Characterization of MB-102, a New Fluorescent Tracer Agent for Point-of-Care Renal Function Monitoring
| Autor: | Richard B. Dorshow, Lung-Fa Kao, I. Rochelle Riley, Jeng-Jong Shieh, Thomas E. Rogers |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Chromatography
Chemistry Iohexol Point-of-Care Systems Pharmaceutical Science Renal function 02 engineering and technology Pharmaceutical formulation 021001 nanoscience & nanotechnology 030226 pharmacology & pharmacy High-performance liquid chromatography Fluorescence Fluorescence spectroscopy 03 medical and health sciences 0302 clinical medicine Pyrazines medicine Molecule Humans 0210 nano-technology Chirality (chemistry) medicine.drug Glomerular Filtration Rate |
| Zdroj: | Journal of pharmaceutical sciences. 109(2) |
| ISSN: | 1520-6017 |
| Popis: | 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 pKa'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). |
| Databáze: | OpenAIRE |
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