Multiple oral administrations of huperzine A tablet as a treatment for Alzheimer's disease
会议名称：《山东省药学会第一届学术年会》
会议日期：2005年
学科分类：1002[医学-临床医学] 100205[医学-精神病与精神卫生学] 10[医学]
关 键 词：HUPERZINE A PHARMACOKINETICS BIOAVAILABILITY
摘 要：THE PHARMACOKINETICS OF HUPERZINE A WAS INVESTIGATED IN DOGS AFTER SINGLE INTRAVENOUS, ORAL AND TWO MULTIPLE ORAL ADMINISTRATIONS AT DOSES OF 10μG/KG/DAY. CONCENTRATIONS OF HUPERZINE A WERE DETERMINED BY A VALIDATED LC/MS/MS METHOD. AFTER SINGLE INTRAVENOUS AND ORAL ADMINISTRATIONS, HUPERZINE A WAS MODESTLY ELIMINATED WITH THE SIMILAR MEAN T1/2 OF 5.61 AND 5. 71 H, RESPECTIVELY. HUPERZINE A WAS WELL DISTRIBUTED INTO TISSUES WITH THE MEAN VD AND Vss OF 5. 36 AND 3. 96 L/KG, RESPECTIVELY. AFTER A SINGLE ORAL ADMINISTRATION, HUPERZINE A WAS RAPIDLY AND NEARLY COMPLETELY ABSORBED WITH THE MEAN TWAX OF 1. 25 H AND THE MEAN ORAL BIOAVAILABILITY OF 93. 7 %. AFTER FIRSTLY ORALLY ADMINISTRATED IN THE MORNING AND THEN AT 6 H AFTER IT DAILY OVER 6 CONSECUTIVE DAYS, HUPERZINE A ATTAINED STEADY STATE LEVELS IN PLASMA BY 4 DAYS WITH THE PTF OF 1.97, THE PTS OF 4. 51, CAV OF 0. 78 NG/ML AND THE RVC OF 1.27. AFTER ORALLY ADMINISTERED EVERY 12 H DAILY OVER 6 CONSECUTIVE DAYS, HUPERZINE A ATTAINED STEADY STATE LEVELS IN PLASMA BY 3 DAYS WITH THE PTF OF 2. 23, THE PTS OF 7. 70, THE GAV OF 0. 59 NG/ML AND THE RAC OF 2. 15. AFTER TWO MULTIPLE ORAL ADMINISTRATIONS OF HUPERZINE A, CAX WERE OBSERVED WITHIN 1.15 H AND T1/2 WAS PROLONGED TO 7.70 AND 10.09 H, RESPECTIVELY. IN CONCLUSION, HUPERZINE A HAVE A RAPID AND NEARLY COMPLETE ORAL ABSORPTION AND IS EXTENSIVELY DISTRIBUTED INTO TISSUES AFTER DRUG ADMINISTRATION IN DOGS. MULTIPLE DOSES ADMINISTRATIONS OF HUPERZINE A, FIRSTLY ADMINISTRATED IN THE MORNING AND THEN AT 6 H AFTER IT DAILY WERE SUPPORTED TO BE BENEFICIAL FOR TREATING PATIENTS WITH AD.