评估（+）-环拉定-5'-酯作为（+）-环拉定在动物体内的前药。
Evaluation of (+)-cyclaradine-5'-esters as prodrugs for (+)-cyclaradine in animals.
作者信息
Lim J, Schwartz J, Loebenberg D, Miller G H, Symchowicz S, Lin C
机构信息
Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Corporation, Bloomfield, New Jersey 07003.
出版信息
Antimicrob Agents Chemother. 1987 Jul;31(7):998-1001. doi: 10.1128/AAC.31.7.998.
Both (+)-cyclaradine-5'-methoxyacetate (CM) and (+)-cyclaradine-5'-ethoxypropionate (CE) were converted to (+)-cyclaradine (C) in squirrel monkey and human sera at 37 degrees C. CE was more stable than CM. After oral administration (20 mg base equivalent per kg) of either CM or CE, no unchanged esters were observed in serum of squirrel monkeys, rabbits, or rats. Instead, C was detected, indicating conversions of CM and CE to C in vivo. In squirrel monkeys, the areas under the curve (AUCs) of C obtained from oral dosing with CM were 61% higher than those obtained from dosing with C, indicating that CM may be a good prodrug for C. In squirrel monkeys, rabbits, and rats, CE resulted in a 20 to 90% higher AUC of C than did CM, indicating that CE was better absorbed than CM.
（+）-环拉定-5'-甲氧基乙酸酯（CM）和（+）-环拉定-5'-乙氧基丙酸酯（CE）在松鼠猴和人血清中于37℃时均转化为（+）-环拉定（C）。CE比CM更稳定。在口服给予松鼠猴、兔或大鼠CM或CE（每千克20毫克碱当量）后，在其血清中未观察到未变化的酯类。相反，检测到了C，表明CM和CE在体内转化为C。在松鼠猴中，口服CM给药后获得的C的曲线下面积（AUC）比口服C给药后获得的高61%，表明CM可能是C的良好前药。在松鼠猴、兔和大鼠中，CE导致的C的AUC比CM高20%至90%，表明CE比CM吸收更好。
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