Improvement of Solubility of Badly Water Soluble Drug (Ibuprofen) by Using Surfactants and Carriers (original) (raw)
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Stamford Journal of …, 2011
The purpose of this study was to prepare and characterize solid dispersions of the NSAID Ibuprofen with PEG 6000, Poloxomer 188 and Poloxomer 407 with the intention of improving its dissolution properties. The solid dispersions were prepared by the fusion method. Evaluation of the properties of the dispersions was performed using dissolution studies. The results obtained showed that the rate of dissolution of Ibuprofen was considerably improved when formulated in solid dispersions with PEG 6000 and poloxomer 188. Solid dispersions with poloxomer 407 showed drug retarding capability which may trigger more research in the intension of exploiting this feature to prepare sustained release dosage form.
Enhancement of Solubility and Dissolution Characteristics of Ibuprofen by Solid Dispersion Technique
In this study solid dispersions (SDs) of ibuprofen were prepared by melt dispersion technique using macrogol 4000 and macrogol 6000 as carrier. Physical mixtures (PMs) of ibuprofen were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile. The solid dispersions and physical mixtures were investigated for drug loading, saturation solubility and dissolution behavior. Saturation solubility study was carried out in phosphate buffer (pH 7.2), 0.1 N HCl solution and distilled water. Solid dispersions were found effective to enhance the solubility of ibuprofen significantly in all the media. Dissolution test was carried out in two different media, phosphate buffer (pH 7.2) and 0.1 N HCl. Solid dispersion containing macrogol 6000 at the ratio of 1:1.5 (drug: carrier) showed faster and higher drug release and was found to be most effective among all the solid dispersions. Drug carrier interactions were studied by comparing Fourier Transform Infrared Spectroscopy (FT-IR) of solid dispersions with pure drug which revealed that the SDs were stable. So, solid dispersion may be an effective technique to enhance dissolution rate of ibuprofen.
International Journal of Current Pharmaceutical Research
Objective: The present study was aimed to enhance the solubility of poorly water soluble drug Ibuprofen using solid dispersion technique and to develop sustained release tablets containing solid dispersion granules of the optimized batch. Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory propertiesMethods: Solid dispersions of Ibuprofen were prepared by using PEG 20000 and Poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Drug-carrier physical mixtures were also prepared. Solid dispersions were characterized by saturation solubility, drug content, in vitro dissolution, FTIR and DSC analysis. Solid dispersion formulation, SDF9 (PEG 20000 and Poloxamer 407, 1:3:3) prepared by solvent evaporation method was considered as the optimized batch. Sustained release tablets containing the solid dispersion granules of the optimized batch were prepared by direct compression method using HPMC K100M at ...
Solid dispersions of ibuprofen (IBU) were prepared by solvent evaporation method using polyvinyl pyrrolidone (PVP) and/or sodium lauryl sulphate (SLS). Physicochemical properties of the various solid dispersion systems were determined by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The results from dissolution studies indicated that ternary solid dispersion systems were more efficacious than the corresponding binary ones. The increase in the dissolution rate of ibuprofen from its solid dispersions with the PVP and/or SLS used in this study could be attributed to several factors such as improved wettability, local solubilisation, and drug particle size reduction. The most effective solid dispersion was the 20:180:10 w/w IBU-PVP-SLS ternary system, which allowed dissolution of 85 % drug after only 9.15 minutes (in comparison with 94.61 minutes for drug alone and 17.92 minutes for the binary system).
Formulation and in vitro characterization of ibuprofen-loaded solid dispersions
2020
The purpose of the study was to formulate solid dispersions of ibuprofen using binary mixtures of Gelucire 50/13 and HPMC by fusion and solvent evaporation methods in order to improve physical and mechanical characteristics of this drug. The dispersions were prepared with the excipients mixtures in the ratios of 1:1, 1:2, 1:4, 2:1 and 4:1 and characterized by determining the Fourier transform infra-red (FTIR) spectroscopy, solubility, entrapment efficiency (EE) and in vitro dissolution rate. The results showed that the EE decreased with increase in the concentrations of both Gelucire 50/13 and HPMC in the dispersions. Batch C containing Gelucire 50/13 and HPMC in the ratio 1:4 respectively showed the highest solubility for the fusion and solvent evaporation methods. Results of the FTIR spectroscopy study showed that there was no remarkable difference between the spectra of ibuprofen in the solid dispersions, physical mixtures and that of the pure sample of drug. The batches prepared by fusion method gave higher release rate in both SIF and SGF compared to those of solvent evaporation. Also, the solid dispersions showed higher release profiles than the commercial sample of ibuprofen. Thus, the Gelucire 50/13 and HPMC (ratio; 1:4, respectively) based ibuprofen solid dispersions represents a promising tool for improving of the solubility of Ibuprofen.
Iran J Pharm Sci, 2007
Ibuprofen solid dispersions were prepared by the solvent and fusion-solvent methods using polyethylene glycol (PEG), polyvinylpyrrolidone (PVP), eudragit RS PO, eudragit RL PO and hydroxypropylmethylcellulose (HPMC) as carriers to improve physicochemical characteristics of ibuprofen. The prepared solid dispersions were evaluated for the flowability, solubility characteristics and dissolution behavior. Flowability studies of powders showed that solid dispersion technique improve flow properties compared with the physical mixtures. Solid dispersion technique found to be effective in increasing the aqueous solubility of ibuprofen. The dissolution of ibuprofen and polymers (PVP, HPMC, eudruagit and PEG-6000) were investigated using UV spectroscopy. Dissolution was carried out in phosphate buffer (pH 6.8) using a standard USP II dissolution apparatus. In vitro dissolution studies showed that in the dispersion systems containing eudragit or HPMC, dissolution of ibuprofen was retarded, which attributed to ionic interaction and gel forming, respectively. But solid dispersion containing PEG, as a carrier, gave faster dissolution rates than the physical mixtures. Finally, solid dispersion of ibuprofen:PEG 6000 prepared in 1:1.5 ratio showed excellent physicochemical characteristics and was found to be described by the zero order kinetic, and was selected as the best formulation in this study.
Drug Development and Industrial Pharmacy, 1998
Solid dispersions of ibuprofen (IBF) were prepared by solvent evaporation method using polyethylene glycol 10000 (PEG), talc, and PEG-talc as dispersion carriers. The drug-carrier(s) interactions in the solid state were investigated using scanning electron microscopy {SEM), digerential scanning calorimetry (DSC), and x-ray diffraction analysis. Interactions in the solution were studied by peqorming dissolution experiments. No important and well-defined chemical interaction was found between the ingredients. The increase in the IBF dissolution rate from the solid dispersions with the carriers used in this study could be attributed to several factors such as improved wettability, local solubilization, and drug particle size reduction.
Preparation and Evaluation of Fast Dissolving Ibuprofen-Polyethylene Glycol 6000 Solid Dispersions
Drug Delivery, 2008
To improve its oral absorption, rapidly dissolving ibuprofen solid dispersions (SD) were prepared in a relatively easy, simple, quick, inexpensive, and reproducible manner, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). They were evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and resolidification as revealed by SEM indicated the formation of effective SDs. Absence or shifting toward the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. However, no such interactions in the solid state were confirmed by FTIR spectra that showed the presence of drug crystalline in SDs. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C max , and a significant decrease in T max over pure ibuprofen. Preliminary results from this study suggested that the preparation of fast-dissolving ibuprofen SDs by low temperature melting method using PEG 6000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution, and absorption rate of ibuprofen.
Stamford Journal of …, 2011
The purpose of this study was to prepare and characterize solid dispersions of the NSAID Ibuprofen with HPMC, HPC, icing sugar, dextrose, mannitol and lactose with the intention of improving its dissolution properties. The solid dispersions were prepared by the fusion method. Evaluation of the properties of the dispersions was performed using dissolution studies. The results obtained showed that the rate of dissolution of Ibuprofen was considerably improved when formulated in solid dispersions with HPMC and HPC. Solid dispersions with icing sugar, dextrose, mannitol and lactose showed drug retarding capability which may trigger more research in the intension of exploiting this feature to prepare sustained release dosage form.
2015
The solubility of the drug substances in water is one of the major factors taken into account in the formulation of oral solutions and parenteral dosage forms. The present study was conducted to improve the solubility of ibuprofen in water by the use of phospholipids and nonionic surfactants (Tween ® 80 and Solutol ® 15HS). These excipients are well tolerated by the parenteral route and allow the solubilization through a micellar system. In our study, a design of experiments approach was tested using a mixture design of nonionic surfactants, phospholipids and ibuprofen. The results showed a significant increase in the solubility in all used mixtures. The analysis of the design space showed that the solubility of ibuprofen varies very closely with the concentration of the three surfactants in water and also with their association.