Intensification Effect of a Multi-Jet Structure on a Multiphase Flow and Desulfurization Process in a Fluidized Bed.

The introduction of a multi-jet structure at the bottom and middle of a fluidized bed can intensify the interphase mixing and improve desulfurization efficiency. The computational fluid dynamics were used to study the gas-liquid-solid flow in a bottom multi-jet fluidized bed and middle multi-jet fluidized bed (BMJFB and MMJFB). It was found that for the gas-liquid-solid interphase mixing, the intensification effect of introducing the multi-jet structure in the middle of the bed is more obvious than that in the bottom.

First-in-human study of deucravacitinib: A selective, potent, allosteric small-molecule inhibitor of tyrosine kinase 2.

This randomized, double-blind, single- and multiple-ascending dose study assessed the pharmacokinetics (PKs), pharmacodynamics, and safety of deucravacitinib (Sotyktu™), a selective and potent small-molecule inhibitor of tyrosine kinase 2, in 100 (75 active, 25 placebo) healthy volunteers (NCT02534636). Deucravacitinib was rapidly absorbed, with a half-life of 8-15 h, and 1.4-1.

Benefit-risk assessment of nivolumab 240 mg flat dose relative to 3 mg/kg Q2W regimen in Japanese patients with advanced cancers.

Nivolumab 3 mg/kg every 2 weeks (Q2W) has been approved in Japan for various cancers; however, use of a flat dose is expected to simplify dosing and administration. A quantitative clinical pharmacology approach was used to assess the benefit-risk profile of nivolumab 240 mg Q2W relative to the approved dose of nivolumab 3 mg/kg Q2W in Japanese patients. Three exposure-response safety analyses were performed for adverse events that led to discontinuation/death, were grade 3 or higher, and were immune-mediated and grade 2 or higher for Japanese patients diagnosed with one of multiple tumor types.

Efficacy of Tea Tree Oil in the Treatment of Equine Streptothricosis.

Streptothricosis is a dermatitis characterized by matted tufts of hair and coalescing, pustular crusts that affects many livestock species, including horses. It results from cutaneous infection by the actinobacterium Dermatophilus congolensis. For economic reasons, the ailment is often treated with commercially available over-the-counter (OTC) products or home remedies rather than prescribed medications.

Pharmacokinetics and tissue distribution of 5,7-dimethoxyflavone in mice following single dose oral administration.

5,7-Dimethoxyflavone (5,7-DMF) is a major active constituent of many herbal plants, such as Kaempferia paviflora, Piper caninum, and Leptospermum scoparium. 5,7-DMF has demonstrated many beneficial pharmacological effects in vitro, including anti-infammatory, anti-oxidant, cardioprotection effects, as well as chemopreventive and chemosensitizing properties. In contrast to the extensive in vitro investigations, the information of the pharmacokinetic (PK) profile of 5,7-DMF in vivo is very limited.

Quantification of 5,7-dimethoxyflavone in mouse plasma using liquid chromatography-tandem mass spectrometry (LC-MS/MS) and its application to a pharmacokinetic study.

5,7-Dimethoxyflavone (5,7-DMF), a natural flavonoid abundant in many plants, has been reported to have many beneficial pharmacological effects, including strong chemopreventive and chemosensitizing properties, anti-oxidant, cardiovascular protectant, and anti-inflammatory activities. However, to date 5,7-DMF was evaluated mainly in vitro and its pharmacokinetics (PK) in vivo remains largely unknown. In addition, current available quantification methods of 5,7-DMF all lack sufficient sensitivity (lower limit of quantification >800 ng/mL).

Enzyme- and transporter-mediated drug interactions with small molecule tyrosine kinase inhibitors.

Among the novel and target-specific classes of anticancer drugs, small molecule tyrosine kinase inhibitors (TKIs) represent an extremely promising and rapidly expanding group. TKIs attack cancer-specific targets and therefore have a favorable safety profile. However, as TKIs are taken orally along with other medications on a daily basis, there is an elevated risk of potentially significant drug-drug interactions.

Pharmacokinetics and pharmacodynamics of midazolam after intravenous and intramuscular administration in alpacas.

Objective: To determine pharmacokinetic and pharmacodynamic properties of midazolam after IV and IM administration in alpacas.

Animals: 6 healthy alpacas.

Procedures: Midazolam (0.

Pharmacokinetics of protocatechuic acid in mouse and its quantification in human plasma using LC-tandem mass spectrometry.

Protocatechuic acid (PCA), a major microbial-mediated metabolite of anthocyanins, has significant anti-oxidative and anti-carcinogenic activities in vitro and in vivo; however, its pharmacokinetics remains largely unknown. In this report, a sensitive and rapid LC-MS/MS method was developed and validated for the measurement of PCA concentrations in both mouse and human plasma. This method showed a linearity of 1-1000ng/mL in both mouse and human plasma with a lower limit of quantification of 1ng/mL.

Engineering nanomedicines for improved melanoma therapy: progress and promises.

Once metastatic, melanoma remains one of the most aggressive and morbid malignancies. Moreover, in past decades, the overall survival for advanced unresectable melanoma exhibited a constancy of poor prognosis. Low response rates and serious adverse effects have been characteristic of standard therapy based on a combination of chemotherapeutic agents or immunotherapy with IL-2.

Formulation of dacarbazine-loaded cubosomes. Part III. Physicochemical characterization.

The purpose of this study was to investigate the physicochemical properties of dacarbazine-loaded cubosomes. The drug-loaded cubosome nanocarriers were prepared by a fragmentation method and then freeze dried. They were then characterized for size, morphology, thermal behavior, and crystallography using dynamic light scattering, transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD), respectively.

Formulation of dacarbazine-loaded Cubosomes--part II: influence of process parameters.

The purpose of this study is to investigate the combined influence of process parameters (independent variables) such as homogenization speed (X(1)), duration (X(2)), and temperature (X(3)) during the preparation of dacarbazine-loaded cubosomes. Box-Behnken design was used to rationalize the influence of these three factors on two responses, namely particle size (Y(1)) and encapsulation efficiency (Y(2)). Independent and dependent variables were analyzed with multiple regressions to establish a full-model second-order polynomial equation.

Formulation of dacarbazine-loaded cubosomes-part I: influence of formulation variables.

The purpose of this study was to investigate the combined influence of three-level, three-factor variables on the formulation of dacarbazine (a water-soluble drug) loaded cubosomes. Box-Behnken design was used to obtain a second-order polynomial equation with interaction terms to predict response values. In this study, the selected and coded variables X(1), X(2), and X(3) representing the amount of monoolein, polymer, and drug as the independent variables, respectively.

Progressive photoreceptor degeneration, outer segment dysplasia, and rhodopsin mislocalization in mice with targeted disruption of the retinitis pigmentosa-1 (Rp1) gene.

Retinitis pigmentosa (RP), a common group of human retinopathic diseases, is characterized by late-onset night blindness, loss of peripheral vision, and diminished or absent electroretinogram (ERG) responses. Mutations in the photoreceptor-specific gene RP1 account for 5-10% of cases of autosomal dominant RP. We generated a mouse model of the RP1 form of RP by targeted disruption of the mouse ortholog (Rp1) of human RP1.