School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, P.R. China.
J Microencapsul. 2012;29(7):657-65. doi: 10.3109/02652048.2012.680508. Epub 2012 Apr 25.
Andrographolide has a low aqueous solubility and oral bioavailability, which limits its clinical application. Reform the dosage forms of andrographolide to improve its aqueous solubility and oral bioavailability. The formulation, characterisation, stability, anti-inflammatory effect, pharmacokinetics and oral toxicity of andrographolide-loaded microemulsion, were studied. An formulation of O/W microemulsion consisting of an oil phase of isopropyl myristate, a surfactant phase of Tween 80, a co-surfactant of alcohol, and water was found to be ideal, with mean droplet size of 15.9 nm, a high capacity of solubilisation for andrographolide (8.02 mg mL(-1)). Such an andrographolide-loaded microemulsion is stable by monitoring the time, temperature and gravity-dependent change, and has a much better anti-inflammatory effect and a higher biological availability than andrographolide tablets. Besides, it also shows a very low acute oral toxicity. The andrographolide-loaded microemulsion is a promising dosage form of andrographolide.
穿心莲内酯的水溶性和口服生物利用度较低，限制了其临床应用。通过改变穿心莲内酯的剂型来提高其水溶性和口服生物利用度。本文研究了载穿心莲内酯微乳的处方、特征、稳定性、抗炎作用、药代动力学和口服毒性。结果表明，以肉豆蔻异丙酯为油相、吐温 80 为表面活性剂、醇为助表面活性剂、水为水相的 O/W 微乳为理想处方，平均粒径为 15.9nm，对穿心莲内酯的增溶能力高（8.02mg/mL）。通过监测时间、温度和重力依赖性变化，发现载穿心莲内酯微乳是稳定的，其抗炎作用和生物利用度明显优于穿心莲内酯片，且急性口服毒性很低。载穿心莲内酯微乳是一种有前途的穿心莲内酯剂型。
