摘要
１２名男性健康志愿者随机分为两组，交叉口服抗胆碱Ⅰ类新药盐酸苯环壬酯片剂２ｍｇ、４ｍｇ和水剂４ｍｇ。采用ＧＣ－ＭＳ方法测定血浆中药物浓度，进行药代动力学及片剂相对生物利用度的研究。结果表明口服两种剂量及两种剂型后均能很快吸收，血药浓度一时间曲线符合二室模型，口服片剂２ｍｇ与４ｍｇ组的Ｔ１／２ｋａ分别为０．４２±０．１３和０．３３±０．１９ｈ；Ｔ１／２ａ分别为０．４６±０．４３和０．５１±０．２９ｈ；Ｔ１／２β分别为３．３３±３．２１和３．９８±３．４４ｈ；Ｔｍａｘ分别为１．６８±０．７８和１．１６±０．３７ｈ，两种剂量上述参数经ｔ检验无显著性差异（Ｐ＞０．０５）。两种浓度的回收率为５４．３±１９．１％（ＣＶ＝１０．３％）和４０．９±６．２％（ＣＶ＝１５．２％）。表明盐酸苯环壬酯在人体内运转过程不受剂量（临床用量范围）的影响。口服相同剂量（４ｍｇ）片剂和水剂的Ｔ１／２β分别为３．９８±３．４４和４．７５±３．０９ｈ；Ｔｍａｘ分别为１．１６±０．３７和０．９５±０．３２ｈ；Ｃｍａｘ分别为１５．４３±１３．８６和１４．７０±９．１０μｇ／ｌ；ＡＵＣ分别为４５．９±４０．４７和５７．３４±２３．７５μｇ·ｈ－１·Ｌ?
The pharmacokinetics and relative bioavailability of phencynonate,a new anticholinergic defined as a new drug of Class l according to《Provisions for New Drug Approval》China,1985.were studied in 12 male healthy volunteers after the crossover oral administration of 2mg,4mg tablets and 4mg in the aqueous solution, Plasma concentration of phencynonate was determined by GC- MS method.Phencynonate in both dosages and both preparations was rapidly absorbed from the gastrointestinal tract.the concertration-time curves of three groups were fitted to a two-compartment model.The T1/2ka of 2 mg and 4 mg tablets were 0.42±0.13 and 0.33±0.19 h; the T1/2 a were 0.46±0.43 and 0.51 ±0.29 h;the T1/2 βwere 3.33±3.21 and 3.97±3.44h;the Tmax were 1.68 ±0.78 and 1.16 ± 0.37 h.respectively. There was no significant difference in pharmacokinetic parameters between two dosages(P>0.05). It showed that there was no influence on the transfer process of phencynonate in vivo.The T1/2βof equal dosages(4mg) in the tablet and in the aqueous solution were 3.98±3.44 and 4.75±3.09 h;the Tmax were 1.16±0.37 and 0.95±0.32h;the Cmax were 15.43± 13.86 and 14.70±9.10 ng/ml; the AUC were 45.49±40.47 and 57.34±23.75μg·h-1·L-1, respectively. There was no significant difference in all of the parameters beteeen preparations of the tablet and the aqueous solution(P>0.05). The relative bioavailability of phencynonate tablet to aqueous was 79.34 %.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1995年第2期98-102,共5页
The Chinese Journal of Clinical Pharmacology
