OBJECTIVE To prepare berberinehydrochloride resincomplex for good taste-masking effectof lyophilized oraldisintegration tablets using berberine hydrochloride as a model drug and using Kyron-T114 as the drug-loaded resin. METHODS The drug-resin composites were prepared by using the static method. Then drawn the adsorption isotherm and adsorption kinetic curves to study the adsorption mechanism of the resin. Afterwards, the characteristic of the berberine hydrochloride resin complex was studied by using the SEM, DSC, XRD and FTIR. Finally, prepared the oral disintegration tablets of berberine hydrochloride and its resin complex by using the lyophilized extrusion technology. Next, studied the in vitro release experiments and evaluated the effect of masking taste. RESULTS According to the research, a berberine hydrochloride-resin complex with the drug loaded of 43.04% was prepared. And the analysis showed that the adsorption of the drug on the resin was the multilayered chemical adsorption. The dissolution of berberine hydrochloride's powder is mainly affected by the solubility of berberine hydrochloride. Moreover, the dissolution mechanism is mainly based on Fick diffusion. The dissolution of berberine hydrochloride's powder is mainly affected by the pH of the solution, along with the concentration and the type of the ion in the solution. In artificial gastric juice, the drug dissociates rapidly from the resin. So the film diffusion was the rate-limiting step for dissolution. On the contrary, the drug dissociated slowly in the water, artificial saliva, artificial intestinal fluids including pH 4.5 and pH 6.8. So the particle diffusion was the rate-limiting step for dissolution. Besides, the dissolution of lyophilized oral disintegration tablets of drug-resin complexes in artificial saliva was significantly lower than that of berberine hydrochloride oral disintegration tablets. Lastly, the results from sensory evaluation and electronic tongue detection proved that the lyophilized oral disintegration tablets of berberine hydrochloride-resin compound has good taste masking effect. CONCLUSION Berberine hydrochloride resin complex lyophilized mouth collapse has good taste masking effect. Moreover, the drug-resin complex prepared by Kyron-T114, a weak cation exchange resin, is beneficial to improve the dissolution of poorly soluble drugs in artificial gastric juice, thereby improving their oral bioavailability. Thus, it can provide a new idea for the taste masking of traditional Chinese medicine.

OBJECTIVE To establish a more sensitive, simple, accurate and stable method for determining the activity of recombinant human α-galactosidase A (rhα-GAL) based on the kinetic theory of enzyme reaction and study the assay conditions for the activity assay. METHODS The optimum conditions of the assay system were as follows: 50 mmol·L^-1 p-nitrophenyl-α-D-galactopyranoside was used as the substrate, the concentration of the enzyme was 1.67 μg·mL^-1, the reaction was accurately carried out in a water bath at 37 ℃ for 15 min, then the reaction was terminated by glycine buffer (pH 10.5), and the absorbance was measured at 400 nm using a microplate reader. RESULTS The method had good specificity. Rhα-GAL showed a good linear relationship with the enzymatic reaction rate in the range of 0.83-2.51 mg·mL^-1 (r=0.999 8). The recoveries of validation solutions at 50%, 80%, 100%, 125% and 150% concentrations were in the range of 94.2%-101.8% (n=18), and the CVs of the measured results were between 2.0% and 5.5% (n=18). The CV of 12 independent tests of the same sample was 2.21% (n=12). The effects of slight changes in water bath temperature, reaction time and substrate concentration in the reaction system on the results were investigated,confirming the good robustness of the method. The reconstituted sample showed good stability when stored at 2-8 ℃ for 48 h. p-Nitrophenol showed a good linear relationship with the absorbance in the range of 0.01-0.15 mmol·L^-1 (r=0.999 7). The recoveries of p-nitrophenol solution at five concentrations were in the range of 94.9%-105.1% (n=9),and the CVs were all below 2.0% (n=9). The activity of two rhα-GAL products was determined by this method. CONCLUSION A chromogenic substrate method was established to determine the activity of rhα-GAL and validated with good sensitivity, precision and accuracy, which can be used for the activity evaluation and quality control of the product.

OBJECTIVE To establish an effective identification method for Jiawa and easily mixed species by using DNA barcoding ITS2 sequence. METHODS The total DNA of 72 Jiawa and its similar species samples were extracted by using the plant genomic DNA Extraction kit,PCR amplification and bidirectional sequencing were carried out for the ITS2 fragments, another 30 items of the genus were downloaded from GenBank. MEGA6.0 software was applied to analyze 102 ITS2 sequences, calculate the intraspecific and interspecific K2-P distance, construct neighber-jioning (N-J) phylogenetic tree, and predict the secondary structure of ITS2. RESULTS K2-P genetic distance analysis showed that, in addition to Pleurospermum franchetianum Hemsl. and Pleurospermum wrightianum de Boiss., Pleurospermum hookeri var. thomsonii C.B. Clarke., Sphallerocarpus gracilis (Bess.) K.-Pol., Vicatia thibetica de Boiss., Carum carvi L., Heracleum millefolium Diels., Ligusticum daucoides (Franch.) Franch. and Anthriscus sylvestris subsp. Nemorosa have obvious barcode spacing. N-J tree cluster analysis showed that each species could be clustered into one branch with a bootstrap support rate of >50%, and the monophyleticity was good. The secondary structure analysis of ITS2 showed that the number, size and position of stem-loops in the four helical regions of Jiawa and its miscible were different. CONCLUSION The ITS2 sequence can be used to identify Jiawa and its easily mixed species, which is beneficial to the rational development and utilization of Jiawa resources.

Natural drugs have been used in clinic for thousands of years in China, with complete and systematic theories, and are the treasure of the Chinese nation. Among them, flavonoids, polysaccharides, iridoid glycosides, saponins and other natural drugs have been proved to have curative effects on many diseases. Generally, the bioavailability of natural drugs absorbed in the intestine after oral administration is relatively low. As one of the ecosystems regulating the host's adaptation to the environment, the gut microbiota has a two-way effect on the host's internal and external environment, which is usually closely related to the efficacy of natural drugs. In order to understand the mechanism of the effect of drugs that are difficult to absorb, the exploration of targeting the gut microbiota has become a new strategy in recent years. The metabolism of natural drugs is often achieved through the enzymes produced by the gut microbiota, which is closely related to its efficacy and safety. The research of metabolic transformation by the gut microbiota is still limited. So in this review, we mainly discussed the characteristics of major metabolic enzymes derived from gut microbiota and the research progress in the metabolism and transformation of natural drugs, aiming to enrich the information on the metabolism mechanism of natural drugs under the action of gut microbiota and provide evidence for proving that gut microbiota is part of the regulation axis of other organs. It also provides some scientific reference for deepening the understanding and cognition of the metabolism and transformation of natural drugs under the action of intestinal bacteria.

Matricaria chamomilla L. is a herbaceous plant belonging to Asteraceae family. It is frequently used as medicinal herb in the Uygur medicines and is mainly produced in Xinjiang Uygur autonomous region, Europe and other places. Its chemical constituents mainly include flavonoids, phenolic acids, essential oil, coumarins and other compounds. This herb has anti-inflammatory, analgesic, antibacterial, antioxidant, anti-tumor, hypoglycemic, hypolipidemic, hypotensive and pharmacological effects on gastrointestinal and nervous system. Based on the overview of the chemical constituents and pharmacological effects of chamomile, this paper conducts a predictive analysis of its quality markers. It is speculated that flavonoids, phenolic acids and sesquiterpenoids can be used as quality markers of chamomile, providing scientific reference for establishing its quality standards.

OBJECTIVE To investigate and analyze the medical information of anti-hypertensive drugs instructions in children and provide reference for clinical rational drug. METHODS A total of 473 instructions of anti-hypertensive drugs were collected. The determine standards for the dosage and medical information guidance of anti-hypertensive drugs in children were established according to Provisions on the Administration of Drug Instructions and Labels, and then the labeling of medical information in children was analyzed. RESULTS The dosage of anti-hypertensive drugs in children was labeled 55.18%, vaguely labeled 5.50% and unlabeled 39.32%, and then the medical guidance information of anti-hypertensive drugs in children was labeled 31.50%, vaguely labeled 28.54% and unlabeled 39.96%. CONCLUSION The information labeling rate of anti-hypertensive drugs in children is low, the medical information is insufficient, and there is still a certain risk of medication in children.

OBJECTIVE To establish a high-performance liquid chromatography method for simultaneous determination of linezolid and its main metabolites PNU-142300 and PNU-142586 in human plasma, and monitor the blood concentration of critically ill patients. METHODS The determination was performed on Diamonsil C₁₈ column (4.6 mm×250 mm, 5 μm) with chloramphenicol as internal standard, acidified acetonitrile as protein precipitator, and bisolvent mobile phase consisting of A acetonitrile, B citric acid (0.1 mol·L^-1)-sodium hydrogen phosphate (0.2 mol·L^-1) buffer solution (pH 3.0). The flow rate was 0.5 mL·min^-1, the detection wavelength was set at 254 nm, the column temperature was maintained at 30 ℃, and the sample size was 20 μL. RESULTS Linezolid had a good linear relationship in the concentration range of 0.5-40 μg·mL^-1 (r=0.999 9). The lower limit of quantitation was 0.5 μg·mL^-1, and the detection limit was 0.1 μg·mL^-1. PNU-142300 and PNU-142586 had good linear relationship in the concentration range of 0.5-20 μg·mL^-1 (r=0.999 8 and r=0.999 6), the lower limit of quantitation was 0.5 μg·mL^-1, and the detection limit was 0.2 μg·mL^-1. In 10 critically ill patients, plasma linezolid and PNU-142300 and PNU-142586 were 3.62, 1.88 and 2.30 times higher in patients with renal insufficiency than in patients with normal renal function, respectively. There was a strong correlation between exposure of linezolid and its metabolites and thrombocytopenia and anemia. CONCLUSION The method is simple, sensitive, and accurate, and can be used to monitor the blood concentration of linezolid and its metabolites PNU-142300 and PNU-142586 in critically ill patients and study the correlation of adverse reactions.

Chemotherapy is one of the commonly used methods for tumor treatment, but the occurrence of multidrug resistance (MDR) in tumors has added great difficulties for tumor treatment, causing serious harm to patients' physiology and psychology. At present, there is a relative lack of research and treatment on tumor resistance in clinical practice, and finding reversal agents and strategies for tumor resistance is an urgent problem to be solved. This article reviews the mechanism of tumor multidrug resistance and its reversal methods and research status of Chinese medicine as reverse agent, aiming to provide reference for future research.

OBJECTIVE To analyze the characteristics of methylphenidate (MPH) related treatment emergent adverse events (TEAE) in children, so as to provide recommendations for prevention of MPH safety events. METHODS Case reports of MPH-induced TEAE in children were retrieved from CNKI, VIP, Wan Fang, PubMed, Web of Science, EMbase and other databases, and the gender, age, dosage, drug combination, time of adverse reactions and clinical manifestations of the patients were statistically analyzed. RESULTS A total of 39 case reports were collected, involving 50 cases, including 47 cases in the treatment group and 3 cases in the non-treatment group. In the treatment group, the ratio of male to female was 3.7∶1, with 40 cases (80%) in patients aged 6-15 years. Most TEAEs occurred within 1-30 d after drug administration (32 cases, 64%), and the TEAEs mainly involved mental system (12 cases, 21.43%) and nervous system (11 cases, 19.64%). In the non-treatment group, 2 patients were overdosed, and adverse reactions occurred within 1 h, mainly involving mental system and nervous system. Among the 50 cases, 49 cases were improved after drug withdrawal and/or symptomatic treatment, and 1 case had unknown prognosis. CONCLUSION It is necessary to prevent the possible safety problems in the use of MPH, so as to improve the level of rational drug use.

OBJECTIVE To analyze the impurity profile of irbesartan and its preparations by LC-MS/MS. METHODS ZORBAX SB-C₁₈ column (4.6 mm×150 mm, 3.5 μm) was used for the separation of the related substances with a mixture of 0.1% formic acid solution (adjusted to pH 3.5 with ammonia) and acetonitrile (62∶38) as the mobile phase by isocratic elution. The structures of the related substances were speculated by ESI-TOF-MS/MS and verified further by reference substances. RESULTS Irbesartan and its related substances were separated under the established chromatographic condition, and a total of 16 related substances were detected. The structures of 10 related substances were verified by reference substances. CONCLUSION The established LC-MS/MS method is effective for separation and identification of the related substances of irbesartan and its preparations, and the results obtained are valuable for its quality control and manufacturing process.