Extemporaneous preparation of methyldopa in two syrup vehicles

Newton, D. Trevor; Rogers, A L; Becker, Charles H.; Torosian, George

doi:10.1093/ajhp/32.8.817

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“…(3) This tendency for degradation frequently generates difficulties with the stability of MD dosage forms. (4)(5)(6)(7) Borate ion is a known chelating agent for 1,2-diols, including catechols. (8,9) A study performed in the middle of the fifties showed that borate exercised a high degree of inhibition on the oxidation of L-dopa and other catecholamines.…”

Section: Introductionmentioning

confidence: 99%

DETERMINATION OF THE INFLUENCE OF BORATE ION ON THE DEGRADATION OF L-Α-Methyldopa USING RP-HPLC WITH PHOTODIODE ARRAY DETECTION

Rembischevski

Gemal

2001

Journal of Liquid Chromatography & Related Technologies

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The degradation of the drug L-α-methyldopa (MD) in alkaline solutions was studied by Reversed-Phase High Performance Liquid Chromatography. It was found that the presence of borate ion in the solution inhibited the formation of MD-melanin, the final product of degradation. It complexes with both MD and intermediates of the pathway, maintaining them longer in the medium. Through the use of a synthetic standard of a half-way intermediate of the oxidation pathway, 5,6-dihydroxy-2-methylindole (Me-DHI), and examination of the UV/vis spectra of the chromatographic peaks, it was possible to demonstrate the stabilization of a later stage degradation intermediate in the presence of borate ion.

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