Pharmaceutical Tablet Preparation Process

Most compacted (compressed) tablets consist of the drug substance(s) and a number of excipients. These excipients may include fillers (diluents), binders, disintegrating agents, lubricants, and glidants. Approved FD&C and D&C dyes or lakes, flavors, and sweetening agents also may be present.

  • Fillers or diluents are added when the quantity of drug substance(s) is too small or the properties of the drug substance do not allow satisfactory compaction in the absence of other ingredients.
  • Binders impart adhesiveness to the powder blend and promote tablet formation and maintenance of drug substance uniformity in the tableting mixture.
  • Disintegrating agents facilitate reduction of the tablet into small particles upon contact with water or biological fluids.
  • Lubricants reduce friction during the compaction and ejection cycles.
  • Glidants improve powder fluidity, powder handling properties, and tablet weight control.
  • Colorants are often added to tablet formulations for aesthetic value or for product identification.

Tablets are prepared from formulations that have been processed by one of three general methods: wet granulation, dry granulation (roll compaction or slugging), or direct compression.

Wet granulation: Involves the mixing of dry powders with a granulating liquid to form a moist granular mass that is dried and sized prior to compression. It is particularly useful in achieving uniform blends of low-dose drug substances and facilitating the wetting and dissolution of poorly soluble, hydrophobic drug substances.

Dry granulation: Can be produced by passing powders between rollers at elevated pressure (roll compaction). Alternatively, dry granulation also can be carried out by the compaction of powders at high pressures on tablet presses, a process also known as slugging. In either case, the compacts are sized before compression. Dry granulation improves the flow and handling properties of the powder formulation without involving moisture in the processing.

Direct compression: Tablet processing involves dry blending of the drug substance(s) and excipients followed by compression. The simplest manufacturing technique, direct compression, is acceptable only when the drug substance and excipients possess acceptable flow and compression properties without prior process steps.

Tablets may be coated to protect the ingredients from air, moisture, or light; to mask unpleasant tastes and odors; to improve tablet appearance; and to reduce dustiness. In addition, coating may be used to protect the drug substance from acidic pH values associated with gastric fluids or to control the rate of drug release in the gastrointestinal tract.

The most common coating in use today is a thin film coating composed of a polymer that is derived from cellulose.

Sugar coating is an alternative, less common approach. Sugar-coated tablets have considerably thicker coatings that are primarily sucrose with a number of inorganic diluents.

A variety of film-coating polymers are available and enable the development of specialized release profiles. These formulations are used to protect acid-labile drug substances from the acidic stomach environment as well as to prolong the release of the drug substance to reduce dosing frequency.

Related Article: Drug Product Quality Tests for Oral Dosage Form

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