Showing papers in "Chinese Journal of Hospital Pharmacy in 2012"

Clinical observation on the efficacy of Shenmai injection in prevention and treatment of neurotoxicity induced by oxaliplatin-containing chemotherapy regimen

Abstract: OBJECTIVE To study the curative effect of Shenmai injection for prevention of the neurotoxicity caused by chemotherapy drug including oxaliplatin.METHODS The investigation was a prospective study of 96 patients of cancer of stomach and cancer of colon with a need for chemotherapy drug including oxaliplatin.The curative group(46 patients)began to use Shenmai injection(50ml)put in 5%GS one day before chemotherapy,1 time/d,d1-14,ivgtt.So did the control group(50patients),except Shenmai injection.To observe the variation of neurotoxicity and determine nerve peronaeus function after 4 cycles.RESULTS Incidence of neurotoxicity in the curative group was 32.6%(15/46),the other 72.0%(36/50)(P0.05).The curative group was better than the other,which was also supported by nerve peronaeus function(P0.05).that the sensory nerves conduction velocity(SCV)of curative group and control group was(40.5±3.2) m·s-1 and(34.3±3.1) m·s-1 respectively;the action potential amplitude of sensory nerves(9.0±3.8) μV and(7.2±3.3) μV.CONCLUSION It was certained that Shenmai injection was effective in preventing the neurotoxicity caused by chemotherapy drug including oxaliplatin.

Effects of Salvia przewalskii Maxim.extract on whole blood viscosity in normal rats and its diuresis in water-loaded rats

Abstract: OBJECTIVE To study the effects of whole blood viscosity in normal rats and diuresis in water load rats by Salvia przewalskii extract(SPE)METHODS SPE at three different doses(50,100,200 mg·kg-1) was administered intragastrically to Wistar normal rats at regular 24 h intervals for 15 daysAn hour later after the last intragastric administration,the blood samples of rats were obtained from rat hearts and whole blood viscosity was measuredSPE at three different doses(50,100,200 mg·kg-1) was administered intragastrically to Wistar water load rats at regular 24 h intervals for 3 daysAfter the last intragastric administration,urine was collected during 7 h in metabolic cagesRESULTS SPE could reduce whole blood viscosity of Wistar normal ratsSPE could increase urine volume of Wistar water load rats during 7 h,and mainly increase urine volume in 1~3 h periodIncrease degree of urine volume by SPE was less than that by hydrochlorothiazideCONCLUSION SPE could obviously reduce whole blood viscosity and improve blood circulation condition,and have mild diuresis effect

Effect of Radix Angelicae Dahuricae extract on P-glycoprotein activity in Caco-2 cells

Abstract: OBJECTIVE To study the effect of Radix Angelicae Dahuricae extract on intestinal transport of flavones ingredients puerarin,baicalin,and combining the effect of Radix Angelicae Dahuricae extract on P-glycoprotein activity,to explore the mechanism of Radix Angelicae Dahuricae extract improving the absorption of puerarin,baicalin.METHODS Caco-2 cell viability was measured using MTT assay in the presence of Radix Angelicae Dahuricae extract at different concentration,and using Caco-2 cell monolayer model to study the effect of Radix Angelicae Dahuricae extract on the absorption of puerarin and baicalin respectively.Rhodamine123(R-123),a P-gp substrate,was selected as fluorescent probe.A fluorescence spectrophotometer method was used to determine the concentration of R-123 in Caco-2 cells.RESULTS Radix Angelicae Dahuricae extract could significant increase the absorption of puerarin in Puerariae and the absorption of baicalin in Radix Scutellariae,the apparent permeability coefficients(Papp) of puerarin and baicalin was increased by 1.6-3.6 folds and 2.3-3.3 folds respectively.Coumarins(0.15-1.5 mg·mL-1) of Radix Angelicae Dahuricae extract,volatile oil(0.24-6.0 μL·mL-1) of Radix Angelicae Dahuricae extract,coumarins combined with volatile oil all could significantly enhance the accumulation of R-123 in Caco-2 cell,and significantly,dose-dependently inhibited P-gp.CONCLUSION The reason of Radix Angelicae Dahuricae extract to improve the absorption of flavones ingredients is related to the inhibitory effect of Radix Angelicae Dahuricae extract on P-gp activity.

Comparative studies on anti-thrombus and anti-coagulation effects of Hirudo of different species

Abstract: OBJECTIVE To study and compare the anti-thrombus effects and anti-coagulation activities of Hirudinaria manillensis and Whitmania pigra in vivo and in vitro.METHODS The in vitro anti-coagulation activities of the two species of leeches after different processes were evaluated by directly titration on thrombin.The cerebral thrombosis induced by intravenous injection with adrenalin-collagen,caudal vein thrombosis caused by carrageenin and thrombosis formed in arteriovenous shunt models were used to assess the anti-thrombus effects of the two species of leeches.The in vitro anti-coagulation activities of the two species of leeches after different processes were evaluated by cutting-tail method and capillary method.RESULTS The anti-coagulation activity in vitro of Whitmania pigra was quite better than the fresh and dry Hirudinaria manillensis.Fresh and dry Hirudinaria manillensis and Whitmania pigra after different processes had anti-thrombus activities in vivo,and fresh Hirudinaria manillensis had the highest activity while Hirudinaria manillensis after decoction hardly had any activity in vivo and in vitro.CONCLUSION The active constituent of Hirudinaria manillensis is dramaticlly different from Whitmania pigra,moreover,Hirudinaria manillensis has much more bioactivity than Whitmania pigra which is widely used recently.

Effects of the volatile oil of Nardostachys chinensis administered at different time points on myocardial ischemia-reperfusion injury in rats

Abstract: OBJECTIVE To investigate the effects of the volatile oil of Nardostachys chinensis administered at different time points on myocardial ischemia-reperfusion injury in rats.METHODS Forty Sprague Dawley rats were randomly divided into sham group(n=10),ischemia/reperfusion group(n=10),the volatile oil of Nardostachys chinensis group-1(n=10);the volatile oil of Nardostachys chinensis group-2(n=10).The infarct size,serum levels of interleukin-6(IL-6) and tumor necrosis factor-α(TNF-α),CK-MB,cTnT in each group were investigated;and the ventricular arrhythmias in each group were recorded.RESULTS The serum levels of CK-MB,cTnT,IL-6,TNF-α and infarct size were significantly reduced in the volatile oil of Nardostachys chinensis group-1 and the volatile oil of Nardostachys chinensis group-2(P0.05),however the reduction was more significant in the volatile oil of Nardostachys chinensis group-1.CONCLUSION The volatile oil of Nardostachys chinensis administered before myocardial ischemia-reperfusion injury in rats had protective effects on myocardial ischemia/reperfusion injury.The mechanism of action may possibly relate to the inhibiting early inflammatory reaction,blocking the L-type calcium channel,and the prolongation of the effective refractory period(ERP) of the heart muscle.

In vitro study on the interactions of P-gp and central depressants

Abstract: OBJECTIVE Based on new detoxication mechanism rescuing for central depressants detoxification through induction P-gp transportation by up-regulate MDR1 gene,it is necessary to establish P-gp substrates spectrum to match the novel methodMETHODS By using ATPase activity assay to identify whether the six central depressants were P-gp substratesRESULTS Sulpiride,ziprasidone,zopiclone,clomipramine,citalopram and moclobemide were all P-gp substrates,sulpiride,ziprasidone and citalopram were non-concentration dependent ATPase inhibitors,zopiclone,clomipramine and moclobemide were concentration-dependent bidirection regulators of ATPaseCONCLUSION The results of this study provide references and basis for clinical application of the new detoxication treatment of central depressants

Comparison on adding sitagliptin or glimepiride in poorly controlled overweight type 2 diabetes with oral metformin

Abstract: OBJECTIVE To compare the efficacy and safety between sitagliptin and glimepiride in poorly controlled overweight type 2 diabetes(T2DM)with oral metformin.METHODS 116 T2DM patients were randomized to two groups of receiving sitagliptin with metformin(treatment group) and glimepiride with metformin(contral group)for 24 weeks.RESULTS After 24 weeks,FPG,2hPG and HbA1c were significantly decreased than before,but there were no statistical difference between two groups(P0.05).The increased weight was less in treatment group(-1.2±0.3)kg than in control group(0.6±0.2)kg(P0.01).Hypoglycemic rate was 1.7% in treatment group and 6.9% in control group(P0.05).CONCLUSION Adding sitagliptin or glimepiride in poorly controlled overweight T2DM patients with metformin could control the glycemia effectively,but sitagliptin will achieve better benefit in reducing weight gain and the incidence of hypoglycemia.

An analytical method built for irinotecan and its active metabolite SN-38 in human plasma using HPLC-FLD

Abstract: OBJECTIVE To develop and validate a method for simultaneous determination of irinotecan(CPT-11) and its metabolite SN-38 in human plasma by HPLC-FLD METHODS Chromatographic separation was performed on a Luna 5u CN 100A column(46 mm×150 mm,5 μm),using acetonitrile: ammonium acetate(50 mmol·L-1,pH=4) as mobile phaseThe detection wavelength of CPT-11 was Ex/Em=368 nm/432 nm,and the detection wavelength of SN-38 was Ex/Em=368 nm/535 nm RESULTS The retention time of CPT-11 and SN-38 was(93±03)min and(48±03)min,respectivelyNo interfering peaks were observed at the retention time of both targets and interna standardsThe assay was linear at the range 469-6 0000 nmol·L-1 for CPT-11(r=0998) and 20-2500 nmol· L-1 for SN-38(r=0998)Both the inter-and intra-batch precisions were less than 20% at the low concentration and less than 15% at the middle and high concentrationsThe inter-and intra-accuracies were all between 85% and 115%The spiked plasma samples were stable at-20 ℃ in a long-term stability testAfter three freeze-thaw cycles of the spiked samples,the changes in levels of SN-38 and CPT-11 were both within 15%The changes in levels of SN-38 and CPT-11 in 24 h after extraction were not obvious CONCLUSION HPLC-FLD method for detection of concentrations of irinotecan(CPT-11) and its active metabolites SN-38 in human plasma is simple,accurate and sensitive

Study on the anti-tumor effect of polysaccharides from Cornus officinalis and its immunologic mechanism

Abstract: OBJECTIVE To study the anti-tumor effect of polysaccharides from Cornus officinalis and its immunologic mechanism. METHODS S180 mice were adopted to observe the anti-tumor effect of polysaccharides from Cornus officinalis and to study in vivo and in vitro immunologic mechanism of action on peripheral blood CD4+T cells,CD8+T cells,interleukin IL-2 and interleukin IL-4 in tumor-bearing mice,compared with negative control. RESULTS Polysaccharides from Cornus officinalis could apparently restrain S180 noticeably(P0.01),increased the expression of CD4+T cells and decreased the expression of CD8+T cells in peripheral blood,and increased the level of interleukin IL-2,decreased interleukin IL-4.It had a positive correlation with dosage and concentration. CONCLUSION Polysaccharides from Cornus officinalis exerted its anti-tumor effect via the mechanism of regulative action on abnormal immunological condition in tumor-bearing mice.

Study on pharmacokinetics-pharmacodynamics of geniposide in HuanglianJieduTang active fraction(HLJDTAF)

Abstract: OBJECTIVE To study the pharmacokinetics pharmacodynamics of geniposide in HLJDTAF in MCAO model rats.METHODS MCAO model was established by electrocoagulation,sham-operated group and model group were given orally with HLJDTAF,the rats' bloods were collected at different time.The concentrations of geniposide in rats' plasma were determined to draw the time-concentration curve;the activity of SOD and the level of MDA in plasma were determined to draw the time-effect curve.Combined with the time-concentration curve and the time-effect curve,the concentrations of geniposide in plasma of sham-operated group and model group were compared after oral administration of the same dose of HLJDTAF.RESULTS Geniposide in model group was absorbed rapidly,fast metabolized and maintained shorter time,which reflected that in body with strong cyclical characteristics;compared with the sham-operated group,geniposide had a better absorption in MCAO rats and its content of MDA in plasma increased significantly.HLJDTAF could significantly reduce the content of MDA in MCAO rats;compared with sham-operated group,activity of SOD decreased in MCAO group and HLJDTAF could increase the activity of SOD.CONCLUSION HLJDTAF played a role in anti-ischemic brain injury,and its function connected with the content of geniposide in vivio;geniposide had effect of anti-ischemic brain injury and could increase the activity of SOD and debase the content of MDA.

Ameliorating effects of essential oil from Fructus Apliniae zerumbet(EOFAZ) on NOS-NO system in human umbilical vein endothelial cells injury(HUVECs) induced by oxidized-low density lipoprotein(ox-LDL) in vitro

Abstract: OBJECTIVE To investigate the protective effects of essential oil from Fructus Apliniae zerumbet(EOFAZ) on human umbilical vein endothelial cells(HUVECs) injury induced by oxidized low density lipoprotein(ox-LDL),and explore the ameliorating effects on NOS-NO systemMETHODS The in vitro cultured HUVECs were pre-incubated with 01 and 001 μg·mL-1 EOFAZ 24 h,and then exposure to ox-LDL 24 hThe cyto-morphological change was observed by inverted phase contrast microscope and Giemsa staining assayThe NO content in medium and NOS subtype activities in cell lysis were assayed by colorimetric methods according to the instruction of commercial kitsRESULTS After exposuring to ox-LDL for 24 h,the numbers and morphology of HUVECs were significantly changed by the inverted phase contrast microscope and Giemsa staining compared with control groupThe NO contents in medium were significantly decrease compared with control group,the tNOS and eNOS activities of cellular lysis as wellPre-treated with EOFAZ which ameliorated the cytomorphology and increased the number of HUVECs,significantly enhanced the activities of tNOS and eNOS of cell lysis,and the NO contents in mediumHowever,there were no any significant changes of iNOS activity whether in model group or pre-treated with EOFAZCONCLUSION EOFAZ can ameliorate the HUVECs injury induced by ox-LDL,and the mechanism maybe related to enhancement of eNOS activity of cells and promotion of promote NO secretion

Study on the chemical constituents and anticancer activity from the roots of Rubia cordifolia L.

Abstract: OBJECTIVE To investigate the chemical constituents and anticancer activity of EtOAc extract fraction from Rubia cordifolia L.METHODS Silica gel column chromatography and various spectral methods were used to isolate and identify the constituents;MTT assay was used to assess the anticancer activity of the isolated compounds on L1210 tumor cells.RESULTS EtOAc extract fraction was shown anticancer activity and the six compounds were isolated from the fraction and their chemical structure were elucidated as β-sitosterol(Ⅰ)、dihydromollugin(Ⅱ)、mollugin(Ⅲ)、2-carbomethoxy-2,3-epoxy-3-prenyl-1,4-naphthaquinone(Ⅳ)、physcion(Ⅴ)、oleanolic acid(Ⅵ).CONCLUSION Compound Ⅴwas isolated first time from Rubia cordifolia L.and compound Ⅳ shown strong anticancer activity.

Studies on antibacterial mechanism of the volatile oils from Eupatorium adenophorum Spreng on Staphylococcus aureus

Abstract: OBJECTIVE To study antibacterial mechanism of the volatile oils from Eupatorium adenophorum Spreng(EAVO)on Staphylococcus aureus.METHODS Electrical conductivity detection,SDS/PAGE electrophoresis and DAPI staining assay were used to primarily explore the antibacterial mechanism of EAEO against S.aureus.RESULTS After treated with EAVO,electrical conductivity,SDS/PAGE and DAPI staining of S.aureus obviously changed.CONCLUSION The antibacterial mechanism of EAEO may involve in affecting cell membrane integrity,soluble protein and nucleic acid synthesis of S.aureus.

Effect and mechanism of action of hydroxysafflor yellow A on myocardial ischemia-reperfusion injury in rats

Abstract: OBJECTIVE To explore whether hydroxysafflor yellow A(HSYA) has protective effects on myocardial ischemia-reperfusion(I/R) in simulating ischemic preconditioning(IPC) and implore its probable mechanism of action.METHODS Based on the model of myocardial I/R and ischemic preconditioning in rats,CK,CGRP and 6-kete-PGF1α in the blood were determined.The myocardial infarction size(MIS) was observed by nitroblue tetrazoluim(NBT) staining.RESULTS In the IPC and HSYA therapy groups,the ratios of the infarct size area were significantly lower than that in I/R group(41.67±9.79)%,which was(15.36±2.21)%,(11.97±3.32)%,(16.57±2.36)% and(22.01±3.45)% respectively,P0.05.Compared to I/R group,the levels of CGRP and 6-kete-PGF1α in IPC and therapy groups were increased,and the levels of CK were decreased obviously.CONCLUSION HSYA could mimic the effects of the ischemic preconditioning on myocardial ischemia-reperfusion injury in rats.

Bioequivalence study of lornoxicam tablets in healthy volunteers by LC-MS/MS method

Abstract: OBJECTIVE To develop an LC-MS/MS method for the determination of lornoxicam in human plasma to evaluate the bioequivalence of lornoxicam in healthy volunteers.METHODS A single oral dose of 8 mg reference and test tablets were given to 20 healthy male volunteers according to a randomized crossover design.Plasma concentrations were determined by LC-MS/MS after deproteinized by methanol.The pharmacokinetic parameters were calculated by DAS 2.0.RESULTS The main pharmacokinetic parameters of lornoxicam in test and reference preparations were as follows:Cmax were(782.0±275.1) μg·L-1 and(823.4±256.1) μg·L-1,tmax were(2.8±1.4) h and(2.6±1.4) h,t1/2 were(3.5±1.2) and(3.3±0.8) h,AUC0-24 h were(4 545±1 714) and(4 516±2 054) μg·h·L-1,respectively.The relative bioavailability of lornoxicam was(103.8±15.0) %.CONCLUSION The method was proved to be accurate,sensitive and convenient;lornoxicam in the test tablets was bioequivalent to the reference tablets.

Determination of total cholic acid in bear bile powder,porcine gall powder,ox bile powder and chicken bile powder and study on the bacteriostatic action of these bile powder

Abstract: OBJECTIVE To develop a method for determining the total cholic acid content in the bear bile powder,the porcine gall powder,the ox bile powder and the chicken bile powder,and to evaluate bacteriostatic action of these bile powder.METHODS Sulfuric acid-water(50∶50) solution was added in each bile powder sample,heated and displayed color in water bath for 18 min at 75 ℃,using cholic acid and ursodesoxycholic acid as reference substance,the total cholic content in each kind of bile powder was determined at wavelength 388 nm,at the same tine,using Staphylococcus aureus and Escherichia coli as experimental bacteria,by determining the OD value at wavelength 650 nm,the bacteriostatic action in vitro of each one was investigated.RESULTS The linear range of cholic acid was 5.7-34.3 μg·mL-1,the linear equations was Y=41.573X-0.166 1,r=0.999 5.The linear range of ursodeoxycholic acid was 4.7-23.5 μg·mL-1,the linear equations was Y=24.957X-0.067 9,r=0.999 6,the recovery of cholic acid in the bear bile powder,the ox bile powder,the porcine gall powder and the chicken bile powder was 98.9%,97.7%,104.1% and 102.9% respectively,RSD was 1.59%,1.08%,2.00%and 1.22% respectively,and the recovery of ursodeoxycholic acid in the bear bile powder,the ox bile powder,the porcine gall powder and the chicken bile powder was 100.5%,98.8%,99.4% and 103.6% respectively,RSD was 1.07%,1.12%,1.67% and 1.78% respectively.All the four kinds of bile powders had obvious bacteriostatic actions on Staphylococcus aureus and Escherichia coli,but but the difference was not significant.CONCLUSION The method is simple,accurate,reproducibility,and suitable for the determination of total cholic acid content in the bear bile powder and other bile powder,each of them has significant inhibitory effect on Staphylococcus aureus and Escherichia coli.

HPLC-UV method for the determination of metoprolol in rabbit plasma and its application in pharmacokinetic study

Abstract: OBJECTIVE A high performance liquid chromatography-ultraviolet(HPLC-UV) method was developed and validated for determining the concentration of metoprolol in rabbit plasma.The pharmacokinetic study in rabbits was investigated.METHODS The HPLC-UV method was developed by using Phenomenex C18 column(250 mm×4.6 mm,5 μm) for separation with phenytoin sodium as internal standard.The mobile phase was methanol-water(60∶40),and the water phase consisted of 385 mL water,1.6 mL triethylamine and 0.5 mL phosphoric acid.The UV detection wavelength was 223 nm.DAS 3.0.1 pharmacokinetics software was used to calculate the pharmacokinetic parameters.RESULTS The linear range of metoprolol was 0.078-7.81 μg·mL-1,the limit of quantification was 0.078 μg·mL-1.Both the intra-and inter-day precisions were less than 10%.At low,medium and high quality control concentrations,the extraction recovery was in the range of 87.5%-92.3% and the accuracy ranged in 95.4%-108.6% respectively.The method was applied for the pharmacokinetics study of metoprolol tartrate tablets by oral administration.The AUC0-t,tmax and Cmax were respectively(338.8±30.9) mg·L-1·min,(45.0±0.0) min and(2.2±0.3)μg·mL-1 respectively.CONCLUSION The HPLC-UV method developed in this work is accurate,rapid and convenient.It provided a simple and easily available analytical method for the pharmacokinetics study of metoprolol.

The myocardial protection of nicorandil plus atorvastatin treatment during percutaneous coronary intervention(PCI)

Abstract: OBJECTIVE To evaluate the myocardial protection of nicorandil plus atorvastatin treatment during percutaneous coronary intervention(PCI)METHODS A total of eighty-five patients undergoing selected PCI were randomly divided into the observation group(n=43) and control group(n=42)The observation group received oral nicorandil(10 mg,tid) combined with atorvastatin(20 mg,qd) for(5±2) days before coronary angiography treatment,the control group was given routine drug therapyThe daily routine dosage was continued for 4 weeks after the procedureFor each patient,the angina pectoris attacks,CK-MB,electrocardiogram and echocardiogram were recordedRESULTS Angina did not occur in observation group during the procedure but occurred in 10 patients in the control group(P001)The changes of ST-segment and T wave during balloon dilatation in PCI procedure were less in the observation group(P005)The CK-MB activity was significantly lower in the observation group compared with the control group in different observing time-point,respectively(P005)Ejection fraction in the observation group was higher than that in the control group after operation 4 weeks [(664±53)% vs(629±82)%,P005]CONCLUSION Nicorandil plus atorvastatin treatment could reduce the frequency of angina pectoris attacks and myocardial damage during PCI,and improve the left ventricular function during follow-up period after PCI

Preparation and drug release in vitro of sustained-release pellet tablets of aspirin

Abstract: OBJECTIVE To prepare aspirin sustained-release pellet tablets.METHODS Using extrusion-spheronization equipment to prepare aspirin pellets,aspirin pellets were coated with Surelease and Acryl-EZE(5∶5) as coating material.The release mechanism of the drug from the pellet tablets was studied.RESULTS The data obtained proved that the formulation was useful for a sustained-release aspirin due to the percentage of 30% at the first two hours,and the less were released in the later 10 hours.Weibull curve fitting equations showed the pellet tablets release met level 1 rate process.CONCLUSION The method and the formulation are successful in providing slow and steady release of aspirin from sustained-release pellet tablets.

Study on the effects of Ginkgo biloba extract on the antioxidation ability and the serum TNF-α contents in adjuvant arthritis rats

Abstract: OBJECTIVE To investigate the antioxidation ability of Ginkgo biloba extract(EGb761) on adjuvant arthritis(AA) in rats and to probe into its underlying mechanism.METHODS The AA was induced by Freund's complete adjuvant(FCA) in male SD rats.Rats were intragastrically administered different doses of EGb761(50,100,and 200 mg·kg-1) on the 12th day after injection of FCA,the drugs were given for 16 days.Tripterygium wilfordii ployglycosidium(TPT) at 40 mg·kg-1 was used as a positive control drug.Rats were killed after FCA was injected on the 28th days.The activities of myeloperoxidase(MPO),superoxide dismutase(SOD),inducible nitric oxide synthase(iNOS),and the contents of malonyldialdehyde(MDA) and nitric oxide(NO) in serum were detected by biochemistry methods.The contents of TNF-α in serum were measured by enzyme-linked immunosorbent assay methods.RESULTS The secondary inflammation of AA rats appeared on the 12th day after injection of FCA.At the same time(d 12),different doses EGb761 were given to AA rats.It was found that EGb761 could significantly inhibit the secondary paw swelling of AA rats from the 20th day.Compared with the model group,the activities of MPO and iNOS and the contents of MDA,NO and TNF-α in serum were significantly decreased(P0.05 or P0.01);the activities of SOD in serum were increased(P0.05 or P0.01).CONCLUSION EGb761 can alleviate the inflammatory reactions in AA through inhibiting oxygen free reaction,exerting antioxidation effects and decreasing the production of TNF-α.

The protective effect of dioscin-containing serum on hydrogen peroxide injured cardiomyocytes of neonate rats

Abstract: OBJECTIVE To study the effects and mechanism of dioscin on hydrogen peroxide(H2O2) injured cardiomyocytes with a serum pharmacological method.METHODS Prepared the serum containing dioscin(600 mg·kg-1) with serum pharmacological method.Cardiomyocytes derived from neonatal rats were cultured in Dulbecco Modified Eagle Medium(DMEM).The cardiomyocytes were injured with hydrogen peroxide(H2O2),and treated with the serum containing different concerntrations of dioscin.The survival rates of cardiomyocytes were measured with MTT method.The contents of malondialdehyde(MDA) and lactate dehydrogenase(LDH),and the activities of total superoxide dismutase(T-SOD) and catalase(CAT) were measured.RESULTS The survival rates of cardiomyocytes injured with H2O2 for 2 h were decreased significantly compared with normal cells(P0.01).The content of MDA and LDH were increased significantly,but the activity of T-SOD and CAT were decreased.After treated with the different concentrations of drug-containing serum,the survival rates were increased with a dose-dependant manner(P0.01).The contents of MDA and LDH were decreased and the activities of SOD and CAT were significantly increased(P0.01).CONCLUSION Dioscin can protect the H2O2 injured cardiomyocytes by increasing antioxidation capability.

Study on the type I allergic reaction of safflower injection

Abstract: OBJECTIVE To study the allergic reaction of safflower injection with active systemic anaphylaxis test and passive cutaneous anaphylaxis test.METHODS Guinea pigs were injected respectively with safflower injection(5 mL·kg-1),sodium chloride injection(5 mL·kg-1) or bovine serum albumin saline injection [5 mL(40 mg)·kg-1],once every other day,continuously for three times.Each group was performed by injecting a single intravenous injection of double dosages of test substance,after 14 d from the end time of sensitization,to observe whether allergic reactions occurred within 30 min;SD rats were received 0.1 mL of antiserum injection for inducing passive sensitization,after 48 hours,respectively injected with safflower injection(5 mL·kg-1),sodium chloride injection(5 mL·kg-1) or bovine serum albumin saline injection [5 mL(40 mg)·kg-1] and 1 mL of 1% Evans blue for performing.After 30 min the rats were sacrificed,and the diameter of blue spots on the dorsal skin were observed.RESULTS There was no any abnormal reaction during sensitization in the safflower injection group.Adverse reactions had been found in one batch of safflower injection group,but death was not observed.Blue spots were found on the SD rats' dorsal skin of the groups of safflower injection and bovine scrum albumin.CONCLUSION The test of active systemic anaphylaxis and passive cutaneous anaphylaxis of safflower injection were proved positive reactions.Safflower injection could increase the sensitization to allergic reaction.

Effect of Ciwujia injection on the activity of CYP3A in rats

Abstract: OBJECTIVE To investigate the effect of Ciwujia injection on the activity of CYP3A in rats.METHODS Liver microsomes of rats were prepared and incubated with Ciwujia injection at the presence of midazolam.Metabolic rate of midazolam was determined by HPLC to determine the effect of Ciwujia injection on the activity of CYP3A.20 rats were divided into control group and experiment group randomly.The control group was given sodium chloride and the experimental group was intravenously given Ciwujia injection for 7 d.The rats were killed after the last treatment by decapitation and livers microsomes protein was prepared,then the CYP3A activities was measured by incubation reactions.RESULTS Ciwujia injection was a potential CYP3A inhibitor in vitro,the IC50 was 5.00 mL/100 mL.CONCLUSION The activities of CYP3A were inhibited obviously by administration of Ciwujia injection,It decreased the metabolism of midazolam by 21.11%.

System evaluation of the efficacy of pantoprazole in treating duodenal ulcer patients

Abstract: OBJECTIVE To evaluate the efficacy and safety of pantoprazole in treating duodenal ulcer patients.METHODS Searching published article,both at home and abroad,about pantoprazol in treating duodenal ulcer through literature and Internet queries.The forest plot with Meta analysis was drawn by RevMan 5.0.RESULTS According to the criterion 21 literatures were selected.Meta analysis showed: 2 weeks healing rate of pantoprazole and ranitidine in treating duodenal ulcer OR=3.11,95% CI =(2.46,3.94),(P0.05);4 weeks healing rate OR=5.72,95% CI =(4.16,7.85),(P0.05);4 weeks healing rate of pantoprazole and famotidine in treating duodenal ulcer:OR=4.70,95% CI=(1.96,11.28),(P0.05);4 weeks healing rate of pantoprazole and cimetidine in treating duodenal ulcer:OR=3.80,95% CI=(1.89,7.65),(P0.05).There were no significant differences in the incidence of adverse reactions.CONCLUSION Compared with ranitidine,famotidine and cimetidine,pantoprazole has advantages of instant effect,easing symptoms quickly,and high rate of ulcer healing over famotidine.So pantoprazole is the better choice for the treatment of duodenal ulcer patients.

Preparation and properties of mPEG-PLGA nanoparticles and evaluation of their in vitro anti-adhesive ability

Abstract: OBJECTIVE To prepare mPEG-PLGA nanoparticles and discuss its physicochemical characterization and anti-adhesive ability.METHODS mPEG-PLGA-NP was prepared by self-emulsion solvent diffusion technique with different amount of mPEG-PLGA as the carrier.The preparation conditions were optimized by means of monofactorial design.Drug-loaded properties of mPEG-PLGA-NP were studied with furanodiene.The in vitro anti-adhesive activity of nanoparticles was evaluated by pig gastric mucin(PM) binding experiments.RESULTS The optimized preparation conditions were obtained as follows: organic solvents was acetone,0.2% Tween-80 was emulsifiers,the amount of mPEG-PLGA was 25 mg,the volume ratio of organic and aqueous phase was 1:15.Particle size and the absolute value of Zeta potential of mPEG-PLGA-NP decreased gradually with the increase of mPEG content.Encapsulation efficiency of mPEG-PLGA-NP was about 50%,drug-loading of mPEG-PLGA-NP was about 10%.PM binding experiments showed that,the anti-adhesive activity of mPEG-PLGA-NP was six times higher than PLGA-NP,and it was increased gradually with the increase of mPEG molecular and content.CONCLUSION This study successfully prepared mPEG-PLGA-NP and characterized its properties.mPEG-PLGA-NP has good drug loading and anti-adhesive activity.

Study on the effects of Yuanhuzhitong formula on pain-related substances in formalin-induced pain model and dysmenorrhea rats

Abstract: OBJECTIVE To investigate the effects of Yuanhuzhitong formula on prostaglandins,β-endorphin and monoamine transmitter of pain models of rats.METHODS Using tool drugs to measure analgesic effect of Yuanhuzhitong formula and detect the content of prostaglandins,β-endorphin and monoamine transmitter in formalin-induced pain model and dysmenorrhea rats.RESULTS Yuanhuzhitong formula had apparent analgesic effect in the experimental models;at the same time,the formula could reduce the content of PGF2α and the ratios of PGF2αand PGE2(P0.05)in the dysmenorrhea rats.In the formalin-induced pain model,the formula could reduce the content of β-endorphin and 5-HT,while there was no effect on the other monoamine transmitters.CONCLUSION Yuanhuzhitong formula alleviates pain through regulating the content of prostaglandins,β-endorphin and monoamine transmitter of pain models of rats.

Effects of ambroxol on lung concentrations of vancomycin in patients with lung MRSA infection

Abstract: OBJECTIVE To study the impact of ambroxol on the concentration of vancomycin of sputum in patients with pulmonary MRSA infection and evaluate the rationality of the combined administration of the two drugsMETHODS 44 cases of MRSA infection in the lung were randomly divided into two groups of A and BGroup A were treated with vancomycin of 10 g ivgtt q12h,and Group B were treated with vancomycin of 10g ivgtt q12h and ambroxol of 60mg ivgtt q12hSputum samples were collected by cough or the negative pressure suction,meanwhile serum samples were collected before the fourth dose of vancomycinVancomycin concentration was determined by fluorescence polarization immunoassay(FPIA)RESULTS The vancomycin sputum concentration of Group A and B were 180±209 μg·mL-1,357±313 μg·mL-1(P005),respectivelyThe vancomycin plasma concentration of Group A and B were 1567±251 μg·mL-1,1468±279 μg·mL-1,(P005),respectivelyCONCLUSION The combined use with ambroxol may remarkably increase the concentration of vancomycin in sputum in patients with pulmonary MRSA infection,but there were no significant difference for concentration of vancomycin in plasma between the two groups

Analysis of the monosaccharide composition of Tricholoma matsutake polysaccharides by HPLC

Abstract: OBJECTIVE To analyze the monosaccharide composition of the Tricholoma matsutake polysaccharides(MTS) and their molar ratioMETHODS The polysaccharide were hydrolyzed into monosaccharides with 2 mol·L-1 trifluoroacetic acidThe monosaccharide derivatives obtained with 1-phenyl-3-methyl-5-pyrazolone(PMP) were separated by reverse-phase HPLC using gradient elution process,and monitored by ultraviolet detector at 250 nmRESULTS The results showed that MTS compose of D-glucose,D-galactose,D-arabinose,D-xylose and their molar ratio was about 1892∶268∶163∶1The peak area of each monosaccharide had a good linear relationship with its concentration(r0998)The average recoveries of glucose,galactose,arabinose and xylose were 940%,885%,939%,959%,respectivelyCONCLUSION This method was simple,accurate and had good reproducibility and could be used to determine the monosaccharide composition of Tricholoma matsutake polysaccharides

Effects of ABCB1polymorphisms on plasma carbamazepine concentration

Abstract: OBJECTIVE To investigate the effects of ABCB1 polymorphisms on plasma carbamazepine(CBZ) concentrations.METHODS The plasma carbamazepine concentrations were determined by FPIA in 275 epileptic patients.C1236T,G2677T/A and C3435T polymorphisms of ABCB1 were genotyped by polymerase chain reaction amplification followed by restriction fragment length polymorphism analysis or by gene sequencing.CBZ concentrations of every genotype were compared using one-way ANOVA.RESULTS In G2677T/A,the adjusted CBZ concentrations of the patients with TT genotype were higher than those with GG genotype(P=0.001).However,no significant difference was observed between the polymorphisms of C1236T and C3435T and the adjusted CBZ concentrations(P0.05).CONCLUSION G2677T/A polymorphism of ABCB1 is associated with different plasma CBZ levels in patients with epilepsy.Our results suggest that the patients with 2677-TT genotype should properly reduce CBZ dose.

The effect of l-menthol on the intranasal absorption to diazepam

Abstract: OBJECTIVE To study the effect of diazepam or combined with l-menthol on the central inhibitory action by intranasal administration.METHODS MES acute seizure model,strychnine seizure threshold test and synergia effect test of diazepam and Barbital drugs in mice were performed to evaluate the effects of l-menthol on Intranasal diazepam's hypnotic and anti-convulsive actions.RESULTS Compared with the control group,intranasal diazepam can inhibit convulsion induced by electrical stimulation or strychnine.And it enhances pentobarbital sleeping effects.The results of intranasal diazepam are similar to the results of gavage administration.In additional,l-menthol can strengthen intranasal diazepam's efficacy a certain extent.CONCLUSION Diazepam via intranasal administration could take sedative-hypnotic action and control the epileptic seizure with a dose-response relationship and the effect was similar to the results of gavage administration.l-menthol could strengthened when combined with l-menthol.