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甲苯磺丁脲(TLB)在2.5,5%吐温-80或去氧胆酸(DAC)溶液中重结晶后,在人工胃液或人工肠液中进行溶出试验,结果表明,在吐温-80中重结晶者其溶出速率较大;用低浓度表面活性剂重结晶者其溶出速率大于高浓度的。生物利用度测定的结果亦表明,从给药后到10小时止,用2.5%吐温-80重结晶的TLB,血药浓度明显高于未处理的TLB,血药浓度峰值C_M及AUC_(0→10)均明显增高。此法是一种提高某些难溶性或微溶性药物溶出速率及生物利用度的有效方法。
Tolbutamide (TLB) was eluted in artificial gastric juice or artificial intestinal juice after recrystallization in 2.5,5% Tween-80 or deoxycholate (DAC) solution. The results showed that in TL-80 Recrystallization rate of dissolution of those larger; with low concentrations of surfactant recrystallization dissolution rate greater than its high concentration. The results of bioassay also showed that the blood concentration of TLB recrystallized with 2.5% Tween-80 was significantly higher than that of untreated TLB, the peak value of plasma concentration C_M and AUC_ (0 → 10) were significantly higher. This method is to improve some of the insoluble or slightly soluble drug dissolution rate and bioavailability of an effective method.