Ultrasound assisted the enzymolysis of ginsenosides to prepare pare ginseng saponin Compound K / 中国中药杂志

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.

Study on pharmacokinetics of 20 (S) -protopanaxadiol lipid cubic nanoparticles / 中国中药杂志

<p><b>OBJECTIVE</b>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.</p><p><b>METHOD</b>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.</p><p><b>RESULT</b>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%.</p><p><b>CONCLUSION</b>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.</p>

Discussion on correlation between preparation, in vivo conversion process and potential structure-activity relationship of ginsenoside / 中国中药杂志

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.

Studies on tanshinone IIA solid dispersion based on chitosan / 中草药

Objective: To prepare and characterize the solid dispersion of tanshinone IIA (Tan IIA) using chitosan (CS) and compare the dissolution of solid dispersion using CS with different molecular weight (MW). Methods: Tan IIA solid dispersion was prepared by the solvent method with CS as the carrier. The physical characteristics and in vitro dissolution of solid dispersion prepared by different MW of CS and different proportions of drug and carrier were further evaluated. Results: The ideal Tan IIA solid dispersion was prepared under the condition as follows: the weight ratio of Tan IIA-CS (MW 3 000-5 000) was 1:9. The in vitro dissolution of Tan IIA solid dispersion reached up to 90% at 60 min. The differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) demonstrated that Tan IIA existed as amorphous state in carriers. Conclusion: The results indicate that in vitro dissolution of Tan IIA is improved greatly by the solid dispersion with CS as the carrier. As a new type of solid dispersion carrier of Tan IIA, CS has its practical value.

Study on preparation and in vitro characteristics of ginsenoside Rg3 binary solid dispersion / 中国中药杂志

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.

Polybasic research on the biopharmaceutical characteristics of 20 (S)-protopanaxadiol / 药学学报

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.

Studies on sustained release solid dispersion of tripterine carried by HPMC-stearic acid / 中国中药杂志

<p><b>OBJECTIVE</b>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.</p><p><b>METHOD</b>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.</p><p><b>RESULT</b>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.</p><p><b>CONCLUSION</b>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.</p>

Response surface method optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis preparation genistein / 药学学报

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.