OBJECTIVE: To improve the in vitro dissolution of nimesulide by preparing nimesulide solid dispersion with hot melt extrusion (HME) technology. METHODS: Using PVP-VA64, PVP K30 or PVA-PEG (Kollicoat IR) as hydrophilic carrier, nimesulide solid dispersion was prepared by hot melt extrusion and characterized by drug dissolution, DSC, XRD and FTIR. RESULTS: Nimesulide exhibited rapid in vitro dissolution from the solid dispersion using PVP-VA64 as carrier. The cumulative release rate was 81% in 10 min, much faster than its physical mixture (only 37% in 1 h). The results of DSC and FTIR showed that nimesulide was amorphously dispersed in the carrier. CONCLUSION: Hot melt extrusion technology is suitable for preparing nimesulide-PVP-VA64 solid dispersion, which can significantly increase drug dissolution.

AIMTo study the chemical constituents of the rhizome of Matteuccia struthiopteris (L.) The constituents were separated and purified by column chromatography with normal Todaro.

METHODSphase silica gel and Sephadex LH-20. Their structures were identified on the basis of physical and spectral data (MS, NMR, HMBC and HMQC).

RESULTSFour compounds were isolated and identified as 1-O-beta-D-gl ucopyranosyl-(2S,3R,4E, 8Z) -2-N-(2'-hydroxydocosanoyl) eicosasphinga-4,8-dienine (1), 1-O-beta-D-galactosyl-(6-->1)-alpha-D-galactosyl-2,3-O-dihexadecanoyl-glycerol (2), succinic acid (3), D-mannitol (4).

CONCLUSIONCompounds 1 and 2 are new compounds. Compounds 3 and 4 were isolated from this plant for the first time.

Ferns ; chemistry ; Galactosides ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Glycerides ; chemistry ; isolation & purification ; Mannitol ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Succinic Acid ; chemistry ; isolation & purification

OBJECTIVETo study the chemical constituents in rhizome of Matteuccia struthiopteris.

METHODThe compounds were isolated by normal phase silica gel chromatography. The structures were identified by physical and spectral data.

RESULTSix compounds were isolated and identified as woodwardic acid (1), ergost-6,22-diene-3beta,5alpha,8alpha-triol (2), apigenin (3), riboflavin (4), 4-O-beta-D-glucopyranosyl-p-coumaric acid (5), 4-O-beta-D-glucopyranosylcaffeic acid (6).

CONCLUSIONAll the compounds were obtained from this plant for the first time.

Apigenin ; chemistry ; isolation & purification ; Caffeic Acids ; chemistry ; isolation & purification ; Dryopteridaceae ; chemistry ; Glucosides ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Riboflavin ; chemistry ; isolation & purification

OBJECTIVETo examine how the thymidine phosphorylase (TP) gene expression is upregulated by interferon-alpha (IFN-alpha) in human hepatocellular carcinoma SMMC-7721 cells.

METHODSTP mRNA levels were determined by RT-PCR. Whether the JAK-STAT cascade mediates IFN-alpha-induced TP mRNA expression was studied by pretreatment with Janus Kinase (JAK) inhibitor, AG-490. Effects of IFN-alpha on TP mRNA stability were detected with additional actinomycin D.

RESULTSThe expression of TP mRNA was induced by IFN-alpha in a dose- and time-dependent manner in SMMC-7721 (human hepatocellular carcinoma) cells. TP mRNA levels rose at 8 h, reached the peak value at 12 h, and remained at a high level up to 72 h in SMMC-7721 cells treated with IFN-alpha 10000 U/ml. IFN-alpha at a dose of 5000 or 10000 U/ml up-regulated TP expression about 3 fold compared with that of non-treated cells (P < 0.05). Induction of TP mRNA expression by IFN-alpha was significantly inhibited in SMMC-7721 cells by pretreatment with AG-490, in comparison with that treated with IFN-alpha alone. Pretreatment of SMMC-7721 cells with IFN-alpha 10000 U/ml for 24 h caused a substantial stabilization of TP mRNA, with a half-live of 35.8 h, compared with 8.5 hr in the control SMMC-7721 cells.

CONCLUSIONIFN-alpha at certain doses upregulates TP mRNA expression via both JAK-STAT transcriptional activation and post-transcriptional mRNA stabilization in human hepatocellular carcinoma SMMC-7721 cells.

Carcinoma, Hepatocellular ; enzymology ; pathology ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Enzyme Inhibitors ; pharmacology ; Gene Expression Regulation, Neoplastic ; Humans ; Interferon-alpha ; administration & dosage ; pharmacology ; Janus Kinases ; metabolism ; Liver Neoplasms ; enzymology ; pathology ; RNA, Messenger ; metabolism ; STAT1 Transcription Factor ; metabolism ; Thymidine Phosphorylase ; biosynthesis ; genetics ; Transcriptional Activation ; drug effects ; Tyrphostins ; pharmacology

OBJECTIVETo study the distribution of prevalence on hypercholesterolemia and borderline high cholesterol of Chinese residents aged 20 years and above.

METHODSTo detect the total fasting plasma cholesterol in 48 299 subjects among 20 year-olds and above.

RESULTSWithin a certain age range, the prevalence of both hypercholesterolemia and borderline high cholesterol increased with age, but there was a decreasing trend after 60-years of age in some regions. The prevalence of hypercholesterolemia increased to 12.53% in over 70 year-olds group from 1.36% in urban 20-year-olds, and increased to 5.15% from 60-year-olds group comparing to 0.98% of the 20-year-old group in rural areas. When comparing to the 20-year-old age group, the prevalence of borderline high cholesterol of the 70 age group in urban and rural increased by 4.4 and 4.2 times, respectively. The prevalence of hypercholesterolemia in each age group in urban were higher than that of in rural areas. In Rural I, it was higher than that of in Rural II , Rural III and Rural IV. The prevalence rates of both hypercholesterolemia and borderline high cholesterol of the males in the less than 50 year-olds group were higher than that in females, which was quite different from the group older than 50 years of age. As to borderline high cholesterol, similar result was also noticed.

CONCLUSIONWithin a certain age range, there was a trend that the prevalence of both hypercholesterolemia and borderline high cholesterol increased with age and related to regions which were classified by economic status. A distinct difference between males and females also existed.

Adult ; Age Factors ; Aged ; Asian Continental Ancestry Group ; China ; epidemiology ; Cholesterol ; blood ; Female ; Humans ; Hypercholesterolemia ; epidemiology ; Male ; Middle Aged ; Prevalence ; Rural Population ; Sex Factors ; Urban Population ; Young Adult

OBJECTIVETo investigate the plasma lipid levels in a national representative sample of subjects and to determine the prevalence of dyslipidemia in the Chinese population.

METHODSPlasma lipid profile was analyzed using the data obtained during the Chinese national nutrition and health survey (CNHS) in 2002 which involved 14 252 participants at the age of 18 years or older.

RESULTSThe mean levels of total cholesterol (TC), triglyceride (TG) and high density lipoprotein cholesterol (HDL-C) in the participants were 3.81 mmol/L, 1.10 mmol/L, and 1.30 mmol/L, respectively. In the groups of participants at the age of 18-44 years, 45-59 years, and over 60 years the mean TC level was 3.70 mmol/L, 4.09 mmol/L and 4.21 mmol/L, respectively, and the mean TG level was 07 mmol/L, 1.21 mmol/L, 1.20 mmol/L, 1.29 mmol/L, 1.33 mmol/L, and 1.33 mmol/L, respectively. The prevalence of dyslipidemia in Chinese adults was 18.6% and 22.2% in males and 15.9% in females. Dyslipidemia prevalence was higher in urban districts than in rural areas (21.0% vs. 17.7%). The prevalence of hypercholesterolemia, hypertriglyceridemia, and low HDL cholesterol was 2.9%, 11.9%, and 7.4% respectively among the participants.

CONCLUSIONDyslipidemia has become one of the important health risk factors in the Chinese population. There is no significantly difference in the prevalence of dyslipidemia between the groups of participants at the age of 45-59 years and over 60 years. This study provides important lipid profile data for policy making and guideline development for the prevention of dyslipidemia in the Chinese population.

Adolescent ; Adult ; China ; epidemiology ; Dyslipidemias ; blood ; epidemiology ; Female ; Humans ; Lipids ; blood ; classification ; Male ; Middle Aged ; Prevalence

OBJECTIVETo study the difference in prevalence of dyslipidemia, hypercholesterolemia, hypertriglyceridemia and low blood high-density lipoprotein cholesterol (HDL-C) between the residents of urban and rural areas of varied regions in China.

METHODSFasting plasma levels of total cholesterol, triglyceride and HDL-C were determined with the enzyme methods for 49,252 subjects aged 18 and over during August to December, 2002.

RESULTSPrevalence of dyslipidemia in Chinese adults aged 18 and over was 18.6%, with 17.0%, 22.9% and 23.4% in the groups of 18-44, 45-59 and over 60 years old, respectively, 22.2% and 15.9% in males and females, respectively, and 21.0% and 17.7% in urban and rural areas, respectively. Prevalence of hypercholesterolemia, hypertriglyceridemia and low blood HDL-C in those aged 18 and over was 2.9%, 11.9% and 7.4%, respectively.

CONCLUSIONSDyslipidemia has become one of important risk factors threatening health of Chinese people, with hypertriglyceridemia and low blood HDL-C as two major types in those aged 18 and over. Prevalence of dyslipidemia was nearly the same in the middle-aged and in the elderly people, and not significantly different in those living in urban areas from those in rural areas. It is very important to pay more attention to earlier comprehensive prevention and control of dyslipidemia.

Adult ; Aged ; Aged, 80 and over ; China ; epidemiology ; Cholesterol ; blood ; Cholesterol, HDL ; blood ; Cholesterol, LDL ; blood ; Dyslipidemias ; blood ; epidemiology ; Female ; Humans ; Hypertriglyceridemia ; blood ; epidemiology ; Male ; Middle Aged ; Prevalence ; Rural Population ; statistics & numerical data ; Triglycerides ; blood ; Urban Population ; statistics & numerical data ; Young Adult

OBJECTIVETo study plasma total cholesterol (TC), triglyceride (TG), high density lipoprotein cholesterol (HDL-C) levels of Chinese adults among different areas in China.

METHODSAnalysis of fasting plasma lipid in 49,252 subjects aged 18 years and above was made.

RESULTSThe mean TC, TG and HDL-C were 3.81 mmol/L, 1.10 mmol/L and 1.30 mmol/L, respectively. The mean TC, TG and HDL-C is 3.96 mmol/L, 1.16 mmol/L, 1.30 mmol/L in adults in urban and 3.75 mmol/L, 1.07 mmol/L and 1.30 mmol/L in adults in rural areas. In age groups of 18 - 44 years, 45 - 59 years and 60 years above, the mean values were 3.70 mmol/L, 4.09 mmol/L, 4.21 mmol/L for TC; 1.07 mmol/L, 1.21 mmol/L, 1.20 mmol/L for TG; and 1.29 mmol/L, 1.33 mmol/L, 1.33 mmol/L for HDL-C.

CONCLUSIONThe results of this study might provide the national representative data of plasma lipid level. TC and TG levels of adults in urban might be higher than those adults in rural. With increasing of age, the plasma TC level should be increased. There is no significant difference in TG levels between the adults aged 45-49 years and over 60 years, while the TG level of both age groups should be higher than those of adults aged 18-44 years.

Adult ; Age Distribution ; China ; Cholesterol ; blood ; Cholesterol, HDL ; blood ; Female ; Humans ; Lipids ; blood ; Male ; Middle Aged ; Rural Population ; statistics & numerical data ; Sex Distribution ; Triglycerides ; blood ; Urban Population ; statistics & numerical data ; Young Adult

OBJECTIVETo study the guidance of four column theory in decision making of Pilon fractures and its result.

METHODSNinety-one cases of Pilon fractures classified by four column method and treated by open reduction internal fixation (ORIF) were reviewed from March 2005 to June 2009. Four column classification:lateral column of 67 cases were involved, posterior column of 34 cases were involved, medial column of 34 cases were involved and anterior column of 34 cases were involved. Among all the 94 fractures, single column of 20 fractures were involved, 2 columns of 49 fractures were involved, 3 columns of 15 fractures were involved and all of 4 columns of 10 fractures were involved.

RESULTSEighty-nine cases had been followed up. The average follow-up time was 16.2 months ranging between 6.0 and 39.0 months. The average healing time was 3.7 months ranging from 3.0 to 5.0 months. Reduction of 91% reviewed Pilon cases were good or acceptable according to Burwell and Charley's radiology evaluation system. Ankle function of 87.6% cases were excellent or good according to AOFAS evaluation system.

CONCLUSIONAs a simple and comprehensive classification, four column classification can contribute to reasonable operating decision making and good prognosis of Pilon fracture.

Adolescent ; Adult ; Aged ; Aged, 80 and over ; Decision Making ; Female ; Follow-Up Studies ; Fracture Fixation, Internal ; methods ; Humans ; Male ; Middle Aged ; Retrospective Studies ; Tibial Fractures ; surgery ; Treatment Outcome ; Young Adult

BACKGROUNDThe role of gastro-protecting agents on symptomatic chronic gastritis is unclear. This multicenter, open, randomized trial was designed to compare the comprehensive effects of gefarnate with sucralfate on erosive gastritis with dyspeptic symptoms.

METHODSTotally 253 dyspepsia patients confirmed with erosive gastritis were enrolled from six centers in China. They randomly received either daily 300 mg gefarnate or 3 g sucralfate for six weeks. The primary endpoint was the effective rate of both treatments on endoscopic erosion at week six.

RESULTSGefarnate showed an effective rate of 72% and 67% on endoscopic score and dyspeptic symptom release, which is statistically higher than sucralfate (40.1% and 39.3%, P < 0.001, intension-to-treat). For histological improvement, gefarnate showed both effective in decreasing mucosal chronic inflammation (57.7% vs. 24.8%, P < 0.001, intension-to-treat) and active inflammation (36.4% vs. 23.1%, P < 0.05, intension-to-treat) than the control. A significant increase of prostaglandins and decrease of myeloperoxidase in mucosa were observed in gefarnate group. Severity of erosion is non-relevant to symptoms but Helicobacter pylori (H. pylori) status does affect the outcome of therapy.

CONCLUSIONSGefarnate demonstrates an effective outcome on the mucosal inflammation in patients with chronic erosive gastritis. Endoscopic and inflammation score should be the major indexes used in gastritis-related trials.

Adolescent ; Adult ; Aged ; Anti-Ulcer Agents ; therapeutic use ; Dyspepsia ; drug therapy ; Female ; Gastritis ; drug therapy ; Gefarnate ; therapeutic use ; Humans ; Male ; Middle Aged ; Sucralfate ; therapeutic use ; Treatment Outcome ; Young Adult