final orally disintegrating tablets

8/8/2019 FINAL Orally Disintegrating Tablets

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ORALLY DISINTEGRATING

TABLETS

IRSHAD AHMED

-T.Y.B.


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Definition

ODTs are solid dosage forms containingmedicinal substances which disintegraterapidly, usually in a matter of seconds,when placed on the tongue.

Products of ODT technologies entered themarket in the 1980s

The first ODT form of a drug to get approvalfrom the U.S. FDA was a Zydis ODTformulation of Claritin (loratadine) inDecember 1996.


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Need for ODTs

Orally disintegrating dosage forms are

particularly suitable for patients find it

inconvenient to swallow traditional tablets andcapsules with glass of water.

Pediatric and geriatric patients

Patients who are unwilling to take solid

preparation due to fear of choking

A 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.


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Advantages of ODTs

1) Good for patients with swallowing difficulties.

2) Good for paediatric compliance

3) Convenient to administer during travelling orworking without need of water

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


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Formulation of ODTs

Active ingredient

Disintegrating agents

Binders

Sweeteners

Flavourants

Glidants, lubricants, anti-adherents.


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Formulation of ODTs

Disintegrating agents:Starch and modified starches (e.g. Primogel,

Carboxy methyl Starches, Pregelatinized, StarchUSP, Starch 1500 )

Cross-linked polyvinylpyrrolidone (eg.Povidone).

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

Alginic acid and sodium alginate

Microcrystalline cellulose e.g. - Avicel DG,Avicel PH-101.


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Formulation of ODTs

Binders

MCC (Microcrystalline cellulose)

SMCC (Silicified microcrystalline cellulose )

SMCC1 SMCC2 SMCC3Starch paste , Natural Gums, Liquid Glucose , etc. )

Flavors: -

a bitter product - mint, cherry oranise may be used

a salty product - peach, apricot orliquorice may be used

a sour product - raspberry or liquorice may be used

an excessively sweet product - vanilla may be used


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Formulation methodology Freeze Drying

A process in which water is sublimated from the product after freezing. Lyophilizationis a pharmaceutical technology which allows drying of heat sensitive drugs andbiological at low temperature under conditions that allow removal of water bysublimation.

Lyophilization results in preparations, which are highly porous, with a very high

specific surface area, which dissolve rapidly and show improved absorption andbioavailability.

Moulding

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

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

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


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Formulation methodology

Sublimation

The slow dissolution of the compressed tablet containing evenhighly water-soluble ingredients is due to the low porosity of thetablets. 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 iscompressed into tablets.

The volatile materials were then removed via sublimation, whichgenerates 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 andcompressed to form tablets.


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Patented TechnologiesFor Fast

Dissolving TabletsZydisTechnology

A Zydis tablet is produced by lyophilizing or freeze-drying the drug in amatrix usually consisting of gelatin.

The product is very lightweight and fragile, and must be dispensed in aspecial 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 )


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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 inorder 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)


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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 flashheat 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.


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DrugsFormulated Into ODTs

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.


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DrugsFormulated Into ODTs

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.


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MarketedFast Dissolving Tablets

in IndiaName of the Product Active Ingredients

Imodium Lingual Imodium

Pepcid RPD famotidineZyprexa Zydis olanzapine

Zofran ODT ondansetron

Remeron Soltab mirtazepine

Claritin Reditab micronized loratadine

Feldene Melt piroxicam

Maxalt-MLT rizatriptan


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Conclusion

Orally disintegrating tablets have better

patient acceptance and compliance and

may offer improved biopharmaceutical

properties, improved efficacy, and bettersafety compared with conventional oral

dosage forms.

ODTs are more widely available as OTC

products for the treatment of allergies,cold, and flu symptoms.


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References -

FDA, CDER data standards manual (C-DRG-00201Version008),www.fda.gov/Drugs/DevelopmentApprovalProcess/FormsSubmissionRequirements/ElectronicSubmissions/DataStandardsManualmonographs/ucm071666.htm,accessed Aug. 20, 2009.

Orally Fast Disintegrating Tablets: Developments,Technologies,Taste-Masking and Clinical Studies Yourong Fu,ShichengYang, Seong Hoon Jeong, Susumu Kimura,& KinamParkPurdue University, Departments of Pharmaceutics andBiomedical Engineering,West Lafayette, Indiana, USA.

http://www.pharmainfo.net/reviews/new-generation-tablet-fast-dissolving-tablet.


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THANK YOUu.

final orally disintegrating tablets

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