Glycine Ester of Metronidazole as a Water-Soluble Prodrug
Small, David S., Jr
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All of the experimental evidence accumulated during this project indicates that metronidazole glycinate is a viable prodrug of metronidazole. Its aqueous solubility is more than sufficient for the concentrations desired, the pH of the MGT is not too low for parenteral administration, and the serum hydrolysis of the prodrug is rapid. The only drawback to metronidazole glycinate that can be determined thus far is that it is instable in solution. This can be avoided, however, by developing an easily reconstitutable freeze-dried solid dosage form. Upon reconstitution in a proper diluent, spontaneous hydrolysis will take place, however, there will be sufficient time for administration before metronidazole begins to precipitate out of solution.