Objective:To study the effect of membrane-coating on dissolution and stability of sirolimus ( SRL) dropping pills to prove the effect and rationality of the coating process. Methods:Opadry was used as the coating material for SRL dropping pills. Com-pared with those of uncoated SRL dropping pills, the dissolution and stability of membrane-coating SRL dropping pills were studied in vitro. Results:Compared with that of uncoated SRL dropping pills, the drug release amount of membrane-coating SRL dropping pills was lower (P<0. 05), however, the stable release rate showed no significant difference (P>0. 05). After the membrane-coating, the stability of SRL dropping pills was notable enhanced under high humidity (75% ± 5%) and strong light (4500lx ± 500lx) conditions, however, the stability showed no improved under high temperature(40℃ ± 2℃) condition. Conclusion: The membrane-coating can enhance the stability of SRL dropping pills without significant effect on drug release in vitro.

Objective:To study the relative bioavailability of sirolimus ( SRL) dropping pills in rats. Methods:PEG6000 as the base, SRL dropping pills were prepared using solvent-melting method. The SRL marketed tablets as the reference preparation and rats as the animals, the relative bioavailability of SRL dropping pills was studied to obtain the pharmaceutical parameters and bioequiavail-ability. Results:Compared with that of the reference preparation, tmax of SRL dropping pills was the same (1 h). There was no signifi-cant difference in Cmax between the dropping pills and the tablets (P>0. 05). AUC0-24 of the dropping pills was notably higher than that of the marketed tablets (P<0. 05) with the bioequiavailability of 121. 98%. Conclusion:SRL dropping pills with promising bioavail-ability are valuable to be studied further.

Objective To explore the clinical therapeutic efficacy and value of endovascular embolization treatment for Hunt-Hess poor-grade intracranial aneurysms. Methods Eighty-seven patients with Hunt-Hess grade Ⅳ - Ⅴ intracranial aneurysrns were treated with endovascular embolization from May 2001 to February 2010,77 patients were grade Ⅳ and 10 patients were grade Ⅴ. Outcomes were assessed by using the Glasgow outcome scale (GOS). Results Follow-up time was from 3 months to 9 years. The therapeutic efficacy was as following according to GOS: 25 patients were grade Ⅰ , 5 patients were grade Ⅱ , 9 patients were grade Ⅲ , 12 patients were grade Ⅳ ,and 36 patients were grade Ⅴ. There were 55.17%(48/87) favorable outcome rate and 28.74% (25/87) mortality rate in all patients. There were 61.70%(29/47) favorable outcome rate and 25.53%(12/47) mortality rate in early stage treatment patients (diseased within 3 d), otherwise there were 47.50% (19/40) favorable outcome rate and 32.50%(13/40) mortality rate in medium and late stage treatment patients (diseased 3 d or later). There were no statistically significance in favorable outcome rate and mortality rate between them (P > 0.05). All the patients were embolized successfully ,technical complications occurred in 8 patients, 10 patients were found angiographic evidence of vasospasm. Conclusions Endovascular embolization is an effective method for treating Hunt-Hess poorgrade intracranial aneurysms. Early stage treatment is a feasible option because it can improve prognosis by reducing rebleeding and vasospasm.

Objective To investigate the surgical treatment and clinical outcome of patients with intracranial posterior circulation poor-grade aneurysms. Methods The clinical data of 35 patients with intracranial posterior circulation poor-grade aneurysms were collected. Seventeen patients were World Federation of Neurosurgical Societies (WFNS) grade IV and 18 patients were WFNS grade V. Twenty- nine patients were definitively treated with open microsurgery treatment(2 patients) and endovascular treatment (27 patients). Six patients received conservative treatment, including 4 patients only receiving external ventricular drainage to decrease intracranial pressure and 2 patients only receiving medical treatment. The nerve function were evaluated by Glasgow outcome scale (GOS) at discharge from hospital and 1 and 12 months after operation. Results In the patients who received conservative treatment, 5 patients were dead in hospital, and 1 patient got good outcome after 12 months. In the patients who received surgical treatment, at discharge from hospital good outcome were achieved in 15 patients (51.7%), poor outcome in 9 patients (31.0%), and death happened in 5 patients (17.2%). At 1 month after operation, good outcomes were achieved in 14 patients (48.3%), poor outcome in 9 patients (31.0%), and death happened in 6 patients (20.7%). At 12 months after operation, good outcome were achieved in 18 patients (62.1%), poor outcome in 5 patients (17.2%), and death happened in 6 patients (20.7%). Conclusions Patients with posterior circulation poor-grade aneurysms have better prognosis after positive surgical treatment.

Objective:To coat sirolimus ( SRL) dropping pills with a membrane to enhance the ability of moisture proof. Meth-ods:Opadry was chosen as the coating material. The solvent, concentration and weight gain of the coating membrane were defined, and the coating parameters were screened. The critical relative humidity ( CRH%) of membrane-coating SRL dropping pills was detec-ted and compared with that of SRL dropping pills without coating. Results: The formula and coating parameters of membrane-coating SRL dropping pills were as follows:95% ethanol was used as the solvent, Opadry concentration was 6. 5%, the weigh gain was 4%, the inlet air temperature was (35 ± 2)℃, the inlet fluid rate was 12 ml·min-1 and the spraying pressure was 3. 0 MPa. The CRH%of memebrane-coating SRLs dropping pills was 63. 1%, which was much higher than that of uncoated SRL dropping pills (36. 1%). Conclusion:The membrane-coating can enhance the moisture proof of SRL dropping pills, which is beneficial to the stability.

To screen the optimal formula and evaluate the quality of testosterone undecanoate ( TU) binary ethosomes to lay the foundation for the transdermal delivery system of TU. Methods:The mixture of ethanol and propylene glycol was used as the softeners, and TU binary ethosomes were prepared by ethanol injection method. The ratio of TU to lipids ( A) , the quality percentage of the mixture of ethanol and propylene glycol ( B) and the ratio of ethanol to propylene glycol ( C) as the influencing factors, and the entrapment efficiency as the index, an orthogonal test was used to optimize the formula of TU binary ethosomes. The morphology, size, zeta potential, in vitro drug release and stability of TU binary ethosomes were studied. Results:The optimal formula of TU binary etho-somes were as follows:the ratio of TU to lipids was 1∶15, the quality percentage of the mixture of ethanol and propylene glycol was 10% and the ratio of propylene glycol to ethanol was 6∶4. The optimal TU binary ethosomes were concentric circles under an optical microscope with uniform size, and the average size was (185. 5 ± 52. 8)nm, zeta potential was ( -15. 87 ± 0. 26)mV, and the entrap-ment efficiency was (79. 14 ± 0. 66)%. TU release from the binary ethosomes in vitro was fitted the first-order equation:Q=20. 79t-11. 01 (r2 =0. 998 4). Under the high temperature, the entrapment efficiency was decreased significantly, while under the other test conditions, all the indices of TU binary ethosomes showed no significant difference. Conclusion:The optimal TU binary ethosomes are easy to be prepared with promising quality and sustained release property in vitro, which are valuable to be studied further.

Objective:To explore the interaction between gossypol and human serum albumin ( HSA) . Methods:The interaction of gossypol and HSA under physiological conditions was studied by fluorescence spectroscopy, and the molecular docking software was used to simulate the interaction. Results:The binding constant of gossypol and HSA at 293K and 303K was 2. 390 6 × 105 L·mol-1 and 3. 576 8 × 103 L·mol-1 , respectively. There was one binding site on HSA for gossypol. Hydrogen bond and Van Der Waals inter-actions were involved in the binding process. The binding of gossypol and HAS was closer to tyrosine residue in HSA. The molecular simulation analysis verified the above results. Conclusion: The gossypol-induced fluorescence quenching of HSA belongs to a static quenching procedure.

Objective To assess the application of three-dimensional digital subtraction angiography (3D-DSA) in evaluation of ruptured intracranial aneurysm after clipping and to discuss the different variable use of vol-ume rendering(VR), gradient rendering (GR) and maximum intensity projection (MIP). Methods From January 2011 to December 2012 , 88 patients with 92 ruptured intracranial aneurysms were treated with clipping using titani-um clips in our hospital and followed up by both 2D-DSA and 3D-DSA. Residual aneurysms , Clips place, clips and parent arteries and stenosis of parent arteries were evaluated by volume rendering (VR), gradient rendering (GR) and maximum intensity projection (MIP). Results Among 92 clipped aneurysms, 23 residual aneurysms were found by 3D-DSA. Residual aneurysms were recorded according to the Sindou grade: 15 of gradeⅠ, 3 of gradeⅡ, 4 of grade Ⅲand 1 of grade Ⅳ. Three patients of grade Ⅲand 1 of grade Ⅳwith residual aneurysms were retreated by clipping or coiling, and 1 patient of grade Ⅲ was dead with rupture of residual aneurysm. The clips and number of clips were clearly visualized , and relationship between the clips and the aneurysms was well demonstrated by VR, GR and MIP images. VR, GR images showed the remnants clearly. Three-dimensional digital subtraction angiography did not showed accurate details of the stenosis of parent arties which required an analysis of 2D-DSA. Conclusion Three-dimensional digital subtraction angiography can be used for definite evaluation of resid-ual aneurysms after clipping, especially by VR, GR images. It is helpful to manage the residual ruptured aneurysms.

Objective To investigate the drug resistance,source and molecular epidemiology of methicillin-resistant Staphyloccus aureus(MRSA)causing nosocomial infection. Methods Fifty-seven pathogenic MRSA strains were isolated from Beijing Tongren Hospital during 2007 and 2008.K-B method,MIC assay,multiple PCR,automatic repetitive element sequence-based PCR(REP-PCR)typing platform and DL MRSA Library were used to identify the resistant phenotypes,Panton-Valentine leukocidin gene (pvl)and REP-PCR types of the MRSA.Results All strains were classified as 6 antibiotic resistant phenotypes(a-f)based on the resistance to rifampin,clindamycin,levofloxacin and cotrimoxazole.The MRSAs with Staphylococcal cassette chromosome mec(SCCmec)Ⅲ and SCCmec Ⅱ accounted for 91.23% (52/57)and 5.26%(3/57)of all strains,respectively.Only one strain was pvl positive.All strains were typed as REP-A-F(6 types)and three single clones by automatic REP-PCR typing platform,in which REP-C was predominant(30/57,52.63%).Three out of 6 REP-D strains were from laryngology wards.The REP-C-SCCmec Ⅲ were genetically most close to the Brazilian clone-SCCmec Ⅲ in DL MRSA Library.Conclusion s REP-C-SCCmec Ⅲ-a type are the major epidemic hospital-associated MRSA and the REP-D-SCCmec Ⅲ-d is usually isolated from patients received laryngeal surgery. Automatic REP-PCR typingplatform combined with DL MRSA Library database is an effective approach to study the nosocomial infection.

Polyamine biosynthesis is controlled primarily by omithine Decarboxylase (ODC) and S-adenosylmethionine decarboxylase (AdoMetDC). Antisense ODC and AdoMetDC sequences were cloned into an adenoviral vector (Ad-ODC-AdoMetDCas). To study the inhibitory effects of Ad-ODC-AdoMetDCas on polyamine biosynthesis and esophageal cancer cell apoptosis, adenovirus-mediated gene tmnsduction efficiency was assessed with counting GFP-positive cells using MTT. The malignant phenotype of Eca109 cells was assessed by growth curve. Western blot and HPLC were used to detect ODC and AdoMetDC expression and polyamine content in Ecal09 cells. TUNEL was used to analyze cell apoptosis. The change of morphology of apoptotic cells was observed by electron microscope. It was demonstrated approximate 70% of Eca 109 cells were infected with Ad-ODC-AdoMetDCas when MOI reached 50. The expression of ODC was inhibited in the infected tumor cells. Ad-ODC-AdoMetDCas could inhibit Ecal09 cell growth and invasive ability. TUNEL proved that Ad-ODC-AdoMetDCas can lead to cell apoptosis. Characterized morphology was observed by electronmicroscope (ehromatincondensation,nuclear disintegration,formation of apoptoticbodies).It was suggested Ad-ODC-AdoMetDCas has significant inhibitory effects on esophageal cancer cell proliferation, leads to cell apoptosis and bears therapeutic potential for the treatment of esophageal cancer.