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Formulation development of vitamin C-based effervescent blend suitable for direct compression

This article presents the findings from a study to establish optimum formulation parameters for effective effervescent vitamin C tablet production.

Introduction

Oral solid dosage forms are the most used means of medication administration due to their ease of assumption, transport and greater stability. Conventionally, tablets are more common because, with good formulation, the manufacturing process is simple and relatively low cost.1

One of the most challenging product development stages for formulators is designing a multivitamin formulation that is as stable as possible”

Active pharmaceutical ingredients (APIs) or supplements delivered through oral dosage forms may encounter the risk of low absorption, but this may be overcome by administering the drug in liquid form. However, because many APIs show limited stability in liquid form, effervescence application has provided a good solution; drug dissolution and immediate consumption enables faster and more complete absorption compared to conventional tablets. Several advantages should be considered, including improved patient compliance (since there is no need to swallow tablets), less stomach and intestinal irritation, accurate dosing and more reproducible pharmacokinetics, to name a few. However, process manufacturing and blend formulation require some specific arrangements in the effervescent field:

  • Larger tablets
  • Complex production and need for specialist packaging materials
  • Tasteless and water-soluble lubricants that are non-toxic.

Lubricant is, for this reason, a critical element that requires thorough evaluation. Magnesium stearate, as with other water-insoluble lubricants, prevents obtaining a clear transparent solution and retards the disintegration and dissolution that is required to be rapid in effervescent tablets.2

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