1.Progress on anti-asthma agents targeted for cytokine
Xinjun CAI ; Xiangcai ZHANG ; Yingying XU
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(03):-
Several cytokines which play key role in asthma patients with chronic inflammation and reconstruction of air duct,are important targets for anti-asthma agents.In this review,we summarize the latest advancement of anti-asthma agents which targeted for cytokines(interleukins,TNF,eotaxin)and investigation development of new anti-asthma agents emerged in recent years.
2.The brain pharmacokinetical study of different diameters neurotoxin-Ⅰ nanoparticles after intranasal administration in rats
Qiang BAO ; Xinjun CAI ; Fanzhu LI
Chinese Pharmacological Bulletin 1986;0(06):-
Aim To prepare NT-Ⅰ loaded nanoparticles with different diameters modified by Methylated-polyethyleneglycol (Me-PEG) and evaluate their brain pharmacokinetics after administered nasally in rats. Methods NT-Ⅰ-NP was prepared by emulsion/solvent evaporation method and MePEG-PLA was used as the carrier material. Microdialysis technique and fluorospectrophotometry were used to determine NT-Ⅰ concentration after nasal administration in the brain of rats. Results The appearance of all NT-Ⅰ-NP groups was round or similar. The AUC(0-t) of below 100 nm NT-Ⅰ-NP was 1.22 fold as that of 100~200 nm NT-Ⅰ-NP,1.34 fold as that of 200~300 nm and 1.60 fold as that of exceed 300 nm NT-Ⅰ-NP(P
3.Determination of Norcantharidin in Norcantharidin in situ Gel by HPLC
Yujie HU ; Feng ZHOU ; Xinjun CAI
China Pharmacist 2016;19(6):1196-1197
Objective: To establish a method for the determination of norcantharidin in norcantharidin in situ gel .Methods:An optimal HPLC method was set up and an Agilent ZORBAX SB-C18 column (150 mm ×4.6 mm, 5μm) was adopted.The mobile phase was acetonitrile-phosphate buffer solution(1∶9, adjusting pH to 3.1 with phosphorjc acid).The flow rate was 0.8 ml· min-1 and the column temperature was 25℃.The detection wavelength was set at 210 nm and the injection volume was 20μl.Results:Norcanthari-din had a good linear relationship within the range of 0.02-1.00 mg· ml-1 (r=0.999 9).The average recovery was 97.5%and RSD was 0.98%(n=9).Conclusion:The method is accurate, simple and reproducible, which can be used for the determination of nor-cantharidin in norcantharidin in situ gel .
4.Analysis of correlated risk factors in evolving cerebral infarction
Xinjun MIAO ; Pingping CAI ; Guodong YUAN
Chinese Journal of Practical Internal Medicine 2001;0(10):-
Objective To analyse correlated risk factors of evolving cerebral infarction(ECI).Methods The follow data was recorded in the acute cerebral infarction (ACI)cases when they were admitted :sex,age,systolic blood pressure(SBP),diastolic blood pressure(DBP),history of disease (diabetes mellitus,hypertension,hyperlipidaemia,cerebral infarction,hyperuricemia or smoking).The following examinations or determinations were done,including:white blood cell count (WBC),platelet count (PLT),blood gluconate(GLU),PT-INR,fibrinogen(FG),TT-INR,APTT-INR,C-reactive protein(CRP),D-dimer(D-D),products of fibrin degradation(FDP),anti-thrombin Ⅲ(ATⅢ),apolipoprotein A(apoA),apolipoprotein B(apoB),blood urea nitrogen(BUN),creatinine(CR),triglyceride (TG),high density lipoprotein (HDL),low density lipoprotein (LDL),very low density lipoprotein (VLDL),GOT,lactate dehydrogenase(LDH),creatine phosphokinase (CPK),MB isoforms of creatine phosphokinase (CPK-MB),? hydroxybutyrate dehydrogenase (?-HBDH),troponin I(TnI),cerebral CT or MRI and carotid ultrasonography.The patients were divided into two groups,ECI and completed cerebral infarction (CCI),according whether neurons function scale deteriorated.When cases of both groups exceeded 50,we took statistic test by SPSS10.0 statistic software.Results 8 of the above 46 markers had significant defference between the two groups,including CRP,WBC,apoB,GLU,LDH,CPK-MB,?-HBDH and DBP.ECI was more common in patients who had lower DBP or higher CRP,WBC,apoB,GLU,LDH,CPK-MB,?-HBDH when they were admitted.Conclusion The increase of CRP,WBC,apoB,GLU,LDH,CPK-MB,?-HBDH or decrease of DBP when patients are admitted can be predictive markers of ECI.
5.Study on Compatibility Stability of Flurbiprofen Axetil Lipid Microspheres Injection
Yuting ZHU ; Jianjun NI ; Xinjun CAI ; Yingying XU ; Feng ZHOU
China Pharmacist 2016;19(9):1781-1782
Objective:To investigate the stability of flurbiprofen axetil lipid microspheres injection combined with 0. 9% sodium chloride injection or 5% dextrose injection, and provide theoretical basis for the clinical application. Methods:The content changes of flurbiprofen axetil in the mixture of flurbiprofen axetil lipid microspheres injection and 0. 9% sodium chloride injection or 5% dextrose injection were determined in 5 h at 25℃ away from light, and the changes in the appearance and particle size of flurbiprofen axetil lip-id microspheres were investigated. The changes in the appearance and particle size of flurbiprofen axetil lipid microspheres in the mix-ture of flurbiprofen axetil lipid microspheres injection and 0. 9% sodium chloride injection before and after freezing and thawing were also investigated. Results:The appearance, particle size and content had no significant changes in all mixtures in 5 h at 25 ℃ away from light. The appearance and particle size of flurbiprofen axetil lipid microspheres in the mixture before and after freezing and thawing had no significant changes as well. Conclusion:The mixture of flurbiprofen axetil lipid microspheres injection and 0. 9% sodium chlo-ride injection or 5% dextrose injection is stable in 5 h away from light.
6.Preparation of ligustrazine-chitosan microspheres by spray drying method
Xinjun CAI ; Qiaoyuan CHENG ; Ning ZHAO ; Fanzhu LI
Chinese Traditional and Herbal Drugs 1994;0(05):-
Objective To prepare ligustrazine-chitosan microspheres and to investigate the drug release behavior in vitro. Methods Microspheres were prepared using the spray drying method.The encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors,the formulation was optimized by L9(34) orthogonal design.Results The optimal formulation and preparation factors were as follows: chitosan concentration(0.01 g/mL),ratio of chitosan to ligustrazine(1∶4),inlet temperature(120 ℃),air flow rate(500 L/h).The optimized microspheres had a spherical shape,the loading capacity was(18.60?0.15)%,entrapment efficiency was(93.01?0.76)%,the average diameter was(10.69?0.64) ?m.The drug release profile in vitro could be described by Higuchi equation Q=19.798 t1/2+25.209(r=0.997) at 1-15 h,which showed the prepared microspheres obviously had the sustained release effect.Conclusion The encapsulation efficiency of ligustrazine-chitosan microspheres is higher,the preparation method is simple,and the process is stable.It will provide the basis for realizing the industrialization in Chinese materia medica microspheres.
7.Preparation and Evaluation of Triptolide Self-microemulsifying Drug Delivery System
Jiawei CAO ; Jun FENG ; Xinjun CAI ; Jianjun NI ; Lunan GU ; Zhongyuan ZHOU
China Pharmacist 2017;20(4):638-642
Objective:To study the formula of triptolide (TRI) self-microemulsifying drug delivery system (SMEDDS) and evaluate the pharmaceutical properties.Methods:The formula and preparation process of triptolide self-microemulsion were screened by the solubility test and pseudo-ternary phase diagram.With the average particle size and self-microemulsifying time as the indices,the further formula optimization of triptolide self-microemulsion was carried out.The pharmaceutical properties of triptolide self-microemulsion were evaluated.Results:The optimal formula of TRI SMEDDS was as follows:the amount of medium chain triglycerides (MCT) was 20%,that of polyoxyethylene castor oil (EL-35) was 40%,and that of polyethylene glycol 400 (PEG-400) was 40% in the oil phase.The average particle size was 43.48 nm,and the time of self-microemulsification was less than 30 s.Conclusion:The average particle size and the appearance of triptolide self-microemulsion are accordance with the requirements of pharmaceutics.Triptolide self-microemulsion has good sustained-release effect,which lays foundation for the further study on pharmacodynamics.
8.Nasal anatomic abnormalities and bacterial infection in chronic rhino sinusitis.
Xinjun MENG ; Changping CAI ; Yuxing NI ; Shili WANG ; Jingyong SUN
Journal of Clinical Otorhinolaryngology Head and Neck Surgery 2010;24(17):779-781
OBJECTIVE:
To study the relationship between nasal anatomic abnormalities and the bacteria infection status of maxillary sinus.
METHOD:
The anatomic abnormalities of 115 cases of maxillary sinuses were detected with the CT images and confirmed with chronic infection, which were divided into two groups: high anatomic abnormality group and low anatomic abnormality group. The sinusal contents were sent to bacteria culture, compare the bacteria infection rate and the distribution of bacteria between the two groups.
RESULT:
The bacteria positive rate of the high anatomic abnormality group and low anatomic abnormality group was 90.32% and 56.60% (P < 0.01) respectively. The contribution of gram-positive bacteria and gram-negative bacteria are 47.76% and 52.24% in high anatomic abnormality group, 62.16% and 37.84% in low anatomic abnormality group.
CONCLUSION
Nasal anatomic abnormalities can improve the bacteria infectious rate of maxillary sinuses. High anatomic abnormality may more induces gram-negative bacteria infections,while low anatomic abnormality may more induces gram-positive bacteria infections.
Adult
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Aged
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Aged, 80 and over
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Bacterial Infections
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etiology
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Chronic Disease
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Humans
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Middle Aged
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Nose
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abnormalities
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Sinusitis
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microbiology
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Young Adult
9.The Combination of Gefitinib and Acetaminophen Exacerbates Hepatotoxicity via ROS-Mediated Apoptosis
Jiangxin XU ; Xiangliang HUANG ; Yourong ZHOU ; Zhifei XU ; Xinjun CAI ; Bo YANG ; Qiaojun HE ; Peihua LUO ; Hao YAN ; Jie JIN
Biomolecules & Therapeutics 2024;32(5):647-657
Gefitinib is the well-tolerated first-line treatment of non-small cell lung cancer. As it needs analgesics during oncology treatment, particularly in the context of the coronavirus disease, where patients are more susceptible to contract high fever and sore throat.This has increased the likelihood of taking both gefitinib and antipyretic analgesic acetaminophen (APAP). Given that gefitinib and APAP overdose can predispose patients to liver injury or even acute liver failure, there is a risk of severe hepatotoxicity when these two drugs are used concomitantly. However, little is known regarding their safety at therapeutic doses. This study simulated the administration of gefitinib and APAP at clinically relevant doses in an animal model and confirmed that gefitinib in combination with APAP exhibited additional hepatotoxicity. We found that gefitinib plus APAP significantly exacerbated cell death, whereas each drug by itself had little or minor effect on hepatocyte survival. Mechanistically, combination of gefitinib and APAP induces hepatocyte death via the apoptotic pathway obviously. Reactive oxygen species (ROS) generation and DNA damage accumulation are involved in hepatocyte apoptosis. Gefitinib plus APAP also promotes the expression of Kelch-like ECH-associated protein 1 (Keap1) and downregulated the antioxidant factor, Nuclear factor erythroid 2-related factor 2 (Nrf2), by inhibiting p62 expression.Taken together, this study revealed the potential ROS-mediated apoptosis-dependent hepatotoxicity effect of the combination of gefitinib and APAP, in which the p62/Keap1/Nrf2 signaling pathway participates and plays an important regulatory role.
10.The Combination of Gefitinib and Acetaminophen Exacerbates Hepatotoxicity via ROS-Mediated Apoptosis
Jiangxin XU ; Xiangliang HUANG ; Yourong ZHOU ; Zhifei XU ; Xinjun CAI ; Bo YANG ; Qiaojun HE ; Peihua LUO ; Hao YAN ; Jie JIN
Biomolecules & Therapeutics 2024;32(5):647-657
Gefitinib is the well-tolerated first-line treatment of non-small cell lung cancer. As it needs analgesics during oncology treatment, particularly in the context of the coronavirus disease, where patients are more susceptible to contract high fever and sore throat.This has increased the likelihood of taking both gefitinib and antipyretic analgesic acetaminophen (APAP). Given that gefitinib and APAP overdose can predispose patients to liver injury or even acute liver failure, there is a risk of severe hepatotoxicity when these two drugs are used concomitantly. However, little is known regarding their safety at therapeutic doses. This study simulated the administration of gefitinib and APAP at clinically relevant doses in an animal model and confirmed that gefitinib in combination with APAP exhibited additional hepatotoxicity. We found that gefitinib plus APAP significantly exacerbated cell death, whereas each drug by itself had little or minor effect on hepatocyte survival. Mechanistically, combination of gefitinib and APAP induces hepatocyte death via the apoptotic pathway obviously. Reactive oxygen species (ROS) generation and DNA damage accumulation are involved in hepatocyte apoptosis. Gefitinib plus APAP also promotes the expression of Kelch-like ECH-associated protein 1 (Keap1) and downregulated the antioxidant factor, Nuclear factor erythroid 2-related factor 2 (Nrf2), by inhibiting p62 expression.Taken together, this study revealed the potential ROS-mediated apoptosis-dependent hepatotoxicity effect of the combination of gefitinib and APAP, in which the p62/Keap1/Nrf2 signaling pathway participates and plays an important regulatory role.