OBJECTIVETo establish the analytical method for the release kinetic (RK) of Aconitum Brachypodum gel based on the nonlinear mixed effect model (NLMEM), in order to rationally evaluate the drug release process and explain the release mechanism.

METHODThe zero-order kinetic model containing for non-corroded drug system with the random effect was taken as the base model. The fixed effect and random effect factors impacting the drug release were analyzed by PROC NLMIXED of SAS to establish the final typical model. Subsequently, 10 training subsets were randomly extracted from the primary data to respectively their RK models, calculate the corresponding predicted root-mean-square error and average relative error, and evaluate the model stability and prediction accuracy.

RESULTThe burst effect F0 had a very significant effect on the RK model. Among the component factors, carbopol 940 showed an obvious effect on the inherence release speed constant k0 and the concentration gradient change constant a, with different variations on the basis of dosage range. The random effect factors of k0 and a had a significant impact. The final RK model was proved to be stable, effective and reliable in the cross validation.

CONCLUSIONThe drug release kinetic analysis method could be used to rationally evaluate the drug release process and explain the release mechanisms.

Aconitum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Gels ; Kinetics ; Monte Carlo Method ; Nonlinear Dynamics

ObjectiveTo observe the protective effect of tetrahydroxystilbene glucoside (TSG) on rats' hippocampal neuronal damage induced by glutamate (Glu) in the culture.MethodsHippocampus was isolated from newborn SD rats and dispersedly cultured in the medium for 9 days. Neurons were incubated with TSG (5—100μmol/L) for 24h, the cells were washed twice with Lock's solution without Mg2+,then Glu 500 μmol/L was added. Thirty min later, the reaction was terminated by washing the monolayer cells twice with the Lock's solution and then cultures were kept at 37℃ for 24h. Cell viability was measured by MTT method and cell membrane damage was determined by LDH leakage; with Fluo-3/AM as an intracellular calcium indicator and added into the bathing medium, fluorescent intensity of intracellular free calcium were observed through laser scanning confocal microscopy (LSCM).ResultsAfter the treatment with 5—100μmol/L TSG for 24h, the decrease of cell viability and the increase of LDH leakage caused by Glu was obviously resisted dose dependently. TSG inhibited increase of Ca2+ in cytoplasm, compared with model group.ConclusionTSG can significantly promote the cell viability and reduce the cell membrane damage in Glu treating hippocampal neurons. The neuroprotective activities of TGS is mediated by inhibiting Ca2+ overload in cytoplasm.

Objective To investigate the efficacy of oxygen uptake efficiency slope (OUES) on evaluation the cardiopulmonary function of patients with chronic obstructive pulmonary disease (COPD). Methods The cardiopulmonary function of 54 stable COPD patients with the cardiopulmonary function of Ⅱ~Ⅳ were evaluated, following a symptom-limited Steep protocol with simultaneous respiratory gas measurement,they were performed exercise tests on a treadmill, simultaneously the oxygen uptake (VO2), carbon dioxide production (VCO2),peak oxygen uptake (VO2peak), minute ventilation (VE), and respiratory gas exchange rate (RER) were measured. OUES was derived from the relation between VO2 and VE during incremental exercise and was determined by VO2=algVE+b, where a=OUES, to measure anaerobic threshold (VAT) meanwhile. Results OUES correlated with the VO2peak (P<0.001). 75% OUES, 90% OUES and 100% OUES were not significantly different (F=0.239, P=0.830). Conclusion OUES can respond the cardiopulmonary function in patients with COPD, 75% OUES from sub-maximal exercise can be an index for cardiopulmonary function.

Animals ; Astragalus Plant ; chemistry ; Coxsackievirus Infections ; physiopathology ; Flavonoids ; pharmacology ; Mice ; Mice, Inbred BALB C ; Myocarditis ; physiopathology ; virology ; Myocytes, Cardiac ; drug effects ; virology

OBJECTIVETo discuss arthroscopic technique of single Kirschner wire and suture avoiding epiphyseal line fixation for tibial intercondylar eminence fracture and its clinical results.

METHODSFrom May 2008 to December 2012, 21 patients (13 males, 8 females, ranging in age from 6 to 14 years old) with tibial intercondylar eminence fracture were treated arthroscopically with single Kirschner wire and suture avoiding epiphyseal line fixation technique. According to Meyers and McKeever classification, 7 patients were type II, 10 patients were type III, and 4 patients were type IV. Active rehabilitation began at one week after operation. The patients were followed up for 10 to 30 months. X-ray films were taken to evaluate fracture healing at 1, 3, 6 months after operation; range of motion, the anterior drawer test, the lachman test and the Lysholm knee score were used to evaluate clinical effects.

RESULTSAll fractures were healed without displacement at 6 weeks after operation. Anterior drawer test and the lachman test were both negative in all patients at 3 months after operation. Lysholm knee score was 95.5 ±2.5 at 6 months after operation, and postoperative X-ray film did not find epiphyseal line broadening or narrowing.

CONCLUSIONArthroscopic treatment for tibial eminence intercondylar fracture with single Kirschner wire and 8-shaped suture avoiding epiphyseal line fixation technique has many advantages, such as firm fixation,early mobilization, less invasive, less injury of physis and satisfactory effect.

Adolescent ; Arthroscopy ; Bone Wires ; Child ; Female ; Fracture Fixation, Internal ; Humans ; Male ; Sutures ; Tibial Fractures ; surgery

OBJECTIVETo observe the expression of inducible nitric oxide synthase (iNOS) in rat dental pulp after direct pulp capping with calcium hydroxide (CH) and mineral trioxide aggregate (MTA).

METHODSSamples from 42 Wistar rats were immediately collected at 1, 3, 7, 14, 21 and 28 days after direct pulp capping with CH and MTA. Pulp tissues were studided with immunohistochemical stain. Software for image analysis was used to test the optical density of each specimen. The data were analyzed by paired t-test and Dunnett-t test with SPSS 11.5.

RESULTSIn normal pulp, the stain of iNOS was negative. After direct pulp capping with CH or MTA, iNOS expression demonstrated weakly positive, positive, weakly positive, negative at different time, the expression was low immediately after capping but became strong after 3 days. Until 7 days the stain became less positive gradually and at 21 days the stain approached normal. The expression was mainly at the fibroblasts, odontoblasts, vascular endothelial cells, neutrophils, etc near the bottom of the pulp capping agent. The diffence of iNOS expression was significant 3 days after direct pulp capping with this two capping agents.

CONCLUSIONAfter direct pulp capping, iNOS expression increasd at first and then decreased, the diffence of capping agents will have an impact on the expression of iNOS 3 days after direct pulp capping.

Aluminum Compounds ; Animals ; Calcium Compounds ; Calcium Hydroxide ; Dental Pulp ; Dental Pulp Capping ; Drug Combinations ; Nitric Oxide Synthase Type II ; Oxides ; Pulp Capping and Pulpectomy Agents ; Rats ; Rats, Wistar ; Root Canal Therapy ; Silicates

Animals ; Disease Models, Animal ; Hypoglycemia ; chemically induced ; metabolism ; Hypothalamus ; drug effects ; metabolism ; Insulin ; pharmacology ; Intracellular Signaling Peptides and Proteins ; metabolism ; Male ; Neuropeptides ; metabolism ; Orexins ; Rats ; Rats, Sprague-Dawley

OBJECTIVE: To study the tongue tissue blood oxygen saturation measurement for evaluating tongue manifestation of blood stasis syndrome, and to explore its correlation with blood rheological disorder in a rat model of acute transient brain ischemia. METHODS: Twenty-eight SD rats were randomly divided into sham-operated group and ischemia group. Middle cerebral artery occlusion was induced by thread in rats of the ischemia group. Tongue tissue blood oxygen saturation, neurological severity score and the changes of blood viscosity, red blood cell deformity, thrombin time and fibrinogen in the rats were measured after 24-hour reperfusion. RESULTS: Blood viscosity and the content of fibrinogen in the ischemia group were significantly higher than those in the sham-operated group. Red blood cell deformity, thrombin time and tongue tissue blood oxygen saturation in the ischemia group were decreased as compared with the sham-operated group. There was a positive correlation between red blood cell deformity and tongue tissue blood oxygen saturation. CONCLUSION: Tongue tissue blood oxygen saturation is a good measurement for evaluating blood stasis in a rat model of focal cerebral ischemia, and this model can be used as a rat model of stroke with blood stasis syndrome.

· AIM: To explore the effects of C3F8 tamponade on hypotony on or after primary operation and the prognosis of severe ocular trauma.· METHODS: Twenty-six cases (26 eyes) of severe ocular trauma were treated with pure C3F8 tamponade on or after primary operation. IOP was observed, and the curative effect of C3F8 tamponade was observed on secondary operation with prognosis evaluated.· RESULTS: Hypotony improved in 23 eyes postoperatively,in which 18 eyes with edematous and cloudy cornea, 15 eyes had clear cornea after gas tamponade. Retina was reattached under the gas action in 21 eyes during the secondary operation. Visual acuity improved in 22 eyes, remained unchanged in 3 eyes and decreased in 1 eye during the follow-up of 3-12months.· CONCLUSION: Application of pure C3F8 tamponade on or after primary operation can effectively improve hypotony after severe ocular trauma and benefit a better prognosis.

Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.
2-Hydroxypropyl-beta-cyclodextrin ; Alkaloids ; chemistry ; Chemistry, Pharmaceutical ; methods ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Rutaceae ; chemistry ; Solubility ; beta-Cyclodextrins ; chemistry