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目的:制备油包水型溴吡斯的明新型纳米乳(novel pyridostigmine bromide nanoemulsion,PPNE),研究其体外释放规律及各胃肠段吸收动力学特征。方法选用3种不同浓度 pH 6.8、pH 7.4、pH 7.8的 PBS 以及 pH 1.2的 HCl 作为释药介质,测定并绘制其体外释药曲线;并采用在体单向肠灌流实验模型,比较溴吡斯的明(pyridostigmine bromide, PB)和 PPNE 在胃肠道的吸收行为。结果在4种释放介质中,PB 释放速率较快,而 PPNE 释放速率相对减缓;PPNE 的吸收速率常数(Ka )和表观渗透系数(Papp )较 PB 在十二指肠、空肠、回肠、结肠段中均增加。经 t 检验,PB 和 PPNE 在4个肠段均有统计学意义(P <0.05)。结论PPNE 可提高药物的生物利用度,明显提高其药物在体肠段的吸收;体外释放中有良好的缓释效果。“,”Aim To prepare the novel pyridostigmine bromide nanoemusion(PPNE)and study its release in vitro, and to investigate the intestinal absorption. Methods Pyridostigmine bromide (PB)and PPNE were tested by HPLC in pH 1 .2 HCl,pH 6.8,pH 7.4,pH 7.8 PBS.Rat single pass intestinal perfusion method was employed to investigate the absorption mechanism of PB and PPNE.Results PB release rate was faster than PB in the four release media;the intes-tinal absorption rate constant(Ka )and apparent perme-ability coefficient(Papp)of PPNE were increased in the duodenum,jejunum,ileum and colon segments.PBand PPNE had significant difference in the duodenum, jejunum,ileum and colon segments by t test (P <0.05).Conclusions PPNE can improve the bioavail-ability of drugs,increase the drugs permeability,sig-nificantly improve the absorption of the drugs in the in-testinal segments. PPNE has obviously sustained effects.