shashank jain
DESCRIPTION
Fast Dissolving Tablets.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.
- Examples : alkyl sulfates, propylene glycol esters, lecithin, sucrose.
- 3.Diluents
- 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.
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- 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