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In vitro dissolution test and pharmacokinetic study in human volunteers were conducted to evaluate the pharmacokinetic characteristics of 300㎎ trimebutine maleate(TMB-M) sustained-release tablet(TMB-M-SR300). As a reference product, 100㎎ trimebutine maleate immediately-release tablet(TMB-M-IR100) was used. Dissolution tests of two products were run in distilled water at 37±0.5℃and agitation of 100±5 rpm by the Paddle method described in KP VI, TMB-M-IR100 was dissolved very rapidly, and it took only 1hr to be dissolved over 97%, whereas 18hr for TMB-M-SR300 or three tablets of TMB-M-IR100 with randomized two period cross-over study. Significant differences between TMB-M-IR100 and TMB-M-SR300 were found in mean times to reach peak concentration, mean resident times and mean terminal phase half-lives, while not in AUC/Dose (Student´s-test). In ANOVA for AUC/Dose to compare the bioavailabilities of two TMB-M products, there was no significant difference. From the comparison of the simulated steady-state plasma concentration-time curves following multiple medications of TMB-M_IR100 (2 tablets t.i.d) and TMB-M-SR300(1 tablet b.i.d) based on the above results obtained from single doses of two TMB-M products, it was noted that the medication of TMB-M-SR300 is more useful in clinical application rather than TMB-B-IR100.
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