The crystallization of poorly soluble drug molecules with an excipient into new solid phases called cocrystals has gained a considerable popularity in the pharmaceutical field. In this work, the cocrystal approach was explored for a very poorly water soluble antifungal active, itraconazole (ITR), which was, for the first time, successfully converted into this multicomponent solid using an aromatic coformer, terephthalic acid (TER). The new cocrystal was characterized in terms of its solid-state and structural properties, and a panel of pharmaceutical tests including wettability and dissolution were performed. Evidence of the cocrystal formation was obtained from liquid-assisted grinding, but not neat grinding. An efficient method of the ITR–TER cocrystal formation was ball milling. The stoichiometry of the ITR–TER phase was 2:1 and the structure was stabilized by H-bonds. When comparing ITR–TER with other cocrystals, the intrinsic dissolution rates and powder dissolution profiles correlated with the aqueous solubility of the coformers. The rank order of the dissolution rates of the active pharmaceutical ingredient (API) from the cocrystals was ITR–oxalic acid > ITR–succinic acid > ITR–TER. Additionally, the ITR–TER cocrystal was stable in aqueous conditions and did not transform to the parent drug. In summary, this work presents another cocrystal of ITR that might be of use in pharmaceutical formulations.

Background/Objectives: Omeprazole undergoes degradation in acidic conditions, which makes it unstable in low pHs found in the gastric environment. The vast majority of already marketed omeprazole formulations use enteric polymer coatings to protect the drug from exposure to acidic pH in the stomach, allowing for drug release in the small intestine where the pH is higher. This study aimed to explore the technical aspects of using stomach acid neutralizers as an alternative to polymeric coatings for omeprazole. Methods: After evaluating various neutralizers, magnesium oxide and sodium bicarbonate were chosen to be incorporated into capsules containing omeprazole, which then underwent in vitro dissolution testing to assess their ability to maintain optimal pH levels and ensure appropriate dissolution kinetics. Hygroscopicity and chemical stability of the selected formulation were tested to prove pharmaceutical quality of the product. An in vivo pharmacokinetic study was conducted to demonstrate the efficacy of the omeprazole–sodium bicarbonate formulation in providing faster absorption in humans. Results: Sodium bicarbonate was selected as the most suitable antacid for ensuring omeprazole stabilization. Its quantity was optimized to effectively neutralize stomach acid, facilitating the rapid release and absorption of omeprazole. In vitro studies demonstrated the ability of the formulation to neutralize gastric acid within five minutes. In vivo studies indicated that maximum concentrations of omeprazole were achieved within half an hour. The product met the requirements of pharmaceutical quality. Conclusions: An easily manufacturable, fast-absorbing oral formulation was developed as an alternative to enteric-coated omeprazole.

Ibuprofen, a common non-steroidal anti-inflammatory drug (NSAID), is widely used in over-the-counter (OTC) settings for pain and fever management, with a maximum daily dose of 1200 mg recommended for non-prescription use. The clinical efficacy of ibuprofen is influenced by formulation-specific differences in drug release profiles. This study systematically compared four ibuprofen formulations: immediate-release (IR) 400 mg tablets, IR 200 mg tablets, lysinate salt equivalent to 400 mg ibuprofen, and a novel bi-layer tablet integrating immediate- and sustained-release (IR/SR) components. Both, in vivo pharmacokinetic (PK) data and physiologically based PK modeling were employed to evaluate absorption kinetics, plasma concentration-time profiles, and therapeutic duration. Plasma concentration thresholds of 6.8 µg/mL and 10.1 µg/mL were used to assess onset and duration of action. The IR/SR 400 mg bi-layer tablet maintained plasma concentrations above these thresholds for eight hours, extending therapeutic coverage by 2-3.5 h compared to other IR formulations. Virtual PK simulations indicated that only IR 200 mg (six doses/day) and IR/SR 400 mg (three doses/day) regimens sustained therapeutic levels over 24 h without surpassing OTC limits. The reduced dosing frequency and prolonged efficacy of the IR/SR formulation support its suitability for providing continuous pain and fever relief.