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.

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This study aimed to formulate and evaluate a floating raft system for the co-delivery of etoricoxib (ETO) and famotidine (FAM) using a combination of glucomannan with natural/semi-synthetic polysaccharides. Formulation variables affect gelation lag time (GLT), floating lag time (FLT), and release percentage of drugs after 1–8 h, Stability, and viscosity parameters were evaluated. In vivo X-ray studies, followed by the pharmacokinetic study, were performed on human volunteers. Formulations exhibited pseudoplastic behavior for ease of swallowing. The optimum raft system (ORS) comprised 1% Na alginate, 0.1% Low Methoxyl (LM) pectin, 0.8% Konjac glucomannan (KGL), 1% Precirol, and 1% CaCO 3 . ORS exhibited rapid GLT and FLT (around 42 and 8 sec respectively) in 0.1 N HCl as well as controlled release of ETO (15% in 1 h and 82% in 8 h) and FAM (29% in 1 h and 85% in 8 h). Formulation stability with the absence of any drug-excipient interactions was observed. The X-ray imaging showed a promising buoyancy ability for approximately 8 h. Compared with marketed products, ORS showed superior relative bioavailability for both drugs. These findings revealed the successful preparation of a promising raft system with improved dual drug delivery.

A Raft-forming system is an auspicious approach for systematic drug delivery with steady plasma profiles and drug sustained release manner. It has advantages like enhanced bioavailability, better floating capabilities than other floating systems, more patient compliance, and promoting drug efficacy. Although, it has some problems as it can’t be used for drugs that possess low acid solubility, drugs that are unstable in gastric media, and drugs used for selective release in the colon along with stability difficulties. This system can be successfully prepared by three methods: the physical approach, chemical approach, and physiologically-stimuli approach. The comparative studies showed that the raft-forming system has more advantage over the other comparatives in the antacid potency and in vitro gastric residence time, allowing an intact prolonged delivery of the antacid drug. All the listed applications of the raft system were, fortunately, possessing promising drug delivery with a well-designed drug delivery system. There was a good variety in the active ingredients formulated in a raft, starting from some anti-coughs, anti-spasmodic, anti-inflammatories, and antacids to drugs treating osteoporosis and finally anti-depressants and anti-epileptic drugs. This diversity along with simple in vitro and in vivo evaluations, gives the potentiality to raft for leading the other gastro retentive drug delivery systems for decades.