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目的 :研究茶碱控释片 (优喘平 )在睡眠呼吸暂停 (SAS)病人中的药物动力学。方法 :采用荧光偏振免疫法 ,测定 6例SAS病人首次口服优喘平 6 0 0mg后 48h内的血清茶碱浓度。结果 :血清中茶碱浓度在 12h左右达峰 ( 7.2 5 μg·ml-1) ,消除半衰期为 11.5h ,分布容积为 44 .49L ,总体清除率为 2 .6 1L·h-1,由此计算出达到有效治疗浓度 ( 10 μg·ml-1)所需的优喘平平均日剂量为 733mg。优喘平服药 3d达稳态时的峰谷浓度波动系数为2 4.31%。结论 :优喘平在SAS病人中口服给药后的药动学特征符合控释制剂要求 ,血药浓度波动较小 ,稳态时可达有效治疗浓度 ,为SAS病人安全有效用药提供了依据。
OBJECTIVE: To study the pharmacokinetics of theophylline controlled-release tablets (optimal asthma tablets) in patients with sleep apnea (SAS). Methods: Fluorescence polarization immunoassay was used to determine the serum theophylline concentration in 6 SAS patients within 48 hours after the first oral administration of You Chuping 600 mg. Results: The serum theophylline concentration peaked at 12h (7.25 μg · ml-1), the elimination half-life was 11.5h, the volume of distribution was 44.49L, and the overall clearance rate was 2.61L · h-1 Calculated to reach the effective therapeutic concentration (10 μg · ml-1) required the average daily dose of asthma is 733mg. The peak-to-peak concentration fluctuation coefficient of Euchrope medication 3d at steady state was 2 4.31%. CONCLUSION: The pharmacokinetic characteristics of Youchuping after oral administration in SAS patients are in line with the requirements of controlled release preparations. Fluvastatin has little fluctuation in plasma concentration and can reach effective treatment concentration in steady state, which provides the basis for the safe and effective medication for patients with SAS.