Aceclofenac

The aim of the research study was the development and validation of a simple, rapid, accurate and precise reversed-phase high performance liquid chromatography (RP-HPLC) stability-indicating method for the determination of aceclofenac in bulk and pharmaceutical dosage forms. The RP-HPLC studies was performed on the instrument Jasco HPLC system with Jasco UV 2010 photo diode array detector, ODS C18 RP-column (Intersile 250 mm × 4.6 mm; i.d. 10 μm), Rheodyne injection syringe with 20µL loop volume and windows based chrompass software was used for separation. The isocratic elution was performed using the mobile phase ratio of methanol: water (65:35 v/v) and UV detection wavelength at 263 nm. The overall run time of the analysis was 20 minutes and the flow rate was 1.0 mL/min. The RP-HPLC method developed for analysis of aceclofenac was validated as per the ICH guidelines with respect to specificity, selectivity, linearity, accuracy, precision and robustness. The linearity for developed method was observed in the concentration range of 5-50 μg/mL with the correlation coefficient (r2) of 0.9992. The percentage accuracy of aceclofenac ranged from 99.40 to 100.79%. The relative standard deviation for inter-day precision was lower than 2.0%. The assay of aceclofenac was determined in tablet dosage form was found to be within limits. Aceclofenac was subjected to stress conditions such as neutral, acidic, alkaline, oxidation, and photolysis degradations as per ICH guidelines. The results of degradation studies revealed that the drug degraded a maximum (32.68%) in acidic conditions followed by alkaline conditions (15.05%). The drug was found to be resistant towards neutral, acidic and photolytic degradation conditions.

The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl methyl cellulose) and hydrophobic (methyl cellulose) polymeric systems by the solvent casting technique. Formulated transdermal patches were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro drug studies of formulations were performed by using Franz diffusion cells. The results followed the release profile of Aceclofenac followed mixed zero-order. However, the release profile of the optimized formulation F9 (99.50±0.09) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 217±7.42 fold enhancements in drug permeation.

Current research is focused on formulation and evaluation of natural gum based fast dissolving tablet of aceclofenac by applying 32 factorial design. Direct compression method was used. Two factors as independent variable (x1)okra gum (x2) sodium saccharin glycol ate were taken with three level (+1, 0,-1) .The level two factors were selected on basis of preliminary experiments conducted and their effect on dependent variable (disintegration time ,in vitro drug release) was estimated formulated tablets were evaluated for parameters (hardness, thickness, weight variance, wetting time and water absorption ratio, disintegration time ,friability,% commutative drug release ).the software design expert (11.0) was used for gee rating experimental design ,modeling the response surface and calculating the static evaluation .The tablet parameters tests of formulation (F1 TO F 10 ) were observed within prescribe limit. DT observed in the range of 51 sec to 9 min. % cumulative drug release 0.31 % to 107.97 %. Batch F10 was observed as promising batch with DT values 46 sec.

The present study deals with application of melt granulation technology to develop sustained release formulation of aceclofenac with lipidic excipients (Compritol 888 ATO). This approach is concerned with the use of minimum number of excipients to reduce the tablet weight and increase the compatibility of the drug. The continuous melt granulation/extrusion was done by optimizing the formulation as well as processing parameter such as drug loading, operating temperature, screw speed and feed rate during the process. The FTIR study revealed that there is no chemical interaction exists in between the drug and lipidic excipients while DSC and XRD studies exhibited crystalline state of the drug after melt granulation. The scanning electron microscopic examination of melt extrudates revealed the agglomerated particles with porous network and rough surface. The developed tablet (80% drug loading) has weight of  250 mg (mini tablet) containing 200mg of aceclofenac and it showed sustained release profile upto 24h.

The present manuscript describes sensitive, rapid, accurate, and precise spectrophotometric method for simultaneous estimation of allopurinol and aceclofenac in pharmaceutical dosage form. Simultaneous equation method used at 250nm & 273nm as λmax of allopurinol and aceclofenac respectively in 0.1N HCl. Both the drugs follow beer-lamber’s law on the concentration range 2-12µg/ml and 2-24µg/ml respectively for allopurinol & aceclofenac. The mean percentage recovery is 100.01% and 99.4% for allopurinol and aceclofenac respectively by simultaneous equation. The method has been validated as per ICH guidelines. The proposed method effectively applied to bulk drug and pharmaceutical formulation. The accuracy and reproducibility are close to 100% with acceptance range of %R.S.D. The method was successfully applied to pharmaceutical dosage form because no interference was found from excipient. 

A simple, accurate, precise and specific RP-HPLC method has been developed for the simultaneous estimation of Aceclofenac and Esomeprazole Sodium in bulk. Chromatographic analysis was carried out on C18 column ( 250mm × 4.6mm, 5µm). Mobile phase used is a homogenous mixture of ACN: Methanol in the ratio of 50:50 v/v. The detection was carried out at 285nm. The retention times were found to be 3.00 and 4.41 min for Aceclofenac and Esomeprazole Na respectively. Both the drugs showed linearity in the range of 30 – 70mcg/ml. The correlation coefficient was found to be 0.99 and 0.992 for Aceclofenac and Esomeprazole Na respectively. The developed method was validated as per ICH guidelines.

Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of drug, oil, surfactant and co-surfactant which spontaneously forms emulsion in aqueous environment under gentle agitation. Many drugs are lipophilic in nature making them difficult for oral delivery as the GI environment is aqueous in nature. The objective of present work was to develop and evaluate the SEDDS of Aceclofenac using oleic acid as oil, tween 20 as surfactant and PEG 400 as  co-surfactant. Compatibility studies showed no interaction between drug and excipients used. Ternary phase diagram was constructed to optimize the formulation. Formulated SEDDSs were evaluated for drug content, zeta-potential, robustness to dilution, globule size and in-vitro drug release. Globule size were between 151.1-182.3 nm and spherical in shape. In-vitro drug release study revealed that the drug release form the formulated SEDDSs were faster when compare to pure drug and marketed product. Formulation S6 showed the highest drug release i.e. 91.71% within 25 m. Formulations were stable during testing period of 3 months. From this work, it was cleared that the SEDDS of Aceclofenac was found to be significant in terms of releasing of the drug as compare to pure drug and marketed product.

The current work deals with the formulation and development of sustained release tablets of Aceclofenac using natural polymers. Anacardium Occidentale (Cashew) gum and xanthan gum were used as a sustained release polymers. Literature survey has revealed that Anacardium Occidentale (Cashew) gum has been used as a pharmaceutical excipient, namely: as a binding agent in tablet formulations, emulsifying agent in emulsions, suspending agent in suspensions and mucoadhesive in mucoadhesive tablet. In this present study we tried to explore its drug release control properties. Aceclofenac drug was used as model drug and xanthan gum was used alone and in combination with cashew gum. Collected cashew gum was purified and checked for its purity by determination of microbial load. Different formulations were set by taking different concentrations of cashew gum, xanthan gum and combinations of both the gums. Tablets were prepared using wet (non-aqueous) granulation method. The flow properties of the granules were evaluated (angle of repose, bulk density, taped density, Car’s index, Hausner’s ratio) and the physical properties of the compressed tablets, namely dimensions, uniformity of weight, hardness, friability and dissolution rate were determined. All results obtained from these tests were found to be within permissible limit. The granules had good flow properties as evidenced by their Hausner’s ratio and Carr’s index values. From the overall result obtained and drug release profile we can conclude that cashew gum can be used as sustained release polymer in sustained release tablet.

A simple, rapid reverse phase high performance liquid chromatographic method (RP- HPLC) has been developed and validated for simultaneous estimation of Aceclofenac and Pregabalin in tablet dosage form. Chromatographic separation was achieved C-18 (250 mm × 4.6 mm, 5.0μ) as stationary phase and mobile phase containing phosphate (pH adjusted to 5.0 ± 0.05 using NaOH.) Buffer: Acetonitrile (30:70 v/v) at flow rate of 1 ml/min using UV detection at 210 nm. The retention time for Aceclofenac and Pregabalin was found to be 3.177 and 5.530 min respectively. The method was validated as per International Conference on Harmonization guideline and successfully used for the quantitative analysis of commercially available tablet. The calibration curve was linear over the concentration range of 20-60μg/ml for Aceclofenac and 15-45μg/ml for Pregabalin.. Lower values of Limit of Detection (0.60μg/ml for Aceclofenac and 0.88μg/ml for Pregabalin) and Limit of Quantification (1.84μg/ml for Aceclofenac and 2.68μg/ml for Pregabalin ) indicated good sensitivity of the method. The method was validate with respect to linearity, robustness, precision and accuracy and was successfully applied for the simultaneous determination of aceclofenac and pregabalin from the combined dosage formulation. The percent amount for both the drugs were found to be within limits in the tablet dosage form for both the methods.

Chitosan, a linear binary heteropolysaccharide, composed of β-1, 4-linked glucosamine (GlcN) with various degrees of N-acetylation of GlcN residues. It is a non-toxic, biocompatible and biodegradable natural polymer of high molecular weight (~500,000 kDa). The degree of deacetylation (DD) and molecular weight (MW) are two fundamental parameters that can affect the properties and functionality of chitosan. HPMC is the dominant hydrophilic vehicle used for the preparation of oral controlled drug delivery systems. Hydrophilic polymers are widely used in controlled release systems due to their favorable functionality. Enhancing the mobility of the polymer chains and diffusing of the drug out from such polymer matrices could be done by inclusion of different types of excipients at different concentrations. The present manuscript describes the attempt undertaken to develop the matrix tablet of Aceclofenac along with different grades of chitosan and HPMC as a copolymer & to study effect of it on the swelling behavior and the drug release pattern.