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The active pharmaceutical ingredient (API) is a drug product's biologically active chemical substance that produces the desired therapeutic effects. Most APIs are small organic molecules commercially available as a crystalline solid phase. Crystalline drugs are preferred in oral dosage formulations for their high purity and stability. However, some commercial drugs have low aqueous solubility, reducing their bioavailability and requiring high doses of API. Thus, discovering/investigating solid crystalline forms or controlling/designing more soluble forms with optimized pharmaceutical properties can be challenging or suitable for the pharmaceutical industry and academia. In this sense, the present work proposes a new physicochemical approach consisting of the average framework energy (Eframework) which is the average intermolecular interaction in crystalline solids to predict the modification of API solubility in new solid forms. This way, it was possible to correlate the intermolecular interactions of a given crystalline solid-state with its respective aqueous solubility. Overall, 60 crystalline forms are involved in this investigation derived from 25 distinct APIs. The results indicate that the average energy framework calculated and the aqueous solubility display a linear upward trend in the distribution of points, meaning that the greater the solubility, the lower the interaction energy. Such an approach is more evident in box plot-based drugs grouped by solubility range indicating a handy predictive model for drug solubility estimation based exclusively on energy framework features. [ABSTRACT FROM AUTHOR]

Objectives: Review of the available data on the currently available single-tablet regimens (STRs), from the analysis of efficacy and safety to the key points of value in terms of adherence, quality of life and pharmacoeconomic evaluation. Methods: For this narrative review, literature searches have been performed in PubMed, IndexRevMed and Cochrane, using the search terms HIV, single-tablet, one-pill, single dose, fixed-dose, and STR. These have been reviewed and complemented with the most recent publications of interest. Results: Fixed-dose combinations are a significant advance in antiretroviral treatment simplification, contributing to an increase in compliance with complex chronic therapies, thus improving patients' quality of life. Reducing the number of pills and daily doses is associated with higher adherence and better quality of life. As a fixeddose combination tablet given once daily, EFV/FTC/TDF was the first available STR combining efficacy, tolerability and convenience, with the simplest dosing schedule and smallest numbers of pills of any ART combination therapy. The RPV/FTC/TDF is a next-generation NNRTI-based STR, a once daily complete ART regimen for the treatment of HIV-1 infection. Recently the combination of EVG/COBI/FTC/TDF was also approved by the European Commission, and is the first integrase inhibitor-based STR. Receiving antiretroviral therapy as once daily STR is associated with both clinical and economic benefits, which confirms previous research. Conclusions: The associated benefits of STRs provide a valid strategy for the treatment of HIV-infected patients. [ABSTRACT FROM AUTHOR]