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

?AlM: To evaluate the clinical efficacy of posterior continuous curvilinear capsulorhexis ( PCCC ) combined with anterior vitrectomy in preventing posterior capsule opacification of congenital cataract surgery.
?METHODS:Postoperative clinical follow-up data of 82 cases ( 87 eyes ) with congenital cataract treated in Eye Center of our hospital from January 2011 to August 2014 were retrospectively analyzed. The patients were divided into the surgical control group ( 38 cases, 40 eyes, recieved phacoemulsification + PCCC ) and the study group ( 44 cases, 47 eyes, accepted phacoemulsification+ PCCC + anterior vitrectomy). The incidence of central optic axis opaque and postoperative visual acuity distribution were recorded at 1a follow - up. lntraoperative and postoperative complications were observed.
?RESULTS:The rate of central optic axis opaque grade 0 in control group was 37. 5%, compared to 76. 6% in study groups. The opacity distribution ratio of grade 1,2,3 and 4 in study group were lower than that of control group, and the central optic axis opacity distribution ratio in study group was significantly better than that of control group (P<0. 05). The 19 eyes(47. 5%) of visual acuity testing ≤0. 5 in control group , was higher than the 7 eyes(14. 89%) of that in the study group, The 21 eyes (52. 5%) of visual acuity testing >0. 5 in control group was lower than the 40 eyes ( 85. 11%) of that in study group. The visual acuity between two groups has statistical significance difference after 1a follow-up ( P<0. 05 ) , and the visual acuity in study group was significantly better than that in the control group. The postoperative intraocular pressure at 1mo and 1a follow-up was lower than before operation in two groups ( P<0. 05), but there was no significant difference between two groups in intraocular pressure (P<0. 05).
?CONCLUSlON: Combination of phacoemulsification, PCCC and anterior vitrectomy presents reliable clinical effects on postoperative central optic axis opacity distribution ratio and visual acuity, and it should be adopted to prevent the occurrence of posterior capsule opacification.

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.

A reasonable and practicable quality standard was developed for mori liquid extract from different sources by TLC, HPLC and fingerprint technology. In TLC method, the compounds were separated on polyamide film using glacial acetic acid-water (1: 3) as mobile phase at a UV wavelength of 365 nm. All qualified samples had the spots of the same color as the control herb and substance. The RP-HPLC method was used to determine the content of mulberroside A with mobile phase of methanol-water (25: 75) at a wave-length of 326 nm. The mulberroside A was in good linear with a regression equation of Y = 46.965X (r = 0.999 6) in the range of 4.6 - 228 mg x L(-1). In 14 batches of samples, the mulberroside A in 4 batches of them was less than 0.5 g x L(-1), and was more than 2.0 g x L(-1) in the other batches. It was suggested that the content limit of mulberroside A should be no less than 1.5 g x L(-1). The HPLC fingerprints were evaluated by the similarities. It has found that the similarities of different mori liquid extracts were very low and the chemical diversity of mori cortex was the major factor of similarity. Moreover, the process impact was minimal. Thus the fingerprint was not included in this quality standard.
China ; Chromatography, High Pressure Liquid ; Disaccharides ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; standards ; Morus ; chemistry ; Quality Control ; Stilbenes ; chemistry ; isolation & purification