Time released theophylline for chronotheraputic treatment of nocturnal asthma

Alhassan H Aodah, Saleh Al-Suwayeh, Ehab I Taha, Alaa Eldeen Bakry Yassin

Abstract


The aim of this work is designing and evaluation of chronotherapeutic dosage form of theophylline (TPH). Film coated tablets were formulated using an Eudragit S-100 based coating formula as time released system and optimized toward a prospective control of nocturnal asthma. Core tablets, containing 200 mg TPH, were formulated by wet granulation process. Different formulae F1, F2, F3 and F4 were prepared by film coating to percentage weight gain of 5%, 10%, 15%, and 20%, respectively. The in vitro release profiling test was done in variant pH media with certain order mimicking GIT media (pH 1.2, 6, 7.5 and 6.8). The in vivo performance of the optimum formula was compared with Avolen® SR, a marketed generic sustained release TPH tablets, in beagle dogs. The results clearly showed the criticality of film thickness in the performance of the coat and its function. F1 and F2 failed to protect TPH tablet in the acidic pH media, while both F3 and F7 showed lag time of release 4 and 5 hours, respectively. F4 exhibited only 52.9% cumulative drug release along the 9 hours dissolution period. The Cmax values were found to be 5.49 ± 0.46 and 5.12 ± 0.85 μg/ml for F3 and Avolen® SR, respectively, F3 showed higher mean plasma concentration than Avolen® SR from the period 1.5 till 5.5 hours post administration indicating high potential as chronotherapeutic treatment of nocturnal asthma.

Keywords


chronotherapy; nocturnal asthma; Eudragit S; Film coating; Beagle dogs

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References


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