中国科技论文统计源期刊 中文核心期刊
美国《化学文摘》《国际药学文摘》
《乌利希期刊指南》
WHO《西太平洋地区医学索引》来源期刊
日本科学技术振兴机构数据库（JST）
第七届湖北十大名刊提名奖
美国《化学文摘》《国际药学文摘》
《乌利希期刊指南》
WHO《西太平洋地区医学索引》来源期刊
日本科学技术振兴机构数据库（JST）
第七届湖北十大名刊提名奖
Quality control of biotech drugs has attracted increasing attentions in recent years. Deamidation reaction is one of the major concerns in quality control of biotech drugs, due to the generation of isoaspartic acid(isoAsp). This paper describes the deamidation of asparagine(Asn) residues and its effects on the biological drugs. The detection methods currently used in China and overeas for this reaction, including pretreatment protocols and instrumental analysis were described. The identification and determination of isoaspartyl sites were also described in detail, along with the positive impact on the development of biotech drugs in China by the studies on deamidation reactions.
Objective To probe into effect of Dracocephalum heterophyllum Benth flavonoids(DHBF) on noradrenaline (NE)-induced myocardial cell hypertrophy,and to study the mechanism. Methods SD neonatal rat myocardial cells were cultured in vitro. The experiment was divided into normal control group, model control group (NE 2 μmol·L-1), prazosin group(prazosin 50 μmol·L-1),low-,medium- and high-dose DHBF group (DHBF 10,25,50 μmol·L-1).Cardiomyocyte hypertrophy were induced by NE(2 μmol·L-1). DHBF and prazosin were intervened respectively. CCK-8 method was used to observe the activity of myocardial cells. RT-PCR technique was used to detect the expression of mRNA of cardiac hypertrophy c-jun and brain natriuretic peptide (BNP),and Western blotting was used to detect the protein expression of CaN and NFAT-3 in myocardial cells. Confocal laser scanning was used to detect the surface area of myocardial cell. Results Compared with the normal control group, survival rate of cardiomyocytes was significantly decreased, expression of mRNA of c-jun and BNP significantly upregulated, protein expression of CaN and NFAT-3 decreased, and surface area increased in model control group (P<0.05). Compared with the cell of model control group, low-,medium- and high-dose DHBF significantly reversed NE-induced decrease of the survival rate, increase of surface area, increase of c-jun and BNP mRNA, and increase of CaN and NFAT-3 protein expression (P<0.05). Conclusion DHBF can improve the survival rate of cardiac hypertrophy patients, down-regulate c-jun and BNP mRNA expression, decrease CaN and NFAT-3 protein expression, and decrease NE-induced surface area of cardiomyocytes.
Objective To evaluate the safety of morphine hydrochloride injection. Methods Ear verin injection was used to evaluate the vascular irritation using the comparison of left side with right side in rabbits. Quadriceps femoris injection was used to evaluate the muscle irritation using the comparison of left side with right side in rabbits. Guinea pigs were intravenously injected with morphine hydrochloride injection at a dose of 2.8 mg·kg-1 once daily 3 times, stimulation was performed on 14 d after the last sensitization and the booster dose was 2 times the sensitization dose. The allergic reactions were observed. The different concentrations of morphine hydrochloride injection were placed in 2% rabbit erythrocyte suspension, and then the hemolyzation and agglutination were observed. Results There were no significant vascular or muscular irritation and injury effects of morphine hydrochloride injection in rabbits. There were no evidenceof hemolyzation and agglutination in rabbit erythrocytes in vitro.No allergic reactions on guinea pigs in vivo were observed. Conclusion After treatment of morphine hydrochloride injection, neither obvious vascular/muscle stimulation or sensitization, nor hemolyzation or agglutination appeared in rabbits. The research results provide basic reference for the clinical rational and safe application of morphine hydrochloride injection.
Objective To observe the effect of Kadsura coccinea on the expression of Bcl-2, Bax and proliferating cell nuclear antigen(PCNA) in liver tissue of experimental hepatic fibrosis rats, to further discuss the mechanism of anti-liver fibrosis. Methods Sixty SD rats were randomly divided into normal control group, model control group, colchicine group, low-dose Kadsura coccinea group (2.5 g·kg-1 ) and high-dose Kadsura coccinea group (5 g·kg-1 ) (n=12). All groups except the normal control group were treated with CCl4, rich fat and poor protein to establishexperimental hepatic fibrosis animal model. The second day after modeling, drug treatmentwas started, till the end of the sixth week. Pathological section of the rat’s liver was examined in order to observe its tissue under a optical microscope. Liver tissues were taken to examine the degree of liver fibrosis by HE and Masson staining, and the expression of Bcl-2, Bax and PCNA protein were detected by immunohistochemistry. Results Kadsura coccinea relieved the degree of necrosis of liver cells, liver fat’s degeneration and collagen fiber hyperplasia significantly. Compared with the model control group, expression of Bax in low-,high-dose Kadsura coccinea group and colchicine group were significantly decreased, and the expression of PCNA in hepatic fibrosis rats were enhanced(P<0.05 or P<0.01). Conclusion Kadsura coccinea has a certain inhibitory effects on experimental hepatic fibrosis in rats, and its mechanism may be related to inhibiting the expression of Bax protein and promoting the expression of PCNA protein in liver tissues.
Objective To investigate the effect of baicalin on CT26.WT cells of colon cancer in mice, and to discuss the cell death form. Methods CT26.WT cells were divided into four groups including of control group , routine cultured in fresh medium, the baicalin group, added with concentration of 100 μmol·L-1 baicalin,the z-VAD-fmk group,was added with final concentration of 20 μmol·L-1 z-VAD-fmk, and the combination group, added final concentration of 20 μmol·L-1 z-VAD-fmk,1 h before adding 100 μmol·L-1 baicalin. Then the inhibitory effect of baicalin on cell proliferation and cell viability were detected by CCK-8 method. The changes of nucleus were detected by DAPI staining, the ultrastructure of cells was observed by TEM, and the effect of baicalin on the expression of RIP3 gene and protein in cells was detected by QPCR method and Western blotting. Results Compared with control group, the differences of baicalin group and combination group had statistically significance (P<0.05). cell death rate for control group was (10.54±0.19)% ,for baicalin group was (34.93±0.16) % ,for z-VAD group was (11.23±0.59)%, and combination group was (23.27±1.20)% (P<0.01). Compared with the normal control group, baicalin group showed nuclear concentration and fragmentation. there was obvious nuclear fragmentation in the combination group against baicalin group. The results of electron microscopy showed that the cells of baicalin were necrotic, cell swelling, mitochondria swelling and contents leaking. Baicalin group significantly up-regulated RIP3 mRNA expression(P<0.01)and enhanced RIP3 protein expression (P<0.05). Conclusion Baicalin induces the necrosis of ct26.WT cells, and can significantly increase the gene and protein expression of RIP3.
Objective To investigate the effects of disulfiram combined with copper (DSF/Cu) on proliferation and migration of brain metastases from lung cancer. Methods The cell were divided into blank control group, valproate group(1.0 mmol·L-1 of valproate), DSF/Cu (1,2,3,4,5 mg/0.17 mg). Brain metastases from lung adenocarcinoma were incubated 72 hours.The changes of proliferative ability of cancer cells were detected by CCK-8 method, the effect of DSF/Cu on the migration ability of cancer cells was detected by Transwell chamber, and the degree of apoptosis of cancer cells was detected by Annexus V-PI double staining method. Results The ability of proliferation was significantly inhibited, the ability of migration was significantly reduced,and the rate of cell apoptosis was significantly increased in each dose group of brain metastases from lung adenocarcinoma compared with the blank control group.With the increase of DSF/Cu dose, its ability to inhibit the proliferation and migration of metastases cancer cells and induce apoptosis of metastases cancer cells has increased gradually. Conclusion DSF/Cu can inhibit the proliferation and migration of brain metastases from lung adenocarcinoma and induce apoptosis. DSF is expected to be a new method of the combined treatment of brain metastases cancer.
Polymorphism of chemical drugs has become a hot topic in pharmaceutical research at home and abroad. In this review, the phenomena, causes and significance of polymorphism were introduced briefly. The international drug development process and characteristics of the polymorphic drug development in our country were analyzed. Finally, the present situation and development in China was summarized from four aspects including the basic theory, technical methods, intellectual property rights and supervision. This paper can provide a reference for correct understanding the research level of polymorphic drugs in China and clarifying the direction of polymorphic drug research.
Objective To study the gastrointestinal absorption process of three letrozole polymorphs in rats, and evaluate the different pharmacokinetics parameters of different polymorphs. Methods A total of 18 SD rats were given the different letrozole polymorphs. Then the high-performance liquid chromatographic method was used for the determination of plasma concentration of letrozole in these SD rats.Finally the pharmacokinetic parameters among the different polymorphs were calculated. Results Cmax of letrozole crystal form I, crystal form II and crystal form III were (9.247±4.612), (23.387±9.049) and (15.682±1.589) mg·L-1, respectively, and AUC0→t were(198.115±47.014), (476.641±125.467) and (271.817±41.068) mg·L-1·h,respectively. Conclusion The different crystal forms of letrozole result in different plasma concentration in SD rats. Crystal form II may be its preponderant polymorphs which deserves further research and development.
The pharmaceutical co-crystal has attracted a lot of attention in recent years as a new direction in the research of polymorphism drugs. The research on pharmaceutical co-crystal has scientific significance for improving the solubility, bioavailability and physical or chemical stability of drugs. In this paper, from the perspective of drugs for the treatment of cardiovascular diseases(including five major types: heart failure, hypertension, coronary heart disease and arrhythmia, stroke), the latest research results of pharmaceutical co-crystal reported in recent years are reviewed, hope to provide reference for the follow-up research and promote the development of pharmaceutical co-crystal in China.
Objective According to the clinical medicinal crystal form——form γ of levonorgestrel, to establish the quantitative analysis method for levonorgestrel form γ by powder X-ray diffraction (PXRD). Methods Firstly, single crystal X-ray diffractometry and powder X-ray diffractometry were used to confirm that the prepared levonorgestrel form γ was 100% polymorphic purity, which provided a standard sample for quantitative analysis by single peak method; then, the standard samples of different quality levonorgestrel form γ for powder X-ray diffraction were weighed, the peak intensity values of characteristic diffraction peaks d=6.4 $\mathring{A}$, d=6.1 $\mathring{A}$ and d=5.6 $\mathring{A}$ of form γ as quantitative parameters selected, a linear relationship between the peak intensity value and the quality of form γ was established;finally, the content of levonorgestrel form γ was quantitatively analyzed. Results The peak intensity values of characteristic diffraction peaks d=6.4 $\mathring{A}$, d=6.1 $\mathring{A}$ and d=5.6 $\mathring{A}$ of levonorgestrel form γ and the quality showed a good linear relationship.In the range of form γ masses of 5 mg to 50 mg, the regression linear equations wereY=459.59X+5 536.5, R2=0.993 0, Y=430.03X+6 867.6, R2=0.990 5,Y=615.95X+6 209.5, R2=0.990 8,respectively. Conclusion The method is simple, rapid, accurate and reliable, it can be used as quality control method for levonorgestrel polymorphs.
Different polymorphs of drugs have different molecular arrangements or molecular forces. Raman spectroscopy can reflect the change of molecular polarizability and can be used for the detection of drug polymorphs. The technology has been recorded for the analysis of polymorphism in European Pharmacacopoeia, British Pharamacopoeia and Chinese pharmacopoeia. This review focuses on the application of Raman spectroscopy in the study of pharmaceutical polymorphism. The advances in Raman spectroscopy in the qualitative, quantitative and dynamic processes of drug polymorphism are summarized and analyzed systematically, aiming to provide reference for researchers in related fields.
Dihydropyridine (DHP) calcium channel blockers drugs (dipine in drug names) are currently used in the treatment of hypertension clinically. In recent years, with the emergence of generic drugs, it has been found that the drug efficacy is quite different from that of the original drug, and the reason is closely related to the difference in the crystal forms of the oral preparations. This paper reviews the polymorphic phenomenon of some DHP calcium channel blockers in the domestic market, introduces the clinical application and research progress of the DHP drugs, analyzes the differences between different crystal forms of the same drugs. This work may provide references and ideas for the research and development of generic drugs or new crystalline drug of DHP drugs.
Objective To study the mangiferin absorption process of mangiferin polymorphs in SD rats thus to find out the optimal crystal form and explore the factors that may affect the clinical effects of mangiferin. Methods Each rat was given one of three crystal forms of mangiferin. Plasma concentration of mangiferin were determined by HPLC-MS method. After liquid-liquid extraction by ethyl acetate, the chromatographic separation was carried out on an Agilent ZORBAX SB-C18 (2.1 mm×100 mm,3.5 μm) with a mobile phase consisting of methanol-0.1% formic acid aqueous solution (30:70). Mass spectrometry were performed in positive ion mode. Ion mass-to-charge ratio was set at 445 and 447 for mangiferin and, cefuroxime sodium (internal standard) respectivel for quantitive analysis. Results The main pharmacokinetic parameters of mangiferin form II, Ⅴ, Ⅵ were as follows:AUC(0-24 h)were (1323.27±218.07),(1974.34±469.24),(1737.79±623.06) ng·mL-1·h,respectively; Cmax were (321.92±85.18),(455.83±277.07),(319.92±86.07) μg·L-1, respectively; tmax were (0.70±0.45),(0.50±0.32),(0.50±0.34) h, respectively; t1/2z were (2.78±1.72),(5.29±2.67),(5.31±2.82) h, respectively. Conclusion The main pharmacokinetic parameters of mangiferin polymorphs in plasma of rats are different, and mangiferin form Ⅴ has the hightest AUC(0-24 h) and Cmax.
Objective To observe the effect of combination use of tramadol and ketorolac tromethamine for patient-controlled intravenous analgesia (PCIA) after gynecological laparoscopic surgery. Methods Ninety patients with American Society of Anesthesiologists (ASA) grade I or Ⅱ undergoing gynecological laparoscopic surgery under general anesthesia were randomly divided into three groups: group T (using tramadol for PCIA),group TK (using tramadol and ketorolac tromethamine for PCIA) and group K (using ketorolac tromethamine for PCIA). The visual analog scale (VAS) scores at rest and moving and Ramsay sedation scale(Ramsay) scores were recorded at 1 h (t1),4 h (t2),8 h (t3),12 h (t4),24 h (t5),36 h (t6),48 h (t7) after surgery.The total dosage of rescue analgesia drug and the times of needing rescue analgesia were recorded. Adverse reactions were also recorded. Results VAS scores at rest in t1,t2,t3,t4,t5 and t6 after surgery were significantly lower in group T and group TK than in group K(P<0.05). VAS scores at movement time was not significantly different. After surgery,incidence rate of nausea,vomiting,dizziness or sleepiness was significantly higher in group T than in group TK and group K(P<0.05). The total dosage of rescue analgesia drug in group K was significantly higher than in group T and in group TK (P<0.05). In 24 h after surgery,patients pressed the button of PCIA (2.89±0.597) times in group TK,(3.05±0.574) times in group T,(6.50±0.859) times in group K.Ramsay scores at each time points after surgery were significantly increased (P<0.05). Total dosage amount of rescue drugs and number of patients using rescue drugs were significantly higher in group K than in group T and group TK (P<0.05). Conclusion Combination use of tramadol and ketorolac tromethamine for PCIA after gynecological laparoscopic surgery has better analgesia effect with reduced side effects.
Objective To investigate the effect of eptazocine hydrobromide on emergence agitation (EA) of patients undergoing video-assisted thoracoscopic surgery at recovery period. Methods One hundred and twenty patients with ASA I or II,scheduled to undergo video-assisted thoracoscopic surgery vats under general anesthesia,were randomly allocated to three groups(n=40): eptazocine hydrobromide injection group (group E),dezocine injection group (group D) and sodium chloride injection group (group NS). Eptazocine hydrobromide injection 0.3 mg·kg-1,dezocine injection 0.1 mg·kg-1 and sodium chloride injectionin equal volume were administrated to group E,group D and group NS,respectively,15 min before the termination of surgery. The operation time,awakening time,extubation time and postanesthesia care unit (PACU) staying time of all patients were recorded. Riker sedation-agitation scores,MAP and HR were documented at the time of awakening (t0) and 10 min (t1),20 min (t2) and 30 min (t3) after awakening,and the incidence of EA was also recorded. Results There were no significant differences in operation time,awakening time,extubation time,PACU staying time among three groups(P>0.05). Compared with the group NS,the riker sedation-agitation scores and MAP in group E and D at t0-t3 were lower,as well as the incidence of EA. HR of group E was lower at t1-t3,while HR of group D was lower at t2 and t3(P<0.05). Compared with group D,riker sedation-agitation scores and MAPs in group E were lower at t1 and t2,while HR was lower at t2(P<0.05). However,there was no difference in incidence of EA between group D and group E (P>0.05). Conclusion Administration 0.3 mg·kg-1 eptazocine hydrobromide,15 min before the termination of surgery,could effectively reduce the incidence of EA in patients undergoing video-assisted thoracoscopic surgery after general anesthesia. Simultaneously,awakening time,extubation time and PACU staying time could not prolonged.
Objective To study the effect of small doses of remifentanil in preventing cardiovascular responses to extubation in the operation of obstructive sleep apnea hypoventilation syndrome(OSAHS). Methods Eighty patients with snoring under general anesthesia were selected. The patients were randomly divided into treatment group and control group with 40 cases in each group. The two groups used the same induction anaesthetics, and sevoflurane and remifentanil were used in both groups for anesthesia maintainance. The control group discontinued all anesthetics at the end of surgery;The treatment group stopped sevoflurane alone, and decreased and continued the infusion of remifentanil until extubation. The changes of heart rate, systolic blood pressure, diastolic blood pressure and oxygen saturation before anesthesia (t1), extubation (t2), 5 min after extubation (t3), 10 min after extubation (t4) and 15 min after extubation (t5) were recorded. Recovery indexesand adverse reactions of anesthesia were recorded. Results The heart rate, systolic blood pressure, diastolic blood pressure were significantly increased at t2, t3, t4 and t5in the two groups (P<0.05). SpO2 in all time intervals after extubation was slightly decreased, but the difference was not statistically significant (P>0.05).No significant differences were found between the two groups in the recovery time of spontaneous respiration, extubation time and the time returning to the ward (P>0.05). The incidence of adverse reactions was significantly lower in the treatment group (7.5%) than in the control group (30.0%) (P<0.05). Conclusion Small doses of remifentanil can effectively prevent the cardiovascular responses during extubation in OSAHS operations, reduce the adverse reactions and increase the safety of extubation.
Through summarizing and analyzing a large number of documents and reports of large academic conferences in China, the current situation and the prospect of individualized drug delivery model were analyzed based on folate metabolic gene in pharmaceutical care. Folate metabolic genemethylenetetrahydrofolate reductase (MTHFR) C677T and methionine synthase reductase (MTRR) A66G were related with development of multiple diseases. Its polymorphism guidesindividualized drug administrationto increase the efficacy of drugs or decrease adverse effects.
Objective To establish limit test method of camphor in Niuhuang qingxin pills (prescription of the bureau). Methods The separation was performed on an HP-INNOWAX capillary column (0.25 mm×30 m,0.25 μm) and the column temperature was 110 ℃. The temperatures of the inlet and the FID detector were 200 and 230 ℃, respectively. The flow rate of the carrier gas was 1.8 mL·min-1 and the split ratio was 10:1. The injection volume was 1 μL. Results Good linearity was obtained for camphor within the range of 1.65 to 165 μg·mL-1, and the average recovery of low,medium,high concentration were 99.12%, 99.56% and 99.56%, respectively,with RSD were 1.01%,0.69% and 0.38%, respectively. Trace camphor was found in 7 samples out of 38 samples from 9 manufactures. Conclusion The proposed method was accurate, sensitive and simple, and was suitable for quality evaluation and safety control of Niuhuang qingxin pills (prescription of the bureau).
Objective To modify polyethyleneimine (PEI) by using Poloxamer 188 (P188), and evaluate its related feature as carriers of genes in vitro. Methods PEI was modified through conjugating one hydroxyl group of P188 to the amino group of PEI by carbonate method. Structural analysis of synthesized polymer was performed by using 1H-NMR. The particle size and Zeta potential of synthesized polymer/DNA complexes were measured. The cytotoxicity of the complexes was evaluated using MTT method in MCF-7 cells, HeLa cells and HepG2 cells. The pGL3-lus was used as a reporter gene, and the transfection efficiency of complexesat HeLa cells was evalutated by measuring activity of luciferase. Results The result of 1H-NMR showed the purity of these synthesized polymers was high. The particle size of complexes were decreased with the increment of N/P ratios. The Zeta potential of complexes increased with the increment of N/P ratios. The cytotoxicity of the complexes increased with the increment of N/P ratios. The synthesized polymers showed lower cytotoxicity than unmodified PEI. The new synthesized polymers had maintained the high transfection efficiency at high N/P ratios. In particular, the optimal transfection efficiency of (P188)1-PEI (N/P=24) was significantly higher than that of PEI (N/P=6). Conclusion The P188 modifed PEI can serve as a effective non-viral gene carriers to transfect Hela cells.
Objective To analyze the prescription regularity of Chinese herbs in the treatment of cancer-related fatigue by TCM inheritance platform system software. Methods A total of documents on treating cancer-related fatigue by Chinese herbs were collected in CNKI database, Wanfang database, VIP database, CBM database from 1999 to 2017. According to the inclusion and exclusion criteria, the eligible prescriptions were selected to establish the database for summing up and analysing prescription regularity. Results A total of 33 articles were included in the analysis of 38 prescriptions, involving 108 kinds of Chinese herbs, of which the most common kinds were hot nature herb, sweetish taste, spleen meridian. Atractylodes, Poria, Licorice, Astragalus, Angelica, Tangerine peel, Codonopsis,Rehmannia had a high frequency of usage. It eventually formed 45 commonly used drug models, evolved into 16 core combinations of 3 to 4 herbs, and clustered into 5 new prescriptions. Conclusion The modern Chinese medicine in treatment of cancer-related fatigue is mainly focused on the spleen and kidney, what’s more, according to the unique nature of cancer treatment, more experts emphasize on the regulation of spleen and stomach function, which provides a useful reference for clinical syndrome differentiation and treatment.
Objective To improve the accuracy of prescription checking and provide reference for rational drug administration. Methods Intervention mistakes exsisting in prescription checking in 2016 were retrospectively studied to analyze pharmacist’s misunderstanding during prescription checking. Results The error rate of prescription intervention was higher in department of cardiology, department of general internal medicine and department of neurology, accounting for 0.6%, 0.24% and 0.23%, respectively.Inaccurate prescriptions for intervention, inaccurate medication and inaccurate repeat injections ranked the top 3 of erroneous prescriptions, with the proportions of 25.11%, 22.98% and 17.45%, respectively. Conclusion Pharmacists should regularly summarize the misconceptions existed in the prescription audit, take individualized medication thoughts as guidance, strengthen the multi-disciplinary knowledge learning.
Objective To establish a real-time monitoring system for hospital special drugs based on internet of things. Methods According to the regulations of special drug administration, combining with the internet of things technology, real-time management of drugs in terms of purchasing, receiving, using and reporting loss recovery were realized. Results After the special drug management system was used, intelligent management of drug use, inventory supervision, application management and prescription audit was realized. Conclusion Establishnment of special medical institutions and drug dynamic supervision information platform and system can realize the whole process of the traceability management, not only improving the work efficiency, also improving the drug safety and management level.
