Preparation and in vitro property evaluation of β-cyclodextrin-daidzein/PEG_(20000)/Carbomer_(940) nanocrystals / 中国中药杂志

This study aims to improve the solubility and bioavailability of daidzein by preparing the β-cyclodextrin-daidzein/PEG_(20000)/Carbomer_(940) nanocrystals. Specifically, the nanocrystals were prepared with daidzein as a model drug, PEG_(20000), Carbomer_(940), and NaOH as a plasticizer, a gelling agent, and a crosslinking agent, respectively. A two-step method was employed to prepare the β-cyclodextrin-daidzein/PEG_(20000)/Carbomer_(940) nanocystals. First, the insoluble drug daidzein was embedded in β-cyclodextrin to form inclusion complexes, which were then encapsulated in the PEG_(20000)/Carbomer_(940) nanocrystals. The optimal mass fraction of NaOH was determined as 0.8% by the drug release rate, redispersability, SEM morphology, encapsulation rate, and drug loading. The inclusion status of daidzein nanocrystals was determined by Fourier transform infrared spectroscopy(FTIR), thermogravimetric analysis(TGA), and X-ray diffraction(XRD) analysis to verify the feasibility of the preparation. The prepared nanocrystals showed the average Zeta potential of(-30.77±0.15)mV and(-37.47±0.64)mV and the particle sizes of(333.60±3.81)nm and(544.60±7.66)nm before and after daidzein loading, respectively. The irregular distribution of nanocrystals before and after daidzein loading was observed under SEM. The redispersability experiment showed high dispersion efficiency of the nanocrystals. The in vitro dissolution rate of nanocrystals in intestinal fluid was significantly faster than that of daidzein, and followed the first-order drug release kinetic model. XRD, FTIR, and TGA were employed to determine the polycrystalline properties, drug loading, and thermal stability of the nanocrystals before and after drug loading. The nanocrystals loaded with daidzein demonstrated obvious antibacterial effect. The nanocrystals had more significant inhibitory effects on Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa than daidzein because of the improved solubility of daidzein. The prepared nanocrystals can significantly increase the dissolution rate and oral bioavailability of the insoluble drug daidzein.

Modern research progress in external application of traditional Chinese medicine to acupoints / 中国中药杂志

Traditional Chinese medicine(TCM) has a long history and abundant experience in external therapy, which marks human wisdom. In the early history of human, people found that fumigation, coating, and sticking of some tree branches and herb stems can help alleviate scabies and remove parasites in productive labor, which indicates the emergence of external therapy. Pathogen usually enters the body through the surface, so external therapy can be used to treat the disease. External therapy is among the major characteristic of surgery of TCM. As one of the external therapies in TCM, external application to acupoints smooths the zang-fu organs through meridians and collaterals, thereby harmonizing yin and yang. This therapy emerged in the early society, formed the Spring and Autumn Period and the Warring States Period, improved in the Song and Ming dynasties, and matured in the Qing dynasty. With the efforts of experts in history, it has had a mature theory. According to modern research, it can avoid the first-pass effect of liver and the gastrointestinal irritation and improve the bioavailability of Chinese medicine. Based on the effect of Chinese medicine and the theory of meridian and collateral, it can stimulate the acupoints, exert regulatory effect on acupoints, and give full play to the efficacy of TCM and the interaction of the two. Thereby, it can regulate qi and blood and balance yin and yang, thus being widely used in the treatment of diseases. In this paper, the use of external application to acupoints, the effect on skin immunity, the regulation of neuro-inflammatory mechanism, the relationship between acupoint application and human circulation network, and the development of its dosage form were summarized through literature review. On this basis, this study is expected to lay a foundation for further research.

Antimicrobial resistance of bacteria:surveillance report from Hunan Pro-vincial Antimicrobial Resistance Surveillance System,2012-2021 / 中国感染控制杂志

Objective To understand the distribution of frequently isolated pathogenic bacteria from clinical speci-mens and their antimicrobial resistance changes in Hunan Province from 2012 to 2021,and to provide scientific evi-dence for the formulation and evaluation of antimicrobial clinical administration policies.Methods Species identifi-cation,selection of quality control strains and antimicrobial susceptibility testing agents were conducted according to the technical scheme of the China Antimicrobial Resistance Surveillance System(CARSS).Duplicate strains were excluded based on the principle of counting the first strain in each case.Statistical analysis was performed by WHO-NET 5.6 software.The the variations in constituent ratio and resistance rate of strains were analyzed with linear trend test,and the magnitude of change was described with Pearson correlation coefficient.Results From 2012 to 2021,the number of clinically isolated bacteria in the analysis increased from 82 759 to 312 914,with Gram-negative bacteria accounting for 69.5％-72.4％.The major Gram-positive bacteria were Staphylococcus aureus,Staphylo-coccus epidermidis,Streptococcus pneumoniae,Enterococcus faecalis and Enterococcus faecium,and the major Gram-negative bacteria were Escherichia coli,Klebsiella pneumoniae,Pseudomonas aeruginosa,Acinetobacter baumannii and Enterobacter cloacae.Isolation rate of Gram-positive bacteria increased yearly(r=0.022,P=0.001).Isolation rate of methicillin-resistant Staphylococcus aureus(MRSA)decreased from 34.3％to 24.8％.Isolation rates of vancomycin-resistant Enterococcus faecium and Enterococcus faecalis were less than 3％and 2％,respectively,presenting a downward trend.The detection rate of penicillin-resistant Streptococcus pneumoniae(PRSP)decreased from 5.6％to 1.0％.Except cefoperazone sulbactam,resistance rates of Escherichia coli to other tested antimicrobial agents showed decreasing trends(r＜0,P=0.001).Isolation rates of third-generation cephalo-sporin-resistant Escherichia coli(CTX/CRO-R-EC)and carbapenem-resistant Escherichia coli(CREC)decreased year by year(from 70.5％to 45.3％,and 12.2％to 2.0％,respectively).Resistance rates of Klebsiella pneumo-niae to imipenem and meropenem have increased year by year,reaching 9.1％and 11.0％respectively in 2021,while isolation rate of carbapenem-resistant Pseudomonas aeruginosa(CRPA)decreased from 28.5％to 15.0％.Resistance rates of Acinetobacter baumannii to most antimicrobial agents were 40％-60％,and remained relatively stable.Isolation rate of carbapenem-resistant Acinetobacter baumannii(CRAB)ranged from 39.5％ to 59.6％.Conclusion The clinical isolation rates of most important special antimicrobial-resistant bacteria have been decrea-sing year by year,while the resistance rate of Klebsiella pneumoniae to carbapenem agents gradually increased.Antimicrobial stewardship as well as the prevention and control of healthcare-associated infection on specific antimi-crobial-resistant bacteria should continue to be implemented in the future.The coverage and quality of antimicrobial resistance surveillance in H unan Province should continue to be improved.

Antimicrobial resistance of bacteria from pleural and peritoneal effusion:surveillance report from Hunan Provincial Antimicrobial Resistance Sys-tem,2012-2021 / 中国感染控制杂志

Objective To understand the distribution and antimicrobial resistance changes of bacteria isolated from pleural and peritoneal effusion in Hunan Province,and provide reference for correct clinical diagnosis and rational antimicrobial use.Methods Data reported by member units of Hunan Provincial Antimicrobial Resistance Survei-llance System from 2012 to 2021 were collected.Bacteria antimicrobial resistance surveillance method was imple-mented according to technical scheme of China Antimicrobial Resistance Surveillance System(CARSS),and WHO-NET 5.6 software was used to analyze the data of bacteria isolated from pleural and peritoneal effusion as well as antimicrobial susceptibility testing results.Results From 2012 to 2021,a total of 28 934 bacterial strains were iso-lated from specimens of pleural and peritoneal effusions from member units of Hunan Provincial Antimicrobial Re-sistance Surveillance System,with 5 752 strains from pleural effusion and 23 182 from peritoneal effusion.The top five bacteria isolated from pleural effusion were Escherichia coli(n=907,15.8％),Staphylococcus aureus(n=535,9.3％),Klebsiella pneumoniae(n=369,6.4％),Staphylococcus epidermidis(n=452,7.9％),and Staphy-lococcus haemolyticus(n=285,5.0％).The detection rate of methicillin-resistant Staphylococcus aureus(MR-SA)from pleural effusion was 24.3％-39.2％,and that of methicillin-resistant coagulase negative Staphylococcus(MRCNS)was 58.8％-77.1％.The top five bacteria isolated from peritoneal effusion were Escherichia coli(n=8 264,35.6％),Klebsiella pneumoniae(n=2 074,9.0％),Enterococcus faecium(n=1 458,6.3％),Staphylo-coccus epidermidis(n=1 383,6.0％),and Pseudomonas aeruginosa(n=1 152,5.0％).The detection rate of MRSA from peritoneal effusion was 22.1％-52.4％,which presented a decreasing trend(P=0.004).The detec-tion rate of MRCNS was 60.4％-79.4％.The resistance rates of Enterobacterales from peritoneal effusion to ce-fazolin,cefuroxime,ceftriaxone and cefepime all showed decreasing trends(all P＜0.05).Vancomycin-,linezo-lid-,and teicoplanin-resistant Staphylococcus strains were not found in pleural and peritoneal effusions.The resis-tance rates of Enterococcus faecium to most tested antimicrobial agents were higher than those of Enterococcus fae-calis.The resistance rates of Enterobacterales to imipenem and meropenem were ≤8.5％.The resistance rates of non-fermentative Gram-negative bacilli to imipenem and meropenem were ≤43.3％.Conclusion The data structure of Hunan Antimicrobial Resistance Surveillance System for pleural and peritoneal effusions from 2012 to 2021 is relatively complete.The constituent and antimicrobial susceptibility of isolated pathogenic bacteria vary in different years.

Antimicrobial resistance of Pseudomonas aeruginosa:surveillance report from Hunan Provincial Antimicrobial Resistance Surveillance System,2012-2021 / 中国感染控制杂志

Objective To understand the distribution and changes in antimicrobial resistance of clinically isolated Pseudomonas aeruginosa(P.aeruginosa)in the member hospitals of Hunan Provincial Antimicrobial Resistance Surveillance System from 2012 to 2021.Methods Antimicrobial susceptibility testing by disk diffusion or automa-ted instrument was performed on clinical isolates.Testing results were determined according to the standards of 2022 edition from American Clinical Laboratory Standards Institute(CLSI).Statistical analysis was performed by WHONET 5.6 software.Data were analyzed by trend test(Cochran-armitage)and Chi-square test with SPSS.Results A total of 176 441 strains of P.aeruginosa were surveilled by Hunan Provincial Antimicrobial Resistance Surveillance System from 2012 to 2021.99.4％of the strains were isolated from hospitalized patients,and about 70％of the strains were isolated from respiratory specimens.8.4％of P.aeruginosa were from children(0-17 years old),91.6％were from adults.Antimicrobial susceptibility testing results showed that P.aeruginosa was most sensitive to polymyxin B over 10 years,with a resis-tance rate of less than 6％.Resistance rates to piperacil-lin,piperacillin/tazobactam,ceftazidime,cefepime,aztreonam,imipenem,amikacin,gentamicin,tobramycin,cip-rofloxacin,levofloxacin,and polymyxin B all showed downward trends.A total of 29 920 carbapenem-resistant P.aeruginosa(CRPA)strains were detected.The average isolation rate of CRPA in this province was 18.0％over 10 years.CRPA detection rate from adult was 18.5％,higher than that from children(12.3％),and both showing downward trends.Conclusion The resistance rate of clinically isolated P.aeruginosa in Hunan Province to most commonly used antimicrobial agents is decreasing.

Antimicrobial resistance of Acinetobacter baumannii:surveillance report from Hunan Provincial Antimicrobial Resistance System,2012-2021 / 中国感染控制杂志

Objective To understand the epidemiology of clinically isolated Acinetobacter baumannii(A.bauma-nnii)in Hunan Province.Methods Bacterial antimicrobial resistance surveillance was carried out according to the requirements of the technical program of National Antimicrobial Resistance Surveillance System.Clinical data of Acinetobacter spp.reported to Hunan Provincial Antimicrobial Resistance Surveillance System by multiple centers in Hunan Province from 2012 to 2021 were summarized and analyzed with reference to the standards of the American Clinical and Laboratory Standards Institute.Results A total of 169 438 strains of Acinetobacter spp.were detected during the 10-year period,with the detection rate of A.baumannii being the highest(82.74％).70 923 strains(53.63％)of carbapenem-resistant A.baumannii(CRAB)and 58 149 strains(43.97％)of carbapenem-sensitive A.baumannii(CSAB)were detected respectively.Both CRAB and CSAB were detected most frequently in the age group＞70 years,which were 34.44％and 32.02％,respectively.The percentage of CRAB and CSAB detected in the intensive care unit were 34.80％and 11.31％,respectively.CRAB and CSAB were mainly isolated from spu-tum/bronchoalveolar lavage fluid,followed by pus/secretion,urine,and blood.The resistance rates of CRAB to commonly used antimicrobial agents didn't change much during the 10-year period.Resistance rates of CRAB to ceftazidime and cefepime were both＞84％,to ampicillin/sulbactam and piperacillin/tazobactam were both＞82％,to aminoglycosides and quinolones were both＞59％,to minocycline and polymyxin B were 15.9％-25.0％and 1.3％-6.9％,respectively.CSAB were sensitive to commonly used antimicrobial agents.Conclusion The isolation rate of CRAB is high and there is no significant change in resistance to commonly used antimicrobial agents.

Research progress in gut-skin axis and its association with traditional Chinese medicine theory / 中国中药杂志

Currently, the gut-organ axis has become a hot research topic. As increasing attention has been paid to the role of gut microbiota in the health of organs, the complex and integrated dialogue mechanism between the gastrointestinal tract and the associated microbiota has been demonstrated in more and more studies. Skin as the largest organ in the human body serves as the primary barrier protecting the human body from damage. The proposal of the gut-skin axis has established a bidirectional link between the gut and the skin. The disturbance of gut microbiota can lead to the occurrence of skin diseases, the mechanism of which is complex and may involve multiple pathways in immunity, metabolism, and internal secretion. According to the theory of traditional Chinese medicine(TCM), the connection between the intestine and the skin can be established through the lung, and the interior disorders will definitely cause symptoms on the exterior. This paper reviews the research progress in the gut-skin axis and its correlation with TCM theory and provides ideas and a basis for cli-nical treatment and drug development of skin and intestinal diseases.

Chronic Toxicity of Triptolide and Ferulic Acid Ethosomes Gel for Percutaneous Administration / 中国实验方剂学杂志

ObjectiveTo investigate the long-term safety of triptolide ferulic acid ethosome gel in percutaneous administration. MethodWe mixed triptolide with ferulic acid to make liposomes gel in different doses and then administrated the gel to SD rats of both sexes with intact skin and damaged skin for 12 weeks. The daily dosages calculated based on triptolide for the low-， middle-， and high-dose groups were 63.75， 127.50， 255.00 μg·kg-1， respectively. The body weight of each rat was measured weekly. The rats were sacrificed in the last week for the determination of serum biochemical parameters and organ indexes as well as the observation of histopathology. The toxicity was assessed based on the body weight and all the parameters and indexes. ResultAfter long-term administration， the body weight and serum biochemical parameters did not show significant difference between the gel-treated groups and the blank group with intact skin， which indicated that the percutaneous administration of triptolide and ferulic acid ethosomes gel was relatively safe. However， the rats in the high-dose group showed sparse hair and were easy to die in the case of unhairing with chloral hydrate at the late stage of the study. Comprared with the female rats with intact skin in the blank control group， the female rats with damaged skin in the middle-dose group showed decreased heart index （P<0.05）， which indicated certain cardiotoxicity. Moreover， damage appeared in skin and lung， which may be influeneced by dosage， sex， and skin state. ConclusionFerulic acid in combination with triptolide is relatively safe for percutaneous administration， whereas there are some risks of skin and lung damage in the case of long-term administration. Individualized administration scheme should be developed according to liver and kidney function and skin conditons to ensure the safety of clinical medication.

Research progress of powder modification of TCM based on particle design theory / 药学学报

Particle design, based on the concept of "quality by design", combines the elements of microbiology, formulation science, heat and mass transfer, solid state physics, powder science, and nanotechnology. It is widely used to develop particles with excellent functional properties. Without affecting the active ingredients, the modification technology of traditional Chinese medicine (TCM) powder based on particle design theory, could improve the flowability, tabletability, disintegration and dissolution behavior, hygroscopicity, wettability, and other functional properties at the physical structure level. This greatly promotes the development of solid preparations of TCM. The present review aims to summarize and discuss the research progress of powder modification of TCM from the perspective of the theory of particle design, powder modification technology, equipment used for powder modification, application in TCM and modification mechanism mainly based on researches published in recent ten years. This review could provide ideas and theory basis for the development of particle design.

Pharmacokinetic behavior and brain tissue distribution of paeoniflorin combined with normal and toxic doses of strychnine in rats after percutaneous administration / 中国中药杂志

This study aims to establish a rapid and sensitive UPLC-MS/MS method for simultaneously determining the content of strychnine and paeoniflorin in plasma and brain tissue of rats, and compare the pharmacokinetic behavior and brain tissue distribution of paeoniflorin combined with normal and toxic doses of strychnine in rats after percutaneous administration. Compared with those in the toxic-dose strychnine group, the AUC_(0-t), AUC_(0-∞), and C_(max) of strychnine decreased by 51.51%, 45.68%, and 46.03%, respectively(P<0.01), and the corresponding values of paeoniflorin increased by 91.41%, 102.31%, and 169.32%, respectively(P<0.01), in the compatibility group. Compared with the normal-dose strychnine group, the compatibility group showed insignificantly decreased C_(max), AUC_(0-t), and AUC_(0-∞) of strychnine, increased C_(max) and T_(max) of paeoniflorin(P<0.01), 66.88% increase in AUC_(0-t), and 70.55% increase in AUC_(0-∞) of paeoniflorin. In addition, the brain tissue concentration of strychnine decreased and that of paeoniflorin increased after compatibility. The combination of paeoniflorin with normal dose and toxic dose of strychnine can inhibit the percutaneous absorption of strychnine, and greatly promote the percutaneous penetration of paeoniflorin, whereas the interaction mechanism remains to be explored. The UPLC-MS/MS method established in this study is easy to operate and has good precision. It is suitable for in vivo study of pharmacokinetic behavior and brain tissue distribution of paeoniflorin and strychnine after percutaneous administration in rats, which provides reference for the safe and rational clinical use of strychnine and the combined use of drugs, and lays a solid foundation for the development of external preparations containing Strychni Semen.

Quality value transfer of material benchmark of Guizhi Jia Gegen Decoction / 中国中药杂志

A total of 15 batches of the substance reference of Guizhi Jia Gegen Decoction(GZGGD) were prepared and the characteristic fingerprints of them were established. Furthermore, the similarity of the fingerprints and peak attributes were explored. The extraction rate, and the content and the transfer rate ranges of the index components, puerarin, paeoniflorin, liquiritin, and ammonium glycyrrhizate were determined for the analysis of the quality value transfer. The result demonstrated that the fingerprints of the 15 batches of the samples showed high similarity(>0.99). A total of 15 characteristic peaks were identified from the fingerprints, with 10 for Puerariae Lobatae Radix, 1 for Cinnamomi Ramulus, 2 for Paeoniae Radix Alba, and 2 for Glycyrrhizae Radix et Rhizoma. The content of puerarin was 11.05-18.35 mg·g~(-1) and the average transfer rate was 21.27%-39.49%. The corresponding figures were 7.95-10.90 mg·g~(-1) and 23.28%-43.23% for paeoniflorin, 3.25-4.95 mg·g~(-1) and 32.31%-61.27% for ammonium glycyrrhizate, and 3.65-5.80 mg·g~(-1) and 14.57%-27.05% for liquiritin. The extraction rate of the 15 batches of samples was in the range of 16.85%-21.78%. In this paper, the quality value transfer of the substance reference of GZGGD was analyzed based on characteristic fingerprint, content of index components, and the extraction rate. This study is expected to lay a basis for the quality control and further development of GZGGD.

Research Progress on Pain Relief of Essential Oils of Traditional Chinese Medicine：A Review / 中国实验方剂学杂志

Volatile oil is widely distributed in Chinese medicinal materials with complex chemical components. The main components are terpenes， aromatics， aliphatics， and nitrogen and sulfur containing. It has a variety of pharmacological activities. Such as antibacterial， anti-inflammatory， analgesic， anti-tumor， anti-oxidant， anti-aging and so on. It is widely used in medical and health care， agricultural efficiency enhancement， and daily products. In recent years， there have been a large number of studies on the pain relief of traditional Chinese medicine （TCM） essential oils， but there is no systematic generalization. The author found that the mechanism of TCM essential oils to exert analgesic effects mainly includes regulation of the central nervous system， anti-inflammatory and analgesic， antispasmodic and analgesic effects by consulting Chinese and foreign literatures in recent years， but the exact mechanism needs to be further verified. This article reviews the research progress of TCM essential oil pain relief from the aspects of pain classification， generation， analgesic mechanism and combination of other technologies， in order to provide reference for related research in the future.

Research Progress in Anti-alcoholic Effect of Puerariae Lobatae Radix / 中国实验方剂学杂志

With advanced brewing technology and contemporary table culture， alcohol drinking， which can be traced back to Dukang wine in the Xia dynasty， is very common in China. However， excessive alcohol intake can easily cause alcohol liver damage， ranging from abdominal pain and venous thrombosis to severe hypoglycemia and fat embolism， coma shock and even life-threatening cases. Puerariae Lobatae Radix has a cool property and sweet taste， with functions of antipyretic， promoting the secretion of saliva or body fluid， rash and hangover alleviation， and so on. It was first recorded in Shen Nong's Materia Medica and has been listed as a special anti-alcoholic medicine in traditional Chinese medicine since ancient times. For example， the ancient medical book Compendium of Materia Medica and other records claim that Puerariae Lobatae Radix has the effect of relieving alcohol and protecting the liver. At the same time， Puerariae Lobatae Radix has a long history in both medicine and food. It was listed in the List of Articles That Both Serve as Food and Medicine published by the National Health Commission. Therefore， there are many products containing pueraria for hangover and liver protection. Prior to this， many scholars have carried out relevant researches on the anti-alcoholism efficacy of Puerariae Lobatae Radix， but there is a lack of systematic summaries. The author has consulted relevant domestic and foreign literatures in recent years. The related products were summarized and it was found that the anti-alcoholic effect of pueraria root mainly came from puerarin， pueraria flavonoids and pueraria polysaccharide， puerarin polypeptide， pueraria daidzein and its derivatives， including the main mechanisms such as inhibiting alcohol absorption， accelerating metabolism， anti-oxidation， protection of liver and cardiomyocytes， and neuroprotection. Related products are abundant and well evaluated， but research on related genes needs to be deepened. This article reviews the main anti-alcoholic components， mechanism of action and related products of pueraria， and puts forward suggestions for future research directions， hoping to provide reference for further related research.

Investigating effect of Faeces Bombycis on intestinal microflora in rats with syndrome of damp retention in middle-jiao by high-throughput sequencing / 中国中药杂志

The aim of this paper was to investigate the effect of Faeces Bombycis(FB) on the intestinal microflora in rats with syndrome of damp retention in middle-jiao, and to explore its mechanism in regulating intestinal microflora from the perspective of microorganisms contained in FB. The contents of antidiuretic hormone(ADH) and C-reactive protein(CRP) in serum and aquaporin 3(AQP3) in jejunum were determined by enzyme-linked immunosorbent assay(ELISA). Illumina Miseq platform was used for high-throughput sequencing of the rat feces and FB. The ELISA results showed that as compared with the normal control group, the contents of ADH and CRP in the model group were significantly increased(P<0.05), and the content of AQP3 was significantly decreased(P<0.05). After drug administration, the ADH, CRP and AQP3 contents were recovered. Sequencing of rat feces showed that the ACE, Chao1 and Shannon indexes of the intestinal microflora were the lowest in the model group. As compared with the normal control group, the levels from phylum to genus were all significantly changed in model group, and Proteobacteria, Acinetobacter, Anaerobacter, Pseudomonas, and Parabacteroides levels were significantly increased(P<0.05), while Marvinbryantia level was significantly decreased(P<0.05). As compared with the model group, Proteobacteria was significantly decreased in the FB low and high dose groups(P<0.05), and Acinetobacter, Anaerobacter, Pseudomonas, Parabacteroides levels were significantly decreased in the low, medium and high dose groups(P<0.05), while Lachnoanaerobaculum, Intestinimonas and Marvinbryantia were increased significantly in the high dose group(P<0.05). Sequencing analysis of FB showed that the relative abundance of Leclercia, Pantoea, Brachybacterium, Shimwellia, Hartmannibacter, Klebsiella, Serratia, Aurantimonas, Paenibacillus and Bacillus was high in the FB, but they were basically not present or little in the rat feces. In conclusion, FB may play a role in the treatment of "syndrome of damp retention in middle-jiao" by balancing the intestinal microflora, and this effect may be related to the metabolites of microorganisms in the FB.

Simultaneous Determination of Pyrrolidine Alkaloids and Their Nitrogen Oxides in Farfarae Flos by UPLC-MS/MS / 中国实验方剂学杂志

<b>Objective::To establish an ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) for the simultaneous determination of 15 pyrrolidine alkaloids (PAs) and their nitrogen oxides, and determine the content of the 15 PAs in the 15 batches of Farfarae Flos samples obtained from different sources, in order to understand the distribution status of these 15 PAs in Farfarae Flos from different sources, and provide relevant references for the safe and rational use of this medicinal materials. <b>Method::The method was achieved by Agilent Eclipse Plus C₁₈ column (3.0 mm×150 mm, 1.8 μm) using a mobile phase made up of 0.05%formic acid and 2.5 mmol·L^-1 ammonium formate in water (A)-0.05%formic acid and 2.5 mmol·L^-1 ammonium formate in methanol(B). The flow rate and the injection volume were 0.4 mL·min^-1 and 2 μL, respectively. The column temperature was 40 ℃. The instrument was Agilent 1290-6470 QQQ ultra high performance liquid chromatography-triple quaternary bar mass spectrometer. The components were detected in multiple reaction monitoring mode by mass spectrometry with ionizationmode of ESI⁺. The content of the components measured in the samples was calculated by using the external standard method, and the difference between samples was analyzed based on RSD of different components. <b>Result::The established method had a high sensitivity and good separation degree. The results of methodological investigation met the requirements. The results showed that all of the 15 batches of Farfarae Flos contained PAs and their nitrogen oxides. These PAs had almost the same types of structure. There were significant differences in the content and distribution of PAs in Farfarae Flos obtained from different sources. <b>Conclusion::In general, Farfarae Flos contains pyrrolidine alkaloids and their nitrogen oxides. Senkirkine with a significant hepatotoxicity is the main compound. The content determination of PAs will provide scientific fundaments for the safe and effective use of Farfarae Flos.

Improving hygroscopicity of fermented Cordyceps powder based on particle design technology of traditional Chinese medicine / 中国中药杂志

Commonly used dosage forms of fermented Cordyceps powder products are capsules and tablets. The hygroscopicity of the powder,as one of the important parameters in the tableting process,has important effects on the tabletting process of the tablets. How to improve the hygroscopicity of powder is of great significance for the development of new composite particles. Therefore,particle design technology was used in this study to prepare composite particle powder,and its hygroscopicity was compared with fermented Cordyceps powder and physically mixed powder. By preparing three different types of powders,the equilibrium moisture absorption,particle size,scanning electron micrograph,angle of repose,contact angle and compression degree were compared to observe the effect of traditional Chinese medicine particle design technology on improving the hygroscopicity of the fermented Cordyceps powder. The results showed that the equilibrium moisture absorption was 21. 2%,19. 6%,14. 5% respectively for the fermented Cordyceps powder,physically mixed powder and composite particle powder; the median diameter was(49. 751± 0. 280),(59. 183± 0. 170),(12. 842±0. 080) μm,respectively; the mode diameter was(185. 479±1. 372),(173. 964± 1. 104),(61. 671± 0. 979) μm,respectively. In the scanning electron micrograph of the composite particle powder,it can be clearly seen that the fermented Cordyceps powder had hydrophobic gas phase nano-silica with a fixed shape and uniform size. The angle of repose was(50. 63 ± 0. 75) °,(49. 25 ± 0. 43) °,(48. 33±0. 84) ° respectively; the contact angle was(7. 4±0. 2) °,(8. 2±0. 3) °,(15. 0±2. 6) ° respectively; and the compression degree was(38. 2±1. 3) %,(35. 8±0. 2) %,(32. 5±2. 6) % respectively. This study showed that after treatment by the vibrating ultrafine pulverizer,the fermented Cordyceps powder particles had obvious and uniform small particle hydrophobic gas phase nano-silica adhered to form a partially wrapped coating structure,which reduced the contact surface of fermented Cordyceps powder with the outside world,thereby reducing the hygroscopicity of the composite particle powder. It further demonstrated that the hygroscopicity of fermented Cordyceps powder can be improved by particle design.

Preparation and evaluation of four kinds of mixed essential oil liposomes in Jieyu Anshen Formula / 中国中药杂志

In order to increase the stability and solubility of essential oil in Jieyu Anshen Formula, this study was to prepare the essential oil into liposomes. In this experiment, the method for the determination of encapsulation efficiency of liposomes was established by ultraviolet spectrophotometer and dextran gel column. The encapsulation efficiency and particle size of liposomes were used as evaluation indexes for single factor investigation and Box-Behnken design-response surface method was used to optimize the design. Then the optimal formulation of volatile oil liposome was characterized using methyleugenol, elemin, β-asarone and α-asarone as index components. Finally, the in vitro transdermal properties of liposomes were studied by modified Franz diffusion cell. The results showed that the concentration of lecithin, the mass ratio of lecithin to volatile oil, and the stirring speed were the three most significant factors affecting the liposome preparation. The optimum formulation of volatile oil liposome was as follows: the concentration of lecithin was 7 g·L~(-1); mass ratio of lecithin to volatile oil was 5∶1; and the stirring speed was 330 r·min~(-1). Under such conditions, the prepared liposomes had blue emulsion light, good fluidity, half translucent, with particle size of(102.6±0.35) nm, Zeta potential of(-17.8±0.306) mV, permeability of(1.67±1.01)%, and stable property if liposome was stored at 4 ℃. 24 h after percutaneous administration, the cumulative osmotic capacity per unit time was(30.485 2±1.238 9),(34.794 8±0.928 3),(26.677 1±1.171 7),(3.066 2±0.175 3) μg·cm~(-2)respectively for methyleugenol, elemin, β-asarone and α-asarone. In vitro transdermal behaviors of methyleugenol, elemin, β-asarone and α-asarone in liposomes were all consistent with Higuchi equation. The prepared volatile oil liposomes met the relevant quality requirements, providing a reference for further research on preparation of multi-component Chinese medicine essential oil liposomes.

Establishment of skin and joint micro-dialysis sampling method of triptolide in vivo by HPLC-MS/MS / 中国中药杂志

To detect the concentration of triptolide in skin and joint after percutaneous administration,an HPLC-MS/MS method and skin and joint micro-dialysis( MD) method of triptolide were established in this study. The separation was achieved on triple quadrupole( AB QTRAP4500) and phenomenex-C18( 4. 6 mm×150 mm,5 μm,luna) column with acetonitrile-water with 0. 1% formic acid( 65 ∶35) as the mobile phase at a flow rate of 0. 7 m L·min-1. An electrospray ionization( ESI) source was applied and operated in the positive multiple reaction monitoring( MRM) mode. The fragment ion for triptolide was m/z 361. 1→145. 0. The effects of different perfusion [Ringer's,PBS( p H 7. 4),30% ethanol saline]drug concentrations and flow rates on the recovery rate,as well as the relationship between the recovery rate and the loss rate were determined by incremental( dialysis) and reduction( retrodialysis) methods.The reduction method was applied in the in vivo study to investigate and determine the stability of the probe recovery rate in 10 h. The results of HPLC-MS/MS detection method conformed to the requirements of biological samples. The perfusion fluid was 30% ethanol saline. The recovery rate of skin and joint probes in vitro of triptolide increased within the flow rate of 0. 5-2. 5 μL·min-1. In order to increase the timeliness of data and the accuracy,the flow rate was determined to be 1 μL·min-1,and the sample interval was determined to be 0. 5 h. The recovery rate of triptolide in skin and joint probes in vitro and the loss rate were stable and equal despite of change of triptolide concentration within 10-200 μg·L-1. This indicated that the effect of drug concentration on the MD probe recovery rate was small,and the recovery rate could be replaced by the loss rate. The loss rate in vivo using MD method was measured at 10 h,indicating that the transfer rate of triptolide was stable within 10 h. The established method of triptolide in MD and HPLC-MS/MS can be applied to investigate the kinetic in skin and joint after percutaneous administration of triptolide.

Pharmacokinetics of skin and blood of Tripterygium wilfordii and Paeonia lactiflora micro-emulsion gel based on micro-dialysis technology / 中国中药杂志

To further investigate the metabolism of Tripterygium wilfordii and Paeonia lactiflora micro-emulsion gel in vivo,an LCMS/MS method was established for the determination of triptolide and paeoniflorin in T. wilfordii and P. lactiflora micro-emulsion gel.The extracorporeal recovery rate of blood probe was measured by concentration difference methods( incremental method and decremental method). Meanwhile,the skin and blood micro-dialysis methods of tripterine and paeoniflorin were established,and the pharmacokinetics of T. wilfordii microemulsion gel in skin and blood was studied by micro-dialysis combined with LC-MS/MS quantitative analysis. The results showed that the established method for the determination of triptolide and paeoniflorin in T. wilfordii microemulsion gel was well linear within the required range,and the specificity,recovery rate and degree of precision of the chromatography all conformed to the research requirements of micro-dialysis samples. The stability of freeze-thawing and the residual effect all conformed to the criteria of biological sample methodology. The probe recovery rates measured by incremental method and decremental method were almost consistent with the extracorporeal recovery rate test. The recovery rates of paeoniflorin in skin and blood micro-dialysis were( 30. 60±1. 09) % and( 28. 01± 1. 75) %,respectively. And the recovery rates of skin and blood micro-dialysis were( 26. 79 ± 2. 78) % and( 25. 39±1. 86) %,respectively. The intraday recovery rate of probes was stable within 11 h. The results of pharmacokinetic study showed that the Cmaxvalues of triptolide in skin and blood were( 148. 03±41. 51) and( 76. 77±15. 27) μg·L-1,respectively. And the Tmaxvalues were( 2. 33±0. 29) and( 3. 00± 0) h,respectively. The AUC0-11 hvalues were( 2 814. 05± 1 070. 37) and( 1 580. 63±208. 27) μg·h·L-1,respectively. The MRT0-11 hvalues were( 4. 20± 0. 33) and( 4. 54± 0. 34) h,respectively. The T1/2 values were( 4. 61±4. 11) and( 1. 07± 0. 13) h,respectively. The Cmaxvalues of paeoniflorin in skin and blood were( 991. 88 ± 152. 22) and( 407. 02±120. 06) μg·L-1,respectively. The Tmaxvalues were( 2. 00±0) h and( 2. 83±0. 29) h,respectively. The AUC0-11 hvalues were( 18 430. 27±3 289. 35) and( 6 338. 59 ± 1 659. 32) μg·h·L-1,respectively. The MRT0-11 hvalues were( 4. 29 ± 0. 16) and( 4. 00±0. 05) h,respectively. The T1/2 values were( 2. 16±0. 43) and( 1. 78±0. 48) h,respectively. The results suggested that micro-emulsion gel played a role in forming skin reservoir through percutaneous penetration. It not only could improve drug transdermal efficiency,but also control the sustained release of drug and form a long-term effect.

Research Progress of Granulation Technology for Taste Masking of Pharmaceutical Preparation / 中国实验方剂学杂志

In commonly used oral solid preparations, poor mouthfeel results in poor patient compliance with the drug, which in turn reduces the market competitiveness of the drug. The problem of taste masking of pharmaceutical preparations has always been one of the important problems faced by pharmaceutics. With the increasing demand for the taste of drugs, the methods of masking bad taste of drugs have gradually increased in recent years. By summarizing the relevant literature covering the bad taste of drugs, the commonly used taste masking techniques include the addition of taste masking agents, inclusion techniques, microsphere/microcapsule technology, solid dispersion technology, ion exchange technology and the like. However, in addition to the above taste masking techniques, in the manufacturing process of the solid preparation, the granulation technique also can achieve the shielding of the bad taste of the medicine, and the granulation technique is simple, and can well achieve the effect of masking the bad taste of the medicine. This paper systematically introduces the research progress of granulation technology in drug taste masking, in order to provide reference for the selection of drug taste masking technology. With the increasing demand for drug taste, drug masking technology has been paid more and more attention by the majority of preparation workers, however, there are still some problems, such as imperfect taste evaluation system and low specificity of methods. This series of problems need to be further studied and solved by relevant pharmaceutical researchers.