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 17 publications

(11 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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“…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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“…One half of the group (arbitrarily designated as IIa, n = 8) after the end of experiments, in the stresscamera, daily for 14 days was treated with a selective inhibitor of the serotonin reuptake fluoxetine that has powerful antidepression properties [32,33]. The rats obtained fluoxetine in the amount of 40 mg/kg with drinking water.…”

Section: Methodsmentioning

confidence: 99%

A new model of depression induced by psychogenic stress

Chichinadze

Damianidze

Matitaishvili

et al. 2012

J Evol Biochem Phys

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A new model of depression based on use of stressors of the psychogenic nature has been created. It turned out that laboratory rats in a special stress-camera were unable to elaborate bilateral reaction of active avoidance, which later on led to formation of their depression-like state. Development of such their state was confirmed by analysis of tests sensitive to depression: forced swimming and tail suspension, dynamics of the animal body mass and their behavior on the whole. This model has turned out to be sensitive to a selective inhibitor of the serotonin uptake-fluoxetine, which also confirms that our obtained model is the model of depression.

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

Cited by 17 publications

References 12 publications

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

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

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

A new model of depression induced by psychogenic stress

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