Physics, chemistry, and Hirshfeld surface analyses of gamma-irradiated thalidomide to evaluate behavior under sterilization doses / 药物分析学报

Thalidomide was indicated as a sedative and antiemetic and prescribed for pregnant women. Its tragic teratogenic effects culminated in withdrawal from the market. Since the discovery of its anti-angiogenic and anti-inflammatory actions, thalidomide has been used in the treatment of leprosy and multiple myeloma, which justify studies of its stability. We investigated the effects of irradiation of thalidomide up to 100 kGy (fourfold the usual sterilizing dose for pharmaceutics). The β polymorph of thalidomide was obtained in an isothermal experiment at 270 °C. All samples underwent gamma irradiation for specific times. At different doses, decomposition of the pharmaceutical was not observed up to 100 kGy. The observed effect was angle turning between the phthalimide and glutarimide rings modulated by repulsion towards the carbonyl group, leading to a stable energetic configuration, as measured by the equilibrium in the torsion angle after irra-diation. The thalidomide molecule has a center of symmetry, so a full turn starting from 57.3° will lead to an identical molecule. Further irradiation will start the process again. Samples irradiated at 30 and 100 kGy have more compact unit cells and a lower volume, which leads to an increase in the intermolecular hydrogen interaction within the unit cel , resulting in higher thermal stability for polymorph α.

Physicochemical characterization, the Hirshfeld surface, and biological evaluation of two meloxicam compounding pharmacy samples / 药物分析学报

Meloxicam (MLX) is an anti-inflammatory drug susceptible to variations and crystalline transitions. In compounding pharmacies, the complete crystallographic evaluation of the raw material is not a routine procedure. We performed a complete crystallographic characterization of aleatory raw MLX samples from compounding pharmacies. X-ray diffraction indicated the presence of two crystalline forms in one sample. DSC experiments suggested that crystallization, or a crystal transition, occurred differently be-tween samples. The FTIR and 1H NMR spectra showed characteristic assignments. 13C solid-state NMR spectroscopy indicated the presence of more than one phase in a sample from pharmacy B. The Hirshfeld surface analysis, with electrostatic potential projection, allowed complete assignment of the UV spectra in ethanol solution. The polymorph I of meloxicam was more active than polymorph Ⅲ in an experi-mental model of acute inflammation in mice. Our results highlighted the need for complete crystal-lographic characterization and the separation of freely used raw materials in compounding pharmacies, as a routine procedure, to ensure the desired dose/effect.

Graphomya Robineau-Desvoidy from Costa Rica: descriptions and first records (Diptera, Muscidae) / Graphomya Robineau-Desvoidy da Costa Rica: descrições e primeiros registros (Diptera, Muscidae)

Graphomya Robineau-Desvoidy (Diptera, Muscidae) occurs in temperate and tropical regions of the world. It is known in the Neotropical Region from fifteen species. The genus is here recorded for the first time from Costa Rica, on the basis of three species: G. auriceps Malloch, 1934; G. mexicana Giglio-Tos, 1893 and G. tropicalis Malloch, 1934. A key for the recognition of these three species is given. G. auriceps is redescribed, including the morphology of male and female terminalia and the male of G. tropicalis is described for the first time. For G. mexicana, a well-known species in the literature, only a brief diagnosis and the material examined are listed.

Graphomya Robineau-Desvoidy (Diptera, Muscidae) ocorre em regiões temperadas e tropicais do mundo. É conhecido na Região Neotropical por quinze espécies. O gênero é aqui registrado, pela primeira vez, para a Costa Rica, através da presença de três espécies: G. auriceps Malloch, 1934; G. mexicana Giglio-Tos, 1893 e G. tropicalis Malloch, 1934. É fornecida uma chave para a segregação destas três espécies. G. auriceps é redescrita, incluindo a morfologia da terminália do macho e da fêmea e o macho de G. tropicalis é descrito pela primeira vez. Para G. mexicana, uma espécie bem conhecida na literatura, uma breve diagnose e a lista do material examinado são listados.

Substituição de milho por sorgo baixo tanino em dietas para suínos: digestibilidade e metabolismo / Replacement of corn by low tannin sorghum in pig diets: digestibility and metabolism

Um experimento foi realizado para avaliar os efeitos digestivos e metabólicos da substituição de milho por sorgo em dietas para suínos. Foram utilizados 12 suínos machos castrados, meio-irmãos paternos, com peso vivo médio inicial de 40,8kg, mantidos em gaiolas metabólicas. O delineamento experimental foi inteiramente casualizado com três tratamentos (T1 = dieta controle; T2 = substituição de 50 por cento do milho por sorgo e T3 = substituição de 100 por cento) e quatro repetições. As digestibilidades da proteína e da energia brutas foram 5 e 4 por cento superiores (P<0,05), respectivamente, nos suínos alimentados com a dieta que tinha 50 por cento de substituição, comparadas àquela com substituição total do milho por sorgo. A substituição total do milho por sorgo reduziu (P<0,05) as digestibilidades, em relação à dieta-controle, em 3 por cento para MS, 8 por cento para PB e 5 por cento para EB. O N fecal foi 25 por cento maior (P<0,05), o N absorvido 10 por cento menor (P<0,05) e a excreção fecal de energia 15 por cento maior (P<0,05) para a dieta com substituição total, em relação à dieta-controle. A excreção fecal de N e energia e a absorção de N são influenciadas negativamente pela substituição total de milho por sorgo nas dietas. A substituição em até 50 por cento do milho por sorgo em dietas para suínos não influi na digestibilidade das dietas e no metabolismo dos animais.

An experiment was carried out to evaluate metabolic and digestive effects replacement of corn by sorghum in pig diets. Twelve half brothers barrows weighing 40.8kg and housed in metabolic cages in a completely randomized design with three treatments (T1 = control diet; T2 = replacement of 50 percent corn by sorghum and T3 = replacement of 100 percent) with four replicates. Crude protein and gross energy the digestibilities were 5 percent and 4 percent higher (P<0.05), respectively, for pigs fed 50 percent of corn replacement diet, in comparison with the diet where corn was totally replaced by sorghum. Total replacement of corn by sorghum diets decreased (P<0.05) the digestibilities, in comparison to control diet, in 3 percent for DM, 8 percent for CP and 5 percent for GE. Fecal N was 25 percent higher (P<0.05), absorbed N was 10 percent lower (P<0.05), and the fecal excretion energy was 15 percent higher (P<0.05) for total substitution diet in comparison to control diet. Fecal excretion and absorption of nitrogen are negatively influenced by total replacement of corn by sorghum in the diets. Replacements of up to 50 percent of corn by sorghum in pig diets do not affect the digestibility diet and metabolism of animals.

A new Notoschoenomyza Malloch and a key to the species (Diptera, Muscidae, Coenosiinae)

Nova espécie de Notoschoenomyza Malloch, N. diminuta sp. nov. do Chile, é descrita, as terminálias de macho e fêmea são ilustradas e uma chave para identificação de todas as espécies de Notoschoenomyza é apresentada.