Davidsonhughes1242

Three phenylpropanoid glycosides were purified by extensive chromatographic techniques including column chromatography over microporous resin, MCI, diol, sephadex LH-20, reverse phase C_(18) from water-extracts of Sophorae Tonkinensis Radix et Rhizoma. Their planar structures were elucidated by combination of various spectroscopic method, such as IR, UV, MS, and NMR. The absolute configuration of aglycone was determined by quantum chemical calculations. Their structures were elucidated as(8R)-3-(4-hydroxyphenyl)-1-propanol-2-O-β-D-glucopyranoside(1), kalopanaxin D(2),(E)-4-hydroxycinnamyl alcohol 4-O-[2'-O-β-D-apiofuranosyl(1″→2')]-β-D-glucopyranoside(3). Compound 1 was undescribed previously. Compounds 2 and 3 were firstly isolated from Sophora genus.At present, there are many difficulties in the development and production of traditional Chinese medicine(TCM) tablets. This work aimed to explore the feasibility of improving dissolution difficulty and large dosage of TCM tablets by co-spray drying TCM extract with a small amount of pore-foaming agent ammonium bicarbonate. A series of porous Fagopyri Dibotryis Rhizoma powders were prepared by co-spray drying Fagopyri Dibotryis Rhizoma with different amounts of ammonium bicarbonate, and their powder pro-perties and tablet properties were comparatively investigated. At the same time, Fagopyri Dibotryis Rhizoma commercial tablets and raw material tablets were used as control drugs, the improvement degree of its compressibility and dissolution rate was investigated. The results showed that there were higher porosity, specific surface area and hollow spheroidal particles structure of powders via co-spray drying Fagopyri Dibotryis Rhizoma with NH_4HCO_3. Compared to parent and commercial Fagopyri Dibotryis Rhizoma tablets, the dissolution rates and compressibility of porous Fagopyri Dibotryis Rhizoma tablets were significantly increasing. High compressibility could increase drug loading by reducing excipients in manufacturing of tablets and lower the dose of Fagopyri Dibotryis Rhizoma tablets.Evaporative light scattering detector(ELSD) and charged aerosol detector(CAD) methods were established in this study for the content determination of four kinds of sugars in Zhusheyong Yiqi Fumai(YQFM), and the factors affecting the accuracy of CAD methods were discussed. HPLC-ELSD chromatographic separation was performed on a Shodex Asahipak NH2 P-50 column with acetonitrile-water(75∶25)as the mobile phase, with a flow rate of 0.8 mL·min~(-1), drift tube temperature of 80 ℃. The analysis by HPLC-CAD was performed on the same column with acetonitrile-water as mobile phase for gradient elution, with a flow rate of 0.8 mL·min~(-1), a neb temperature of 45 ℃, and power function(PF) of 1.3. The samples of YQFM were detected by ELSD and CAD respectively. It was found that YQFM was composed of fructose, glucose, sucrose and maltose. The linear relationship of the two methods was good, and the recoveries, reproducibility and stability of these four kinds of sugars measured by the two methods satisfied the requirements of methodology. Both CAD and ELSD detectors were accurate and reliable in detecting saccharides components in YQFM. In addition, it was revealed in this study for the first time that the PF parameter of CAD had an important influence on the accuracy of sugar determination and acted as the key parameter of CAD method. It was also found that for CAD, a non-linear detector, there was no significant difference between the results of linear regression and logarithmic regression.To prepare a new dosage form that can improve the drug loading of the film--ginkgolide B nanosuspension lyophilized powder orodispersible film(GB-NS-LP-ODF) and to evaluate its quality. Firstly, ginkgolide B nanosuspension(GB-NS) was prepared by media milling method, and then ginkgolide B nanosuspension lyophilized powder(GB-NS-LP) was prepared with freeze-drying method. The mannitol was used as lyoprotectant and its dosage was also investigated. find more GB-NS-LP-ODF was prepared by solvent casting method and its formulation was screened by single factor test method and optimized by orthogonal test. The appearance, mechanical properties, content uniformity and in vitro dissolution of the optimized GB-NS-LP-ODF were investigated. The particle size of prepared GB-NS was about 201 nm, and the optimal dosage of mannitol was 8%. According to the optimal formula, the GB-NS-LP-ODF was prepared with GB-NS-LP 35.6%, PVA 0588 49.4%, PEG 400 10.7% and CMS-Na 4.3%, and completely disintegrated in about 30 s, and the particle size of reconstituted GB nanoparticles from ODF was about 210 nm. The film with smooth appearance and good mechanical properties was stable within 30 days and the content uniformity(A+2.2 S<15) conformed to the regulations. Scanning electron microscope(SEM) showed that GB-NS-LP-ODFs were evenly distributed and the particle size was about 200 nm. X-rays diffraction(XRD) showed that its crystallinity was significantly lower than that of GB raw drug and GB-ODF. The results of in vitro release test showed that the drug film was completely dissoluted within 10 minutes. These results indicated that nanosuspension lyophilized powder was prepared by freeze drying of nanosuspensions, and then loaded into the orodispersible film to effectively increase the drug loading of the ODF and have broad application prospects.Orthogonal experiments were used to optimize the process parameters of curcumin TPP-PEG-PCL nanomicelles; the particle size, electric potential and morphology under the electron microscope were systematically detected for the curcumin TPP-PEG-PCL nanomicelles; and the stability and in vitro release of the curcumin TPP-PEG-PCL nanomicelles were investigated. With DID fluorescent dye as the fluorescent probe, flow cytometry was used to study the uptake of nanomicelles by breast cancer cells, and laser confocal microscopy was used to study the mitochondrial targeting and lysosomal escape functions of nanomicelles. Under the same dosage conditions, the effect of curcumin TPP-PEG-PCL nanomicelles on promoting the apoptosis of breast cancer cells was evaluated. The optimal particle size of curcumin TPP-PEG-PCL nanomicelle was(17.3±0.3) nm, and the Zeta potential was(14.6±2.6) mV in orthogonal test. Under such conditions, the micelle appeared as regular spheres under the transmission electron microscope. Fluorescence test results showed that TPP-PEG-PCL nanomicelles can promote drug uptake by tumor cells, escape from lysosomal phagocytosis, and target the mitochondria.