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. What meloxicam tablets look like and contents of the pack meloxicam 7. 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. 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. Formulation and dissolution properties of meloxicam solid. Solubility is the important parameter to design a dosage form. Research article formulation and in vitro evaluation of fast. Meloxicam solid dispersion incorporated buccal patches were prepared and.
It is practically insoluble in water leading to poor dissolution, variations in bioavailability and gastric irritation on oral administration. 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. The high drug content values indicated the suitability of the technique. 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. In order to modulate its gastric side effect and to increase aqueous solubility, physical mixture and solid dispersion of the drug. Pdf kneading technique for preparation of binary solid. Surface solid dispersion and solid dispersion of meloxicam ncbi. Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of meloxicam with enhanced dissolution property and storage stability. Studies on solubility of meloxicam by solid dispersion method. Client information sheet for meloxidyl meloxicam 1. 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. 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. Solubility is a critical determinant of oral bioavailability of poorly watersoluble drugs such as meloxicam 1,2. Solidstate characterization and dissolution properties of.
Enhancement of solubility and dissolution of glipizide by solid dispersion kneading technique. The drug can be dispersed molecularly, in amorphous particles clusters or in crystalline particles by. Application of a solid dispersion system is one of the methods used to increase the bioavailability of poorly watersoluble drugs. Materials and methods meloxicam was supplied as gift sample from unimark pharmaceuticals ltd. This work illustrates the potential of freezedrying for obtaining pharmaceutical cocrystals when the solubilities of individual components differ drastically. Meloxicam is almost completely metabolized to four pharmacologically inactive metabolites. 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. The analgesic, antiinflammatory and ulcerogenic effects were assessed for physical mixture and solid dispersion in comparison with meloxicam alone.
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. Solubility behavior of a drug is one of the key determinants of its oral bioavailability. Pharmacokinetic profiling and bioavailability assessment of. Preparation of a solid dispersion by a dropping methodto. Development and evaluation of meloxicam solid dispersion. Pdf on apr 29, someshwar mankar and others published formulation and evaluation of glipizide solid dispersion incorporated gel. Research article formulation and in vitro evaluation of. Solid dispersions is an efficient means of improving the dissolution rate and hence the bioavailability of a range of poorly soluble drugs. Physicochemical and pharmacokinetic characterization of. 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.
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. A sample of solid dispersion equivalent to 15 mg of meloxicam was used in each test. Investigation of drugpolymer miscibility and solubilization. The poor solubility and wettability of meloxicam leads to poor dissolution and hence showing variations in bioavailability. Meloxicam me, a nonsteroidal antiinflammatory drug that is poorly. 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. A 32 full factorial design approach was used for optimization wherein the drug, polymer ratio x 1, and the kneading time x 2. 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. 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. Meloxicam excretion is predominantly in the form of metabolites, and occurs to equal extents in the urine and feces. In this study, mlx solid dispersions mlx sds were prepared to improve the water solubility of this poorly watersoluble drug.
Physicochemical characterization and dissolution properties. Pdf preparation and evaluation of meloxicam solid dispersion by. Solid dispersion is a frequently used technique to improve the aqueous solubility of drug where one or more active ingredients is uniformly. Meloxicam solid dispersion incorporated buccal patches were prepared and evaluated for drug content, invitro diffusion, invivo release of meloxicam in rabbits and stability study. Amorphous solid dispersion of meloxicam enhanced oral. Solid dispersion technique is a promising method to improve the solubility of poorly water soluble drugs. Poor solubility of meloxicam was overcome by solid dispersion technique.
Preparation, characterization and in vitro dissolution studies of. Factorially designed dosage form for geriatric population article pdf available in acta pharmaceutica 581. 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. 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. Nanocrystalline cellulose as a novel tablet excipient for. Preparation and physicochemical characterization of meloxicam. 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. Material may be irritating to the mucous membranes and upper respiratory tract. Mxtablets were prepared by direct compression of different coground sds or physical mixtures. Preparation and physicochemical characterization of.
The solid binary systems were prepared at various drug concentrations5. A meloxicam mlx solid dispersion was prepared via the solvent evaporation method with polyvinylpyrrolidone pvp k30. 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. Boxes containing 2 blister packs of 10 tablets each, boxes containing 3 blister packs of 10 tablets each. 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. The methods for characterization were scanning electron microscopy sem, differential scanning calorimetry dsc, and powder xray diffraction. Crospovidone cpv, a hydrophilic carrier was selected for ssd preparation on the basis of 89% in vitro mlx adsorption, 19%. Solid dispersions prepared with various carriers by solvent evaporation, fusion and. 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. Mantralayam road, navodaya nagar development revised on.
Meloxicam is a non steroidal antiinflammatory drug, used in the treatment of rheumatoid arthritis and oestoarthritis. Samples of dissolution fluid were withdrawn through a filter 0. Mlx is practically insoluble in water and exhibits a slow onset of action. This study aimed to develop an amorphous solid dispersion asd of mel to achieve rapid oral absorption in severe pain patients. Surface solid dispersion and solid dispersion of meloxicam. All solid dispersion incorporated patches showed increased invitro drug release i. Amorphous solid dispersion of meloxicam enhanced oral absorption in rats with impaired gastric motility. Kneading technique for preparation of binary solid. Preparation and evaluation of meloxicam solid dispersion by melting method. The in vitro drug release pattern was determined by rotating dialysis bag method.
Kneading technique for preparation of binary solid dispersion. Nonblinded, openlabel, crossover study was performed in six healthy volunteers for the determination of pharmacokinetic parameters. Factorially designed dosage form for geriatric population. Only traces of the unchanged parent compound are excreted in the urine 0.
Solid dispersions of mel sdms were prepared by solvent evaporation method using the polymers mentioned above. Meloxicam mlx is a nonsteroidal, antiinflammatory drug that is prescribed in the treatment of rheumatoid arthritis and osteoarthritis. Pdf drug formulation as solid dispersion sd represents a good method for the enhancement in solubility of poorly water soluble drugs. The meloxicam concentration was maintained at 10% ww for blends with and without meglumine. Improving dissolution of meloxicam using solid dispersions. The present study is aimed to increase solubility and dissolution of the drug using solid dispersion techniques. Meloxicam mel shows a slow onset of action in severe pain patients on account of delayed gastric motility. 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.
Solubility studies was carried out by taking excess amount of solid dispersion in 3 ml of phosphate buffer ph 7. Pdf formulation and characterization of meloxicam solid. Meloxicam solid dispersion incorporated buccal patch msm2 containing meloxicam solid dispersion meloxicam 150mg, pvp250mg, peg6000 175mg and mixture of lactose and mcc4. Pharmacokinetic profiling and bioavailability assessment. The inactive ingredients in mobic meloxicam tablets include colloidal silicon dioxide, crospovidone, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone and sodium citrate dihydrate. Oct 28, 2009 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. In situ salt formation during melt extrusion for improved. 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. Analgesic, antiinflammatory and ulcerogenic studies of. 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. 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.
Preparation and evaluation of solid dispersion of meloxicam. Meloxicam has an apparent partition coefficient log p app 0. Meloxicam is a pastel yellow solid, practically insoluble in water, with higher solubility observed in strong acids and bases. 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. Preparation, characterization and in vitro dissolution. Secondly to develop patient friendly dosage form and evaluate it. Poor solubility of meloxicam was overcome by solid dispersion technique and the same karnataka, india. 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. Free fulltext pdf articles from hundreds of disciplines, all in one place. The kneading technique was used to prepare solid dispersions. Meloxicam solid dispersion loaded buccal patch msp1 containing of lactose and mcc4. Cryosynthesis of cocrystals of poorly watersoluble.
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