A new self-emulsifying formulation of mefenamic acid with enhanced drug dissolution

Sriamornsak, Pornsak; Limmatvapirat, Sontaya; Piriyaprasarth, Suchada; Mansukmanee, Punyanutch; Huang, Zongkang

doi:10.1016/j.ajps.2014.10.003

Cited by 44 publications

(44 citation statements)

References 12 publications

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“…[19] Mefenamic acid also has a higher solubility in hydrophilic surfactant, for example, Tween 80. [6] The composition of the surfactant greatly influences the stability of the mixture; the more surfactant used, the mixture will become clearer. The increasing surfactant competition led to more formation of nanoemulsion.…”

Section: Results and Discussion Formulation Snedds Of Mefenamic Acidmentioning

confidence: 99%

“…[5] Self-emulsifying formulation consisting of oil, surfactant, and cosurfactant can enhance the dissolution and absorption of mefenamic acid and improve the bioavailability of mefenamic acid. [6] SNEDDS is a mixture of isotropic oil, surfactant, cosurfactant, and drugs that form nanoemulsion oil-in-water (o/w) when emulsified in water. [7] SNEDDS has several advantages compared to nanoemulsion preparations that are ready to use, including having higher physical or chemical stability in longterm storage, having smaller volumes of dosage forms that can be given in the form of soft or hard capsules, and improving patient compliance.…”

Section: Introductionmentioning

confidence: 99%

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Suryani¹

2019

AJP

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Introduction:Mefenamic acid is one of the nonsteroidal anti-inflammatory drugs that have analgesic, antipyretic, and anti-inflammatory properties. However, in the biopharmaceutical classification system, mefenamic acid is included in Class II compounds with low oral bioavailability based on its dissolution rate or solubility in the digestive tract. One way to overcome the solubility problem of mefenamic acid is by formulating it into self-nanoemulsifying drug delivery system (SNEDDS). Previous research has shown that self-emulsifying drug delivery system of mefenamic acid produced greater drug solubility. In our research, we formulated SNEDDS of mefenamic acid to improve its solubility. SNEDDS is a mixture of isotropic oil, surfactants, cosurfactants, and drugs that form nanoemulsion oil in water when emulsified in water. The aim of this study was to formulate mefenamic acid SNEDDS using two different oil phases and compare their characteristics. Materials and Methods: Mefenamic acid SNEDDS formulation was carried out using the oil phase (olive oil and virgin coconut oil [VCO]), surfactant (tween 80 and tween 20), and cosurfactant (propylene glycol and polyethylene glycol [PEG] 400) with various concentrations. Optimization of the mefenamic acid SNEDDS formula was determined by observing the emulsification and clarity times, which were clarified with % transmittance. Then, further characterization of particle size, potential zeta, and stability was conducted. Results and Discussion: The optimization results obtained by F24 had a composition of olive oil, tween 80, and PEG 400 with a ratio of 1:8:1 and the results obtained by F53 had a composition of VCO, tween 80, and PEG 400 with a ratio of 1:5:1 meeting the requirements with emulsification time of 57 and 50 s, and transmittance values of 90% and 95%. The characterization results showed that F24 with the composition of olive oil, tween 80, and PEG 400 ratio 1:8:1 had a particle distribution of 569.4 nm, zeta potential +9.0 mV, and stability in gastric fluid media. Meanwhile, the characterization results showed that F53 having the composition of VCO, tween 80, and PEG 400 with the ratio of 1:5:1 had a particle distribution of 16.8 nm, zeta potential +2.9 mV, and stability in gastric fluid media. Conclusion: Based on the data, it can be concluded that the oil phase of VCO produced mefenamic acid SNEDDS formulas, which are better than the olive oil phase.

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Section: Results and Discussion Formulation Snedds Of Mefenamic Acidmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Untitled

Suryani¹

2019

AJP

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“…The improved dissolution may also be contributed to spontaneous emulsification and high hydrophilic-lipophilic balance (HLB) of the surfactant, apart being influenced by smaller globule size. The high HLB of SHS15 (14)(15)(16) resulting in increased hydrophilicity that causes increased drug dissolution and diffusion in the dissolution medium 56,57 . The predicted values of Y 5 and Y 6 were found to be in proximity to the experimental ones ( Table 1).…”

Section: Impact Of Formulation Components On Emulsification Time (Y 4 )mentioning

confidence: 99%

Fabrication of lipidic nanocarriers of loratadine for facilitated intestinal permeation using multivariate design approach

Verma

Singh

Verma

2015

Drug Development and Industrial Pharmacy

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In this investigation, multivariate design approach was employed to develop self-nanoemulsifying drug delivery system (SNEDDS) of loratadine and to exploit its potential for intestinal permeability. Drug solubility was determined in various vehicles and existence of self-nanoemulsifying region was evaluated by phase diagram studies. The influence of formulation variables X1 (Capmul MCM C8) and X2 (Solutol HS15) on SNEDDS was assessed for mean globule sizes in different media (Y1-Y3), emulsification time (Y4) and drug-release parameters (Y5-Y6), to improve quality attributes of SNEDDS. Significant models were generated, statistically analyzed by analysis of variance and validated using the residual and leverage plots. The interaction, contour and response plots explicitly demonstrated the influence of one factor on the other and displayed trend of factor-effect on responses. The pH-independent optimized formulation was obtained with appreciable global desirability (0.9266). The strenuous act of determining emulsification time is innovatively replaced by the use of oil-soluble dye to produce visibly distinct globules that otherwise may be deceiving. TEM images displayed non-aggregated state of spherical globules (size < 25 nm) and also revealed the structural transitions occurring during emulsification. Optimized formulation exhibited non-Newtonian flow justified by the model-fit and also presented the stability to dilution effects and thermodynamic stress testing. The ex vivo permeation study using confocal laser scanning microscopy indicate strong potential of rhodamine 123-loaded loratadine-SNEDDS to inhibit P-gp efflux and facilitate intestinal permeation. To conclude, the effectiveness of design yields a stable optimized SNEDDS with enhanced permeation potential, which is expected to improve oral bioavailability of loratadine.

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“…Mefenamic acid (MA) is used as an anti-inflammatory, antipyretic, and potent analgesic agent to treat rheumatoid arthritis, osteoarthritis, dental pain, and dysmenorrhea. 1–3 According to the biopharmaceutical classification system (BCS), MA is a class II drug that exhibits high permeability and low water solubility (i.e. 20 mg/L, which is practically insoluble in water) 4 .…”

Section: Introductionmentioning

confidence: 99%

“…This low solubility affects its rate of absorption from the GI tract and thus consequently will likely adversely affect its oral bioavailability. 1,5 Solid dispersion is a promising technique for overcoming this problem; it involves processing the poorly soluble drugs with inert carriers to change the nature of the drug, i.e. converting the crystalline form of the drug into an amorphous form that subsequently improves drug solubility and further increases drug bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Investigation of the combined effect of MgO and PEG on the release profile of mefenamic acid prepared via hot-melt extrusion techniques

Alshehri

Tiwari

Alsulays

et al. 2016

Pharmaceutical Development and Technology

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This study aimed to investigate the combined effect of magnesium oxide (MgO) as an alkalizer and polyethylene glycol (PEG) as a plasticizer and wetting agent in the presence of Kollidon® 12 PF and 17 PF polymer carriers on the release profile of mefenamic acid (MA), which was prepared via hot-melt extrusion (HME) technique. Various drug loads of MA and various ratios of the polymers, PEG 3350, and MgO were blended using a V-shell blender and extruded using a twin-screw extruder (16-mm Prism EuroLab, ThermoFisher Scientific) at different screw speeds and temperatures to prepare a solid dispersion system. Differential scanning calorimetry and X-ray diffraction data of the extruded material confirmed that the drug existed in the amorphous form, as evidenced by the absence of corresponding peaks. MgO and PEG altered the micro-environmental pH to be more alkaline (pH 9) and increased the hydrophilicity and dispersibility of the extrudates to enhance MA solubility and release, respectively. The in vitro release study demonstrated an immediate release for 2 h with more than 80% drug release within 45 min in matrices containing MgO and PEG in combination with PVP, when compared to the binary mixture, physical mixture, and pure drug.

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A new self-emulsifying formulation of mefenamic acid with enhanced drug dissolution

Cited by 44 publications

References 12 publications

Untitled

Untitled

Fabrication of lipidic nanocarriers of loratadine for facilitated intestinal permeation using multivariate design approach

Investigation of the combined effect of MgO and PEG on the release profile of mefenamic acid prepared via hot-melt extrusion techniques

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