[Prediction of PAHs Content in Soil Around Gas Stations in Beijing Based on BP Neural Network].

With the rapid development of urbanization in China, the number of gas stations in cities is increasing. The composition of oil products in gas stations is complex and diverse, and a series of pollutants will be generated in the process of oil diffusion. Polycyclic aromatic hydrocarbons (PAHs) produced by gas stations can pollute the nearby soil and affect human health. In this study, soil samples (0-20 cm) near 117 gas stations in Beijing were collected, and the contents of seven PAHs were analyzed. Based on the BP neural network model, the contents of PAHs in soil of Beijing gas stations in 2025 and 2030 were predicted. The results showed that the total concentrations of the seven PAHs were 0.01-3.53 mg·kg-1. The concentrations of PAHs were lower than the soil environmental quality risk control standard for soil contamination of development land (Trial) GB 36600-2018. At the same time, the toxic equivalent concentrations (TEQ) of the above seven PAHs were lower than the standard value (1 mg·kg-1) of the World Health Organization (WHO), which they indicate a lower risk to human health. The prediction results showed that the rapid development of urbanization had a positive correlation with the increase in soil PAHs content. By 2030, the content of PAHs in Beijing gas station soil will continue to grow. The predicted concentrations of PAHs in the soil of Beijing gas stations in 2025 and 2030 were 0.085-4.077 mg·kg-1and 0.132-4.412 mg·kg-1, respectively. The contents of seven PAHs were lower than the soil pollution risk screening value of GB 36600-2018; however, the concentration of PAHs increased over time.The contents of PAHs in Chaoyang, Fengtai, and Haidian were relatively higher, which requires further attention.

[Ultrasound assisted the enzymolysis of ginsenosides to prepare pare ginseng saponin Compound K].

To prepare ginseng saponin Compound K with ultrasound-assisted total zymolytic ginseng saponins. The conversion rate was taken as the index to detect the pre-treatment factors such as ultrasonic power and ultrasonic time, as well as the impact of enzymatic factors, such as pH value, temperature, concentration of substrate, dosage of enzyme and reaction time, on the conversion rate. The response surface method was used to optimize the preparation conditions. The enzymolytic products were identified with MS, 1H-NMR and 13C-NMR. The results showed that the optimum conditions of the ultrasound-assisted enzymolysis were 250 W for ultrasonic power, 15 min for ultrasonic time, 5.5 for enzymolytic pH, 50 degrees C for enzymolytic temperature, 36 h for enzymolytic time, 4:5 for enzymolytic dosage: substrate and 1.0 g x L(-1) for concentration of substrate. The relative molecular mass of reaction products was 622.4. Therefore, the nuclear magnetic map verified that the reaction product was rare ginseng saponin Compound K. Under the above conditions, based on the total zymolytic ginseng saponins, the conversion rate of rare ginseng saponin Compound K was 6.91% in proportion to the total of ginsenosides. The process features gentle reaction conditions, high conversion rate and simple and reliable process, which is suitable for industrial production.

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles.

We prepared solid dispersions (SDs) of tanshinone IIA (TSIIA) with silica nanoparticles, which function as dispersing carriers, using a spray-drying method and evaluated their in vitro dissolution and in vivo performance. The extent of TSIIA dissolution in the silica nanoparticles/TSIIA system (weight ratio, 5:1) was approximately 92% higher than that of the pure drug after 60 minutes. However, increasing the content of silica nanoparticles from 5:1 to 7:1 in this system did not significantly increase the rate or extent of TSIIA dissolution. The physicochemical properties of SDs were investigated using scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and Fourier transforms infrared spectroscopy. Studying the stability of the SDs of TSIIA revealed that the drug content of the formulation and dissolution behavior was unchanged under the applied storage conditions. In vivo tests showed that SDs of the silica nanoparticles/TSIIA had a significantly larger area under the concentration-time curve, which was 1.27 times more than that of TSIIA (P < 0.01). Additionally, the values of maximum plasma concentration and the time to reach maximum plasma concentration of the SDs were higher than those of TSIIA and the physical mixing system. Based on these results, we conclude that the silica nanoparticle based SDs achieved complete dissolution, increased absorption rate, maintained drug stability, and showed improved oral bioavailability compared to TSIIA alone.

[Polybasic research on the biopharmaceutical characteristics of 20 (S)-protopanaxadiol].

In this study, the biopharmaceutical properties of 20 (S)-protopanaxadiol (PPD) were studied. Firstly, the equilibrium solubility and apparent oil/water partition coefficient of PPD were used to predict the absorption in vivo. Meanwhile the membrane permeability and absorption window were studied by Caco-2 cell model and single-pass intestinal perfusion model. Furthermore, the bioavailability and metabolism were combined to study the absorption properties and metabolic properties in vivo. All of them were used to provide theoretical and practical foundation for designing PPD preparation. The results showed that PPD is poorly water-soluble, and the equilibrium solubility in water is only 35.24 mg x L(-1). The oil-water partition coefficient is 46.21 (logP = 1.66). By Caco-2 cell model, the results showed PPD uptake in general, and it also has efflux. By in situ intestinal perfusion model, the results showed that the absorption of PPD in the intestine is good, and the effective permeability coefficient were duodenum > jejunum > ileum > colon. The oral bioavailability of PPD was 29.39%. It was not well. Metabolic studies showed PPD in vivo presented a wide spread metabolism. So the main factors that restricted oral bioavailability of PPD were the poor solubility and first-pass effect.

[Study on pharmacokinetics of 20 (S) -protopanaxadiol lipid cubic nanoparticles].

OBJECTIVE: To establish a high-performance liquid chromatographic/tandem mass spectrometry (HPLC-MS/MS) method for determining 20(S)-protopanaxadiol (PPD) in rat plasma, in order to analyze pharmacokinetic characteristics of PPD and PPD cubic nanoparticles. METHOD: Sprague-Dawley rats were administered orally with PPD and PPD cubic nanoparticles, respectively. Their blood samples were obtained from fossa orbitalis at regular time points. The mobile phase was 0.05% formic acidac etonitrile-0.05% formic acidac water (95:5). Electrospray ionization (ESI) was adopted for the quadrupole tandem mass spectrum. SCAN mode was used for the quantitative analysis, with m/z 460. 4/425.3 and m/z 622.9/318.3 (Rh2, interior label) as secondary fragment ions. The concentration of PPD in plasma was analyzed. The concentration-time curve was mapped. The data were calculated by DAS program. RESULT: The linearity of the PPD plasma concentration determination method ranged between 10-1 407 microg x L(-1), with the limit of quantification of 2.5 microg x L(-1). Both of the inter-day and intra-day precisions (RSD) were less than 13.25%, and the accuracy (relative error) was between +/- 8.50%. CONCLUSION: The method was so highly specific and sensitive with less plasma that it is suitable for pharmacokinetic studies. The prepared 20(S)-protopanaxadiol lipid cubic nanoparticles can enhance its absorption in vivo. Its relative bioavailability is 166% of the raw material.

Enhanced dissolution and oral bioavailability of tanshinone IIA base by solid dispersion system with low-molecular-weight chitosan.

OBJECTIVES: The aim of this study is to improve the dissolution and oral bioavailability of tanshinone IIA (TAN). METHODS: Solid dispersions of TAN with low-molecular-weight chitosan (LMC) were prepared and the in-vitro dissolution and in-vivo performance were evaluated. KEY FINDINGS: At 1 h, the extent of dissolution of TAN from the LMC-TAN system (weight ratio 9 : 1) increased about 368.2% compared with the pure drug. Increasing the LMC content from 9 : 1 to 12 : 1 in this system did not significantly increase the rate and the extent of dissolution. Differential scanning calorimetry, X-ray diffraction and scanning electron microscopy demonstrated the formation of amorphous tanshinone IIA and the absence of crystallinity in the solid dispersion. Fourier transform infrared spectroscopy revealed that there was no interaction between drug and carrier. In-vivo test showed that LMC-TAN solid dispersion system presented significantly larger AUC0-t , which was 0.67 times that of physical mixtures and 1.17 times that of TAN. Additionally, the solid dispersion generated obviously higher Cmax and shortened Tmax compared with TAN and physical mixtures. CONCLUSIONS: In conclusion, the LMC -based solid dispersions could achieve complete dissolution, accelerated absorption rate and superior oral bioavailability.

[Discussion on correlation between preparation, in vivo conversion process and potential structure-activity relationship of ginsenoside].

Ginseng is one of traditional Chinese medicines widely used worldwide according to the theory that "food and medicine share the same origin". Its main active ingredients are believed to be ginsenoside. In the past decades, studies on their chemical structure and pharmacological activity have made significant progress. So far, however, there is not a specific describtion on ginseng preparation and in vivo conversion process as well as an explanation on why rare ginsenoside can enhance anticancer activity. Therefore, this essay first describes the diversity of ginsenoside contained in ginseng, including natural ginsenoside, special ginsenoside generated from preparation and bioconversion processes. Subsequently, it summarizes the preparation and in vitro conversion processes, and discusses the potential structure-activity relationship between rare ginsenoside and its pharmacological activity. The study on the correlation between these chemical changes and their pharmacological activity help bring forth new ideas to the enhancement of anticancer activity of ginsenoside, and facilitate the development of new anticancer drugs.

[Study on preparation and in vitro characteristics of ginsenoside Rg3 binary solid dispersion].

With low molecular weight chitosan and poloxamer 188 as the joint carriers, ginsenoside Rg3 solid dispersions were prepared by using the solvent evaporation method for an in vitro dissolution test. Subsequently, differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray diffraction (X-RD) were adopted for a phase analysis. The results showed that the 60 min in vitro cumulative dissolution rate of ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 at the ratio of 2:1 exceeded 90%, and the drug was dispersed in carriers in an amorphous state. Therefore, ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 could help significantly improve the drug dissolution, with a practical application value.

[Response surface method optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis preparation genistein].

This article reports that nano-silica solid dispersion technology was used to raise genistein efficiency through increasing the enzymatic hydrolysis rate. Firstly, genistin-nano-silica solid dispersion was prepared by solvent method. And differential scanning calorimetry (DSC) and transmission electron microscopy (TEM) were used to verify the formation of solid dispersion, then enzymatic hydrolysis of solid dispersion was done by snailase to get genistein. With the conversion of genistein as criteria, single factor experiments were used to study the different factors affecting enzymatic hydrolysis of genistin and its solid dispersion. And then, response surface method was used to optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis. The optimum condition to get genistein through enzymatic hydrolysis of genistin-nano-silica solid dispersion was pH 7.1, temperature 52.2 degrees C, enzyme concentration 5.0 mg x mL(-1) and reaction time 7 h. Under this condition, the conversion of genistein was (93.47 +/- 2.40)%. Comparing with that without forming the genistin-nano-silica solid dispersion, the conversion increased 2.62 fold. At the same time, the product of hydrolysis was purified to get pure genistein. The method of enzymatic hydrolysis of genistin-nano-silica solid dispersion by snailase to obtain genistein is simple, efficiency and suitable for the modern scale production.

[Studies on sustained release solid dispersion of tripterine carried by HPMC-stearic acid].

OBJECTIVE: To prepare the sustained release solid dispersion of tripterine, using HPMC-stearic acid with the intention of improving drug dissolution and controlling drug releases moderate, so that the drug performances lower toxicity. METHOD: Tripterine sustained release solid dispersions was prepared by the solvent method with different weight ratios of HPMC-stearic acid and tripterine, which were dissolved in 95% ethanol. And in vitro dissolution experiment was conducted. Differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction can prove the formation of solid dispersions. RESULT: The ideal tripterine sustained release solid dispersions were prepared under the condition as follows, the weight ratio of tripterine and HPMC-stearic acid was 1: 10, and the release rate of drug can keep moderate and controllable. In vitro cumulative release of tripterine sustained release solid dispersion is up to more than 90% after 8 h, and the tripterine exist as amorphous in the solid dispersion. CONCLUSION: The sustained release solid dispersion of tripterine, carried by HPMC-stearic acid, can improve the release of tripterine effectively and controls the release rate keep moderate and controllable, and the preparation process is simple, which has potential applications.

Relationship between anti-oxidant activities and doxorubicin-induced lipid peroxidation in P388 tumour cells and heart and liver in mice.

1. The present study found that, compared with mouse heart and liver, P388 ascitic tumour had significantly lower superoxide dismutase (SOD) activity and that compared with the mouse liver, the heart had significantly lower SOD and catalase activities, as well as a lower glutathione content. 2. At 7.5 mg/kg, doxorubicin (DOX), a superoxide radical inducer, induced significant lipid peroxidation only in the tumour, whereas 15.0 mg/kg DOX induced lipid peroxidation in both the tumour and heart, but not in the liver. 3. Overall, the results of the present study suggest that the differential anti-oxidant activities in P388 ascitic tumour, heart and liver in mice may explain their differential responses and, hence, susceptibility to DOX-induced lipid peroxidation.

Dietary fish oil and vitamin E enhance doxorubicin effects in P388 tumor-bearing mice.

In this study, four kinds of rodent diets, CO, FO, CVe, and FVe, were used by addition of canola oil, oil mixture (fish oil + canola oil), canola oil plus vitamin E, and oil mixture plus vitamin E, respectively, to a basic diet, AIN-93G, to investigate the influence of dietary fish oil and vitamin E on doxorubicin (DOX) treatment in P388 ascitic mice. Animal life span (LS) and heart damage were recorded in mice fed the four different diets and treated with different doses of DOX. The optimal doses of DOX for antitumor effect as manifested by increased LS were 6.0 and 9.0 mg/kg. Both fish oil and vitamin E significantly enhanced this effect. On the other hand, DOX at 12.0 mg/kg induced severe heart damage, which was also significantly aggravated by both fish oil and vitamin E, as shown by both decreased LS and increased serum creatine phosphokinase activity. Fish oil and vitamin E appeared to enhance the antitumor effect of optimal doses of DOX but to aggravate cardiotoxicity owing to DOX overdose.