<p>Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers</p>

Abstract

Purpose Bupropion is an antidepressant drug that facilitates weight loss. It is a highly water-soluble drug that needs multiple dosing, so it is considered a potential candidate for oral controlled-release dosage form. The aim of this research was to formulate and evaluate satiety-inducing swellable floating bupropion tablets by direct compression targeting depression associated with eating disorders. Various combinations of natural and semi-synthetic hydrogels were selected to achieve maximum swelling and remaining buoyant in the stomach. This synergistically enhances weight loss by increasing satiety. Methods An I-optimal mixture design was conducted to establish the optimal quantitative composition of tablets. Friability, floating lag time, swelling index after 4 and 8 hours, along with the percent of bupropion released at 1 and 8 hours were selected as dependent variables. The optimized formulation was characterized by physicochemical properties, thermal stability, and chemical interaction. In vivo radiographic evaluation of gastric residence besides, the oral bioavailability relative to marketed Wellbutrin ® sustained-release tablets were investigated using human volunteers. Results The optimized formulation (73.3 mg xanthan, 120 mg glucomannan, 8.4 mg tamarind kernel powder, 78.3 mg HPMC K15M) was achieved with the overall desirability equals 0.782. In vivo radiographic study showed that formulation was retained for >8 hours in the stomach. Compared with the marketed BUP tablets, the C max was almost the same with a significant increase (p =0.004) for T max . Conclusion Using combinations of these hydrogels would be promising gastroretentive delivery systems in the control of bupropion rate release with enhanced floating and swelling features.

Preparation of solid dispersion systems for enhanced dissolution of poorly water soluble diacerein: In-vitro evaluation, optimization and physiologically based pharmacokinetic modeling

“…High R 2 values, displayed in Table 5 , as well as good agreement between the adjusted R 2 and the predicted R 2 show that data were best fitted to the chosen models. In addition, high adequacy of the chosen models was confirmed by adequate precision values > 4 [ 57 ].…”

Binge Eating Disorders; Updated and Emerging Approaches

“…Multiple studies revealed that bupropion able to improve hyperphagic depressed individuals and overweight or obese patients with depression [51][52][53][54][55]. The efficacy of bupropion and sertraline in the treatment of BED and comorbid depression was comparably evaluated in a 24-week retrospective cohort study [56].…”

Relevancy of Nizatidine’s Release from Floating Tablets with Viscosity of Various Cellulose Ethers

“…The dissolution study of floating tablets was conducted using a 6 vessel USP type II dissolution apparatus containing 900 mL of freshly prepared 0.1N HCl maintained at pH 1.2 [20,21]. The bath temperature was set at 37 ± 0.5 • C. One tablet in each vessel was placed and the apparatus was started with a paddle speed of 50 rpm.…”