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β-受体阻滞剂心得安的口服剂型吸收差且差异大。人口服用药(80mg)后,血药浓度变化可达7倍,而同一受试者静脉注射10mg血药浓度变化为2倍。再者,根据曲线下面积(AUC)计算,口服80mg的生物利用度仅为静脉注射10mg的16%。口服血药浓度和生物利用度的变化是由于药物在肠胃道吸收时广泛代谢和首次通过效应所引起。鼠和狗作试验表明,心得安经鼻粘膜吸收迅速且完全。本文进行了人鼻粘膜吸收的研究。受试者为6例25～35岁健康男性,住院作任意交叉研究。禁食8小时后于早晨7时开始给心得安盐酸盐。口服给药为40mg(二片)溶于30ml水中,再饮150ml水;静脉给药为10ml注射液(1mg/1ml)以0.73mg/分的速度输
Beta-blockers propranolol oral formulations of poor absorption and differences. After oral administration of drug (80mg), the plasma concentration changes up to 7 times, while the same subject intravenous injection of 10mg blood concentration changes of 2 times. Again, according to the area under the curve (AUC), the oral bioavailability of 80 mg was only 16% for intravenous injection of 10 mg. Changes in oral plasma concentrations and bioavailability are due to extensive metabolism and first pass effects of the drug upon gastrointestinal uptake. Experiments in rats and dogs showed that nasal mucosal absorption is rapid and complete. In this paper, the study of human nasal mucosa absorption. The subjects were 6 healthy men aged 25-35 years and were hospitalized for any crossover study. After 8 hours of fasting, propranolol hydrochloride was given at 7:00 a.m. Oral administration of 40mg (two tablets) dissolved in 30ml of water, and then drink 150ml water; intravenous administration of 10ml injection (1mg / 1ml) at a rate of 0.73mg / min lose