer pH 6.8 & time required fo...
5. Friability test
Determined using Roche friability.
Subjected to 100 revolutions (25rpm/minute).
Formula
f = (1- W0 / W)...
7. Wetting time
Tablet is placed on a piece of tissue paper folded
twice and kept in a Petri dish (ID = 6.5 cm)
containing...
9. Dissolution test
Dissolution study performed using USP
apparatus (paddal speed 50rpm).

II

USP monographs dissolutions...
Afterword withdraw & analyse for physical
characterization (visual defects, hardness,
friability, disintegration, dissolut...
Promising Drugs to be incorporated In FDT
Analgesics and Anti-inflammatory Agents
Anti-Arrhythmic Agents
Anti-bacterial Ag...
Gastro-Intestinal Agents
Histamine H,-Receptor Antagonists
Stimulants
Lipid Regulating Agents
Local Anaesthetics
Neuro -Mu...
Cardiac Inotropic Agents
Corticosteroids
Enzymes
Diuretics

67
References
 Prashant B Pawar, “MOUTH DISSOLVING TABLET: A REVIEW”,
International Journal of Herbal Drug Research, Vol I, ...
 Velmurugan S., “Oral Disintegrating Tablets: An Overview”,
International Journal of Chemical and Pharmaceutical Sciences...
Thank u…!

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mouth dissolving tablet by raja

  1. 1. Review: On Mouth Dissolving Tablet Presented By S. B. THOKE [M. PHARM] [DEPT OF PHARMACEUTICS]
  2. 2. Content’s  Definition  Significance  Requirements of ODTs  Formulation Methodologies  Patented Technologies  Superdisintegrants employed in ODT  Evaluation  References 2
  3. 3. Definition Fast Dissolving Tablets (FDTs) or “mouth dissolving tablets” (MDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth. 3
  4. 4. According to European pharmacopoeia, these MDTs should dissolve/disintegrate in less than three minutes. US FDA defined ODTs as “A solid dosage form containing medicinal substances or active ingredients which disintegrates rapidly within a few seconds when placed up on tongue” 4
  5. 5. Mouth dissolving tablets are also called as  Orodispersible tablets (ODTs),  Fast disintegrating tablets,  Orally disintegrating tablets,  Quick disintegrating tablets,  Fast dissolving tablets,  Rapid dissolving tablets,  Porous tablets,  Quick melt tablets &  Rapid melt tablets. 5
  6. 6. Significance  It offer all advantages of solid dosage forms and liquid dosage forms along with special advantages, includes  It provide good stability, accurate dosing, easy manufacturing, small packaging size & easy to handle.  No need of water to swallow the dosage form.  Easy to administer for paediatric, geriatric & institutionalized patients.  More rapid drug absorption from the pregastric area which may produce Quick onset of action. 6
  7. 7.  Pre-gastric absorption of drug avoids hepatic metabolism, which reduces the dose and increase the bioavailability.  The risk of chocking or suffocation during oral administration avoided.  Good mouth feel property of MDDDS helps to change the basic view of medication as "bitter pill"  Patient’s compliance for disabled bedridden patients and for travelling and busy people, who do not have ready access to water. 7
  8. 8. Requirements of ODTs An ideal FDT should I. Dissolve / disintegrate in the mouth in matter of seconds without water. II. Have sufficient mechanical strength and good package design. III. Not affected by drug properties. IV. Effective taste masking technologies should be adopted for bitter taste drugs. V. Leave minimal or no residue in mouth after oral administration. VI. Exhibit low sensitivity to environment condition such as humidity and temperature. 8
  9. 9. Formulation Methodologies 1. 2. 3. 4. 5. 6. 7. 8. a) b) c) Freeze drying or lyophilization Molding Cotton candy process Spray drying Mass extrusion Nanonization Three-dimensional Printing (3DP) Compaction Melt granulation Phase transition process Sublimation 9
  10. 10. 9. Conventional methods a)Dry granulation b)Wet granulation c)Direct compression 10
  11. 11. 1. Freeze drying or lyophilization This process includes the removal of solvent from a frozen suspension or solution of drug with structure-forming additives. Freeze-drying of drug along with additives imparts glossy amorphous structure resulting in highly porous and lightweight product. MDTs formed by lyophilization have low mechanical strength, poor stability at higher temperature, and humidity 11
  12. 12. 2. Molding Molded tablets are prepared by using water-soluble ingredients. The powder blend is hydroalcoholic solvent. moistened with a Molded into tablets under pressure lower than that used in conventional tablet compression. Solvent is then removed by air-drying. Molded tablets are very less compact than compressed tablets. 12
  13. 13. 3. Cotton candy process This process involves formation of matrix of polysaccharides or saccharides by simultaneous action of flash melting and spinning. Formed matrix is partially re-crystallized to have improved flow properties and compressibility. This candy floss matrix is then milled. Blended with active ingredients and excipients and subsequently compressed to FDTs. 13
  14. 14. 4. Spray drying In this method hydrolyzed and nonhydrolyzed gelatin were used as supporting matrix. Mannitol as bulking agent Sodium starch glycolate or crosscarmellose sodium as superdisintegrant. Acidic substances (citric acid) or alkali substance (sodium bicarbonate) further increase disintegration and dissolution. 14
  15. 15. This technology produces highly porous and fine powders as processing solvent is evaporated during process. Disintegration time < 20 sec 15
  16. 16. 5. Mass extrusion Involves softening the active blend using the solvent mixture of water-soluble polyethylene glycol and methanol. Subsequent expulsion of softened mass through the extruder or syringe. To get a cylinder of the product into even segments using heated blade to form tablets. 16
  17. 17. 6. Nanonization Nanomelt technology involves reduction in the particle size of drug by proprietary wet-milling technique. Nanocrystals of the drug are stabilized against agglomeration by surface adsorption on selected stabilizers, which are then incorporated into MDTs. Advantages For poor water soluble drugs. Fast disintegration/dissolution of nanoparticles . .. leads to increased absorption and bioavailability. Reduction in dose. 17
  18. 18. 7. Three-dimensional Printing (3DP) It is a rapid prototyping (RP) technology. Prototyping involves constructing specific layers that uses powder processing and liquid binding materials. Loose powders in it was fabricated using 3DP process. Based on computer-aided design models TAG tablets seemed due to the rapid water penetration into the tablet resulting from the large pore size 18
  19. 19. 8. Compaction a) Melt granulation Powders are efficiently agglomerated by a melt able binder. Advantages:- No water or organic solvents is needed. For this, purpose high shear mixers are utilized. Product temperature is raised above the melting point of binder by a heating jacket or by the heat of friction generated by impeller blades. 19
  20. 20. It involves the use of a hydrophilic waxy binder (Superpolystate©, PEG-6-stearate). Superpolystate© having melting point 33–37°C and a HLB value 9. So it will not only act as a binder but will also help the disintegration. 20
  21. 21. b) Phase transition process In this compress powder containing erythritol (melting point: 122 °C) and xylitol (melting point: 93 - 95 °C), and then heating at about 93 °C for 15 min. After heating, the median pore size and tablet hardness was increased. Heating process enhances the bonding among particles leads to sufficient hardness of tablets. 21
  22. 22. c) Sublimation When inert volatile solid ingredients like ammonium bicarbonate, ammonium carbonate, benzoic acid, camphor, hexamethylene tetramine, naphthalene, phthalicanhydride, urea and urethane were added to other tablet excipients. Blend was compressed in to a table & finally subjected to sublimation resulting in highly porous structures. Tablets produce by this method exhibit good mechanical strengthhigh, porosity (approximately 30%), dissolved within 15 seconds in saliva. 22
  23. 23. Figure:- Steps Involved in sublimation 23
  24. 24. 9. Conventional methods a) Direct compression Easiest way to manufacture tablets. Conventional equipment, commonly available excipients and a limited number of processing steps are involved in direct compression. Also high doses can be accommodated and final weight of tablet can easily exceed that of other production methods. Tablet disintegration time can be optimized by concentrating the disintegrants. 24
  25. 25. Below critical concentration, tablet disintegration time is inversely proportional to disintegrants concentration. Above the critical concentration level, disintegration time remains approximately constant or even increases. The major drawback of effervescent excipients is their hygroscopicity (i.e., the ability to absorb atmospheric moisture). Another approach is the use of sugar‐based excipients (e.g., dextrose, fructose, isomalt, maltitok, maltose, mannitol, sorbitol, starch hydrolyse, polydextrose, and xylitol). 25
  26. 26. Which are having high aqueous solubility and sweetness. It impart taste masking and a pleasing mouthfeel. Microcrystalline cellulose, cross linked carboxymethyl cellulose sodium, cross linked polyvinyl pyrrolidone and partially substituted hydroxypropyl cellulose, though water insoluble, absorb water and swell due to capillary action and act as effective disintegrants. 26
  27. 27. b) Wet granulation Acid component of the effervescent couple presented in the tablet with lower than 5%, quick disintegration times could be achieved. In the patent, the formulation includes polyalcohols (e.g., mannitol, xylitol, sorbitol, maltitol, erythritol, and lactitol). 1–30% of an edible acid & an active ingredient as the dry mixture wet granulated with an aqueous solution of a water-soluble or water-dispersible polymer (e.g., poly(ethylene glycols), carrageenan, and ethylcellulose). 27
  28. 28. which consisted of 1–10% of the final weight of the granule in a fluid bed. Granules with high porosity and low apparent density disintegration times ranging from 3 to 30 seconds in the saliva were obtained. 28
  29. 29. c) Dry granulation Low-density alkali earth metal salts or watersoluble carbohydrates were precompacted, and the resulting granules were compressed into tablets. Powdered material with a density of 0.2–0.55 g/mL was precompacted to increase the density to 0.4–0.75 g/mL by applying a force ranging from 1 to 9 kN/cm. The resulting granules were compressed into tablets. 29
  30. 30. Patented Technologies 1. OraSolv technology OraSolv technology (Cima Labs) produces tablets by low compression pressure It uses an effervescent disintegration pair that releases gas upon contact with water. Widely used effervescent disintegration pairs Acid sources Carbonate sources Citric acid, Tartaric acid, Sodium bicarbonate, Malic acid, Fumaric Sodium carbonate, acid, Adipic acid, and Potassium bicarbonate, Succinic acids. and Potassium carbonate. 30
  31. 31. The carbon dioxide evolved from the reaction may provide some “fizzing” sensation, which is a positive organoleptic sensation. 20–25% of total weight of tablet effervescent agent is used. OraSolv tablets - soft and fragile nature. PakSolv - Special packaging system  “Dome-shaped” blister package  Prevents the vertical movement of the tablet within the depressions.  Protect the tablets from breaking during transport and storage also offers light, moisture, and child resistance. 31
  32. 32. 2. DuraSolv Technology Developed by Ciba, second-generation technology. To Produce stronger tablets for packaging in blisters or bottles. Tablets have low friability, about 2% or less when tested according to the USP. Hardness of the tablets - at least about 15–20 N. Disintegration time is less than 60 seconds. By Direct compression method tablets produce. conventional tableting methodologies & conventional package equipment are used. 32
  33. 33. Key ingredients Non-direct compression filler and lubricant. Non-direct compression filler particle size 20-65 μm. e.g. dextrose, mannitol, sorbitol, lactose, & sucrose. advantage - quick dissolution and avoid gritty or sandy texture. 60–95% amount of the total tablet weight is used. Direct compressible fillers – at least 85% of the particles are over 100 μm size. Have some of the gritty or sandy texture. 33
  34. 34. Higher amounts (1–2.5%) of hydrophobic lubricants, such as magnesium stearate, can be added. lubricant blending times can also be increased to 10–25 minutes or longer. 0.2–1% lubricant in conventional tablets. Relatively modest compressive force is needed to compress the formulation. 34
  35. 35. 3. WOWTAB Technology Patented by "Yamanouchi Pharmaceutical Co. " WOW means "Without Water ". In this process, API is mixed with a low mouldability saccharide and granulated with a high mouldability saccharide and compressed into tablet. There is no single saccharide that can make tablets having both high strength and fast disintegration properties. 35
  36. 36. Low moldability saccharides e.g. lactose, mannitol, glucose, sucrose, and xylitol. Tablets with hardness 0-2 kg, when 150 mg of such a saccharide is compressed under pressure of 10–50 kg/cm2 using a die 8 mm in diameter. High-moldability saccharides e.g. maltose, oligosaccharides, maltitol, & sorbitol. Produce tablets with hardness above 2 kg when prepared under identical conditions. The typical high- moldability saccharides are 36
  37. 37. 4. Flashtab Technology Prographarm laboratories Flashtab technology. have patented the Drug micro granules may be prepared by using the conventional techniques like coacervation, micro encapsulation, and extrusion spheronisation. Excipients mixtureis prepared by either dry or wet granulation methods. Excipients used - two groups of components: 1] Disintegrating agents- carboxymethylcellulose or insoluble reticulated polyvinylpyrrolidone; and 37
  38. 38. 2] Swelling agents- carboxymethylcellulose, starch, modified starch, carboxymethylated starch, microcrystalline cellulose, and possibly directly compressible sugars. 38
  39. 39. 5. AdvaTab Technology Patented by Kyowa Hakko Kogyo Lubrication is dispensed onto each tablet by using a spray. 10–30 times less hydrophobic lubricant employed & 30–0% stronger than conventional tablets. Handle high drug loading and coated drug particles. Traditional tablets produced using an internal lubrication system, which disperses lubricant on the inside and the surface of the tablets, decrease tablet mechanical strength. 39
  40. 40. 6. Dispersible Tablet Technology Lek in Yugoslavia was issued patents for dispersible tablets of dihydroergotoxine and cimetidine Dihydroergotoxine is poorly water soluble in free base form. Improved dissolution rate of dihydroergotoxine methanesulphonate was observed with dispersible tablets containing 0.8– 10%, preferably about 4% by weight, of an organic acids. 40
  41. 41. Cimetidine formulated with one of disintegrating agent. It provides rapid swelling and/or good wetting capability to the tablets and thereby a quick disintegration. Disintegrating agents e.g. starch or modified starches, microcrystalline cellulose, alginic acid, cross-linked sodium carboxymethyl cellulose, and cyclodextrin polymers. Combination of two or more disintegrating agents produced better disintegration results. 41
  42. 42. 7. Pharmaburst Technology Process involves a dry blend of a drug, flavor, and lubricant that are compressed into tablets on a standard tablet press with stock tooling. uses off- the-shelf coprocessed excipients, depending on the type of active and loading (up to 700mg), dissolves within 30–40 seconds. Manufacture process can be carried out under normal temperature and humanity conditions. The tablets can be packaged in blister packs or bottle. 42
  43. 43. 8. OraQuick technology It utilizes a patented taste masking technology. KV Pharmaceutical claims its microsphere technology, known as MicroMask. Taste masking process does not utilize solvents of any kind, it leads to faster and more efficient production. Lower heat of production than alternative fast‐ dissolving/disintegrating technologies makes OraQuick appropriate for heat‐sensitive drugs. Matrix that surrounds and protects the drug powder in microencapsulated particles is more 43 pliable.
  44. 44. Tablets can be compressed to achieve significant mechanical strength without disrupting taste masking. KV Pharmaceutical has products in development such as analgesics, scheduled drugs, cough and cold, psychotropics, and anti‐infectives 44
  45. 45. 9. Quick –Dis technology Lavipharm Laboratories Inc. (Lavipharm) invented this ideal intraoral FDDS. Thin, flexible, and quick‐dissolving film. Quick‐Dis™ provided in various packaging configurations, unit‐dose pouches to multiple‐dose blister packages. Film with a thickness of 2 mm have disintegration time 5 to 10 seconds & dissolving time, is around 30 seconds. Typical release profile of API is 50% released within 30 seconds and 95% within 1 minute. 45
  46. 46. 10. Zydis technology Zydis is a unique freeze dried oral solid dosage form. Dissolves in less than 3 seconds. Drug is physically trapped in a water soluble matrix, and then freeze dried. Thirteen products are currently available based on zydis technology. In worldwide market, zydis formulations available for oxazepam, lorazepam, loperamide, and enalapril. 46
  47. 47. Matrix contain excipients like 1] Polymers (e.g., gelatine, alginates, and dextrin) to provide strength and rigidity to tablets; 2] Polysaccharides (e.g.,mannitol and sorbitol) to impart crystallinity and hardness to the matrix and to improve palatability; 3] Collapse protectants (e.g, glycin) to prevent the product from shrinking in its packaging during manufacturing or storage; 4] Flocculating agents (e.g, xanthan gum and acacia) to provide uniform dispersion of drug particles; 5] Preservatives(e.g., parabens) to prevent microbial growth; 47
  48. 48. 6] Permeation enhancers (e.g., sodium lauryl sulphate) to improve transmucosal permeability; 7] pH adjusters (e.g, citric acid) to optimize chemical stability; 8] Flavours and sweeteners to improve patient compliance and 9] water to ensure formation of porous units. In US, zydis products availableClaritin Reditab, Dimetapp Quick Dissolve, Feldene Melt, Maxalt-MLT, Pepcid RPD, Zofran FDT, and Zyprexa Zydis. 48
  49. 49. 11. Frosta technology Patented by Akina. It utilizes core concept of formulating plastic granules and compressing at low pressure to produce strong tablets with high porosity. Process involves mixing the porous plastic material with water penetration enhancer and granulated with binder. Used for - aspirin, loratidine, caffeine, and folic acid, vitamins and dietary supplements. 49
  50. 50. Superdisintegrants employed in ODT Super Commercially disintegrants available grades Crosslinked Crosscarmellose® Cellulose Ac-Di-Sol®, Nymce ZSX® Primellose®, Solutab®, Vivasol®, L-HPC Crosslinked PVP Mechanism of action Swells 4-8 folds in < 10 seconds. Swelling and wicking both. Crosspovidon M® Swells very little Kollidon® and returns to Polyplasdone® original size after compression but act by capillary action. Special comment Swells in two dimensions. Direct compression or Granulation Starch free. Water insoluble and spongy in nature so get porous tablet. 50
  51. 51. Crosslinked starch Explotab® Primogel® Swells 7-12 folds in < 30 seconds. Swells in three dimensions and high level serve as sustain release matrix. Crosslinked alginic Acid Alginic acid NF Rapid swelling in aqueous medium or wicking action. Promote disintegration in both dry or wet granulation. Soy Emcosoy® Polysaccharides Calcium silicate Does not contain any starch or Sugar. Used in Nutritional products. Wicking action Highly porous, Light weight. 51
  52. 52. Marketed product of MDTs Brand name Claritin® RediTabs® Feldene Melt® Maxalt® -MLT® Pepeid® ODT Zyperxa® Zofran® ODT Resperdal® MTab TM Klonopin® wafer Imodium Istant Melts Nasea OD Tempra Quicksolv® Active ingredient Loratadine Application Antihistamine Piroxicam Rizatritpan benzoate Femotidene Olazepine Olandansetron NSAIDs Migrane Resperidone Schizophrenia Merck Eli Lilly Galaxo Smith kline Janssen Clonazepam Loperamide HCL Sedation Antidiarrheal Roche Jannsen Ramosetoron HCl Acetaminophen Anti-emetic Analgesic Yamanouchi Bristol-M ters squibb Anti-ulcer Psychotropic Antiemetic company Scherig corporation Pfizer Merck 52
  53. 53. Preformulation Studies 1. Bulk Density Formula Where : ρb - Bulk density, M- Weight of powder, and V- Volume of powder. 2. Tapped Density Formula ρt = M / Vt Where : ρt - Tapped density, M- Weight of powder, and Vt- Minimum volume occupied after tapping. 53
  54. 54. 3. Compressibility Index Simplest way for measurement of flow of powder. Formula % C.I. = ρt – ρb/ρt x100 4. Hausner ratio Hausner ratio is an indirect index of ease of powder flow. Lower the value of Housner ratio better is the flow property. Formula Hausner ratio = ρt/ ρb 54
  55. 55. Flow property % C.I. Hosner ratio Excellent Good Fair Passable Poor Very poor Very, very poor ≤10 11-15 16-20 21-25 26-31 32-37 >38 1.00-1.11 1.12-1.18 1.19-1.25 1.26-1.34 1.35-1.45 1.46-1.59 >1.6 55
  56. 56. 5. Porosity Formula ε = ( 1 - ρapp / ρtrue) X 100 Where, ε- Porosity, ρapp- Apparent density, and ρtrue- True density. 6.Voide Volume Formula V = Vb - Vp Where, V- Voide volume, Vb- Bulk volume, and Vp- Tapped volume. 56
  57. 57. 7. Angle of repose Formula ϴ = Tan-1 ( h / r ) Where, ϴ- Angle of repose, h- Hight of the heap, and r- Radius of the heap. Flow property Excellent Good Fair- aid not needed Angle of repose (degrees) 25-30 31-35 36-40 Passable- must agitate, vibrate 41-45 Poor Very poor 46-55 56-65 Very, very poor >66 57
  58. 58. Evaluation of Mouth dissolving 1. Thickness Measured using Vernier calipers. 2. Hardness Force required to break a tablet by compression in the radial direction. Pfizer hardness testers Monsanto hardness tester. 58
  59. 59. 3. Uniformity of weight 20 tablets randomly take from lot and weighted individually to check for weight variation. Weight variation specification as per IP Average weight of tablet 80 mg or less More than 80 mg but less than 250 mg % Deviation ±10 ±7.5 250 mg or more ±5 59
  60. 60. 4. In-vitro dispersion time test Drop a tablet in a beaker containing 50ml of sorrenson’s buffer pH 6.8 & time required for complete dispersion was determined. 60
  61. 61. 5. Friability test Determined using Roche friability. Subjected to 100 revolutions (25rpm/minute). Formula f = (1- W0 / W) × 100 Where, f- Friability, W0- Weight of the tablets before, and W- Weight of the tablet after the test. 6. In vivo Disintegration time Time required for complete disintegration of tablets in oral cavity determined by administering tablets to 10 healthy volunteers. 61
  62. 62. 7. Wetting time Tablet is placed on a piece of tissue paper folded twice and kept in a Petri dish (ID = 6.5 cm) containing 6 ml of water, and the time for complete wetting is measured. 8. Water absorption ratio This test performed as like wetting time Formula R = 10 ( Wa /Wb) Where, R- Water absorption ratio, Wb- Weight of tablet before water absorption, & Wa- weight of tablet after water absorption. 62
  63. 63. 9. Dissolution test Dissolution study performed using USP apparatus (paddal speed 50rpm). II USP monographs dissolutions conditions should be followed in addition 0.1N HCl, pH 4.5 & 6.8 buffers should be evaluated. 10. Stability study As per ICH Q1A guidelines for accelerated studies. Tablets stored at 40±1ºC/75% ± 5% RH for 4 weeks. 63
  64. 64. Afterword withdraw & analyse for physical characterization (visual defects, hardness, friability, disintegration, dissolution etc.) drug content. 64
  65. 65. Promising Drugs to be incorporated In FDT Analgesics and Anti-inflammatory Agents Anti-Arrhythmic Agents Anti-bacterial Agents Anti-coagulants Anti-Epileptics Anti-Fungal Agents Anti-Gout Agents Anti-Hypertensive Agents Anti-Malarials Anti-Neoplastic Agents And Immunosuppressants Anti Protozoal Agents Anti-Muscarinic Agents Anti-Parkinson Agents 65
  66. 66. Gastro-Intestinal Agents Histamine H,-Receptor Antagonists Stimulants Lipid Regulating Agents Local Anaesthetics Neuro -Muscular Agents Nitrates And Other Anti-Anginal Agents Nutritional Agents Opioid Analgesics Oral Vaccines Proteins, Peptides And Recombinant Drugs Sex Hormones Anti-Thyroid Agents Anxiolytic, Sedatives, Hypnotics And Neuroleptics Tj-Blockers 66
  67. 67. Cardiac Inotropic Agents Corticosteroids Enzymes Diuretics 67
  68. 68. References  Prashant B Pawar, “MOUTH DISSOLVING TABLET: A REVIEW”, International Journal of Herbal Drug Research, Vol I, Issue II;2011, Page no.- 22-29. Debjit Bhowmik, “Fast dissolving tablet: A review on revolution of novel drug delivery system and new market opportunities” Scholars Research Library, Der Pharmacia Lettre, 1 (2); 2009, Page no.- 262-276.  Alok Kumar Gupta, “Fast Dissolving Tablet- A Review”, The Pharma Innovation, Vol. 1(1); 2012, ISSN 2277-7695, Page no.- 1- 7.  V. Dinesh kumar, “A comprehensive review on fast dissolving tablet technology”, Journal of Applied Pharmaceutical Science, 01 (05); 2011, ISSN: 2231-3354, Page no.- 50-58.  A. Gupta, “Recent Trends of Fast Dissolving Tablet - An Overview of Formulation Technology”, International Journal of Pharmaceutical & Biological Archives, 1(1); 2010, Page no.- 1-10. 68
  69. 69.  Velmurugan S., “Oral Disintegrating Tablets: An Overview”, International Journal of Chemical and Pharmaceutical Sciences, Vol.1 (2); Dec. 2010, Page no.- 1-12.  P. Ashish, “A Review- Formulation of Mouth Dissolving tablet”, International Journal of Pharmaceutical and Clinical Science, 1 (1); 2011, Page no.- 1-8.  Bhupendra G Prajapati, “A Review on Recent patents on Fast Dissolving Drug Delivery System”, International Journal of Pharm Tech Research CODEN( USA): IJPRIF ISSN : 0974-4304, Vol.1, No.3; July-Sept 2009, Page no.- 790-798.  Mukesh P. Ratnaparkhi, “Review On: Fast Dissolving Tablet”, Journal of Pharmacy Research, Vol.2, Issue 1; January 2009, Page no.- 5-12.  Tejvir Kaur, “Mouth Dissolving Tablets: A Novel Approach To Drug Delivery”, International Journal of Current Pharmaceutical Research, ISSN- 0975-7066, Vol 3, Issue 1; 2011, Page no.- 1-7.  Jaysukh J Hirani, “Orally Disintegrating Tablets: A Review”, Tropical Journal of Pharmaceutical Research, 8 (2); April 2009, Page no.- 161-172 69
  70. 70. Thank u…! 70

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