Eller M G, Wright C, Della-Coletta A A
Clinical Pharmacokinetics Unit, Upjohn Company, Kalamazoo, MI 49001.
Biopharm Drug Dispos. 1989 May-Jun;10(3):269-78. doi: 10.1002/bdd.2510100306.
The bioavailability of rectally administered sodium ibuprofen solution and aluminum ibuprofen suspension was determined in eight normal subjects relative to the same treatments administered orally. The results indicate that the suspension was less bioavailable than the solution irrespective of the route of administration. Although not bioequivalent, rectally administered ibuprofen solution compared favourably with orally administered ibuprofen solution. The mean AUC and Cmax from rectal administration were 87 per cent and 62 per cent of the corresponding values achieved after oral administration. Mean residence times and peak times were 1-3 h longer with the rectal solution, indicating a slower rate of absorption. Absorption after rectal administration was zero order in some subjects while absorption after oral administration was first order. This may be due to the large differences in surface area between absorption sites. Since sodium ibuprofen solution is absorbed when given rectally, this route of administration could be used in patients unable to take oral ibuprofen.
在八名正常受试者中，相对于口服相同治疗药物，测定了直肠给药的布洛芬钠溶液和布洛芬铝混悬液的生物利用度。结果表明，无论给药途径如何，混悬液的生物利用度均低于溶液。虽然直肠给药的布洛芬溶液与口服给药的布洛芬溶液并非生物等效，但相比之下表现良好。直肠给药后的平均药时曲线下面积（AUC）和最大血药浓度（Cmax）分别为口服给药后相应值的87%和62%。直肠溶液的平均驻留时间和达峰时间比口服溶液长1 - 3小时，表明吸收速率较慢。在一些受试者中，直肠给药后的吸收为零级，而口服给药后的吸收为一级。这可能是由于吸收部位表面积存在较大差异。由于直肠给药时布洛芬钠溶液可被吸收，这种给药途径可用于无法口服布洛芬的患者。
