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1.
Neurochem Res ; 43(2): 297-305, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29090409

RESUMO

Oxidative stress and cytotoxic damage induced by amyloid beta (Aß) have been considered pivotal in the pathogenesis of Alzheimer's disease (AD) and may represent a target for treatment. The phosphatidylinositol 3-kinase (PI3K)/Akt pathway elicits a survival signal to protect against multiple injuries, and the transcription factor nuclear factor erythroid 2-related factor 2 (Nrf2), a downstream target of the PI3K/Akt pathway, can bind to HO-1. Resveratrol, a natural polyphenol derived from grapes, has been widely reported to have diverse antioxidative effects against AD, but the mechanisms have not been fully elucidated. The present study aims to investigate the effects of resveratrol on Aß1-42-induced cytotoxicity in PC12 cells and to explore the potential mechanisms of these effects. PC12 cells were cultured and treated with Aß1-42. Oxidative stress was assessed by measuring malondialdehyde (MDA), glutathione (GSH), and superoxide dismutase (SOD) levels. After treating with resveratrol at different concentrations (0, 10, 20, 40 µM) and for different durations (24, 48, 72 h), the generation of MDA, GSH, and SOD were detected; cell viability was assessed by MTT assay. The production of reactive oxygen species (ROS) was determined using an ROS Assay Kit. Western blotting was used to detect the protein expression. Our studies showed that pretreatment with resveratrol could reduce Aß1-42-induced oxidative stress in PC12 cells by inhibiting the generation of MDA and ROS and increasing the production of SOD and GSH. Resveratrol markedly attenuated the Aß1-42-induced loss in cell viability in PC12 cells in both a dose- and time-dependent manner. More importantly, resveratrol stimulated the activation of HO-1, Nrf2, PI3K, and phosphorylated Akt. Notably, the neuroprotective effects of resveratrol were eliminated by the HO-1 inhibitor zinc protoporphyrin IX (ZnPP), Nrf2 small interfering RNA (siRNA), and the PI3K/Akt inhibitor LY294002. Taken together, the findings suggest that the cytoprotection of resveratrol against the cytotoxicity induced by Aß1-42 in PC12 cells is through the upregulation of HO-1 expression via the activation of the PI3K/AKT/Nrf2 intracellular signaling pathway, which might provide novel insights for understanding the mechanism of the neuroprotective effect of resveratrol as an anti-AD drug.


Assuntos
Peptídeos beta-Amiloides/metabolismo , Heme Oxigenase-1/efeitos dos fármacos , Fator 2 Relacionado a NF-E2/metabolismo , Estilbenos/farmacologia , Animais , Antioxidantes/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Heme Oxigenase-1/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Células PC12 , Fosfatidilinositol 3-Quinase/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos , Espécies Reativas de Oxigênio/metabolismo , Resveratrol , Transdução de Sinais/efeitos dos fármacos
2.
China Pharmacy ; (12): 916-918, 2017.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-510174

RESUMO

OBJECTIVE:To study the pharmacokinetic characteristics of Recombinant hirudin enteric-coated capsule by single and multiple administration in Beagle dogs. METHODS:12 Beagle dogs were divided into single ig group and single iv group by random control method,6 in each group. Recombinant hirudin 0.2 mg/kg was intragastrically administrated or intravenously inject-ed,blood sample was collected;after 2 weeks of cleaning,12 dogs were intragastrically administrated recombinant hirudin 0.2 mg/kg,for 7 d. Sample blood was collected,referred to multiple ig group. Recombinant hirudin concentration in plasma was deter-mined by enzyme-linked immunosorbent assay,and pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS:The results showed that pharmacokinetics by ig and iv recombinant hirudin in Beagle dogs fitted to two-compartment model,abso-lute bioavailability of ig Recombinant hirudin enteric-coated capsule was(14.908±1.868)%;the pharmacokinetic parameters in sin-gle ig group and multiple ig group were tpeak of(2.105±0.243),(3.000±0.000)h,t1/2β of(8.660±2.965),(14.870±2.710)h, cmax of(10.700±0.872),(12.05±1.587)ng/mL,AUC0-1440 min of(55.250±4.386),(58.978±6.002)ng·h/mL,without statistical significances in two groups(P>0.05). CONCLUSIONS:The ig Recombinant hirudin enteric-coated capsule can be absorbed into the blood to a certain extent. There is no accumulation for ig Recombinant hirudin enteric-coated capsule for several days,and it dose not change the pharmacokinetic characteristics.

3.
China Pharmacy ; (12): 3522-3524, 2017.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-611013

RESUMO

OBJECTIVE:To study the pharmacokinetic characteristics of arotinoid ethyl ester (RO) in Beagle dogs in vivo. METHODS:18 Beagle dogs were randomly divided into high-dose,medium-dose,low-dose groups (40,20,10 mg/kg),6 in each group. Rats were intragastrically administrated related doses of RO. Blood sample 1 mL was taken after 0.5,1.0,2.0,4.0, 6.0,8.0,12.0,24.0,36.0,48.0,60.0,72.0 h of administration,and plasma was separated. RP-HPLC was used to determine the concentrations of RO and its metabolite arotinoid acetic acid(RA)in plasma. Using DAS 2.0 software for fitting,pharmacokinetic parameters were calculated. RESULTS:Both RO and RA showed a distribution in one-compartment model in dogs in vivo. The cmax of RO high-dose,medium-dose,low-dose groups in dogs in vivo were (0.42 ± 0.87),(0.54 ± 0.09),(0.31 ± 0.05)μg/mL;t1/2z were(1.20±0.33),(1.14±0.45),(1.90±0.65)h;AUC0-72 h were(3.55±0.90),(0.87±0.50),(0.92±0.31)μg·h/mL;and CL/F were(11.99±4.01),(19.87±10.79),(12.29±7.57)L/(kg·h). The cmax of RA high-dose,medium-dose,low-dose groups in dogs in vivo were (32.51 ± 4.04),(19.87 ± 2.78),(16.55 ± 4.06)μg/mL;t1/2z were (7.27 ± 4.20),(7.17 ± 4.20),(10.18 ± 4.01) h;AUC0-72 h were (408.14 ± 96.61),(333.39 ± 61.28),(286.55 ± 30.96)μg·h/mL;and CL/F were (1.30 ± 0.53)、(0.76 ± 0.87)、(0.54±0.10)L/(kg·h). CONCLUSIONS:Orally taking RO is easy to absorb with rapid elimination. Its active metabolite RA has longer accumulation time in vivo.

4.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-480781

RESUMO

Objective To investigate the diagnosis and treatment of autoimmune pancreatitis (AIP).Methods The clinical data of 25 patients with AIP who were admitted to the Cancer Hospital of Tianjin Medical University between January 2009 and December 2013 were retrospectively analyzed.Patients received the test of serum γ-globulin and IgG4 and abdominal imaging examination.The revised HISORt or results of postoperative pathological examination were performed as diagnostic criteria.Patients who were unable to tolerate surgery were treated by oral prednisone.The focal masses were apparent in the pancreas by imaging examination,which cannot exclude the possibility of malignancy because of ambiguous pathologic characters of masses.Patients who received ineffective hormonal therapy and were able to tolerate surgery underwent surgery.All the patients were followed up by outpatient examination and telephone interview up to December 2014.Results Primary symptoms:jaundice was detected in 16 patients,obvious weight loss (weight loss > 10% standard body mass) in 4 patients,chronic diarrhea (duration of diarrhea > 2 months or 2 weeks < duration of intermittent diarrhea < 4 weeks) in 3 patients and abdominal pain in 2 patients.Abnormal level of serum γ-globulin and increasing level of IgG4 were detected in 13 and 1 pateints.The results of imaging examinations showed that pancreatic masses,stenosis of bile duct and extrapancreactic organ involvement were detected in 19,6 and 11 patients.Of 25 patients with AIP,10 underwent conservative treatment without adverse reaction and 15 underwent surgical treatment,including 13 of 15 patients undergoing pancreaticoduodenectomy and 2 of 15 patients undergoing resection of the body and tail of the pancreas + splenectomy.The operation time,volume of intraoperative blood loss and postoperative recovery time of gastrointestinal function in 15 patients undergoing surgery were (271 ±59) minutes,(268 ± 109) mL and (3.8 ± 1.2)days.After operation,2 patients were complicated with abdominal infection and had remission of symptoms by symptomatic treatment,including 1 with pancreatic fistula and 1 with delayed gastric emptying.The duration of hospital stay of 15 patients undergoing surgery was (11.5 ± 2.9)days.The results of postoperative pathological examination showed that there were central acinar atrophy,extensive fibrosis,lymphoplasmacytic cell infiltration,nerve tissue surrounded by the plasma cell lymphoma and obstructive phlebitis.The absolute value of positive cells of IgG4 was more than 50 high power field and number of positive cells of IgG4 was more than positive cells of 40% IgG.Twenty-five patients were followed up for a median time of 27 months (range,6-47months).Nineteen patients had remission of symptoms at month 6 after treatment with normal level of serum γ-globulin and IgG4 and without recurrence of pancreatic masses,including 7 receiving conservative treatment and 12 receiving surgical treatment.Conclusions The clinical signs of AIP are jaundice,abnormal serum γglobulin and pancreatic masses which are found by imaging examination.Surgery is safe and effective for the treatment of AIP,while surgical indications should be strictly followed because of the surgical trauma.

5.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-459815

RESUMO

Objective:To discusse the clinical features of sarcomatoid hepatocellular carcinoma to improve the understanding of diagnosis and treatment for sarcomatoid hepatocellular carcinoma. Methods:Data including clinical features and follow-up from 8 pa-tients admitted in Tianjin Medical University Cancer Institute and Hospital from January 2009 to April 2014 were retrospectively ana-lyzed. Results: The average age of all patients was 56.6 years old, and the male-to-female ratio was 3:1. Preoperative CT or MRI showed specific characteristics but it was difficult to confirm diagnosis. Pathological and immunohistochemical examination revealed an expressed epithelial-like phenotype. All 8 patients had advanced local tumor invasion and high lymph node metastasis rates. These patients received surgery, and the median survival time was 10.8 months (3 months to 35 months). Conclusion:Diagnosis of sarcoma-toid hepatocellular carcinoma mainly depended on postoperative pathological examination. Immunohistochemistry was beneficial for sarcomatoid hepatocellular carcinoma diagnosis and differential diagnosis. Surgical treatment prolonged survival time, but the overall prognosis remained poor.

6.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-442715

RESUMO

Objective To analyze the clinicopathological characteristics,diagnosis,treatment outcomes and prognosis of patients with pancreatic neuroendocrine tumors (PanNETs).Methods The clinicopathological characteristcs and prognostic factors of 88 patients who were diagnosed with pancreatic neuroendocrine tumors by postoperative pathology were analyzed retrospectively.The data included age,sex,symptoms,tumor size,pathological grades,TNM staging,treatment and follow up.Results There were 28 males and 60 females.The ratio of male to female was 1 ∶ 2.1,with a mean age of 42 (range 8~75) years.Of the 88 PanNETs,74(84.1%) were nonfunctional tumors.Using the WHO 2000 pathological classification system,there were 35 well differentiated endocrine tumors (WDET),29 well differentiated endocrine carcinomas (WDEC),and 24 poorly differentiated endocrine carcinomas (PDEC).Using the 7th AJCC TNM staging system,23(26.1%),46(52.3%),13(14.8%) and 6 patients (6.8%) were diagnosed to have stage Ⅰ,Ⅱ,Ⅲ and Ⅳ,respectively.The overall 5-year survival rate was 72.0 %.Univariable analysis revealed tumor size,histopathological grades,TNM staging and radical surgery were associated with prognosis.Multivariate analysis showed histopathological grades,TNM staging and radical surgery were independent risk factors of survival.Conclusions PanNETs are rare pancreatic neoplasms with high heterogeneity and low malignant potential.PanNETs have various clinical manifestations and the preoperative misdiagnosis rate is high.A definitive diagnosis depends on pathological examination.The new TNM and pathological classification systems have good predictive abilities on survival.The majority of patients who received radical surgery or surgical comprehensive therapy have good prognosis.

7.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-622328

RESUMO

AIM: To investigate correlation between the expression of survivin and caspase-3 proteins in juvenile laryngeal papilloma. METHODS: The expression of survivin and caspase-3 proteins were detected with immunohistochemial method in 43 cases of juvenile laryngeal papilloma, 25 vocal nodules and 25 normal laryngeal mucosa. RESULTS: The positive rates of survivin protein in juvenile laryngeal papilloma were 57.14% and higher than that in voeal nodules (P<0.01)and the normal laryngeal moeusa (P<0.01). And the Caspase-3 protein positive rate was 26.19% in juvenile laryngeal papilloma and lower than that in voeal nodules and the normal laryngeal mucosa (P<0.01).There was a significant negative correlation between the expression of survivin and caspase-3 in juvenile laryngeal papilloma. CONCLUSION: The abnormal expression of survivin and caspase-3 may play important role in the pathogenesis of juvenile laryngeal papilloma.

8.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-265399

RESUMO

<p><b>OBJECTIVE</b>To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs.</p><p><b>METHOD</b>Applying to double cycle self crossover design, a single oral or intravenous dose of 10 mg x kg(-1) sinomenine was given to 10 beagle dogs. Drug concentrations in plasma were determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program.</p><p><b>RESULT</b>The concentration-time curves of oral administration fitted to one compartment model in the beagle dogs. The T(max), C(max), t1/2 and AUC(0-T) was (82.5 +/- 13.9) min, (0.15 +/- 0.027) mg x L(-1), (87.6 +/- 28.3) min and (28.43 +/- 3.48) mg x min x L(-1), respectively. The concentration -time curves of i.v. fitted to two compartment model in the beagle dogs. The t1/2beta and AUC(0-T) was (106.7 +/- 120.2) min and (93.32 +/- 82.08) mg x min x L(-1). The absolute bioavailability for oral use was (30.46 +/- 4.24)%.</p><p><b>CONCLUSION</b>The absolute bioavailability of sinomenine is low, and the elimination of sinomenine tablet is fast.</p>


Assuntos
Animais , Cães , Feminino , Masculino , Disponibilidade Biológica , Medicamentos de Ervas Chinesas , Farmacocinética , Injeções Intravenosas , Morfinanos , Farmacocinética , Distribuição Tecidual
9.
China Pharmacy ; (12)2007.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-533038

RESUMO

OBJECTIVE:To explore the effect of Xiaoyu anshen capsule on the space learning-memory ability of chronic stress-induced depressed model rats.METHODS:The enrolled rats were divided into 6 groups:blank control group,model group,Fluoxetine group,Xiaoyu anshen capsule groups(high,medium and low dose).Chronic depression rat model was induced by chronic stress and isolated breeding.Water-maze video tracking analysis system was used to detect the capacity of rats' space learning-memory,and the indexes such as the body weight of rats before and after modeling and the consumption of sucrose,etc.were measured.RESUTLS:Compared with the blank control group,the model control group showed significantly decreased space learning-memory capacity,significantly lower in body weight increase and significantly less sucrose solution consumption.Compared with the model control group,the high,medium and low dose Xiaoyu anshen capsule-treated group showed significantly shortened escape latency,the high and medium dose groups showed increased number of times of crossing the hidden platform and body weight increase,and in high dose Xiaoyu anshen capsale group sucrose consumption increased.CONCLUSION:Xiaoyu anshen capsule is a nootropic Chinese herbal medicine for its inhibitory effect on the abnormality in body weight and sucrose solution consumption of chronic stress-induced depressed model rats and their action in enhancing the space learning-memory ability.

10.
China Pharmacy ; (12)2007.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-531265

RESUMO

OBJECTIVE:To study the pharmacokinetics of tramadol hydrochloride paracetamol tablets in healthy volunteers.METHODS:10 healthy volunteers were assigned to receive oral single dose of tramadol hydrochloride paracetamol tablets.Plasma concentrations of tramadol hydrochloride and paracetamol were measured by HPLC and the pharmacokinetic parameters were computed by 3p97 software.RESULTS:The concentration-time curves of tramadol hydrochloride and paracetamol all fitted one compartment open model.The pharmacokinetic parameters of tramadol hydrochloride and paracetamol were as follows:t1/2Ka were(0.23?0.16)h and(0.64?0.60)h,t1/2ke were(2.12?0.78)h and(5.48?2.90)h,tmax were(0.90?0.43)h and(1.88?1.12)h,Cmax were(9.37?2.56)?g?mL-1 and(115.27?98.88)ng?mL-1,CL/F(s) were(24.52?7.12)L?h-1 and(0.15?0.08)L?h-1,AUC0~t were(30.38?7.47)?g?h?mL-1 and(598.36?232.14)ng?h?mL-1,AUC0~∞ were(33.02?9.15)?g?h?mL-1 and(800.12?420.92)ng?h?mL-1,MRT0~t were(3.75?1.41)h and(5.46?1.64)h,MRT0~∞ were(5.24?2.92)h and(9.86?6.00)h,respectively.CONCLUSION:This study provided a basis for clinical application of tramadol hydrochloride paracetamol tablets.

11.
China Pharmacy ; (12)2007.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-529553

RESUMO

OBJECTIVE:To explore the anti-inflammatory effect of Musk eye drops on acute ceratitis.METHODS:The model of acute ceratitis resulting from surgical injury was established in rabbits and which were randomly assigned to Musk eye drops groups(0.3%,0.15%,and 0.05%),0.5% Cortisone acetete eye drops group and 0.9% Normal Saline group(control).The corneal epithelium growth at 24,48h,and 72h was observed by fluorescein(2%)staining,levels of protein,Ca2+,IL-1? in the aqueous humor were determined,corneas were weighted and corneas tissues were sampled for histopathologic examination.The anti-inflammatory effect of Musk eye drops on acute ceratitis resulting from surgical injury was discussed.RESULTS:Corneal bedewing was mitigated,transmigration of neutrophilic leukocytes were inhibited,levels of protein and IL-1? in the aqueous humor were decreased,level of Ca2+ in the aqueous humor was altered and the corneal epithelium growth was promoted in Musk eye drops groups(0.3%,0.15%,and 0.05%).CONCLUSION:Musk eye drops had remarkable anti-inflammatory effect on acute ceratistis.

12.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-683506

RESUMO

Objective:To study the effect of yemazhui on concentration of levofloxacin in rinse solution of mice tracheae. Methods:50 mice were randomly divided into blank group、anwhlor group、yemazhui large-dose group、yemazhui middle-dose group, yemazhui low-dose group, each group had 10 mice. After administration of liquor natrii chloridi isotonicus (NS) 30 ml/10kg, amchlor1.00g/kg、yemazhui large dose 64.45g (curde drug)/kg、yemazhui middle dose 32.73g (curde drug)/kg, yemazhui low dose16.36g(curde drug)/kg, mice were intraperitoneal injected levofloxaein at dosage of 0.07g/kg 2hours after administration. The concentration of levofloxacin in excretion of mice tracheae was detected by HPLC. Results:Comparion with blank group, concentration of levofloxacin in excretion of mice tracheae of yemazhui large-dose group、yemazhui middle-dose group、yemazhui low-dose group was 4.58 times、3.18 times、1.86 times the amout of that. Conclusion:Yemazhui can enhance concentration of lwvofloxacin in rinse solution of mice tracheae.

13.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-527330

RESUMO

Objective: To explore the protective effect of Shenmai lyophilized preparation (SMP, 参麦冻干剂) on acute myocardial infarction (AMI) in cats. Methods: AMI cat model was induced by ligation of the left coronary artery for 4 hours. Cats were randomly divided into five groups: AMI group (4 ml/kg of normal saline ), large dose SMP group (1.76 g/kg), small dose SMP group (0.88 g/kg), Shenmai injection (参麦注射液) group (0.88 g/kg) and nitroglycerine group (0.44 mg/kg). Drugs were given 5 minutes after the left coronary artery ligation. Mean arterial pressure (MAP) and ventricle cardiac arrhythmia were monitored by multichannel biological signal analytical system. MultiCD*2lead ?ST on chest was recorded by cardiofax after myocardial ischemia for 4 hours, the area of AMI was measured by dyes with triphenyl tetrazolium chloride (TTC). Changes of creatine kinase (CK) and lactate dehydrogenase (LDH) in serum were assayed by colorimetric assay. Results: SMP at the dosage of 0.88 and 1.76 g/kg increased MAP, decreased ?ST and incidence of ventricle cardiac arrhythmia in cats with AMI, shrank the area of AMI and decreased the LDH content and CK activity in serum, respectively compared to the AMI group, the differences being significant in the aboveCD*2mentioned parameters (P

14.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-563402

RESUMO

Objective To investigate the effect of recombinant human keratinocyte growth factor variant(K102) on mechanical corneal injury in rabbits.Methods Mechanical corneal injury was made in 108 rabbits surgically.K102 eye drop was given respectively at dose of 0.5,0.25,0.125 mg/ml,taking Beifushu eye drops and Dexamethasone sodium phosphate eye drops as the positive control,and K102 eye drop solvent as the blank control;4 times per day.Corneal haze was determined with slit lamp microscope and the histopathological changes were observed under light and electron microscope.Results Three months after operation,the corneal haze was less severe and the average number of corneal cells in shallow 50 ?m corneal basement was less than that in Beifushu group and blank group after 0.5 mg/ml K102 treatment.The results of light and electron microscopy showed the epithelial hypertrophy,disorders of cells and collagen arrangement after 0.5 mg/ml K102 treatment were much lighter than that in Beifushu group and blank group.Conclusion Local application of K102 eye drops reduces the number of stromal keratocyte,then effectively inhibits corneal haze at early stage after mechanical corneal injury in rabbits.

15.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-559931

RESUMO

Aim To study the protective effects of sodium magnesium fructose diphosphate (FDPM) on the kidney in hemorrhagic shock rats. Methods The study utilized Wiggers hemorrhagic shock model. Sixty Wistar rats were divided into six groups randomly: normal saline control group,three doses of FDPM group (90.0,45.0,22.5 mg?kg -1 ),1,6-fructose diphosphate group(37.5 mg?kg -1 ) and magnesium sulfate group (3.4 mg?kg -1 ). Mean arterial pressure was monitored before shock, 10, 30 and 60 minuts after drug administration and 0, 30 and 60 minuts after shed blood reinfusion Blood urea nitrogen and creatinine, the content of malondiadehyde, and the activity of Na+-K+-ATPase, Ca 2+ -ATPase, Mg 2+ -ATPase, and superoxide dismutase in kidney were also measured. Results FDPM significantly improved mean arterial blood pressure of hemorrhagic shock rats, reduced blood urea nitrogen and creatinine, decreased the content of malondiadehyde and increased the activity of Na+,K+-ATPase,Ca 2+ -ATPase,Mg 2+ -ATPase and superoxide dismutase in kidney. Conclusion FDPM had protective effects on the ischemia-hypoxia injury of kidney by improving energy metabolism and attenuating tissue injury caused by free radicals in hemorrhagic shock.

16.
China Pharmacy ; (12)2001.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-525126

RESUMO

OBJECTIVE:To study pharmacokinetic parameters of melatonin tablet in beagle dogs.METHODS:A single oral dose of3mg melatonin tablet was given to6beagle dogs,drug concentrations in plasma were determined by HPLC method,the pharmacokinetic parameters were calculated by3P97pharmacokinetic program.RESULTS:The concentration-time curves of melatonin fitted two compartment model in the beagle dogs.The t 1/2Ka 、t 1/2Ke 、t max 、C max 、CL and AUC (0~T) were(0.16?0.10)h、(1.21?0.52)h、(0.50?0.18)h、(11.27?3.77)ng/ml、(0.13?0.04)L/h and(25.23?7.71)(ng?h)/ml re-spectively.CONCLUSION:It is rapid to absorb melatonin and initiate sleep in beagle dogs,but it's hold-time is short.

17.
China Pharmacy ; (12)2001.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-523348

RESUMO

OBJECTIVE:To study the relative bioavailability and pharmacokinetics of salbutamol sulfate orally disinte?grating tablets.METHODS:A single dose of8mg salbutamol sulfate orally disintegrating tablets or commercial salbutamol tablets was administered in a randomized crossover design in18volunteers and the plasma concentrations of salbutamol were determined by HPLC.The pharmacokinetic parameters were calculated with3p97pharmacokinetic program and the bioequiv?alency was evaluated.RESULTS:The concentration-time curve of two preparations fitted to two-compartment model.The peak plasma levels(C max )of salbutamol sulfate orally disintegrating tablet and commercial salbutamol sulfate tablet were(17.65?6.48)ng/ml and(16.60?6.21)ng/ml,respectively.The peak time(T max )were(1.92?1.18)h and(2.03?1.17)h and AUC 0~24 were(127.23?32.41)ng/(h?ml)and(131.42?37.73)ng/(h?ml),respectively.The relative bioavailability of salbu_ tamol sulfate orally disintegrating tablet was(99.32?15.58)%.CONCLUSION:The results of two one-side tests suggests that salbutamol sulfate orally disintegrating tablet is bioequivalent to the commercial salbutamol tablet.

18.
China Pharmacy ; (12)2001.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-519914

RESUMO

OBJECTIVE: To study the bioequivalence of Bei Shi metformin hydrochloride(METBS) and Bo Lai metformin hyddrochloride tablets(METBL) in healthy volunteers.METHODS: A single oral dose of 1 OOOmg METBS and METBL were given to 20 healthy volunteers in an open randomized crossover study.Drug concentrations in serum were determined by HPLC.The pharmacokinetic parameters were calculated and analysed by 3p97 program with a statistic analysis of ANOVA, two-one-side t - test and confidence zone of (la-2a)% .RESULTS: The Tmax, Cmax and AUC(10-24) of METBS tables and METBL tables were (2.42 + 1.03) h and (2.50+1.08) h, (2.22+0.69) ug/ml and (2.1210.47) ug/ml, (16.491 5.70) mg/ (h . L) and (16.98 + 6.38) mg/ (h . L), respectively.There were no significant differences between the two formulations in the Tmax, Cmax and AUC (0-24).CONCLUSION: The mean relative bioavailability of METBS tables was(98.29 + 11.98) % compared with METBL tables.The RESULTS: suggest that two products are bioequivalent.

19.
China Pharmacy ; (12)2001.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-518419

RESUMO

OBJECTIVE:To study the pharmacodynamic effects of Yemazhui METHODS:Experiments were carried out with conventional cough and asthma models of mouse or guineapig and in vitro antibacterial test RESULTS:Intragastric administration of extracts of Yemazhui to mice,in dosages of 45 1g herb/kg,22 6g herb/kg and 11 3g herb/kg,could exert obvious antitussive,expectorant and antiasthmatic effects and the extract could inhibit common pathogenic bacteria CONCLUSI_ON:Extract of Yemazhui has antitussive,antiasthmatic and expectorant actions

20.
China Pharmacy ; (12)2001.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-532037

RESUMO

OBJECTIVE:To explore the protective effect of the extracts from Radix et Rhizoma Rhei and Alisma orientalis against acute kidney injury induced by diethylene glycol (DEG) and its action mechanism. METHODS: The acute kidney injury model of mice was induced by intragastric administration of DEG. Then the model mice were administered intragastrically with the extracts of Radix et Rhizoma Rhei and Alisma orientalis. Serum levels of creatinine(Cr) and blood urea nitrogen (BUN), the activities of superoxide dismutase (SOD) and glutathione peroxidase(GSH-PX) and the content of malonaldehyde(MDA) were determined. RESULTS: After administration of DEG, the mice presents with obvious toxic reactions including the increase of the ratio of kidney to body weight, the increase of serum levels of BUN and Cr, the decrease of the activities of SOD and GSH-PX in kidney tissue, the increase of the content of MDA. However, after treatment with the extracts of Radix et Rhizoma Rhei and Alisma orientalis, the toxic symptoms in mice were attenuated markedly, the ratio of kidney to body weight decreased, serum levels of BUN and Cr decreased significantly, the activities of SOD and GSH-PX in renal tissues increased and the content of MDA decreased. CONCLUSION: The remarkable protective effect of the extracts from Radix et Rhizoma Rhei and Alisma orientalis against DEG-induced acute kidney injury in mice might be related to its actions of improving the activity of antioxidase of kidney while inhibiting lipid peroxidation.

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