BINDERS PHARMACEUTICAL APPLICATIONS

Seshu Kumar Kodati

INTRODUCTION
In the development of tablets, whether manufactured by wet granulation, dry granulation or direct compression, the key aim is to ensure that the resultant product achieves satisfactory physical and performance characteristics throughout its shelf life. This is achieved, in part, through the selection of an appropriate binder which may be introduced in the wet granulation stage, via dry granulation, or by careful selection of directly compressible fillerbinders.

INTRODUCTION
Traditionally, tablets have been manufactured by wet granulation followed by drying, sizing, blending/ lubrication and compression of the final granulation. Direct compression, and to a lesser extent dry granulation, are becoming increasingly popular methods of tablet manufacture. Direct compression requires only blending and compression. Reducing the number of unit operations requires less time and energy consumption, and allows for cost advantages both from an operational and capital investment point of view. However, the inherent compactibility of raw materials becomes more important in direct compression. In this regard, direct compression presents a challenge for many poorly compressible actives. The challenge of achieving desirable tablet mechanical properties, such as tablet strength and friability from a poorly compressible high-dose active, can be overcome by selection of an appropriate tablet binder.

INTRODUCTION
An ideal binder should have good binding properties, as determined by compressibility under pressure, high plasticity, low elasticity and small particle size. Small particle size facilitates even distribution of the binder through the inter-particulate void spaces in a tablet. Uniform binder distribution in the tablet results in decreased pore structure and subsequent enhancement in tablet crushing strength. To reduce friability, a binder with highly plastic properties (high deformability) is essential. A further requirement for a good binder is low hygroscopicity. Excessive uptake of moisture (greater than 5 percent) or high moisture content can lead to instability and sticking during production.

INTRODUCTION
Commonly used binders include: starch, gelatin and sugars as sucrose, glucose, dextrose, and lactose. Natural and synthetic gums which have been used include acacia, sodium alginate, carboxy- methylcellulose, methylcellulose, polyvinyl pyrrolidone, Veegum. Other agents which may be considered binders under certain circumstances are polyethylene glycol, ethylcelulose, waxes, water and alcohol.
There are many excipients used as binders in the direct compression; these include hydroxypropylcellulose (HPC), methylcellulose (MC), povidone (PVP), hydroxypropylmethylcellulose (HPMC), and starches and their derivatives, such as pregelatinized and granulated starches.

INTRODUCTION
The quantity of binder used has considerable influence on the characteristics of the compressed tablets. The use of too much binder or too strong a binder will make a hard tablet which will not disintegrate easily and which will cause excessive wear of punches and dies. Usually materials which have no cohesive qualities of their own will require a stronger binder than those with these qualities.

INTRODUCTION
Binders are used both as a solution and in a dry form depending on other ingredients and method of preparation. The same amount of binder in solution will be more effective than if it were in a dry form and moistened with the solvent. So it is preferable to incorporate the binding agent in solution. If the drug substance is adversely affected by an aqueous binder , a non aqueous binder can be used or binder can be added dry. The direct-compression method for preparing tablets requires a material that not only is free-flowing but also sufficiently cohesive to act as a binder.

MECHANISM OF BINDERS
When binder added to powder diluents mixtures in the form of slurry ,suspension (or) solution. Liquid bridges are developed between the particles and tensile strength of their bonds get increased with the amount of liquid present in binder. Surface tension forces ,capillary pressures are primarily responsible for granule strength and its formation. After this step the excess of moisture content in binder is removed by drying to appropriate levels.In this stage interparticle bonds are resulted from fusion/re crystallization and curing of binding agent with vanderwall forces playing a significant role .

BINDER SELECTION
1. Choosing binder 2. Quantity of binder to be used 3. Mode of use of binder 4. Binders strength
glucose>acacia>gelatin>simple syrup>starch

5. Binders for moisture sensitive drugs

Ex: PVP, HPMC, Polymethacrylates (NE 30 D,Rs 30D) and pregelatinised starch.

BINDER IN DIFFERENT TYPES OF TABLETS

Effervescent tablets:
Effervescence evolving bubbles of gases from liquid due to chemical reaction. Use of binders in effervescence tablets are limited to i) limited water solubility ii) disintegration Binders such as natural gum & starch Cellulose derivatives are not used. Dry binders sucrose, lactose and mannitol are not used. Best to use pvp as dry binder along with ethanol,isopropanol in water.

Sublingual tablets:
They are intended to be placed beneath the tongue and held there until complete absorption of medicament takes place. Must use water soluble excipient lactose of particle size 120mesh . To increase hardness and reduces erosions on edjes use glucose ,sucrose and acacia gums as binders Eg: GTN tablets

BINDER IN DIFFERENT TYPES OF TABLETS

BUCCAL/VAGINAL TABLETS:
Use of viscous natural gum/ synthetic gums/mix of gums , which absorbs moisture to form a hydrated surface layer from which medicament diffuses and available for absorption through buccal mucosa. Eg:HPMC,HPC,EC Muco adhesive polymers are generally used like Eg:carbopol and PAMA

Chewable tablets:
Mainly conceded the chew ability and sweetness. Eg:honey-tab:60% honey + wheat flour Crystaflo-granular molaris co crystallized with syrup +caramel No specific binder is required but us e the sugars which are compress able(method : direct compression) E.g. : Di- pac(97% sucrose+3% dextrin) Nu-Tab(96%sucrose + 4% invert sugar) E molex(95% dextrin +maltose and other saccarhides for improve compress ability)

BINDER IN DIFFERENT TYPES OF TABLETS

Rectal tablets:
Tablet will disintegrate to form a paste within few minutes in the presence of less available water(moisture). So use strong disintegrants like dross carmellose sodium,crosslinked povidone are used.

Lozenzes:
Flavoured medicated dosage forms intended to sucked and held in mouth / pharynx. E g : Beet-sugar Cane-sugar Corn-sugar