Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

Daravath, Bhaskar; Chella, Naveen; Vemula, Sateesh Kumar; Tadikonda, Rama Rao

doi:10.1590/s2175-97902017000400010

Cited by 14 publications

(5 citation statements)

References 20 publications

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“…Ketoprofen’s solubility in PBS was within the range reported by Cayman (500 mg/L) [ 60 ] and Shohin et al (3310 mg/L) [ 61 ] but lower than the one of Felton et al [ 56 ]. For flurbiprofen, the determined PBS solubility was in accordance with Sadik et al (130 ± 40 mg/L) [ 62 ] and Daravath et al (98 ± 10 mg/L) [ 63 ], despite the heterogeneity of values reported (98 to 4445 mg/L) [ 56 , 62 , 63 , 64 , 65 ]. The value obtained for naproxen was in agreement with Cayman (1000 mg/L) and Kumar et al (750 ± 250) mg/L, being lower than Felton and co-authors’ value (4259 mg/L).…”

Section: Resultssupporting

confidence: 85%

Therapeutic Liquid Formulations Based on Low Transition Temperature Mixtures for the Incorporation of Anti-Inflammatory Drugs

2021

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Most nonsteroidal anti-inflammatory drugs (NSAIDs) present poor aqueous solubility, impairing their efficiency in physiological media. In this context, Low Transition Temperature Mixtures (LTTMs) are a promising platform to overcome drugs’ poor solubility, forming therapeutic liquid formulations. In this work, the LTTMs of citric acid:L-arginine:water (C:A:W) and glycerol:sorbitol (G:S) were studied in terms of their features and assessed in terms of their ability to increase the solubility of six NSAIDs in physiological media. The physicochemical properties of LTTMs were characterized by state-of-art techniques commonly used for these systems. The cytotoxicity of G:S was also evaluated in L929 mouse fibroblasts and the viscosity, polarity, and pH properties of the studied mixtures were related to the solubility of NSAIDs. The pH and polarity were the parameters that most influenced the drugs’ solubility. Ibuprofen, naproxen, ketoprofen, indomethacin, and flurbiprofen did not present any solubility improvement in the formulations tested. However, concentrated mixtures of C:A:W or G:S in the physiologic-mimicked media (PBS) rendered a celecoxib solubility 4 and 5 times higher than PBS, respectively. These therapeutic liquid formulations of celecoxib in C:A:W or G:S can be a promising tool to increase celecoxib’s therapeutic efficiency in local applications.

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Section: Resultssupporting

confidence: 85%

Therapeutic Liquid Formulations Based on Low Transition Temperature Mixtures for the Incorporation of Anti-Inflammatory Drugs

2021

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“…Here, the effect of a drug to carrier ratio on solubility was studied and it was found that a 1:2 ratio gave maximum solubility of meloxicam in distilled water. Higher is the molecular weight, higher is the solubility [22]. Therefore, PEG-15,000 was found to be more effective in enhancing solubility than PEG-6000 based on molecular weight.…”

Section: Solubility Study Of Solid Dispersionmentioning

confidence: 97%

Formulation and Evaluation of Mouth Dissolving Tablet of Meloxicam Using Natural Superdisintegrants

Pawar¹,

Mutha²,

Bhise³

et al. 2020

Asian J Pharm Clin Res

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Objective: The objective of the present work was the preparation and evaluation of mouth dissolving tablets (MDTs) of meloxicam using natural superdisintegrants. Methods: Meloxicam is BCS Class II (low soluble, and high permeable) drug increasing the dissolution properties of the poorly water-soluble drug meloxicam using a solid dispersion method (solvent evaporation method). Solvent evaporation method using drug and carrier as polyethylene glycol (PEG)-6000 and PEG-15,000 the ratio of 1:1, 1:2 (drug:carrier), and acetone as solvent. In house prepared banana powder were used as natural superdisintegrant. Manufacturing of MDT was done by the direct compression method. In this MDTs, various excipients were used such as mannitol used as the diluent, sodium saccharin used as a sweetening agent, Avicel pH-102 used as a binding agent, and talc and sodium lauryl sulfate (SLS) used as lubricant and glidant. The best formula of the tablet was selected according to the disintegration time (DT) and friability tests. Results: The results have shown that an increase in the meloxicam solubility was obtained using solid dispersion with the solvent evaporation method using PEG-15000 as a carrier in the ratio of 1:2 (drug:carrier). Taste masking was also done by a solid dispersion method. Tablet prepared with in house prepared banana powder gave less DT (70 s) as compared to tablet prepared with branded banana powder (80 s), but formulation F5 failed in friability testing. Improved strength of tablet obtained using SLS (<1%) also showed an increase in the dissolution performance of the tablet in formulation F6. This F6 formulation having 10% natural super disintegrating agent (in house prepared banana powder) has shown 99% cumulative drug release within 18 min. It also passed the friability test. Conclusion: Accordingly, the solubility of meloxicam was successfully enhanced through solid dispersion with carrier PEG-15,000 and formulated as a MDT to improve its oral absorption. PEG has also been used as a taste masking agent in these formulations. It was concluded that in house banana powder had excellent DT as compared to branded banana powder. Banana powder is “economical” and “easily available” than other commonly used synthetic superdisintegrants. The process of banana powder preparation is eco friendly. The meloxicam MDT formulated with natural superdisintegrant in house prepared banana powder found to pass all pharmacopeial tests.

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“…The drug content estimated spectrophotometrically at 247nm. [15][16][17] Release Kinetic Study Different kinetic models such as zero order, first order, Higuchi, and Korsmeyer-Peppa's were used to infer the drug release rate from the buccal patches comprising of flurbiprofen solid dispersions. The drug release data was substituted in various kinetic models to envisage the kinetics and mechanism.…”

Section: In Vitro Release Studymentioning

confidence: 99%

Formulation and Evaluation of Flurbiprofen Solid Dispersions Incorporated Buccal Patches

Sadik

Khan

2020

Int. J. Pharm. Sci. Drug Res.

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Flurbiprofen is an anti-inflammatory drug used in treating rheumatoid arthritis and ankylosing spondylitis. The present work is aimed at overcoming the deprived solubility of flurbiprofen by solid dispersion (SD) technique. The current paper is the continuance of the published solid dispersion by considering the best final optimized formulation containing flurbiprofen drug: AQOAT AS: SLS as drug: polymer: surfactant in 1:5:2 ratios, and incorporating it into buccal patches to overcome the gastric side effect and attaining sustained drug release. In this study 15 buccal patches were formulated by adopting solvent casting technique using polymers like polyvinyl hydroxyethylcellulose (HEC), hydroxypropryl methyl cellulose E15 (HPMC E15), polyvinyl pyrrolidone (PVP), carbopol and analyzed for the drug content, drug diffusion, in-vivo dissolution and stability studies. All SD loaded patches displayed superior drug release (95% to 99.96%) over 12 h. The formulation BP14 showed excellent drug release extended over 12 h with drug release of 99.96% whereas marketed formulation which is sustained release Tablet showed 96.86% drug release within 6 h. The drug release kinetics show that the buccal patches follow zero order release kinetics with correlation coefficient (R2) ranging between 0.905-0.971 and BP14 formulation shown best R2 value. All the formulations exhibited best fit to Higuchi model with R2 ranging between 0.9911 – 0.9962 indicating drug release by diffusion process. The results conclude that buccal patches are superior alternatives for flurbiprofen that facilitates enhanced drug release for prolonged period of time in the effective management of rheumatoid arthritis.

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Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

Cited by 14 publications

References 20 publications

Therapeutic Liquid Formulations Based on Low Transition Temperature Mixtures for the Incorporation of Anti-Inflammatory Drugs

Therapeutic Liquid Formulations Based on Low Transition Temperature Mixtures for the Incorporation of Anti-Inflammatory Drugs

Formulation and Evaluation of Mouth Dissolving Tablet of Meloxicam Using Natural Superdisintegrants

Formulation and Evaluation of Flurbiprofen Solid Dispersions Incorporated Buccal Patches

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