Acetylation of Rehmannia glutinosa polysaccharides and antioxidant activity of acetylated derivatives / 中国中药杂志

This study aims to acetylate Rehmannia glutinosa polysaccharides by acetic anhydride method, optimize process parameters and evaluate their antioxidant activity. With the degree of substitution(D_s) as a criterion, the effects of reaction time, acetic anhydride-to-polysaccharides ratio and temperature were investigated. Process parameters were optimized by single-factor experiment and response surface methodology. The infrared spectroscopy(IR) and scanning electron microscopy(SEM) proved the successful acetylation and were employed to preliminarily analyze the structural characteristics of acetylated derivatives. The results showed that the D_s was 0.327 under the optimal technological conditions, including m(acetic anhydride):m(R. glutinosa polysaccharides)=2.70, reaction time 3.0 h and temperature 48 ℃. Further, the antioxidant properties of acetylated derivatives were investigated in vitro and acetylation was found effective to improve the antioxidant activity of R. glutinosa polysaccharides. This study provides a reference for the further development and application of R. glutinosa polysaccharides.

Quality evaluation of Aralia taibaiensis based on spectrum-activity relationship / 中国中药杂志

A spectrum-activity relationship is established with high performance liquid chromatography(HPLC) fingerprints and the in vitro antioxidant activity to improve the quality evaluation system of Aralia taibaiensis. The HPLC profiles of 12 batches of samples were collected, and the similarity evaluation, heat map analysis and principal component analysis were conducted for the chemometric study of the fingerprint data. Combined with grey correlation analysis, the contributions of the common peaks in the fingerprints to the antioxidant activity were clarified, and the important peaks reflecting the efficacy were identified. The results showed that 17 common peaks were found in 12 batches of A. taibaiensis samples, and 6 of them were identified as saponins. Similarity evaluation, heat map analysis and principal component analysis roughly classified the A. taibaiensis herbs into two categories, i.e.,(1) S1-S10, S12 and(2) S11. Twelve batches of samples showed different antioxidant activities in a dose-dependent manner. In particular, S9 had the strongest antioxidant activity, while S11 was the weakest in antioxidant capacity, which was basically consistent with the overall score results. The results of grey correlation analysis demonstrated that the 17 common peaks scavenged DPPH radicals in the following order: X_3>X_(17)>X_4>X_8>X_7>X_(13)>X_2>X_6>X_(11)>X_(10)>X_(16)>X_(12)>X_9>X_5>X_(14)>X_1>X_(15), and scavenged ABTS radicals in the order of X_4>X_3>X_7>X_8>X_2>X_(17)>X_(13)>X_6>X_(16)>X_(11)>X_5>X_(12)>X_(10)>X_9>X_(14)>X_1>X_(15). Among them, X_3, X_4, X_7(araloside C), X_8 and X_(17) were the important peaks reflecting the efficacy of A. taibaiensis, which were basically consistent with those contained in the principal component 1. In this study, the correlation between the HPLC fingerprints of 12 batches of A. taibaiensis and its antioxidant activity provides a reference for the Q-marker screening and quality control of A. taibaiensis.

Powder modificationfor improving content uniformity of Ziyin Yiwei Capsules / 中国中药杂志

Based on the defects in powder properties of the contents of Ziyin Yiwei Capsules, this study screened out the main medicinal slice powders causing the poor powdery properties, and introduced the powder modification process to improve the powdery properties of these slice powders, the pharmaceutical properties of the capsule contents, and the content uniformity of Ziyin Yiwei Capsules, so as to provide a demonstration for the application of powder modification technology to the preparation of Chinese medicinal solid preparations. Through the investigation on the powder properties of the contents of Ziyin Yiwei Capsules, it was clarified that the pulverized particle size of the capsule contents had a good correlation with the pulverization time. According to the measurement results of the powder fluidity and wettability, the quality defects of the capsule contents were caused by the fine powders of Taraxaci Herba and Lungwortlike Herba. "Core-shell" composite particles were prepared from medicinal excipients magnesium stearate and fine powders of Taraxaci Herba and Lungwortlike Herba slices after ultra-fine pulverization to improve the powder properties of the problematic fine powders. Powder characterization data including fluidity and wettability were measured, followed by scanning electron microscopy(SEM) and infrared ray(IR) detection. It was determined that the optimal dosage of magnesium stearate was 2%, and the compositing time was 3 min. The composite particles were then used as content components of the Ziyin Yiwei Capsules. The powder characteristics between the original capsule and the modified composite capsule including the particle size, fluidity, wettability, uniformity of bulk density, and uniformity of chromatism as well as the content uniformity and in vitro dissolution were compared. The results showed that the powder characteristics and content uniformity of the prepared composite capsule were significantly improved, while the material basis of the preparation was not changed before and after modification. The preparation process was proved to be stable and feasible. The powder modification technology solved the pharmaceutical defects that were easy to appear in the preparation of traditional capsules, which has provided experimental evidence for the use of powder modification technology for improving the quality of Chinese medicinal solid preparations and promoting the secondary development and upgrading of traditional Chinese medicinal dosage forms such as capsules.

Particle design for improving content uniformity of Hewei Jiangni Capsules / 中国中药杂志

Targeting the poor powder characteristics of the contents in Hewei Jiangni Capsules, this study characterized the powder properties of the contents and employed particle design technique for improving the content quality. The content composite particles of Hewei Jiangni Capsules prepared by the particle design technique were evaluated by scanning electron microscopy(SEM), followed by infrared ray(IR), content uniformity, and in vitro dissolution detection. It was found that there was a good correlation between the crushed particle size of slices and the crushing time, and the calcined Haematitum was responsible for the poor content uniformity. After the fine powder of calcined Haematitum was super-finely ground for 8.5 min and those of the other contents in the capsule for 1 min, they were prepared into the composite particles, whose property characterizations were compared with those of the physical mixtures. The content uniformity of the prepared composite particles was significantly improved, and the preparation process was stable and reliable. The adoption of particle design technology to correct the poor uniformity of the physical mixture, solve the pharmaceutical defects of Hewei Jiangni Capsules, and improve the quality of prescriptions has provided important reference for the clinical application and development of Chinese medicinal preparations.

Particle design for improving taste and homogeneity of traditional Chinese medicinal powder: taking Zhuhuang Chuihou Powder as an example / 中国中药杂志

Due to the complex source and different physical and chemical properties of traditional Chinese medicines(TCM) powder, there are many common pharmaceutical problems in its preparation, such as large particle size difference, poor mixing uniformity, and poor compliance with oral intake, which has directly affected the quality of solid preparations as well as their clinical efficacy and safety. This study observed the property of Zhuhuang Chuihou Powder and extract its pharmaceutical defects. It was found that realgar and calcined Borax in Zhuhuang Chuihou Powder were heavy in texture and toxic, and they were easy to be isolated, indicating the potential safety hazard. At the same time, Coptidis Rhizoma and Phellodendri Chinensis Cortex were the main sources of its bitterness. Therefore, based on the idea of "drug-excipients unity", the particle design technology was used to prepare core/shell-type composite particles with bitter medicines as the core and mineral medicines as shell. Both infrared spectroscopy and scanning electron microscopy results indicated the formation of composite particles, and the taste of these composite particles were improved. Compared with the physical mixtures, the composite particles exhibited significantly decreased RSD values in the content uniformity of berberine hydrochloride, arsenic disulfide, and sodium tetraborate and appearance uniformity. The introduction of particle design technology solved the problem of uneven dispersion of Zhuhuang Chuihou Powder, thus ensuring its uniform dispersion, stability, and control and improving the quality of the original preparation. This has provided a scientific basis for the quality control of TCM powder.

Application of design technology for preparing Lingzhu Powder particles based on solvent evaporation method / 中国中药杂志

Targeting the deficiencies of Lingzhu Powder, this study introduced the particle design technology to improve its quality. Based on the mechanism of particle design for powder and the characteristics of solvent evaporation method, composite particles consisting of Succinum, Cinnabaris, and artificial Bovis Calculus were prepared. And the powder properties of composite particles and physical mixtures as well as the content uniformity of toxic components were investigated for exploring the technological advantages of particle design in improving the quality of Lingzhu Powder. The results showed that the composite particles prepared using solvent evaporation method and particle design technology were micro-particles, and the stable agglomerate structure could be observed under SEM. Composite particles exhibited better fluidity and compliance in oral intake than physical mixtures. The differences in chromatism, bulk density, and content uniformity of the composite particles were smaller than those of physical mixtures, and the corresponding RSD values \[4.8%, 1.8%, 3.4%(bilirubin), and 0.63%(HgS), respectively\] were smaller. The solvent evaporation combined with particle design technology can be utilized to significantly improve the quality of Lingzhu Powder, which has provided new ideas for the optimization of the quality of traditional Chinese medicinal powder.

Application of particle design technology in field of traditional Chinese medicine powder / 中国中药杂志

Solid preparations account for more than 50% of traditional Chinese medicines(TCM). TCM powder is an important raw material for solid preparations of TCM. Its powder properties directly affect the quality of solid preparations, and even clinical safety and effectiveness. Particle design technology based on the characteristics of powder in TCM is an important means to improve and enhance the quality of solid preparations. This study summarized the relevant principles, methods, characteristics, classification, equipment, and other elements of particle design technology in recent years, analyzed the difficulties in its application in the field of TCM powder, and proposed the strategies in conjunction with the development of computer data mining. The present study is expected to provide a reference for the suitability of particle design in the field of TCM powder.

Study on Stability of Volatile Oil in Foeniculi Fructus and Screening Its Antioxidants in Accelerated Oxidation Environment / 中国实验方剂学杂志

Objective: To screen the accelerated oxidation environment with the most drastic changes in the volatile oil composition of Foeniculi Fructus, and to optimize the type and concentration of antioxidants. Method: The volatile oil of Foeniculi Fructus was extracted by steam distillation. Taking thiobarbituric acid reactive substances (TBARS) value and peroxide value (POV) as evaluation indexes, response surface method was used to investigate the effects of temperature, concentrations of ferrous ion (Fe2+) and azoamidine initiator V50 (AAPH) on volatile oil components of Foeniculi Fructus and its oxidation products. TBARS and POV were detected by ultraviolet chromatography. The oxidative environment with the most drastic changes of volatile oil composition of Foeniculi Fructus was screened. The type and concentration of antioxidants were selected by single factor experiments. The change discipline of volatile oil in Foeniculi Fructus after added different concentrations of antioxidants were analyzed by GC-MS. Result: The worst oxidizing environment for volatile oil of Foeniculi Fructus was as follows:temperature at 42.5℃,AAPH concentration of 1 g·L-1,Fe2+ concentration of 20.85 mg·L-1. Ascorbyl palmitate with concentrations of 0.2 mol·L-1 and 0.8 mol·L-1 could effectively improve the stability of volatile oil from Foeniculi Fructus. Conclusion: Under the accelerated oxidation environment, the terpenes in volatile oil from Foeniculi Fructus are significantly changed, but its stability can be improved by ascorbyl palmitate.

Extraction kinetics of volatile oil from galangal by steam distillation / 中国中药杂志

To reveal the extraction regularity of volatile oil from galangal by GC-MS analysis. The volatile oil in galangal was extracted by steam distillation. The extract was collected every 30 min, the oil part and the water part were separated. GC-MS was used to analyze the extraction liquid collected at different time periods. A total of 140 volatile components were obtained by GC-MS analysis. Among them, the main components were eucalyptus oil alcohol, alpha-pine oil alcohol and 4-terpene alcohol; 22 special components were dissolved in water, 77 special components were dissolved in oil and 41 components were dissolved in both oil and water. With the increase of specific components in water, the content of Eucalyptus in water increased in a linear manner. The increase of eucalyptus oil further promoted the dissolution or dispersion of alpha PN in water, and the change of specific components in oil was positively correlated with the content of Eucalyptus and alpha-terpilenol in oil. The results of principal component analysis show that the physical and chemical properties of the compounds were important factors affecting the distribution of components. PC1 (molecular weight, melting point, boiling point positive correlation), PC2 (negative correlation of refractive index) and PC3 (positive correlation of water solubility) were the main components that lead to the differences in composition distribution. The process of extracting volatile oil from galangal through steam distillation was affected by the physical and chemical properties of volatile components. Some components were specifically distributed in the fragrance and volatile oil system. The endemic components of aromatic water increased the content of the main components in the water system, which may lead to the "emulsification", reduction of the yield and low quality of the volatile oil.

Tissue distribution of araloside A in rats / 中国中药杂志

Araloside A is one of the main active ingredients of Aralia taibaiensis. In this study, HPLC-MS/MS analysis method of araloside A in the main organs of SD rats was established. At the same time, the content of araloside A in the main organs (heart, liver, spleen, lung, kidney, brain) after oral administration with araloside A (50 mg•kg⁻¹) were determined to explore the tissue distribution characteristics of araloside A in vivo. The results showed that the methodological study of araloside A in the main organs of SD rats met the requirements, araloside A distributed in heart, liver, spleen, lung, kidney and brain tissues reached peak at 1 h or 2 h after oral administration with 50 mg•kg-1.The distributions of araloside A at different time points after administration were distinct as follows： the content of araloside A at 20 min：liver>heart>spleen>lung>kidney>brain; the content of araloside A at 1 h： liver>spleen>kidney>lung>heart>brain; the content of araloside A at 2 h： liver>kidney>heart>spleen>lung>brain; the content of araloside A at 4 h： kidney>liver>spleen>heart>lung>brain; the content of araloside A at 8 h： spleen>heart>liver>kidney>lung>brain. Therefore, araloside A was mainly distributed in liver tissue, which had a certain correlation with the common use of Aralia taibaiensis in the treatment of hepatic disease. In addition, araloside A shows a low content but an obvious distribution in brain tissues, which indicates that the drug can pass through blood-brain barrier, and provides the basis for the study of araloside A in brain tissue.

Effects of treadmill exercise on central hemodynamics in patients below 60 years of age with coronary artery disease / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effects of treadmill exercise on central hemodynamics in patients with coronary artery disease.</p><p><b>METHODS</b>Sixty-eight consecutive patients below 60 years of age with the diagnosis of coronary artery disease (CAD) between July, 2013 and April, 2014 underwent treadmill exercise test following the standard Bruce protocol. Ninety-seven individuals without CAD served as the control group. Central hemodynamics of the subjects, including the central aortic blood pressure (cSBP), augmentation index (AI) and augmentation pressure (AP), were examined before and after the exercise.</p><p><b>RESULTS</b>cSBP increased significantly after acute exercise in both groups (P<0.001). Immediately after treadmill exercise, AI showed no significant changes in CAD patients (P=0.561) but decreased significantly in the control subjects (P<0.001). AI before exercise and cSBP after exercise were significantly higher in CAD group than in the control group (P=0.009 and 0.009, respectively). Stepwise regression analysis showed that the maximal heart rate after exercise was the main factor that affected cSBP increment in CAD group (P=0.012), and the occurrence of ischemia after exercise was associated with a lower cSBP increment (P=0.048).</p><p><b>CONCLUSION</b>AI does not decrease significantly after acute exercise in patients with CAD, suggesting that AI is closely associated with coronary artery blood perfusion after exercise and may serve as a potential target for improving ischemic threshold during rehabilitation of the patients.</p>

In vivo intestinal absorption characteristics of phloridzin in rats / 中国中药杂志

To study the in vivo intestinal absorption kinetics of phloridzin in rats. The absorption of phloridzin in the small intestines and colon of rats was investigated using an in vivo single-pass perfusion method and the drug concentration was measured by HPLC. The effects on intestinal absorption of different drug concentration and P-glycoprotein (P-gp) inhibitor were conducted. The results showed that the phloridzin could be absorbed in whole intestine, but more fully in the jejunum and colon segment,poorly absorbed in the duodenum and ileum. The absorption rate constant (Ka) and the apparent absorption coefficient（Papp）of phloridzin decreased following the sequence of jejunum> colon > duodenum > ileum. Absorption parameters of phloridzin had no significant difference at different concentration (5.14, 10.28, 20.56 mg•L⁻¹) . The saturate phenomena was not observed under the test range of drug concentration, and the absorption mechanism may be the passive diffusion transport.There had a significant difference in Ka and Papp values between P-gp inhibitor and no P-gp inhibitor groups. Phloridzin may be the substrate of P-gp.

Nasal submicron emulsion of Scutellariae Radix extract preparation technology research based on phase transfer of solute technology / 中国中药杂志

Based on the demand of nasal drug delivery high drug loadings, using the unique phase transfer of solute, integrating the phospholipid complex preparation and submicron emulsion molding process of Scutellariae Radix extract, the study obtained the preparation of the high drug loadings submicron emulsion of Scutellariae Radix extract. In the study of drug solution dispersion method, the uniformity of drug dispersed as the evaluation index, the traditional mixing method, grinding, homogenate and solute phase transfer technology were investigated, and the solute phase transfer technology was adopted in the last. With the adoption of new technology, the drug loading capacity reached 1.33% (phospholipid complex was 4%). The drug loading capacity was improved significantly. The transfer of solute method and timing were studied as follows,join the oil phase when the volume of phospholipid complex anhydrous ethanol solution remaining 30%, the solute phase transfer was completed with the continued recycling of anhydrous ethanol. After drug dissolved away to oil phase, the preparation technology of colostrum was determined with the evaluation index of emulsion droplet form. The particle size of submicron emulsion, PDI and stability parameters were used as evaluation index, orthogonal methodology were adopted to optimize the submicron emulsion ingredient and main influential factors of high pressure homogenization technology. The optimized preparation technology of Scutellariae Radix extract nasal submicron emulsion is practical and stable.

Basic property of baicalin-phospholipid complex / 中草药

Objective To investigate the basic property of baicalin complex with phospholipid. Methods To study the baicalin complex with phospholipid by means of IR, 1H-NMR, quantum chemistry, dissolubility, and the property of permeation membrane. Results The result of IR indicated that spectrogram of baicalin complex with phospholipid had the same tendency in property with baicalin and mixture. While the peak shape and wave number of -C=O, -N-H appeared abnormal. The 1H-NMR indicated that the phospholipid complex did not produce new chemical bonds between the two molecules. But the peak shape and chemical shift produced a certain change. The quantum chemistry result revealed that the two molecules did not form new compounds. On the basis of space matching, the two formed a relatively stable spatial relation by a weaker atomic orbitaols overlap method. The solubility of baicalin was significantly improved, the permeation membrane ratio of baicalin was boost. Conclusion The formation of baicalin-phospholipid complex does not produce new chemical bonds. The two form a relatively stable complex by some weak interaction force. The physicochemical properties and biological characteristics of the complex are greatly improved.

Determination of stilbene derivative in shengfa powders by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a new method for the determination of the idiosyncratic component, 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside in Shengfa Powders.</p><p><b>METHOD</b>A HPLC method was set up, using Hypersil BDS C18 column (5 microns, 4.6 mm x 150 mm), acetonitrile-water(18:82) as mobile phase, with detection at 320 nm.</p><p><b>RESULT</b>The calibration curve was linear in the range of 0.45-2.25 micrograms, r = 0.9998, the average recovery was 99.5%, RSD = 1.2%(n = 6).</p><p><b>CONCLUSION</b>The active constituent 2,3,5,4'-tetrahydroxy-stilbene-2-O-beta-D-glycoside in Shengfa Powders can be separated effectively. This method is simple, specific and exact.</p>