Till A E, Constanzer M L, Demetriades J, Irvin J D, Lee R B, Ferguson R K
Biopharm Drug Dispos. 1982 Jan-Mar;3(1):19-28. doi: 10.1002/bdd.2510030104.
Cyclobenzaprine hydrochloride was administered to healthy volunteers as a 10 mg oral tablet, 10 mg and 20 mg intramuscular injections, and a 10 mg intravenous injection. Urinary excretion and plasma level data for cyclobenzaprine together provide evidence for route dependent biotransformation. Urinary excretion of total cyclobenzaprine (unchanged plus the glucuronide conjugate) was greater for the oral treatment than for the parenteral treatments (i.m. and i.v.). Area under the plasma concentration-time curve for unchanged cyclobenzaprine, however, was less for the oral treatment than for the parenteral treatments. Based on area calculations, the bioavailability of the 10 mg oral tablet, 10 mg i.m. and 20 mg i.m. injection was 0.33, 0.76, and 0.56, respectively, when compared to the 10 mg i.v. injection of cyclobenzaprine hydrochloride. The four treatments were well tolerated and no clinically adverse effects were observed.
盐酸环苯扎林以10毫克口服片剂、10毫克和20毫克肌肉注射剂以及10毫克静脉注射剂的形式给予健康志愿者。环苯扎林的尿排泄和血浆水平数据共同为与给药途径相关的生物转化提供了证据。口服治疗中环苯扎林总量（未改变的加上葡糖醛酸共轭物）的尿排泄量高于非肠道治疗（肌肉注射和静脉注射）。然而，未改变的环苯扎林的血浆浓度-时间曲线下面积，口服治疗低于非肠道治疗。基于面积计算，与10毫克盐酸环苯扎林静脉注射相比，10毫克口服片剂、10毫克肌肉注射剂和20毫克肌肉注射剂的生物利用度分别为0.33、0.76和0.56。这四种治疗耐受性良好，未观察到临床不良反应。
