Dissolution Modulating Mechanism of Flurbiprofen Solid Dispersions: Characterization, Physical Stability and in vivo Performance: Formulation Considerations and optimization study

Tiwari, Ruchi; Tiwari, Gaurav; Pranaywal,; Ankitawal,

doi:10.5530/phm.2017.8.20

Cited by 4 publications

(3 citation statements)

References 8 publications

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“…A total of 1 mL of above solution was further diluted with ethanol and assayed spectrophotometrically at 247 nm by using the previously developed calibration curve. Results are expressed in drug content (drug entrapped) [ 49 ].

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Section: Methodsmentioning

confidence: 99%

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

et al. 2022

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The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow properties, % yield, and entrapment efficiency), four formulations were selected for further detailed studies. Solid-state characterization of optimized formulations (S1, S6, S7, and S12) showed successful drug incorporation in the solid dispersion at the molecular state without any noticeable interactions. The in vitro solubility and release study showed an increase in solubility and 98–100% of drug release in 30–45 min. The in vivo gastro-protective effect of the optimized formulations containing flurbiprofen and silica (1:1) with 25% w/w gelucire (S6 and S12) showed a reduction in the gastric lesion index (GLI) after four days of treatment. Moreover, histological images of the stomach lining (S6 and S12) illustrated normal epithelial cells and a partially protected mucosal membrane. Thus, TSD exhibited a significant increase in solubility and the dissolution rate and reduced the gastric ulceration. Therefore, TSDs are dubbed as efficacious carriers to enhance the bioavailability of flurbiprofen while simultaneously reducing its side effects.

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…”

Section: Methodsmentioning

confidence: 99%

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

et al. 2022

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“…Flurbiprofen, [2-(2-fluoro-4-biphenylyl) propionic acid] is a potent chiral non-steroidal anti-inflammatory agent with antipyretic and analgesic action and is approved by USFDA for the treatment of rheumatoid arthritis, osteoarthritis, and alkylosing spondylitis. It has a half-life of 4.7 h and needs frequent administration and its chronic intake could result in systemic side effects like gastric irritation and gastric bleeding [1][2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Formulation Optimization and Evaluation of Flurbiprofen Emulgel

Chodankar

Kudchadkar

Gude³

et al. 2020

Int J Pharm Pharm Sci

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Objective: The objective of the present study was to formulate flurbiprofen (FLB) emulgel, evaluation of the formulations and the selection of an optimized formulation through in vitro drug release and drug content studies. Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) requiring frequent administration and its chronic intake can lead to systemic side effects like gastric irritation and GI bleeding. The development of a dermal drug delivery system can overcome these side effects. Methods: The emulgel formulations were produced using different combinations of oil and emulsifying agents. Carbopol 940 was used as a gelling agent. The prepared emulgels were evaluated for general appearance, pH, spreadability, extrudability, drug content, in vitro drug release, average globule size and viscosity. Results: Optimized formulation F7 showed a better in vitro drug release compared to the marketed gel preparation. The stability study for the optimized formulation was carried out at 25 °C/60 % RH for 3 mo and the emulgel was found to be stable concerning the physical appearance, pH and drug content. Conclusion: The study revolved around the formulation of emulgel containing Flurbiprofen for dermal delivery of the drug. Emulgel was formulated with the purpose to enhance the permeation of poorly water-soluble drug FLB. The study concluded that the optimized emulgel containing FLB exhibited better in vitro drug release profile compared to the marketed formulation.

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“…The half-life of Flurbiprofen is 4.7 h and requires frequent dosing, but its chronic oral intake can result in systemic side effects such as gastric irritation and gastric bleeding. 2 In this study, an attempt was made to deliver Flurbiprofen into the systemic circulation by incorporating it as microsponges in a gel for transdermal delivery. Formulating Flurbiprofen as microsponges will extend the release of drug for a long period of time and further incorporating them into a transdermal gel will avoid gastrointestinal side effects.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Controlled Release Flurbiprofen Microsponges Loaded in Gels

Vernekar¹,

Gude²,

Ghadi³

et al. 2019

IJPER

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Objective:The main objective of this study was to formulate transdermal gels containing Flurbiprofen microsponges for controlled drug delivery. Methods: Microsponges containing Flurbiprofen and ethylcellulose were prepared by the quasi-emulsion solvent diffusion method. By varying the amount of drug and the polymer, seven batches of microsponges were formulated. Microsponges formed were characterized for surface morphology, thermal behavior, drug content, particle size, X-ray powder diffraction studies and in vitro drug dissolution studies. Results: SEM confirmed the spherical and the porous nature of the microsponges. Formulation F7 showed highest drug content and in vitro drug release of 92.74% at the end of 8 h and all the formulations followed zero order kinetics. Based on the results of drug content and in vitro release studies, formulation F4 was selected as the optimized batch and was incorporated into a carbopol gel base. The in vitro drug release from the microsponge gel was found to be extended over a longer period of time as compared to that from the marketed Flurbiprofen gel. Conclusion: Formulating Flurbiprofen in microsponges facilitated the controlled release of drug for long period of time thus eliminating the need of frequent dosing.

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Dissolution Modulating Mechanism of Flurbiprofen Solid Dispersions: Characterization, Physical Stability and in vivo Performance: Formulation Considerations and optimization study

Cited by 4 publications

References 8 publications

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

Formulation Optimization and Evaluation of Flurbiprofen Emulgel

Formulation and Characterization of Controlled Release Flurbiprofen Microsponges Loaded in Gels

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