OBJECTIVE: To prepare Panax notoginseng saponins-loaded complex nano vesicles (PNS-CNV) with MPEG-PLGA nanoparticles as the core and investigate the physicochemical property of PNS-CNV and protective action on acute myocardial ischemia in rats. METHODS: Double emulsification-solvent evaporation method was used to prepare Panax notoginseng saponins-loaded nanoparticles using different molecular weight MPEG-PLGA (PNS-NP). Thin-film hydration method was applied to entrap PNS-NP as the core to form PNS-CNV. Ultrafiltration, transmission electron microscope, dynamic light scattering and electrophoretic light scattering were employed to study the entrapment efficiency of each index component in PNS and physicochemical parameters of PNS-CNV. Acute myocardial ischemia model in rats was established to investigate the protective effect of PNS-CNV. RESULTS: The molecular weight of MPEG-PLGA did not affect the entrapment efficiency, particle size and Zeta potential of PNS-CNV. The pharmacodynamic experiment indicated that comparing with PNS solution group, the SOD activity of rat myocardium in PNS-CNV group was elevated with markedly decreased H2O2, MDA and serum LDH activity (P<0.05). The protective effect of PNS-CNV with MPEG5000-PLGA was the most significant. CONCLUSION: CNV may be used as potential new oral drug delivery carriers.

Objective: To study the enzymatic reaction kinetics of dl- tetrahydropalmatine (TET) in total alkaloid (TA) of Corydali Rhizoma in rat liver microsomes and to investigate the compatible effects of the effective components such as coumarin (Cou) and volatile oil (VO) in Angelicae Dahuricae Radix with TA in Corydali Rhizoma on enzymatic reaction kinetics of TET. Methods: Rat liver microsomes were prepared by ultracentrifugation and the TET concentration in incubation medium was determined by HPLC. Comparative study on the enzymatic reaction kinetics of TET in each group of TA, TA-Cou, TA-VO, and TA-Cou-VO to deduce the michaelis constant (Km) and maximum reaction rate (Vmax) of TET in each group and calculate the clearance rate (CLint) of TET in each group. Results: The Km, V max, and CLint in TA group were 0.12 μmol/ (L·min·mg), 5.40 μmol/L, and 0.022 L/(min·mg), respectively; In TA-Cou group they were 0.27 μmol/(L·min·mg), 40.18 μmol/L, and 0.006 L/(min·mg), respectively; In TA-VO group they were 0.57 μmol/(L·min·mg), 22.60 μmol/L, and 0.025 L/(min·mg), respectively; In TA-Cou-VO they were 0.84 μmol/(L·min·mg), 23.25 μmol/L, and 0.036 L/(min·mg), respectively. Conclusion: The effective components of TA in Corydali Rhizoma with Cou and VO in Angelicae Dahuricae Radix could decrease CLint of TET in TA of liver.

Objective: Comparing the powder characteristics and dissolution rate between common powder and micropowder of Drynariae Rhizoma to provide experimental evidence for the micropowder application and the control of paticle size. Methods: Particle size and distribution, hygroscopicity, and powder morphology of the powder characteristics and dissolution behavior were used to evaluate the impact of particle size on powder characteristics and dissolution of Drynariae Rhizoma powders. Results: There were significant differences between common powder and micropowder in powder characteristics and dissolution rate. In addition to the micropowder III, the dissolution rates and the concentrations of naringin in micropowders were higher than those in the common powder of Drynariae Rhizoma. Conclusion: An appropriate degree of micronization is helpful for the dissolution of the active components in Drynariae Rhizoma and the application of micronization technology to Drynariae Rhizoma is feasible. The particle diameter (D90) of the micropowders should be controlled in 61.4-23.5 μm.

It was difficult to prepare traditional Chinese medicine pellets due to the adverse characteristics of the herbal extract. In this study, Danshen extract (DS) powder mixed with different proportions of microcrystalline cellulose (MCC), lactose and starch were made into pellets by extrusion-spheronization. Particle size, span, bulk density, tapping density, compressibility, Hausner ratio and angle of repose were used to evaluate the micromeritic properties of mixing powders. Feret diameter, aspect ratio, yield, density and friability were used to evaluate the properties of the pellets. The correlations between micromeritic properties of raw material powders and the formability of their pellets were analyzed by cluster analysis, principal component analysis and partial least squares regression analysis. As a result, the particle size of the powders was negatively correlated with the size, density, yield, and was positively correlated with the friability of their pellets. The span, density, compressibility and angle of repose of the powders were positively correlated with the size, density, yield, and were negatively correlated with the friability of their pellets. So there were certain correlations between the micromeritic properties of raw material powders and the properties of their pellets prepared by extrusion-spheronization. This research provided a foundation for the technology and method of traditional Chinese medicine extract pellets.
Cellulose ; chemistry ; Drug Compounding ; methods ; Drug Implants ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Excipients ; chemistry ; Lactose ; chemistry ; Medicine, Chinese Traditional ; methods ; Particle Size ; Powders ; chemistry ; Starch ; chemistry

OBJECTIVETo establish an HPLC method for the simultaneous determination of three major bioactive components in Jingzhi Guizhi Fuling capsules namely laetrile, paeoniflorin and paeonol.

METHODA LiChrospher C18 column (4.6 mm x 250 mm, 5 microm) was used. The chromatography was carried out with a stepwise gradient programming. The mobile phase was acetonitrile-water (containing 0.1% phosphorous acid) and the flow rate was 1.0 mL x min.

RESULTThe linear range of laetrile was 12.87-102.94 micron x mL(-1), r = 0.999 9, paeoniflorin 24.84 - 198.7 microg x mL(-1), r = 0.9999 and paeonol 12.57-100.56 microg x mL(-1), r = 0.999 9. The method is accurate with variation less than 1.5 % and recovery more than 95 %.

CONCLUSIONThe method was successfully applied to analyze three major bioactive components in Jingzhi Guizhi Fuling capsules.

Acetophenones ; analysis ; Amygdalin ; analysis ; Benzoates ; analysis ; Bridged-Ring Compounds ; analysis ; Capsules ; Chromatography, High Pressure Liquid ; methods ; Cinnamomum ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Glucosides ; analysis ; Monoterpenes ; Paeonia ; chemistry ; Plants, Medicinal ; chemistry ; Polyporales ; chemistry ; Reproducibility of Results

OBJECTIVE: To investigate the relationship between the process parameters and granulation behavior during high shear granulation process. METHODS: Andrographis extract was utilized as a model drug and mixed with microcryslalline cellulose (MCC) or soluble starch at the ratio of 1:1 by weigh, respectively. The process parameters were selected according to fractional factorial experiment. The granules were prepared by using high shear granulation. The aggregation behavior was evaluated by granule yield and ratio of lumps and fine powder. The effect of process parameters on granulation behavior was analyzed through stepwise regression. Standard least squares regression analysis was used to establish the mathematical model of granule yield. RESULTS: The process parameters had different effects on the granulation behaviors of MCC and starch mixtures. The granule yield predicted by the fitting model was (66.66 ± 3.7)%, and the measured values for MCC and starch mixture were 68.9% and 66.1%, respectively. CONCULSION: The established mathematical model is useful in predicting the performance of materials duing high shear granulation process. Understanding the impact of process parameters on granulation behavior provides the basis of modulating granulation parameters in order to optimize product performance and improve the yield.

With the content of gallic acid, loganin, paeoniflorin and paeonol as the indexes, to screen out dissolution determination conditions, establish the dissolution determination method for multi-index components in Liuwei Dihuang concentrated pills, calculate and map the accumulative dissolution curve, and then compare the dissolution of products from different pharmaceutical factories through the similarity factor (f2). According to the results, the optimum dissolution determination conditions were the paddle method, with 250 mL 0.1 mol x L(-1) hydrochloric acid as the dissolution medium, and a rotation rate of 100 r x min(-1). The similarity factor values (f2) of the dissolution curves of the four main components of Liuwei Dihuang concentrated pills from different pharmaceutical factories were mostly less than 50. This demonstrated a significant difference in the dissolution of Liuwei Dihuang concentrated pills from different pharmaceutical factories, and provided scientific basis for improving the equality evaluation of Liuwei Dihuang concentrated pills.
Drugs, Chinese Herbal ; chemistry ; Humans ; Organic Chemicals ; analysis ; Quality Control ; Solvents ; chemistry

The impact of key physical properties on granulated products by the high-speed mixing wet method was studied. Andrographis extracts were utilized as the model drug. Four processing methods were adopted to prepare mixed powder of microcrystalline cellulose (MCC) and starch with the mass ratio 1:0.5, 1:1 and 1:2 by the high-speed mixing wet method. The properties of the prepared granules were evaluated with such indexes as granule yield, the ratio of lumps and fine powder, granule-AOR and granule-HR. The impact of key physical properties on granulated products was analyzed through stepwise regression analysis. The results showed that angle of repose, moisture content, pore volume, density and contact angle with water were key physical properties of the powder. The key physical properties of Chinese medical extracts powder are the important factor impacting granulated products made by the high-speed mixing wet method. In this study, the impact of key physical properties on granulated products of Chinese medical extracts was analyzed from the physical angle.
Andrographis ; chemistry ; Drug Compounding ; instrumentation ; methods ; Drugs, Chinese Herbal ; chemistry ; Particle Size ; Powders ; chemistry

Objective: To explore the dynamic distribution of moistening agent in Andrographis paniculata granule (APG) during the high shear wet granulation (HSG). Methods: A. paniculata extract was utilized as a model drug and mixed with microcrystalline cellulose (MCC) with the ratio of 1∶1.5 by weight. The granules were prepared using HSG with 60% ethanol as the moistening agent. Sodium fluorescein was incorporated as a tracer in the moistening agent in order to detect its distribution in the granules during the process. Results: The moistening agent was heterogeneously distributed at the beginning of the process, fractional powder was over wetted, meanwhile partial powder was not wetted, and granule size distribution was polarization. The moistening agent tended to be evenly distributed and the granule size distribution presented nearly unimodal distribution with the increase of granulation time. Conclusion: The distribution of moistening agent obeys the first-order kinetics model during HSG of APG.

To explore the mechanism of the absorption enhancement of Angelica dahurica extract (Ade), the absorption mechanism of baicalin in the Scutcllaria water extraction as well as the effect of Angelica dahurica extract on absorption of baicalin were investigated. In order to determine the main absorption site, everted intestinal sac model was used to study the effect of Angelica dahurica extract on the absorption of baicalin at duodenum, jejunum, ileum and colon. In situ single pass intestinal perfusion model was performed to study the absorption of various concentrations of baicalin and the effect of Angelica dahurica extract on the absorption of baicalin at the main absorption site. To authenticate the consequence of perfusion by getting the blood from the hepatic portal vein and determine the concentration of the baicalin in the blood. The result showed that baicalin could be absorbed at all of the four intestinal segments with increasing absorption amount per unit as follows: ileum > colon > jejunum > duodenum. The absorption ofbaicalin in the duodenum significantly increased with Angelica dahurica extract, thus, duodenum was chosen to be the studying site. Apparent permeability values (Papp) and absorption rate constant (Ka) of baicalin in the duodenum increased gradually with higher concentrations. When the concentration of baicalin rises to a certain degree, the absorption increase had a saturable process, the absorption of baicalin may be an active transportation. Baicalin may be not a substrate of P-gp as verapamil which had not significantly affected the Papp and Ka of baicalin. The absorption of baicalin in the duodenum significantly increased (P < 0.01) in the two models with Angelica dahurica extract and the concentration of baicalin in the blood from the hepatic portal vein showed that the Angelica dahurica extract can increase the absorption of baicalin.
Angelica ; chemistry ; Animals ; Drug Synergism ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Duodenum ; metabolism ; Flavonoids ; isolation & purification ; pharmacokinetics ; Herb-Drug Interactions ; Intestinal Absorption ; drug effects ; Intestines ; metabolism ; Male ; Perfusion ; Permeability ; Plants, Medicinal ; chemistry ; Portal Vein ; metabolism ; Rats ; Rats, Sprague-Dawley ; Scutellaria ; chemistry ; Verapamil ; pharmacology