It showed that the drug was stable in solid dispersion. Preparation characterization and evaluation of solid. A1 1 department of pharmaceutics, luqman college of pharmacy, gulbarga. The dissolution rate of the drug was affected by nature and amount of polymer used. Solid dispersion of aceclofenac was tried with peg6000, beta cyclodextrin, gelatin hydrolysate, sls and croscarmellose. Solid dispersion is a unique approach which was introduced by sekiguchi and obi. Drug and carriers physical mixture prepared by lightly grinding drug aceclofenac and carriers in mortar for 2 min at the required drug carrier level 1. Solid dispersion of drug aceclofenac nsaid was prepared by using different polymers i. The solution lies in preparing solid dispersion of aceclofenac with several hydrophilic polymers to increase its aqueous solubility and dissolution 2. In vivo studies indicate that optimized ternary solid dispersion provides rapid pharmacological responses in mice and rats compared to marketed formulation. Dissolution enhancement of aceclofenac tablet by solid.
It is concluded that solubility of the aceclofenac was improved by solid dispersion with pvp k30. Cyclodextrin, in situ absorption, polyvinyl pyrrolidone. Solid dispersion technology is the science of diffusing one or even more principal components in a solid state in an inert matrix to obtain enhanced dissolution or constant discharge of drugs, modified solid state properties as well as increased stability leonardi et al. Formulation of solid dispersion solid dispersion of aceclofenac was prepared by using four carriers. Enhancement of dissolution rate of aceclofenac by solid. A solid dispersion generally composed of two components the drug and the polymer matrix. In vitro dissolution rate of aceclofenac from solid dispersion sd was significantly higher compared to pure aceclofenac. To improve its solubility, we try to prepare solid dispersions. Solid dispersion technology was spread on several watch glasses in thin layers for. Pdf solubility enhancement of aceclofenac by solid dispersion. The aim of the study was to improve the dissolution rate of poorly watersoluble drug aceclofenac bcsclass ii, using avicel 200 and sylysia 350 as carriers by surface solid dispersion technique ssd. A comparative study of solubility enhancement of aceclofenac by. Wetting and dispersion properties of phospholipids an amphiphilic surfactant increased the solubility of the drug and hence improved the dissolution profile of the complex.
In order to minimize the gastrointestinal side e ects and to attain controlled release delivery of the drug, the development. Enhancement of dissolution rate of etoricoxib through solid. Solid dispersions was studied using disso 2000, lab india 8station dissolution rate test apparatus with a paddle stirrer. Development of aceclofenac mouth dissolving tablets using. Introduction a method is reported for studying gastro intestinal drug absorption from isolated gut segments of the anesthetized rat in situ. Formulation and evaluation of aceclofenac solid dispersion. Effect of excipients on dissolution enhancement of. Therefore, solid dispersions sds of aceclofenac were prepared using lactose, mannitol and urea to increase its aqueous solubility.
Dissolution of drug increased by the solid dispersion and hence solubility was also increased. It was observed that the dissolution rate of drug from solid dispersions increases with the increase in lactose amount in comparison to corn starch with the optimum ratio of 1. Hence, solid dispersion technique can be sucessfully used for the improvement of the dissolution profile of aceclofenac. Solid dispersion was prepared by using different concentration of urea as a carrier and solid. Solid dispersions containing poloxamer 407 and peg 6000 showed higher dissolution rates compared with aceclofenac alone. Equilibrium solubility data of aceclofenac and solubility enhancement ratio in urea solution of varying concentrations f. Enhancement of solubility of aceclofenac by using different. Solid dispersions of aceclofenac were prepared with c arriers urea and mannitol in in1. Materials and methods aceclofenac was obtained as a gift sample from yarrow chem products batch no12031216v, mumbai, india. Reduction of the particle size of the incorporated drug 2. In conclusion, the dissolution of aceclofenac can be enhanced by the use of hydrophilic carrier like pvp. Preparation of solid dispersion it was attempted to improve the aqueous solubility of ace by solid dispersion technique. Dissolution enhancement was due to decrease in crystallinity of drug and solubilizing effect of the carrier from the solid dispersion of the aceclofenac.
The dissolution rate of aceclofenac avicel 200 solid dispersion 1. Optimization of aceclofenac solid dispersion using boxbehnken design. Dissolution rate enhancement of aceclofenac by solid. In vitro dissolution of pure drug, physical mixtures and solid dispersions were carried out. Triethanolamine was also used to prepare aceclofenac salt to improve the solubility 19. Optimization of aceclofenac solid dispersion using box. Solid dispersion of aceclofenac and mannitol was prepared by physical mixture, melting method and melt solvent method by different ratios 1. Dissolution enhancement of aceclofenac tablet by solid dispersion technique.
The study was carried out to enhance the dissolution rate of poorly water soluble drug aceclofenac bcsii, by solid dispersion technique using different carrier and super disintegrant by kneading method. Formulation and enhancement of dissolution rate of poorly. Sodium lauryl sulphate was added to the dissolution fluid to maintain sink. Present study was carried out to enhace the dissolution rate of poorly water soluble drug aceclofenac bcs ii, by solid dispersion technique using different. The results of sem, dsc and xrd demonstrated that aceclofenac is amorphous in solid dispersion. Formulation design involving different aceclofenac loaded solid dispersions. Pdf the aim of the study was to improve the solubility of aceclofenac, which is poorly water soluble drug belongs to bcs classii. Download as pdf about authors bhumika kumar department of pharmaceutics, delhi pharmaceutical sciences and research university, new delhi, india abstract solid dispersion is an effective way of improving the dissolution rate of poorly water soluble drugs and hence its bioavailability. Solid dispersions were prepared by solvent wetting method using 32 full factorial design for each of the carrier. The increase tendency of dissolution rate of the drug may be due. International journal of research pharmaceutical and nano. Pdf the aim of this study was to prepare and characterize solid dispersions of aceclofenac, employing a mixed excipient system composed of lactose. Effect of lyophilization and polymer compositions on.
Preparation of different formulation series of aceclofenac by solid dispersion method it has discovered that 510 % ww of fluid compound could be consolidated in peg 6000 without huge loss of its strong properties. In conclusion, the dissolution of aceclofenac can be. Solid dispersion of aceclofenac with all four carriers urea, mannitol, pvp and pvpva64 showed considerable increase in the dissolution rate in comparison with physical mixture and pure drug in 0. Solid dispersion technique has been used for a wide variety of poorly aqueous soluble drugs such as nimesulide, ketoprofen, tenoxicam, nifedipine, aceclofenac, valdecoxib using various hydrophilic carriers like polyethylene glycol, polyvinylpyrrolidone. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally.
The solid dissolution is a complex process which is affected by various factorslike the particle size, crystal habit, surface area, surface energies and wettability. Dissolution enhancement of aceclofenac tablet by solid dispersion. The dissolution behavior of solid dispersions was compared with pure acf api and airtal deawoong, co, korea as control groups in simulated phosphate buffer at ph 6. It was found that the aceclofenac croscarmellose complex has given the. In vitro solubility of pure drug and solid dispersions were carried out. Solid dispersion technique was successfully used to enhance the dissolution of poorly aqueous soluble drugs aceclofenac. Prepared aceclofenac solid dispersions were evaluated for physical appearance, drug content uniformity, and in vitro dissolution studies. It also depends on the proportion and properties of the polymer carrier used in the composition of solid dispersion 8. In order to enhance the bioavailability it is necessary. Preparation, characterization and in vitro evaluation of.
Preparation and comparison of dissolution profiles of. Pdf improvement of dissolution rate of aceclofenac by. Polaxomer 188, pvp k30, peg 6000, in different ratios 1. Eight different formulations were designed by the varying carrier and the drug. With a view to develop fast release formulation of aceclofenac and hence improve its dissolution characteristics. Dissolution, bioavailability, solid dispersion, physical mixture, solvent wetting, aceclofenac.
Sodium lauryl sulphate was added to the dissolution fluid to maintain sink condition. Aceclofenac, solid dispersion, lactose, mannitol, urea. Pdf dissolution enhancement of aceclofenac tablet by solid. It is very slightly soluble in water and hence orally administered drug is less bioavailable. Jun 17, 2019 ranitidine can be found in many pharmaceutical firms such as tablets, injectable solutions and oral dissolution enhancement of aceclofenac tablet by solid dispersion technique. Pdf improvement of dissolution rate of aceclofenac by solid. In solid dispersion method, the drug is dispersed in. Batch p2 preparation of solid dispersion by solvent evaporation method. The dissolution was determined by usp xxiii apparatus using phosphate buffer ph 7. Solid dispersion technique for improving solubility of. The in vitro dissolution behaviour of the prepared solid dispersion by different methods was compared with those of pure drug.
Rjpt solubility enhancement of aceclofenac by hot melt. Numerous methods are existing to prepare the solid dispersions such as melting method, solvent evaporation method, fusion method, kneading method. Pulla reddy college of pharmacy, mehdipatnam, hyderabad. Solid dispersion technique for improving solubility of some. Aceclofenac is an effective nsaids is practically insoluble in water. The term solid dispersion refers to the dispersion of one or more active ingredient in an inert carrier or matrix at solid state prepared by melting fusion, solvent, or the melting solvent method. Suggested that the drug was present in a eutectic mixture in a microcrystalline. Surface solid dispersion ssd was prepared by kneading method using.
It is concluded that the solubility of aceclofenac increases synergistically by mixed hydrotropy. Solid dispersion definition a solid dispersion can be defined as the dispersion of one or more active ingredients in an inert carrier matrix in a solid state prepared by a melting fusion, solvent evaporation, etc. A nonsteroidal antiinflammatory drug related to diclofenac, it is used in the management of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. The water soluble carriers used in preparation of solid dispersion enhance the. Introduction aceclofenac is an orally effective nonsteroidal anti. International journal of biopharmaceutics formulation.
Pdf dissolution enhancement of aceclofenac tablet by. Solid dispersion definition a solid dispersion can be defined as the dispersion of one or more active ingredients in an inert carrier matrix in a solidstate prepared by a melting fusion, solvent evaporation, etc. The aim of present study was to enhance the dissolution rate of poorly watersoluble drug aceclofenac by solid dispersion technique using corn starch, dicalcium phosphate, lactose, and microcrystalline cellulose as carriers. The carriers are melted at elevated temperatures and the drugs are dissolved in molten carriers. Mechanism of action of sds to improve aqueous solubility 1. Formulation and characterization of aceclofenacloaded. Peg 6000 was used as carrier for preparation of solid dispersion with aceclofenac due to their characteristics i. Characterization of aceclofenac solid dispersion was performed by sem, dsc, xrd and ftir. The powder equivalent to 100 mg of aceclofenac was weighed and filled in the capsule by hand filling method. Aceclofenac binary solid dispersions sd with different drug loadings were prepared using the melting or fusion method. Solid dispersion of aceclofenac with all four carriers urea, mannitol, pvp and pvpva64 showed considerable increase in the. The present study is aimed at improving the dissolution of poorly watersoluble drug, aceclofenac.
Solid dispersion sd of ace was prepared by solvent evaporation method using peg 6000 as carrier. Ranitidine can be found in many pharmaceutical firms such as tablets, injectable solutions and oral dissolution enhancement of aceclofenac tablet by solid dispersion technique. Solid dispersion technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage in order to achieve increased dissolution rate, sustained release of drugs, altered solid state properties, and enhanced release of drugs from ointment and suppository bases, and improved solubility and stability 7. The stability study during 6 months confirms that aceclofenac exhibits high stability in solid dispersion. Solid dispersion of aceclofenac with pvp showed considerable increase in the solubility in. Formulation and evaluation of solid dispersions of aceclofenac. Improvement of dissolution rate of aceclofenac by solid. Pdf dissolution rate enhancement of aceclofenac by solid. Pdf solubility enhancement of aceclofenac by solid.
Preparation of solid dispersion solid dispersions are prepared using aceclofenac as a drug and various carriers like pvp, peg6000, crosscarmellose and urea. Aceclofenac, solid dispersions, croscarmellose sodium, wistar rats, immunosuppression. Development and evaluation of pharmacosomes of aceclofenac. Aceclofenac is a monocarboxylic acid that is the carboxymethyl ester of diclofenac. The aim of the present study was to improve the solubility of aceclofenac ace by solid dispersion sd technique and formulate it as mouth dissolving tablets using some superdisintegrants. Introduction oral bioavailability of a drug depends on its solubility andor dissolution rate, therefore efforts to increase dissolution of drugs with limited water solubility is often needed. African journal of pharmacy and pharmacology formulation. Formulation and evaluation of aceclofenac solid dispersion for improving the solubility and dissolution rate.
Articulo original preparation, characterization and in vitro. Solubility enhancement of aceclofenac by solid dispersion naseeb basha shaik 1, manasa toleti 1, divija kanaru 1 and latha kukati 1 1. Solid dispersion tablet showed a percentage drug release of 84% in 50min as compared to that of the 67% in 50 min of the marketed conventional formulation. Enhancement of dissolution rate of etoricoxib through.
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