Isolation and characterization of novel degradation products of Doxofylline using HPLC, FTIR, LCMS and NMR

Raju, Ch. Krishnam; Pandey, Avadhesh Kumar; S, Gururaj; Ghosh, Kaushik; Pola, Arunima; Goud, Palusa Sanath Kumar; Jaywant, Mrunal A.; Navalgund, Sameer G.

doi:10.1016/j.jpba.2017.02.044

Cited by 6 publications

(1 citation statement)

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“…It is a purine alkaloid possessing pharmacological properties , and used as a therapeutic agent for its antiasthmatic and anti-inflammatory activities and a bronchodilating effect on smooth muscles. DFL has been extensively applied for controlling and managing asthma and chronic obstructive pulmonary disease. − The therapeutic mechanism of DFL is related to its ability to inhibit phosphodiesterase activity and appears to have less affinities toward adenosine A 1 and A 2 receptors, showing a better safety profile than another agent, theophylline. A number of clinical trials have shown that DFL is devoid of direct stimulation, effectively avoiding the adverse effects of bronchodilator arrhythmia in patients with respiratory diseases. − …”

Section: Introductionmentioning

confidence: 99%

Solubility and Model Correlation of Doxofylline in Pure Solvents at the Temperature Range of 283.15–323.15 K

et al. 2021

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Doxofylline (DFL) is a theophylline derivative with poor solubility in water. In this paper, the solubility of DFL (as mole fraction) in 17 organic solvents including 4 esters (ethyl acetate, n-propyl acetate, n-butyl acetate, methyl propionate), 8 alcohols (methanol, ethanol, n-propanol, iso-propanol, n-butanol, iso-butanol, sec-butanol, n-pentanol), 3 ketones (acetone, 2-butanone, cyclohexanone), acetonitrile, and water was studied at the temperatures ranging from “T = 283.15 to 323.15 K”. The solubility of DFL in pure solvents was simulated using three semiempirical models (modified Apelblat, λh, and three-parameter Van’t Hoff) and two activity coefficient models (Wilson and NRTL). In addition, the thermodynamic mixing properties (Δmix G, Δmix H, Δmix S, ln (γ1 ∞) and H 1 E,∞) were evaluated using the solubility data and the Wilson model.

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