Influence of Inclusion of Nonsteroidal Antiinflammatory Drugs with β-Cyclodextrin on the Irritation to Stomach of Rats upon Oral Administration

概要

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Nonsteroidal antiinflammatory drugs are generally very slightly soluble in water and sometimes cause an adverse reaction due to a stimulant property to stomach upon oral administration. The present study was attempted to investigate the effect of inclusion with β-cyclodextrin (β-CD) on the irritation to stomach of three kinds of drugs, i.e., indomethacin (IMC), flufenamic acid (FFA) and phenylbutazone (PBZ) using Wistar male rats. The samples of the inclusion compounds or the intact ones were administered to stomach of rats, and the degree of injury of mucosa of stomach was observed by a dissection microscope, being evaluated by the six grades of numerical marks from 0 to 4.0. Any significant difference was not observed between the freeze-dried inclusion compounds and intact drugs of both IMC and FFA. There observed no significant difference between the two dosages of IMC. In the case of PBZ, however, there was a significant difference between the freeze-dried inclusion compound and intact drug by t-test at 5% level, suggesting that owing to its basic property the inclusion compound was effective in reducing the stomach injury due to the drug.
公益社団法人日本薬学会の論文
1978-12-25