Bioavailability of Mefenamic Acid: Influence of Food and Water Intake

Hamaguchi, Tsuneo; Shinkuma, Denji; Yamanaka, You; Mizuno, Nobuyasu

doi:10.1002/jps.2600750914

Cited by 18 publications

(4 citation statements)

References 16 publications

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“…Mefenamic acid is poorly soluble in both the proposed fasted and fed state simulated intestinal media, with only 5–7% of a 250 mg dose dissolving in 500 mL of media during dissolution testing. The similar extent of dissolution in vitro was linked to in vivo data on the drug showing similar absorption fasted and fed 70. However, a weakness of this argument is that the solubility of a weak acid with a p K a of 4.2 will be highly pH dependent over the pH range typical of the small intestine (pH 5.0–7.5), and pH 5.0, the pH for FeSSIF is rather low as a pH for all but the duodenal pH (at the very top of the small intestine) experienced by the drug in the fed state intestine.…”

Section: Results‐selected Example Drugsmentioning

confidence: 90%

The Developability Classification System: Application of Biopharmaceutics Concepts to Formulation Development

Butler

Dressman

2010

Journal of Pharmaceutical Sciences

346

194

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Section: Results‐selected Example Drugsmentioning

confidence: 90%

The Developability Classification System: Application of Biopharmaceutics Concepts to Formulation Development

Butler

Dressman

2010

Journal of Pharmaceutical Sciences

346

194

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“…In some cases, two or three data points have been used to derive an estimate for the terminal slope. [1][2][3][4][5][6] Although the use of two data points to estimate terminal slope by log-linear regression is not statistically or theoretically justified, the method can be quite satisfactory when limited experimental error is encountered. However, a poor estimate may be obtained when the experimental error is high because measurements in the proximity of the least quantifiable concentration have been carried out and/or sampling has not be continued for a long enough time to ensure that absorption or disposition processes do not disturb the elimination process.…”

Section: Introductionmentioning

confidence: 99%

An alternative method for the estimation of the terminal slope when a few data points are available

Dokoumetzidis¹,

Iliadis²,

Macheras³

1999

Journal of Pharmaceutical Sciences

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Phase plane plots are graphical expressions for differential equations plotting the state derivative dc/dt versus the state c. Using these plots, we developed a novel method for the estimation of the terminal slope from time-concentration data. The values of the derivatives used for the construction of the phase plane plots were calculated by two different methods of numerical differentiation. The first method (D1) is based on the classical calculation of slope of the line connecting two successive data points. The alternative method (D2) relies on an initial second-order polynomial interpolation utilizing three successive data points followed by the calculation of the derivative at each one of the concentration values. A forced-through-zero linear regression of the phase plane plot data is used to derive an estimate for the slope. For comparative purposes, the standard approach based on the semilogarithmic plot was also applied. For a hypothetical drug absorbed by first-order process into a one-compartment model, simulated time-concentration data disturbed by a Gaussian zero mean random error with various coefficients of variation were generated. Various sampling schedules, with two, three, four, or five data points, were utilized for the estimation of the terminal slope. Performances of the proposed methods on simulated data were expressed by means of root-mean-squared error, bias, and standard deviation. In all cases, D2 was superior to D1. The D2 method outperforms the standard method in that it furnishes estimates closer to the real values in all cases when two data points and in most cases when three data points were used. All methods behave similarly when four or five data points were used.

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“…It is also characterized as a practically insoluble drug with the water solubility of 0.9 µg/ml [2] . After administration, it rapidly permeates through gastrointestinal membrane and reaching maximum plasma concentration within 2-4 h [3,4] . Due to high permeability and low solubility characteristics, MF was classified to Biopharmaceutical Classification System (BCS) class II.…”

mentioning

confidence: 99%

Salt Formation Stability Study and Tablet Formulation of Mefenamic Acid with Improved Drug Dissolution

Sutthapitaksakul¹,

Thanawuth²,

Sriamornsak³

2022

IJPS

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Sutthapıtaksakul et al.: Salt Formation and Formulation of Mefenamic AcidMefenamic acid is characterized by a low oral bioavailability due to its slow dissolution and absorption. The purpose of this study was to investigate the effect of salt formation on dissolution of mefenamic acid and its physical stability. Potassium, sodium and lysine salts of mefenamic acid were prepared. The resulting salts formed were characterized by scanning electron microscopy, hot-stage microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry. In addition, the accelerated stability test was performed at 45°±2° and 75 %±5 % relative humidity for 3 mo. The dissolution of prepared salts was evaluated in comparison to untreated mefenamic acid. The results showed that the potassium and sodium salts of mefenamic acid were successfully prepared, while lysine salt of mefenamic acid could not be formed by the same method. The dissolution of both potassium and sodium salts of mefenamic acid was not significantly different, but the sodium salt was more stable than potassium salt. For this reason, sodium mefenamate was selected for formulating immediate-release tablets. It was also found that the formulated tablets containing sodium mefenamate gave rapid drug dissolution, compared to untreated mefenamic acid. Thus, it can be concluded that the formation of sodium mefenamate and its tablet formulation improve the dissolution of mefenamic acid.

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Bioavailability of Mefenamic Acid: Influence of Food and Water Intake

Cited by 18 publications

References 16 publications

The Developability Classification System: Application of Biopharmaceutics Concepts to Formulation Development

The Developability Classification System: Application of Biopharmaceutics Concepts to Formulation Development

An alternative method for the estimation of the terminal slope when a few data points are available

Salt Formation Stability Study and Tablet Formulation of Mefenamic Acid with Improved Drug Dissolution

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