Alendronic acid is one of the most effective diphosphonate compounds used for clinical treatment of bone disorders. It is administered orally as its monosodium salt, for which hydrate and anhydrous crystal forms are known. The monosodium alendronate trihydrate form (NaH 4 A•3H 2 O) is incorporated into medicines as the Active Pharmaceutical Ingredient (API). The NaH 4 A•3H 2 O form can be dehydrated at temperatures above 115 °C, resulting in the anhydrous form (NaH 4 A). Although the crystal structures of both forms have already been reported, an investigation of the reversible dehydration/hydration solid-phase transition is presented here for the first time. A solid-state mechanism for the phase transition, which involves the reversible dehydration−hydration of the NaH 4 A•3H 2 O and NaH 4 A forms, is also proposed. A systematic study comparing the equilibrium solubility and discriminatory intrinsic dissolution of the NaH 4 A•3H 2 O and NaH 4 A forms is included. To achieve this goal, an alternative method of quantifying alendronate anions released from the crystal forms into solution, flame photometry, is proposed and validated. The stability and interconversion of the NaH 4 A•3H 2 O and NaH 4 A forms are probed by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy−attenuated total reflectance (FTIR-ATR), and powder X-ray diffraction (PXRD).
The oil obtained from baru (Dipteryx alata Vog.) almonds exhibits high energy value and is reported in popular medicine for the treatment of rheumatic diseases and reproductive disturbances. Although baru oil is used in domestic cuisine, the chemical characterization of this oil and its effects on lipid metabolism are still poorly understood. Therefore, this study evaluated the fatty acid (FA) profile and the effects of baru oil on liver and aorta in a murine model of dyslipidemia. The chromatographic profile of baru oil showed high levels of unsaturated FAs, especially oleic acid. Saturated FAs, such as palmitic and lignoceric acids, were found in lower amounts. Hypercholesterolemia was induced in male Wistar rats by daily administration of a lipid emulsion by gavage for 15 weeks. Biochemical and histopathological analysis were performed on serum, aorta, and liver. The results demonstrated that animals developed marked hypercholesterolemia, liver steatosis, and increased lipid peroxidation in the aorta. Treatment with baru oil attenuated lipid peroxidation and drastically reduced liver damage, especially ballooning degeneration and steatosis. By restricting vascular and hepatic injury, this oil showed potential applicability as a functional food, reinforcing its use in popular medicine and domestic cuisine.
Many authors attribute the antioxidant activity of brewed coffee to its caffeine content. In addition, caffeine intake has been associated with increased performance during physical exercise. This study analyzed the in vivo effects of drinking caffeinated and decaffeinated instant coffee (8%, w/v) on oxidative stress and antioxidant enzyme activity in the anterior tibialis muscles of rats subjected to intense exercise. It was observed that exercise induced lipid peroxidation (estimated using malondialdehyde) and protein oxidation (evaluated by determining the formation of carbonyl groups) in the muscle (P < 0.05). Decaffeinated instant coffee and caffeine solution did not exhibit antioxidant activity in vivo. Caffeinated instant coffee beverage intake did not induce changes in superoxide dismutase and glutathione peroxidase activities but was able to diminish lipid and protein oxidation in the anterior tibialis muscles of rats after exercise (P < 0.05), contributing to a reduction in the oxidative stress triggered by exercise.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.