ABSTRACT
Mogroside V is the most abundant [approximately 0.50%] cucurbitane-type triterpene glycoside in Siraitia grosvenorii and exhibits significant antitussive, expectorant, anti-carcinogenic, and anti-inflammatory effects. A sensitive, robust and selective liquid chromatography tandem with mass spectrometry [LC-MS/MS] was developed and validated for the determination and pharmacokinetic investigation of mogroside V in rat plasma. Samples were prepared through an one-step deproteinization procedure with 250 microL of methanol to a 75-microL plasma sample. Plasma samples were effectively separated on a Shiseido Capcell Pak UG120 C18 column [2.0 × 50mm, 3.0microm] using a mobile phase consisting of methanol: water [60:40, v/v] with an isocratic elution program. The running time for each sample was 7.0 min and the elution times of mogroside V and IS were 2.0 and 4.8 min, respectively. The detection relied on a triplequadrupole tandem with mass spectrometer equipped with negative-ion electrospray ionization interface by selectedreaction monitoring [SRM] of the transitions at m/z 1285.6 - 1123.7 for mogroside V and m/z 1089.6 - 649.6 for IS. The calibration curve was linear over the range of 96.0-96000 ng/mL with a limit of quantitation [LOQ] of 96.0ng/mL. Intra-day and inter-day precisions were both <10.1%. Mean recovery and matrix effect of mogroside V in plasma were in the range of 91.3-95.7% and 98.2-105.0%, respectively. This method was successfully applied in the pharmacokinetic study of mogroside V after intravenous or intraperitoneal administration of 1.12mg/kg mogroside V in rats
ABSTRACT
Targeted therapeutic drug,having such advantages as targeting,safety,convenience,etc,is increasingly favored by non-small cell lung cancer (NSCLC) patients.At present,there are many kinds of molecular targeted drugs used in clinic,and remarkable efficacy was achieved,and the pain caused by conventional chemotherapy was avoided.At the same time,with the deepening of the understanding of the mechanism of tumor immune,new targeted drugs will also continue to be developed.The emergence of the third generation EGFR-TKI brings new hope for first generation EGFR-TKI resistant patients.Combined use of different immune therapeutic agents,combined application of immunotherapy drugs and cytotoxic chemotherapy drugs and radiotherapy,and the exploration of its predictive biomarkers will become a hot spot in the research of lung cancer.This will undoubtedly bring a new dawn for the treatment of NSCLC.Based on the domestic and foreign research literatures and related materials,this article reviews the latest research progress of various molecular targeted drugs for treatment of NSCLC.
ABSTRACT
OBJECTIVE:To provide reference for promoting rational use of vancomycin in the clinic. METHODS:Referring to vancomycin instruction,Guiding Principles for Clinical Use of Antibacterials (2015 edition) and Chinese Expert Consensus on Clinical Use of Vancomycin (2011 edition),720 inpatient medical records of vancomycin were collected from our hospital during Jan. 2013-Dec. 2014,and then drug use of those inpatients were analyzed retrospectively. RESULTS:Among 720 cases,male (428 cases)was more than female(292 cases),and most of them aged 41-65(45.83%). There were 50 cases of prophylactic drug use(6.94%)and 670 cases of therapeutic drug use(93.06%). The patients came from 36 departments. Among 720 cases,the dose of 19 cases were higher than 2 g/d,and there were 13 ADR cases(1.81%). Among 670 cases of therapeutic drug use,587 cases of microbiological samples (87.61%) were detected,and other antibacterials were used in 522 cases additionally (77.91%). DUI of vancomycin was equal to 0.96 in 549 cases no younger than 18 years old of herapeutic drug use. There were 240 cases of unsuit-able drug use (33.33%) in total,including 192 cases of unsuitable solvent (26.67%),28 cases of unsuitable usage and dosage (3.89%)and 20 cases of unsuitable drug combination(2.78%). CONCLUSIONS:The use of vancomycin in our hospital is basi-cally rational;vancomycin is widely used in departments;drug combination is a common phenomenon;the inspection rate of mi-crobiological samples is qualified;no drug abuse is found. However,there still is inappropriate use in the clinic. It is recommended to strengthen special evaluation and training about rational use of vancomycin,and further standardize monitoring for vancomycin use so as to guarantee the safety of drug use.
ABSTRACT
OBJECTIVE:To provide reference for solving the shortage of national essential medicines in Changchun. METH-ODS:According to preliminary work,a questionnaire was conducted to investigate and statistically analyze the shortage situation of essential medicines in 22 higher than secondary and 50 basic medical and health institutions in Changchun;ABC analysis was used to analyze the national essential medicines in shortage;the bid results and shortage causes of the primary and secondary nation-al essential medicines in shortage were inquired. RESULTS:Totally 72 questionnaire were send out,and 72 were recycled with ef-fective recovery of 100%. The investigation results showed there were 19 shortage breeds(22 dosage forms),which lost the bid-ding,and 99 breeds(111 dosage forms)of national essential medicines in shortage,which won the bidding,including 85 kinds of chemical medicines and biological products,14 kinds of Chinese patent medicine in Changchun. Cardiovascular system drugs shows the largest number in the bid chemical medicines and biological products,and the Chinese patent medicine were mainly Fu-zheng agent and Quyu agent(internal medicine). Results of ABC analysis showed,among the 111 bid shortage dosage forms,17 were primary and 23 were secondary. The main causes for them were price raising in raw materials,lack of production,no produc-ing in manufacturers and purchase price higher than winning bids. CONCLUSIONS:Low accessibility of raw material drugs,low enthusiasm to production,lower drug price than a reasonable level,and small clinical requirements can lead to the shortage of na-tional essential medicines. It is suggested to intensify in supervising the raw materials’marketing,raising the enthusiasm of manu-facturers,perfecting the system of drug bidding,developing fixed-point production and building drug reserve system to guarantee the production and supply of national essential medicines,and satisfy clinical demands.
ABSTRACT
Objective To study the effect of resveratrol on hepatitis B virus (HBV) and hepatic fibrosis.Methods The rat model of HBV infection was established by intraperitoneal injection of rAAV8-1.3HBV.After successfully establishing the modle, were randomly divided into four groups:negative control group, resveratrol low dose group, high dose group, positive control group, and five rats in each group.Giving a physiological saline, 20 mg/kg respectively resveratrol, 40 mg/kg, 0.1 mg/kg acyclovir via gastrogavage respectively.2、4、8、12 weeks later ,we detected the HBsAg, HBeAg, HBV-DNA via tail vein blooding.HSC-T6 cell model was established.Then rats were divided into two groups, control and resveratrol serum group.Each group was administrated with normal sodium and resveratrol via gastrogavage to make serum.The HSC-T6 viability was observed by AlamarBlue assay.The expression of Col I and TGP-β1 mRNA was determined by Realtime PCR.The expressions of Col I and TGP-β1 Protein was analyzed by WesternBlot.Results Using ELISA method to detect HBsAg、HBeAg、HBV-DNA and found that the expression of HBsAg and HBeAg of negative control group were significantly higher than the rest of the three groups (P<0.05) at the second and the fourth week.The highest expression of HBsAg and HBeAg were (4118 ±367) IU/mL、(160.2 ±56.90) NCU/mL at the second week.The expression of HBV-DNA of negative control group is significantly higher than the rest of the three groups (P<0.05) at the second week.AlamarBlue assay indicated that different concentration of serum of resveratrol can inhibit HSC-T6 proliferation.Compared with control group, serum with drug resveratrol significantly down-regulated the mRNA and protein expression of Col I and TGP-β1.Conclusion Resveratrol inhibits HBV and liver fibrosis by inhibiting type I collagen and TGF-β1.
ABSTRACT
Objective To study effect of a novel schiff base ruthenium coordination compound on cell proliferation and apoptosis of gastric cancer SGC-7901 cell.Method Gastric cancer SGC-7901 cell were divided into four groups according to different treatment of novel schiff base ruthenium coordination compound (concentration of 10, 30, 50μmol/L) and blank group with DMSO.Cell proliferation was detected by MTT assay, cell apoptosis and cell cycle were analysed by flow cytometry.ResuIts MTT results showed the inhibitory effect of novel schiff base ruthenium coordination compound on SGC-7901 cell enhanced with the increase of its concentration, and inhibitory rates were higher than that of blank group at 24, 48, 72 h.Flow cytometry results showed the apoptosis rate of novel ruthenium coordination compound groups of 10, 30, 50μmol/L were (17.64 ±1.21)%, (26.47 ± 0.61)%, (55.63 ±1.49)%, respectively, all higher than that of blank group (P<0.05).The cell proportion of G1 phase increased with the increasing of the novel schiff base ruthenium coordination.ConcIusion A novel schiff base ruthenium coordination compound could inhibit the growth of gastric cancer SGC-7901 cells, promote apoptosis and arrest gastric cancer SGC-7901 cells at G1.
ABSTRACT
Objective To investigate the immune response of Adefovir ester combine the Fuzheng Huayu in the process of the treatment of chronic hepatitis B.Methods 100 cases with CHB from March 2010 to October 2014 collected in outpatients clinic or hospital were randomly divided into Adefovir ester treatment group and Adefovir ester joint the Fuzheng Huayu treatment group.Levels of AST, ALT, HBsAg and HBV DNA pre-and-post treatment were detected.CD3-CD56 +,CD244 +NK,CD3 +,CD3 +CD4 +,CD3 +CD8 +T cells and the contents of CD 4 +T cells in serum of two groups were measured by flow cytometry analysis.Results The levels of AST、ALT、HBV-DNA of two group post-treatment were all significantly lower than pre-treatment(P<0.05),and the level of AST and ALT in Adefovir ester and Fuzhengh Huayu treatment group at 3 months and 6 months were obviously lower than Adefovir ester treatment group.HBV-DNA contents between two groups had no significant difference.HbsAg levels of two groups were all significantly increased after 6,9,12 months’treatment (P<0.05),While there was no significant difference between two groups post-treatment.CD3-CD56 +cell at 6,9,12 months in two groups were all higher than pre-treatment(P<0.05), which in Adefovir ester and Fuzhengh Huayu treatment group were more higher than Adefovir ester treatment group(P<0.05).CD244 +NK,CD3 +T cell, CD3 +CD4 +Tcell at each point post-treatment in peripheral blood of two groups were all increased significantly(P<0.05),which in Adefovir ester and Fuzhengh Huayu treatment group increased more obviously than Adefovir ester treatment group (P<0.05).However, CD3 +CD8 +cells were reduced obviously after treatment in two groups(P<0.05), which besides 3 month point, its ratio in Adefovir ester and Fuzhengh Huayu treatment group decreased more significantly than Adefovir ester treatment group at other points( P<0.05 ).Cytokines in serum of two groups were all increased significantly post-treatment ( P<0.05 ) , which in Adefovir ester and Fuzhengh Huayu treatment group were more lower (P<0.05).Conclusion Adefovir ester and Fuzhengh Huayu treatment can improve the situation of AST, ALT, HBV DNA and HBsAg in patients with chronic hepatitis B,promote the expression of NK cells,T cells and Tcell secrited cytokines,and the efficacy is better than Adefovir estertreatment alone.
ABSTRACT
OBJECTIVE:To discuss the role of clinical pharmacist on drug use intervention in pediatric ward. METHODS:During Aug.-Dec. in 2014,clinical pharmacists provided whole-course pharmaceutical care for 493 pediatric patients with chronic disease in pediatric ward of our hospital,guided rational drug use,and analyzed and summarized the problems. RESULTS:Clini-cal pharmacists intervened in drug use in 70.99%patients,with success rate of 96%. Among them,top three types of the non-stan-dard medication were:non-standard medication time,incorrect usage and missed medication. CONCLUSIONS:Due to clinical phar-macists’intervention,the problems of drug therapy can be found so as to put forward reasonable suggestions and guidance,reduce the incidence of ADR,and improve the effective rate and success rate.
ABSTRACT
OBJECTIVE:To provide a reference for clinical use of anti-tumor adjuvant drugs as is reasonable,effective and economical. METHODS:By retrospective investigation and analysis,the utilization of anti-tumor adjuvant drugs in the oncology department of our hospital during 2010 and 2013 was analyzed statistically in respect of the type,dosage form,consumption amount,DDDs,DDC,DUI etc. RESULTS:The anti-tumor adjuvant drugs in our hospital were dominated by injections,especial-ly domestic drugs,the consumption amount of which accounted for 80% of the total consumption amount of anti-tumor adjuvant drugs each year. The anti-tumor adjuvant drugs were mainly used for symptomatic treatment of various adverse reactions. Drug syn-chronization was relatively good each year,however,excessive use of individual drugs existed. CONCLUSIONS:Anti-tumor adju-vant drugs have relatively better synchronism in the drugs quantities and medication number. However,individual drugs have exces-sive use and other irrational use.
ABSTRACT
Objective To explore the inhibition of Zn(PMFPCl) 2 on HepG2 cells and its mechanism.Methods The HepG2 cells were divided into control group and experimental group of 10, 30 and 70 μmol/L.The cell proliferation was detected by MTT assay, cell apoptosis and cell cycle was analysed by flow cytometry, cellular morphological change was observed with inverted microscope and the expressions of apoptosis-regulated proteins of p53, p21, caspase-3, bax and bcl-2 in HepG2 cells were detected by Western blot.Results The inhibitory rates of experimental groups (10, 30, 70μmol/L) at 24, 48 and 72h were significantly higher than those of control group (P<0.05), and the highest one was 63.29% of 70 μmol/L Zn (PMFPCl)2at 72 h.The apoptosis rates of each experimental group at 48h was significantly higher than that of control group (P<0.05).The cells were induced a remarkable G1 arrest by Zn(PMFPCl) 2 which could inhibit proliferation.The number of adherent cells reduced and cells shrank, convex on cytomembrane surface appeared and the cells changed to round and were brighter.Western blot results showed that the protein levels of p53, p21, caspase-3 and bax increased and bcl-2 decreased with the Zn(PMFPCl)2concentration increasing (P<0.05).Conclusion Zn(PMFPCl)2 could inhibit the proliferation and promote apoptosis of HepG2 cells whose mechanisms are promotation of p53, p21, caspase-3 and bax expressions and inhibition of bcl-2 expression.
ABSTRACT
Objective To understand the progress of paclitaxel carriers, to provide theoretical support for research of paclitaxel carriers and clinical use of paclitaxel.Methods To study literatures on paclitaxel carriers recently and understand the research direction of paclitaxel carriers.Subsequently, the advantages and disadvantages of various paclitaxel carriers were analyzed and summarized.Results Paclitaxel as an effective anti-tumor chemotherapy drugs, had poorly water-soluble, serious toxicity and side effects, which limited the wide application of paclitaxel to some degree.Development of liposomes, micelles, microspheres, nanoparticles and other new dosage forms had broken these restrictions, which had vital significance.Conclusion Paclitaxel carriers can improve the solubility of the drug, reduce side effects, and develop toward multi-functional and finely targeted.
ABSTRACT
Objective To determine serum concentration of methotrexate in children with acute lymphoblastic leukemia by HPLC and explore the application practice.Methods The separation was performed in a Wondasil C18-WR column (4.6 mm ×150 mm, 5 μm) with a mobile phase of methanol-0.15%phosphoric acid solution(21:79 ) and determined at 306 nm.The sample of serum was centrifuged after protein precipitation with perchloric acid.Detected results for children to establish monitoring files.ResuIts The linearity was well at 0.02 ~50 μg/mL of methotrexate ( r =0.9990,n=6).The average recovery was 96.50%, RSD of within day and between days were less than 15%.Established monitoring files for six children and after 3 courses of treatment, the blood concentration of methotrexate in 4 children were small and they were in a safe range , which could reduce the frequency of monitoring.ConcIusion This method is simple, sensitive and accurate for methotrexate detection in serum.The children with stable concentration and within safety range, can reduce monitioring frequency.It could bring the children less pain and relieve the burden of family.
ABSTRACT
Lurasidone is a new atypical antipsychotic drug, it was approved by the Food and Drug Administration ( FDA ) for treatment of schizophrenia on october 28,2010.The article is to provide an review about pharmacological effects, clinical applications, pharmacokinetics, dosage, drug interactions, adverse reactions of Lurasidone.
ABSTRACT
Objective To investigate effect of high glucose on the function of endothelial and the underlying mechanisms in human umbilical vascular endothelial cells (HUVECs).Methods The experiment was divided into 4 groups: normal group (NG), low dose group (LG), middle dose group (MG) and high dose group ( HG) .The concentration of glucose in the culture medium was 5.5, 10, 20, 30 mmol/L in the 4 groups, respectively.The HUVECs was cultured for 0, 24, 48 h.At different time point, the cell viability were measured by MTT.The secretary content of nitric oxide (NO) in the supernatant were detected using test kit.The extraction of protein were extracted for Western blot analysis to detect the expression of endothelial nitric oxide synthase (eNOS).ResuIts Compared with normal group at same time point (cultured for 24 h), the cell viability and the content of NO were significantly decreased in LG, MG(P<0.05).The expression of eNOS in HG were markedly reduced (P<0.01).Compared with normal group at same time point (cultured for 48 h), the cell viability decreased significantly in HG (P <0.05).The expression of eNOS were markedly decreased 11.91, 25.72 and 34.50% in LG, MG and HG, respectively.A rising trend of cell viability were found in NG, LG and MG, but a descending trend were found in HG within 48 h.ConcIusion The cell viability were significantly affected by high glucose.The endothelial dysfunction induced by high glucose may be associated with the reduction of eNOS and NO production.
ABSTRACT
Objective To study the inhibitory effect of miR-199a on bladder cancer.Methods T24 bladder cancer cells were divided into control group, pre-scamble group and pre-miR-199a group according to different treatment.Cell proliferation was assayed by MTT, cell apoptosis and cell cycle by flow cytometry, and cell invasion by Transwell.ResuIts The OD value of pre-miR-199a group (0.436 ±0.042) was significantly lower than that of control group (0.634 ±0.020) and pre-scamble group (0.601 ±0.059)(P<0.05).Cell apoptosis of pre-miR-199a group(19.25 ±1.57)% was higher than that of control group(10.19 ±0.98)% and pre-scamble group(12.27 ±1.38)%(P<0.05).The cell ratio in G1 phase of control group、pre-scamble group and pre-miR-199a group was 45.09%, 47.57%, and 58.62%, respectively.The cell cycle arrested in G1 phase after transfected with pre-miR-199a.The cells migration number of pre-miR-199a group (46.00 ±1.58) was lower than those of control group(67.00 ±1.58) and pre-scamble group(61.20 ±1.30)(P<0.05).ConcIusion MiR-199a could inhibit the growth of bladder cancer cells.
ABSTRACT
Objective To prepare butenafine hydrochloride plastics,investigate the prescription composition and make a quality control standard for the preparation.Methods Film-forming time and appearance quality as the evaluation index,the quality control standard of butenafine hydrochloride according to the Chinese pharmacopoeia two section ( 2010 edition ) was made.ResuIts The prescription of butenafine hydrochloride plastics was identified as:1%butenafine hydrochloride(w/w),10%glycerol(w/w),3%carbomer 971PNF(w/w),0.1% ethyl p-hydroxybenzoate(w/w),moderate anhydrous sodium sulfite(pH adjusting agent) and 95% ethanol (solution).The preparation was colorless,transparent and viscous semi-solid with pH4.5.A content determination method of butenafine hydrochloride with HPLC was established and the result was stable and reliable .ConcIusion The butenafine hydrochloride has several advantages such as preparation simply , stable property,application convenience and quality control.It is a potential preparation to develop.
ABSTRACT
Objective To prepare pemirolast potassium nasal spray which could be used in treatment of allergic rhinitis and make a quality control standard for the preparation.Methods The preparation materials of nasal spray was selected which could meet the physical and chemical properties of pemirolast potassium as well as the characteristics of intranasal administration.The quality control standards for pemirolast potassium nasal spray was made according to the nasal spray quality standards for the formulation pH, property, loading capacity, total bottle spray times, puff volume, sedimentation volume ratio and detection of content of “Chinese Pharmacopoeia” two section (2010 edition).Results The formulation prescription of pemirolast potassium nasal spray was:0.1% potassium pemirolast, 0.8% CMC-Na, 0.01% benzalkonium bromide, glacial acetic acid ( pH adjusting agent) and the solution was 5% mannitol.The formulation was a white suspension, pH=7.The mean value of installed capacity was (25.12 ±0.16) mL and installed capacity of each bottle was above 23.75 mL(95%); total spray times of each bottle was above 160 sprays and spray volume was above 0.140 0 g/press; sedimentation volume ratio was 1, the above testing programmes of quality standard met the requirements and were controlled.The standard curve of pemirolast potassium reference substance was Y=81085X+15264(r=0.999 8), linearity range was 0.5~25.0μg/mL.The average recovery rate of pemirolast potassium sample was 99.39%, and precision met the requirements.The pemirolast potassium content of test sample was 99.2% of labeled amount.Conclusion The formulation prescription of pemirolast potassium nasal spray is suitable and the preparation is possessed several advantages such as stability, well-distributed spray, application convenience and quality controlled.Therefore, nasal administrated formulation of pemirolast potassium is potentially in further.
ABSTRACT
Objective To investigate effect of glucose and lipid metabolism on acute cerebral infarction patients by Rhodiola injection. Methods 201 cases of acute cerebral infarction patients were selected,and divided into experiment group and control group.The control group of 101 cases were treated by clinical routine therapy,the experiment group 100 cases were treated with Rhodiola injection.The clinical efficacy, blood rheology and blood lipids, blood glucose index were compared before and after treatment.Results After 2 weeks of treatment, the total effective rate in experimental group was significantly higher than the control group(χ2 =12.596, P<0.05), with statistical difference.Patients in the experimental group,FBG was significantly lower than the control group, the difference was statistically significant (t=8.830, P<0.05).Patients in the experimental group TG, TC, LDL-C were significantly lower than that of control group, HDL-C was significantly higher than control group (P<0.05).Blood rheology indexes decreased significantly better than the control group ( P<0.05 ) .Conclusion Rhodiola injection on patients with acute cerebral infarction has good clinical curative effect, and can effectively improve the blood lipid, blood glucose level, reduce blood viscosity, is of great significance to the clinical treatment of cerebral infarction.
ABSTRACT
Objective To discuss the important role of clinical pharmacists in medication reconciliation through the prac‐tice of clinical pharmacists of nephrology department .Methods The medication reconciliation serviced for the patients newly admitted to nephrology department was carried out through the way of interrogation .The difference and the causes between the results of pharmacist′s interrogation and the doctors′were analyzed .Results 20 patients were enrolled .The quantity was not consistent with what hospital doctor′s advice rate (60% ) ,drugs produced in different areas (55% ) ,different producing areas pharmacist had higher accuracy .Conclusion It had certain effect on medication management and could reduce the ADR .Clinical pharmacists and doctors should pay more attention on the medication reconciliation ,strengthen the ability of interrogation to im‐prove patient compliance and establish a complete medication reconciliation system .
ABSTRACT
Pinoresinol diglucoside [PD], a typical marker compound in Ecommia ulmoides Oliv., is an important and natural antihypertensive drug. A selective, sensitive, and rapid liquid chromatography tandem mass spectrometric [LCMS/ MS] analytical method was developed for the determination of PD in rats. After simple protein precipitation with acetonitrile, chromatographic separation of PD was conducted using a reversed-phase ZORBAX SB C[18] analytical column [4.6mm × 150mm, 5[micro]m particles] with a mobile phase of 10mM ammonium acetate-methanol-acetic acid [50:50:0.15, v/v/v] and quantified by selected reaction monitoring mode under positive electrospray ionization condition. The chromatographic run time was 3.4 min for each sample, in which the retention times of PD and the internal standard were 2.87 and 2.65min, respectively. The calibration curves were linear over the range of 1.003000ng/mL and the lower limit of quantification was 1.00ng/mL in rat plasma. The precision expressed by relative standard deviations were <8.9% for intra-batch precision and <2.0% for inter-batch precision, and the intra- and inter-batch accuracy by relative error was within the range of -3.9%-7.3%, which met acceptable criteria. The LC-MS/MS method was successfully applied to investigate the pharmacokinetics and oral bioavailability of PD in rats, with the bioavailability being only 2.5%