论文部分内容阅读
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?
Twelve male healthy volunteers were randomly divided into two groups. The anticholinergic class I drug was administered in combination with 2 mg, 4 mg and 4 mg of phencynonate hydrochloride tablets. The drug concentration in plasma was determined by GC-MS method, and the pharmacokinetics and relative bioavailability of tablets were studied. The results showed that oral administration of two doses and two formulations can be quickly absorbed, plasma concentration time curve in line with the two-compartment model, oral tablets 2mg and 4mg group T1 / 2ka were 0.42 ± 0.13 and 0 .33 ± 0.19h; T1 / 2a were 0.46 ± 0.43 and 0.51 ± 0.29h; T1 / 2β were 3.33 ± 3.21 and 3.98 ± 3.44h respectively; Tmax Respectively, 1.68 ± 0.78 and 1.16 ± 0.37h respectively. There was no significant difference between the above two parameters by t test (P> 0.05). The recoveries for both concentrations were 54.3 ± 19.1% (CV = 10.3%) and 40.9 ± 6.2% (CV = 15.2%). It shows that phencynonate hydrochloride is not affected by the dose (clinical dosage range) in the human body. The T1 / 2β of the oral administration of the same dose (4mg) tablet and the aqueous solution were 3.98 ± 3.44 and 4.75 ± 3.09h respectively; the Tmax were 1.16 ± 0.37 and 0.95 ± 0 respectively. 32h; Cmax were 15.43 ± 13.86 and 14.70 ± 9.10μg / l; AUC were 45.9 ± 40.47 and 57.34 ± 23.75μg · h-1 · L?