Meloxicam is almost completely metabolized to four pharmacologically inactive metabolites. Meloxicam solid dispersion incorporated buccal patches were prepared and. Meloxicam is a non steroidal antiinflammatory drug, used in the treatment of rheumatoid arthritis and oestoarthritis. A comparative study was carried out between surface solid dispersion ssd and solid dispersion sd of meloxicam mlx to assess the solubility and dissolution enhancement approach and thereafter develop as patient friendly orodispersible tablet. Pdf drug formulation as solid dispersion sd represents a good method for the enhancement in solubility of poorly water soluble drugs. Materials and methods meloxicam was supplied as gift sample from unimark pharmaceuticals ltd. This work aims to study the solubilizing capacity of solid dispersion technology with three kinds of polymers and explore the factors affecting the dissolution and stability of solid dispersions from drugpolymer miscibility, phase solubility, and crystallization inhibition. This work illustrates the potential of freezedrying for obtaining pharmaceutical cocrystals when the solubilities of individual components differ drastically. Application of a solid dispersion system is one of the methods used to increase the bioavailability of poorly watersoluble drugs. Surface solid dispersion and solid dispersion of meloxicam. The poor solubility and wettability of meloxicam leads to poor dissolution and hence showing variations in bioavailability. In situ salt formation during melt extrusion for improved. Client information sheet for meloxidyl meloxicam 1. Mantralayam road, navodaya nagar development revised on.
Preparation, characterization and in vitro dissolution studies of. Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of meloxicam with enhanced dissolution property and storage stability. Solubility studies was carried out by taking excess amount of solid dispersion in 3 ml of phosphate buffer ph 7. The purpose of this study is to understand the mechanism behind this stabilization and its impact on the performance of a meloxicamkollidon va64 amorphous solid dispersion. The solid binary systems were prepared at various drug concentrations5. The objective of the present work was to improve the dissolution properties of the poorly watersoluble drug meloxicam by preparing solid dispersions with hydroxyethyl cellulose hec, mannitol and polyethylene glycol peg 4000 and to develop a dosage form for geriatric population. Factorially designed dosage form for geriatric population. Adaptation of the dropping method from the chemical industry as a formulation procedure may help the scalingup process and simplify the formulation of poorly watersoluble compounds. Meloxicam, sold under the brand name mobic among others, is a nonsteroidal antiinflammatory drug nsaid used to treat pain and inflammation in rheumatic diseases and osteoarthritis. Solid dispersion is a frequently used technique to improve the aqueous solubility of drug where one or more active ingredients is uniformly. The inactive ingredients in mobic meloxicam tablets include colloidal silicon dioxide, crospovidone, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone and sodium citrate dihydrate. Meloxicam mel shows a slow onset of action in severe pain patients on account of delayed gastric motility. The aim of the present study was to enhance the dissolution rate of meloxicam mlx, a practically waterinsoluble drug by preparation of solid dispersion using a hydrophilic polymer, poloxamer 188 pxm. The in vitro drug release pattern was determined by rotating dialysis bag method.
Solid dispersion technique is a promising method to improve the solubility of poorly water soluble drugs. The analgesic, antiinflammatory and ulcerogenic effects were assessed for physical mixture and solid dispersion in comparison with meloxicam alone. Meloxicam is a pastel yellow solid, practically insoluble in water, with higher solubility observed in strong acids and bases. Development and evaluation of meloxicam solid dispersion. Solid dispersions of mel sdms were prepared by solvent evaporation method using the polymers mentioned above. Solubility behavior of a drug is one of the key determinants of its oral bioavailability. Mlx is practically insoluble in water and exhibits a slow onset of action. In case of solid dispersion with mannitol by hot melt method, solubility of meloxicam was lesser then the value observed in the case of solvent evaporation method. Factorially designed dosage form for geriatric population article pdf available in acta pharmaceutica 581. Solidstate characterization and dissolution properties of.
Preparation and physicochemical characterization of meloxicam. Solid dispersions is an efficient means of improving the dissolution rate and hence the bioavailability of a range of poorly soluble drugs. Preparation and evaluation of solid dispersion of meloxicam. In order to modulate its gastric side effect and to increase aqueous solubility, physical mixture and solid dispersion of the drug. Kneading technique for preparation of binary solid dispersion. Solubility is a critical determinant of oral bioavailability of poorly watersoluble drugs such as meloxicam 1,2. Meloxicam solid dispersion incorporated buccal patch msm2 containing meloxicam solid dispersion meloxicam 150mg, pvp250mg, peg6000 175mg and mixture of lactose and mcc4. Physicochemical characterization and dissolution properties. Free fulltext pdf articles from hundreds of disciplines, all in one place physicochemical and pharmacokinetic characterization of amorphous solid dispersion of meloxicam with enhanced dissolution property and storage stability pdf paperity. Pharmacokinetic profiling and bioavailability assessment of.
The rate of release of meloxicam from the fine solid dispersion of its cocrystal with succinic acid in polyethylenglycol obtained by freezedrying was significantly higher than dissolution rates of a pure meloxicam cocrystals with succinic acid obtained by different variants of freezedrying thin film freezing, tff, and spray freezedrying. Solid dispersion the term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic matrix and a hydrophobic drug. Pharmacokinetic profiling and bioavailability assessment. The objective of the present work was to improve the dissolution properties of the poorly watersoluble drug meloxicam by preparing solid dispersions with hydroxyethyl cellulose hec, mannitol. In order to modulate its gastric side effect and to increase aqueous solubility, physical mixture and solid dispersion of the drug were prepared with polyethylene glycol 6000 and polyvinyl pyrrolidine. A 32 full factorial design approach was used for optimization wherein the drug, polymer ratio x 1, and the kneading time x 2. Only traces of the unchanged parent compound are excreted in the urine 0. Pdf on apr 29, someshwar mankar and others published formulation and evaluation of glipizide solid dispersion incorporated gel. The drug can be dispersed molecularly, in amorphous particles clusters or in crystalline particles by. Poor solubility of meloxicam was overcome by solid dispersion technique. Solubility is the important parameter to design a dosage form. Nonblinded, openlabel, crossover study was performed in six healthy volunteers for the determination of pharmacokinetic parameters.
Mar 25, 2015 solid dispersion the term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic matrix and a hydrophobic drug. Amorphous solid dispersion of meloxicam enhanced oral absorption in rats with impaired gastric motility. Studies on solubility of meloxicam by solid dispersion method. Free fulltext pdf articles from hundreds of disciplines, all in one place. Analgesic, antiinflammatory and ulcerogenic studies of. Research article formulation and in vitro evaluation of fast. This study aimed to develop an amorphous solid dispersion asd of mel to achieve rapid oral absorption in severe pain patients. Secondly to develop patient friendly dosage form and evaluate it. Research article formulation and in vitro evaluation of. Dissolution profiles of meloxicam liquisolid systems f4 to f6 the percent drug content % of the meloxicam in liquisolid systems were found to be in the range of93. Meloxicam me, a nonsteroidal antiinflammatory drug that is poorly.
Poor solubility of meloxicam was overcome by solid dispersion technique and the same karnataka, india. The purpose of the current study is to characterize the solid state properties of the solid dispersion system of meloxicam in gelucire 50 prepared at different ratios using the spray drying technique. Physicochemical and pharmacokinetic characterization of. Meloxicam solid dispersion loaded buccal patch msp1 containing of lactose and mcc4.
What meloxicam tablets look like and contents of the pack meloxicam 7. This study explored the effect of nanocrystalline cellulose ncc on meloxicam mx solid dispersion sd prepared by cogrinding technique compared to microcrystalline cellulose mcc in presence of lactose. Cocrystals of a model systemmeloxicam and succinic acidcould be obtained both as a pure crystalline phase and forming a solid dispersion with a polymeric carrier. Crospovidone cpv, a hydrophilic carrier was selected for ssd preparation on the basis of 89% in vitro mlx adsorption, 19%. The kneading technique was used to prepare solid dispersions. This study concerned with preparation and invitro evaluation of fast dissolving tablets of meloxicam solid dispersion, since meloxicam is a practically insoluble in aqueous media after oral administration and the rate of absorption is often controlled by the rate of dissolution. Mxtablets were prepared by direct compression of different coground sds or physical mixtures. Cryosynthesis of cocrystals of poorly watersoluble.
Preparation, characterization and in vitro dissolution. Improving dissolution of meloxicam using solid dispersions. Preparation and evaluation of meloxicam solid dispersion by melting method. Investigation of drugpolymer miscibility and solubilization. Meloxicam excretion is predominantly in the form of metabolites, and occurs to equal extents in the urine and feces. Enhancement of solubility and dissolution of glipizide by solid dispersion kneading technique. Boxes containing 2 blister packs of 10 tablets each, boxes containing 3 blister packs of 10 tablets each.
Amorphous solid dispersion of meloxicam enhanced oral. Pdf preparation and evaluation of meloxicam solid dispersion by. Improving dissolution of meloxicam using solid dispersions article pdf available in iranian journal of pharmaceutical research ijpr 4 january 2006 with 366 reads how we measure reads. Preparation of a solid dispersion by a dropping methodto. Material may be irritating to the mucous membranes and upper respiratory tract.
Pdf kneading technique for preparation of binary solid. Crospovidone cpv, a hydrophilic carrier was selected for ssd preparation on. Meloxicam is bcs class ii low soluble, and high permeable drug increasing the dissolution properties of the poorly watersoluble drug meloxicam using a solid dispersion method solvent. A sample of solid dispersion equivalent to 15 mg of meloxicam was used in each test. Preparation and physicochemical characterization of. All solid dispersion incorporated patches showed increased invitro drug release i. Preparation and physicochemical characterization of meloxicam orally fast disintegration tablet using its solid dispersion zahra shoormeij1, azade taheri 1, alireza homayouni 1 1 novel drug delivery systems research center, department of pharmaceutics, faculty of pharmacy, isfahan university of medical sciences, isfahan, iran. In this study, mlx solid dispersions mlx sds were prepared to improve the water solubility of this poorly watersoluble drug. The methods for characterization were scanning electron microscopy sem, differential scanning calorimetry dsc, and powder xray diffraction. The present study is aimed to increase solubility and dissolution of the drug using solid dispersion techniques. Meloxicam mlx is a nonsteroidal, antiinflammatory drug that is prescribed in the treatment of rheumatoid arthritis and osteoarthritis. The present investigation was focused on the comparative bioavailability assessment of meloxicam tablet prepared using modified gum karaya solid dispersion and commercial tablets of meloxicam.
Various techniques such as size reduction, use of cosolvent and surfactants, inclusion complex formation, microparticles, salt formation, prodrug, and solid dispersion are employed for increasing the solubility of the drugs of which the technique of solid. Nanocrystalline cellulose as a novel tablet excipient for. The meloxicam concentration was maintained at 10% ww for blends with and without meglumine. Surface solid dispersion and solid dispersion of meloxicam ncbi. In this present study deals with the enhancement of solubility of poorly water soluble drug meloxicam the liquisolid system is a novel technique for solubility enhancement and dissolution improvement of low soluble drugs. The purpose of the current study is to characterize the solidstate properties of the solid dispersion system of meloxicam in gelucire 50 prepared at different ratios using the spray drying technique. The high drug content values indicated the suitability of the technique. Preparation and evaluation of solid dispersion of meloxicam with skimmed milk sengodan gurusamy vijaya kumar anddinanathmishra department of pharmaceutical sciences, guru jambheshwar university, hisar 125001, haryana, india received september 26, 2005. Meloxicam has an apparent partition coefficient log p app 0. Drug formulation as solid dispersion sd represents a good method for the enhancement in solubility of poorly water soluble drugs, as well as for the reduction of.
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