TABLET FORMULATION DESIGN

TABLET FORMULATION DESIGN. Fakultas Farmasi Universitas Jember.

3. Binder. To ensure that granules and tablets can be formed with the required mechanical strength Holds powders together to form granules Holds granules to form tablets in compression process Binder concentration in tablet formulation  due to tablet’s hardness and friability Binder quality and quantity  Tablet Quality!! Most common binder: glucose, starch paste, gelatin solution, acacia, sucrose.

Incorporation of BINDER. Dry powder Binder powder mixed with other ingredients before wet granulation Binder powder in dry granulation (roller compaction, slugging) Solution binder As a solution in wet granulation Binder can be added either dry with other excipients for granulation or Already dissolved in the granulating fluid Water is the most common granulating fluid.

Typical binder concentration is 2– 2 0 % by weight Binders can be: Insoluble in water, e.g. starch Soluble in water e.g. HPMC Soluble in water and ethanol e.g.Povidone.

Picture2. 5. Bahan Pengikat yang digunakan dalam pembuatan tablet dengan metode granulasi basah :.

Picture1. 6.

4. Disintegrant. 7. Makes the tablet breaks up into small fragments, when in contact with a liquid Promotes rapid drug dissolution.

The liquid wets the solid and penetrates the pores of the tablet. T ablet breaks into smaller fragments (aggregates of primary particles ). The aggregates will de-aggregate into their primary powder particles . Tablet  breaks into small fragments  API dissolve  API absorbed  therapeutic effect.

Hubungan proses disintegrasi , pelepasan , disolusi , dan absorbsi obat.

Disintegrants Addition Method. a. Intragranular Addition Mixed with other ingredients prior to granulation and thus incorporated within the granules b. Extragranular Addition Mixed with the dry granules c. Incorporated as both an intragranular and an extra granular portion.

Disintegrant Mechanism of Action. 11. Water Uptake (= Efek kapiler ) Disintegrants agent that shown water uptake characteristic  amylum , explotap , avicel , primogel Swelling Effect Swelling nature of disintegrant agent will promote tablet disintegration Na alginat > Na CMC > Gelatine > Soluble starch > Starch.

Disintegrant Mechanism of Action. 12. Water Uptake Swelling Effect.

Disintegrant Enzime Amylum Amilase Selullose derivative Selullase Gum Hemiselullase Gelatine Protease Sukrose Invertase Alginate Carragenase.

Penghancur2. 14. Picture2.

5. Antifriction Agent. Prevent friction during compaction process: Friction between tablet-punch and tablet-die Friction between punch and die Friction inter-powder of the mixture Added into powder mixture before compaction.

Lubricant. Lubricants prevent adherence of granule/powder to die wall and to promote smooth ejection from the die after compaction. Lubricants tend to be hydrophobic Under-lubricated blends tend to flow poorly and show compression sticking problems Over-lubricated blends can adversely affect tablet hardness and dissolution rate, as well as tablet strength Eg : Magnesium Stearate, Calcium Stearate , Talc, Stearic Acid, Sodium Lauryl Sulfate, liquid Paraffin, propylene glycol.

Pelicin 1. 17.

Antiadherent. Reduce adhesion between the powder and the punch faces and thus prevent particles sticking to the punches; due to excess moisture or engraved and/or embossed punch face Many lubricants, such as magnesium stearate, have also antiadherent properties Also talc and starch can act as antiadherents.

Pelicin 2. Glidant. Improve flowability of the powder/ granule  good tablet weight uniformity A dded during direct compaction and to granulation before tableting( they reducing interparticulate friction) Common Glidants :.

Pelicin 3. 20.

6. FLAVORING AGENT. Give the tablet a more pleasant taste or to mask an unpleasant one Flavoring agents are often thermo-labile and so cannot be added prior to an operation involving heat They are often mixed with the granules as an alcohol solution (added with essential oil) Can be added with sweeteners: mannitol , dextrose, saccharine, and sucrose.

COLORING AGENT. A dded to tablets to aid identification and patient compliance A dded during coating or added prior to compaction (can be added as an insoluble powder or dissolved in the granulation liquid) Non-therapeutic agent, give no effect on API effectivity and bioavailability, shown good stability.

Pelicin 4. Common coloring agent Dyes ( soluble): Clear solution, max conc. 0.05%, added into binder solution Pigment/ lake ( insoluble): Dispersed into mixture of powder.

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