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.
Introduction: The main objective of the current study is to enhance the solubility and dissolution of poorly water-soluble drug flurbiprofen, a propionic acid derivative, used as non-steroidal anti-inflammatory drug by formulating into solid dispersion (SD) employing various hydrophilic polymers as carriers in the formulation. Materials and Methods: The solubility of drug in various polymers such as AQOAT AS, PVP-K30, hydroxypropryl methyl cellulose, Soluplus, and Kollidon VA 64 was studied. Total 15 SD formulations were prepared by solvent evaporation technique with different polymers and were evaluated for particle size analysis, % practical yield, drug content determination, and in vitro dissolution studies. Results: Based on the evaluation parameters and dissolution studies, SD6 was found to be optimized formulation. The SD6 prepared using flurbiprofen:AQOAT AS:sodium lauryl sulfate as drug:polymer:surfactant in 1:5:2 ratios showed maximum drug release of 99.86 in 15 min when compared with other formulation and the solubility of the formulation SD6 was enhanced 44 folds when compared to that of pure drug. Drug excipient compatibility studies were conducted using FTIR and XRD and scanning electron microscope (SEM) studies were also conducted. FTIR studies showed the compatibility between drug and polymers. XRD and SEM studies showed that the optimized formulation was in amorphous form which fetched in better dissolution of the drug from the SD formulation when compared to the pure drug. Conclusion: This indicates the formulation technology employed with a potential of enhancing bioavailability of poorly water-soluble drug by improving its dissolution rate.
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