Recent advances in tablet formulation technology

 


Recent advances in tablet formulation technology

The recent trends in tablet formulation are:

1.    Versatile immediate release tablet systems including fast dissolving drug delivery systems, orally disintegrating tablets/ orally dispersible tablets, orally dispersible mini tablets, mouth dissolving/ fast dissolving tablets, novel fixed dose combination tablet ACCU-BREAK technology inactive layer between two different drug layers), conventional effervescent, uncoated and film–coated tablets etc.

2.    Modified release tablet formulations including ring cap coated tablet ALZA, layered tablets (in lay, tablet in tablet, bilayered tablet), novel chewable sustained release tablet and direct compression medicated chewing gum.

3.    Excipient technology is advancing to produce directly compressible materials for both immediate release as in mouth dissolving systems, or for sustained release systems. The research in excipients is meeting pace with the high throughput production of tablets. Research is also advancing into obtaining excipients from natural sources. Various commercial excipients such as Lycoat, Readily coat, Instamodel and Instanute DR are available in the market.

Patented Technologies for Fast Dissolving Tablets

Zydis Technology

Zydis, the best known of the fast-dissolving/disintegrating tablet preparations was the first marketed new technology tablet. The tablet dissolves in the mouth within seconds after placement on the tongue. A 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. The Zydis formulation is also self-preserving because the final water concentration in the freeze-dried product is too low to allow for microbial growth.

Durasolv Technology

Durasolv is the patented technology of CIMA labs. 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.

Orasolv Technology

Orasolv Technology has been developed by CIMA labs. 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.

Flash Dose Technology

Flash dose technology has been patented by Fuisz. 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". Shearform matrices are prepared by flash heat processing.

Wowtab Technology

Wowtab Technology is patented by Yamanouchi Pharmaceutical Co. 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.

Flashtab Technology

Prographarm laboratories have patented the Flashtab technology. Tablets prepared by this system consist of an active ingredient in the form of micro crystals. Drug micro granules may be prepared by using the conventional techniques like coacervation, micro encapsulation, and extrusion spheronisation. All the processing utilized conventional tabletting technology.

Marketed scope in tablet compression technology

The market for tablet compression technology and the demands placed on equipment manufacturers have changed quite significantly in recent years. This has been driven by a number of factors. Firstly, the pharmaceutical industry has seen a significant shift of investments in solid dosage production equipment towards generics and contract manufacturing. As the companies in this segment of the market are, by nature, strongly focused on cost reduction, a big emphasis is placed on productivity, flexibility and process yield (i.e., minimal product loss). Equipment cost and reliability, as well as fast on-site assistance have also become key selection criteria. research and development based companies have also been forced to follow this cost reduction trend. Secondly, the meteoric growth of new pharmaceutical markets in the Middle East and the Far East (e.g., India, China, South Korea) has led investments in solid dosage equipment in these regions to surpass the investments made in North America and Europe. This puts an increased pressure on equipment price and has resulted in several Western based companies moving the design, manufacture and assembly of their equipment to Asia.

Mottling

Unequal distribution of colour on the tablet surface with light and dark areas standing out in an otherwise uniform coloured surface

Cause:

  • Variation in the colors of ingredients (drug and other additives)
  • Drugs with degradation nature and have different colored degraded products
  • Migration of dye to the surface of granulation during drying. At high temperature dyes are easily migrate to surface and spread to upper surface.
  • Uneven distribution of colored adhesive gel solutions resulting in precipitation
  • The improper size either large or small particles enhances color distribution. During preparation dyes are not properly mixed and not selected ideally or any incompatibility will tends to enhance appearance of color on tablet surface.
  • Improper storage conditions.

Remedy:

  • By using bright coloring agent that will mask all the color variations of the ingredients
  • Proper drying by reducing the drying temperature
  • Colored adhesive gel solutions must be added when they are hot too much cooler powder mixtures to avoid precipitation
  • It is better to incorporate fine powder adhesives like acacia and tragacanth into product before adding the granulating fluid
  • By changing the solvent system or binder system
  • Grinding to small particle size

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