Archive

• 01 October 2012 Volume 31 Issue 10

    

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  药物研究
  精神科用药专栏
  药物与临床
  药物制剂与药品质量控制
  用药指南
  药事管理
  

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药物研究
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  药物研究

  Study on Immunoregulation Function of Nucleoside Including Thiazolidin-4-one Ring

  LI Na;CHEN Dongzhi;LI Chunxiao;YANG Miao;ZHOU Lei;HONG Yang;CHEN Hua;MENG Ming

  2012, 31(10): 1253-1256. https://doi.org/10.3870/yydb.2012.10.002

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  Objective To further illustrate the immunostimulating activity of the nucleosides containing thiazolidin4one ring, and evaluate the potential value as a drug. Methods The influence of thiazolidin4one derivates CH1a, CH2a, CH1b or CH2b on the proliferation of spleen lymphocyte treated by mitogens (ConA, LPS) was observed by cytology experiment in vitro.Using mice ELISA kit, the levels of the cytokines, such as interleukin4 (IL-4), IL-2, and interferonγ (IFN-γ) were detected from the supernatant of cell cultures.All test indexes were compared with pidotimod. Results CH1a, CH2a, CH1b or CH2b significantly promoted proliferation of Con Ainduced T cells at certain concentrations, as compared with pidotimod (P＜0.01).CH1b and CH2b significantly enhanced proliferation of LPSinduced splenocytes as compared with pidotimod (P＜0.01).CH1a and CH2a did not significantly increase the proliferation of LPSinduced splenocytes (P＞0.05).As compared with Con A alone or pidotimod, a combination of Con A and CH1a, CH2a, CH1b or CH2b significantly increased the levels of IL-2 and IL-4 secretion (P＜0.01).CH1a, CH2a and pidotimod significantly increased the secretion level of IFN-γ (P＜0.01), while CH1b and CH2b had no effects on IFN-γ secretion. Conclusion The nucleoside containing thiazolidin4one ring (CH1a, CH2a, CH1b and CH2b) have certain activity of immunostimulating in mice and hold a potential as immunomodulators.
  
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  药物研究

  Mechanism of Rosiglitazone on Delaying the Progress of Chronic Kidney Disease

  HE Yong;NING Yong;ZENG Rui;HAN Min;MA Zu-fu;XIONG Yan;HE Jin-seng;YAO Ying

  2012, 31(10): 1257-1261. https://doi.org/10.3870/yydb.2012.10.003

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  Objective To investigate the protective effects of PPARγ antagonist rosiglitazone on kidney and the possible mechanism in 5/6 nephrectomy rats with renal failure. Methods SD male rats, weighting 180-200 g, were randomly divided into shamoperation group, model group and rosiglitazone group.After 12 weeks, the rats were killed with decapitation method, and serum urea nitrogen, creatinine and 24 h urinary protein were detected.Residual kidney tissues were pathologically examined to determine glomerular sclerosis and tubulointerstitial injury.The distribution of PPARγ and nNOS in the kidney tissues was detected by immunohistochemistry.RTPCR and Western Blot were used to detect the mRNA expression of PPARγ and nNOS. Results 24 h urine protein, serum urea nitrogen and creatinine of rats in the model and rosiglitazone groups were significantly higher than those in the shamoperation group (P＜0.01) and osiglitazone group than in model group (P＜0.05);and these indicators were significantly lower in rosiglitazone group than in model group (P＜0.05);The renal glomerular sclerosis and tubulointerstitial damage, glomerular sclerosis index and tubulointerstitial damage index in model group were significantly higher than those in shamoperation group (P＜0.01);and these indexes were significantly lower in rosiglitazone group than in model group (P＜0.05).Immunohistochemistry showed that PPARγ mainly distributed in renal tubular epithelial cells, mesangial cells and infiltrating macrophages of the 5/6 nephrectomy rats.nNOS of cortex was mainly localized in dense patches, and also expressed in inner medullary collecting duct.As compared with the shamoperation group, the protein and mRNA expression of PPARγ and nNOS was significantly decreased in model group (P＜0.05), while the expression levels of PPARγ and nNOS in rosiglitazone group were significantly higher than those in model group (P＜0.05). Conclusion Rosiglitazone can significantly reduce glomerulosclerosis and the degree of renal interstitial fibrosis in the 5/6 nephrectomy rats, and its mechanism may be related to increased gene expression of PPARγ and nNOS.
  
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  药物研究

  Skin Allergy and Irritation Tests of Tinidazole and Spironolactone Cream

  LONG Feng;PENG Xian-dong;TANG Zhi-li;TAN Zheng-huai;XIONG Jing-yue

  2012, 31(10): 1262-1264. https://doi.org/10.3870/yydb.2012.10.004

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  Objective To evaluate the allergy and irritation of tinidazole and spironolactone cream on animals’ skin, and to provide safety evaluation of preclinical application. Methods Tinidazole and spironolactone cream, excipient, or 2, 4-dinitrochlorobenzene was repeatedly used to sensitize guinea pigs’ skin.The guinea pigs’ reaction was observed on the 28th day.The rabbits’ damaged skin and healthy skin were locally treated with tinidazole and spironolactone cream, excipient, or 2, 4-dinitrochlorobenzene, and their symptoms were observed day by day. Results The incidence rates of allergic reaction of excipient, tinidazole and spironolactone cream, and 2, 4-dinitrochlorobenzene were 0, 20.0%, and 100.0%, respectively.The stimulation scores of tinidazole and spironolactone cream and excipient were 0. Conclusion Tinidazole and spironolactone cream has only mild sensitization on guinea pigs’ skin and no irritation on rabbits’ skin, and it is a safe preparation.
  
  
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  药物研究

  Effect of Radix Fici Hirtae on Gastrointestinal Function of Spleen Rat Model

  YANG Min;XIA Quan

  2012, 31(10): 1264-1267. https://doi.org/10.3870/yydb.2012.10.005

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  Objective To investigate the pharmacologic effect of Radix Fici Hirtae on gastrointestinal function of spleen deficiency syndrome rat model. Methods The rats were randomly divided into blank control group ,model control group, Astragalus positive control group, high-does Radix Fici Hirtae aqueous extract, mediumdoes Radix Fici Hirtae aqueous extract, low-does Radix Fici Hirtae aqueous extract.Excluding the blank control group, the other groups were induced by reserpine to copy of spleen deficiency syndrome models.After the drug treatment, the rats body quality and quantity diet changes were observed in the day of 0 and 14, and Elisa was used to detect the expression of β-EP, MTL, GAS In the plasma. Results Compared with model group, Radix Fici Hirtae aqueous extract could significantly improve the body quality and quantity diet;Compared with blank control group, the levels of β-EP,MTL,GAS were significantly lower in the group of spleen deficiency syndrome model(P<0.01);Compared with model control group, the levels of β-EP was significantly higher in high-does and mediumdoes groups(P<0.01 or P<0.05), the levels of MTL was significantly higher in high-does groups(P<0.05), the levels of GAS was significantly higher in high-does and low-does groups(P<0.05). Conclusion Radix Fici Hirtae aqueous extract may effectively improve the spleen deficiency of rats by adjusting the levels of β-EP,MTL and GAS, this mayplay a role on treatment spleen deficiency symptoms by the efficacy of spleennourishing.
  
  
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  药物研究

  Comparison of Polysaccharide Content in Different Species of Bupleurum under Different Growth Conditions in Northwest Area of Hubei Province

  YE Fang;YANG Guang-yi;DU Shi-ming;WANG Gang;SUN Rong-jin

  2012, 31(10): 1268-1270. https://doi.org/10.3870/yydb.2012.10.006

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  Objective To compare the content of polysaccharide in different species of Bupleurum under different growth conditions in Northwest area of Hubei Province. Methods The contents of polysaccharide in Bupleurum was determinated by colorimetric method and detected at 620 nm. Results Polysaccharide content in wild Bupleurum marginatum Wall. ex DC. was higher than that in the planted Bupleurum in Northwest Area of Hubei Province, but lower than that in Bupleurum chinese DC. of Shanxi Province and that in B. falcatum L. of Hubei Nanzhang. Conclusion Polysaccharide content of Bupleurum Radix Bupleurum is different under different growth conditions, but no significant difference between the polysaccharide content in different varieties of Bupleurum Radix.
  
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  药物研究

  Influences of Long Term Administration of Allopurinol Sustained-release Capsules on Blood System of Rats with Hyperuricacidemia

  REN Jie;ZHOU You-cai;YAO Wei-fan;ZHAO Hai-shan;CHEN Qiu-chen;HUANG Bai-lin;WEI Min-jie

  2012, 31(10): 1271-1275. https://doi.org/10.3870/yydb.2012.10.007

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  Objective To study the influences of long term administration of allopurinol sustainedrelease capsules (ASRC) on blood system in rats with hyperuricacidemia. Methods 90 Wistar rats were randomly divided into 6 groups: the normal control, hyperuricacidemia model control, ASRC treatment groups (27, 54 mg.kg^-1.d^-1), allopurinol tablet treatment groups (32, 64 mg.kg^-1.d^-1).There were 10 rats in the normal control group and 16 rats in each of the other groups.The hyperuricemia rats model was created by continually intragastric (i.g) treatment with adenine and ethambutol hydrochloride for 3 weeks, and then changing administration to every other day till 12 weeks.The body weight of rats were monitored periodically.By the end of 12 weeks, the serum level of uric acid (UA) and peripheral hemogram were assayed, the bone marrow smear was examed, IL-1β secretion was checked and renal tissue sections were checked under a light microscope by PAS staining. Results Compared with the normal control, the serum level of UA, the count of WBC and PLT were remarkably increased, while the weigth of rats and the count of RBC were sharply reduced.The serum level of IL-1β was obviously increased too, and the inflammatory cells infiltration was found in renal tissues of the model rats.Compared with the model control, the ASRC at low-dose increased the count of RBC, decreased WBC and PLT (P<0.05), and effectively suppressed IL-1β secretion.The ASRC at high-dose inhibited the weight loss of hyperuricemia rat, decreased the content of serum UA and IL-1β.Only a few inflammatory cell infiltration was found in renal interstitial. Conclusion Long-term administration of ASRC at low-dose can reverse abnormal changes of peripheral hemogram in hyperuricacidemia rats, which is related to its effectively restraining the inflammatory response induced by IL-1β and slight changes of renal structure.The ASRC at high-dose could more effectively lower serum level of UA, which suggests that attentions should be paid to the dose in clinic uses.
  
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  药物研究

  Preparation and Pharmacokinetic Study Long Circulating Nano-Liposomes of Quercetin in Rats

  WANG Gang;DU Shi-ming;CHANG Ming-quan;ZENG Nan;YE Fang;CHEN Yong-shun

  2012, 31(10): 1275-1278. https://doi.org/10.3870/yydb.2012.10.008

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  Objective To prepare the long circulating nanoliposomes (QUE-LCL) of quercetin and measure their pharmacokinetic parameters in rats. Methods QUE-LCL was prepared by emulsified evaporation and solidification at low temperature.The blood samples were collected at different time points and concentrations of quercetin and QUE-LCL were measured by HPLC.The pharmacokinetic parameters were calculated with the software 3p97. Results The plasma QUE concentration and area under the curve (AUC) of QUE-LCL in rats were obviously higher than those of quercetin suspension.The volume of distribution (Vd) and plasma clearances of QUE-LCL were lower than those of quercetin suspension. Conclusion QUE-LCL prepared by emulsified evaporation and solidification at low temperature can prolong the circulation of quercetin in plasma, leading to 1ong circulating effects.
  
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  药物研究

  Effect of Ittirfil Baras on Mouse Model of Vitiligo

  Abdujelil Abdugheni;Rabigul Islam;Israpil Abay;

  2012, 31(10): 1279-1281. https://doi.org/10.3870/yydb.2012.10.009

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  Objective To analyze disassembled prescriptions of Ittirfil Baras and to explore the effect on mouse model of vitiligo. Methods C57BL mice were selected and the mouse model of vitiligo was established by chemical decolorization.Effects of different disassembled prescriptions of Ittirfil Baras on the formation of melanin in mouse hair follicle were observed.Besides, malondialdehyde (MDA), cholinesterase (CHE), monoamine oxidase (MAO) in serum and the local skin tissue, and serum tumor necrosis factor (TNFalpha) and interleukin2 (IL-2) levels were determined as well. Results The main drugs + supporting drugs and the whole prescription of Ittirfil Baras reduced serum MAO level (P<0.01);the main drugs, the main drugs + supporting drugs, the main drugs +adjusting drugs, the whole prescription of Ittirfil Baras reduced the MDA level of skin tissue (P<0.05 or P<0.01);the main drugs +adjusting drugs reduced the CHE level of skin tissue homogenate (P<0.05);the main drug, the main drugs + supporting drugs, and the whole prescription reduced the MAO level of skin tissue homogenate (P<0.05 or P<0.01). Conclusion Ittirfil Baras might play a role in reducing the level of serum MAO and the MAO, MDA, CHE levels of skin in the experimental mouse model of vitiligo.
  
  

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  药物研究

  Effects of Urotensin Ⅱ on Cardiomyocyte Oxidative Stress and NADPH Oxidase p22 phox Expression

  SHAO Zhi-ling;XIANG Jin-yi

  2012, 31(10): 1282-1284. https://doi.org/10.3870/yydb.2012.10.010

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  Objective To investigate the effects and mechanism of urotensin II (UⅡ) on cardiomyocyte oxidative stress. Methods The model of cardiomyocyte oxidative stress induced by UⅡwas established in the primary culture of neonatal rat cardiomyocytes.The content of reactive oxygen species(ROS) was measured by ROS sensitive 2,7dichlorofluorescein diacetate(DCFHDA) probe.As indexes of cardiomyocyte oxidative stress, the cell vialibity, cellular contents of MDA, SOD, and LDH were tested.The expression of NADPH oxidase p22 phox was assessed by Western blot. Results Urotensin Ⅱ significantly enhanced the intracellular dichlorofluorescein(DCF) signal, inhibited cell survival and SOD activity, upregulated LDH and MDA, and increased the p22 phox expression. Conclusion The stimulation of urotensin Ⅱ for cardiomyocyte oxidative stress may be associated with upregulation of p22 phox expression.
  
  
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  药物研究

  Effect of Rhein on NADPH Gene Expression in the Kidney of Diabetic Rats

  HUANG Juan;CHEN Wen-li;Huang Yun-fang;NIU Li

  2012, 31(10): 1285-1288. https://doi.org/10.3870/yydb.2012.10.011

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  Objective To observe the effect of Rhein on oxidative stress of kidney in diabetic rats. Methods Streptozotocin (STZ)induced diabetic nephropathy rats were randomly divided into model group and treatment group. Malondialdehyde (MDA) content and superoxide dismutase (SOD) activity in the rat renal tissues of the two groups were compared six weeks after the treatment. At the same time, blood glucose, serum creatinine, blood urea nitrogen, and 24 h urine protein quantitation were detected. Expression of p22phox and p47phox was determined by RTPCR. Results Urinary albumin, urea nitrogen level and kidney hypertrophy index were significantly improved in the treatment group, as compared with the model group. Kidney MDA content was decreased significantly (P<0.05), and the activity of SOD increased significantly (P<0.05). As compared with the control group, mRNA expression levels of p47phox and p22phox in the model group were increased significantly, and the expression levels were significantly reduced after Rhein intervention. Conclusion Rhein plays a protective role in type 2 diabetic nephropathy probably through inhibition of oxidative stress in the diabetic rats. Downregulating p22phox and p47phox expression in type 2 diabetic model rat kidney can protect rat kidney.
  
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  药物研究

  Effects of Compound Ant Wine on Accessory Sex Organs, Serum Testosterone and Nitric Oxide in Mice

  HUANG Pin-xin;LI Yan;CHENG Chang-ming;GUO Lian-jun

  2012, 31(10): 1288-1290. https://doi.org/10.3870/yydb.2012.10.012

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  Objective To study the effects of compound ant wine on accessory sex organ weight, the contents of serum testosterone and nitric oxide (NO) in mice. Methods The mice were intragastrically administered with compound ant wine at doses of 1.2 g.kg^-1 and 4.8 g.kg^-1.Then accessory sex organs of juvenile castrated mice, young mice and old mice were weighed.The sperm number of the young mice and the contents of serum testosterone and NO of the old mice were determined. Results Compound ant wine significantly increased the weight of seminal vesicle, prostate and preputial glands of the juvenile castrated mice, increased testicular weight and sperm count of the young mice, and increased the testis weight, contents of serum testosterone and NO of the old mice. Conclusion Compound ant wine can significantly increase the weight of the accessory sex organs in mice and its mechanism may be related to the increase in serum testosterone and NO content.
  
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  药物研究

  Pharmacokinetics and Bioavailability of Dexibuprofen Sustained Release Capsules in Rats

  XIE Bin;FANG Jian-guo;WANG Wen-qing;RAO Zi-chao;ZHANG Guang-xun;REN Xia;XIAO Jie-yu

  2012, 31(10): 1291-1294. https://doi.org/10.3870/yydb.2012.10.013

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  Objective To investigate the pharmacokinetics and bioavailability of selfprepared dexibuprofen sustained release capsules and reference formulation in rats. Methods An RP-HPLC method was established to determine the concentration of dexibuprofen in plasma. Dexibuprofen sustained release capsule was prepared, and its pharmacokinetic parameters and bioavailability in SD rats were studied after oral administration. Results The pharmacokinetics parameters of dexibuprofen showed that C_max was (1 173.87±281.68) and (1 186.06±268.79) μg.mL^-1, AUC_(0-t) (4 276.53±578.59) and (4 489.83±645.73) mg.L^-1.h, AUC_(0-∞) (5 095.58±683.82) and (5 466.37±753.35) mg.L^-1.h, t_max (1.33±0.26) and (1.58±0.49) h for self-prepared dexibuprofen sustained release capsules and reference formulation, respectively. There was no significant difference between the parameters of the two formulations (P>0.05). The relative bioavailability of self-prepared dexibuprofen sustained release capsules to reference formulation is (93.2±12.5)%. Conclusion The Results of statistical analysis show that selfprepared dexibuprofen sustained release capsules and reference formulation are bioequivalent.
  
  
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  药物研究

  Comparison of Cytotoxicity and Anti-HBV of Lamivudine and Interferon α2b in Vitro

  MA Yan;JIN Xiao-bao;HUANG Yan-ting;LU Xue-mei

  2012, 31(10): 1294-1297. https://doi.org/10.3870/yydb.2012.10.014

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  Objective To compare the cytotoxicity and antihepatitis B virus effect of lamivudine and α-interferon in vitro. Methods L-02 and HepG2.2.15 were treated with different concentrations of lamivudine and interferon α2b for 72 h in vitro, the survival rates of L-02 and HepG2.2.15 were assayed by MTT.HbsAg and HBeAg secretion of HepG2.2.15 was detected by ELISA. Results Lamivudine could inhibit L-02 and HepG2.2.15 in a certain extent, while interferon α2b promoted the proliferation of normal cells.Inhibition effect of lamivudine on HBsAg and HbeAg was greater than that of interferon α2b, and HBsAg inhibition rate of lamivudine was higher, while HbeAg inhibition rate of interferon α2b was the higher. Conclusion Combined use of lamivudine and α-interferon can improve the anti-HBV effect and quality.
  
  
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  药物研究

  Bioequivalence of Dirithromycin Enteric-coated Micropill Granules in Healthy Volunteers

  WANG Gui-fa;DING Yu-feng;ZHAO Hong-ying;LI Gong-hua

  2012, 31(10): 1297-1300. https://doi.org/10.3870/yydb.2012.10.015

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  Objective To study relative bioavailability and evaluate bioequivalence following oraladministration of reference capsules and test Entericcoated micropill granules of dirithromycin in healthy volunteers. Methods A single oral dose of 500 mg test or reference preparations of dirithromycin was given to 20 healthy volunteers in a randomized crossover study. The plasma concentrations of erythromycylamine were determined by HPLC-MS. The pharmacokinetic parameters were calculated with DAS2.0. The bioavailability and bioequivalence were evaluated. Results The detection limit of erythromycylamine in plasma was 5 ng.mL^-1and a good linearity relationship was obtained over the range of 5-1 000 ng.mL^-1,the linearity relationship was A＝68.87C +1.47 (r＝0.999 7). The relative standard deviation of withinday and betweenday was less than 9%.The pharmacokinetic parameters of test and reference preparations after a single oral dose were as following: AUC_0→96 were (3 537.39±576.32) and (3 065.47±558.63) ng.mL^-1.h;AUC_0→∞ were (4 059.27±737.25) and (3 831.76±687.51) ng.mL^-1.h;Cmax were (415.84±81.24) and (420.36±63.21)ng.mL^-1;tmax were(3.25±0.28) and (3.47±0.35)h.the relative bioavailability of tested granules was(105.72±17.83)%. Conclusion The LC-MS method was suitable for assaying erythromycylamine in plasma. Statistic analysis showed no significant differences between the two preparations of dirithromycin, and the bioequivalence of two preparations was equal.
  
  
精神科用药专栏
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  精神科用药专栏

  Therapeutic Effect of Sertraline on Patients with Coronary Heart Disease Accompanied by Anxiety and Depression

  XIONG Rong-hong;XIONG Shi-xi;ZHANG Hong

  2012, 31(10): 1301-1304. https://doi.org/10.3870/yydb.2012.10.016

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  Objective To investigate sertraline hydrochloride on symptoms of anxiety and depression in patients with coronary heart disease. Methods One hundred and seventynine cases with coronary heart disease accompanied by anxiety and depression were randomly divided into control group (87 cases) and intervention group (92 cases).They were given conventional treatment of coronary heart disease and psychological treatment, and at the same time the intervention group was orally administered with sertraline hydrochloride.Clinical symptoms (ECG STsegment change, the level of chest pain, etc.) and the SAS, SDS, SCL-90 scale scores were evaluated after treatment for 2 weeks and 8 weeks, respectively. Results After 8 weeks of treatment, the clinical symptoms in the intervention group (with sertraline hydrochloride) were alleviated significantly with totally efficiency rate (96.7%) higher than that in the control group (86.2%) (P<0.05).After treatment for 2 weeks and 8 weeks, SAS and SDS scores in the intervention group were significantly decreased as compared with those in the control group (P<0.01).In the intervention group, SAS and SDS scores were decreased significantly as compared with those in the control group (P<0.05) after treatment for weeks.SCL90 scale result showed that somatization, depression and anxiety status were improved significantly after treatment for 2 weeks and 8 weeks. Conclusion Sertraline can significantly improve anxiety and depression symptoms in patients with coronary heart disease, and significantly alleviate the acute clinical symptoms of patients with coronary heart disease.
  
  
药物与临床
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  药物与临床

  Therapeutic Effect of Sildenafil in Persistent Pulmonary Hypertension of the Newborn

  CHEN Ling

  2012, 31(10): 1315-1317. https://doi.org/10.3870/yydb.2012.10.021

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  Objective To evaluate the effectiveness of sildenafil (SIL) in the treatment of neonatal pulmonary hypertension. Methods Thirty fullterm and nearly fullterm neonates with persistent pulmonary hypertension (PPHN) were randomly assigned to two groups: 18 infants in treatment group received 0.5 mg.kg^-1 of oral sildenafil every 6 h for 3 days, and 12 infants in control group received placebo. All infants received comprehensive treatment including mechanical ventilation, expansion of infusion, and so on. Arterial blood gases were taken before and 3 days after treatment. Oxygenation index (OI) was calculated. Hear rate, blood pressure, vomit and so on were recorded. Results After 3 days of treatment, all infants get significantly higher PaO2 and lower OI and PAP (all P<0.01). Meanwhile, we observed significantly better oxygenation parameters (PaO2, OI) and lower pulmonary artery pressure (PAP) in treatment group than in control group after 3 days of SIL administration. No side effects happened in all patients treated with SIL. Conclusion Oral sildenafil is an effective and safe drug to reduce PAP and improve oxygenation in patients with PPHN.
  
  
  
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  药物与临床

  Efficacy and Safety of Sorafenib in Patients with Renal Cell Carcinoma Brain Metastases

  YANG Lin;DING Ying-jun;SHI Lei;YU Shi-ying

  2012, 31(10): 1318-1321. https://doi.org/10.3870/yydb.2012.10.022

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  Objective To evaluate safety and efficacy of sorafenib in patients with renal cell carcinoma brain metastases (RCCBM). Methods Sorafenibrelated adverse events and the clinical efficacy in RCCBM patients were retrospectively analyzed.The category, severity and turnover of sorafeinbrelated adverse events were observed.Also, the disease control rate (DCR), progressionfree survival (PFS) and overall survival (OS) were analyzed. Results In the seven RCCBM patients treated with sorafenib, the most common adverse events were handfoot syndrome, diarrhea, rash, hypertension, fatigue and alopecia.Most of the adverse events happened in mild to moderate degree, and were alleviated after corresponding treatment.No severe adverse events like intracranial hemorrhage happened.The DCR, median progress free survival and median overall survival were 57.1%, 5 months and 16 months, respectively. Conclusion The safety of sorafenib in RCCBM patients is satisfying.After local treatment, patients can obtain longterm clinical benefit from sorafenib treatment.
  
药物制剂与药品质量控制
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  药物制剂与药品质量控制

  TCL Identification of Chief Ingredient and Determination of Volatile Oil Content in Compound Rhinobol Tablet

  MO Ming-xiu;ZHANG Xiao-ying;LIANG Hui-ming;OUYANG Shu-jing

  2012, 31(10): 1344-1347. https://doi.org/10.3870/yydb.2012.10.031

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  Objective To establish a method of quality control for Compound Rhinobol tablet. Methods Radix Glycyrrhizae, Herba Asari and Flos Magnoliae in the Compound Rhinobol tablet were identified by method of thinlayer chromatography (TLC). Content of the essential volatile oil in the tablet was determined by using the method in “Pharmacopoeia of the People’s Republic of China” (2010). Results The spots in TLC were clear and easily distinguished without interference in negative control. The average content of the essential volatile oil in Compound Rhinobol tablets was 0.42%. Conclusion The method is reliable and easily operated, with accurate result. It can be used for the quality control of the Compound Rhinobol Tablet.
  
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  药物制剂与药品质量控制

  Determination of Content of Itraconazole Transfersomes and Its Entrapment Efficiency by HPLC

  ZHENG Wen-sheng;FANG Xia-qin;ZHANG Yu-jia;WANG Lu-lu

  2012, 31(10): 1347-1349. https://doi.org/10.3870/yydb.2012.10.032

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  Objective To establish an HPLC method for determination of content and entrapment efficiency of itraconazole transfersomes. Methods The content of itraconazole was separated with a C18 column (150 mm×4.6 mm,5 μm).The mobile phase was acetonitrilewater (65:35) at a flow rate of 1.0 mL.min^-1 and itraconazole was detected at 261 nm and room temperature. Results The linear range of itraconazol was 1 to 100 μg.mL^-1 (r＝0.999 7).The average recovery was 101.9% and RSD was 1.7%. Conclusion This method is simple, accurate, sensitive and applicable for determination of the content and entrapment efficiency of itraconazole transfersomes.
  
  
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  药物制剂与药品质量控制

  Preparation and Optimized Formation of Orally Disintegrating Tablets of Imidafenacin

  LI Li-ran;GUO Hong;WANG Cheng-gang;REN Xiao-wen

  2012, 31(10): 1350-1354. https://doi.org/10.3870/yydb.2012.10.033

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  Objective To investigate the preparation and formulation of orally disintegrating tablets of Imidafenacin. Methods The orally disintegrating tablets of imidafenacin were prepared by using the technology of direct compression and sublimation drying.The formulation was optimized by single factor test, in which, the kind of disintegrants, amount of disintegrants and sublimation agent were investigated.All formulations were evaluated by flow properties, wetting time, and in vitro disintegration time (DT).Based on the established formulation, the relationship between tablet hardness and disintegration time was studied.The best prescription and the orally disintegrating tablets with high porosity and good hardness were obtained. Results The tablets were composed of mnnitol, 40% MCC, 5% PVPP, and 10% Ammonium bicarbonate, with the hardness of 4.0-6.0 kg, the optimal product was prepared after drying in vacuum oven at 60 ℃ for 90 min. Conclusion The method is simple and accurate in preparation.
  
  
用药指南
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  用药指南

  Interaction of Valproic Acid and Carbapenem Antibiotics

  LI Juan;JIANG Hui;WEI Jin-xia

  2012, 31(10): 1364-1366. https://doi.org/10.3870/yydb.2012.10.038

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  Objective To discuss the drug interaction between valproic acid (VPA) and carbapenem antibiotics (CP) in epileptic patients. Methods The clinical data of seven symptomatic epileptic patients with severe pneumonia treated with VPA and CP were analyzed retrospectively.The serum concentration of VPA was monitored before, during and after the combined use of VPA and CP. Results In four cases with combined use of VPA and meropenem, VPA was decreased significantly, with the level ranging from 4 to 15 μg.mL^-1, which was 40-70 μg.mL^-1 lower than before the treatment.In one patient prescribed with VPA and meropenem at the same time, the serum concentration of VPA could not reach the therapeutic window.In two cases with concomitant use of VPA and imipenem, the serum level of VPA did not decrease. Conclusion Concomitant administration of VPA and meropenem leads to a rapid decline in serum concentration of VPA.To avoid the recurrence of epileptic seizures, the concomitant administration of VPA and meropenem should be avoided in clinic.There is no decrease of serum concentration of VPA in the concomitant administration of VPA and imipenem, but more data are needed to demonstrate it.
  
  
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  药事管理

  Evaluation and Analysis of Outpatients and Emergency Prescriptions in Ten Hospitals of Luzhou Area and Control Measures

  LUO Hong-li;XIAO Shun-lin;WANG Shu-rong

  2012, 31(10): 1387-1388. https://doi.org/10.3870/yydb.2012.10.047

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  Objective To investigate the enforcement of the “prescription management method” in primary hospitals so as to promote rational drug use. Methods A total of 6 000 outpatients and emergency prescriptions in 10 hospitals of Luzhou area from Mar.to Jun.in 2011 were randomly checked, and seven core indicators were collected for the analysis of prescription quality. Results In Luzhou area, an average of 2.59 and 2.69 kinds of drugs in secondary and tertiary hospital were prescribed respectively in each prescription;the utilization rates of antibacterials, injection, essential drugs, the drugs prescribed in their common names and antibacterials amount accounted for 37.59% or 31.58%, 24.21% or 28.50%, 47.69% or 42.92%, 83.99% or 93.18%, 24.52% or 20.50%, respectively in secondary and tertiary hospital.An average consumption sum of 80.75, 127.30 Yuan respectively in secondary and tertiary hospital was involved in each prescription.The conformity rate of prescriptions was 76.46% and 83.92% respectively. Conclusion The drug use for the outpatients in these hospitals is rational on the whole, but measures should be taken to tighten control on the drug use by teaching doctors so as to reduce the incidence of irrational drug use.