MOHAMMAD ALI KADIWALA

Definition

“ODTs are solid dosage forms containing medicinal substances which disintegrate rapidly, usually in a matter of seconds, when placed on the tongue”.

• Products of ODT technologies entered the market in the 1980s

• The first ODT form of a drug to get approval from the U.S. FDA was a Zydis ODT formulation of Claritin (loratadine) in December 1996.

Need for ODTs

“Orally disintegrating dosage forms are particularly suitable for patients find it inconvenient to swallow traditional tablets and capsules with glass of water”.

Pediatric and geriatric patientsPatients who are unwilling to take solid

preparation due to fear of chokingA patient with persistent nausea, who may

be in journey, or has little or no access to water

Increased bioavailability and faster onset of action are a major claim of these formulations.

Advantages of ODT’s

1)Good for patients with swallowing difficulties.

2)Good for paediatric compliance

3)Convenient to administer during travelling or working without need of water

4) The pre-gastric drug absorption avoids the first-pass metabolism

Formulation of ODT’s

Active ingredient Disintegrating agents Binders Sweeteners Flavourants Glidants, lubricants, anti-adherents.

Formulation of ODT’sDisintegrating agents: Starch and modified starches (e.g. –

Primogel, Carboxy methyl Starches, Pregelatinized, Starch USP, Starch 1500 )

Cross-linked polyvinylpyrrolidone (eg. Povidone).

Modified celluloses such as cross-linked sodium carboxymethylcellulose (eg. Ac-Di-Sol)

Alginic acid and sodium alginate Microcrystalline cellulose e.g. - Avicel

DG, Avicel PH-101.

Formulation of ODT’sBinders –

MCC (Microcrystalline cellulose)

SMCC (Silicified microcrystalline cellulose )

SMCC1 SMCC2 SMCC3

Starch paste , Natural Gums, Liquid Glucose , etc. )

Flavors: -

a bitter product - mint, cherry or anise may be used

a salty product - peach, apricot or liquorice may be used

a sour product - raspberry or liquorice may be used

an excessively sweet product - vanilla may be used

Formulation methodology Freeze Drying

A process in which water is sublimated from the product after freezing. Lyophilization is a pharmaceutical technology which allows drying of heat sensitive drugs and biological at low temperature under conditions that allow removal of water by sublimation.

Lyophilization results in preparations, which are highly porous, with a very high specific surface area, which dissolve rapidly and show improved absorption and bioavailability.

Moulding

In this method, molded tablets are prepared by using water-soluble ingredients so that the tablets dissolve completely and rapidly.

The powder blend is moistened with a hydro-alcoholic solvent and is molded into tablets under pressure lower than that used in conventional tablet compression.

The solvent is then removed by air-drying. Molded tablets are very less compact than compressed tablets. These possess porous structure that enhances dissolution.

Formulation methodology• Sublimation

The slow dissolution of the compressed tablet containing even highly water-soluble ingredients is due to the low porosity of the tablets. Inert solid ingredients that volatilize readily (e.g.  urea,  ammonium  carbonate,  ammonium  bicarbonate, camphor etc.) were added to the other tablet ingredients and the mixture is compressed into tablets. The volatile materials were then removed via sublimation, which generates porous structures. Additionally, several solvents (e.g. cyclohexane, benzene) can be also used as pore forming agents.

• Direct Compression All the excipients along with the active are weighed,

sieved and compressed to form tablets.

Patented Technologies For Fast Dissolving Tablets

Zydis TechnologyA Zydis tablet is produced by lyophilizing or freeze-drying the drug in a matrix usually consisting of gelatin.

The product is very lightweight and fragile, and must be dispensed in a special blister pack.

Patients should be advised not to push the tablets through the foil film, but instead peel the film back to release the tablet.

The Zydis product is made to dissolve on the tongue in 2 to 3 seconds.

Feldene Melt (Piroxicam 20 mg )

Claritin Reditab (Loratidine 10 mg )

Cont…. Durasolv Technology

The tablets made by this technology consist of a drug, fillers and a lubricant.

Tablets are prepared by using conventional tableting equipment and have good rigidity.

These can be packed into conventional packaging system like blisters.

Durasolv is an appropriate technology for products requiring low amounts of active ingredients.

Parcopa® (levodopa and carbidopa)

NuLev® (hyoscyamine)

Orasolv Technology

In this system active medicament is taste masked.

It also contains effervescent disintegrating agent.

Tablets are made by direct compression technique at low compression force in order to minimize oral dissolution time.

Conventional blenders and tablet machine is used to produce the tablets.

The tablets produced are soft and friable and packaged in specially designed pick and place system.

FazaClo® (clozapine)

Orapred ODT®** (prednisolone sodium phosphate)

Cont…

Flash Dose Technology- Nurofen meltlet, a new form of ibuprofen as melt-in-mouth tablets, prepared using flash dose technology is the first commercial product launched by Biovail Corporation.

- Flash dose tablets consists of self binding shearform matrix termed as "floss". Shear form matrices are prepared by flash heat processing.

Wowtab Technology- WOW means "Without Water ".

- In this process, combination of low mouldability saccharides and high mouldability saccharides is used to obtain a rapidly melting strong tablet.

- The active ingredient is mixed with a low mouldability saccharide and granulated with a high mouldability saccharide and compressed into tablet.

Drugs Formulated Into ODT’s Analgesics and Anti-inflammatory

Agents: e.g. Azapropazone, Meclofenamic Acid, Indomethacin, Phenylbutazone, etc.

Anthelmintics e.g. Albendazole, Mebendazole, Dichlorophen, etc.

Anti-coagulants: e.g.Dicoumarol, Nicoumalone, Phenindione, etc.

Drugs Formulated Into ODT’s Anti-bacterial Agents:

e.g. Penicillin, Ciprofloxacin, Clarithromycin, Clofazimine, Cloxacillin, Demeclocycline, Doxycycline, Erythromycin, Ethionamide,

Anti-Epileptics:

e.g. Carbamazepine, Clonazepam, Ethotoin, Methoin, etc.

Anti-Fungal Agents:

e.g. Amphotericin, Clotrimazole, Econazole Nitrate, Fluconazole, Fiucytosine, Griseofulvin, Itraconazole, Ketoconazole, Miconazole, Natamycin, Nystatin. Etc.

Marketed Fast Dissolving Tablets in IndiaName of the Product Active Ingredients

Imodium Lingual Imodium

Pepcid RPD famotidine

Zyprexa Zydis olanzapine

Zofran ODT ondansetron 

Remeron Soltab mirtazepine 

Claritin Reditab micronized loratadine

Feldene Melt piroxicam

Maxalt-MLT rizatriptan

Conclusion

Orally disintegrating tablets have better patient acceptance and compliance and may offer improved biopharmaceutical properties, improved efficacy, and better safety compared with conventional oral dosage forms.

ODTs are more widely available as OTC products for the treatment of allergies, cold, and flu symptoms.

THANK YOU….