Preparation and evaluation of ibuprofen solid dispersion. Preparation, characterization, and dissolution studies of ibuprofen solid dispersions using polyethylene glycol peg, talc, and pegtalc as dispersion carriers. Therefore, the rapid ibuprofen absorption could be a prerequisite for the quick onset of its action. Ibuprofen is a biopharmaceutical classification system class ii drug that exhibits poor dissolution rate in the gastrointestinal tract. Solubility and dissolution enhancement of ibuprofen by solid dispersion technique using peg 6000pvp k 30 combination carrier article pdf available january 2012 with 3,504 reads how we. Dissolution enhancement of aceclofenac tablet by solid. Solubility practical insoluble in water, freely soluble in acetone, dichloromethane and methanol. Nov 21, 2008 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.
The very slow dissolution rate was observed for pure diazepam and the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Improvement of dissolution rate of ibuprofen by solid dispersion. Investigation of solid dispersion technique in improvement of. Food and drug administration fda issued information for healthcare providers and consumers regarding unapproved topical combination products containing ibuprofen. Thermodynamic study of the solubility of ibuprofen in acetone. Impact assessment of different polymers on physicochemical. Specification ibuprofen dc 100 description specification test method appearance white or nearly white agglomerate ph.
Unlike oral ibuprofen products which are fdaapproved, topical products containing ibuprofen are not fdaapproved. Enhanced dissolution of ibuprofen using solid dispersion with. With single doses up to 800 mg, a linear relationship exists between amount of drug administered and the integrated area under the serum drug concentration vs time curve. It is established that these systems belong to the eutectic type. Another example is described to obtain solid dispersions of ibuprofen in poloxamer 407 in order to increase the solubility and consequently the dissolution rate of this drug newa, 2008.
The internal rotations and interconformational jumps of ibuprofen in the solid state are fully characterized by the simultaneous analysis of a variety of low. Applying supercritical fluid technology to prepare ibuprofen solid. Solid dispersion of ibuprofen containing peg 6000 in combination with poloxamer 407 at the ratio of 1. Powder xray scans of ibuprofen and ibuprofendmpg solid dispersion were made to determine if there is a loss or modification of the pure drugs crystal structure after it is formed into a phospholipid solid dispersion, and to determine if any new crystalline phases may have formed. Public assessment report scientific discussion ibuprofen apotex 400 mg capsules, soft ibuprofen nlh2790001mr date.
Enhancement of solubility, dissolution and bioavailability. Gupta,1 patel 1mitul g1 2, patel nimesh s, madhulika kedawat,1 dept. Solid dispersions of ibuprofen ibf were prepared by solvent evaporation method using polyethylene glycol 0 peg, talc, and pegtalc as dispersion carriers. Effects of spray drying and spray chilling on ibuprofen dissolution amal a. Product information for auspar caldolor ibuprofen phebra pty ltd pm20100239331 final 2 january 20.
The ibuprofen in motrin tablets is rapidly absorbed. We prepared solid dispersions sds of ibuprofen ibu with kollicoat ir as the carrier using a newly developed pulse combustion dryer systemhypulcon. Enhanced dissolution of ibuprofen using solid dispersion. Thus, in this work, solid dispersions of ibuprofen in cethyl alcohol sd ca, stearic.
Data sources include ibm watson micromedex updated 10 apr 2020, cerner multum updated 6 apr 2020, wolters kluwer updated. Therefore, the rapid ibuprofen absorption could be. A solid dispersion is defined as a formulation of poorly soluble compounds as solid dispersions might lead to particle size reduction, improved wetting, reduced agglomeration, changes in the physical state of the drug and possibly dispersion on a molecular level, according to the physical state of the solid dispersion. Detailed characterization of the dynamics of ibuprofen in. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. Abstract ibuprofen is a propionic acid derivative that belongs to the class nsaids. Among 41 formulations, solid dispersions of ibuprofen in peg 6000 with each of pvp k30, poloxamer 237, and nacmc at ratio of 2. Phase equilibria in dispersed solid systems of ibuprofen with. Enhancement of solubility and dissolution characteristics of. 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 hpmc 6cps, hpc, kollicoat ir, kollidon va 64 respectively.
Biyani anuradha college of pharmacy, chikhli, 443201. Prolongedrelease solid dispersions of ibuprofen japs. Margret chandira1, debjit bhowmik1, rahul yadav1, b. Pdf on jan 10, 20, abdul wahab and others published preparation and evaluation of solid dispersions of ibuprofen using glucosamine hcl as a carrier. Pdf preparation and evaluation of solid dispersions of ibuprofen. A total of 20 tablets of each of the two studied pharmaceutical preparations ibuprofen, panfarma, belgrade, serbia and brufen, galenika a. After the study of sem, ftir and dsc it was found that solid dispersion of ibuprofen using poloxamer 407 and peg 6000 show satisfactory results. Absorption in vivo studies indicate that ibuprofen is well absorbed orally from the suspension formulation, with peak. Enhancing dissolution profile of diazepam using hydrophilic. 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. The aim of the present study is to enhance the dissolution of ibuprofen in presence of glucosamine.
Ibuprofen is a nonsteroidal antiinflammatory drug that has been widely used in the treatment of mild to moderate pain and fever. Solid dispersion granules were prepared using waterbased solid dispersion and waterretained pcs with the wet granulation method and a highspeed agitation granulator. Razia begum department of pharmaceutical technology, shri vishnu college of pharmacy, vishnupur, bhimavaram534202, ap, india. Improved dissolution and antiinflammatory activity of ibuprofenpolyethylene glycol 8000 solid dispersion systems. Preparation and evaluation of solid dispersions of ibuprofen using. Formulation and evaluation of ibuprofen controlled release matrix tablets using its solid dispersion article pdf available in international journal of applied pharmaceutics 112. Preparation, characterization and in vivo evaluation of. Major adverse reactions associated with ibuprofen are related to git and include peptic and mucosal ulcers, dyspepsia, severe gastric pain and bleeding, that results in excessive treatment failure.
Essab auniversity of sunderland, faculty of applied sciences, department of pharmacy, health and wellbeing, sunderland, sr1 3sd, uk buniversity of tanta, faculty of pharmacy, egypt abstract. Figures 2, 3 and 4 show the relaxation time measurements. Department pharmaceutics, bapatla college of pharmacy, guntur d, andhra pradesh, india. Pdf preparation, characterization, and dissolution. The known excess samples ibuprofen solid dispersions, physical mixtures and pure ibuprofen, 0. Formulation, physicochemical evaluation, and dissolution studies of carbamazepine solid dispersions m. 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. In this study solid dispersions sds of ibuprofen were prepared by melt dispersion technique using macrogol 4000 and macrogol 6000 as carrier. Solid dispersion sd technology has attracted considerable interest as an efficient means of improving the dissolution rate, and hence, the bioavailability of a range of hydrophobic drugs.
Kneading is the simplest process for the preparation of solid dispersion where drug polymers and appropriate. To improve its solubility, dissolution, and bioavailability. Quantitative analysis of ibuprofen 881 procedure for tablets and cream. Ibuprofen is a nonsteroidal anti inflammatory drug nsaid with analgesic, antipyretic, and. Enteric coating of ibuprofen tablets 200 mg using an aqueous dispersion system 101 logies, inc. Another example is described to obtain solid dispersions of ibuprofen in poloxamer 407 in order to increase the solubility and consequently the dissolution rate. To induce closure of a clinicallysignificant patent ductus arteriosus pda in premature infants weighing between 5001500 g and who are. Thermodynamic study of the solubility of ibuprofen in acetone and dichloromethane 229 ibp solubility analysis in terms of solubility parameters although experimental solubility is a complex phenomenon, definitions have been proposed in order to explain this important physicochemical property of drugs. Among them, solid dispersion is promising technologies to improve dissolution which is defined as the dispersion of active ingredient in an inert carrier in solid state. Josephine leno jenita1, and parvin zakerimilani3, 1department of pharmaceutics, dayananda sagar college of pharmacy, kumaraswamy, layout, bangalore 560078, karnataka, india. Quantitative analysis of ibuprofen in pharmaceuticals. Loss of individual surface properties during melting and resolidification as revealed by sem micrographs. Study of binary and ternary solid dispersion of ibuprofen for. Ibuprofenpolyethylene glycol 8000 peg 8000 solid dispersions sds with different drug loadings were prepared, characterized by scanning electron microscopy sem and differential scanning calorimetry dsc, and evaluated for solubility, invitro release, and oral bioavailability of ibuprofen in rats.
Figure 1 shows the 1 h nmr spectrum of 200 mm ibuprofen in cdcl 3. Pdf preparation, characterization, and dissolution studies. Research article enhancement of dissolution rate of ibuprofen by preparing solid dispersion using different methods m. Ibuprofen, solid dispersions, physical mixtures, hydrogenated castor oil, stearic.
Study of binary and ternary solid dispersion of ibuprofen. Ibuprofen, polyethylene glycol, poloxomer, solid dispersion, fusion. So, solid dispersion may be an effective technique to enhance dissolution rate of ibuprofen. Enhancement of solubility and dissolution characteristics of ibuprofen by solid dispersion technique article pdf available in dhaka university journal of pharmaceutical sciences 111. Both t 1 and t 2 values of the exchanging hydroxyl proton can be seen in the spectrum. 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. Formulation and evaluation the oral tablets ibuprofen. Enhancement of solubility, dissolution and bioavailability of. The purpose of this study was to develop ibuprofen ibpolyethylene glycol peg 8000 solid dispersions sds and investigate them for in vitro dissolution and in vivo antiinflammatory activity. Ibuprofen is a painkiller, which is available overthecounter, without a prescription. It is simple, scalable, convenient method and prepared using numerous processes 3. Preparation and evaluation of fast dissolving ibuprofen. Wayne, nj and magnesium stearate fmc corporation, usa were used as directly compressible. Comparative study of sustainedrelease lipid microparticles and.
Abstract ibuprofen is a nonsteroidal antiinflammatory drug with poor water solubility. Vinayaka mission college of pharmacy, salem, tamilnadu 2. Formulation, physicochemical evaluation, and dissolution. Ibuprofen was the first member of propionic acid derivatives to be introduced in 1969 as a better alternative to aspirin. Effect of water soluble polymers on dissolution enhancement of. 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 present work aims to evaluate the potential of the solid dispersion technique for development of fastdissolving tablets of frmd using ssg as the hydrophilic carrier. An overview of clinical pharmacology of ibuprofen rabia bushra1 and nousheen aslam2 introduction i buprofen is 2rs142methyl propyl phenyl propionic acid bp. Enteric coating of ibuprofen tablets 200 mg using an. Formulation and evaluation of solid dispersions of furosemide. Solid dispersions of ibuprofen were prepared by using peg 20000 and poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Formulation and evaluation the oral tablets ibuprofen r. Sustainedrelease solid dispersions of ibuprofen prepared by.
To improve its oral absorption, rapidly dissolving ibuprofen solid dispersions sd were prepared in a relatively easy, simple, quick, inexpensive, and. The solid dispersions of ibuprofenstearic acid and ibuprofenhydrogenated castor oil showed the best flow characteristics compared with pure ibuprofen. Ibpeg 8000 sds were prepared by fusion method using varying. Essab auniversity of sunderland, faculty of applied sciences, department of pharmacy, health and wellbeing, sunderland, sr1 3sd, uk. Public assessment report scientific discussion ibuprofen. The points of nonvariant equilibrium of the ibuprofenpiracetam and ibuprofenurea systems correspond to a 65. This product information was approved at the time this a uspar. Design and development of fast dissolving tablets of ibuprofen v sai kishore, d gowtham kumar, b sudheer and m sandeep. Phase equilibria in dispersed solid systems of ibuprofen.
Apr 15, 2009 the solid dispersion systems ibuprofen piracetam and ibuprofen urea have been studied by differential scanning calorimetry. This spectrum was documented in just a single scan which took only 7 seconds to obtain. Peak serum ibuprofen levels are generally attained one to two hours after administration. This can be attributed to improved wettability and. Drugdrug solid dispersion is a unique approach to present a poorly soluble drug in an extremely fine state of subdivision to the gastro intestinal fluids. The solid dispersion of ibuprofen in cethyl alcohol showed a higher percentage of particles between 500 and m. Extreme high moderate low section 1 chemical product and company identification product name ibuprofen statement of hazardous nature considered a hazardous substance according to osha 29 cfr 1910. In vivo in vitro evaluation of solid dispersion containing.
Evaluation of enhancement of solubility of paracetamol by solid dispersion technique using different polymers concentration anupama singh, pramod kumar sharma, jay gopal meher, rishabha malviya department of pharmaceutical technology, meerut institute of engineering and technology, meerut 250005, u. Development and characterization of solid dispersion for. Ibuprofen ib is one of the most important nonsteroidal antiinflammatory drugs used in the treatment of inflammatory chronic diseases. Physicochemical characterization and dissolution study of. Department of pharmaceutical sciences, coimbatore medical college, coimbatore. The points of nonvariant equilibrium of the ibuprofen piracetam and ibuprofen urea systems correspond to a 65. Physicochemical characterization and dissolution study of ibuprofen compressioncoated tablets using locust bean gum negar bashardoust1,2, j. Thermodynamic study of the solubility of ibuprofen in.
It has a role as a nonsteroidal antiinflammatory drug, a nonnarcotic analgesic, a cyclooxygenase 2 inhibitor, a cyclooxygenase 1 inhibitor, an antipyretic, a xenobiotic, an environmental contaminant, a radical scavenger and a drug allergen. Fei han 1, wei zhang 1, ying wang 2,3, ziyue xi 1, lu chen 1, sanming li 1. Formulation and evaluation of solid dispersions of. Studies in adults have established the doseproportionality of ibuprofen as a single oral dose from 50 to 600 mg for total drug and up to 1200 mg for free drug. Design and development of fast dissolving tablets of ibuprofen. Physical mixtures pms of ibuprofen were also prepared with the same carrier and in the same drugcarrier ratio 1. In vivoin vitro evaluation of solid dispersion containing ibuprofen sachin k.
Pdf solubility and dissolution enhancement of ibuprofen. Solid dispersion technique can be used to enhance the solubility, dissolution. The solid dispersion systems ibuprofenpiracetam and ibuprofenurea have been studied by differential scanning calorimetry. The paper is devoted to the investigation of microwave irradiation mw for the preparation of solvent free solid dispersion sd. 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. It dissolves in dilute solutions of alkali hydroxides an dcarbonates ph. Ibuprofen is a monocarboxylic acid that is propionic acid in which one of the hydrogens at position 2 is substituted by a 42methylpropylphenyl group. Proton nmr spectrum of 200 mm ibuprofen in cdcl 3 1 h nmr relaxation. Pdf on apr 25, 2007, teofilo vasconcelos and others published ddw103 development of a rapid dissolving ibuprofen solid dispersion find, read and cite. Ibuprofen, urea, solid dispersions, dissolution rate. Furthermore, this study seeks to investigate kneading as a method for the preparation of. Solid dispersions by hotmelt extrusion pharmaceutical.
Effects of spray drying and spray chilling on ibuprofen. Ibuprofen serum concentrations and its analgesic effect have been shown to be correlated. 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. Furthermore, this study seeks to investigate kneading as. Improved dissolution and antiinflammatory activity of. Investigation of solid dispersion technique in improvement. Pdf formulation and evaluation of ibuprofen controlled. With single doses up to 800 mg, a linear relationship exists between amount of drug administered and the integrated. Pdf ddw103 development of a rapid dissolving ibuprofen solid.
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