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采用亚微米乳剂给药系统降低葛根素溶血副作用的研究。

The study to reduce the hemolysis side effect of puerarin by a submicron emulsion delivery system.

作者信息

Yue Peng-Fei, Hai-Long Yuan Hai-Long, Zhu Wei-Feng, Cong Long-Bo, Xie Huan, Liu Zhi-Guo, Wang Lu-Jun, Xiao Xiao-He

机构信息

302 Hospital of PLA&PLA Institute of Chinese Materia Medica, Beijing, China.

出版信息

Biol Pharm Bull. 2008 Jan;31(1):45-50. doi: 10.1248/bpb.31.45.

Abstract

A safe and effective delivery system with a submicron emulsion for puerarin was studied. Puerarin submicron emulsion was prepared by a novel complex-phase inversion-high press homogenization technology. The mechanism to reduce the hemolysis side effect of puerarin was studied by blood cell counts in rabbits. The average diameter, zeta potential and entrapment efficiency of the emulsion prepared was 198.14+/-8.61 nm, -29.45+/-1.47 mV, 87.32+/-0.34%, respectively. Compared with control group, the red blood cell values, packed cell volume, plasma hemoglobin level, haptoglobin level and osmotic fragility of puerarin i.v. group was significantly different (p<0.05) at 42, 43 d, respectively. The blood cell parameter values of puerarin submicron emulsion group were not significantly different (p>0.05) in contrast to control group. Such observations indicated that the intravascular hemolysis occurred at 42, 43 d in puerarin i.v. group rabbits, the hemolysis did not occur for puerarin emulsion group rabbits. As an explanation for these results, it was proposed that the puerarin was either incorporated into the lipophilic core or intercalated between the phospholipid molecules at the interface. It could be concluded that puerarin submicron emulsions prepared markedly reduced the hemolysis effect of puerarin.

摘要

研究了一种用于葛根素的具有亚微米乳液的安全有效的给药系统。采用新型复相相转变-高压均质技术制备葛根素亚微米乳液。通过家兔血细胞计数研究降低葛根素溶血副作用的机制。所制备乳液的平均直径、ζ电位和包封率分别为198.14±8.61nm、-29.45±1.47mV、87.32±0.34%。与对照组相比,葛根素静脉注射组在第42、43天时红细胞值、红细胞压积、血浆血红蛋白水平、触珠蛋白水平和渗透脆性有显著差异(p<0.05)。葛根素亚微米乳液组的血细胞参数值与对照组相比无显著差异(p>0.05)。这些观察结果表明,葛根素静脉注射组家兔在第42、43天时发生血管内溶血,而葛根素乳液组家兔未发生溶血。作为对这些结果的解释,有人提出葛根素要么被纳入亲脂性核心,要么插入界面处的磷脂分子之间。可以得出结论,所制备的葛根素亚微米乳液显著降低了葛根素的溶血作用。

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