Antidepressant behavioral effects of duloxetine and fluoxetine in the rat forced swimming test

Ciulla, Leandro; Menezes, Honório Sampaio; Bueno, Bárbara Beatriz Moreira; Schuh, Alexandre; Alves, Rafael José Vargas; Abegg, Milena Pacheco

doi:10.1590/s0102-86502007000500005

Cited by 18 publications

(13 citation statements)

References 12 publications

(7 reference statements)

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“…In vivo efficacy was evaluated on male Swiss albino mice by forced swim test (20). The protocol for the study was approved by the Institutional Ethics Committee of Bombay College of Pharmacy, Mumbai, India, and the animal handling throughout the experiment was performed in accordance to the Committee for the Purpose of Control and Supervision of Experiments on Animals guidelines.…”

Section: Evaluation Of Chemical Stability In Aqueous and Acidic Mediamentioning

confidence: 99%

Duloxetine HCl Lipid Nanoparticles: Preparation, Characterization, and Dosage Form Design

2011

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Abstract. Solid lipid nanoparticles (SLNs) of duloxetine hydrochloride (DLX) were prepared to circumvent the problems of DLX, which include acid labile nature, high first-pass metabolism, and highdosing frequency. The DLX-SLNs were prepared by using two different techniques, viz. solvent diffusion method and ultrasound dispersion method, and evaluated for particle size, zeta potential, entrapment efficiency, physical characteristics, and chemical stability. Best results were obtained when SLNs were prepared by ultrasound dispersion method using glyceryl mono stearate as solid lipid and DLX in ratio of 1:20 and mixture of polysorbate 80 and poloxamer 188 as surfactant in concentration of 3%. The mean particle size of formulation and entrapment efficiency was 91.7 nm and 87%, respectively, and had excellent stability in acidic medium. Differential scanning calorimetry and X-ray diffraction data showed complete amorphization of DLX in lipid. In vitro drug release from SLNs was observed for 48 h and was in accordance with Higuchi kinetics. In vivo antidepressant activity was evaluated in mice by forced swim test. DLX-SLNs showed significant enhancement in antidepressant activity at 24 h when administered orally in comparison to drug solution. These results confirm the potential of SLNs in enhancing chemical stability and improving the efficacy of DLX via oral route. The SLN dispersion was converted into solid granules by adsorbing on colloidal silicon dioxide and characterized for particle size after redispersion, morphology, and flow properties. Results indicated that nanoparticles were successfully adsorbed on the carrier and released SLNs when dispersed in water.

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Section: Evaluation Of Chemical Stability In Aqueous and Acidic Mediamentioning

confidence: 99%

Duloxetine HCl Lipid Nanoparticles: Preparation, Characterization, and Dosage Form Design

2011

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“…Duloxetine showed reversal of cognitive deficit at dose range of 10~30 mg/kg in rodents [13]. In forced swim test, the immobility period was significantly reduced at 10 mg/kg dose [14, 15]. In addition to 5-HT and NE reuptake inhibitors, nootropic agents like piracetam [16] also play an important role in cognition.…”

Section: Introductionmentioning

confidence: 99%

The Combination of Antidepressant Duloxetine with Piracetam in Mice does not Produce Enhancement of Nootropic Activity

et al. 2014

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There is a strong association between depression and memory impairment. The present study aims to assess the nootropic activity of duloxetine and piracetam combination. Male Swiss Albino mice were divided randomly into 4 groups. Treatment of normal saline (10 ml/kg), duloxetine (10 mg/kg), piracetam (100 mg/kg), and duloxetine (5 mg/kg) plus piracetam (50 mg/kg) were given through intra-peritoneal route to group I-IV, respectively. Transfer latency in elevated plus maze (EPM) and time spent in target quadrant in Morris water maze (MWM) were recorded. Estimation of brain monoamines in hippocampus, cerebral cortex, and whole brain were done using HPLC with fluorescence detector. Piracetam treated group showed significant decrease in transfer latency in EPM and increase in time spent in target quadrant recorded in MWM. Combination treated group failed to produce statistically significant nootropic effect in both EPM and MWM. Combination treated group failed to increase brain monoamine levels when compared against duloxetine and piracetam treated groups, separately. But there was exception of significant increase in norepinephrine levels in hippocampi when compared against duloxetine treated group. Results indicate no cognitive benefits with piracetam plus duloxetine combination. These findings can be further probed with the aim of understanding the interaction between duloxetine and piracetam as a future endeavor.

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“…Therefore, the reduction in the serum duloxetine concentration seen during the forced swimming test would have been caused by decreased absorption due to direct reactions between duloxetine and MgO, rather than by in vivo pharmacokinetic interactions. In the clinical setting, the dosage of MgO used to treat constipation is generally about 1000-2000 mg/d, 13,14) and the standard dose of duloxetine is about 40-60 mg/d. Therefore, the dose ratio of MgO to duloxetine is about 16.7-50.…”

Section: Discussionmentioning

confidence: 99%

Effects of Magnesium Oxide on the Serum Duloxetine Concentration and Antidepressant-Like Effects of Duloxetine in Rats

Esumi

Kitamura

Yokota-Kumasaki

et al. 2018

Biological & Pharmaceutical Bulletin

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Duloxetine is a serotonin/noradrenaline reuptake inhibitor that is used as an antidepressant. However, it is known to cause constipation as a side effect. Magnesium compounds, such as magnesium oxide and magnesium hydroxide aqueous solution, are often combined with duloxetine to ameliorate the constipation caused by duloxetine. However, there is concern that these magnesium compounds might alter the effects of duloxetine via physicochemical interactions. In this study, we attempted to clarify the interactions that take place between duloxetine and magnesium oxide using in vivo and in vitro experiments. We evaluated the influence of magnesium oxide on in vitro duloxetine concentrations using HPLC. In addition, we examined the in vivo antidepressant-like effects and serum concentrations of duloxetine in rats. In the in vitro experiment, the duloxetine concentration was significantly decreased by co-treatment with magnesium oxide. In the in vivo experiment, the antidepressant-like effects of duloxetine were not affected by the combined oral administration of magnesium oxide and a duloxetine formulation although the serum duloxetine level was significantly decreased. However, the antidepressant-like effects of a duloxetine reagent were significantly attenuated by the co-administration of magnesium oxide. These results suggest that duloxetine and magnesium oxide directly interact and that such interactions affect the absorption and antidepressant-like effects of duloxetine.

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Antidepressant behavioral effects of duloxetine and fluoxetine in the rat forced swimming test

Cited by 18 publications

References 12 publications

Duloxetine HCl Lipid Nanoparticles: Preparation, Characterization, and Dosage Form Design

Duloxetine HCl Lipid Nanoparticles: Preparation, Characterization, and Dosage Form Design

The Combination of Antidepressant Duloxetine with Piracetam in Mice does not Produce Enhancement of Nootropic Activity

Effects of Magnesium Oxide on the Serum Duloxetine Concentration and Antidepressant-Like Effects of Duloxetine in Rats

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