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2012 Vol. 30, No. 6

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Progress of Raman spectroscopy in fast detection of counterfeit drugs
LIU Yan, YIN Li-hui, LU Feng
2012, 30(6): 401-404,446. doi: 10.3969/j.issn.1006-0111.2012.06.001
Abstract(13353) PDF (859KB)(3254)
Counterfeit drugs not only affected drug safe and function, but also disturbed the commerce and social order. It had become so urgently to combat counterfeit drugs. Recently, Raman spectroscopy had been a more and more popular technique in the fast detection of counterfeits. In this paper, the advantages of Raman spectroscopy in fast detection of counterfeit drugs were explained. Combined with the discussion of the methods of the spectral pretreatment and qualitative analysis, the application of Raman spectroscopy in fast detection of counterfeit drugs was reviewed. On the basis of the overview of the present progress of the Raman spectroscopy in fast detection, the future research direction and areas were forecasted.
Clinical application of Sugammadex
WANG Yun, CAO Yong-bing, JIANG Yuan-ying, YAN Tian-hua
2012, 30(6): 405-407,453. doi: 10.3969/j.issn.1006-0111.2012.06.002
Abstract(7892) PDF (613KB)(2772)
Sugammadex had been licensed for reversal of rocuronium and vecuronium induced neuromuscular blockade in Europe since 2008, which had shown to be efficacious and had a good safety profile so far. The potential for Sugammadex to change the management of NMB, in routine clinical practice, in emergency situations and in special populations were reviewed in this paper.
Progress on drug treatment of chronic obstructive pulmonary disease
CHEN Kai-yu, JIANG Li-ping, CHEN Sheng-xin
2012, 30(6): 408-411. doi: 10.3969/j.issn.1006-0111.2012.06.003
Abstract(14796) PDF (600KB)(2647)
Chronic obstructive pulmonary disease(COPD), the fourth leading cause of death in the world, represented an important public health challenge. Appropriate medicine therapy in COPD was used to reduce symptoms, the frequency and severity of exacerbations, and improve exercise tolerance and health status. Rational use of the drugs that have different mechanisms, different duration of action was a research focus of COPD. The progress of COPD drug during these years and the strategy of drug treatment were reviewed in this paper.
Progress on the impurities in Oxaliplatin
NIU Chong, LIU Gui-hua, ZHANG Zhong-hu
2012, 30(6): 412-414,436. doi: 10.3969/j.issn.1006-0111.2012.06.004
Abstract(13840) PDF (630KB)(2808)
The research progress on the preparation and impurities of Oxaliplatin were summarized based on the recent documents, which generalize the impurity organization, impurity controlling and preparation stability. The principal impurities in Oxaliplatin were oxalic acid, impurity B, impurity C, impurity D and impurity E. All of the impurities were produced during the syntheses and also could be degraded from Oxaliplatin and its preparation. The impurities in Oxaliplatin and its preparation must be controlled respectively to ensure the security and effect of the drugs.
Studies on compliance in the treatment of depression
WEI Long-jing
2012, 30(6): 415-417,474. doi: 10.3969/j.issn.1006-0111.2012.06.005
Abstract(4600) PDF (599KB)(1908)
The definition, evaluation methods, grade classification, research status, influence factors and intervention measures of the compliance in the treatment of depression were reviewed in this paper based on the literatures home and aboard. It was clarified that the compliance in the treatment of depression was effected jointly by several factors. Making intervention plan for patients individually could improve the anti-depressant adherence and had a greater decrease in depressive symptoms. The review was to attract more attention to the study on compliance in the treatment of depression and offer some references to the related research.
Advance in chiral separation and stereo selectivity pharmacokinetics of azole antifungal drugs
GUO Kai-xin, SHI Kuan, WEN Jun, ZHOU Ting-ting, FAN Guo-rong
2012, 30(6): 418-421. doi: 10.3969/j.issn.1006-0111.2012.06.006
Abstract(4225) PDF (485KB)(1727)
Generally azole antifungal drugs possessed chiral center. After administration of the racemate, the results indicated the differences in plasma concentrations and pharmacokinetic parameters between enantiomers were stereoselctive. The metabolism might be mainly responsible for the chiral pharmacikinetics of the enantiomers. The quantitation of enantiomers in biological matrix was based on the development of chiral separation techniques. In this paper, the chiral separation techniques of these agents and the advance in chiral pharmacokinetics of ketoconazole and itraconazole were reviewed, which could provide some references to the discovery of azole antifungal new agents.
Design, synthesis and anti-tumor activity of N-Phenyl-2-(4-phenyl)-cyclo-propane-1-carboxylic acid-1-amide
CHEN Huan, GENG Dong-ping, LI Ke
2012, 30(6): 422-426,461. doi: 10.3969/j.issn.1006-0111.2012.06.007
Abstract(13102) PDF (904KB)(1374)
Objective To design, synthesize and study the anti-tumor activity in vitro of N-Phenyl-2-(4-phenyl)-cyclopropane-1-carboxylic acid-1-amide compounds. Methods The target compounds were obtained through knoevenagel condensation, cyclization, hydrolysis and amidation reaction, microwave reaction equipment contributed to improve efficiency. Structure of the target compounds were determined by 1H NMR and LC-MS. Results Design, synthesis of 20 novel cyclopropyl-amide compounds and anti-tumor assay showed all of the target compounds had significant anticancer activity in vitro. Compound 5b had the best activity in A549 cell with IC50 6.8 μM. Conclusion 4-trifluoromethyl substituted phenyl compounds had better anticancer activity than 4-chlorine substituted phenyl compounds.Electron-withdrawing group made more contributed than electron-donating group for anticancer activity in vitro.
Synthesis and antitumor activities of 5-hydroxy-4'-nitro-7-substituted benzyloxy-isoflavone
WANG Xiao-hua, WANG Wei, LIU Chao-mei
2012, 30(6): 427-429. doi: 10.3969/j.issn.1006-0111.2012.06.008
Abstract(6186) PDF (532KB)(1294)
Objective To design and synthesize genistein's derivatives:5-hydroxy-4'-nitro-7 -substituted benzyloxo-isoflavones and evaluate the antitumor effects in vitro. Methods Benzyl chloride was used as the starting reagent, to obtain title compounds by multi-step reaction:substitution, nitration, Friedel-Crafts reaction, cyclation reaction and benzylation. Results Two important intermediates:4'-nitrodeoxybenzoin and 4'-nitrogenistein and seven title compounds were synthesized, which had been identified by elemental analysis and 1H NMR. Conclusion Introduction of simple substituted benzyl group to 7-posion hydroxy could not enhance the antitumor effects of this type of compounds.
Synthesis and biological activity of 1H-pyrrol-2(5H)-ones
ZHAO Fang-zhen, ZHUANG Chun-lin, GUO Zi-zhao, SHENG Chun-quan, YAO Jian-zhong, MIAO Zhen-yuan, ZHANG Wan-nian
2012, 30(6): 430-432,456. doi: 10.3969/j.issn.1006-0111.2012.06.009
Abstract(5166) PDF (717KB)(1519)
Objective To study the biological activity of 1H-pyrrol-2(5H)-ones which introduced substituted phenyl group as side chain. Methods By introduction of 5-substituted phenyl group, a serial 1H-pyrrol-2(5H)-ones were synthesized and their structures were confirmed by 1H NMR and MS. The binding constant Ki was assayed by the fluorescence polarization binding assay method. Results Thirteen title compounds exhibited stronger protein binding activities and compound 4e showed five times higher than positive drug. Conclusion The introduction of electron-attracting groups was beneficial to improve their activities. Among them, the nitro group was preferred group.
Determination of four major steroid glycosides in Anemarrhena asphodeloides by HPLC-ELSD
YIN Cha, WU Ting-ting, ZHU Dong-liang, LIU Zhi-rui, CHAI Yi-feng
2012, 30(6): 433-436. doi: 10.3969/j.issn.1006-0111.2012.06.010
Abstract(14400) PDF (591KB)(2867)
Objective To develop a new high performance liquid chromatography (HPLC) coupled with Evaporative Light Scattering Detector (ELSD) method for simultaneous determination of four major steroid glycosides (Timosaponin B, Timosaponin E1, Timosaponin BⅡ and Timosaponin AⅢ). Methods HPLC analysis was performed on an Agilent Zorbax SB-C18 column (4.6 mm×250 mm, 5 μm) with a mobile phase of water (adjust to pH 3.3 by acetic acid) (A) and acetonitrile (B). The gradient elution program was as follow:0~8 min, 12%~23% B;8~25 min, 23% B;25~35 min, 23%~45% B;35~40 min, 45%~95% B. The temperature of drift tube was 55℃ and the nebulizer nitrogen flow rate was 4.0 Bar. Results The linearity was obtained over 42.10~252.6 μg/ml (r=0.999 3) for Timosaponin B, 48.80~292.8 μg/ml (r=0.999 1) for Timosaponin E1, 192.2~1153 μg/ml (r=0.999 7) for Timosaponin BⅡ and 8.512~85.12 μg/ml (r=0.998 5) for Timosaponin AⅢ. The RSDs of precision and stability of the samples were both less than 1% in 48 hours. The average recovery was between 96.04%~102.8%. Conclusions The present method, with satisfactory efficacy, was simple which could simultaneously determine multiple steroid glycosides in Anemarrhena asphodeloides Bge. from different areas.
Analysis on chemical constituents of Scutellaria barbata by HPLC-TOF/MS
JI Song-gang, LIU Yue, MAO Fei, LI Xiang, CHAI Yi-feng
2012, 30(6): 437-439,472. doi: 10.3969/j.issn.1006-0111.2012.06.011
Abstract(4698) PDF (710KB)(2014)
Objective To analyze chemical constituents of Scutellaria barbata D.Don by high pressure liquid chromatography-time of flight mass spectrometry (HPLC-TOF/MS). Methods A SHISEIDO CAPCELL PAK C18 (100 mm×3.0 mm, 3 μm) was used to separate. The mobile phase consisted of water containing 0.1% methane acid and acetonitrile was used as gradient elute. The flow rate was 0.6 ml/min. TOF/MS was applied for qualitative analysis under positive ion mode. Results Under optimized condition, 15 major constituents in Scutellaria barbata D.Don were identified by time of flight mass spectrometry and structure-relevant fragment ions. Conclusion A simple and reliable method using HPLC-TOF/MS was established to identify the chemical constituents of Scutellaria barbata D.Don.
Penetration enhancement of electret and united Azone on cyclosporin A transdermal delivery in vitro
LIU Hong-yue, JIANG Jian, MA Lin, LIANG Yuan-yuan, DONG Fa-jie, CUI Li-li
2012, 30(6): 440-442,466. doi: 10.3969/j.issn.1006-0111.2012.06.012
Abstract(4488) PDF (873KB)(1224)
Objective To study the penetration enhancement of electret and united Azone on cyclosporin A transdermalde livery in vitro. Methods Using corona charged -500 V, -1 000 V and -2 000 V polypropylene (PP) as electrets, 1%, 3% and 5% Azone as chemical enhancers, the transdermal behaviours of the cyclosporine A in solution were evaluated by modified Franze diffusion cell method. The concentration of cyclosporine A was measured by HPLC. Results All the electrets and chemical enhancers used in this study enhanced the cumulative penetration amount of the drug. The combination of -1 000 V and 1% Azone showed a slight increase in cumulative penetration amount of the drug compared with that of the 1% Azone used alone. Conclusion Both the negative electret and Azone could enhance the transdermal delivery of cyclosporin A individually. But negative electret and Azone had no synergistic enhancing effect on cyclosporin A transdermal delivery.
Therapeutic effects of Thesium chinensis on adriamycin-induced nephropathy rats
XUAN Wei-dong, TANG Da-hai, BIAN Jun, HU Shui-gen, HU Jiang-feng, FAN Zheng-ping
2012, 30(6): 443-446. doi: 10.3969/j.issn.1006-0111.2012.06.013
Abstract(4061) PDF (901KB)(2075)
Objective To investigate the therapeutic effects of Thesium chinensis Turcz on Adriamycin-induced nephropathy rats. Methods 40 SD rats were divided into 4 groups averagely:normal control group, model control group, low-dosage group (1.0 g/(kg·d) and high-dosage group(5.0 g/(kg·d). Nephritic syndrome models were established in 30 rats by intravenous injection of Adriamycin (6.0 mg/kg). The rats of low-dosage group and high-dosage group were intragastric administrated decoction of Thesium chinensis Turcz daily, the model control group rats were given running water(2 ml). During 5 weeks treatment process, the 24 hour urine volume, 24 hour urine protein concentration of rats were observed. The level of total serum protein(TP), serum albumin(ALP), total cholesterol(TCH), triglycerides(TG) and UREA were determined, and the pathological changes of kidney tissue were assayed after the therapy process. Results The symptoms of nephritic syndromes, such as edema, tail-rot disease, were relieved by Thesium chinensis Turcz. After 2 weeks therapy, the 24 hour urine volume of low-dosage group and high-dosage group were significantly higher than model control, and the 24 hour urine protein concentration were significantly lower than model control after 3 weeks. The level of TP and ALP of low-dosage group were significantly higher than model control, as well as the level of TCH and TG were significantly lower after 5 weeks. Conclusion Thesium chinensis Turcz could eliminate tissue edema and decrease the urine protein concentration by diuretic action and improves renal pathology to protect the kidney from damage by reducing the serum cholesterol level, decreased blood lipid content, and increased the plasma protein level.
Therapeutic effect and adverse reaction of Thalidomide combined with dexamethasone in elderly patients with multiple myeloma
WU Ning-ning
2012, 30(6): 447-448. doi: 10.3969/j.issn.1006-0111.2012.06.014
Abstract(6300) PDF (445KB)(2477)
Objective To observe the efficiency and safety of thalidomide combined with dexamethasone in elderly patients with multiple myeloma. Methods A total of 50 elderly patients with multiple myeloma in initial treatment were administered thalidomide combined with dexamethasone. Thalidomide was administered at an initial dose of 50 mg once-daily orally followed by gradually increased in 50 mg according to patients' tolerance to a maximum of 200 mg once-daily orally, dexamethasone was administered at 20 mg once-daily IV in 1~4 d, 9~12 d and 17~20 d with 28 d as a course of treatment. The efficiency after 4 courses of treatment eva-luate was evauated. Results Complete remission were in 15 cases, immense partial remission in 12 cases, partial remission in 13 cases, no change in 5 cases and progression of disease in 5 cases. The total effective rate was 80%. During treatment, there were 17 patients suffering from hypersomnia, 16 onstipation, 16 lassitude, 10 increased blood sugar, 8 peripheral neuropathy and 3 rashes. All the patients could tolerant after expectant treatment. Conclusion It could be an effective method of thalidomide combined with dexamethasone in elderly patients with multiple myeloma.
Clinical observation of dermlin combined nursing care in treatment of superficial degree Ⅱ burn
MAO Qiao-yan
2012, 30(6): 449-450. doi: 10.3969/j.issn.1006-0111.2012.06.015
Abstract(3920) PDF (442KB)(1090)
Objective To explore the effect of dermlin combined nursing care in treatment of superficial degree Ⅱ burn. Methods By simple randomization, the patients were assigned to the control group and the observed group(accepted the treatment of dermlin). The difference of the clinical efficacy, healing time and infection complications were compared between the two groups. Results The clinical efficacy in the observed group were significantly higher than that in the control group(P<0.05), the healing time and infection complications in the observed group were significantly lower than that in the control group(P<0.05). Conclusion Dermlin and nursing care had a good effect in treatment of superficial degree Ⅱ burn.
Determination of quercetin in Gnaphalium affine
WEI Shao-xuan, XIA Ai-jun, LIAO Hou-zhi
2012, 30(6): 451-453. doi: 10.3969/j.issn.1006-0111.2012.06.016
Abstract(3720) PDF (595KB)(2114)
Objective To establish the determination method of Quercetin content in Gnaphalium affine D. Don. Methods VP-ODS Cl8(4.6 mm×150 mm, 5 μm) colmnn was used, the mobile phase was methanol-0.2% phosphoric acid solution(45:55) with the flow rate as 1.0 ml/min. The detection wavelength was 375 nm. Results The linear relation of hyperin was good in the range from 10.22 μg/ml to 51.10 μg/ml. The average recovery was 100.18%, RSD was 1.38%. Conclusion The method established was accurate, sensitive and good in reproducibility which could be applied to the quality control of G. affine D. Don.
Determination of residue organic solvents in Loperamide Hydrochloride by headspace capillary gas chromatography
HU Meng-shen, HONG Zhi-ling, HUANG Jian-ying
2012, 30(6): 454-456. doi: 10.3969/j.issn.1006-0111.2012.06.017
Abstract(5537) PDF (625KB)(1661)
Objective To develop a method of headspace capillary gas chromatography for determining residual organic solvents in loperamide hydrochloride. Methods The carrier gas was nitrogen and FID as detector. The nine organic solvents including methanol, isopropanol, n-hexane, ethyl acetate, tetrahydrofuran, chloroform, methyl isobutyl ketone, toluene, benzene were separated on a DB-624 capillary column(30 m×0.32 mm×0.25 μm)by programmable increased temperature and headspace gas chromatography. Results The nine organic solvents were separated and each of them showed linear relationship in the concentration range measured. The recoveries and RSDs were in range from 95.2% to 102.3% and 0.8% to 2.9%, respectively. Conclusion The method was simple, accurate and reproducible.
Determinatin of chlorogenic acid in hawthorn by HPLC
LIANG Rui-shu, ZHANG Chuan, ZOU Hao, JIN Lei
2012, 30(6): 457-458,477. doi: 10.3969/j.issn.1006-0111.2012.06.018
Abstract(9304) PDF (580KB)(2644)
Objective To establish a HPLC method for determination of chlorogenic acid in the hawthorn. Methods Sunfire C18 (4.6 mm×250 mm, 5 μm) column was used. The mobile phase was methanol:sodium dihydrogen phosphate(25:75). The flow rate was 1.0 ml/min, and the temperature was at 28℃. The detection wavelength was 327 nm. Results The calibration curve was at the range of 7.03~70.3 μg/ml (r=0.999 6), RSD was 0. 92% (n=6) and the average recovery was 96.92%. Conclusion The method was simple, reliable, accurate for determination of chlorogenic acid in the hawthorn.
Surveillance and analysis of quality of pharmaceutical Tween 80
GUO Zhi-xin, SUN Hui-min, YANG Rui, GAO Zhi-feng, WANG Hua
2012, 30(6): 459-461. doi: 10.3969/j.issn.1006-0111.2012.06.019
Abstract(13734) PDF (530KB)(3109)
Objective To study the quality state of pharmaceutical Tween 80 in China. Methods Pharmaceutical Tween 80 from 10 factories were sampled and examined. The irregular qualify and sensitization in TCM injection of Tween were discussed. Results Some suggestions and strategies were presented about the quality problem of pharmaceutical Tween 80. Conclusion The use of Tween 80 in injection should be further specificated.
Cost utility analysis of vinorelbine versus gemcitabine combined with cisplatin of advanced non-small cell lung cancer
HE Zhi-gao, YAN Jun, CHEN Guo-han, BAO Si-wei, ZHAI Xiao-bo, JIN Li, SHI Yan
2012, 30(6): 462-463,480. doi: 10.3969/j.issn.1006-0111.2012.06.020
Abstract(4036) PDF (534KB)(1000)
Objective To compare and evaluate the effectiveness and cost utility of vinorelbine versus gemcitabine combined with cisplatin of advanced non-small cell lung cancer. Methods 60 advanced patients wit NSCLC were enrolled into two groups, the effectiveness and cost utility were evaluated after 2 cycles. Results The efficacy rate wit NP and GP were 36.6%and 40.0% respectively, An existence period wit NP and GP were 8.52 and 8.37 respectively, showing no significant difference (P>0.05) between the two groups. One year survival rate with NP and GP were 36.6%and 40.0% respectively; two year survival rate with NP and GP were 16.6%and 13.3% respectively. The ratio of cost utility with NP and GP were 1123.41and 1556.61 respectively. Conclusion The effectiveness of NP versus GP of advanced non-small cell lung cancer was similar, the cost utility of NP was more than GP.
Working pattern for rationality checking of the orders in pharmacy intravenous admixture center
TANG Zhi-hui, PEI Bao-xiang, LIANG Xiao
2012, 30(6): 464-466. doi: 10.3969/j.issn.1006-0111.2012.06.021
Abstract(4130) PDF (650KB)(1210)
Objective To describe the work pattern for rationality checking of the orders in Pharmacy intravenous admixture center. Methods Irrational orders checked from Jan. to Oct. in 2011 were analyzed to evaluate the rationality and practicability of the normalized work pattern for real-time checking the rationality of drug use. Results The process of real-time checking and interfering the irrational orders was set up. The order checking was carried out by assigned people, the omission mistake was avoided in checking irrational orders and the rationality of orders was improved, the communication with doctors and nurses was strengthened. Conclusions The establishment of work pattern for real-time checking and interfering of the irrational orders consistent with the standard of hospital supplied a standardized and normalized method for the checking of rational drug use.
Analysis of antibiotic injections for pediatric in outpatient department in our hospital
2012, 30(6): 467-469,474. doi: 10.3969/j.issn.1006-0111.2012.06.022
Abstract(4079) PDF (593KB)(1827)
Objective To study the rational use of antibiotic injections for pediatric in outpatient department in our hospital. Methods 669 prescriptions of pediatric outpatient from January to August of 2011 were randomly collected, according to the Antibiotics Application Guideline, the application of the antibiotic injections was judged and descriptive statistical analyzed. Results The numbers of prescriptions of intravenous antibiotics were 658, which took 98.4% in total. 13 kinds of antibiotic injections in five categories were used. The used rate of third generation cephalosporin was34.7%, and macrolide was 14.1%. The number of combined application of antibiotics prescriptions were 72(10.8%), combined application of non-antibiotics prescriptions were 648(96.9%). The average number of prescription was 3.2. The medication of 607(90.5%) prescriptions was consistent with the diagnosis. There were many deficiency in package inserts for pediatric patients. Conclusion The antibiotic injections were rationally used for pediatric in outpatient department in our hospital, but it still had some problems.Therefore, more efforts should be done to promote the reasonable application of antibiotic injections in children.
A case and literature analysis of epileptic seizure caused by metronidazole injection
GONG Yan-bo
2012, 30(6): 470-472. doi: 10.3969/j.issn.1006-0111.2012.06.023
Abstract(3459) PDF (531KB)(1330)
Objective To discuss the factors of epileptic seizure caused by metronidazole injection and give some prevention measure. Methods A case of epileptic seizure caused by metronidazole injection were analyzed, and the literatures about epileptic seizure caused by metronidazole were retrieved and analyzed. Results The metronidazole could cause epileptic seizure, which seldom could be seen. Conclusion The age of patient and using interval should be remarked to avoid epileptic seizure when the metronidazole injection was used.
2012, 30(6): 473-474. doi: 10.3969/j.issn.1006-0111.2012.06.024
Abstract(3444) PDF (499KB)(1393)
Discussion on teaching innovation of pharmacy administration
WANG Rui-li, BAI Ke-hua, ZHANG Li-feng
2012, 30(6): 475-477. doi: 10.3969/j.issn.1006-0111.2012.06.025
Abstract(4057) PDF (512KB)(1101)
According to the situation of pharmacy administration in our school, certain beneficial improvement method and assumption on Pharmacy Administration Course were put forward, in related to the teaching method, content as well as resource of teacher according to teaching practices of many years.
Practice of constructivism theory in pharmacy continuing education
SHI Ming-li, GAO yue, LV chao
2012, 30(6): 478-480. doi: 10.3969/j.issn.1006-0111.2012.06.026
Abstract(13028) PDF (512KB)(1143)
Objective To summarize the practice of pharmacy continuing education in recent years and gather experiences for improving teaching quality and teaching standard of the continuing education. Methods Adult learners' characteristic was analyzed and constructivism theory was applied to guild teaching design and teaching practice. Results By using new form and new structure of lessons, the enthusiasm and creativity of teachers and students, the teaching quality and effect were fully promoted. Conclusion The Application of constructivism theory to teaching process design for licensed pharmacist continuing education was effective.