Venlafaxine HCl Research Articles

Formulation and Evaluation of Sustained Release Dosage Form of Venlafaxine Hydrochloride for Enhanced Treatment of Neurodisorders

In the present study, we have designed and developed a sustained-release tablet formulation of Venlafaxine Hydrochloride. The optimized formulation was then subjected to various evaluation parameters. The formulation of venlafaxine hydrochloride sustained release tablets with a dosage of 500 mg included the utilization of several hydrophilic polymers, including jackfruit mucilage, HPMC K4, and PVPK30, as release retardants. This was done to extend the duration of drug release to 12 hours. The formulation features, including pre-compression and post-compression investigations, were conducted individually according to established protocols. The tablets were determined to be compliant in terms of weight uniformity, hardness, thickness, diameter, friability, and drug content. Separate in-vitro dissolution studies were done for both tablets. The venlafaxine hydrochloride SR formulation F18 was optimized to provide the desired release profile for up to 12 hours. The Venlafaxine Hydrochloride SR formulation was optimized and exhibited zero-order release kinetics. The stability studies conducted under accelerated conditions at a temperature of 40 ± 2°C and a relative humidity of 75 ± 5% yielded good results. The study indicated that the sustained release administration of Venlafaxine HCl is potentially efficacious. It reduces the frequency at which the patient has to take medication and improves patient adherence. Our objective is to conduct in-vivo pharmacokinetic studies of the formulation to verify the drug’s entry into the systemic circulation.

A rational study of transduction mechanisms of different materials for all solid contact-ISEs

The new era of solid contact ion selective electrodes (SC-ISEs) miniaturized design has received an extensive amount of concern. Because it eliminated the requirement for ongoing internal solution composition optimization and created a two-phase system with stronger detection limitations. Herein, the determination of venlafaxine HCl is based on a comparison study between different ion- to electron transduction materials (such as; multiwalled carbon nanotubes (MWCNTs), polyaniline (PANi), and ferrocene) and illustrating their mechanisms in their applied sensors. Their different electrochemical features (such as bulk resistance (Rb**), double-layer capacitance (Cdl), geometric capacitance (Cg), and specific capacitance (Cp)) were evaluated and discussed by using the Electrochemical Impedance Spectroscopy (EIS), Chronopotentiometry (CP), and Cyclic Voltammetry (CV) experiments. The results indicated that each transducer's influence on the proposed sensor's electrochemical characteristics is determined by their unique chemical and physical properties. The electrochemical features vary for different solid contact materials used in transduction mechanisms. The results confirm that the MWCNT sensor revealed the best electrochemical behavior with the potentiometric response of a near-Nernestian slope of 56.1 ± 0.8 mV/decade with detection limits of 3.8 × 10−6 mol/L (r2 = 0.999) and a low potential drift (∆E/∆t) of 34.6 µV/s. Also, the selectivity study was performed in the presence of different interfering species either in single or complex matrices. This demonstrates excellent selectivity, stability, conductivity, and reliability as a VEN-TPB ion pair sensor for accurately measuring VEN in its various formulations. The proposed method was compared to HPLC reported technique and confirmed no significant difference between them. So, the proposed sensors fulfill their solutions' demand features for VEN appraisal.

Passive Targeted Drug Delivery of Venlafaxine HCl to the Brain by Modified Chitosan Nanoparticles: Characterization, Cellular Safety Assessment, and In Vivo Evaluation

Passive Targeted Drug Delivery of Venlafaxine HCl to the Brain by Modified Chitosan Nanoparticles: Characterization, Cellular Safety Assessment, and In Vivo Evaluation

A pH responsive and superporous biocomposite hydrogel of Salvia spinosa polysaccharide-co-methacrylic acid for intelligent drug delivery.

Herein, a drug delivery system (SSH-co-MAA) based on the mucilage from seeds of Salvia spinosa (SSH; polymer) and methacrylic acid (MAA; monomer) is introduced for the controlled delivery of venlafaxine HCl using a sustainable chemical approach. The optimized conditions for the designing of the ideal formulation (M4) of SSH-co-MAA were found to be 2.5% (w/w) of SSH, 30.0% (w/w) of MAA, 0.4% (w/w) of both N,N'-methylene-bis-acrylamide (MBA; cross-linker) and potassium persulfate (KPS; initiator). The structure characterization of SSH-co-MAA by Fourier transform infrared and solid-state CP/MAS 13C-NMR spectroscopy has confirmed the grafting of MAA onto SSH. The thermogravimetric analysis revealed that SSH-co-MAA is a stable entity before and after loading of the venlafaxine HCl-loaded SSH-co-MAA (VSSH-co-MAA). Scanning electron microscopy images of SSH-co-MAA after swelling then freeze drying showed the superporous nature of the hydrogel. The gel fraction (%) of SSH-co-MAA depended upon concentration of SSH, MAA, and MBA. The porosity (%) was increased with the increase in the concentration of SSH and decreased with the decrease in the concentration of MAA and MBA. The swelling indices, venlafaxine HCl loading, and release (24 h at the pH of the gastrointestinal tract) from VSSH-co-MAA were found to be dependent on the pH of the swelling media and the concentration of SSH, MAA, and MBA. The release of venlafaxine HCl followed non-Fickian diffusion mechanism. Conclusively, SSH-co-MAA is a novel material for potential application in targeted drug delivery applications.

Synthesis, characterization, and acute toxicity of pH-responsive Salvia spinosa mucilage-co-acrylic acid hydrogel: A smart excipient for drug release applications

Owing to the increasing demand for pH-responsive excipients based on natural polysaccharides, a copolymeric biocomposite material was developed for sustained release drug delivery system (DDS). A novel pH-responsive, non-toxic, and superabsorbent graft copolymeric hydrogel (SSH-co-AA) based on mucilage from Salvia spinosa seeds (SSH) and acrylic acid (AA; monomer) was fabricated through free radical copolymerization using N,N′-methylene-bis-acrylamide (MBA; cross-linker) and potassium persulfate (KPS; initiator). The Fourier transform infrared and CP/MAS 13C‐NMR solid-state NMR spectroscopic analyses confirmed the successful grafting of AA onto SSH. The Powder X-ray diffraction analysis indicated the complete entrapment of crystalline drug in the amorphous polymeric network. Newly fabricated hydrogel is thermally more stable than SSH as revealed through thermogravimetric analysis (TGA). The scanning electron microscopic images indicated the porous nature of SSH-co-AA. An increase in the gel fraction is observed by increasing the concentration of SSH, AA, and MBA. The porosity of SSH-co-AA is directly proportional to the concentration of SSH and AA and inversely proportional to the concentration of MBA. The swelling of SSH-co-AA followed second-order kinetics and the sustained release of venlafaxine HCl followed the Korsmeyer-Peppas model and non-fickian diffusion mechanism. Acute oral toxicity studies of SSH-co-AA reported non-toxic and non-irritant attributes.

ONE FACTOR RESPONSE SURFACE METHODOLOGY (RSM) FOR THE OPTIMIZATION OF ORAL VENLAFAXINE HCL CONTROLLED RELEASE ORGANOGEL

Objective: The aim of this study was to develop the oral Venlafaxine HCl controlled-release organogel (organogel–CR) by using one-factor response surface methodology (RSM). Methods: In this study, Drug-excipient compatibility was evaluated by FT-IR. A total of 14 experimental runs were carried out employing the detailed conditions designed by a single factor completely randomized design based on the response surface methodology was used to check the concentration effect of 12-Hydroxy stearic acid (12-HSA) at different cooling rates on drug release at 10 h (Q10) and after 12 h (Q12). Multiple linear regression analysis, analysis of variance (ANOVA) and graphical representation of the influence factor were performed by using design expert 12. The developed organogel was also evaluated for viscosity, strength, transition temperature, diffusivity and Scanning electron microscopy (SEM). Prepared organogel was filled in the capsule and investigated for weight variation, drug content, erosion of organogel and In vitro drug release study. Results: FT-IR results showed that there was no chemical interaction between the drug and excipients. The SEM photograph indicates that the developed organogel was highly viscous with 3D network structure. The experimental confirmation tests showed a correlation between the predicted and experimental responses (R2 = 0.9937 and 0.9709). The results of ANOVA suggested that calculated F values of all dependent variables are greater than tabulated values. The optimal point obtained was located in the valid region and the optimum in vitro release of the predicted batch containing 7.9% concentration of 12-HSA with gradual cooling rate. To validate the evolved mathematical models, a checkpoint was selected and its desirability value was found to be 0.866. Conclusion: Oral controlled release Venlafaxine HCl organogel fix the problem of repeated dosing and patient noncompliance.

Application of mathematical modelling to alginate chitosan polyelectrolyte complexes for the prediction of system behavior with Venlafaxine HCl as a model charged drug

PurposeThis work aimed to develop and analyze the performance of chitosan/alginate polyelectrolyte complex (PEC). Multiple regression and Lab fit curve fitting were applied to derive empirical models for the prediction of zeta potential of plain systems as a function of alginate chitosan ratio. Venlafaxine-HCl was loaded as a model charged drug and empirical models for prediction of its release as a function of time were also derived. MethodsCoacervation method was used for the preparation of green PECs. Preliminary studies were conducted to optimize the preparation method. Pre-adjustment of the pH of alginate and chitosan sols enabled the formation of PECs at alginate/chitosan ratios starting from 1:9 to 9:1. On mixing of alginate and chitosan sols, equal volume dilution method produced spherical particles, while direct mixing method gave fibrous particles. Twenty-seven PECs nanoparticle formulae were prepared using nine alginate/chitosan ratios and three levels of total polymer concentrations. ResultsStatistical analysis showed that Zeta potential of the nanoparticle was significantly dependent on alginate/chitosan ratio, while particle size was a function of total polymer concentration. Nine fiber formulae were prepared and evaluated for their appearance and zeta potential. Venlafaxine-HCl release followed anomalous transport mechanism. FT-IR and DSC studies confirmed complexation at the carboxylate and amine site at alginate and chitosan respectively. ConclusionChitosan/alginate PECs were successfully obtained without a cross-linker and empirical equations were obtained to help finding the best composition for loading charged drugs and to predict their release profiles.

Venlafaxine HCl Encapsulated in Niosome: Green and Eco-friendly Formulation for the Management of Pain

The goal of this experimentation was to increase the cutaneous absorption of venlafaxine HCl (VFX) encapsulated in a niosome (venlasosme) produced by an ultrasonic approach. The impact of the cholesterol:surfactant (Chol:Surf) proportion was examined to modify the venlasosme properties. Photon correlation spectroscopy, powder X-ray diffraction (PXRD), SEM, DSC, and ATR-FTIR spectroscopy were utilized to investigate the solid-state and morphology of VFX in the venlasosme. The studies revealed that increasing the level of Chol in the venlasosme increased the size of the particles. Alterations in the Chol to surfactant ratios (when Chol decreased from 2.5 to 0%) caused the zeta potential enhancement from 7.37 ± 0.67 to 15.53 ± 1.47 mV. The venlasosme with the highest cholesterol concentration (2.5%) had the highest encapsulation efficiency (approximately 63%). PXRD results revealed that VFX in venlasosme was in the amorphous form. The levels of VFX in the cutaneous layers and the receiver compartment were higher for the venlasosme gel than for VFX simple gel in the cutaneous permeability study and showed no cutaneous irritancy in rats. Furthermore, the venlasosme gel demonstrated significant antinociceptive and anti-inflammatory responses when compared to the control groups (VFX simple gel and diclofenac gel). The topical administration of the venlasosme gel also considerably increased the tail-flick and hot-plate response time when compared to the VFX simple gel, control groups, and diclofenac gel (p < 0.05). These findings suggest that niosomes can improve VFX efficacy as an antinociceptive and anti-inflammatory substance by improving the medicaments delivery to the specified site.

Brain targeting of venlafaxine HCl as a hydrophilic agent prepared through green lipid nanotechnology

This study aimed to improve venlafaxine HCl brain delivery using solid lipid nanoparticles (SLNs) made by an ultrasonication method. The impact of the ratio of two surfactants (Tween:Span) on nanoparticle behaviors and their efficiency was examined to achieve optimal brain delivery for venlafaxine. To study the solid-state of venlafaxine in SLNs and detect any potential interactions between the drug and other formulation excipients, PCS, TEM, ATR-FTIR, and DSC were employed. By reducing the HLB (Hydrophilic–lipophilic balance) of the binary surfactants, the particle size of SLN increased. The optimized nanoparticles showed an average particle size of 311.33 ± 9.29 nm when the HLB of the ratio of the surfactants (Tween:Span) was adjusted to 8. The zeta potential of SLNs decreased from −15.90 ± 0.70 to −6.95 ± 0.42 mV when the HLB of the system was reduced from 14 to 8. According to the results, the highest entrapment efficiency of 76.05 ± 1.42% was observed for the formulation with the largest particle size and the lowest HLB value (HLB 8). DSC analysis showed that venlafaxine was in an amorphous state in SLN. The findings of the ATR-FTIR also excluded any chemical interactions between excipients and the drug. Venlafaxine-SLN had a prolonged release pattern, according to the in vitro diffusion process. Venlafaxine oral absorption from SLN was also substantially higher than venlafaxine solution after single-dose oral administration of venlafaxine preparations. This research demonstrated that the venlafaxine-SLN might be employed as a potential nano-vehicle for venlafaxine brain delivery and potentially opens up new avenues for depression treatment.

A Review on Analytical Method for Determination of Venlafaxine HCl in Bulk and Pharmaceutical dosage form

Venlafaxine HCl is one of the antidepressant agent which comes under the category of serotonin-norepinephrine reuptake inhibitor i.e SNRI. This medication is usually used to treat major depressive disorder in adult. It may help to improve the mood and energy level and also to regain the interest in daily activities in the depressed person. The present review focus on various approaches for the analysis on Venlafaxine in bulk and pharmaceutical dosage forms. The review represents the various analytical method like the RP-HPLC, HPTLC, UV Spectroscopy and Stability Indicating Methods which were used for the investigation of Venlafaxine in bulk and different dosage formulations.

Optimizing similarity factor of in vitro drug release profile for development of early stage formulation of drug using linear regression model

The objective of this article is to optimize the similarity factor within immediate release (IR) and modified release (MR) of in vitro drug release profiles. The least square method is used to minimize the difference between empirical and regression curve fitting data of in vitro IR/MR drug release profiles. An estimation of percentage drug release at intermediate timepoints has been done to improve the similarity factor f_{2} using linear curve fit method. In this study linear regression model is used to analyze the similarity factor f_{2} for Nitrofurantoin MR Capsules, Venlafaxine HCl MR Tablets and Lurasidone IR Tablets in order to exhibit the significance as well as similarity owing to the consideration of extra intervening timepoints. This linear regression model may help pharmaceutical industries to examine the inside comparison of IR/MR in vitro drug release profile with few modifications in timepoint selection to improve similarity factor f_{2}.

Formulation Development and Characterization of Controlled Release Core-in-cup Matrix Tablets of Venlafaxine HCl

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor, which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for a prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in a cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl was prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium stearate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification. In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson-crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in an acceptable range for all formulations. Based on the in vitro dissolution profile, formulation F-9was considered to be the optimized, extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and when compared with the innovator product (flavix XR), showed better drug release profile. Conclusion: The core-in-cup technology has the potential to control the release rate of freely water soluble drugs for single administration per day by optimization with the combined use of hydrophilic and hydrophobic polymers.

Optimization and evaluation of venlafaxine hydrochloride fast dissolving oral films

Three factors, three levels (33) full factorial design was used to develop venlafaxine HCl fast dissolving oral films (FDOFs) to optimize the concentrations of the film forming polymer; hydroxypropyl methylcellulose HPMC (X1), superdisintegrant; sodium starch glycolate SSG, (X2) and glycerol as the film plasticizer (X3). Effects of the three factors on the disintegration time (Y1), swelling index (Y2), and dissolution efficiency at 15 min; DE%15 (Y3) of the prepared FDOFs were evaluated by using statistical models. The optimized film formula was characterized in term of x-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and morphological characteristics.Disintegration time was found to increase with the increase in HPMC (X1) concentration, and the shortest disintegration time (21.67 ± 2.08 s) was observed in case of F2 formula (lowest HPMC level and highest glycerol level in absence of SSG). The highest swelling index (3.64 ± 0.59) was observed in case of film formula F1 (medium concentrations of both HPMC and glycerol and highest SSG concentration. The results also indicated that as the concentration of HPMC increased the DE%15 decreased. SSG (X2), with highest value (72.33 ± 1.71%) was recorded for in case of F12 (using 2% HPMC, 5%SSG and 1.5% glycerol). The optimized FDOF formula derived by the statistical models suggested 2% HPMC, 5% SSG, and 1% glycerol.The data obtained from DSC and XRPD revealed no interaction between drug and FDOT excipients. In addition, XRPD studies proved that the venlafaxine HCl was homogeneously dispersed in the film matrix.

Venlafaxine Hydrochloride Controlled Release Bilayer Tablets: Optimization of Formulation Variable by Using Dyspnea on Exertion

The current research work was to develop bilayer tablet of venlafaxine hydrochloride to increase drug efficacy for efficient treatment of depression. The satisfactory result of treatment can be achieved upon the maintenance of drug concentration within an effective level in the body, so a uniform and constant drug supply are desirable. An immediate layer of venlafaxine HCl was formulated using super disintegrants, i.e., croscarmellose sodium (CCS) and sodium starch glycolate (SSG); tablet compact by direct compression. HPMC K100M and ethylcellulose (EC) were utilized as release retarding polymers in sustained release layer by wet granulation technique with the help of PVP K30 in IPA solution (10%) as a granulating agent. Full 32 factorial designs were used to find out the optimum quantity of release retardant polymers. Bilayer tablet was evaluated for various parameters, i.e. hardness, friability, weight variation, % drug content, disintegration time (IR layer), and % drug release study. Statically, an analysis was carried out using factor X1 (HPMC K100M) and X2 (EC) for dependent variable % drug release at 8, 12, and 20 hours. A formulation was optimized and a formulation containing 305.36 mg of HPMC K100M and 54.03 mg of ethyl cellulose. Optimized formulation show 47.12 ± 2.1, 59.89 ± 2.2, and 89.06 ± 2.3 drug release at 8, 12, and 20 hours, respectively, which is almost similar to theoretical dose calculation with similarity factor f2 97, 99, and 98%, respectively. Bilayer tablet formulation was observed to be stable and fulfilled all compendia specifications.

Development and validation of an HPLC-UV method for accelerated stability study and pharmacokinetic analysis of venlafaxine

A reverse phase high performance liquid chromatography method has been developed and validated for accelerated stability study and determination of pharmacokinetic parameters of venlafaxine HCl. The chromatographic separation was carried out using ODS analytical column (250 × 4.6 mm i.d., 5 µm particle size). The mobile phase included acetonitrile, methanol and potassium dihydrogen phosphate buffer (30:30:40; pH 6.1) at a flow rate 1.5 mL min−1. UV-Visible detector was used at wavelength of 227 nm to monitor elutions. Retention time observed was 2.745 min. The method was validated for linearity, accuracy, precision, sensitivity and robustness. Accelerated stability study of venlafaxine HCl capsules was carried out at 40 and 50 oC under 75% RH level. Suggested method was successfully applied for the pharmacokinetic analysis of venlafaxine hydrochloride tablets. Each of ten albino rabbits (≈ 1.2 kg each) was orally administered with 5 mg dose of venlafaxine HCl. The method was proved to be linear (R2 >0.998), accurate (98.25-99.27%), sensitive (LOD: 35ngmL−1; LOQ: 105 ng mL−1) and robust (RSD<1%). The drug showed stability at accelerated conditions of temperature and humidity. The main pharmacokinetic parameters of tested products were as follows: tmax was 2.5h, Cmax was 56.5 µg mL−1, t1/2 was 8.2 h, AUC0-36 was 845.9 µg h mL−1. The developed method is suitable to apply for quality control analysis and pharmacokinetic studies.

Formulation Development and Characterization of Controlled Release Core-in-cup Matrix Tablets of Venlafaxine HCl

Formulation Development and Characterization of Controlled Release Core-in-cup Matrix Tablets of Venlafaxine HCl

Design of Experiment Approach in Development of Hydrophilic Matrix Tablet of Venlafaxine HCl: In vitro and In vivo studies

Design of Experiment Approach in Development of Hydrophilic Matrix Tablet of Venlafaxine HCl: In vitro and In vivo studies

Preparation and In vitro Characterisation Venlafaxine HCl Controlled Release Tablets

Preparation and <i>In vitro</i> Characterisation Venlafaxine HCl Controlled Release Tablets

Low Dose of Abilify (Aripiprazole) in Combination With Effexor XR (Venlafaxine HCl) Resulted in Cessation of Lactation

Postpartum depression (PPD) is a relatively common experience for women, especially those who have a history of preconception and/or prenatal depression. In some cases, pharmaceutical treatment is required to treat the symptoms of PPD. Unfortunately, the use of some of these treatments may have unintended consequences that affect both the newborn and the new mother. Here we report a case where Abilify (aripiprazole) at a low dose (2 mg/day) was prescribed in conjunction with Effexor XR (venlafaxine HCl) at a high dose (225 mg/day), which resulted in the cessation of lactation.

Formulation and Evaluation of Pulsatile Drug Delivery System of Venlafaxine HCL

Formulation and Evaluation of Pulsatile Drug Delivery System of Venlafaxine HCL