Pharmaceutical Research Of Indirubin Self-microemulsifying Drug Delivery System

Indirubin for the active ingredients of Chinese herbs, such as Indigo, has anti-inflammatory, anti-tumor effects, clinical trial for the treatme myelogenous leukemia. But due to the low oral bioavailability, slow onset and other issues, which greatly limits their clinical application.The self-micro emulsifying technology used in this paper aiming at enhancing its oral bioavailability, providing the theoretical basis and references for new formulations, insoluble drugs and SMEDDS research.The optimum prescription was1944CS:EL:Trans P=25:80:19.47(m:m:m), drug loading was(553.26±1.56) μg/g, emulsification time was (3.26±0.06) min, particle sizes was (41.19±0.49) nm, compared to indirubin its solubility increased at least97.39times, and in good quality evaluation.Indirubin SMEDDS rat gastrointestinal absorption results:Stomach and the throughout intestinal paragraph are has absorption, stomach Department speculated for passive proliferation mechanism; intestinal paragraph absorption trend for duodenal> jejunum> colon> ileum, exists concentration saturated inhibition phenomenon, presumably facilitated diffusion or active transport mechanism, not excluded absorption exists enterohepatic cycle; absorption inhibitor studies show indirubin SMEDDS not MRP2substrate, which may be P-gp substrates, and needs energy.Indirubin SMEDDS and raw liquid in rats in vivo pharmacokinetic study display: Rats fed indirubin SMEDDS and raw liquid AUC oâ†'48were202.969and114.4μg·h·L-1;AUC0â†'∞were211.295and134.109μg·h·L-1;Cmax were22.35and5.4μg·L-1;Tmax were2and15h; The relative bioavailability was1.58times of the raw liquid of indirubin.In summary, this research preparation of SMEDDS studies confirmed significant improvement in solubility and oral bioavailability of indirubin, achieve research goals.