Moolenaar F, Grasmeijer G, Visser J, Meijer D K
Biopharm Drug Dispos. 1983 Apr-Jun;4(2):195-9. doi: 10.1002/bdd.2510040212.
Rectal absorption of codeine phosphate from various dosage forms was studied in man. The rectal dosage forms included aqueous solutions and fatty suppositories. A comparison was made with an orally administered solution. The plasma concentrations of codeine were measured by means of HPLC analysis after a single dose of 60 mg codeine phosphate in a cross-over study in 7 volunteers. Compared with oral dosing rectal absorption from an aqueous solution or a fatty suppository produced an almost identical plasma concentration profile with similar interindividual variations. Comparing the absorption rate characteristics it appeared that rectal absorption from an alkaline solution containing codeine phosphate proceeded significantly (P less than 0.05) more rapid than after oral dosing. No essential difference in bioavailability was observed between the various rectal and oral dosage forms.
在人体中研究了磷酸可待因从各种剂型的直肠吸收情况。直肠剂型包括水溶液和脂肪性栓剂。并与口服溶液进行了比较。在7名志愿者的交叉研究中，单次给予60mg磷酸可待因后，通过高效液相色谱分析测定血浆中可待因的浓度。与口服给药相比，从水溶液或脂肪性栓剂的直肠吸收产生了几乎相同的血浆浓度曲线，个体间差异相似。比较吸收速率特征发现，从含磷酸可待因的碱性溶液直肠吸收比口服给药显著更快（P小于0.05）。各种直肠和口服剂型之间未观察到生物利用度的本质差异。
