Effects of pharmaceutical processing on pepsin activity during the formulation of solid dosage forms

Katalin Kristó, Klára Pintye-Hódi

Research output: Contribution to journalReview article

2 Citations (Scopus)

Abstract

The main aim of this study was to investigate the effects of pharmaceutical technological methods on pepsin activity during the formulation of solid dosage forms. The circumstances of direct compression and wet granulation were modeled. During direct compression, the heat and the compression force must be taken into consideration. The effects of these parameters were investigated in three materials (pure pepsin, and 1:1 (w/w) pepsin-tartaric acid and 1:1 (w/w) pepsin-citric acid powder mixtures). It was concluded that direct compression is appropriate for the formulation of solid dosage forms containing pepsin through application without acids or with acids at low compression force. The effects of wet granulation were investigated with a factorial design for the same three materials. The factors were time, temperature and moisture content. There was no significant effect of the factors when acids were not applied. Temperature was a significant factor when acids were applied. The negative effect was significantly higher for citric acid than for tartaric acid. It was found that wet granulation can be utilized for the processing of pepsin into solid dosage forms under well-controlled circumstances. The application of citric acid is not recommended during the formulation of solid dosage forms through wet granulation. A mathematically based optimization may be necessary for preformulation studies of the preparation of dosage forms containing sensitive enzymes.

Original languageEnglish
Pages (from-to)17-21
Number of pages5
JournalPharmaceutical Development and Technology
Volume18
Issue number1
DOIs
Publication statusPublished - Feb 1 2013

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Keywords

  • Direct compression
  • Enzyme activity
  • Factorial design
  • Pepsin
  • Wet conditions

ASJC Scopus subject areas

  • Pharmaceutical Science

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