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Novel drug-drug solid-forms of NSAIDs and PPIs: development, characterization and biological evaluation in vitro and in vivo

Grant number: 21/08289-6
Support type:Scholarships abroad - Research Internship - Post-doctor
Effective date (Start): December 01, 2021
Effective date (End): November 30, 2022
Field of knowledge:Health Sciences - Pharmacy - Pharmaceutical Technology
Principal researcher:Marlus Chorilli
Grantee:André Luiz Carneiro Soares do Nascimento
Supervisor abroad: Thomas Rades
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Research place: University of Copenhagen, Denmark  
Associated to the scholarship:18/23357-5 - Multidrug co-crystals of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) and Proton Pump Inhibitors (PPIs): development, characterization and biological evaluation in vitro and in vivo, BP.PD


Pharmaceutical cocrystals have been explored by many researchers as a strategy to optimize the physicochemical properties of solid-state drugs. Their improvements in solubility, bioavailability, and the reduced tendency for phase transformation occurrence, are factors that highlight the benefits of pharmaceutical co-crystals among other solid forms. Another approach that has been standing out is the transformation of a drug from the crystalline state to a high-energy amorphous form, which generally leads to an increase in solubility. The coamorphous solid is a single-phase system containing an active pharmaceutical ingredient (API) and other low molecular weight molecules that might be pharmacologically relevant APIs or excipients. These formulations also exhibit considerable advantages over neat crystalline or amorphous material, including improved physical stability, dissolution profiles, and potentially enhanced therapeutic efficacy. According to the Biopharmaceutical Classification System (BCS), non-steroidal anti-inflammatory drugs (NSAIDs) are class II drugs, which have low aqueous solubility, and therefore co-crystallization has the potential to optimize NSAID product properties. In therapy with non-selective NSAIDs, these drugs also inhibit normal processes of homeostasis and therefore cause a series of side effects, mainly gastrointestinal symptoms. Proton pump inhibitors (PPIs), such as omeprazole, act by reducing gastric acid production, inhibiting the H +/K + ATPase enzyme found in the parietal cells of the stomach, and have been the basis of therapy in several disorders related to the gastrointestinal tract. In addition, drug-drug solid-state combinations constitute a novel strategy that can overcome some problems associated with traditional fixed-dose mixing, its side effects, and pill burden, which may provide better pharmacological and pharmacotechnical performance and also result in potential advantages due to possible synergistic and/or additive effects. Therefore, this research aims to develop, characterize and evaluate biologically, using in vitro and in vivo assays, drug-drug solid forms of some non-selective NSAIDs derived from acetic acid (indomethacin, aceclofenac, and diclofenac) and PPIs. (AU)

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