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KMID : 0369819970270030181
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Jorunal of Korean Pharmaceutical Sciences
1997 Volume.27 No. 3 p.181 ~ p.187
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Pharmacokinetics of Ethanol After Oral Administration of Aspartate-Containing Compositions
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김태완/Kim TW
이범진/최한곤/김종국/신희종/김정우/Lee BJ/Choi HG/Kim CK/Shin HJ/Kim JW
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Abstract
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The purpose of this work was to investigate pharmacokinetics of alcohol as a function of dose and time of administration of ethanol. The pharmacokinetics of alcohol 15 min after and before oral administration of aspartate-containing compositions to rats were also evaluated. The retention time of acetaldehyde, alcohol and isopropyl alcohol an internal standard in gas chromatogram was 3.6, 6.0 and 10.5 min, respectively. The maximum concentration of alcohol (Cmax) and area under the blood concentration (AUC) were significanly increased as a function of ethanol dose in a nonlinear fashion. The significant diurnal variation of alcohol pharmacokinetics was also noted, showing fast metabolism and elimination when given orally in the night time. When APAP was given after administration alcohol (1g/kg) to rats, AUC and Cmax were increased when compared to alcohol only. However, AUC and Cmax were decreased when aspartate or standard complex compositions containing aceaminophen (APAP, 250mg). sodium L-aspartate(25 mg), dl-methionine (125 mg) and anhydrous caffeine (25 mg) was orally given by coupling malate/asparate shuttle in hepatocyte. The blood alcohol concentration profiles between aspartate and standard complex compositions were similar when given before or after administration alcohol (1g/kg) to rats. No significant difference of administration sequence was observed. However, it was noted that AUC and Cmax of standard complex compositions given before alcohol administration were significantly lower when compared with alcohol only. Based on these findings, dose, time of administration and composition of drugs to improve alcohol metabolism and elimination were considered to be important in the pharmacokinetics of alcohol. The administration sequence of drug compositions and alcohol might be also considerd.
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KEYWORD
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Alcohol pharmacokinetics, Aspartate, Acetaminophen, Complex compositions, Circadian rhythm
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