Preparation and Evaluation of Ibuprofen Liquid Fill Formulations for Soft Gels (original) (raw)
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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.
Improvement of Solubility of Badly Water Soluble Drug (Ibuprofen) by Using Surfactants and Carriers
International Journal of Pharmaceutical Sciences and Research
Although there was a great interest in solid dispersion systems during the past four decades to increase dissolution rate and bioavailability of badly water-soluble drugs, their profitable use has been very limited, primarily because of manufacturing difficulties and stability problems. In this study solid solutions of drugs were generally produced by fusion method. The drug along with the excipients (surfactants and carriers) was heated first and then hardened by cooling to room temperatures. They were then pulverized, sieved, and encapsulated into hard gelatin capsules, then drug release was studied USP basket method at 50 rpm and controlling the temperature 370C. Ibuprofen is a non-steroidal anti-inflammatory drug commonly used to reduce fever, pain and stiffness. An attempt was taken to study the effect of surfactants and carriers in badly water soluble drug (Ibuprofen) by using solid solution method. In this trial Sodium Lauryl Sulfate, Poloxamer, Polyethylene Glycol (PEG)-6000...
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.
Dhaka University Journal of Pharmaceutical Sciences
In the present study, solid dispersions of ibuprofen were prepared to improve aqueous solubility of ibuprofen. A series of formulations were prepared where PEG 6000 with polymers named PVP K30, cross PVP, poloxamer 237, HPMC ASLF, pregelatinized starch, Na-CMC, Eudragit L100, and kollidon IR were used in different ratios. Among 41 formulations, solid dispersions of ibuprofen in PEG 6000 with each of PVP K30, poloxamer 237, and Na-CMC at ratio of 2:9:7 revealed improved solubility of 952.73 ± 1.31, 878.18 ± 0.97, and 1263.64 ± 1.58 μg/ml, respectively. The physicochemical properties of these preparations were ascertained by FTIR, SEM, DSC, and particle size analyses. FTIR spectrum showed absence of chemical interactions and physical compatibilities between ibuprofen and polymers were confirmed by DSC. Disappearance of individual surface properties in solid dispersions were revealed by SEM studies, which indicated the formation of effective preparations. On the other hand, particle si...
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.
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.
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.
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 ...
NOVEL ORAL DELIVERY OF IBUPROFEN SOLUTION IN HARD GELATIN CAPSULES Original Article
International Journal of Pharmacy and Pharmaceutical Sciences, 2019
Objective: The primary objective of the project was to formulate and evaluate hard capsule containing the solution of ibuprofen. It also included enhancement of solubility of ibuprofen in hydrophilic solvents to obtain a unit dose capsule acceptable for human consumption. Methods: Solution of ibuprofen was developed by the salt formation of partial drug using potassium hydroxide in PEG 600 and water. The solution was encapsulated in hard capsules with band sealing. The final formulation was evaluated for uniformity of weight, disintegration, drug content and stability. The dissolution profile was compared with that of available marketed tablets and softgels. Results: The capsules were evaluated and found compliant as per specifications mentioned in general monograph of capsules in IP 2014. The uniformity of weight of the batch of capsules was found to be 734.8 mg (±0.58). The disintegration time of these capsules was observed to be 4.45 min. The drug content was found to be 100.03% and the product is stable over three months of test period under room temperature as well as accelerated conditions. The dissolution profile showed that softgels take longer time to release the drug whereas marketed tablets showed a dissolution profile comparable with that of formulated capsules. Conclusion: The developed capsule is a unit dose of liquid containing solubilized ibuprofen delivering the drug directly into the gastrointestinal tract (GIT). These are newer solid oral dosage forms with higher patient compliance and ease in manufacturing. They require lesser steps and manufacturing area when compared to the manufacturing of compressed tablets.