A population of 20 normal lactating females between the ages of 20 and 35 years was treated with a single 5 mg/kg intragluteal dose of dyphylline, 7-(2,3-dihydroxypropyl)theophylline. The distribution of the drug between blood and milk and its pharmacokinetics of elimination were determined. The apparent volume of distribution (Vd) of dyphylline was found to be 0.505 +/- 0.162 l./kg, the elimination rate constant (Kel) was 0.228 +/- 0.055 hr-1, the biological half-life (t1/2) was 3.21 +/- 0.76 hr, and the total body clearance (CI) was 0.109 +/- 0.036 l./kg/hr. The ratio described by dyphylline distribution between milk and serum (M/S) was 2.08 +/- 0.52. The elimination rate from milk was equivalent to that from blood.