Humans ; Hypertension, Pulmonary ; diagnosis ; therapy

ATP-Binding Cassette Transporters ; metabolism ; Adenocarcinoma ; genetics ; metabolism ; pathology ; Adult ; Aged ; Blotting, Western ; Female ; Humans ; Immunohistochemistry ; Lung ; metabolism ; pathology ; Lung Neoplasms ; genetics ; metabolism ; pathology ; Male ; Middle Aged ; Neoplasm Staging ; RNA, Messenger ; metabolism ; Reverse Transcriptase Polymerase Chain Reaction

OBJECTIVETo study clinical effects of the over-articular external fixator combined with limited internal fixation for the treatment of Pilon fractures caused by high energy.

METHODSFrom September 2003 to April 2011, 36 patients with Pilon fractures caused by high energy were treated with the over-articular external fixator combined with limited internal fixator. There were 25 males and 11 females, ranging in age from 16 to 72 years old,with an average of 38 years old. The diagnoses of all patients were determined by conventional X-ray examination or three-dimensional spiral CT examination. The AOFAS scoring criteria was used to evaluate the therapeutic effects. The patients with comminuted fractures were treated with screw or Kirschner wire fixation without uncovering periost so as to enhance stability between fracture end and bone blocks,followed by the fixation with over-articular external fixators.

RESULTSAll the patients were followed up, and the duration ranged from 4 to 27 months, with an average of 13 months. Thirty-two patients got wound healing at the first stage. And the bone union duration ranged from 2 to 6 months, with a mean of 3 months. According to the AOFAS ankle-hindfoot subjective scoring standard, 13 patients got an excellent result, 20 good and 3 fair, with an score of 88.2 +/- 3.6. Twelve patients had infections at pinhole, 5 patients had pinhole pain. One patient had the fixator broken induced by over loading, who was cured after treatment. There were no complications such as nerve or vascular injuries, or osteomyelitis.

CONCLUSIONThe over-articular external fixation combined with limited internal fixation for the treatment of Pilon fractures caused by high energy is an ideal method, which has such advantages as reliable fixation, simple operation, coincidence with principles of biomechanical fixation, and benefit for fracture healing.

Adolescent ; Adult ; Aged ; Ankle Injuries ; diagnostic imaging ; surgery ; Ankle Joint ; diagnostic imaging ; surgery ; External Fixators ; Female ; Fracture Fixation ; Fracture Fixation, Internal ; Humans ; Internal Fixators ; Male ; Middle Aged ; Radiography ; Treatment Outcome ; Young Adult

OBJECTIVETo evaluate the efficacy and safety of entecavir (ETV) as a long-term treatment in patients with lamivudine (LAM)-refractory chronic hepatitis B (CHB).

METHODSIn this phase II study of ETV-056, 32 CHB patients with resistance to LAM monotherapy were administered ETV at 1.0 mg/day and monitored over a period of 8 years. The virologic, serologic and biochemical responses were measured throughout the treatment course. Outcomes analysis was conducted according to intention-to-treat principles.

RESULTSAt baseline and treatment weeks 8, 12, 24, 48, 96, 144, 192, 240, and 420, the proportion of patients with HBV DNA less than 300 copies/ml was 0, 6.3% (2/32), 9.4% (3/32), 18.8% (6/32), 18.8%(6/32), 46.9% (15/32), 43.8% (14/32), 50.0% (16/32), 50.0% (16/32), and 62.5% (20/32). At treatment weeks 48, 96, 168, 192, 240, and 420, the proportion of patients experiencing virological breakthrough was 6.1% (2/32), 9.4% (3/32), 12.5% (4/32), 18.8%(6/32), 25.0%(8/32), and 28.1% (9/32). In the 8 year study period, 32.3% (10/31) of patients achieved HBs seroconversion and four patients achieved HBe seroconversion.

CONCLUSIONWhile treatment with 1.0 mg/day ETV for up to 8 years resulted in mild HBV DNA suppression and increase of HBeAg seroconversion, the safety profile of this therapy was good but the economic cost was high and virological breakthrough rates were high.

Adolescent ; Adult ; Antiviral Agents ; adverse effects ; therapeutic use ; Drug Resistance, Viral ; Female ; Guanine ; adverse effects ; analogs & derivatives ; therapeutic use ; Hepatitis B, Chronic ; drug therapy ; Humans ; Lamivudine ; therapeutic use ; Male ; Middle Aged ; Treatment Failure ; Treatment Outcome ; Young Adult

OBJECTIVETo evaluate the efficacy and safety of entecavir (ETV) in treating lamivudine refractory chronic hepatitis B (CHB) patients.

METHODSThis was part of a multicenter, double-blinded, randomized (4:1) and placebo-controlled trial comparing the safety and efficacy of ETV (1.0 mg once q.d.) for 12 weeks in lamivudine refractory CHB patients. All patients were treated with ETV (1.0 mg q.d.) for 168 weeks. During the treatment period, HBV DNA levels were regularly measured by quantitative PCR. Liver function tests, HBV serology and safety assessments were also conducted.

RESULTSThe mean of HBV DNA log10 decreased from 9.14 to 6.27 at week 2, decreased to 6.28 at week 4, to 5.46 at week 8, to 5.10 at week 12, to 4.49 at week 24, to 4.41 at week 48, to 3.91 at week 96, to 4.05 at week 144, and decreased to 4.21 at week 168. The proportion of HBV DNA more than 10(5) copies/ml gradually dropped from 100% at baseline to 46.43% at week 12 and to 17.86% at week 96. HBV DNA less than 10(3) copies/ml raised from 0 at baseline to 7.14% at week 8, to 10.71% at week 12, to 46.43% at week 96, and raised to 57.14% at week 168. The proportion with HBeAg seroconversion was 10.07% at the end of the study. The mean of ALT became normal at week 12 and remained normal throughout week 168. There was one patient who had a severe adverse event during the trial.

CONCLUSIONETV can effectively inhibit the replication of HBV DNA and normalize the levels of ALT in lamivudine refractory CHB patients, and from our study we think the use of ETV is safe.

Adult ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; Double-Blind Method ; Female ; Guanine ; analogs & derivatives ; therapeutic use ; Hepatitis B virus ; drug effects ; physiology ; Hepatitis B, Chronic ; drug therapy ; Humans ; Lamivudine ; therapeutic use ; Treatment Failure ; Virus Replication ; drug effects ; Young Adult

OBJECTIVETo evaluate the efficacy and safety of five-year trail of entecavir for chronic hepatitis B patients failed with lamivudine therapy in the Chongqing area.

METHODS32 patients failed with lamivudine therapy were enrolled in this study. In the double-blind phase, patients were randomly divided into entecavir 1.0 mg/d group (n = 28) and placebo group(n = 4) for 12 weeks. In the open-lable phase, patients received ETV 1.0 mg/d for 240 weeks. HBV DNA level, liver function, HBV serology were observed.

RESULTSThe mean reduction in HBV DNA level at week 12 was 4.05 log10 copies/ml in ETV group, and 0.08 log10 copies/ml in placebo group (P less than 0.05). The mean of HBV DNA level after 240 weeks of ETV treatment was decreased to 2.58 log10 copies/ml. The proportion of patients with HBV DNA less than 3 log10 copies/ml was 0, 6.25%, 15.6% , 50%, and 57.14% at 0, 8, 24, 96 and 240 weeks respectivfely. There were 2 patients with HBsAg seroconversion and 4 patients with HBeAg seroconversion at the end of the study. The ALT level returned to normal at week 12 and remained normal throughout the following 240 weeks. One patient had a severe adverse event during the trail.

CONCLUSIONEntecavir is effective and safe for the chronic hepatitis B patients failed with lamivudine therapy.

Adult ; Alanine Transaminase ; blood ; Antiviral Agents ; administration & dosage ; therapeutic use ; DNA, Viral ; blood ; Double-Blind Method ; Drug Resistance, Viral ; Female ; Guanine ; administration & dosage ; analogs & derivatives ; therapeutic use ; Hepatitis B Surface Antigens ; analysis ; Hepatitis B e Antigens ; analysis ; Hepatitis B, Chronic ; drug therapy ; virology ; Humans ; Lamivudine ; administration & dosage ; therapeutic use ; Male ; Time Factors ; Treatment Outcome ; Virus Replication ; drug effects ; Young Adult

Antiviral Agents ; pharmacology ; therapeutic use ; DNA, Viral ; blood ; Hepatitis B ; blood ; drug therapy ; virology ; Hepatitis B Surface Antigens ; blood ; Hepatitis B e Antigens ; blood ; Hepatitis B virus ; drug effects ; physiology ; Humans ; Interferon-alpha ; pharmacology ; therapeutic use ; Kinetics ; Lamivudine ; pharmacology ; therapeutic use ; Models, Statistical ; Viral Load

AIMIn order to look for new active compounds, the structure of (+)-praeruptorin A is modified.

METHODS(+)-Praeruptorin A was isolated from the root of Peucedanum praeruptorum, basic hydrolysis of (+)-praeruptorin A and acyled reactions of hydrolysis product of (+)-praeruptorin A were carried out.

RESULTSEighteen compounds were semi-synthesized from (+)-praeruptorin A.

CONCLUSIONFourteen compounds (5-18) among them are new compounds. Preliminary bioactivity assay indicated that the new compounds show calcium antagonist activity, but they are not as strong as (+)-praeruptorin A.

Animals ; Aorta, Thoracic ; drug effects ; Apiaceae ; chemistry ; Calcium Channel Blockers ; chemical synthesis ; isolation & purification ; pharmacology ; Coumarins ; chemical synthesis ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; chemical synthesis ; isolation & purification ; pharmacology ; Molecular Structure ; Muscle Contraction ; drug effects ; Muscle, Smooth, Vascular ; drug effects ; Plants, Medicinal ; chemistry ; Rats

A sensitive, rapid and accurate liquid chromatography-tandem mass spectrometric (LC-MS/MS) method with pre-column derivatization was developed for the simultaneous determination of erdosteine and its thiol-containing active metabolite in human plasma. Paracetamol and captopril were chosen as the internal standard of erdosteine and its active metabolite, respectively. Aliquots of 100 microL plasma sample were derivatized by 2-bromine-3'-methoxy acetophenone, then separated on an Agilent XDB-C18 (50 mm x 4.6 mm ID, 1.8 microm) column using 0.1% formic acid methanol--0.1% formic acid 5 mmol x L(-1) ammonium acetate as mobile phase, in a gradient mode. Detection of erdosteine and its active metabolite were achieved by ESI MS/MS in the positive ion mode. The linear calibration curves for erdosteine and its active metabolite were obtained in the concentration ranges of 5-3 000 ng x mL(-1) and 5-10 000 ng x mL(-1), respectively. The lower limit of quantification of erdosteine and its active metabolite were both 5.00 ng x mL(-1). The pharmacokinetic results of erdosteine and its thiol-containing active metabolite showed that the area under curve (AUC) of the thiol-containing active metabolite was 6.2 times of that of erdosteine after a single oral dose of 600 mg erdosteine tables in 32 healthy volunteers, The mean residence time (MRT) of the thiol-containing active metabolite was (7.51 +/- 0.788) h, which provided a pharmacokinetic basis for the rational dosage regimen.
Administration, Oral ; Area Under Curve ; Chromatography, Liquid ; Female ; Humans ; Male ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry ; Thioglycolates ; administration & dosage ; blood ; metabolism ; pharmacokinetics ; Thiophenes ; administration & dosage ; blood ; metabolism ; pharmacokinetics

OBJECTIVETo study the stability of chlorogenic acid, cynaroside and 3,5-O-discaffeoylquinc acid in Hangbaiju and Gongju and to predict their term of validity.

METHODHangbaiju and Gongju were incubated in an environmental chamber at different temperatures and relative humidities. After the incubation, quantitative determination of chlorogenic acid, cynaroside, 3,5-O-discaffeoylquinc acid in Hangbaiju and Gongju were measured by HPLC. The effective period of the preparation was calculated according to Arrhinius index law. Quantitative determination of 3,5-O-discaffeoylquinc acid, cynaroside, chlorogenic acid in Hangju and Gongju were analyzed by HPLC.

RESULTThe stable life of Hangbaiju has been determined as 2.25 years. The stable life of Gongju has been determined as 4.31 years.

CONCLUSIONThe high temperature is not conducive to the stability of Hangbaiju and Gongju, which needs to be placed in a dark and cool place.

Chlorogenic Acid ; analysis ; Chromatography, High Pressure Liquid ; Chrysanthemum ; chemistry ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Temperature