Esterification of Ibuprofen in Soft Gelatin Capsules Formulations-Identification, Synthesis and Liquid Chromatography Separation of the Degradation Products (original) (raw)
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Novel Oral Delivery of Ibuprofen Solution in Hard Gelatin Capsules
International Journal of Pharmacy and Pharmaceutical Sciences
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% ...
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.
Preparation and Evaluation of Ibuprofen Liquid Fill Formulations for Soft Gels
INDIAN DRUGS, 2017
The present investigation was undertaken with an objective to prepare and evaluate liquid fill formulations of non-steroidal anti-inflammatory drug, ibuprofen (IBU), in order to improve its dissolution properties and thereby its bioavailability. Liquid fill formulations were prepared by employing different co-solvents and surfactants like polyethylene glycol 400 (PEG 400), propylene glycol (PG) and polyvinylpyrrolidone (PVP K-30). The liquid fills were characterized by assay, rheology, clarity, in vitro dissolution studies and FTIR. More than 90% of the drug was released within 5 min from PVP K30 based formulations. Formulations containing PVP K 30 gave better dissolution properties when compared to formulations without PVP K 30, and complete drug dissolution was observed within 5min. Compatibility studies of IBU PEG 400, PG and PVP by IR method indicated that the excipients are compatible.
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...
Journal of Controlled Release, 1999
Controlled-release (CR) matrix tablets of ibuprofen (IBF) and Carbopol® 934P, and blended mixture of Carbopol® 934P and 971P resins, at different drug to polymers ratios, were prepared by the direct compression method. The investigation focuses on the influence of the proportion of the matrix material, and several co-excipients (lactose, microcrystalline cellulose (MCC), and starch) on the mechanism and release rate of the drug from the tablets. In vitro drug release in pH 7.2 phosphate buffer solution appears to occur both by diffusion and a swelling-controlled mechanism, exhibiting either anomalous or Case II type transport. The release process could be described by plotting the fraction released versus time and n fitting data to the simple exponential model: M /M 5kt . The release kinetics were modified when the blended mixtures of tC arbopol® 934P and 971P resins were used as the matrix materials. In general, all of the co-excipients, used in this study, enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared to microcrystalline cellulose or starch. The dissolution T and T values for the three co-excipients were in the order of 50 90 lactose.microcrystalline cellulose.starch. report carbomer matrix tablets showed to 0168-3659 / 99 / $ -see front matter
A comparative UV−HPLC analysis of ten brands of ibuprofen tablets
Asian Pacific Journal of Tropical Biomedicine, 2015
To investigate the pharmaceutical equivalence of ten brands of ibuprofen tablets (400 mg) purchased from pharmacies in Benin City, Nigeria. Methods: The drug samples were subjected to uniformity of weight, crushing strength, friability, melting point, disintegration and dissolution tests following acceptable and official protocols. The ibuprofen content was determined using UV and high performance liquid chromatography method. Results: Crushing strength values of the drug samples ranged between 6 and 16 kp while the disintegration times were between 7.43 and 10.40 min (for uncoated tablets) and 3.25-37.32 min (for coated tablets). Friability values were less than 1% and the melting points of recrystallized ibuprofen from the samples ranged from 73.5 to 76.0 C. The amount of ibuprofen released within 1 h ranged between 18% and 102% and two brands failed the content of active ingredient in the UV method of assay while all the brands passed the test using HPLC. Conclusions: Ibuprofen (400 mg) tablets marketed in Benin City, Nigeria vary in pharmaceutical quality.
Colloids and Surfaces B: Biointerfaces, 2011
In the current study Ibuprofen was embedded in a methacrylate copolymer (Eudragit ® EPO) matrix to produce solid dispersions by hot-melt extrusion (HME) processing. The obtained granules were incorporated in orally disintegrating tablets (ODTs). The tablets were developed by varying the ratio of superdisintegrants such as sodium croscarmellose and crosslinked polyvinylpyrrolidone grades while a direct compression process was used to compress the ODTs under various compaction forces to optimize tablet robustness. The properties of the compressed tablets which included porosity, hardness, friability and dissolution profiles were further evaluated and compared with Nurofen ® Meltlet ODTs. The taste and sensory evaluation in human volunteers demonstrated excellence in masking the bitter active and improved tablet palatability.
Journal of Controlled Release, 1999
Controlled-release (CR) matrix tablets of ibuprofen (IBF) and Carbopol® 934P, and blended mixture of Carbopol® 934P and 971P resins, at different drug to polymers ratios, were prepared by the direct compression method. The investigation focuses on the influence of the proportion of the matrix material, and several co-excipients (lactose, microcrystalline cellulose (MCC), and starch) on the mechanism and release rate of the drug from the tablets. In vitro drug release in pH 7.2 phosphate buffer solution appears to occur both by diffusion and a swelling-controlled mechanism, exhibiting either anomalous or Case II type transport. The release process could be described by plotting the fraction released versus time and n fitting data to the simple exponential model: M /M 5kt . The release kinetics were modified when the blended mixtures of tC arbopol® 934P and 971P resins were used as the matrix materials. In general, all of the co-excipients, used in this study, enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared to microcrystalline cellulose or starch. The dissolution T and T values for the three co-excipients were in the order of 50 90 lactose.microcrystalline cellulose.starch. report carbomer matrix tablets showed to 0168-3659 / 99 / $ -see front matter
Formulation and Evaluation of Ibuprofen Gel using a Natural Polymer
The East and Central African Journal of Pharmaceutical Sciences, 2015
Prolonged oral use of ibuprofen for chronic conditions such as arthritis may cause peptic ulcer disease. Topical gel formulations have been developed to overcome this shortcoming. An immediate release formulation of ibuprofen would find application as a transdermal patch for management of chronic inflammatory conditions. In our study, a topical ibuprofen gel was found to have a better release profile for the active pharmaceutical ingredient than the marketed brand. Keywords: Ibuprofen, gel, immediate release, peptic ulcer disease
Identification of degradation products of Ibuprofen arising from oxidative and thermal treatments
Journal of Pharmaceutical and Biomedical Analysis, 2002
Ibuprofen is a widely utilised analgesic anti-inflammatory drug. It is sensitive to oxidation and photodegradation. In this work, the oxidative and thermal degradations were investigated. The treatments adopted allowed the detection of 13 degradation products, seven of which have never been reported: hydratropic acid, 4-ethylbenzaldehyde, 4-(1carboxyethyl)benzoic acid, 1-(4-isobutylphenyl)-1-ethanol, 2-[4-(1-hydroxy-2-methylpropyl)phenyl]propanoic acid, 1isobutyl-4-vinylbenzene, 4-isobutylphenol. For 1-(4-isobutylphenyl)-1-ethanol, the in vitro toxic effects have already been described in the literature. To detect all degradation products, two RP-HPLC methods and a GC-MS procedure were developed or modified from the official monographs. The identification was conducted by evaluating chromatographic and spectral data and the structural attributions were confirmed by simple and univocal synthesis. Moreover, the actual presence of these molecules in marketed medicinal products was investigated. #