Objective: To study the effect of theophylline controlled release tablet combined with β2 receptor agonist therapy on airway function and inflammation in patients with bronchial asthma. Methods: A total of 112 patients with bronchial asthma treated in our hospital between June 2014 and December 2015 were selected as the research subjects and randomly divided into two groups: observation group received corticosteroid for anti-inflammation and theophylline controlled release tablet combined with β2 receptor agonist for airway dilation, and control group received glucocorticoid for anti-inflammation and β2 receptor agonist for airway dilation. After 8 weeks of treatment, airway function, signal pathway molecule and cytokine content in serum as well as immune cell content in peripheral blood were determined. Results: After 8 weeks of treatment, VT, FEV1 and PEF levels of observation group were significantly higher than those of control group while FeNO content was significantly lower than that of control group; serum TLR2, MyD88, JNK, IL-4 and IL-5 content of observation group were significantly lower than those of control group while IFN-γ, IL-2, IL-10 and TGF-β content were significantly higher than those of control group; CD4+IFNγ+Th1 cell and CD4+CD25+Foxp3+Treg cell content in peripheral blood of observation group were significantly higher than those of control group while CD4+IL-4+Th2 cell content was significantly lower than that of control group. Conclusions: Theophylline controlled release tablet combined with β2 receptor agonist therapy can improve the airway function in patients with bronchial asthma and reduce the TLR2-mediated inflammation as well as T lymphocyte subset dysfunction.