Aminophylline Anhydrous

Gangwar, Manish, et al. NeuroQuantology, 2022, 20(11), 1457.

Researchers created anhydrous aminophylline mucoadhesive matrix tablets using natural hydrophilic bioadhesive polymers like HPMC K4M, Carbomer-940, Aspartame, E.C, Lactose to slow the drug's release in the digestive system. The tablets were evaluated for various parameters and all batches had acceptable physical parameters. Tablets from batch F8 (formulation shown as table 6) had good mucoadhesion and in vitro drug release.
Action Mechanism of Aminophylline
Aminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, which relaxes the smooth muscle of the bronchial airways and pulmonary vessels and reduces airway responsiveness to histamine, acetylcholine, adenosine, and allergens. Theophylline competitively inhibits type III and IV phosphodiesterases (PDEs), the enzymes responsible for breaking down cyclic adenosine monophosphate in smooth muscle cells, potentially leading to bronchodilation. Theophylline also binds to adenosine A2B receptors, blocking adenosine-mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylases, preventing the transcription of inflammatory genes that require histone acetylation to begin transcription.

Kaur, Rajneet, et al. Journal of Pharmaceutical Technology, Research and Management, 2017, 5(2), 117-133.

This study focused on the potential of aminophylline to suppress behavioral changes induced by stress in rats. Changes in reduced glutathione, lipid peroxidase, catalase, and superoxide dismutase in restraint-stressed animals were also investigated to determine the biochemical basis of the anti-stress mechanism of aminophylline.
· Evaluation Methods
The animals were subjected to restraint stress before being treated with different doses of aminophylline (1mg/kg, 2mg/kg, and 4mg/kg). Behavioral changes were analyzed to assess the intensity and degree of stress by using various paradigms to assess changes in exploratory behavior, spontaneous activity, and social behavior. As a result of stress, changes in behavioral patterns were assessed by changes in locomotor activity, the number of head drops, and an increase in avoidance behavior.
· Results
Aminophylline (4mg/kg) modulated behavioral changes induced by stress, and significant biochemical changes induced by oxidative stress were observed (p < 0.001). Under stress conditions, TNF-α expression increases and, together with other neuroinflammatory mediators, leads to behavioral changes. Aminophylline modulates TNF-α activity in the brain, thereby creating the potential to counteract and inhibit stress-induced behavioral changes.