The systems which combine the advantages of gastroretentive and pulsatile approaches are urgently needed to enhance drug absorption and allow its delivery at the time necessary to alleviate chronopathological complications. The current work aimed to explore the pharmacokinetics of theophylline anhydrous (THE) following oral administration of THE-loaded core-in-cup tablets and Quibron®-T tablets in six healthy, non-smoking, male volunteers at 100 mg doses. The pharmacokinetic parameters for the two treatments were determined from the plasma concentration time data adopting the non-compartmental module. The maximum drug concentration (Cmax), the time to reach Cmax (Tmax), the mean residence time from zero to infinity (MRT(0– ∞), h), the area under the plasma concentration–time curve up to the last measured sampling time at 24 hour (AUC0–24) and up to infinity (AUC0–∞) were estimated. The results proved that Quibron®-T tablets showed a mean Cmax of 6.55 ng/ml at a median Tmax of 3 h. Statistically significant (P < 0.05) and higher mean Cmax value (9.61 µg/ml) was estimated at a median Tmax of 7 h for THE-loaded core-in-cup tablets. The rapid release of the drug following a TL of 5 hours could prove the pulsatile delivery of THE in human volunteers. This study paves the way for the pulsatile delivery of other sparingly-soluble drugs.
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