Background/Objectives: The aim of this work was to prepare and characterize gastroretentive floating combination tablets (GRCTs) containing 500 mg of amoxicillin trihydrate (AMX) and 125 mg of levofloxacin (LVX) that provide sustained drug release and stability at gastric pH levels for the eradication of resistant Helicobacter pylori. Method: GRCTs were prepared with low-density excipients and hydrophilic swellable polymers, including hydroxypropyl methylcellulose (HPMC) of various viscosities, polyethylene oxide (PEO), and carboxymethylcellulose (CMC), by the direct compression method. The prepared GRCTs were investigated and optimized in terms of pH stability, tablet hardness, floating lag time and total floating time, drug release rate, gel strength. Results: AMX and LVX in GRCT were stable at the HP eradication target pH above 4.0. The effervescent GRCT composition (AMX/LVX/HPMC [4000 cP]/CMC/microcrystalline cellulose/citric acid/sodium bicarbonate/calcium silicate/silicon dioxide/magnesium stearate = 500/125/50/50/125/40/60/30/10/10, w/w) yielded acceptable hardness (>6 kp), reduced floating lag time (12 h), and sustained release rates of AMX and LVX (>90% until 12 h). This optimized GRCT had a gel strength of 107.33 ± 10.69 g and pH > 4.0, which maintained the tablets’ shape and AMX stability for 12 h. Conclusions: Collectively, the formulated effervescent GRCTs combining AMX and LVX represented a promising candidate dosage form for eradicating resistant H. pylori.

The objective of this work was to develop a supersaturated gel formulation (SGF) loaded with the maximum atorvastatin calcium trihydrate (ATR) dose. The maximum dose strength of ATR needs to be reduced through improving solubility and dissolution rate to mitigate side effects due to the necessity of taking high doses. ATR has highly pH-dependent solubility at 37 °C, leading to poor solubility (60%, w/w), and the combined use of TPGS and PEG 200 formed an organogel state and suppressed ATR precipitation, showing 15-fold higher dispersion solubility in buffer solution at pH 1.2 compared to the formulation with PEG 200 alone. The optimal SGF composition (ATR/PEG 200/TPGS = 10/60/30, w/w) exhibited an over 95% dissolution rate within 2 h at pH 1.2, compared to less than 50% for the original commercial product. In a transmission electron microscope analysis, the SGF suppressed ATR precipitation and revealed smaller precipitated particles (<300 nm) compared to the control samples. In the XRD analysis, the SGF was physically stable for 100 days at room temperature without the recrystallization of ATR. In conclusion, the SGF suggested in this work would be an alternative formulation for the treatment of dyslipidemia with enhanced solubility, dissolution, and physical stability.

This study aimed to develop a supersaturated liquid formulation (SSLF) to enhance the solubility and dissolution of pazopanib hydrochloride (PZH). SSLFs were prepared by a simple stirring method in a heated silicon oil bath (70 °C). PZH showed highly pH-dependent solubility (pH 1.2 > water >> pH 4.0 and pH 6.8) at 37 °C. The SSLF containing glycerol and polyvinylpyrrolidone K30 (PVP K30) increased PZH dispersion solubility (273.66 ± 48.91 μg/mL) at pH 6.8 by more than 50-fold compared with that of glycerol alone (<5 μg/mL), and the PZH precipitate particle size was considerably small (90%) and 6.8 (>55%) until 360 min, whereas PZH powder and PZH glycerol solution showed pH-dependent, low dissolution rates (<10%) under similar conditions. The supersaturation ratio of SSLF10 was very high at 29.88 and 18.36 at pH 6.8 and 4.0, respectively, indicating a stable PZH supersaturation solution. In the transmission electron microscopy analysis, PVP K30 and PG in SSLF10 synergistically suppressed PZH precipitation and recrystallization with small amorphous particles (<200 nm). Therefore, SSLF10 would be a promising formulation with enhanced solubility and dissolution rates regardless of medium pH.