Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 2 de 2
Filtrar
Más filtros

Bases de datos
Tipo del documento
País de afiliación
Intervalo de año de publicación
1.
AAPS PharmSciTech ; 22(3): 114, 2021 Mar 24.
Artículo en Inglés | MEDLINE | ID: mdl-33763759

RESUMEN

Lisofylline (LSF) is an anti-inflammatory molecule with high aqueous solubility and rapid metabolic interconversion to its parent drug, pentoxifylline (PTX) resulting in very poor pharmacokinetic (PK) parameters, necessitating high dose and dosing frequency. In the present study, we resolved the physicochemical and pharmacokinetic limitations associated with LSF and designed its oral dosage form as a tablet for effective treatment in type 1 diabetes (T1D). Self-assembling polymeric micelles of LSF (lisofylline-linoleic acid polymeric micelles (LSF-LA PLM)) were optimized for scale-up (6 g batch size) and lyophilized followed by compression into tablets. Powder blend and tablets were evaluated as per USP. LSF-LA PLM tablet so formed was evaluated for in vitro release in simulated biological fluids (with enzymes) and for cell viability in MIN-6 cells. LSF-LA PLM in tablet formulation was further evaluated for intestinal permeability (in situ) along with LSF and LSF-LA self-assembled micelles (SM) as controls in a rat model using single-pass intestinal perfusion (SPIP) study. SPIP studies revealed 1.8-fold higher oral absorption of LSF-LA from LSF-LA PLM as compared to LSF-LA SM and ~5.9-fold higher than LSF (alone) solution. Pharmacokinetic studies of LSF-LA PLM tablet showed greater Cmax than LSF, LSF-LA, and LSF-LA PLM. Designed facile LSF-LA PLM tablet dosage form has potential for an immediate decrease in the postprandial glucose levels in patients of T1D.


Asunto(s)
Diabetes Mellitus Tipo 1/metabolismo , Yeyuno/metabolismo , Ácido Linoleico/farmacocinética , Nanopartículas/metabolismo , Pentoxifilina/análogos & derivados , Perfusión/métodos , Administración Oral , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Diabetes Mellitus Tipo 1/tratamiento farmacológico , Formas de Dosificación , Yeyuno/efectos de los fármacos , Ácido Linoleico/administración & dosificación , Ácido Linoleico/síntesis química , Masculino , Ratones , Nanopartículas/administración & dosificación , Nanopartículas/química , Pentoxifilina/administración & dosificación , Pentoxifilina/síntesis química , Pentoxifilina/farmacocinética , Ratas , Ratas Wistar , Comprimidos
2.
Talanta ; 116: 56-64, 2013 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-24148373

RESUMEN

The applicability of high-performance liquid chromatography with ultraviolet light (HPLC-UV) for the determination of the presence of statins in macromycetes of the genus Pleurotus was analyzed. The fungi were obtained by liquid-state fermentation (LSF) using unconventional sources of carbon as substrates and solid-state fermentation (SSF) employing agro industrial wastes. Five statins were used as standards: lovastatin and simvastatin in the lactone form (LOVL and SIML), their corresponding hydro-acidic forms (LOVH and SIMH) and pravastatin (PRA). The following measures were evaluated: the linearity, accuracy and precision, detection limit (DL) and quantification limit (QL). The results demonstrated HPLC-UV to be an effective tool for detecting the presence of statins in extracts of LSF and SSF products. Likewise, it was hypothesized that the strains that were used for the study do not produce statins. This finding highlights the importance of continuing to evaluate other strains of the same genus by using techniques such as HPLC to first separate sufficient quantities of the compounds that were detected using the standard technique but that did not match the retention time (tR) of any of the standards used.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Lovastatina/aislamiento & purificación , Pleurotus/metabolismo , Pravastatina/aislamiento & purificación , Simvastatina/aislamiento & purificación , Agricultura , Cromatografía Líquida de Alta Presión/normas , Estabilidad de Medicamentos , Fermentación , Límite de Detección , Lovastatina/biosíntesis , Pravastatina/biosíntesis , Simvastatina/metabolismo , Residuos
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA