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OBJECTIVES: This study aimed to evaluate the effects of prucalopride, a prokinetic agent that acts as a potent serotonin agonist of 5-HT4 receptors, on gastric emptying and small bowel transit and assess its impact on the absorption of metronidazole. METHODS: Six healthy volunteers, three men and three women, aged between 20 and 27 years, with a body weight ranging from 50 to 80 kg, were enrolled in this study. The pharmacokinetics and gastrointestinal transit parameters were evaluated simultaneously through pharmacomagnetography assessment, combining alternating current biosusceptometry and blood analysis. KEY FINDINGS: The results showed that prucalopride enhances gastric emptying and small bowel transit when administered orally and significantly impacts the rate of metronidazole absorption, leading to enhanced bioavailability and rapid therapeutic response. CONCLUSION: Pharmacomagnetography assessment allows simultaneous tracking of transit by images and is a valuable method for analysing drug absorption using multiple instruments.
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Vaciamiento Gástrico , Metronidazol , Masculino , Humanos , Femenino , Adulto Joven , Adulto , Metronidazol/farmacología , Tránsito GastrointestinalRESUMEN
BACKGROUND: Platelet-rich plasma (PRP) has been used to favor anterior cruciate ligament (ACL) healing after reconstruction surgeries. However, clinical data are still inconclusive and subjective about PRP. Thus, we propose a quantitative method to demonstrate that PRP produced morphological structure changes. METHODS: Thirty-four patients undergoing ACL reconstruction surgery were evaluated and divided into control group (sixteen patients) without PRP application and experiment group (eighteen patients) with intraoperative application of PRP. Magnetic resonance imaging (MRI) scans were performed 3 months after surgery. We used Matlab® and machine learning (ML) in Orange Canvas® to texture analysis (TA) features extraction. Experienced radiologists delimited the regions of interest (RoIs) in the T2-weighted images. Sixty-two texture parameters were extracted, including gray-level co-occurrence matrix and gray level run length. We used the algorithms logistic regression (LR), naive Bayes (NB), and stochastic gradient descent (SGD). RESULTS: The accuracy of the classification with NB, LR, and SGD was 83.3%, 75%, 75%, respectively. For the area under the curve, NB, LR, and SGD presented values of 91.7%, 94.4%, 75%, respectively. In clinical evaluations, the groups show similar responses in terms of improvement in pain and increase in the IKDC index (International Knee Documentation Committee) and Lysholm score indices differing only in the assessment of flexion, which presents a significant difference for the group treated with PRP. CONCLUSIONS: Here, we demonstrated quantitatively that patients who received PRP presented texture changes when compared to the control group. Thus, our findings suggest that PRP interferes with morphological parameters of the ACL. TRIAL REGISTRATION: Protocol no. CAAE 56164316.6.0000.5411.
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Ligamento Cruzado Anterior/patología , Ligamento Cruzado Anterior/cirugía , Procedimientos Ortopédicos/métodos , Procedimientos de Cirugía Plástica/métodos , Plasma Rico en Plaquetas , Adulto , Ligamento Cruzado Anterior/diagnóstico por imagen , Ligamento Cruzado Anterior/fisiopatología , Femenino , Humanos , Cuidados Intraoperatorios , Modelos Logísticos , Aprendizaje Automático , Imagen por Resonancia Magnética , Masculino , Cicatrización de HeridasRESUMEN
A magnetic enteric-coated tablet containing diclofenac sodium was produced, and its performance under physiological and disturbed gastrointestinal motility was assessed through pharmacomagnetography analysis. In vitro studies were performed using conventional methods and in vivo studies were conducted on healthy volunteers before (control) and after domperidone administration. The magnetic tablet's gastrointestinal (GI) transit and disintegration process were monitored using the Alternating Current Biosusceptometry sensors combined with drug plasmatic concentration. The Gastric Residence Time, Colon Arrival Time, Small Bowel Transit Time, Disintegration Time and the pharmacokinetics parameters were calculated. The pH-dependent polymers used to coat the magnetic tablets were able to avoid the premature drug release on gastric or small intestine simulated medium. Gastric Residence Time was accelerated compared with the control group (p < 0.01). No significant differences were found regarding small bowel transit, colon arrival, disintegration process, or pharmacokinetics parameters. A strong correlation between magnetic monitoring and pharmacokinetics parameters analysis was determinant to evaluate the efficiency in the drug delivery at a specific site in the human gastrointestinal tract. In addition, a tablet with a damaged coating was used as a proof of concept to show the suitability of our methodology to evaluate the tablet. Our study showed that pharmacomagnetography is a multi-instrumental approach towards assessing drug delivery and bioavailability.
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Domperidona/administración & dosificación , Sistemas de Liberación de Medicamentos , Fenómenos Magnéticos , Polímeros/química , Adulto , Disponibilidad Biológica , Química Farmacéutica , Domperidona/farmacocinética , Método Doble Ciego , Liberación de Fármacos , Femenino , Motilidad Gastrointestinal , Tracto Gastrointestinal/metabolismo , Tránsito Gastrointestinal , Humanos , Concentración de Iones de Hidrógeno , Masculino , Comprimidos Recubiertos , Distribución Tisular , Adulto JovenRESUMEN
Cerebral blood flow (CBF) assessment is mainly performed by scintigraphy, computed tomography (CT) and magnetic resonance imaging (MRI). New approaches to assess the CBF through the passage of magnetic nanoparticles (MNPs) to blood-brain barrier (BBB) are convenient to help decrease the use of ionizing radiation and unleash the required MRI schedule in clinics. The development of nanomedicine and new biomedical devices, such as the magnetic particle imaging (MPI), enabled new approaches to study dynamic brain blood flow. In this paper, we employed MNPs and the alternating current biosusceptometry (ACB) to study the brain perfusion. We utilized the mannitol, before the MNPs, injection to modulate the BBB permeability and study its effects on the circulation time of the MNPs in the brain of rats. Also, we characterized a new ACB sensor to increase the systems' applicability to study the MNPs' accumulation, especially in the animals' brain. Our data showed that the injection of mannitol increased the circulation time of MNPs in the brain. Also, the mannitol increased the accumulation of MNPs in the brain. This paper suggests the use of the ACB as a tool to study brain perfusion and accumulation of MNPs in studies of new nano agents focused on the brain diagnostics and treatment.
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Encéfalo/fisiopatología , Circulación Cerebrovascular/fisiología , Imagen por Resonancia Magnética/métodos , Animales , Nanopartículas de Magnetita , Masculino , Perfusión/métodos , RatasRESUMEN
OBJECTIVE: The objective of this study was to develop and validate a computational tool to assist radiological decisions on necrotizing enterocolitis. METHODOLOGY: Patients that exhibited clinical signs and radiographic evidence of Bell's stage 2 or higher were included in the study, resulting in 64 exams. The tool was used to classify localized bowel wall thickening and intestinal pneumatosis using full-width at half-maximum measurements and texture analyses based on wavelet energy decomposition. Radiological findings of suspicious bowel wall thickening and intestinal pneumatosis loops were confirmed by both patient surgery and histopathological analysis. Two experienced radiologists selected an involved bowel and a normal bowel in the same radiography. The full-width at half-maximum and wavelet-based texture feature were then calculated and compared using the Mann-Whitney U test. Specificity, sensibility, positive and negative predictive values were calculated. RESULTS: The full-width at half-maximum results were significantly different between normal and distended loops (median of 10.30 and 15.13, respectively). Horizontal, vertical, and diagonal wavelet energy measurements were evaluated at eight levels of decomposition. Levels 7 and 8 in the horizontal direction presented significant differences. For level 7, median was 0.034 and 0.088 for normal and intestinal pneumatosis groups, respectively, and for level 8 median was 0.19 and 0.34, respectively. CONCLUSIONS: The developed tool could detect differences in radiographic findings of bowel wall thickening and IP that are difficult to diagnose, demonstrating the its potential in clinical routine. The tool that was developed in the present study may help physicians to investigate suspicious bowel loops, thereby considerably improving diagnosis and clinical decisions.
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Enterocolitis Necrotizante/diagnóstico por imagen , Enfermedades del Recién Nacido/diagnóstico por imagen , Humanos , Procesamiento de Imagen Asistido por Computador , Recién Nacido , Intestinos/fisiopatología , Radiografía Abdominal , Estudios Retrospectivos , Sensibilidad y Especificidad , Índice de Severidad de la Enfermedad , Validación de Programas de Computación , Estadísticas no Paramétricas , Análisis de OndículasRESUMEN
CONTEXT: Alternating Current Biosusceptometry is a magnetically method used to characterize drug delivery systems. This work presents a system composed by an automated ACB sensor to acquire magnetic images of floating tablets. OBJECTIVE: The purpose of this study was to use an automated Alternating Current Biosusceptometry (ACB) to characterize magnetic floating tablets for controlled drug delivery. MATERIALS AND METHODS: Floating tablets were prepared with hydroxypropyl methylcellulose (HPMC) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and ferrite as magnetic marker. ACB was used to characterize the floating lag time and the tablet hydration rate, by quantification of the magnetic images to magnetic area. Besides the buoyancy, the floating tablets were evaluated for weight uniformity, hardness, swelling and in vitro drug release. RESULTS: The optimized tablets were prepared with equal amounts of HPMC and ferrite, and began to float within 4 min, maintaining the flotation during more than 24 h. The data of all physical parameters lied within the pharmacopeial limits. Drug release at 24 h was about 40%. CONCLUSIONS: The ACB results showed that this study provided a new approach for in vitro investigation of controlled-release dosage forms. Moreover, using automated ACB will also be possible to test these parameters in humans allowing to establish an in vitro.in vivo correlation (IVIVC).