Re-evaluation of bioequivalence of generic drugs is one of the key research focus currently. As a means to ensure consistency of the therapeutic effectiveness of drug products, clinical bioequivalence has been widely accepted as a gold standard test. In vitro dissolution testing based on the theory of the BCS is the best alternative to in vivo bioequivalence study. In this article, the conventional dissolution method and flow-through cell method were used to investigate the dissolution profiles of domestic amoxicillin capsules in different dissolution media, and the absorption behavior of the drugs with different release rates (t85% = 15-180 min) in the gastrointestinal tract was predicted by Gastro Plus. The flow-through cell method was thought better to reflect the release characteristics in vivo, and amoxicillin capsules with regard to the release rates up to 45 min (t85% = 45 min) were having a satisfied bioequivalence with the oral solution according to the C(max) and AUC. Although two different dissolution profiles of domestic amoxicillin capsules were found by flow-through cell methods, prediction results revealed that domestic capsules were probably bioequivalent to each other.
Amoxicillin ; pharmacokinetics ; Capsules ; Computer Simulation ; Gastrointestinal Tract ; Humans ; Software ; Solubility ; Therapeutic Equivalency

Powder X-ray diffraction (PXRD) technology combined with cluster analysis method was used to classify 75 batches of crystalline ceftriaxone sodium into subtypes, the crystalline characteristics of each subtype were measured with scanning electron microscope (SEM). By comparing some parameters of these subtypes correlated to crystallization process of ceftriaxone sodium, such as salification rate, water content in different subtypes, as well as by studying different lattice stabilities, different compatibilities with rubber closures during accelerated stability tests, the key point to improve the quality of domestic ceftriaxone sodium was disclosed. The results of this paper indicated that the fine structure of the products could be controlled well by improving the salification and crystallization process. As a result, the subtype II of ceftriaxone sodium with high stability can be produced.
Ceftriaxone ; chemistry ; classification ; Crystallization ; Microscopy, Electron, Scanning ; Powders ; Water ; X-Ray Diffraction

OBJECTIVETo investigate the effect of sea cucumber cerebroside(SCC) and its long-chain base(LCB) on lipid and glucose metabolism in obese mice.

METHODSThe mouse obese model was established by feeding high fat diet. The mice were randomly assigned to 4 groups: control group, model group, SCC group and LCB group. After 4 weeks, the glucose tolerance test was undertaken. After 5 weeks, the body fat content, organic indexes, serum lipid level, glycemic index and liver lipid level were determined.

RESULTSCompared with the model group, the glucose tolerance in the SCC group and LCB group was ameliorated significantly (P<0.01, P<0.05); glycemic index (P<0.01, P<0.01), the weight of adipose tissue (P<0.05, P<0.01) and the hepatic TG were reduced significantly (P<0.05, P<0.05).

CONCLUSIONSea cucumber cerebroside and its long-chain base can improve the glucose and lipid metabolism in obese mice.

Animals ; Blood Glucose ; metabolism ; Cerebrosides ; pharmacology ; Lipid Metabolism ; Lipids ; blood ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Obese ; Obesity ; blood ; drug therapy ; Sea Cucumbers ; chemistry

Objective To investigate the dynamics and development trends of drinking water type of endemic fluorosis after water improvement in Xinbaerhuyouqi of Hulunbeir city, Inner Mongolia and to provide a scientific evidence for the development of countermeasures. Methods We mainly selected Adunchulusumu and Kerlunsumu in Xinbaerhuyouqi of Hulunbeir city as the two monitoring points after water improvement in 2000 -2009. Of these, 1 sample of centralized water supply source water and 3 samples of tap water and 5 samples of noncentralized water supply source water according to water well locations of east, west, south, north and center were collected and the levels of water fluoride were tested; the prevalence of dental fluorosis of school children aged 8 to 12 were examined; from 2002 onwards, the urine samples of 30 children aged 8 to 12(five age groups, six urine samples for each age group) were collected, and all urine samples were collected in the case of less than 30, and urine fluoride was tested. Dental fluorosis was diagnosed using Dean method; water fluoride was tested using fluoride ion selective electrode(WS/T 106-1999); urinary fluoride was tested by determination of fluoride in urine using ion-selective electrode(WS/T 89-1996). Results In 2000 - 2009, the mean levels of fluorine in drinking water in Adunchulusumu and Kerlunsumu were 1.79 - 4.35 mg/L and 1.38 - 3.18 mg/L, respectively; the detection rate of dental fluorosis of children aged 8 to 12 were 45.24％(19/42) - 89.78％(123/137) and 40.00％ (28/70) - 74.47％ (70/94), respectively; the median urinary fluoride of them were 2.30 - 4.15 mg/L and 2.73 - 4.55 mg/L, respectively. ConclusionsThe detection rate of children's dental fluorosis remains high in Xinbaerhuyouqi during the past 10 years after changing water. The endemic fluorosis remains a serious disease. Effective prevention and control measures must be taken to control the occurrence of fluorosis in the future.

Objective To establish a method to determine the contents of total flavonoids and shikimic acid in pine needles of Pinus massoniana Lamb.in Wudang Area.Methods Rutin was used as reference standard,and the content of total flavonoids in pine needles of Pinus massoniana Lamb. was determined by UV spectrometry at wavelength of 500 nm. The content of shikimic acid was determined by HPLC-DAD. The Fortis Xi C8 column (5 μm, 250 mm × 4.6 mm) was adopted with acetonitrile - 0.4% phosphoric acid solution (8:92, V/V) as mobile phase at the flow rate of 0.9 mL/min. The detection wavelength was 213 nm; the column temperature was 30 ℃; the injection volume was 20 μL. Results The linear range was 8.26-49.54 μg for rutin (r=0.999 4) with an average recovery of 99.2%, RSD=1.94%. The linear range was 10.26-61.56 μg for shikimic acid (r=0.999 4) with an average recovery of 99.5%,RSD=1.93%.The contents of total flavonoids in pine needles of Pinus massoniana Lamb.was 28.33 mg/g, and shikimic acid was 15.25 mg/g, respectively. Conclusion The method is simple, rapid, accurate and reproducible. It can be used for the content determination of total flavonoids and shikimic acid in pine needles of Pinus massoniana Lamb. in Wudang Area.

Amino Acids ; blood ; Amino Acids, Branched-Chain ; blood ; Capsules ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Hepatitis B, Chronic ; blood ; drug therapy ; Humans ; Liver Cirrhosis ; blood ; drug therapy ; Male ; Phytotherapy

OBJECTIVETo construct a replication-defective recombinant adenovirus expressing the ORF2 (112-660aa) antigen of hepatitis E virus (HEV) and evaluate its immunization effect in BALB/c mice by mucosal inoculation.

METHODSThe HEV ORF2 gene encoding for 112-660aa was amplified from plasmid pUC-HEV and inserted into the transfer vector pTrack-CMV. The recombinant plasmid and adenoviral backbone plasmid pAdEasy-1 were co-transformed into E. coli strain BJ5183. Taking the advantage of the high efficient homologous recombination machinery presented in bacteria, the recombinant adenovirus backbone plasmid was generated in BJ5183, and then was transfected into 293 cells. Recombinant Adenoviruses were propagated in 293 cells with high titers. 8-week-old BALB/c mice were inoculated intraperitoneally and intranasally with 10(7) pfu recombinant adenovirus each on weeks 0, 3, 5, 7, 10.

RESULTSBoth groups of mice induced humoral IgG immune response with the highest titers 1:1,000 and 1:10,000 each. Only the group inoculated intranasally could induce mucosal IgA immune response.

CONCLUSIONSThe adenoviral recombinant can stimulate specific humoral and mucosal immune response in mice and is potentially to be used as a candidate vaccine for the treatment of HEV infection.

Adenoviruses, Human ; genetics ; Animals ; Hepatitis Antigens ; genetics ; immunology ; Immunoglobulin A ; immunology ; Immunoglobulin G ; immunology ; Male ; Mice ; Mice, Inbred BALB C ; Nasal Mucosa ; immunology ; Peritoneum ; immunology ; Recombinant Proteins ; biosynthesis ; genetics ; immunology ; Viral Hepatitis Vaccines ; Viral Proteins ; biosynthesis ; genetics ; immunology

A quantitative analytical method of ultra-high performance liquid chromatography (UPLC) was developed for simultaneously determining twelve components in Tibetan medicine Zuozhu Daxi. SIMPCA 12.0 software was used a principal component analysis PCA) and partial small squares analysis (PLSD-DA) on the twelve components in 10 batches from four pharmaceutical factories. Acquity UPLC BEH C15 column (2.1 mm x 100 mm, 1.7 µm) was adopted at the column temperature of 35 °C and eluted with acetonitrile (A) -0.05% phosphate acid solution (B) as the mobile phase with a flow rate of 0. 3 mL · min(-1). The injection volume was 1 µL. The detection wavelengths were set at 210 nm for alantolactone, isoalantolactone and oleanolic; 260 nm for trychnine and brucine; 288 nm for protopine; 306 nm for protopine, resveratrol and piperine; 370 nm for quercetin and isorhamnetin. The results showed a good separation among index components, with a good linearity relationship (R2 = 0.999 6) within the selected concentration range. The average sample recovery rates ranged between 99.44%-101.8%, with RSD between 0.37%-1.7%, indicating the method is rapid and accurate with a good repeatability and stability. The PCA and PLSD-DA analysis on the sample determination results revealed a great difference among samples from different pharmaceutical factories. The twelve components included in this study contributed significantly to the quantitative determination of intrinsic quality of Zuozhu Daxi. The UPLC established for to the quantitative determination of the twelve components can provide scientific basis for the comprehensive quality evaluation of Zuozhu Daxi.
Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Quality Control ; Tibet

OBJECTIVETo investigate the effect of early intervention by pravastatin with two different dosage on inflammatory factors and endothelial vasodilator function in patients with unstable angina (UA).

METHODS108 patients with UA were investigated consecutively and divided randomly into three groups (group 20 mg, n = 37; group 10 mg, n = 37; group control, n = 34). Blood samples were examined at admission and 4, 8 weeks after the therapy of pravastatin. Fourty patients of UA were chosen from those three groups (15, 15 and 10 cases respectively). The endothelium-dependent vasodilation and the function of vascular endothelium of them were measured. In the dosage of 20 mg pravastatin group non-endothelium-dependent vasodilation in brachial artery was also tested by ultrasound before and 8 weeks after the therapy. Cardiac events were followed up for 2 months.

RESULTS(1) The use of pravastatin in early admission period of UA could significantly reduce inflammatory factors and improve vascular endothelium function, which was more obviously in the group of 20 mg/d than in group of 10 mg/d. These benefits occurred in 4th week and more obviously in 8th week after the therapy. (2) The lipid lowering therapy in the early stage of admission (24 - 48 h) resulted in the reduction of cardiac events in the hospital.

CONCLUSIONThe use of pravastatin 20 mg/d seems better than that of 10 mg/d in all the fields as above in early admission period of UA patients.

Adult ; Aged ; Angina, Unstable ; drug therapy ; Anticholesteremic Agents ; administration & dosage ; therapeutic use ; Female ; Follow-Up Studies ; Humans ; Inpatients ; Male ; Middle Aged ; Pravastatin ; administration & dosage ; therapeutic use ; Prospective Studies

OBJECTIVETo evaluate and analyze prognostic factors for surgical treatment of patients with neoadjuvant chemotherapy.

METHODSRecords of 256 patients who underwent operation after chemotherapy for lung cancer from June 1995 to May 2007 were reviewed retrospectively. Potential prognostic factors which were univariately and multivariately analyzed by COX proportional hazard regression model, included gender, age, p-TNM stage, size of tumor, metastasis of lymph node, histological type and operation extent. Kaplan-Meier method was used for survival curve and rate. However, survival difference was calculate by Log-rank test.

RESULTSEleven patients (4.3%) developed postoperative complications. Two hundred and thirty-six patients (92.2%) underwent radical resection (169 for lobectomies, 53 for pneumonectomies and 14 for extended resections). On the contrary, 20 cases had palliative resection. The overall 1-, 3- and 5-year survival rate was 79.3%, 38.7% and 27.0% respectively. Age, p-TNM stage, size of tumor, metastasis of lymph node and type of operation were valued as prognostic factors in COX univariate analysis, p-TNM stage (OR = 1.323, 95% CI: 1.068 to 1.641, P = 0.017) and age (OR = 1.562, 95% CI: 1.148 to 2.125, P = 0.005) were identified independent prognostic factors in COX multivariate analysis.

CONCLUSIONSLong-term outcome for lung cancer of patients with neoadjuvant chemotherapy are encouraging, p-TNM stage and surgical type are the crucial prognostic factors for surgical treatment of patients with neoadjuvant chemotherapy.

Adult ; Aged ; Aged, 80 and over ; Chemotherapy, Adjuvant ; Female ; Follow-Up Studies ; Humans ; Lung Neoplasms ; drug therapy ; Male ; Middle Aged ; Prognosis ; Retrospective Studies ; Survival Analysis ; Treatment Outcome