Investigation of solid dispersion technique in improvement of. Preparation of solid dispersions, and determination of drug content and percent yieldibuprofen. Sustainedrelease solid dispersions of ibuprofen prepared. Here we focus on solubility parameters as a tool for predicting the solubility of a drug in certain carriers. Effect of water soluble polymers on dissolution enhancement of ibuprofen solid dispersion prepared by fusion method. Preparation, characterization and in vivo evaluation of. The aim of this study was to prepare and evaluate ibuprofen ibu solid dispersion tablets with improved dissolution and less sticking using porous calcium silicate pcs. Ternary solid dispersions were prepared by hotmelt granulation in which the drug, ibuprofen was dispersed in a molten dispersion carrier and coated onto an adsorbent. Litster2, ivan marziano3 1 school of chemical of engineering, the university of queensland. The release characteristics were determined as a function of the solvent used, carriertodrug ratio, surfaceactive agents incorporated such as sodium lauryl sulphate sls, cetrimide and sorbitan monopalmitate span 60 and the ph of the dissolution medium. The solid dispersions of ibuprofenstearic acid and ibuprofenhydrogenated castor oil showed the best flow characteristics compared with pure ibuprofen. Precisely, sustained release solid dispersions containing different drugtopolymer ratios were developed by means of microwave technology using ibuprofen ibu as a model drug and glyceryl monostarate imwitor 900, gm as a lipophilic sustained release agent. In this study solid dispersions sds of ibuprofen were prepared by melt dispersion technique using macrogol 4000 and macrogol 6000 as carrier.
Abstract ibuprofen is a nonsteroidal antiinflammatory drug with poor water solubility. A tablet of the invention, for examples, provides a high level of ibuprofen for a given size. Crystallization kinetics of ibuprofen from ethanol and. Comparison of in vitro dissolution tests for commercially.
The solid dispersion showing better release profile was chosen to formulate into a tablet dosage form of weight 600 mg. Preparation and evaluation of immediate release ibuprofen. When the earlier sample was completely dissolved, another 5g ibuprofen was added and the procedure was repeated until any undissolved ibuprofen was visible. Enteric coating of ibuprofen tablets 200 mg using an. Physical mixtures pms of ibuprofen were also prepared with the same carrier and in the same drugcarrier ratio 1. To improve its dissolution, ibuprofen solid dispersions sds were prepared, characterized by scanning electron microscopy sem, differential scanning calorimetry dsc, and fourier transform infrared spectroscopy ftir, and evaluated for solubility, and invitro ibuprofen release. Solid dispersions of ibuprofen were prepared by using peg 20000 and poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Drugpolymer complex was prepared using batch method. Preparation, characterization, and dissolution studies of ibuprofen solid dispersions using polyethylene glycol peg, talc, and pegtalc as dispersion carriers. Ibuprofen was the first member of propionic acid derivatives to be introduced in 1969 as a better alternative to aspirin.
In vivoin vitro evaluation of solid dispersion containing ibuprofen sachin k. Applying supercritical fluid technology to prepare ibuprofen solid dispersions with. Investigation of solid dispersion technique in improvement. The purpose of this study was to improve the dissolution rate and antiinflammatory effect of ibuprofen by a solid dispersion sd method. In present study the attempts have been made to increase the dissolution of bcs class ii drug ibuprofen using hydrophilic polymers namely polyethylene glycol peg 6000 and polyvinyl pyrrolidone pvp k30 by microwave induced solid dispersion and conventional fusion method.
Study of binary and ternary solid dispersion of ibuprofen. An overview of clinical pharmacology of ibuprofen rabia bushra1 and nousheen aslam2 introduction i buprofen is 2rs142methyl propyl phenyl propionic acid bp. Pdf effect of water soluble polymers on dissolution. The solid dispersion of ibuprofen in cetyl alcohol sd ca did not show flowability. Crystallization kinetics of ibuprofen from ethanol and aqueous ethanol abdur rashid1, edward t. Solubility enhancement of nimesulide and ibuprofen by solid dispersion technique. Improved dissolution and antiinflammatory activity of ibuprofen. As can be seen, solid dispersions of ibuprofen in hydrogenated castor oil and stearic acid presented a higher percentage of particles with average size higher than m. Solidstate characterization of the dispersions was conducted by differential scanning calorimetry dsc, powder xray diffraction pxrd, and scanning electron microscopy sem. The solid dispersion of ibuprofen in cethyl alcohol showed a higher percentage of particles between 500 and m. To develop an ibuprofen transdermal gel with a capability for both topical and systemic. Thermosensitive in situ gel based on solid dispersion for rectal. Ibuprofen solid dispersions were prepared by the solvent and fusionsolvent methods using polyethylene glycol peg, polyvinylpyrrolidone pvp, eudragit rs.
Preparation and evaluation of solid dispersions of. Solubilization of ibuprofen for freeze dried parenteral. Solid dispersions of ibuprofen with various phospholipids were prepared, and the effect of phospholipids on the in vitro dissolution and in vivo gastrointestinal toxicity of ibuprofen was evaluated. Preparation, characterization and dissolution of solid. Higher drug dissolution rates from a sd can be facilitated by optimizing the wetting characteristics of the. Design, development and evaluation of immediate release. Filter the mixture, and evaporate the filtrate with the aid of a stream of nitrogen to dryness. Pdf dissolution profile of ibuprofen solid dispersion. The binary mixtures of ibuprofen and magnesium aluminometasilicate were prepared by blending both substances in a mortar at room temperature for 5 min.
Investigation of solid dispersion technique in improvement of physicochemical characteristics of ibuprofen powder mohammad ali dabbagh, behzad taghipour department of pharmaceutics, school of pharmacy, jundishapour university of medical sciences, ahwaz, iran abstract ibuprofen solid dispersions were prepared by the solvent and fusionsolvent. Preparation and evaluation of ibuprofen solid dispersion. The paper is devoted to the investigation of microwave irradiation mw for the preparation of solvent free solid dispersion sd. In this study, supercritical fluid scf technology was applied to prepare reliable solid dispersions of pharmaceutical compounds with limited bioavailability using ibuprofen ibu as a model compound.
Dispersion of ibuprofen in sorbitol showed maximum enhancement of solubility up to 75%. By means of thermal analysis, we have demonstrated the total immiscibility, in solid state, of the corresponding binary mixtures. Preparation of ibuprofen solid dispersion by melting method ibuprofen. From the results, it was clear that solid dispersion formulation showed improved dissolution rate than pure drug and physical mixture.
Applying supercritical fluid technology to prepare. The most notable problem by these dispersions is drugcarrier insolubility. Determination of solubility parameters of ibuprofen and. Interactionstability of the drug with carriers in solid dispersions was tested by uv scanning, tlc and infrared analysis. Development and evaluation of ibuprofen transdermal gel. A pharmaceutical granulate composition which comprises, by weight thereof, 85 to 99% by weight ibuprofen and 1 to 15% by weight croscarmellose sodium. Solubility enhancement of nimesulide and ibuprofen by solid dispersion technique article in indian journal of pharmaceutical sciences 646. Solubility enhancement of nimesulide and ibuprofen by.
Pharmaceutics free fulltext applying supercritical. In vivo in vitro evaluation of solid dispersion containing. Solid dispersion granules were prepared using waterbased solid dispersion and waterretained pcs with the wet granulation method and a highspeed agitation granulator. Dissolution profile of ibuprofen solid dispersion prepared with cellulosic polymers and sugar by fusion method. This drug presents, in the pure state, poor physical and. In recent years there has been a growing interest in formulating solid dispersions, which purposes mainly include solubility enhancement, sustained drug release and taste masking. Biyani anuradha college of pharmacy, chikhli, 443201. In addition, many of theses systems are provided as liquid dispersions, which can be problematic when handling, transporting and controlling storage conditions cunningham, fegley, 2001. Ibuprofen is a nonsteroidal anti inflammatory drug nsaid with analgesic, antipyretic, and. Initial screening was developed based on drug solubility in carriers in the liquid state to select a suitable watersoluble carrier system for. Development and evaluation of ibuprofen transdermal gel formulations bazigha k abdul rasool 1, eman f abugharbieh 1, sahar a fahmy 2, heyam s saad 1 and saeed a khan 1 1dubai pharmacy college, dubai, uae, 2helwan university, helwan, egypt abstract purpose. Comparative study of sustainedrelease lipid microparticles and. This work examines the release of ibuprofen from various molecular weight fractions of polyvinylpyrrolidone pvp solid dispersions. Pdf ddw103 development of a rapid dissolving ibuprofen.
The known excess samples ibuprofen solid dispersions, physical mixtures and pure ibuprofen, 0. Solid dispersions of ibuprofen prepared by the freeze drying method provided the highest dissolution rate and per centage of drug dissolved. On the other hand, the solid dispersion of ibuprofen in stearic acid sd sa showed a flowability of 6. Prolonged release of ibuprofen was achieved with the lipid microparticles and solid dispersions prepared with the different types of excipients. Solid dispersions sds are resulted by dispersion of drug in biologically inert matrix.
Ibuprofen ibu, a poorly watersoluble drug, is widely used as one of the besttolerated nonsteroidal antiin. They can be used to increase the solubility of a drug with low aqueous solubility, thereby improving its oral bioavailability. Evaluation of solid dispersed particles for formulation of oral. Thermosensitive in situ gel based on solid dispersion for rectal delivery of ibuprofen. Characteristics of the in vitro release of ibuprofen from.
Methods and polymers to increase the solubility of poorly soluble drugs ladan 1akbarpour nikghalb, gurinder singh2, gaurav singh2 and kimia fazaeli kahkeshan1 1gautam college of pharmacy, bangalore, karnataka, india. Read physicochemical stability of solid dispersions of enantiomeric or racemic ibuprofen in stearic acid, journal of pharmaceutical science on deepdyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips. The aim of the present work was to prepare solid dispersion of ibuprofen with peg 6000 to increase the aqueous solubility of the drug and to develop the solid dispersed ibuprofen into. Saquib hasnain, amit kumar nayak 120 tives of this investigation are. Pdf enteric coating of ibuprofen tablets 200 mg using. Enhanced dissolution of ibuprofen using solid dispersion. Ibuprofen ib is one of the most important nonsteroidal antiinflammatory drugs used in the treatment of inflammatory chronic diseases. Ibuprofen encapsulation by eudragit rs100 as microspheres.
Incomplete drug release may be due to physico chemical drug interaction with the polymer andor perfectly drug crystal encapsulated by the polymer. Solid dispersion technique can be used to enhance the. Ibuprofen, a weakly acidic nonsteroidal antiinflammatory drug having poor aqueous solubility, is a challenging drug for the development of pharmaceutical formulations, resulting in numerous research attempts focusing on improvement of its solubility and consequently bioavailability. Ibuprofen is a nonsteroidal antiinflammatory drug nsaid with analgesic, antipyretic, and antiinflammatory properties methods. Solid dispersions of ibuprofen were prepared by fusion using peg 4000, peg 6000, mannitol, urea, sorbitol, dextrose, sucrose and their mixtures as carriers in 1. The purpose of this study was to develop ibuprofen ibpolyethylene glycol peg 8000 solid dispersions sds and investigate them for in vitro dissolution and. Ibuprofen, urea, solid dispersions, dissolution rate. Physical mixtures pms of ibuprofen were also prepared with the same carrier and in the same drugcarrier. This drug presents, in the pure state, poor physical and mechanical characteristics and their use in solid dosage forms needs the addition of excipients which improve these properties. Grind 1 tablet to a fine powder in a mortar, add about 5 ml of chloroform, and swirl. Ibuprofen poloxamer 188 p 188 binary solid dispersions sd with different drug loadings were prepared, characterized by scanning electron microscopy sem, differential scanning calorimetry dsc and fourier transform infrared spectroscopy ftir, and evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Most phospholipids improved the dissolution of ibuprofen.
Loss of individual surface properties during melting and resolidification as revealed by sem micrographs. Preparation, characterization and ex vivo intestinal permeability. Seven physical mixtures were prepared in different ibuprofen to neusilin mass ratios as listed in table 1. To improve its oral absorption, rapidly dissolving ibuprofen solid dispersions sd were prepared in a relatively easy, simple, quick, inexpensive, and.
Pdf preparation, characterization, and dissolution. To develop a novel ibuprofen loaded solid dispersion system sds with enhanced dissolution rate, binary and ternary solid dispersion were prepared by coprecipitation method using poloxamer407 only and mixture of poloxamer407 with a second polymer such as. The aim of this study was to investigate the solid dispersion phase behavior of s. The results from microraman spectrometry confirmed the uniformity of the samples. Pvp k30mcc and pvp k30peg6000 also markedly increased the solubility of ibuprofen. Solidstate interaction of ibuprofen and neusilin us2. It is an analgesic, antiinflammatory and antipyretic. Improved dissolution and antiinflammatory effect of. Prolongedrelease solid dispersions of ibuprofen request pdf. Preparation and evaluation of fast dissolving ibuprofen.