【摘要】：目的制備油包水型溴吡斯的明新型納米乳(novel pyridostigmine bromide nanoemulsion,PPNE),研究其體外釋放規(guī)律及各胃腸段吸收動力學特征。方法選用3種不同濃度pH 6.8、pH 7.4、pH 7.8的PBS以及pH 1.2的HCl作為釋藥介質,測定并繪制其體外釋藥曲線;并采用在體單向腸灌流實驗模型,比較溴吡斯的明(pyridostigmine bromide,PB)和PPNE在胃腸道的吸收行為。結果在4種釋放介質中,PB釋放速率較快,而PPNE釋放速率相對減緩;PPNE的吸收速率常數(shù)(K_a)和表觀滲透系數(shù)(P_(app))較PB在十二指腸、空腸、回腸、結腸段中均增加。經t檢驗,PB和PPNE在4個腸段均有統(tǒng)計學意義(P0.05)。結論 PPNE可提高藥物的生物利用度,明顯提高其藥物在體腸段的吸收;體外釋放中有良好的緩釋效果。
[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.
【作者單位】： 重慶醫(yī)科大學重慶高校藥物工程研究中心;
【基金】：重慶市科委資助項目(Nocstc2015jcyjBX2007)
【分類號】：R965

【參考文獻】

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