Objective To build the cohort of drug resistance and analyze treatment efficiency of AIDS patients and situation of drug resistant mutations among HIV-1 infected individuals.Methods A cohort of 116 HIV-1 infected patients was built and their treatment progress were acquired once every 6 months.At the sanle time CD4+ T cell counts and HIV-1 viral load were measured and genotyping for drug resistance was determined by a home brew nested PCR.Results The CD4+ T cell count(470±251/ml)was higher than that before treatment in patients who were treated by AZT/DDI/NVP or D4T/DDL/NVP.The viral load was lower than that before treatmenL The drug resistant mutation frequency increased gradually along with treatment.The CD4+ T cell count was decreased and viral load was increased and the prevalence of drug resistant mutation was increased in the patients who changed regimens to AZT/3TC/NVP or D41/3TC/NVP.Only one primary mutation that was resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs)was detected in the naive patients.The cross-resistant mutation was detected in two patients after 6 months treatment. The intermediate resistance to lopinavir(LPV) was detected after 12 months treatment.The prevalence of high-grade resistances to NNRTIs was increased obviously,and the prevalence of multi-resistance and cross-resistance was detected in 5 patients after 36 months treatment.Conclusions The prevalence of primary mutation was rare in naive HIV-1 infected patients.The prevalence of drug resistant mutation was inereased gradually along with treatment.Ahhough few regimens were available,the treatment effect could last relatively long period of time if patients keep taking medicine stably.The regimens could be changed according to the results of drug resistant test.

Objective To research and analyze nursing measures of phlebitis caused by vein medication Amiodarone Hydrochloride. Methods 150 arrhythmias patients in the Traditional Chinese. Medicine Hospital of Wenling were selected as the subjects. The control group was given routine transfusion nursing, the experimental group was given comprehensive nursing intervention on the basis of the control group, saline irrigation before and after transfusion, observed the local reaction of patients, and controlled the concentration and external application of potato chips. Results After the corresponding nursing measures, in the control group, accounting for 46.7%. 35 cases of phlebitis occurred in the experimental group. The incidence of phlebitis in the experimental group was 16.0%, which was significantly lower than that (46.7%) in the control group, which was statistically significant (P<0.05). In the experimental group, the number of patients with I degree phlebitis was 8, and the proportion was 66.67%. In the control group, there were 7 cases of I degree phlebitis, accounting for 20%, which was statistically significant (P<0.05). In the experimental group, there were 4 cases of II degree phlebitis, the proportion was 33.33%, significantly lower than that (54.28%) of the control group (19 cases of II degree phlebitis) with statistical significance (P<0.05). Conclusion The application of comprehensive nursing measures in arrhythmia patients treated with Amiodarone Hydrochloride vein medication, could significantly reduce the occurrence of phlebitis and improve the curative effect with high safety and clinical significance.

To study the effect of alpha1-acid glycoprotein 1 (ORM1) polymorphism on the concentration of free nortriptyline in serum, genotyping analysis was employed in ORM1 by sequencing. Eighteen unrelated male adults were chosen and given a single dose of 25 mg nortriptyline orally, then the blood samples were taken at 0, 1, 2, 3, 4, 6, 8, 12, 24, 32, 48, 72, 96 and 168 hours after drug administration. Nortriptyline and 10-OH-nortriptyline in serum and ultrafiltrate were detected for the total and free concentration by using HPLC-MS/MS. Pharmacokinetic parameters were compared among different ORM1 genotypes. No significant differences were shown in the pharmacokinetic parameters of total nortriptyline and 10-OH-nortriptyline. The mean AUC(0-infinity) of free nortritpyline in ORM1 * F/ * F1 subjects was significantly higher than that in ORM1 * F1/ * S and ORM1 * S/ * S subjects [(119.1 +/- 74.4) ng x mL(-1) x h vs (51.4 +/- 23.2) ng x mL(-1) x h and (42.4 +/- 11.6) ng x mL(-1) x h]. The percentage of protein binding in subjects with ORM1 * F1/ * F1 genotype at 2, 3, 4, 6, 8 and 12 h after administration was slightly lower than in those with ORM1 * F1/ * S and ORM1 * S/ * S genotypes while the distinct difference was shown at 4 h (P < 0.05). Different ORM1 genotypes might affect the protein binding percentage and the concentration of serum free nortriptyline. The ability binding to the drug was higher in subjects with ORM1 * S/ * S genotype than in those with other two genotypes, so as to cause the lower concentration of free nortriptyline.
Adult ; Area Under Curve ; Genotype ; Humans ; Male ; Nortriptyline ; analogs & derivatives ; blood ; pharmacokinetics ; Orosomucoid ; genetics ; metabolism ; Polymorphism, Genetic ; Protein Binding

Objective: To explore the structural domains of the CENP-E protein that interact with Mps1 protein.Methods: Two recombinant vectors named pEGFP-CENPE2(containing 674-1085 amino acids of CENP-E protein) and pEGFP-CENPE 3(containing 1200~2134 amino acids of CENP-E protein) were transfected into human embryo kidney 293(HEK293) cells respectively.The respective energy transfer efficiency(Ef) between either EGFP-CENPE2 and Mps1,or EGFP-CENPE3 and Mps1 were detected by FRET through selective photobleaching of the acceptors.Results: Both recombinant proteins expressed in HEK293 cells transfected by the recombinant plasmids were found to co-localize with the Mps1 protein as confirmed by confocal microscopy.The Ef between EGFP-CENPE3 and Mps1 protein was [(12.63?0.48)%,n=30] and that between EGFP-CENPE3 and Mps1 protein was [(3.17?0.21)%,n=30] as revealed by the results from FRET,the result of FRET was confirmed by co-Immunoprecipitate(CO-IP) method.When compared with that between the control and Mps1,the Ef between EGFP-CENPE3 and Mps1 was significantly higher(p

In recent studies some urea derivatives have been identified as potent anti-tuberculosis agents by targeting mycobacterial membrane protein large 3 (MmpL3). However, this compound series as exemplified by AU1235 exhibited poor in vitro pharmacokinetic profile. With AU1235 as the lead, we have identified a novel benzimidazole series as potential anti-tuberculosis agents by using scaffold hopping approach. Among these synthesized compounds, 2-aminobenzimidazole derivative 8b showed the potent anti-tuberculosis activity with the MIC value of 0.03 microg x mL(-1). This compound also showed improved metabolic stability compared to AU1235. Our investigation indicated that benzimidazole derivatives are the promising lead for further optimization as anti-tuberculosis agents.
Antitubercular Agents ; pharmacology ; Benzimidazoles ; chemistry ; pharmacology ; Drug Design ; Humans ; Structure-Activity Relationship ; Tuberculosis ; drug therapy

OBJECTIVETo study processing method and mechanism of Calamine.

METHODThermogravimetry analysis method and nano-technology were adopted to analyze and synthesize the components in Calamine, Tetracycline was took as the comparison drug to determine the antibacterial activity of Calamine and its components.

RESULTA part of zinc carbonate in Calamine was decomposed into zinc oxide when processing, and the particle size was smaller than before. The antibacterial activity of Calamine is decided by the content and particle size of zinc oxide, and has nothing with zinc carbonate. The more content and the smaller particle size of zinc oxide, the more powerful antibacterial activity of Calamine.

CONCLUSIONThe content and the particle size of zinc oxide can be the important targets in the processing of Calamine.

Anti-Bacterial Agents ; pharmacology ; Carbonates ; chemistry ; pharmacology ; Drug Combinations ; Escherichia coli ; drug effects ; Ferric Compounds ; chemistry ; pharmacology ; Materia Medica ; chemistry ; pharmacology ; Nanostructures ; Nanotechnology ; Particle Size ; Pseudomonas aeruginosa ; drug effects ; Salmonella ; drug effects ; Staphylococcus aureus ; drug effects ; Technology, Pharmaceutical ; methods ; Tetracycline ; pharmacology ; Thermogravimetry ; Zinc Compounds ; chemistry ; pharmacology ; Zinc Oxide ; analysis ; chemistry ; pharmacology

AIMTo study the drug release mechanism of famotidine time-controlled release pellets and to explore the mechanism of "organic acid-induced type drug delivery system".

METHODSThe effects of dissociated and undissociated forms of succinic acid on the drug release behavior of famotidine time-controlled release pellets were studied from the following aspects: ion-exchange reaction, hydration, etc.

RESULTSThe dissociated succinic acid created new ionic circumstances by ion-exchange reaction with Eudragit RS100. Whereas undissociated succinic acid increased the flexibility of the film by distribution in the hydrophobic segment of Eudragit RS100. Effects of both forms of the succinic acid could improve the hydration of Eudragit RS film. As a result, the permeability of the film was improved evidently.

CONCLUSIONThe lag time of famotidine time-controlled release pellets is induced by the hydrophobicity of the film. After water dissolve the organic acid, the dissociated and undissociated forms of succinic acid interact with the film through different ways. These interactions can change the structure of the film. Therefore the permeability of the film will be improved markedly.

Acrylic Resins ; chemistry ; Anti-Ulcer Agents ; chemistry ; pharmacokinetics ; Delayed-Action Preparations ; chemistry ; pharmacokinetics ; Famotidine ; chemistry ; pharmacokinetics ; Ion Exchange ; Succinic Acid ; chemistry ; Time Factors ; Water ; chemistry

Associated with the aging of our world population is a sharp increase in the incidence of Alzheimer's disease, which not only poses a significant health issue but also presents a serious social problem. Although pharmacological treatments were developed based on existing hypotheses, the disease pathogenesis remains to be fully elucidated. Given the complexity of Alzheimer's disease, Chinese herbal medicine appears to have therapeutic potential for Alzheimer's disease through multi-target and multi-pathway approach at cellular and molecular levels and holistic adjustment of the body at organ system levels. Recently, a significant breakthrough has been made in the research of Chinese medicine for Alzheimer's disease. In this article, we review the experimental research progress in understanding how Chinese medicine could be used for the treatment of Alzheimer's disease.
Alzheimer Disease ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Phytochemicals ; therapeutic use