Objective:To prepare enteric-coated pellets of ( R)-rabeprazole sodium and investigate the drug release behavior in vitro. Methods:The pellets of ( R)-rabeprazole sodium were prepared by a fluid bed coating technology, and HPMC and Eudragit L30D-55 was used as the material of isolation layer and enteric coating, respectively. The similarity of in vitro drug release was com-pared between the reference preparation and the self-prepared preparation. Similar factor ( f2 ) was used to evaluate the similarity of re-lease curves. Results:The coating formula of ( R)-rabeprazole sodium enteric-coated pellets was as follows: the weight of HPMC E5 and Eudragit L30D-55 was 12. 0% and 45. 0%, respectively, and the plasticizer was 8. 0% of the weight of the polymers. The f2 of the reference preparation and the self-prepared preparation was more than 50, which indicated the release behavior was similar. Con-clusion:The release behavior of ( R)-rabeprazole sodium enteric-coated pellets is quite promising, and the preparation technology can be used in the industrial production.

Objective To explore the possible mechanism of SchA ,which decreases MPP+induce SH-SY5Y cell damage .Meth-ods Cultured cells were divided into 5 groups ,one as control group ,cultured by free-blood serum media;the other 4 groups were treated with different concentrations of SchA(1 ,3 ,5 μmol/L) and MPP+ (1 mmol/L) for 48 h named model group ,1 ,3 ,5 μmol/L SchA group respetivly .The content of nitric oxide(NO) were measured by NO kit ;The expression levels of total Akt and p-Akt proteins were detected by Western blot .Results Compared with the control group ,the content of NO in group significantly in-creased after MPP+stimulating(P<0 .05);compared to the control group ,the content of NO in 5μmol/L SchA group significantly decreased(P<0 .05) .The expression levels of total Akt in all groups had no significant difference(P>0 .05) .The expression levels of p-Akt in model group significantly lowered ,while SchA(1、3、5 μmol/L) significantly increased the expression levels of p-Akt in comparision with cells in model group .Conclusion Decreasing MPP+ induced SH-SY5Y cell damage of SchA may be related to the content of NO and p-Akt expression .

Objective The purpose of this investigation was to observe the effects of the glutamate/aspartate transporter(GLAST) antibody to auditory brainstem response(ABR) and the pathologic morphology of hair cells in the guinea pig's cochlea. Methods 20 guinea pigs were randomly divided into the experimental group and control group. By perfusing the antibody to GLAST into tympanic canal in the cochlea of guinea pigs in experimental group and artificial perilymph into the guinea's cochlea in control group,the results of ABR ,basilar membrane stretched preparation and transmission electron microscope were observed. Results After antibody perfusion,the ABR was not induced from the third day to the ninth day.In control group,the ABR was nearly absent on the third day,but could be evolved,on the sixth day and the ninth day in all guinea pigs with the average threshold of 62.50?5.25 dB SPL and 47.50?6.18 dB SPL,respectively. The ABR thresholds at different time in control group were significantly different(P

In this study,thermosensitive and repairable molecularly imprinted solid-phase microextraction fibers were synthesized using spiramycin as template molecule,methacrylic acid and N-isopropylacrylamide as functional monomers,ethylene glycol dimethacrylate as crosslinking agent,and silanized quartz capillary as carrier. The prepared molecularly imprinted solid-phase microextraction fibers were characterized by scanning electron microscope and nitrogen adsorption/desorption,and various parameters affecting the extraction efficiency were optimized. Due to high selectivity and sensitivity of the fibers for macrolide antibiotics,the quantitative analysis of four macrolide antibiotics in food matrix,spiramycin,tilmicosin,tylosin,and josamycin,was peroformed in combination with high performance liquid chromatography. In the range of 0.5 to 50 μg/mL,the chromatographic peak area showed a good linear relationship with the concentration. The spike recoveries of the samples at three different addition levels were between 81.8% and 119.1%;the inter-day precisions were less than 13.8% (n=6),and the intra-day precisions were less than 15.5% (n=3).

In this paper, we developed an accurate and sensitive LC-MS/MS method for the determination of amoxicillin and clavulanic acid in human plasma. A 50% aqueous acetic acid solution was used as a stabilizer, and the plasma samples were evaporated to dryness and resolved after protein precipitation on ice bathing and then were placed in an autosampler for injection. The gradient was eluted by Hedera ODS-2 column(2. 1 mm×150 mm). The aqueous phase was an aqueous solution containing 0. 2% acetic acid. The organic phase was methanol. The amoxicillin and clavulanic acid were detected under negative ion detection with electrospray ionization(ESI)in multiple reaction monitoring(MRM)mode of m/z 364. 1→223. 1 and 198. 1→135. 9 in the triple quagdrupole tandem mass spectrometer(Triple Quad TM 6500+). The concentration ranges of plasma from 20. 0 ng/mL to 5 000 ng/mL for amoxicillin and 10. 0 ng/mL to 2 500 ng/mL for clavulanic acid were good linear relationship. The accuracy deviation were ±15. 0% and precision were less than 15. 0% for the intra-assay and inter-assay. The matrix effect and recovery meeted the acceptance criteria, amoxicillin and clavulanic acid were stable under storage and processing conditions. Healthy subjects were given a test preparation of amoxicillin and clavulanate potassium granules 1 bag(125 mg/31. 25 mg/bag)and the reference preparation amoxicillin clavulanate potassium dry mix Suspension “Augmentin® ” 5 mL(125 mg/31. 25 mg/5 mL)was used to determine the plasma concentration of amoxicillin and clavulanic acid. The Phoenix WinNonlin 6. 4 software was used to estimate the pharmacokinetic parameters of non-compartmental models. The pharmacokinetic parameters of amoxicillin and clavulanic acid were statistically calculated and evaluated the bioequivalence. what′s more, we evaluated the diet on the pharmacokinetics of amoxicillin and clavulanic acid. The analytical method was rapid and sensitive, which was successfully employed in the bioequivalence study of amoxicillin(125 mg/bag)and clavulanate potassium granules(31. 25 mg/bag)for determining the concentration of amoxicillin and clavulanic acid.

Objective: To investigate the value of fibrinogen to albumin ratio (FAR) at admission on predicting spontaneous recanalization of infarct-related artery (IRA) in patients with acute ST-segment elevation myocardial infarction (STEMI). Methods: Clinical data from 255 acute STEMI patients ((61.1±11.2) years old, 189 males) who underwent emergency coronary angiography within 12 hours in our hospital from December 2015 to April 2018 were retrospectively analyzed. The acute STEMI patients were divided into non-spontaneous recanalization group (thrombolysis in myocardial infarction (TIMI) flow grade 0-1, 203 cases) and spontaneous recanalization group (TIMI flow grade 2-3, 52 cases). Multivariate logistic regression analysis was used to evaluate related factors of IRA spontaneous recanalization. The receiver operating characteristic (ROC) curve was used to evaluate the value of FAR in predicting spontaneous coronary recanalization. Results: There was no significant difference in age,gender, hypertension, diabetes, smoking,systolic blood pressure,diastolic blood pressure,heart rate, duration of chest pain, type of infarction, infarct-related artery, door-to-balloon time, and drug used before admission between non-spontaneous recanalization group and spontaneous recanalization group (all P>0.05). The FAR and high-sensitivity C-reactive protein levels were significantly lower in the spontaneous recanalization group than in the non-spontaneous recanalization group (8.20±1.85 vs. 11.02±2.75, P<0.001; (6.87±3.36) g/L vs. (8.51±3.72) g/L, P=0.004). Multivariate logistic regression analysis showed that FAR (OR=0.492, 95%CI 0.354-0.686, P<0.001), serum uric acid (OR=0.994, 95%CI 0.989-0.999, P=0.018) and high-sensitivity C-reactive protein (OR=0.774, 95%CI 0.614-0.975, P=0.030) were independent negative correlation with spontaneous recanalization of infarct-related artery in patients with acute STEMI. The ROC curve showed that the area under the curve of FAR predicting spontaneous recanalization of infarct-related artery in patients with acute STEMI was 0.807 (95%CI 0.630-0.758, P<0.001), and the diagnostic threshold was 9.26, the sensitivity was 76.9%, the specificity was 75.9%. Conclusion The level of admission FAR has certain predictive value for spontaneous recanalization of infarct-related arteries in patients with acute STEMI.

The long-term presence of non-steroidal anti-inflammatory drugs (NSAIDs) in the environmental water samples not only affects the life safety of aquatic organisms and disturbs the ecoenvironment, but also poses a serious threat to human health. In this study, amino-functionalized Fe3O4 nanoparticles (Fe3O4-NH2) were firstly prepared by solvothermal method. Subsequently, polyethyleneimine (PEI) with a branched chain structure was successfully grafted onto Fe3O4 nanoparticles by Schiff base reaction in aqueous solution at room temperature using glutaraldehyde as a cross-linking agent, and a recyclable PEI-grafted magnetic nano-sorbent (Fe3O4@PEI) was synthesized and applied for the detection of NSAIDs in the environmental water samples. The compositional properties of Fe3O4@PEI were investigated by different characterization methods and the parameters affecting the extraction of NSAIDs were optimized. Due to high adsorption of Fe3O4@PEI for NSAIDs, the quantitative analysis of four NSAIDs in the environmental water samples, ketoprofen, naproxen, diclofenac and tolfenamic acid, was performed in combination with high-performance liquid chromatography. A good linear relationship between the chromatographic peak area and concentration was observed in the range of 1−500 µg/mL. The recoveries of the samples at three different spiked levels ranged from 85.6% to 107.8%; the intra-day precision was less than 7.8% (n=6); and the inter-day precision was less than 9.5% (n=3). The method is simple, rapid, accurate and reliable, and can be used for the analysis of NSAIDs in the environmental water samples．

OBJECTIVE To establish a method for the content determination of 11 components such as protodioscin in Guge fengtong tablets， and to evaluate the comprehensive quality of Guge fengtong tablets by combining with chemometric analysis and entropy weight-technique for order preference by similarity to ideal solution （EW-TOPSIS） method. METHODS HPLC method was adopted. The determination was performed on Agilent Eclipse Plus C18 column with a mobile phase consisted of acetonitrile- 0.2% phosphoric acid solution at the flow rate of 1.0 mL/min by gradient elution. The column temperature was set at 30 ℃ . The detection wavelengths were set at 203 nm （0-28 min， protodioscin， methyl protodioscin， pseudoprotodioscin， dioscin） and 280 nm （28-60 min， catechin， epicatechin， liquiritigenin， medicarpin， 6-gingerol， 8-gingerol， 10-gingerol）； the sample size was 10 μL. Using epicatechin as the internal reference， quantitative analysis of multi-components by single marker （QAMS） method was used to determine the contents of protodioscin， methyl protodioscin， pseudoprotodioscin， dioscin， catechin， liquiritigenin， medicarpin， 6-gingerol， 8-gingerol and 10-gingerol， which were compared with the results of the external standard method. SPSS 26.0 software and SIMCA 14.1 software were used for principal component analysis and orthogonal partial least squares-discriminant analysis， with variable importance in projection （VIP） value greater than 1 as the standard， to screen for differential markers that affect the quality； the EW-TOPSIS method was adopted to evaluate the quality of 15 batches of samples comprehensively.RESULTS The contents of protodioscin， methyl protodioscin， pseudoprotodioscin， dioscin， catechin， liquiritigenin， medi-carpin， 6-gingerol， 8-gingerol and 10-gingerol determined by HPLC combined with QAMS were 6.330-10.863， 1.150-2.274， 0.431- 0.740， 2.818-4.823， 0.826-1.510， 0.043-0.094， 0.079-0.231， 0.479-1.020， 0.146-0.288， 0.118-0.318 mg/g， respectively； there were no statistical significances， compared with the external standard method （P＞0.05）. A total of 15 batches of samples were clustered into 3 groups， with S1-S6， S7-S10， and S11-S15 clustered into one group， respectively. The VIP values of protodioscin， epicatechin， dioscin and 6-gingerol were greater than 1. Euclidean closeness values of the optimal solution （C）i for 15 batches of samples were 0.163 5 to 0.703 7， and Ci values of S11-S15 were all higher than 0.6. CONCLUSIONS The established QAMS method is accurate and simple， and can be used for comprehensive quality evaluation of Guge fengtong tablets， by combining with chemometric analysis and EW-TOPSIS method. Protodioscin， epicatechin， dioscin and 6-gingerol are the differential markers that affect the quality of Guge fengtong tablets. Samples S11-S15 have better quality.