Abstract

The aim of this work was to develop a gastric juice-resistant tablet formulation of viable lactic acid bacteria (LAB). As excipients, hydroxypropyl-methylcellulose acetate succinate (HPMCAS) and sodium alginate were applied to enhance gastric juice-resistance, and Avicel® as used to modifytablet disintegration in the intestine. The formulation was optimized using statistical experimentaldesign methodology. The influence of the relevant process variables (amounts of excipients applied and compaction force) on the loss of viable cells during the tablet production, on acid stability, and on tablet disintegration time was investigated. It was found that the content of HPMCAS and the compaction force were the most important test variables for tablet preparation. They influence theloss of bacteria during the tableting process, gastric juice resistance, and the disintegration time of tablets after incubation in artificial intestinal fluid. Avicel® had little influence on all three test parameters, while sodium alginate only affected disintegration time in phosphate buffer pH 6.8.

Highlights

  • Lactic acid bacteria (LAB) are a heterogeneous group of gram-positive rods and cocci that use carbohydrates as an energy source and produce lactic acid either as the sole product of metabolism or as the major end product

  • Stated health-promoting effects of LAB include improved absorption of nutrients, alleviation of lactose intolerance symptoms, metabolism of some drugs, reduction of serum cholesterol, decrease of enzymes implicated in carcinogen production, improvement of intestinal motility, stimulation of the immune system, and reduction of tumor incidence

  • As shown by the analysis of the central composite design, the loss of viable bacteria was dependent on the compaction force

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Summary

Introduction

Lactic acid bacteria (LAB) are a heterogeneous group of gram-positive rods and cocci that use carbohydrates as an energy source and produce lactic acid either as the sole product of metabolism or as the major end product. LAB present in the human and animal gut are introduced through fermented milk products, food and feed supplements, and through pharmaceutical products'. LAB have been used to promote health for hundreds of years; their most obvious effect is the inhibition of pathogen growth in traditionally fermented food systems, accomplished primarily by the acidic nature of these cultures[2]. Stated health-promoting effects of LAB include improved absorption of nutrients, alleviation of lactose intolerance symptoms, metabolism of some drugs, reduction of serum cholesterol, decrease of enzymes implicated in carcinogen production, improvement of intestinal motility, stimulation of the immune system, and reduction of tumor incidence. Mixtures of LAB and buffer substances, which raise the pH value of the gastric medium for a few hours after application, should facilitate the transit of viable bacteria from the stomach to the intestine[6]. As in the present study bacteria can be embedded in acid resistant excipients, such as HPMCAS, by direct compression

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