MACROMOLECULAR PRODRUGS .15. COLON-TARGETED DELIVERY - BIOAVAILABILITY OF NAPROXEN FROM ORALLY-ADMINISTERED DEXTRAN NAPROXEN ESTER PRODRUGS VARYING IN MOLECULAR-SIZE IN THE PIG
MACROMOLECULAR PRODRUGS .15. COLON-TARGETED DELIVERY - BIOAVAILABILITY OF NAPROXEN FROM ORALLY-ADMINISTERED DEXTRAN NAPROXEN ESTER PRODRUGS VARYING IN MOLECULAR-SIZE IN THE PIG
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DOI：
10.1023/a:1015981126732
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发表时间：
1989-11-01
影响因子：
3.7
通讯作者：
OLESEN, HP
中科院分区：
文献类型：
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作者：
HARBOE, E;LARSEN, C;OLESEN, HP
测定了猪口服各种右旋糖酐-萘普生酯前药水溶液后萘普生的生物利用度。右旋糖酐前药的分子量从10000到500000不等。相对于母体萘普生的等效口服剂量计算，所有衍生物的吸收分数接近100%。萘普生生物利用度的个体间差异较小。所有给药前体的萘普生血浆谱显示出萘普生在血液中出现的特征性滞后时间（2-3小时）。与单独给药前体相比，同时给药过量的母体葡聚糖进一步延缓了萘普生从胃肠道的吸收。本研究的结果证明了右旋糖酐前药在结肠部位特异性递送含有羧酸官能团的药物方面的潜力。
The bioavailability of naproxen after oral administration of aqueous solutions of various dextran-naproxen ester prodrugs in pigs was determined. The dextran prodrugs employed ranged in molecular weight from 10,000 to 500,000. As calculated relative to an equivalent oral dose of parent naproxen, the absorption fractions of all the derivatives were close to 100%. Only small interindividual variation of naproxen bioavailability was observed. The naproxen plasma profiles for all the administered prodrugs exhibited a characteristic lag time of naproxen appearance in the blood (2-3 hr). Compared to administration of the prodrugs alone, coadministration of excess of the parent dextran further delayed the absorption of naproxen from the GI tract. The results of the present study demonstrate the potential of dextran prodrugs for colon site-specific delivery of drugs containing a carboxylic acid functional group.