Bioanalytical Method Development and Validation of Memantine in Human Plasma by High Performance Liquid Chromatography with Tandem Mass Spectrometry: Application to Bioequivalence Study

A simple, sensitive, and rapid HPLC-MS/MS method was developed and validated for quantitative estimation of memantine in human plasma. Chromatography was performed on Zorbax SB-C18 (4.6 × 75 mm, 3.5 μm) column. Memantine (ME) and internal standard Memantine-d6(MED6) were extracted by using liquid-liquid extraction and analyzed by LC-ESI-MS/MS using multiple-reaction monitoring (MRM) mode. The assay exhibited a linear dynamic range of 50.00–50000.00 pg/ml for ME in human plasma. This method demonstrated an intra- and interday precision within the range of 2.1–3.7 and 1.4–7.8%, respectively. Further intra- and interday accuracy was within the range of 95.6–99.8 and 95.7–99.1% correspondingly. The mean recovery of ME and MED6 was 86.07 ± 6.87 and 80.31 ± 5.70%, respectively. The described method was successfully employed in bioequivalence study of ME in Indian male healthy human volunteers under fasting conditions

Fabrication and in vitro evaluation of subgingival strips of calcium alginate for controlled delivery of ofloxacin and metronidazole

Objetivos: Elaborar y evaluar tiras subgingivales combinadas compuestas por Ofloxacino y metronidazol in vitro con alginato de calcio biodegradable.Métodos: las tiras se prepararon utilizando el método de evaporación del disolvente. Se usó una concentración del 10% de CaCl2 para la gelificación.de las tiras.Resultados: el grosor de las tiras se encuentra dentro de las recomendaciones (>320 μm). In vitro, la liberación de la droga siguió una cinética bifásica que fue suficiente para alcanzar la CMI e inhibir el crecimiento de microorganismos durante 5 días. La “tasa de liberación de la droga” es inversamente proporcional a la concentración de polímero de la formulación. La liberación de la “droga” fue por difusión y en segunda fase por disolución.Discusión: Las preparaciones OM1 y OM2 que contienen un 90 y un 75% de polímero respectivamente, podrían ser empleadas en liberación controlada durante cinco días en infecciones sublinguales. Siendo el alginato cálcico biodegradable una buena elección como polímero retardanteAim: Subgingival strips of combined ofloxacin (OFX) and metronidazole (MET) were fabricated and evaluated in vitro using biodegradable calcium alginate.Methods: Strips of drug:polymer (10:90, 25:75, 50:50 and 75:25) were prepared using solvent casting method. A 10%w/v CaCl2 solution was used for gelation of the strips.Results: The thickness of strips were at par of recommended thickness (<320 μm). In vitro release of drugs followed a biphasic kinetics which was sufficient to maintain the minimum inhibitory concentrations (MIC) to inhibit the growth of the microorganisms for 5 days. The rate of drug release was inversely proportional to polymer concentration in the formulations. The drug release was by diffusion in second phase of dissolution.Conclusions: The formulations OM1 and OM2 which contain 90 and 75%w/w of polymer could be employed for controlled delivery of combined OFX and MET for 5 days in subgingival infections. Calcium alginate, being a biodegradable is a good choice as drug retarding polymer

Bio-analytical method development and validation of Rasagiline by high performance liquid chromatography tandem mass spectrometry detection and its application to pharmacokinetic study

The most suitable bio-analytical method based on liquidâliquid extraction has been developed and validated for quantification of Rasagiline in human plasma. Rasagiline-13C3 mesylate was used as an internal standard for Rasagiline. Zorbax Eclipse Plus C18 (2.1 mmÃ50 mm, 3.5 μm) column provided chromatographic separation of analyte followed by detection with mass spectrometry. The method involved simple isocratic chromatographic condition and mass spectrometric detection in the positive ionization mode using an API-4000 system. The total run time was 3.0 min. The proposed method has been validated with the linear range of 5â12000 pg/mL for Rasagiline. The intra-run and inter-run precision values were within 1.3%â2.9% and 1.6%â2.2% respectively for Rasagiline. The overall recovery for Rasagiline and Rasagiline-13C3 mesylate analog was 96.9% and 96.7% respectively. This validated method was successfully applied to the bioequivalence and pharmacokinetic study of human volunteers under fasting condition. Keywords: High performance liquid chromatography, Mass spectrometry, Rasagiline, Liquidâliquid extractio

Elaboración y evaluación in vitro de tiras subgingivales de alginato de calcio para la liberación controlada de ofloxacino y metronidazol

Aim: Subgingival strips of combined ofloxacin (OFX) and metronidazole (MET) were fabricated and evaluated in vitro using biodegradable calcium alginate. Methods: Strips of drug:polymer (10:90, 25:75, 50:50 and 75:25) were prepared using solvent casting method. A 10%w/v CaCl2 solution was used for gelation of the strips. Results: The thickness of strips were at par of recommended thickness (<320 μm). In vitro release of drugs followed a biphasic kinetics which was sufficient to maintain the minimum inhibitory concentrations (MIC) to inhibit the growth of the microorganisms for 5 days. The rate of drug release was inversely proportional to polymer concentration in the formulations. The drug release was by diffusion in second phase of dissolution. Conclusions: The formulations OM1 and OM2 which contain 90 and 75%w/w of polymer could be employed for controlled delivery of combined OFX and MET for 5 days in subgingival infections. Calcium alginate, being a biodegradable is a good choice as drug retarding polymer.Objetivos: Elaborar y evaluar tiras subgingivales combinadas compuestas por Ofloxacino y metronidazol in vitro con alginato de calcio biodegradable Métodos: las tiras se prepararon utilizando el método de evaporación del disolvente. Se usó una concentración del 10% de CaCl2 para la gelificación.de las tiras. Resultados: el grosor de las tiras se encuentra dentro de las recomendaciones (>320 μm). In vitro, la liberación de la droga siguió una cinética bifásica que fue suficiente para alcanzar la CMI e inhibir el crecimiento de microorganismos durante 5 días. La “tasa de liberación de la droga” es inversamente proporcional a la concentración de polímero de la formulación. La liberación de la “droga” fue por difusión y en segunda fase por disolución Discusión: Las preparaciones OM1 y OM2 que contienen un 90 y un 75% de polímero respectivamente, podrían ser empleadas en liberación controlada durante cinco días en infecciones sublinguales. Siendo el alginato cálcico biodegradable una buena elección como polímero retardante.El estudio se ha realizado con los medios habituales de que dispone el Departamento de Nutrición y Bromatología y a través de los recursos aportados por el Máster Universitario en Atención Farmacéutica (EuropharmNES) de la Universidad de Granada