Dryness-alleviating effect of processed Aurantii Fructus from Lingnan based on correlation of fecal metabolomics and dryness / 中国中药杂志

With the approach of untargeted metabolomics and correlation analysis, this study aimed to explore the mechanism of Aurantii Fructus from Lingnan region in alleviating dryness by analyzing the different effects of raw Aurantii Fructus(RAF) and processed Aurantii Fructus(PAF) on fecal endogenous metabolism in normal rats. Eighteen Sprague-Dawley(SD) rats were randomly divided into a control group(C), an RAF group(10 g·kg~(-1)), and a PAF group(10 g·kg~(-1)). After seven days of administration, the effects of RAF and PAF on dryness-related indexes were compared, including water intake, fecal water content, salivary secretion, the expression of AQP5, VIP, and 5-HT in the submandibular gland, as well as the expression of AQP3, VIP, and 5-HT in the colon. The fecal samples in each group were determined by LC-MS. Multivariate statistical analysis and Pearson correlation coefficient were used for screening the differential metabolites and metabolic pathways in alleviating dryness of RAF. The results indicated that both RAF and PAF showed certain dryness, and the dryness of RAF was more significant. Moreover, PAF could alleviate dryness of RAF to a certain extent by reducing the water intake, fecal water content, and the expression of AQP3, VIP, and 5-HT in the colon and increasing the salivary secretion and the levels of AQP5, VIP, and 5-HT in the submandibular gland. According to the analysis of fecal metabolomics, 99 and 58 metabolites related to dryness were found in RAF and PAF respectively, where 16 of them played an important role in alleviating dryness of RAF. Pathway analysis revealed that the mechanism of PAF in alleviating dryness of RAF was presumably related to the regulation of riboflavin metabolism, purine metabolism, arginine biosynthesis, pyrimidine metabolism, alanine metabolism, aspartate metabolism, glutamate metabolism, and retinol metabolism pathways. This study suggested that PAF might alleviate dryness of RAF by affecting the metabolic levels of the body, which provides a new basis for further clarifying the processing mechanism of PAF.

Research Progress of Targeted Drug Delivery Nanocarriers Through Blood-brain Barrier / 中国实验方剂学杂志

The small size， moderate drug loading， and targeting properties of nano-preparations make them can be excellent delivery tools for drugs， genes or proteins crossing the cell or blood-brain barrier （BBB）. Currently， facilitating drug crossing BBB with innovative nano-drug delivery systems is considered as a strategic approach for the prevention， diagnosis and treatment of central nervous system （CNS） diseases. However， with the deepening of the research， the adverse reactions and toxicity of nanocarriers have gradually attracted the attention of researchers. Based on this， this paper summarized the situation of BBB-penetrating targeted nano-preparations at home and abroad in recent years from the perspective of classification of types and properties of nanocarriers， and analyzed the advantages and disadvantages of each carrier. The results showed that nano-preparations with active ingredients of traditional Chinese medicine （TCM） as carriers have become a promising way of cancer treatment， but the complexity and diversity of TCM components limited its application to a certain extent. Further studies should be strengthened to lay a foundation for the application and development of TCM nano-preparations in the field of CNS diseases.

Research Status of Zexietang / 中国实验方剂学杂志

Zexietang is derived from Jingui Yaolue （《金匮要略》）， which is composed of Alismatis Rhizoma and Atractylodis Macrocephalae Rhizoma， and has the effect of inducing diuresis and invigorating the spleen to produce water. Compared with western medicine in the treatment of related diseases， Zexietang can not only improve the curative effect， but also reduce the occurrence of adverse reactions， so as to achieve long-term stable administration. The authors sorted out and analyzed the chemical composition， pharmacological effect and clinical application of Zexietang in recent years. It was found that the main active components of Zexietang were alismol A and B， 23-acetyl-alismol B and C， atractylenolides （atractylenolide Ⅰ， Ⅱ， Ⅲ） and polysaccharides. Pharmacological experiments showed that they had diuretic， hypolipidemic， anti-inflammatory and others. And it can be used in the treatment of hypertension， hyperlipidemia， vertigo， cerebral vascular insufficiency and other diseases combined with other Chinese materia medica， and the curative effect is obvious. By summarizing the research status of Zexietang in recent years， its active components and pharmacological mechanism can be further clarified， which provides the basis for the clinical application of Zexietang and guides the direction of its further research.

Exploration of objective quality evaluation parameter of Alismatis Rhizoma decoction pieces / 中国中药杂志

To establish a quality constant evaluation system of Alismatis Rhizoma decoction pieces,in order to provide reference for regulating the market circulation of this decoction pieces. A total of 18 batches of Alismatis Rhizoma decoction pieces were collected from different pharmaceutical factories,and the morphological parameters of each sample were tested. The content of alisol B 23-acetate in Alismatis Rhizoma decoction pieces was determined by HPLC in the 2015 edition of Chinese Pharmacopoeia,and the parameters such as quality constant and relative quality constant were calculated. The quality constant range of 18 batches of Alismatis Rhizoma decoction pieces was 0. 390-2. 076. If 18 batches of Alismatis Rhizoma decoction pieces were divided into 3 grades,taking 80% of the maximum quality constant as first grade,50% to 80% as second grade,and the rest as third grade,then the quality constant of firstgrade samples was ≥1. 66,the quality constant of second-grade samples was ≥1. 04 and <1. 66,and the quality constant of third-grade samples was <1. 04. The established quality constant evaluation method is objective and feasible,which can be used to classify the grade of Alismatis Rhizoma decoction pieces and provide a reference method to control the quality of this decoction pieces.

Consideration about chemistry, manufacture and control (CMC) key problems in simplified registration of classical traditional Chinese medicine excellent prescriptions / 中国中药杂志

As an outstanding representative of traditional Chinese medicine(TCM) prescriptions accumulated from famous TCM doctors' clinical experiences in past dynasties, classical TCM excellent prescriptions (cTCMeP) are the most valuable part of TCM system. To support the research and development of cTCMeP, a series of regulations and measures were issued to encourage its simplified registration. There is still a long-way to go because many key problems and puzzles about technology, registration and administration in cTCMeP R&D process are not resolved. Based on the analysis of registration and management regulations of botanical drug products in FDA of USA and Japan, and EMA of Europe, the possible key problems and countermeasures in chemistry, manufacture and control (CMC) of simplified registration of cTCMeP were analyzed on the consideration of its actual situation. The method of "reference decoction extract by traditional prescription" (RDETP) was firstly proposed as standard to evaluate the quality and preparation uniformity between the new developing product under simplified registration and traditional original usages of cTCMeP, instead of Standard Decoction method in Japan. "Totality of the evidence" approach, mass balance and bioassay/biological assay of cTCMeP were emphatically suggested to introduce to the quality uniformity evaluation system in the raw drug material, drug substance and final product between the modern product and traditional decoction.

Progress of mesoporous silica nanoparticles in targeting drug delivery system of antitumor drug / 中国中药杂志

Currently, chemotherapy is one of the main therapy for cancer. But the traditional antitumor drugs are systemic distribution in vivo, they are difficult to achieve an effective drug concentration in the tumor tissue and don't have the ability to distinguish normal cells and tumor cells by themselves, that cause systemic toxicity easily and can not meet the clinical needs. With the research on mesoporous silica nanoparticles (MSNs) deepening, more and more attention in the drug delivery system have been payed to in recent years, because of its unique physicochemical structure characteristics, it has the effect on specific targets, directly inhibits the tumor cell growth, reduces the side effects to normal cells, tissues and organs and can be long-term medication, etc. It is expected to be excellent carriers of antitumor drugs. MSNs application in the field of cancer treatment has now become a hot research field of medicine. In this paper, the latest research about MSNs in antitumor drugs targeting delivery system from 2008 to 2015 is summarized, including the application of MSNs separately in antitumor drug targeting, passive targeting, active targeting, physical or chemical conditions response targeting and other compound targeting drug delivery system. We expect it to provide a reference to the toxicity reducing and efficacy enhancing and further development of chemical medicine, natural medicine and monomeric compound of chinese herbal medicine.

Simultaneous determination of ephedrine hydrochloride, D-pseudoephedrine and amygdalin in xiao'er pingchuan qutan granule by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To establish an HPLC method for the determination of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin in Xiao'er Pingchuan Qutan granule.</p><p><b>METHOD</b>Pheny ether chromatographic column (4.6 mm x 250 mm, 5 microm) was adopted, with acetonitrile-0.1% phosphoric acid (containing 0.1% three ethylamine) (3:97) as the mobile phase. The UV detection wavelength was at 210 nm, with the flow rate of 1 mL x min(-1), and column temperature was at 35 degrees C.</p><p><b>RESULT</b>The linearity of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin ranged between 0.078 60-3.144 microg (r = 1.000 0), 0.103 4-2.068 microg (r = 0.999 7) and 0.430 5-3.157 microg (r = 0.999 8), respectively. Their average recoveries were 98.46% (RSD 1.1%), 103.0% (RSD 1.5%) and 97.15% (RSD 2.1%), respectively.</p><p><b>CONCLUSION</b>The method is simple, stable and reliable that it can be used to determine the content of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin in Xiao'er Pingchuan Qutan granule.</p>

Evaluation on preparation process of brevisapin colon-specific tables and its in vitro release / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare the new traditional Chinese medicine preparation--pH-dependent brevisapin colon-specific tablets, and investigate its in vitro release, in order to discuss the feasibility of preparing colon-targeted traditional Chinese medicines.</p><p><b>METHOD</b>With scutellarin, the active ingredient in brevisapin, as the evaluation index, coating prescriptions of the preparation was screened. The in vitro release determination method was adopted to detect the in vitro release performance of the preparation.</p><p><b>RESULT</b>The in vitro release determination results showed no brevisapin in artificial pH 1. 2 dilute hydrochloric acid solution for 2 h, an accumulated dissolution rate of less than 5% in pH 6. 8 phosphate buffer solution for 4 h, but an accumulated dissolution rate exceeding 90% in pH 7. 6 phosphate buffer solution for 1 h.</p><p><b>CONCLUSION</b>Brevisapin colon-specific tablets prepared can realize colon-specific release.</p>

Evaluation on gelling properties of shuanghuanglian in situ gel by dynamic rheology / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the rheological properties of shuanghuanglian in situ gel (SHL-gel) by using dynamic rheological experiments, in order to evaluate its gelling properties shuanghuanglian in situ gel and predict its gelling behavior in vivo.</p><p><b>METHOD</b>Rheological parameters were determined by scanning of shear rate and frequency at different temperatures. The phase transition process from liquid to semisolid was described by testing of process heating/cooling and acute heating/cooling.</p><p><b>RESULT</b>SHL-gel was Newtonian fluid under the conditions of a phase angle approaching 90 degrees at low temperature or room temperature, with its viscous characteristics dominated. It was shear-thinning pseudoplastic fluid under the conditions of a low phase angle at body temperature, with its elastic characteristics dominated. During the phase transition process, the phase angle delta was getting sharp, with exponential increase of the modulus. The gelling temperature (Tg) was at (35.38 +/- 0.05) degrees C, the phase transition temperature ranged from 33.71 to 37.01%, and phase transition time was 140 s.</p><p><b>CONCLUSION</b>The dynamic rheological experiment characterizes the gelling properties of Shuanghuanglian in situ gel so precisely that it can be used as the basis of for in vitro evaluation and quality control of products.</p>

Extraction of sex hormone from antler velvet with supercritical CO2 / 中国中药杂志

<p><b>OBJECTIVE</b>To study the method of extraction of sex hormone from antler velvet with supercritical CO2.</p><p><b>METHOD</b>Supercritical fluid extraction (SFE) was used to extract sex hormone from antler velvet and radioimmunoassay (RIA) was used to analyze the extracts. The chemical compositions in extracts were identified by GC-MS, TLC and HPLC, respectively.</p><p><b>RESULT</b>The experimental results indicated that the extraction yield was 1.56% when 85% ethanol was used as co-solvent at temperature of 65 degrees C and extraction pressure of 30 MPa. Estradiol and progesterone in the extracts were 3.07, 776.18 ng x g(-1) respectively.</p><p><b>CONCLUSION</b>It is feasible to extract hormone from antler velvet with supercritical CO2.</p>

Methodological studies on equivalent relationship between granule for clinical prescription and clinical decoction of fructus evodiae / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the equivalent relationship between granule for clinical prescription and clincal decoction by use of fructus evodiae as a demonstrated object.</p><p><b>METHOD</b>Compared the equivalent ratio relationship of granule for clincal prescription and clincal decoction by determination of evodiamine, rutaecarpine, evodine, total alkaloids and dried extract ratio as markers, ten batches reference decoctions were prepared according to clinical usage as evaluation standards, common-use processed fructus evodiae products, such as salt-processed fructus evodiae, liquorice-proccesed fructus evodiae, as researching objects, and finally validated by pharmacological trials.</p><p><b>RESULT</b>Equivalent ratios of granule for clical prescription to clincal decoction are about two in all processed products, and the pharmacological evaluation showed no siginificant difference in this ratio.</p><p><b>CONCLUSION</b>This equivalent ratio model could be referenced in the production. But, it must be noticed that different herbal medicines perhaps have different equivalent ratio, which should be studied further according to its techniques and production conditions, and finally need to be revalidated by clinical trial.</p>