Theophylline Sodium Glycinate

Theophylline sodium glycinate is a soluble salt form of theophylline that dissociates in vivo to release the active theophylline base. Theophylline acts as a non-selective phosphodiesterase inhibitor, preventing the breakdown of cyclic AMP and cyclic GMP in airway smooth muscle cells, leading to bronchodilation. The drug also functions as an adenosine receptor antagonist, blocking A1 and A2 adenosine receptors which mediate bronchoconstriction and mast cell activation. Additionally, theophylline possesses immunomodulatory and anti-inflammatory properties by activating histone deacetylase, which suppresses the transcription of inflammatory genes.
A pharmacokinetic study of theophylline sodium glycinate sustained-release tablets was conducted in 10 healthy subjects using an asymmetric twice-daily regimen: one 0.1 g tablet in the morning and four 0.1 g tablets in the evening for six consecutive days. This regimen produced steady plasma theophylline levels with morning trough levels of 4.97 μg/mL and peak levels of 10.68 μg/mL, while evening peak levels reached 9.72 μg/mL without exceeding toxic concentrations. The asymmetric regimen aligned with the chronobiology of asthma, providing higher drug levels during the night when symptoms typically worsen.

Fig. 1 Mean steady-state plasma theophylline concentration–time profile after oral sustained-release theophylline sodium glycerinate tablets. (Wang P.; et al. 2003)