Effect of Absorption Enhancers on the Permeation of Morphine in the Isolated Rectum of Rabbit

概要

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The morphine hydrochloride suppository (MoS) containing sodium caprate (CA-MoS) or sodium 5methoxysalicylate (MS-MoS) was studied physicochemically and biopharmaceutically. The hardness and melting point of such suppository freshly prepared or stored for 4 weeks were not affected by the absorption enhancers on comparison with those of MoS. The release of morphine from CA-MoS was much slower than that from MoS or MS-MoS. In the absorption experiments in vitro using the isolated rectal preparation of rabbit, percent of drug amount that was absorbed (i.e.accumulated in the tissue and permeated) after the application of MoS, CA-MoS and MS-MoS was 61.7, 63.1, and 86.5%, respectively. The rectal transport of morphine in vitro was significantly enhanced in the presence of sodium 5-methoxysalicylate. No histological change was observed in mucosal tissue of the rectum exposed to these absorption enhancers.
日本医療薬学会の論文
1990-10-20