文章基本信息

标题：Oral Delivery of Synthetic Eel Calcitonin, Elcatonin, in Rats
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作者：Taro OGISO ; Natsuko FUNAHASHI ; Yoshinori TSUKIOKA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2001
卷号：24
期号：6
页码：656-661
DOI：10.1248/bpb.24.656
出版社：The Pharmaceutical Society of Japan
摘要：This study was designed to develop an oral dosage form of elcatonin (EC), a hypocalcemic peptide. The EC absorption was estimated by the reduction in plasma calcium concentrations. When EC was orally coadministered with nitroso-N-acetyl-D, L-penicillamine (SNAP, 4.0 mg) and 0.02% Carbopol solution or with taurocholate (20 mM) and 0.02% Carbopol solution, the lowering effect was increased compared with that after EC alone, but the F values (0.32 and 0.30%) were extremely small. The oral administration of the mucoadhesive emulsion, which was prepared by coating the W/O/W emulsion with 0.1% Carbopol, enhanced the calcium lowering effect, with the F value of 0.43%. The strong mucoadhesion of the mucoadhesive emulsion to the gastrointestinal mucosa was observed. A capsule containing EC (500 μg), taurocholate (6 mg) and lyophilized Carbopol (3.5 mg) administered orally gave a sustained but comparatively small calcium lowering effect. In the in vitro enzymatic hydrolysis experiment, EC was more rapidly hydrolyzed in the intestinal fluid than in the mucosal extract. The combination of 20 mM taurocholate with 0.02% Carbopol showed the greatest inhibitory effect in both fluid and extract. These data indicated that EC was effectively absorbed through the intestinal wall, but the peptide was dominantly degraded by proteolytic enzymes in the GI tract. These results will offer a potential approach to the oral delivery of EC.
关键词：elcatonin;intestinal absorption;absorption enhancement;mucoadhesive emulsion;capsule