Objective:To prepare nevirapine nanosuspensions ( Nev-NS) and study the pharmacokinetics in rats. Methods:Nev-NS was prepared by a high pressure homogenization technology. The particle size, PDI and Zeta potential of the nanosuspensions were used as the indices to determine the influencing factors in the preparation process. Nevirapine plasma concentration was detected by HPLC and the pharmacokinetic parameters were calculated by 3P97 software. Results: The particle size, PDI and Zeta potential of Nev-NS was (456. 1 ± 72. 1) nm, 0. 441 ± 0. 072 and ( -24. 4 ± 4. 7) mV, respectively. AUC0-12 of Nev and Nev-NS was (7. 57 ± 0.52) and (11.72 ±1.83) mg·h·L-1, t1/2 was (2.45 ±0.31) and (3.16 ±0.39) h, Tmax was (1.43 ±0.38) and (1.61 ± 0. 32) h and Cmax was (1. 62 ± 0. 42) and (3. 15 ± 0. 52) mg·L-1 , respectively. Conclusion:Nev-NS can improve the pharmacoki-netic behavior of Nev in rats significantly, and obviously enhance the bioavailability when compared with nevirapine suspensions.

Ginseng and its effective components are famous for their influence to enhance human immunity, regulate endocrine and antioxidant action. However, the different effects of different components are not clear. In this study, Wistar rats were used to study the effects of main components of ginseng, including total ginsenoside, panaxadiol saponins, panaxtrol saponin and ginseng polysaccharide. The results showed that the effects of panaxadiol saponins and ginseng polysaccharide on improving animal immune organ weight, plasma interleukin 2 (IL-2), interleukin 6 (IL-6), plasma gamma-interferon (IFN-γ), tumor necrosis factor alpha (TNF-α) were better than that of the other groups. Total ginsenoside and panaxtrol saponin can effectively increase the concentration of spleen NK cells (NKC) while panaxadiol saponins and ginseng polysaccharide can significantly increase the concentrations of rat plasma adrenocorticotrophic hormone (ACTH), corticosterone (CORT) and thyroid stimulating hormone (TSH). As for the effect of increasing organization nitric oxide (NO) and superoxide dismutase (SOD), glutathione (GSH) and malondialdehyde (MDA), total ginsenoside is better than that of other groups. In brief, different components in ginseng possess different effects on enhancing immunity, regulating endocrine and resisting oxidation. Panaxadiol saponins and ginseng polysaccharide are better in enhancing immune, and total ginsenoside shows advantages in resisting oxidation and stress.
Adrenal Glands ; drug effects ; growth & development ; Adrenocorticotropic Hormone ; blood ; Animals ; Brain ; drug effects ; metabolism ; Corticosterone ; blood ; Ginsenosides ; pharmacology ; Glutathione ; metabolism ; Immune System ; drug effects ; physiology ; Interferon-gamma ; blood ; Interleukin-2 ; blood ; Interleukin-6 ; blood ; Killer Cells, Natural ; drug effects ; Malondialdehyde ; metabolism ; Nitric Oxide ; metabolism ; Organ Size ; drug effects ; Panax ; chemistry ; Polysaccharides ; pharmacology ; Random Allocation ; Rats, Wistar ; Saponins ; pharmacology ; Spleen ; drug effects ; growth & development ; Superoxide Dismutase ; metabolism ; Thymus Gland ; drug effects ; growth & development ; Thyrotropin ; blood

Resistance is one of the most important reasons that restrict the clinical application of most chemotherapeutic medicines. Docetaxel is a very widely applicated antitumor medicine. Most of the researches on the mechanism of resistance against docetaxel focused on the drug transporters, changes in drug metabolism and pathway alteration of cell cycle and apoptnsis. The mechanism of docetaxel resistance and the predictive data based on clinical research to docetaxel therapy in cancer treatment were reviewed.

Objective To determine the ED50 of remifentanil needed for tracheal intubation without neuromuscular relaxant in children when combined with sevoflurane inhalation.Methods Twenty-five ASA Ⅰ or Ⅱ children of both sexes,aged 4-9 yr,scheduled for elective surgery under general anesthesia were enrolled in this study.Anesthesia was induced with inhalation of 5% sevoflurane in 100% oxygen and PETCOM2was maintained at 30-35 mm Hg.Remifentanil was injected intravenously over 30 s after 3 min inhalation of sevoflurane.Tracheal intubation was performed 90 s after the completion of remifentanil injection.The experiment was performed using the modified Dixon's up-and-down method.The initial dose of remifentanil was set at 1.2 μg/kg and the ratio between two successive doses was 1.2.Intubation conditions were assessed by a blinded observer using Viby-Mogensen scale.If the conditions were not good,roenronium 0.3 mg/kg was then injected intravenously to facilitate intubation.The ED50 of remifentanil and 95% confidence interval (95% CI) were calculated.Results The ED50 of remifentanil combined with inhalation of scvoflurane required for successful intubation was 0.68 μg/kg in the absence of neuromuscular relaxant,and 95% CI was 0.65-0.71 μg/kg.Conclusion The ED50 of remifentanil required for tracheal intubatiun without neuromuscular relaxant drug is 0.68 μg/kg (95% CI 0.65-0.71 μg/kg) when combined with 5% sevoflurane inhalation in children.

AIM: To study the suitable conditions of the extraction-separation process of the indirubin in Folium Isatidis with NIR. METHODS: The indirubin was chromatographed on an aluminium oxide column and chloroform-ethyl acetate as eluting agent,eluate was recrystalized by methanol-acetone. RESULTS: The indirubin extracted by this method was of high purity (97.78%).The sample purity was similar to reference substance one((98.01%)).The spectra of NMR and IR are the same. CONCLUSION: This method is proved to be fast,safe,lower cost,simple and has good results.

Due to its effect of systems regulation and promotion on body, Ginseng is always referred to be long-term used as a dietary supplement. But it was still unclear about its target of the tonic effects and also the side-effects long-term use may bring. Urine metabolomic method is suitable for long-term studies of pharmaco-dynamics, pharmacology and toxicology of traditional Chinese medicine because of its characteristics of non-invasive and monitoring the whole-body metabolism. This study was designed to detect the dynamic variation of rat urine metabolome along with a long-term administration of total ginsenosides using GC-TOF based metabolomic technology. Our result showed that either short-term or chronic administration of ginsenosides did not impact the rat urine metabolome significantly (as the PCA subgroup was not successful). By comparison, the short-term (1-3 w) dose of ginsenosides had the biggest metabolic influence including TCA cycle, catecholamines and neurotransmitter amino acids. Medium-term (6-10 w) dose had a gradually lower effect and long-term (27 w) dose almost had no effect. Our study indicates that both short and long-term administration of ginsenosides showed almost no obvious side-effect on the experimental animals.
Animals ; Drugs, Chinese Herbal ; metabolism ; Ginsenosides ; metabolism ; urine ; Male ; Metabolomics ; Panax ; metabolism ; Rats ; Rats, Wistar ; Time Factors

There are many different kinds of drugs which can treat ischemic stroke. This study aims to analyze the clinical treatment of ischemic stroke using Chinese and western medicines and their combination scheme. Data abstracted from 15 national 3a grad hospitals' hospital information system (HIS) databases were collected, then were used frequencies to find the common used drug and type, and were used association rules to anylizs the common combined medication scheme of Chinese and western medicines. It was found that the Shuxuetong (9 015 cases, 22.66%), Danhong (7 369 cases,18.53%) and Xueshuaitong (5 302 cases,13.33%) injections were the most frequently used drugs, and blood-activating and stasis-dissolving prescription (30 384 cases, 76.39%), resuscitative prescription (6 850 cases,17.22%) and tonic prescription (5 997 cases,15.08%) were the most commonly used types of Chinese medicine. The oral dose of aspirin (20 924 cases, 52.60%), Guangxi pp injection (10 771 cases, 27.08%) and insulin injection (10 599 cases, 26.65%) were frequently used. And the types of antiplatelet agents (23 049 cases, 57.95%), vasodilator (19 608 cases, 59.29%) and antihypertensive drug (15 475 cases, 39.90%) were commonly used. The drug combination of aspirin, twenty five pearl pill, Danhong and Xueshuaitong injection were the most frequently used group and its confidence coefficient is 97.5%. The type combination of blood-activating and stasis-dissolving prescription, thrombolytic drug, insulin and vasodilator was the most commonly used group and its confidence coefficient is 97.424%. This study concludes that the drug combination of aspirin, twenty five pearl pill, Danhong and Xueshuaitong injection and the type combination of blood-activating and stasis-dissolving prescription, thrombolytic drug, insulin and vasodilator were commonly used in clinical.
Adult ; Aged ; Aged, 80 and over ; Aspirin ; therapeutic use ; Drug Combinations ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Fibrinolytic Agents ; therapeutic use ; Humans ; Insulin ; therapeutic use ; Male ; Middle Aged ; Platelet Aggregation Inhibitors ; therapeutic use ; Stroke ; drug therapy ; Vasodilator Agents ; therapeutic use

Objective To evaluate the reliability of Amsterdam Preoperative Anxiety and Information Scale (APAIS) score in evaluating the preoperative anxiety of Chinese people.Methods One hundred sixty Chinese patients of both sexes, aged 18-60 yr, of American Society of Anesthesiologists physical status Ⅰ-Ⅲ, scheduled for elective surgery, were enrolled.Preoperative anxiety of the patients was assessed with APAIS score and Spielberger's State-Anxiety Inventory (S-AI) questionnaire during the preoperative interview.Cronbach's alpha of total anxiety and need for information scores was calculated.Four thresholds of total anxiety score in identifying preoperative severe anxiety was set as 10, 11, 12 and 13.S-AI questionnaire was considered as the standard, and the correlation between total anxiety score and S-AI questionaire was tested.Results The Cronbach's alpha of total anxiety and need for information scores was 0.84 and 0.71, respectively.When the threshold of total anxiety score in identifying preoperative severe anxiety was 12, the total anxiety score was highly correlated with S-AI questionnaire, the Kappa value was 0.62, 95％ confidence interval was 0.46-0.78, the sensitivity was 0.71, the specificity was 0.90, and the positive predictive value was 0.78.Conclusion APAIS score can be used to assess the preoperative anxiety of Chinese people.

Abstract: Fifteen novel ligustrazine-tetrahydroisoquinoline derivatives were designed and synthesized according to the association principle of pharmaceutical chemistry. The structures were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by ADP and AA have been measured by Bron method. Preliminary pharmacological results showed that compounds 7g, 7h and 7n had potent inhibitory activity against platelet aggregation induced by AA, and the compound 7o showed significant inhibitory activity against platelet aggregation induced by ADP.
Drug Design ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; Pyrazines ; chemical synthesis ; chemistry ; Tetrahydroisoquinolines ; chemical synthesis ; chemistry

Objective To evaluate the effect of injection of ozone (O3) through lateral recess for the treatment of radiculitis caused by lumbar disc herniation on the blood glucose in patients with diabetes mellitus.Methods Ninety-six patients with radiculitis caused by lumbar disc herniation involving 48 patients with diabetes mellitus and 48 patients without diabetes mellitus were enrolled in the study.The diabetic or non-diabetic patients were randomly divided into 2 groups ( n =24 each):non-diabetic patients-O3 group (group N-O3 ),non-diabetic patients-ghcocorticoid group (group N-GC),diabetic patients-O3 group (group D-O3 ),and diabetic patients-glucocorticoid group (group D-GC).In N-O3 and D-O3 groups,30 mg/L O3 10 ml was injected via the lateral recess.In N-GC and D-GC groups,compound betamethasone injection 3.5 mg was injected via the lateral recess.The blood glucose level was measured before treatment (T1),1 and 4 h after treatment (T3,4),and 1,3 and 7 days after treatment (T5-7).VAS score was recorded at T1,immediately after treatment (T2),and at T5-7.The patients' quality of life was measured using the Medical Outcomes Study 36-Item Short-Form Health Survey (MOS SF-36 Health Survey) questionnaire at T1,7.The therapeutic effect was evaluated at T7.The side effects were recorded.Results Compared with the baseline value at T1,VAS scores were significantly decreased after treatment,while the MOS SF-36 Health Survey questionnaire scores for physical functioning,bodily pain,role emotional,and mental health in all groups,for general health in group N-GC,and for vitality in groups D-O3 and N-O3 were significantly increased at T7,and the blood glucose level was significantly increased at T4 in groups N-GC and D-O3,and at T3-7 in group D-GC ( P ＜ 0.05).There was no significant change in the blood glucose level before and after treatment in group N-O3.The blood glucose level was significantly higher in group N-GC than in group N-O3,and in group D-GC than in group D-O3 ( P ＜ 0.05).There were no significant differences in the excellent and good rates and all the MOS SF-36 Health Survey questionnaire scores among all groups.No side effects were found in the study.Conclusion Injection of ozone through lateral recess for treatment of radiculitis caused by lumbar disc herniation exerts no influence on the blood glucose level in patients with diabetes mellitus.