Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China.
J Pharm Sci. 2011 Mar;100(3):933-41. doi: 10.1002/jps.22333. Epub 2010 Sep 22.
The main objective of the study was to investigate the efficacy of microemulsion (ME) to facilitate bioavailability of puerarin (PUE) after oral and nasal administration. The pseudo-ternary phase diagrams were constructed to screen the ME components and optimize the ME formulation. The optimized formulation for bioavailability assessment consisted of 20% Tween 80, 20% glycerin, and 1.6% ethyl oleate. The solubility (27.8 mg/mL) of PUE in ME was significantly improved compared to that (4.58 mg/mL) of crude PUE in water. The ME droplets were spherical with a mean particle diameter of 23.4 nm. After nasal (5 mg/kg) and oral (20 mg/kg) administration of a single dose of PUE as ME to fasted rabbits, the absolute bioavailability was 34.58% and 13.54%, respectively. It showed a shorter T(max) (0.75 h) for nasal administration than that (1.0 h) for oral administration of PUE-loaded ME. The C(max) of PUE-loaded ME was 0.55 μg/mL after nasal administration and 0.64 μg/mL after oral administration, respectively. The results showed that nasal administration might be a promising route to enhance the absorption of PUE in the form of ME.
本研究的主要目的是研究微乳（ME）在口服和鼻内给药后促进葛根素（PUE）生物利用度的效果。构建伪三元相图以筛选 ME 成分并优化 ME 配方。用于生物利用度评估的优化配方由 20%吐温 80、20%甘油和 1.6%油酸乙酯组成。与粗 PUE 在水中的溶解度（4.58mg/mL）相比，PUE 在 ME 中的溶解度（27.8mg/mL）显著提高。ME 液滴呈球形，平均粒径为 23.4nm。经鼻（5mg/kg）和口服（20mg/kg）给予单剂量 PUE 作为 ME 给禁食兔后，绝对生物利用度分别为 34.58%和 13.54%。与口服 PUE-载 ME（1.0h）相比，其鼻腔给药的 T（max）（0.75h）更短。鼻内给予 PUE-载 ME 的 C（max）为 0.55μg/mL，口服给予 PUE-载 ME 的 C（max）为 0.64μg/mL。结果表明，鼻内给药可能是一种有前途的途径，可增强以 ME 形式存在的 PUE 的吸收。
