Fosfatriclaben, a prodrug of triclabendazole: Preparation, stability, and fasciolicidal activity of three new intramuscular formulations.

In this study, we present the preparation, stability, and in vivo fasciolicidal activity of three new intramuscular formulations in sheep of a prodrug based on triclabendazole, named fosfatriclaben. The new formulations were ready-to-use aqueous solutions with volumes recommended for intramuscular administration in sheep. The use of poloxamers (P-407 and P-188) and polysorbates (PS-20 and PS-80) in the new formulations improved the aqueous solubility of fosfatriclaben by 8-fold at pH 7.4. High-performance liquid chromatography with UV detection was used to evaluate the stability of fosfatriclaben in the three formulations. High recovery (> 90%) of fosfatriclaben was found for all formulations after exposure at 57 ± 2 °C for 50 h. The three intramuscular formulations showed high fasciolicidal activity at a dose of 6 mg/kg, which was equivalent to the triclabendazole content. The fasciolicidal activity of fosfatriclaben was similar to commercial oral (Fasimec®) and intramuscular (Endovet®) triclabendazole formulations at a dose of 12 mg/kg. In the in vivo experiments, all formulations administered intramuscularly reduced egg excretion by 100%, and formulations F1, F2, and F3 presented fasciolicidal activities of 100%, 100%, and 99.6%, respectively.

Efficiency comparison of experimental fosfatriclaben with three commercial fasciolicides in experimentally infected sheep.

In this work, we compare and evaluate the efficiency of fosfatriclaben with three commercial fasciolicides in experimentally infected sheep. Fosfatriclaben is a novel prodrug derived from triclabendazole; it is highly water-soluble with excellent aqueous stability at pH 7, properties that make it ideal for developing intramuscular pharmaceutical compositions in the form of solutions. In order to compare, 30 mixed breed sheep, previously diagnosed negative to fluke eggs, were infected with 200 metacercariae of Fasciola hepatica, twice. Five groups of six animals/each were formed for treatments. Group 1 (G1) was treated with closantel 5% injectable at 5 mg/kg subcutaneously, G2 with clorsulon at 2 mg/kg subcutaneously, G3 with triclabendazole at 12 mg/kg per os, G4 with fosfatriclaben at 6 mg/kg intramuscularly (dose equivalent to triclabendazole content), and G5 remained as the non-treated control. On day 110, fecal samples were examined to determine the percentage of egg reduction after treatment, and sheep were humanely euthanized. The livers were collected, the flukes were extracted, measured, and counted. Efficiency in egg reduction was of 86.8, 90.5, 98.4, and 97.3% for closantel, clorsulon, triclabendazole, and fosfatriclaben, respectively, and efficiency against flukes was of 96.2, 91.9, 99.4, and 95.7%, respectively. No statistical differences were found between treatments. It is concluded that fosfatriclaben at 6 mg/kg intramuscularly presented a high fasciolicide efficiency, similar to the best commercial fasciolicides, having advantage over its predecessor since it uses half of the dose required by triclabendazole to remove flukes in sheep under study.

A short nutritional intervention in a cohort of hematological inpatients improves energy and protein intake and stabilizes nutritional status.

INTRODUCTION: Oncohematological diseases are associated with an important prevalence of malnutrition. AIM: Our aim is to determine if early recognition and treatment of malnourished hematological inpatients can improve their oral intake, nutritional status and reduce the length of hospital stay. METHODS: Prospective 2-year study conducted in a cohort of hematology inpatients. Malnutrition Screening Tool (MST) was carried out on the first day of admission. Patients with a positive screening were recruited to have a complete nutritional evaluation and intervention, following usual clinical practice. Nutritional evaluation was repeated after one week. RESULTS: Six hundred and seventeen hematological patients were screened (37.8% with positive screening). After one week, median diet intake increased from 80% to 90% (p < 0.001), and an increase of 407.36 Kcal (SD 679.37) and 17.58 g of protein (SD 31.97) was also achieved. More patients reached their energy and protein requirements (41.6 vs.% 63.3%, p = 0.009) and nutritional parameters remained stable. A trend to a lower stay (3.5 to 4.5 days less) was detected in the groups of patients who covered their needs. CONCLUSIONS: The implementation of early malnutrition screening and short nutritional interventions improved energy and protein intake, increasing the percentage of patients who meet their requirements and avoiding deterioration of nutritional status.

A short nutritional intervention in a cohort of hematological inpatients improves energy and protein intake and stabilizes nutritional status / Una intervención nutricional en una cohorte de pacientes hospitalizados hematológicos mejora la ingesta calórico-proteica y estabiliza el estado nutricional

Introduction: Oncohematological diseases are associated with an important prevalence of malnutrition. Aim: Our aim is to determine if early recognition and treatment of malnourished hematological inpatients can improve their oral intake, nutritional status and reduce the length of hospital stay. Methods: Prospective 2-year study conducted in a cohort of hematology inpatients. Malnutrition Screening Tool (MST) was carried out on the first day of admission. Patients with a positive screening were recruited to have a complete nutritional evaluation and intervention, following usual clinical practice. Nutritional evaluation was repeated after one week. Results: Six hundred and seventeen hematological patients were screened (37.8% with positive screening). After one week, median diet intake increased from 80% to 90% (p < 0.001), and an increase of 407.36 Kcal (SD 679.37) and 17.58 g of protein (SD 31.97) was also achieved. More patients reached their energy and protein requirements (41.6 vs.% 63.3%, p = 0.009) and nutritional parameters remained stable. A trend to a lower stay (3.5 to 4.5 days less) was detected in the groups of patients who covered their needs. Conclusions: The implementation of early malnutrition screening and short nutritional interventions improved energy and protein intake, increasing the percentage of patients who meet their requirements and avoiding deterioration of nutritional status (AU)

Introducción: las enfermedades oncohematológicas se asocian con una elevada prevalencia de malnutrición. Objetivo: nuestro objetivo es determinar si la detección y el tratamiento precoz de la malnutrición en los pacientes hematológicos hospitalizados pueden mejorar su ingesta, su estado nutricional y reducir la estancia hospitalaria. Métodos: estudio prospectivo de 2 años de duración realizado en una cohorte de pacientes hematológicos hospitalizados. El Malnutrition Screening Tool (MST) fue el método de cribado efectuado el primer día del ingreso. En los pacientes con un resultado positivo en el cribado se realizó una valoración nutricional completa y una intervención terapéutica cuando fue preciso, siguiendo la práctica clínica habitual. La valoración nutricional se repitió una semana después de la inicial. Resultados: se evaluaron 617 pacientes hematológicos (de los cuales el 37,8% tuvo un resultado positivo en el cribado). Tras una semana de ingreso, la mediana de ingesta aumentó del 80% al 90% de la dieta (p < 0,001), y se logró un incremento en el consumo de 407,36 (DE 679,37) Kcal y 17,58 (DE 31,97) g de proteínas. El número de pacientes que alcanzaron sus requerimientos calórico-proteicos aumentó (41,6% vs. 63,3%, p = 0,009) y los parámetros nutricionales permanecieron estables. La estancia hospitalaria tendió a ser menor en los pacientes que cubrían sus necesidades nutricionales (3,5 a 4,5 días menos). Conclusiones: la implantación de un método de cribado nutricional precoz y la realización de intervenciones nutricionales cortas consiguió mejorar la ingesta calórico-proteica, aumentando el porcentaje de pacientes que cubrían sus necesidades y evitando el deterioro del estado nutricional (AU)

[Screening of the nutritional risk in elderly hospitalized patients with different tools]. / Valoración del riesgo nutricional en pacientes ancianos hospitalizados mediante diferentes herramientas.

BACKGROUND AND OBJECTIVE: Nutritional assessment in the elderly is difficult and different from that performed in younger people. There are specific tools for that purpose, such as the Geriatric Nutritional Risk Index (GNRI). The study objective was to compare this index to the Nutritional Risk Index (NRI). MATERIALS AND METHODS: A retrospective, observational analytical study including 113 hospitalized patients over 75 years of age receiving nutritional support. Weight, height, age, length of stay, Mini Nutritional Assessment (MNA), nutrition type and duration, and occurrence of complications were collected. GNRI and NRI were calculated. Both indexes were compared to each other and with parameters measured. RESULTS: Mean GNRI was 88.79 (SD: 13.1), mean NRI 79.96 (SD: 10.8), and mean MNA 17.49 (SD: 4.9). Complications occurred in 50.4% of patients, and 14% died. NRI and GNRI did not correlate with length of stay (R=0.136) or with length of nutrition (R=0.041). No significant correlation was seen between GNRI and complications, but a significant relationship was found with NRI. After stratification into surgical and medical patients, NRI was seen to be significantly related to complications in surgical patients only (p<0.05). GNRI was not related to complications in either surgical or medical patients. CONCLUSIONS: In hospitalized elderly patients, NRI is a better predictor of complications and may be more appropriate for assessing the risk of death than GNRI. GNRI underestimated nutritional risk as compared to NRI.

Valoración del riesgo nutricional en pacientes ancianos hospitalizados mediante diferentes herramientas / Screening of the nutritional risk in elderly hospitalized patients with different tools

Antecedentes y objetivo La valoración nutricional en el paciente anciano es compleja y no comparable a la de personas más jóvenes. Para ello existen herramientas específicas como el Índice de riesgo nutricional geriátrico (GNRI). El objetivo del estudio fue comparar este índice con el Índice de riesgo nutricional (NRI). Material y métodos Estudio observacional analítico retrospectivo que incluyó a 113 pacientes hospitalizados mayores de 75 años en seguimiento nutricional. Se recogió: peso, talla, edad, estancia media, Mini Nutritional Assessment (MNA), tipo de nutrición y duración de la misma y presencia de complicaciones. Se calcularon el NRI y el GNRI. Se compararon ambos índices entre sí y con los parámetros medidos. Resultados La media del GNRI fue 88,79 (DE: 13,1), la del NRI 79,96 (DE: 10,8) y la del MNA 17,49 (DE: 4,9). Un 50,4% sufrió complicaciones y un 14% fue éxitus. No se correlacionó el NRI ni el GNRI con estancia media R=0,136 ni con duración de la nutrición R=0,041. Al relacionar el riesgo nutricional con la presencia de complicaciones se observó que no había relación significativa con el GNRI, pero sí cñon el NRI (p<0,05). Estratificando en pacientes quirúrgicos y médicos existió relación significativa del NRI con las complicaciones sólo en pacientes quirúrgicos (p<0,05), siendo no significativa en pacientes médicos. Al analizar el GNRI se observó que no había relación significativa en ninguno de los grupos. Conclusiones En pacientes ancianos hospitalizados, el NRI predice mejor las complicaciones y podría ser más adecuado a la hora de valorar el riesgo de éxitus que el GNRI. El GNRI infraestima el riesgo nutricional respecto del NRI (AU)

Background and objective: Nutritional assessment in the elderly is difficult and different fromthat performed in younger people. There are specific tools for that purpose, such as the GeriatricNutritional Risk Index (GNRI). The study objective was to compare this index to the NutritionalRisk Index (NRI).Materials and methods: A retrospective, observational analytical study including 113 hospitalizedpatients over 75 years of age receiving nutritional support. Weight, height, age, lengthof stay, Mini Nutritional Assessment (MNA), nutrition type and duration, and occurrence ofcomplications were collected. GNRI and NRI were calculated. Both indexes were compared toeach other and with parameters measured. Results: Mean GNRI was 88.79 (SD: 13.1), mean NRI 79.96 (SD: 10.8), and mean MNA 17.49 (SD:4.9). Complications occurred in 50.4% of patients, and 14% died. NRI and GNRI did not correlatewith length of stay (R = 0.136) or with length of nutrition (R = 0.041). No significant correlationwas seen between GNRI and complications, but a significant relationship was found with NRI.After stratification into surgical and medical patients, NRI was seen to be significantly relatedto complications in surgical patients only (p < 0.05). GNRI was not related to complications ineither surgical or medical patients.Conclusions: In hospitalized elderly patients, NRI is a better predictor of complications and maybe more appropriate for assessing the risk of death than GNRI. GNRI underestimated nutritionalrisk as compared to NRI (AU)