溴吡斯的明新型纳米乳体外释放和大鼠在体胃肠吸收
发布时间：2018-12-21 18:34
【摘要】：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(K_a)和表观渗透系数(P_(app))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(P0.05)。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。
[Abstract]:Objective to prepare a novel brompiridamine nanoemulsion (novel pyridostigmine bromide nanoemulsion,PPNE) with water in oil and study its release in vitro and the absorption kinetics of various gastrointestinal segments. Methods three kinds of PBS (pH 7.4 ~ 7.8) and HCl (pH 1.2) with different concentrations of pH were used as drug release media, and the drug release curves in vitro were determined and drawn. The absorption behavior of pyridostigmine bromide,PB and PPNE in gastrointestinal tract was compared with in vivo unidirectional intestinal perfusion model. Results in the four release media, the release rate of PB was faster than that of PPNE. The absorption rate constant (K _ a) and apparent osmotic coefficient (P _ (app) of PPNE were higher than those of PB in duodenum, jejunum, ileum and colon. By t test, PB and PPNE were statistically significant in 4 intestinal segments (P0.05). Conclusion PPNE can increase the bioavailability of drugs and increase the absorption of the drugs in the intestinal segment in vivo, and the drug release in vitro has a good sustained release effect.
【作者单位】： 重庆医科大学重庆高校药物工程研究中心;
【基金】：重庆市科委资助项目(Nocstc2015jcyjBX2007)
【分类号】：R965
[Abstract]:Objective to prepare a novel brompiridamine nanoemulsion (novel pyridostigmine bromide nanoemulsion,PPNE) with water in oil and study its release in vitro and the absorption kinetics of various gastrointestinal segments. Methods three kinds of PBS (pH 7.4 ~ 7.8) and HCl (pH 1.2) with different concentrations of pH were used as drug release media, and the drug release curves in vitro were determined and drawn. The absorption behavior of pyridostigmine bromide,PB and PPNE in gastrointestinal tract was compared with in vivo unidirectional intestinal perfusion model. Results in the four release media, the release rate of PB was faster than that of PPNE. The absorption rate constant (K _ a) and apparent osmotic coefficient (P _ (app) of PPNE were higher than those of PB in duodenum, jejunum, ileum and colon. By t test, PB and PPNE were statistically significant in 4 intestinal segments (P0.05). Conclusion PPNE can increase the bioavailability of drugs and increase the absorption of the drugs in the intestinal segment in vivo, and the drug release in vitro has a good sustained release effect.
【作者单位】： 重庆医科大学重庆高校药物工程研究中心;
【基金】：重庆市科委资助项目(Nocstc2015jcyjBX2007)
【分类号】：R965
【参考文献】
相关期刊论文 前8条
1 罗见春;何丹;杨梅;吴建勇;张景R，
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