Abstract

Hydrogen, as a medical gas, is a promising emerging treatment for many diseases related to inflammation and oxidative stress. Molecular hydrogen can be generated through hydrogen ion reduction by a metal, and magnesium-containing effervescent tablets constitute an attractive formulation strategy for oral delivery. In this regard, saccharide-based excipients represent an important class of potential fillers with high water solubility and sweet taste. In this study, we investigated the effect of different saccharides on the morphological and mechanical properties and the disintegration of hydrogen-generating effervescent tablets prepared by dry granulation. Mannitol was found to be superior to other investigated saccharides and promoted far more rapid hydrogen generation combined with acceptable mechanical properties. In further product optimization involving investigation of lubricant effects, adipic acid was selected for the optimized tablet, due to regulatory considerations.

Highlights

  • In recent years, molecular hydrogen has found increasing use as a medical gas that exerts benefits in many diseases and under diverse physiological conditions [1,2,3,4]

  • Several clinical studies confirming the positive effects of hydrogen gas in acute cerebral infarction [9], ischemic stroke [10], hemodialysis [11], type 2 diabetes [12], and metabolic syndrome [13] have been published

  • We recently proposed that molecular hydrogen may be beneficial for the treatment of acute and chronic fatigue [17]

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Summary

Introduction

Molecular hydrogen has found increasing use as a medical gas that exerts benefits in many diseases and under diverse physiological conditions [1,2,3,4]. Several clinical studies confirming the positive effects of hydrogen gas in acute cerebral infarction [9], ischemic stroke [10], hemodialysis [11], type 2 diabetes [12], and metabolic syndrome [13] have been published. Molecular hydrogen can enhance ergogenic effects in athletes [14,15,16]. The spectrum of diseases for which hydrogen has been shown to be effective is broad, due to the fact that many diseases are associated with inflammation and an enhanced production of reactive oxygen and nitrogen species (ROS/RNS) [18,19,20]. The beneficial effects of molecular hydrogen involve activation of the cell’s antioxidant system via the transcription factor Nrf2 [6]. Anti-inflammatory effects [1,22,23] have been attributed to hydrogen

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