目的 考察原人參二醇納米混懸劑的在體腸吸收特征。方法 采用溶劑蒸發(fā)法, 以白蛋白作為穩(wěn)定劑制備原人參二醇納米混懸劑。以酚紅為標(biāo)示物, 采用大鼠在體單向腸灌流法評(píng)價(jià)原人參二醇納米混懸劑的大鼠在體腸吸收特性。結(jié)果 Zetasizer nano ZS儀測(cè)得原人參二醇納米混懸劑平均粒徑為(220±10)nm, Zeta電位為(-28±0.2)mV。腸吸收實(shí)驗(yàn)表明, 原人參二醇納米混懸劑在整個(gè)腸段都有吸收, 且吸收速率常數(shù)(K_a)與滲透系數(shù)(P_eff)均大于原人參二醇原藥(P<0.05), 原人參二醇納米混懸劑在小腸段(十二指腸、空腸和回腸)的K_a與P_eff均大于結(jié)腸(P<0.05)。結(jié)論 原人參二醇納米混懸劑能夠有效促進(jìn)原人參二醇的大鼠在體腸吸收, 其轉(zhuǎn)運(yùn)機(jī)制可能為主動(dòng)轉(zhuǎn)運(yùn)或促進(jìn)擴(kuò)散。

Objective To investigate the rat intestinal absorption characters of protopanaxadiol (PPD) nanosuspensions (NPS). Methods PPD-NPS were made by using solvent evaporation method with bovinel serum albumin as carrier. The absorption of PPD-NPS were evaluated with phenol red as the marker by in situ single-pass perfusion model of rats. Results The mean diameter of the particle (220 ± 10) nm and the Zeta potential (-28 ± 0.2) mV were studied using Zetasizer nano ZS instrument. The result of rat intestinal absorption indicated that the absorption of PPD-NPS was observed in the whole intestinal tract. The absorption constant (K_a) and the effective absorption coefficient (P_eff) of PPD-NPS were higher than those of the bulk drug (P<0.05), the K_a and P_eff of PPD-NPS at small intestine (duodenum, jejunum, and ileum) were higher than those at colon (P<0.05). Conclusion PPD-NPS can improve the absorption of PPD in rat intestine. The transport mechanism may be active transport or facilitated diffusion.

國(guó)家自然科學(xué)基金(NO 81102813);黑龍江中醫(yī)藥大學(xué)重點(diǎn)實(shí)驗(yàn)室開(kāi)放課題(2013kf05)