Preparation and Evaluation of Oral Dosage Form Using Acylglycerols. II. Effect of Food Ingestion on Dissolution and Absorption of Aspirin from the Granules Prepared by Acylglycerols in Human Subjects

概要

論文の詳細を見る
The dissolution behavior of the aspirin enteric granule prepared using acylglycerols, glyceryl monostearate (GMS) and glyceryl trilaurate (GTL), was investigated in vitro and in human subjects in a fasting or non-fasting state. Aspirin was slowly released from the granule in vitro at pH 1.2. No acceleration of the aspirin dissolution rate in the medium without lipase and cholic acid was observed when the pH level of the medium increased to a neutral region (pH 6.4). However, the dissolution of aspirin was significantly increased by increasing the concentrations of lipase and cholic acid in the medium. Lipase appears to play an essential role in the dissolution process of aspirin granules. In human subjects, the average levels of the cumulative amount of total salicylate excreted in a urine-time curve, and the mean residence time (MRT) obtained after oral administration of a granule in the fasting state were markedly delayed in comparison with the results observed using and aqueous solution and a crystalline form of aspirin. In comparing the fasting condition with the non-fasting condtion (after food ingestion), no significant difference was recognized in the total amount of salicylate excreted in urine to an infinite time (A_e(∞)), whether the MRT was obtained by granule, crystalline form or aqueous solution. It can be concluded that aspirin granule prepared by GMS and GTL has a property of pancreatic lipase-sensitive dissolution, and its bioavailability is unaffected by food intake.
公益社団法人日本薬学会の論文
1991-09-25

Preparation and Evaluation of Oral Dosage Form Using Acylglycerols. II. Effect of Food Ingestion on Dissolution and Absorption of Aspirin from the Granules Prepared by Acylglycerols in Human Subjects

スポンサーリンク

概要

著者

関連論文

スポンサーリンク