ORAL DISINTEGRATING TABLETS PRESENTER : SHASHANK JAIN GUIDED BY : DR. ROHERA
Transcript
ORAL DISINTEGRATING TABLETS PRESENTER : SHASHANK JAIN GUIDED BY
: DR. ROHERA
Introduction
Why oral drug delivery is preferred ?
So why not continue with the traditional method of oral
delivery?
Dysphasia
Unpleasent taste
Delayed response
Bioavailability problems
What is the solution ?
Oral disintegrating tablets(ODT)/FDDT
Oral Disintegrating Tablets
According to the Guidance ODTs [should] be considered oral
preparations that dissolve/disintegrate rapidly in the oral cavity,
with an in vitro disintegration time of approximately 30 seconds or
less ...
Fig.1. Rapid disintegration of a lyophilize Zydis tablet in
minimal volume of water
Desired criteria for mouth dissolving drug delivery system
1. Not require water to swallow
2. Be compatible with taste masking.
3. Be portable without fragility concern.
4. Have a pleasing mouth feel.
5. Leave minimal or no residue in the mouth
6. Exhibit low sensitivity to environmental conditions as
humidity and temperature.
7. Allows the manufacture of tablet using conventional
processing and packaging equipment at low cost.
Advantages
1. Improved compliance/added convenience
2. No water needed
3. Better taste
4. Improved bioavailability.
5. Suitable for controlled/sustained release actives
6. Allows high drug loading.
7. Adaptable and amenable to existing processing and packaging
machinery
8. Cost- effective .
Key ingredients to use
Should allow quick release of drug
Should not impart bitter taste
Temperature preferred for the excipients should be between
30-35 c
Commom excipients-
Binder
Emulsifiers
Diluents
Disintegrants
Flavor and taste masking agents
1.Binders
Binders keep the composition of these fast-melting tablets
together during the compression stage.
They are critical for achieving the desired sensory and melting
characteristics, and for the faster release of active
ingredients.
Provide smooth texture and disintegration characteristics to
the system.
Examples :Fats such as cocoa butter and hydrogenated vegetable
oils.
2.Emulsifying agents
They aid in rapid disintegration and drug release.
Stabilize the immiscible blends and enhancing
bioavailability.
The range of 0.05 per cent to about 15 per cent by weight of
the final composition.
Sugar-based excipients are mainly used because of their high
aqueous solubility and sweetness in ODT formulations
Improve the textural characteristics that in turn enhance the
disintegration in the mouth
Range of 10 per cent to about 90 per cent by weight of the
final composition.
Such as mannitol, polydextrose, lactitol and starch
hydrolysate
4.Disintegrants
Three main type of disintegrants used-
Effervescent disintegrating agents
Non Effervescent disintegrating agents
Modern approach
-Superdisintegrants
1.Effervescent Disintegrating Agents
When these agents come in contact with water they absorb water
and disintegrate very quickly and impart fast dissolving property
to the tablets.
Disadvantages-
Excipients shows inability to prevent moisture absorption
(Controlled manufacturing enviornment)
The cost of ODTs is higher than the cost of standard tablets
made by direct compression
2.Non Effervescent disintegrating agents
They have their own property which makes them enable to cause
disintegration of tablets.
Directly compressible starches (such as starch 1500)
Modified starches (such as carboxy methyl starches and sodium
starch glycolate)
Starch derivatives (such as amylose)
3.Modern Approach-Superdisintegants
Superdisintegants are generally used at a low level in the
solid dosage form, typically 110% by weight relative to the total
weight of the dosage unit.
Examples :
Crospovidone A1
Crospovidone A2
Crospovidone B
Sodium starch glycolate
Croscarmellose sodium
Avg. particle size and flow index for industrially used
superdisintegrants . Crospovidone A2 found to be best suited .
Taste and flavour
Improve organoleptic characterstic.
They can be-
a) Nutritive Sweeteners-
sugar, dextrose ,fructose etc.
b) Non Nutritive Sweeteners-
aspartame, sugar alcohols, sucralose etc.
Various Approaches for Fast Dissolving Tablets
Freeze drying or lyophilization
Direct compression
Spray drying
Sublimation
Mass extrusion
1.Freeze drying-
What is freeze drying?
Advantages
Non Elevated temperature
Less shelf life stability problem
Enhancing dissolution profile
Major technologies using this phenomenon
1. Zydis
2. Lyoc
3. Quicksolv
1.1 ZYDIS (R.P. Scherer, Inc.)
The first marketed product utilizing this technology .
The ideal drug candidate for Zydis would be chemically stable
and water insoluble, and have a small particle size.
the dose is usually limited to 60 mg
FEATURES ZYDIS COMPRESSED Speed of dispersion < 3 secs >20sec
Mouth Feel Smooth Gritty Dose Handling