Based On Nanoparticle Suspension Technology Difficult Soluble Active Ingredients Of Traditional Chinese Medicines Research Of Drug Delivery Systems

As we know, most of the active components extracted from the traditional Chinese herbs are low water solubility and low bioavailability. It has become a hot issues about how to improve their water solubility and bioavailability. As a new nanoparticle technique, nanosuspension is one of the prospective and effective method in the pharmaceutical industry because of its characteristic, the very high specific surface area, which can be expected to have a positive effect on the dissolution rate thus obtain the high bioavailability. Making use of nanosuspension technology in the study of the drug delivery systems is one of the best solution to increase the dissolution rate and absorption of poorly water soluble active components of traditional Chinese medicine.Herpetrione (PEDX), extracted from Herpetospermum caudigerum, is a novel and potent antiviral agent. However, due to poor water solubility, oral bioavailability of the drug is relatively low. In this paper, with PEDX as a model drug, using international advanced nanosuspension technology, study the drug delivery systems of poorly water soluble active components of traditional Chinese medicine, and provide industrialization demonstration for the nano-medicines of poorly water soluble active components of traditional Chinese medicine.Based on the investigation of the extraction and purification process, ultimately determining the best preparation of the PEDX is that add5times amount of80%alcohol, reflux-extracting for3times1hours each time,24hours after standing, filter, the filtrate recovered alcohol to have no alcohol flavor, put it aside for12hours, remove to the oil, and then use a4times amount of ethyl acetate, combine the ethyl acetate solution, vacuum concentrated at50℃, then add8times amount of ligroin and acetone to the obtained Herpetospermum caudigerum total lignans, separate PEDX using medium voltage preparation apparatus, the mobile phase consist of20parts ligroin,70parts ethyl acetate and10parts acetone, the DAD detector was set at the wave-length of240nm and the flow rate was120mL/min.In this paper, PEDX nanosuspension (PEDX-NS) were prepared by high pressure homogenization method. Through the study of preparation process, the final selection of the best preparation is that take PEDX3g, SDS0.6g, PVPK300.9g, add300ml of distilled water, stir and mix, after high-speed probe phacoemulsificated at 8000r/min for5times, prepare the PEDX-NS by high-pressure homogenization at1000bar for10times.In order to improve the stability of PEDX-NS, with appearance, change difference of size, and redispersion as the index, its solidification process was investigated. Finally, the results showed that the best solidification method is freeze-drying techniques.In this study, the freeze-dried PEDX nanoparticles were characterized in terms of morphology, size distribution, zeta potential, powder X-ray diffraction (PXRD) and in vitro dissolution rate. Results showed that a narrow size distributed nanosuspension with a mean particle size of286.3nm, a polydispersity index of0.183and a zeta potential of-26.9mV was obtained. The result of PXRD showed that PEDX was amorphous state in both coarse powder and nanosuspension. In the in vitro dissolution test, dissolution velocities of the freeze-dried PEDX nanosuspension powder were distinctly superior compared to the crude powder and physical mixture. Within60min, approximately86.87%of PEDX was dissolved from the freeze-dried PEDX nanosuspension. In contrast to this, only38.15%and48.37%were dissolved from the raw PEDX and physical mixture, respectively.In the in vivo study, PEDX pharmacokinetic process calculated by DAS2.0software was fitted to two-compartment model in rats, and compared with the raw PEDX, the nanosuspension had higher Cmax (144.96%higher), AUC0-∞>(125.76%higher) and shorter Tmax(50%shorter), which indicated PEDX nanosuspension was easier to be absorbed.In summary, nanosuspension can improve notably the dissolution rate and bioavailability of the poorly water soluble drug PEDX, and making use of nanosuspension technology in the study of the drug delivery systems is a effective method to increase the dissolution rate and absorption of poorly water soluble active components of traditional Chinese medicine.