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.

• • 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