Pure and drug hydrophilic matrix tablets were prepared by direct compression method with theophylline as a model drug. The characteristics of four hydrophilic matrix polymers, hydroxypropylmethylcellulose (HPMC), polyethylene oxide (PEO), sodium alginate (NaAlg) and xanthan gum (XG), were compared by investigating the water absorption, swelling, erosion and gel layer strength. The sequence of water absorption rate was XG >> NaAlg (H) > PEO > NaAlg (L) >> HPMC; The sequence of swelling index was XG >> PEO >> HPMC >> NaAlg; The sequence of erosion rate was NaAlg (L) > NaAlg (H) >> PEO80 > PEO200 > PEO300 > XG approximately PEO400 approximately K4M > K15M > PEO600 approximately K100M; The sequence of the gel layer strength was PEO > HPMC > XG >> NaAlg. For the PEO and HPMC matrix tablets, with the polymer molecular weight increased, the drug release mechanism was gradually transferred from mainly depending on the erosion to the diffusion; for SAL matrix tablets, the drug release mainly depends on erosion mechanism; and for XG matrix tablets, the drug release mainly depends on non-Fick diffusion mechanism. Comparison of the performance difference between the polymer materials will contribute to rational design and prediction of drug release behaviors from matrix tables and ultimately to achieve clinical needs.

OBJECTIVE: To prepare Polylactic-co-glycolic acid)(PLGA) microspheres loaded with Chinese herbal extract cucurbitacin B.METHODS: Cucurbitacin B loaded by PLGA microspheres were prepared by modified emulsification-solvent evaporation method.Central composite design-response surface method was applied to optimize the formulation with PVA concentration and ratio of drug to polymer as independent variables,and with yield of microspheres(Y1),drug loading amount(Y2),encapsulation efficiency(Y3),mean particle diameter(Y4),and the cumulative percentage of the drug release in 24 hr(Y5) as indexes to conduct multiple linear regression and second-order polynomial equation fitting.In vitro release test was performed by modified immediate release method.RESULTS: The results showed that all response variables were greatly fitted by a second-order polynomial equation.The optimal formulation was proved to be as follows: PVA concentration was 0.014 and ratio of drug to polymer was 0.066 5.The microspheres prepared in the optimal formulation were spherical and had smooth surface.Y1,Y2,Y3,Y4,and Y5 were 79.9%,7.83%,80.5%,56.18 ?m and 6.98%,respectively.The cumulative release from microspheres within 35 days reached 86.73%.CONCLUSION: Cucurbitacin B-PLGA microspheres are characterized by prolonged action and sustained-release.Furthermore,the established model has satisfactory predictability.

Objective To optimize the formula of konjac glucomannan-paeonol matrix tablets. Methods The formula of paeonol matrix tablets was optimized by the orthogonal design with the accumulative release rate in vitro as index, with the viscosity of konjac glucomannan ( KGM) , the amount of KGM and lactose as influence factors. Results The optimized formula was as follows:the viscosity of konjac glucomannan was 20 000 mPa·s, KGM 30%, lactose 20% and the release in vitro fit into the Higuchi equation. Conclusion The formula of the paeonol matrix tablets is reasonable and the tablets have well release effect in vitro.

Objective To study the role of endothelial cells on the inflammatory cytokine release in septic shock through the septic shock serum stimulating human primary endothelial cells (HPAEC) and peripheral blood mononuclear cells(PBMC).Methods PBMC isolated from healthy people by density gradient centrifugation.HPAEC cell surface markers CD144 and von Willebrand factor(vWF) molecule expression by RT-PCR and Western blot.Serum levels of IL-6,TNF-α,MCP-1 from septic shock patients and healthy human detected by ELISA.HPAEC and PBMC were stimulated with the isolated serums and LPS,respectively.ELISA was used to detect the supernatant IL-6,TNF-α,MCP-1 levels.HPAEC membrane molecules ICAM-1 expression was detected by flow cytometry with serum shock and LPS stimulation.Supernatant levels of IL-6,TNF-α,MCP-1 of HPAEC with S1P1 receptor agonist CYM-5442 pretreatment was detected by ELISA after shock serum stimulation.Results Endothelial cell markers CD144 and vWF molecules could be detected in the HPAEC.Levels of inflammatory cytokines IL-6,TNF-α,MCP-1 in patients with septic shock serum were significantly higher than healthy people (P＜0.01).PBMC and HPAEC with LPS or shock serum treatment respectively,compared with normal group,levels of inflammatory cytokines in the culture supernatant were significantly higher(P＜0.01).For PBMC,the level of inflammatory cytokines between shock group and LPS group were not significantly different (P＞0.05).But for HPAEC,levels of inflammatory cytokines in the supernatant of the shock group compared to the LPS group was significantly higher (P＜0.01).Similarly,when two cells after LPS stimulation,IL-6,TNF-α levels of HPAEC's supernatant were significantly lower than PBMC' s (P＜0.01),MCP-1 levels was no difference (P＞ 0.05).But when the stimulation of shock serum,HPAEC of IL-6,TNF-α levels and PBMC no significant difference (P ＞0.05).MCP-1 was significantly increased (P＜0.01).Shock patients serum stimulation S1P1 receptorspecific agonist CYM-5442 pretreatment of HPAEC with pretreatment of S1P1 receptor specific agonist CYM-5442,the culture supernatant of inflammatory cytokines IL-6,TNF-α,MCP-1 levels were significantly lower (P＜0.01).Conclusion Endothelial cells may play a central role on the release of inflammatory cytokine during septic shock.

Objective To study the in vivo expression and biodistribution of Ad5-Fluc (Adenovirus carrying firefly luciferase genes) in mice.Methods The recombinant Ad5-Fluc virus was constructed and infected to BALB/c or nude mice through three different routes.The protein expression level,tissue distribution and the characteristics of infection were analyzed by in vivo bioluminescence imaging technology.Results Compared to other two routes,the BALB/c mice infected through muscular route had the longest expression cycle (over 60 days) and the highest expression level,while the virus was transferred into the liver and spleen after infection.The nude mice had a significantly extended expression cycle than BALB/c mice.Moreover,the characteristic of liver tropism was eliminated after Ad5 F35 infection in mice,while maintained similar expression efficiency.Conclusion Due to the highest expression efficiency,the muscular route would be the optimal route for Ad5 vector based vaccination.In addition,Ad5F35 virus could become an ideal alternative vaccine vector for eliminating the liver tropism.

Objective To investigate the effects of circumferential pulmonary vein isolation (CPVI) on atrial effective refractory period (ERP) in patients with paroxysmal atrial fibrillation.Methods 30 patients who underwent radiofrequency catheter ablation for paroxysmal AF were enrolled in this study.Using FAM mode,the RA and LA anatomical models were achieved in the CARTO 3 system.SVC,MRA,RAA,LA-A,LA-R,LA-P,LAA,LSPV,LIPV,RSPV,RIPV,CSp,CSd,were respectively located in the RA or LA anatomical model.Before and after CPVI,ERPs were measured in different locations of the atrium using programmed stimulation.The ERPs of the RA (SVC,MRA,RAA,CSp),LA (LA-A,LA-R,LA-P,LAA,CSd),PVs (LSPV,RSPV,LIPV,RIPV) were compared.Bilateral CPVIs were completed in all patients,and PV-LA bidirectional conduction block was achieved.The changes of electrophysiological characteristics of atrium before and after CPVI were observed.Results (1) ERP at different locations in the atrium before CPVI:Comparisons of ERPs at different locations of atrium:RAA had the minimal ERPs[(197.4 ± 28.6) ms (P ＜ 0.01);followed by PVs measuring,respectively,LSPV (213.0 ± 47.5) ms,LIPV (208.9 ± 45.9) ms,RSPV (209.3 ± 43.6) ms,RIPV (213.5 ± 48.1) ms and LAA (218.1 ± 27.7) ms.Comparisons of ERPs in RA,LA,and PVs showed:PVs had the lowest ERPs (211.2 ± 35.2) ms versus RA ERP (227.0 ± 23.7) ms versus LA ERP (241.0 ± 21.5) ms (P ＜ 0.05).(2) Comparisons of ERPs before and after CPVI:Comparisons of ERPs at different locations of atrium showed:RAA [(197.4 ± 28.6) ms vs.(208.6 ± 32.2) ms,P=0.003],CSp [(234.7 ± 29.1) ms vs.(246.9 ± 29.7) ms,P=0.007],LA-R [(242.9 ± 28.9) ms vs.(258.3 ± 26.9) ms,P=0.003],LA-P [(252.2 ± 28.5) ms vs.(261.1 ± 30.2) ms,P=0.039]and CSd [(238.6 ± 28.3) ms vs.(250.3 ± 23.6) ms,P =0.009].ERPs were found statistically prolonged at all different locations after CPVI.Comparisons of ERPs at RAand LA after CPVI showed:RA [(227.0 ± 23.7) ms vs.(235.9 ± 21.7)ms,P=0.002]and LA [(241.0 ± 21.5) ms vs.(249.7 ± 19.9) ms,P =0.001],which were statistically increased after CPVI.(3) A total of 90 episodes of atrial arrhythmias were induced before CPVI which were found at RAA (n =17),LAA (n =12),and PVs (n =36).After CPVI,8 episodes of atrial arrhythmias were induced which were found at,RAA (n =4),LAA (n =3),and SVC (n =1).Conclusions (1) Compared with other parts of atrium,ERPs at PVs,LAA and RAA are significantly shorter in patients with paroxysmal AF.At PVs,LAA and RAA,atrial arrhythmias are easily to be induce by programmed stimulation.(2) In patients with paroxysmal Af:PVs has the shortest ERPsfollowed by RAs whereas LA ERPs is the longest.There is a large ERP gradient change between PVs and LA.(3) The ERPs at RAs,LAs,As,and LA-PV are prolonged after CPVI.(4) Atrial arrhythmia is less likely to be induced after CPVI.

Objective To investigate the characteristics of growth, accumulation of indole alkaloid, and the optical concentration of the nutrition components in the Catharanthus roseus mutant cells induced by the colchicine, looking forward to getting the ideal material producing alkaloids which was suited for industrialized cell cultivation. Methods Mutant cells cultivated on the MS medium were harvested according to experiment designs,and the fresh weight was got.The indole alkaloid as extracted by organic solvent. The ajmalicine and catharanthine extracted from the samples were analyzed by RP-HPLC. Results The growth rate was faster and the indole alkaloid accumulation was more when the mutant cells were cultivated generations 30 and the both were sharply decreased at generations 45, while the contents of medical compounds amounted to the peak at the generations 20. The content of medical components and alkaloid accumulation were evidently prompted by the tryptophan added in the media, especially at the concentration of Ca2+ 1 760 and Zn2+ 12.6 mg/L, respectively. Conclusion C.roseus mutant cells probably is an ideal material for industrialized cell cultivation.

Objective:To evaluate the effect of driving pressure-guided individualized positive end-expiratory pressure (PEEP) titration on atelectasis in elderly patients undergoing robot-assisted radical prostatectomy.Methods:Fifty elderly patients, aged 65-80 yr, of American Society of Anesthesiologists physical status Ⅱ or Ⅲ, with body mass index of 19-28 kg/m 2, undergoing elective robot-assisted radical prostatectomy under general anesthesia, were divided into 2 groups ( n=25 each) according to the random number table method: traditional lung-protective ventilation group (group C) and driving pressure-guided individualized PEEP group (group D). The method for setting PEEP was as follows: PEEP 5 cmH 2O was used throughout operation in group C. In group D, the optimal PEEP was titrated after intubation and mechanical ventilation and Trendelenburg position-pneumoperitoneum construction, the initial value was the lowest PEEP allowed by the anesthesia machine, the PEEP was increased by 1 cmH 2O (PEEP≤12 cmH 2O) every 4 min, the plateau pressure and PEEP were simultaneously recorded to calculate the driving pressure, and the corresponding PEEP was considered as the optimal PEEP for the individual when the driving pressure reached the minimum.Ultrasound examination was performed after catheterization of radial artery (T 0), after anesthesia induction (T 1), 4 min after developing optimal PEEP ventilation (T 2, 4 min after developing ventilation in group C), after restoration of body position (T 3), before extubation (T 4), and at 2 h after admission to postanesthesia care unit (T 5). Atelectatic aeration loss scores were recorded at T 0, T 1, T 4 and T 5.Bilateral optic nerve sheath diameter was measured at T 0-4.Arterial blood gas analysis was performed at T 0, T 2, T 3 and T 5, PaO 2 and PaCO 2 were recorded, and oxygenation index was calculated.The postoperative pulmonary complications within 3 days after operation were recorded. Results:Compared with group C, atelectasis aeration loss scores at T 4, 5 and PaCO 2 at T 2, 3 were significantly decreased, and PaO 2 and oxygenation index were increased at T 2, 3, 5 in group D ( P<0.05). There were no significant differences in the bilateral optic nerve sheath diameter and incidence of postoperative pulmonary complications between the two groups ( P>0.05). Conclusion:Driving pressure-guided individualized PEEP can increase intraoperative oxygenation and decrease the development of atelectasis in elderly patients undergoing robot-assisted radical prostatectomy.