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Pharm Res ; 9(5): 595-600, 1992 May.
Article in English | MEDLINE | ID: mdl-1608888

ABSTRACT

Gabapentin is a gamma-aminobutyric acid analogue, which has been shown to be an effective antiepileptic. The solution stability of gabapentin in buffered systems was studied in order to facilitate the formulation of a liquid product. The degradation of the drug was followed as a function of pH, buffer concentration, ionic strength, and temperature. The results indicated that the rate of degradation was proportional to the buffer concentration and temperature. The pH-rate profile of gabapentin degradation showed that the rate of degradation was minimum at an approximate pH of 6.0. Further, the data suggested a slower solvent-catalyzed degradation rate for the zwitterionic species compared to the cationic or anionic species in the pH range of 4.5 to 7.0. There was no influence of ionic strength on the rate of degradation. Arrhenius plots of the data indicated that a shelf life of 2 years or more at room temperature may be obtained in an aqueous solution at a pH value of 6.0.


Subject(s)
Acetates/chemistry , Amines , Anticonvulsants/chemistry , Cyclohexanecarboxylic Acids , Water/chemistry , gamma-Aminobutyric Acid , Buffers , Drug Stability , Gabapentin , Hydrogen-Ion Concentration , Kinetics , Molecular Structure , Osmolar Concentration , Solutions , Temperature
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