The relationship between pH and concentrations of antioxidants and vasoconstrictors in local anesthetic solutions.
pH affects the efficacy of local anesthetics by determining the percentage of the lipid-soluble base form of the anesthetic available for diffusion and penetration of the nerve sheath. The purpose of this study was to determine the relationship between pH and the concentrations of antioxidant and vasoconstrictor in dental local anesthetic solutions over real-time and after accelerated aging. Several batches of lidocaine and mepivacaine with vasoconstrictors were tested. Results showed that, immediately upon receipt from the manufacturers, three batches were below the USP pH limit (pH 3.3), and two batches contained less than the minimum limit of vasoconstrictors (90%). Real-time tests on batches that were within normal limits revealed that solutions were stable past 4 yr. Accelerated aging tests revealed a strong correlation between a decrease in pH and loss of antioxidants and vasoconstrictors. In conclusion, a quality batch of local anesthetic should remain efficacious long past the manufacturer's stated shelf life; a batch that is less than optimal, or one that is exposed to environmental stresses, will degrade rapidly, and efficacy may be affected by decreases in pH and loss of vasoconstrictor. pH may be an inexpensive, readily available screening test for efficacy of local anesthetics.
D000779:Anesthetics, Local / Q000737:chemistry* / Q000493:pharmacokinetics; D000975:Antioxidants / Q000032:analysis* / Q000493:pharmacokinetics; D001682:Biological Availability; D004355:Drug Stability; D004356:Drug Storage; D004837:Epinephrine / Q000032:analysis; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008012:Lidocaine / Q000737:chemistry; D008619:Mepivacaine / Q000737:chemistry; D008771:Nordefrin / Q000032:analysis; D019999:Pharmaceutical Solutions / Q000737:chemistry; D012044:Regression Analysis; D013447:Sulfites / Q000032:analysis; D014662:Vasoconstrictor Agents / Q000032:analysis* / Q000493:pharmacokinetics