For the minimized phase transtorming risk, the most stable polymorph is generally considered as the desirable solid form for pharmaceutical applications. However, occasionally, the stable form may have some shortcomings such as low solubility, dissolution rate and bioavailability, etc. In that case, the metastable form which is kinetically stable at room or lower temperature could be selected. Using metastable form may result in polymorph transformation in pharmaceutical manufacture and storage. Hence, the knowledge of the transformation between solid forms is essential to the development of the drug materials. In this paper, we will review the recent studies in the area of crystal conversion of polymorphs and hydrates, to illustrate some cases to introduce the types, conditions and mechanisms of the crystalline solid transformation.
Biological Availability ; Chemistry, Pharmaceutical ; methods ; Crystallization ; Drug Stability ; Kinetics ; Pharmaceutical Preparations ; chemistry ; Solubility

Objective To evaluate the efficacy of jaw thrust device in the upper airway obstruction. Methods Thirty-five ASA Ⅰ or Ⅱ patients aged 18-64 yr with body mass index < 30 kg/m~2 undergoing elective surgery under general anesthesia were included in this study. The anesthesia face mask was placed and held tightly by 4 straps of JTD and connected to the anesthesia machine. Anesthesia was induced with midazolam, propefol, fentanyl and atracurium. When muscle relaxation was achieved, tracheal intubation was not performed. The airway obstruction was assessed by airway peak pressure and stridor score (breathing sounds detected by auscultation over the trachea). And then tracheal intubation was performed, and the patients were mechanically ventilated. Results There was no significant difference in airway pressure and stridor scores between JTD and jaw thrust maneuver. Conclusion JTD can effectively lift the jaw and improve the upper airway obstruction.

Objective To research the method and effect about the bronchoscopic lung volume reduction by ?-cyanoac- rylate in the therapy of chronic obstructive pulmonary disease (COPD).Methods The 14 patients had been examined bosoms by CT before the operation and determined the type of emphysema and the distributing of pneumatocele,had blood gas analyzed and pulmonary function checked.The operation was carried through trachea cannula and intravenous anesthe- sia.When the bronchoscope came to the goal bronchia,we infused the meglumine diatrizoate through the biopsy orifice and approved the location of pneumatocele forward。Then,we infused erythromycin and ?-cyanoacrylate in turn through the biopsy orifice by silica del tube.Results The 3 pneumothorax patients had been removed the drainage tube in 3 days af- ter the operation.8 cases had been counterchecked sternite in one week and the pneumatocele was just like before,among which,1 case developed exudation.1 case had shown pleural thickening in the right-up lung counterchecked sternite 9 months later.1 case been checked the pulmonary function,the FEV_1 enhanced from 24.7% pred before operation to 32. 9% pred after operation one week.3 cases felt polypnea improved greatly and 7 cases felt polypnea improved a little.Con- clusion The bronchoscopic lung volume reduction by ?-cyanoacrylate is a safe,effective and economical method in the therapy of COPD.

· Vascular endothelial growth factor is indispensable inducing factor in retinalangiogenesis. After the retinal neovascularization of proliferative diabetic retinopathy ( PDR ) patients, it can cause fibrovascular membrane formation, epiretinal membrane fibrosis increased, resulting in traction retinal detachment with further aggravate the condition. The recent research suggests that cytokines promote fibroblast proliferation, movement, adhesion, and secretion of extracellular matrix functions in the diabetic state of the environment changes to profibrogenic state, resulting in the accumulation and fibrosis of extracellular matrix. This paper reviewed the status quo of the correlation between vascular endothelial growth factor and fibrosis-related cytokine.

To study the effect of sodium aescinate in inducing human breast cancer MCF-7 cells apoptosis and its possible mechanism. MTT assay was used to detect the inhibitory effect of sodium aescinate on the proliferation of MCF-7 cells. The morphological changes were observed under inverted microscope. DAPI nuclear staining was used to detect the changes in cell nucleus. Annexin V-FITC/PI flow cytometry was adopted to test the apoptosis rate. Changes in apoptosis-related proteins (PARP, cleaved caspase-8 and pro-caspase-3), cell survival-associated signal molecules (AKT and ERK) and their common upstream kinase SRC was detected by Western blotting. The result showed that after different concentrations of sodium aescinate were used to treat breast cancer MCF-7 cells, they inhibited the proliferation of MCF-7 cells in a dose-dependent manner, induced cell apoptosis (typical morphological changes in nucleus, significant increase in cell apoptosis rate). The expressions of cleaved PARP and caspase-8 increased, while the expression of pro-caspase-3 decreased, which further verified sodium aescinate's effect in inducing cell apoptosis. Sodium aescinate significantly inhibited the phosphorylation of cell survival-related signal molecules (AKT, ERK) and down-regulate the activation of their common up-stream kinase SRC. The findings indicated that sodium aescinate can block signals transiting to downstream molecules AKT, ERK, inhibit the proliferation of breast cancer cell MCF-7 cell apoptosis and induced cell apoptosis by suppressing the activation of SRC.
Antineoplastic Agents, Phytogenic ; pharmacology ; Apoptosis ; drug effects ; Breast Neoplasms ; drug therapy ; enzymology ; genetics ; physiopathology ; Down-Regulation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Extracellular Signal-Regulated MAP Kinases ; genetics ; metabolism ; Female ; Humans ; MCF-7 Cells ; Proto-Oncogene Proteins c-akt ; genetics ; metabolism ; Saponins ; pharmacology ; Signal Transduction ; drug effects ; Triterpenes ; pharmacology ; src-Family Kinases ; genetics ; metabolism

OBJECTIVETo study the cleavage activity on the HCV RNA of a chimeric recombinant of HCV specific ribozyme and U1 small nuclear RNA, which compartmentalizes within the nucleolus.

METHODSThe third stem-loop sequence of human U1 snRNA (position 95-116) within pBSIISK+ U1 was substituted by hammerhead ribozyme against HCV RNA by PCR and cloning methods, and the constructed plasmid was named pBSIISK+ (U1-Rz). Then the whole gene fragment of the chimeric ribozyme was cloned into a pGEM-T vector under the control of T7 promoter, and the constructed plasmid was named pGEM- (U1-Rz). The pGEM- (U1-Rz) and pGEM-Rz (containing the same ribozyme sequence as that in U1-Rz) transcripts as enzyme were transcribed in vitro. Also the (32)P-labeled pCMV/T7-NCRC luc (containing the gene sequence of the whole 5'-NCR and part core of HCV RNA) transcripts as target-RNAs were transcribed in vitro. The enzymes were incubated with the target RNAs under different conditions and autoradiographed after denaturing gel-electrophoresis.

RESULTSThe sequencing result showed that the construction of U1 snRNA chimeric ribozyme was correct. Compared with the ribozyme alone, both of them were active at 37 degree C and with Mg2+ (10 mmol/L) and TrisCl (10 mmol/L, pH7.9), and there was no remarkable difference between them. The cleavage activity of the chimeric ribozyme increased with the prolongation of reaction time and increment of enzyme concentration.

CONCLUSIONBoth ribozyme and U1 snRNA chimeric ribozyme exhibited specifically catalytic activity against HCV RNA in vitro. There was no remarkable difference between their cleavage efficiencies.

Chimera ; genetics ; Genetic Therapy ; Hepacivirus ; genetics ; Hepatitis C ; therapy ; RNA, Catalytic ; genetics ; metabolism ; RNA, Small Nuclear ; genetics ; pharmacology ; RNA, Viral ; genetics ; Recombinant Fusion Proteins ; pharmacology

Calcinosis ; pathology ; Child ; Humans ; Inhibins ; metabolism ; Male ; S100 Proteins ; metabolism ; Sertoli Cell Tumor ; metabolism ; pathology ; surgery ; Testicular Neoplasms ; metabolism ; pathology ; surgery ; Vimentin ; metabolism

Lipoproteins are biological lipids carriers. The natural and reconstituted lipoprotein based drug delivery systems have been extensively developed in recent years. This article reviews the development of natural and reconstituted low-density lipoprotein and high-density lipoprotein based vehicles in the antitumor area.
Animals ; Antineoplastic Agents ; administration & dosage ; chemistry ; Apolipoproteins B ; administration & dosage ; chemistry ; Drug Carriers ; administration & dosage ; chemistry ; Humans ; Lipoproteins ; administration & dosage ; chemistry ; Lipoproteins, HDL ; administration & dosage ; chemistry ; Lipoproteins, LDL ; administration & dosage ; chemistry ; Nanoparticles ; Neoplasms ; drug therapy ; Peptides ; administration & dosage ; chemistry ; Pharmaceutical Vehicles ; chemistry

Objective A large number of injured earthquake patients were accepted by the hospital whilethe professional surgeons were relatively lack. This article introduced the hospital emergency management in 2008Sichuan Wenchuan Earthquake, China. Method Within 3 days, Central Hospital of Mianyang accepted andtreated over 1000 patients after Wenchuan Earthquake jolted on 12 May 2008,and within 2 weeks, the number ofpatients reached 1500. The hospital carded out emergency management plan: (1) emergency comprehensive treat-ment district was established, which was divided into traumatic surgery district, general surgery district, and gen-eral medical district. Traumatic surgery district is responsible for treating traumatic patients, and most doctors andnurses were in this district. The district also had preview, contamination, operation, isolation, monitoring sec-tions, and the tents were numbered and labeled. General surgery district and general medical district were responsi-ble for patients not from earthquake, and only few doctors and nurses were in the two districts. According to the in-jury degree, all the wounded were classified into acute and severe, moderate and minor injuries, and wore red,yellow and blue label on the wrists, respectively. The name, gender, age and diagnosis of each patient and thename of doctor were written on the label. The infectious patients and non-infectious patients were separated.Results Near 200 operations and near 300 operations were performed at one night and at one day, respectively.Within one week, only 1 patient had the lung infection, and one patient with gangrenous emphysema was effective-ly treated. In-hospital cross infection and epidemic of infection disease didn't happen. Conclusions Emergencymanagement model and mechanism, which referred to the model of the battlefield ambulance, played an importantrole in treating a large number of injured patients.

Objective To investigate Helicobacter pylori(Hp)infection and HLA-DQA1 allelic frequency in family members of children with recurrent abdominal pain.Methods One hundred and eighteen family members of 20 children with recurrent abdominal pain were divided into two groups:with and without recurrent abdominal pain.Serum Hp antibody was tested by dot immunogold filtration assay and immunophenotyping was determined by Western blot(immunobiot)technique.Polymerase chain reactionsequence specific primers(PCR-SSP)technique Was applied to identify HLA-DQAi allelic frequencies.Hardy-Weinberg equilibrium test was performed(P>0.05),and Chi-square test was used to compare the frequency of HLA-DQA1 alleles between the groups.Results The Hp seropositive rate in 118 members Was 100%and the Hp immunophenotyping was 96.6%.The prevalence of Hp Ⅰ and Ⅱ type was 55.1%(65/118)and41.5%(49/118).HLA-DQA1*0302 allelic frequency Was significantly higher in subjects with recurrent abdominal pain than that in subjects without one(23%vs.2%,X2=13.277,P=0.000).Conclusion There is immunogenetic difference between familial members with and without recurrent abdominal pain infected by Hp,and HLA-DQA1*0302 may be the associated gene contributing to different clinical outcomes after Hp infections.