You are hereCOMPARATIVE DISSOLUTION STUDIES FOR ACECLOFENAC MARKETED DOSAGE FORMS

COMPARATIVE DISSOLUTION STUDIES FOR ACECLOFENAC MARKETED DOSAGE FORMS


C.  ACECLOFENAC

Development of Discriminating Method for Dissolution of Aceclofenac Marketed Formulations26
Tejal Soni , Chirag Nagda ,Teja Gandhi and N. P. Chotai
Abstract
: The development of a meaningful dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Aceclofenac (BCS Class II drug) is a nonsteroidal anti-inflammatory drug. There is no official dissolution medium available in the literature. In the present study, parameters such as solubility, medium pH, surfactant type, dissolution behavior of formulations, influence of sink conditions, stability, and discriminatory effect of dissolution testing were studied for the selection of a proper dissolution medium. Results of solubility data revealed that solubility increased with an increase in pH. Sink conditions were exhibited in all media except double-distilled water and 0.1 N HCl. The drug and marketed formulations were stable in the dissolution media used. An agitation speed of 50 rpm showed a more discriminating drug release profile than 75 rpm. The discriminating dissolution method for aceclofenac formulation is paddle at 50 rpm, 900 mL pH 6.8 phosphate buffer, greater than 80% of the label amount is released over 60 minutes.

Assessment of Dissolution Profile of Aceclofenac Tablets Available in Bangladesh27
Tajnin Ahmed, Afia Ferdous, Subrata Kumar Biswas, Farhana Sharif

Abstract: The objective of this work is to find out brand-to-brand variation by applying profile comparison approaches to the dissolution data of marketed aceclofenac tablet formulations. Commercially available five brands of aceclofenac tablets were studied in simulated intestinal medium (pH 6.8) for 60 minutes time period using USP reference dissolution apparatus. Four samples complied with the USP in vitro dissolution specifications for drug release (not less than 80% of the labeled amount of Aceclofenac should be dissolved in 60 minutes). One brand (Code: S1) failed to meet the criteria; drug release was 66.85% within the specified time period.

Assessment of dissolution profile of marketed aceclofenac formulations4
Soni T, Chotai N.
Abstract
: Statistical comparison of dissolution profiles under a variety of conditions relating to formulation characteristics, lot-to-lot, and brand-to-brand variation attracts interest of pharmaceutical scientist. The objective of this work is to apply several profile comparison approaches to the dissolution data of five-marketed aceclofenac tablet formulations. Model-independent approaches including ANOVA-based procedures, ratio test procedure, and pair wise procedure. The ratio test includes percentage, area under the curve, mean dissolution time, while the pair wise procedure includes difference factor (f1), similarity factor (f2), and Rescigno index. In the model-dependent approach, zero order, first order, Hixson-Crowell, Higuchi, and Weibull models were applied to the utilization of fit factors. All the approaches were applicable and useful. ANOVA with multiple comparison tests was found to be sensitive and discriminating for comparing the profiles. Weibull parameters were more sensitive to the difference between two release kinetic data in terms of curve shape and level.

Development and Characterization of Once a Daily Tablet Formulation of Aceclofenac28
Punit B. Parejiya, Bhavesh S. Barot, Hetal K. Patel, Pragna K. Shelat
Abstract
: Sustained release Aceclofenac matrix tablets constituting Kollidon SR (Polyvinyl acetate- povidone based matrix retarding polymer) were developed for manifesting desirable release profile. Matrix tablets were prepared by direct compression of Kollidon SR varying proportion with fixed percentage of aceclofenac. Tablets containing 50 % Kollidon SR demonstrated a rapid rate of drug release with an initial burst effect. Incorporation of more Kollidon SR in the tablet prolonged drug release with subsequent minimization of burst effect as confirmed by mean dissolution time, dissolution efficiency, f2 and drug release kinetic data. The formulation showed close resemblance to commercial product Senafen. The results were explored and explained by the difference of physico-chemical property and micromeritic characteristics. Insignificant effect of various factors e.g. pH, ionic strength, paddle speed was found on drug release. The formulation followed Korsmeyer and peppas kinetic of drug release. Stability study data indicated stable character after short term stability study.

Formulation and Evaluation of Sustained Release Tablets of Aceclofenac using Hydrophilic Matrix System29
Subramaniam Kannan, Rangasamy Manivannan, Kugalur Ganesan Parthiban Kakkatummal Nishad and Natesan Senthil Kumar
Abstract
:: The objective of the present study was to develop “once daily” sustained release tablets of Aceclofenac (200mg) by wet granulation using hydrophilic polymer like Hydroxy propyl methyl cellulose K -100. The drug excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical studies, in- vitro drug release, kinetic studies and stability studies. FTIR studies shown there was no interaction between drug and polymer. The physicochemical properties of tablets were found within the limits. Aceclofenac is a non steroidal anti-inflammatory agent used in symptomatic treatment of rheumatoid arthritis, osteoarthritis and spondylitis. The drug release from optimized formulations was extended for a period of 24 hrs. The kinetic treatment of selected formulation (F8) showed that the release of drug follows zero order models. The optimized formulations were subjected to stability studies for one month at 45° temperature with RH 75±5% and showed there were no significant changes in drug content, physicochemical parameters and release pattern. Results of the present study indicated the suitability of hydrophilic polymers in the preparation of matrix based sustained release formulation of Aceclofenac.

Formulation and evaluation of fast dissolving tablet of Aceclofenac30
Sudhir Bhardwaj, Vinay Jain, R.C. Jat, Ashish Mangal, Suman Jain
Abstract
: Fast disintegrating drug delivery system offers a solution for these patients having difficulty in swallowing tablets/ capsules etc. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor aqueous solubility of the drug results in variable dissolution rate and hence poor bioavailability. In the present study, an attempt had been made to prepare fast dissolving tablets of the drug using various super disintegrates sodium starch glycolate following by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, disintegration time, water absorption ratio and wetting time, in vitro dissolution studies. All the formulation showed disintegration time in range of 12.2 to 27.5 second along with rapid in vitro dissolution. It was concluded that the fast dissolving tablets of the poor soluble drug can be made by direct compression technique using selective super disintegrantes showing enhanced dissolution, taste masking and hence better patient compliance and effective therapy.

Preparation and evaluation of aceclofenac sustained release formulation and comparison of formulated and marketed product31
Santanu Ghosh and B. B. Barik
Abstract:
The objective of the study was to develop matrix tablets for oral controlled release of aceclofenac. Matrix tablets of aceclofenac, using various viscosity of hydrophilic polymer HPMC in two different proportions, hydrophobic polymer ethyl cellulose and Guar gum were prepared by wet granulation method and subjected to in vitro drug release studies. The drug release from all HPMC matrix tablets followed various release kinetics, formulation no -F7 followed higuchi kinetics. Furthermore, the results of the in vitro studies in pH 7.5 phosphate buffer medium showed that F7 tablets provided controlled release comparable with market sustained release formulation (Aeroff-SR tablets). F7 tablets showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40°C with 75% RH for 6 months. Based on the results of the in vitro studies, it was concluded that the HPMC matrix tablets provided oral controlled release of aceclofenac.

Formulation and evaluation of once-daily sustained release Aceclofenac Prosophis juliflora gum matrix tablets32
Hindustan Abdul Ahad, Chitta Suresh Kumar, Pilli Yesupadam, Harika B, Deepika D, Leela Lakshmi V, Chandra Sekhar A
Abstract
: The main aim of the present investigation was to develop matrix tablets of Aceclofenac with Prosophis juliflora gum andto study its functionality as a matrix forming agent for once daily sustained release tablet formulations. Physicochemicalproperties of dried powdered Prosophis juliflora gum were studied. Various formulations of Aceclofenac Prosophisjuliflora gum were prepared. The formulated tablets found to have better uniformity of weight and drug content with lowSD values. The swelling behavior and release rate characteristics were studied. The dissolution study proved that the driedProsophis juliflora gum can be used as a matrix forming material for making once daily Sustained release matrix tablets.

Development of colon specific drug delivery of Aceclofenac by using effective binder system of Ethyl Acetate Cellulose33
Raosaheb S. Shendge , Fatima J. Sayyad , Kishor S.Salunnkhe and D.Bhalke
Abstract

Colon targeted drug delivery system by using dextrin, polysaccharide, as a carrier for Aceclofenac is the objective of the present study. Very common wet granulation technique is used for preparation of matrix tablet. Different binder like ethyl cellulose, sodium CMC and sucrose were used during preparation of matrix tablets containing dextrin and various excipients. Evaluation was done by different IPQC tests, content uniformity and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Drug release profile in simulated gastric, intestinal fluid and colonic fluid decide the best formulation. The matrix tablet containing binder system of ethyl cellulose and dextrin as a carrier was found to be suitable for targeting the colon as compare to other matrix tablets containing different binders because of fewer amounts (8-10%) of drug release in the simulated gastric and intestinal fluid. Matrix tablets containing dextrin releases 82.43 % of Aceclofenac in simulated colonic fluid with 4 % human fecal matter solution. No change was found in physical appearance and dissolution profile upon storage at 400C / 75 % relative humidity for six months with the tablets containing dextrin polysaccharide as a carrier. Ethyl cellulose as binder was most suitable binder to deliver the drug specifically in colonic region as compare to matrix tablets of dextrin with other binder systems.

Simultaneous estimation of aceclofenac, tramadol hydrochloride and paracetamol by UV spectrophotometric simultaneous equation method from tablet formulation34
Deepali Gharge, Pandurang Dhabale.
Abstract
: A simple, accurate, precise and economical procedure for simultaneous estimation of aceclofenac, tramadol hydrochloride and paracetamol in three component tablet dosage form has been developed utilizing concept of internal standard addition. The method is based upon determination of aceclofenac at 275.5nm, tramadol hydrochloride at 271.0 nm and paracetamol at 247.0 nm in methanol diluted with distilled water. Aceclofenac, tramadol hydrochloride and paracetamol at their respective ëmax 275.5nm, 271.0 nm and 247.0 nm shows linearity in the concentration range of 5- 25 ìg/ml, 20-100 ìg/ml and 3-15 ìg/ml respectively. The method was validated statistically. Recovery study was performed to confirm the accuracy of the method.]

Studies on Aceclofenac solid dispersion in corporated gels : Development , Characterisation and Invitro Evaluation35
Aejaz A , Azmail K , Sanaullah S , Mohsin A
Abstract
: Aceclofenac, an analgesic and anti inflammatory drug is used in treatment of osteo arthritis, rheumatoid arthritis and ankylosing spondylitis. Various compositions of Aceclofenac solid dispersions were prepared by physical mixing, fusion and solvent evaporation methods using. PVP, PEG 6000, mannitol and urea as carrier to enhance the solubility of drug. The formulations evaluated for drug content, invitro dissolution study and also characterized by IR and DSC studies. There is no interaction between drug and carrier. The general trend indicated that there was a increase in invitro drug release for solid dispersion prepared in the following order Urea > PEG 6000 > PVP > Mannitol. Based on invtiro drug release pattern, 1:3 drug carrier ratio was selected as ideal dispersion for gels. HPMC selected as ideal gel base for preparation of gels and dispersions are incorporated to gel bases by trituration. Formulations were characterized for rheological studies, drug content estimation and invitro diffusion study, IR spectro scopy. All these properties were found to be ideal. The in vitro release of Aceclofenac solid dispersion incorporated gel is significantly improved when compared to pure drug in corporated gel.

RP-HPLC method for determination of Aceclofenac, Chlorzoxazone and Paracetamol in bulk and pharmaceutical formulation36
H. Yadav,L. P. Kothapalli , A. N. Barhate, H. I. Pawar, C.R.Pawar .
Abstract
: A reverse phase high performance liquid chromatographic method (HPLC) has been developed for the simultaneous estimation of Aceclofenac (ACE), Chlorzoxazone (CHZ) and Paracetamol (PARA) in the pharmaceutical formulation using RP-C8 column. The mobile phase (Acetonitrile and Double distilled water) was pumped at a flow rate of 1 ml/min in the ratio of 60:40 and the eluents were monitored at 230.0 nm. Linearity was obtained in the concentration range of 1-60 μg/ml for ACE, 1-50 μg/ml for both PARA and CHZ. The method was statistically validated and RSD was found to be less than 2% indicating high degree of accuracy and precision of the proposed HPLC method. Due to its simplicity, rapidness, high precision and accuracy, the proposed HPLC method may be used for determining Aceclofenac, Chlorzoxazone and Paracetamol in bulk drug samples or in pharmaceutical dosage form.

PROFILES

Drug Profile

ACECLOFENAC37
Aceclofenac is an orally administered phenyl acetic acid derivatives with effects on a variety of inflammatory mediators.


CAS Registry Number: 89796-99-6

Molecular Weight:354.2

Molecular Formula :C16H13Cl2NO4

Melting Point :149-153 ° C

Chemical Name :  2-[[2-[2-[(2, 6-dichlorophenyl) amino] phenyl] acetyl] oxy] acetic acid.

Content:  Aceclofenac contains not less than 99.0% and not more than the equivalent of 101.0 percent of  C16H13Cl2NO4 calculated on the dried basis.

Description:It is a white or almost white crystalline powder.

Solubility:Practically insoluble in water, Freely soluble in acetone, Soluble in alcohol(95%) .

Storage:Stored in air tight container protected from light at room temperature not exceeding 300c.

Therapeutic-Category:Anti-inflammatory; analgesic.

pKa :4.7

Specifications:

Loss on drying

≤0.5%

Heavy metals

≤10ppm

Sulphated ash

≤0.1%

Related substances(HPLC)

Single impurity ≤0.2% 
Total impurity ≤0.5%

Assay

99.0%-101.0%

It is an effective analgesic and anti-inflammatory agent with a good tolerability profile. Through its analgesic and anti-inflammatory properties, aceclofenac provides symptomatic relief in a variety of painful conditions. A reduction in the stimulated generation of reactive oxygen species (O2), which may play a role in joint damage, was observed after 15 days in these patients, but after 180 days. At day 180, O2 release was similar to that seen in a group of 41 healthy untreated individuals.

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