Effect of Pirprofen on Protein Binding of Warfarin and Tolbutamide in Human Plasma

Luders, Richard C.; Chao, Dolly

doi:10.1002/jps.2600701221

Cited by 5 publications

(1 citation statement)

References 17 publications

(10 reference statements)

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“…Two controls were also tested, sulfamethoxazole (39.5%, SD of 0.030) and warfarin (1.18%, SD of 0.0032), which agree with literature values. 20,21 Comparison of Blood-to-Plasma Ratio of MB-102 and Iohexol in Male Human Blood…”

Section: Comparison Of Human Plasma Proteins Binding Of Mb-102 and Iomentioning

confidence: 99%

Characterization of MB-102, a New Fluorescent Tracer Agent for Point-of-Care Renal Function Monitoring

Shieh

Riley

Rogers

et al. 2020

Journal of Pharmaceutical Sciences

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MB-102 is a fluorescent tracer agent designed for measurement of point-of-care glomerular filtration rate (GFR) and is currently in clinical studies. MB-102 possesses a strong UV absorbance at 266 nm and 435 nm, and broad fluorescent emission at~560 nm when excited at~440 nm. The MB-102 formulation is stable at 2 C-8 C for >3 years. The pK a 's of the 2 acid groups are 2.71 and 3.40. Both X-ray crystallography and HPLC confirmed the D, D chirality of MB-102 in solid, in solution, and in the drug formulation. Initial safety and toxicity was published previously [Bugaj and Dorshow, 2015], which enabled the commencement of clinical studies. In vitro studies showed that 4.1% of MB-102 is bound to human plasma proteins, compared to 6.0% for the accepted standard GFR agent iohexol. The blood-to-plasma ratio for MB-102 was 0.590, illustrating minimal distribution of MB-102 into red blood cells. The manufacture of MB-102 under good manufacturing practice yields the designed molecular structure at high purity (>95% wt/wt).

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Section: Comparison Of Human Plasma Proteins Binding Of Mb-102 and Iomentioning

confidence: 99%

Characterization of MB-102, a New Fluorescent Tracer Agent for Point-of-Care Renal Function Monitoring

Shieh

Riley

Rogers

et al. 2020

Journal of Pharmaceutical Sciences

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Interaction of pirprofen enantiomers with human serum albumin

Oravcová

Mlynárik²,

Bystrický

et al. 1991

Chirality

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The interaction of pirprofen enantiomers with human serum albumin (HSA) was investigated by means of high-performance liquid chromatography (HPLC), circular dichroism (CD), and 1H NMR spectroscopy. HPLC experiments indicated that both pirprofen enantiomers were bound to one class of high-affinity binding sites (n(+) = 1.91 +/- 0.13, K(+) = (4.09 +/- 0.64) x 10(5) M-1, n(-) = 2.07 +/- 0.13, K(-) = (6.56 +/- 1.35) x 10(5) M-1) together with nonspecific binding (n'K'(+) = (1.51 +/- 0.21) x 10(4) M-1, n'K'(-) = (0.88 +/- 0.13) x 10(-4) M-1). Slight stereoselectivity in specific binding was demonstrated by the difference in product n(+)K(+) = (0.77 +/- 0.08) x 10(6) M-1 vs. n(-)K(-) = (1.30 +/- 0.21) x 10(6) M-1, i.e., the ratio n(-)K(-)/n(+)K(+) = 1.7. CD measurements showed changes in the binding sites located on the aromatic amino acid side chains (a small positive band at 315 nm and a pronounced negative extrinsic Cotton effect in the region 250-280 nm). The protein remains, however, in its predominantly alpha-helical conformation. The 1H NMR difference spectra confirmed that both pirprofen enantiomers interacted with HSA specifically, most probably with site II on the albumin molecule.

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Glibenclamide and Tolbutamide in Human Serum: Rapid Measurement of the Free Fraction

Arcelloni

Fermo

Paroni

et al. 1990

Journal of Liquid Chromatography

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Effect of Pirprofen on Protein Binding of Warfarin and Tolbutamide in Human Plasma

Cited by 5 publications

References 17 publications

Characterization of MB-102, a New Fluorescent Tracer Agent for Point-of-Care Renal Function Monitoring

Characterization of MB-102, a New Fluorescent Tracer Agent for Point-of-Care Renal Function Monitoring

Interaction of pirprofen enantiomers with human serum albumin

Glibenclamide and Tolbutamide in Human Serum: Rapid Measurement of the Free Fraction

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