Oleanolic acid-precipitated calcium carbonate solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry and scanning electron microscopy (SEM). And its in vitro release also was investigated. The properties of the precipitated calcium carbonate was studied which was as a carrier of oleanolic acid solid dispersion. Differential scanning calorimetry analysis suggested that oleanolic acid may be present in solid dispersion as amorphous substance. The in vitro release determination results of oleanolic acid-precipitated calcium carbonate (1: 5) solid dispersion showed accumulated dissolution rate of.oleanolic acid was up to 90% at 45 min. Accelerating experiment showed that content and in vitro dissolution of oleanolic acid solid dispersion did not change after storing over 6 months. The results indicated that in vitro dissolution of oleanolic acid was improved greatly by the solid dispersion with precipitated calcium carbonate as a carrier. The solid dispersion is a stabilizing system which has actual applied value.
Calcium Carbonate ; chemistry ; Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Drug Carriers ; chemistry ; Drug Stability ; Microscopy, Electron, Scanning ; Oleanolic Acid ; chemistry ; Plant Extracts ; chemistry ; Solubility

Objective To analyze the drug resistance profile and risk factors for extensively drug resistant tuberculosis (XDR-TB) patients. Methods XDR-TB cases were identified by sixteen anti-TB drug susceptibility kits among inpatients with a diagnosis of laboratory-confirmed mycobacterium tuberculosis. Single-factor and Logistic analysis were used to analyze the risk factors for drug resistant of the first and second-line anti-TB drugs in XDR-TB patients. Results Resistant rate of rifampin, isoniazid and rifampicin were 100%, Resistant rate of streptomycin, rifampicin and dean, b sulfur isoniazid, levofloxacin and capreomycin were from 90% to 100%, resistant rate of kanamycin and amino salicylic acid were from 70% to 80%, resistant rate of amikacin from 60% to 70%, resistant rate of sulfur isoniazid was from 50% to 60%, resistant rate of ethambutol and moxifloxacin were from 40% to 50%, resistant rate of clarithromycin was from 10% to 20%, resistant rate of clofazimine 5.2%. 92.1% of XDR-TB patients were resistant to more than 10 anti-TB drugs, and the least of the patients were resistant to 6 anti-TB drugs.Logistic regression analysis showed the risk factors for XDR-TB first-and second-line anti-tb drugs included age ［20-40 year (OR=6.318, 95% CI:1.204-33.15, P=0.029;40-60 year (OR=4.772, 95% CI:0.973-23.392, P=0.054); 60 year (OR=41.366, 95% CI:2.909-588.265, P=0.006)］and anti-TB treatment history was retreatment(OR=28.013, 95% CI:3.357-233.766, P=0.002). Conclusions XDR-TB patients have serious drug resistance, but there were some drug treatable drug resistance types, and the risk factors mainly come from age and anti-TB treatment history.

In order to improve the dissolution in vitro of components by processing tanshinone with the pray drying method, the physical properties of tanshinone power was analyzed by BET, differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction, and its dissolution in vitro was also investigated. The results of characterization showed decreased power size and increased specific surface area of tanshinone powder, and its existence in an amorphous state. Within 4 h, the accumulated dissolutions of tanshinone I and tanshinone II(A) in components of tanshinone reached 78.3%, 81.9%, respectively. Therefore, the spray-drying method was conducive to enhance the dissolution of components of tanshinone.
Chemistry, Pharmaceutical ; methods ; Diterpenes, Abietane ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Particle Size ; Solubility

OBJECTIVETo prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific delivery and rapid drug release.

METHODBaicalin-eudragit S100 solid dispersion was prepared by using the solvent method. The microscopic structure and physicochemical properties were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared spectroscopy (IR). And its in vitro release was also investigated.

RESULTThe results of DSC and XRD analysis suggested that baicalin may be dispersed in solid dispersion in the amorphous state. IR results indicated a non-covalent bond effect may exist between baicalin and eudragit S100. The results of in vitro release determination showed that very few baicalins in pH 1.2 diluted hydrochloric acid solution for 2 h at the baicalin-eudragit S100 ratio of 1 : 6. The accumulated dissolution rate was less than 15% in pH 6.8 phosphate buffer solution for 4 h, but exceeding 90% in pH 7.6 phosphate buffer solution for 1 h.

CONCLUSIONThe prepared baicalin-eudragit S100 solid dispersion could achieve the objective of colon-specific delivery and rapid drug release, and helps increase the concentration of baicalin in colons.

Colon ; metabolism ; Flavonoids ; chemistry ; Hydrogen-Ion Concentration ; Polymethacrylic Acids ; chemistry ; Solubility ; Solvents ; chemistry ; X-Ray Diffraction ; methods

The experiment's aim was to optimize the processing technology of Xanthii Fructus which through comparing the difference of UPLC fingerprint and contents of toxicity ingredient in water extract of 16 batches of processed sample. The determination condition of UPLC chromatographic and contents of toxicity ingredient were as follows. UPLC chromatographic: ACQUITY BEH C18 column (2.1 mm x 100 mm, 1.7 microm) eluted with the mobile phases of acetonitrile and 0.1% phosphoric acidwater in gradient mode, the flow rate was 0.25 mL x min(-1) and the detection wavelength was set at 327 nm. Contents of toxicity ingredient: Agilent TC-C18 column (4.6 mm x 250 mm, 5 microm), mobile phase was methanol-0.01 mol x L(-1) sodium dihydrogen phosphate (35: 65), flow rate was 1.0 mL x min(-1), and detection wavelength was 203 nm. The chromatographic fingerprints 16 batches of samples were analyzed in using the similarity evaluation system of chromatographic, fingerprint of traditional Chinese medicine, SPSS16.0 and SIMCA13.0 software, respectively. The similarity degrees of the 16 batches samples were more than 0.97, all the samples were classified into four categories, and the PCA showed that the peak area of chlorogenic acid, 3,5-dicaffeoylquinic acid and caffeic acid were significantly effect index in fingerprint of processed Xanthii Fructus sample. The outcome of determination showed that the toxicity ingredient contents of all samples reduced significantly after processing. This method can be used in optimizing the processing technology of Xanthii Fructus.
Caffeic Acids ; analysis ; toxicity ; Chemistry, Pharmaceutical ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; toxicity ; Quinic Acid ; analogs & derivatives ; analysis ; toxicity ; Xanthium ; chemistry ; classification

To study the application characteristics of copovidone (PVP-S630) in Xinyueshu extracts during the spray drying process, and its effect on such pharmaceutical properties as micromeritics and drug release behavior. PVP-S630 was added into Xinyueshu extracts to study on the spray drying, the effect of different dosages of PVP-S630 against the wall sticking effect of the spray drying, as well as the power property of Xinyueshu spray drying power and the dissolution in vitro behavior of the effective component of hyperoside. The results showed that PVP-S630 revealed a significant anti-wall sticking effect, with no notable change in the grain size of the spray drying power, increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior of hyperoside. It was worth further studying the application of PVP-S630 in spray drying power of traditional Chinese medicine.
Absorption ; Desiccation ; methods ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Porosity ; Powders ; Pyrrolidines ; chemistry ; Vinyl Compounds ; chemistry ; Wettability

To apply chitooligosaccharide in the preparation of baicalin compound, in order to increase the drug dissolution in vitro, and investigate the basic property of the compound. Baicalin-chitooligosaccharide compound was prepared by using the solvent method. The structure and physicochemical properties of compound were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared vibrational spectrum (IR), and its dissolution behavior was also investigated. The results showed that the compound prepared at baicalin-chitooligosaccharide molar ratio of 1 : 1 could significantly improve the dissolution of baicalin. The results of DSC and XRD analysis suggested that baicalin may exist in an amorphous state. IR results indicated the interaction between baicalin and chitooligosaccharide. The baicalin-chitooligosaccharide compound could significantly improve dissolution in vitro of drug.
Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Oligosaccharides ; chemistry ; Spectroscopy, Fourier Transform Infrared

Objective To observe the effects of chloroquine phosphate on apoptosis of leukemic cell line U937, and investigate whether chloroquine phosphate induces leukemic cell apoptosis by normalizing protein PNAS-2's abnormal subcellular location. Methods Chloroquine phosphate of different concentrations were added into culture fluid of leukemic cell line U937 at logarithmic phase. MTr was used to measure cell proliferation, flow cytometry and laser confocal microscopy were applied to detect cell apoptosis, and immunofluorescence technology was employed to observe the effects of chloroquine phosphate on the changes of subcellular location of protein PNAS-2. Results Apoptosis of leukemic cell line U937 was significantly induced by 50 μg/mL chloroquine phosphate, and subcellular location of protein PNAS-2 was changed. Conclusion Chlorequine phosphate can induce apoptosis of leukemic cell line U937, and the mechanism may be related to the normalization of PNAS-2's abnormal subcellular location in U937 cell line. Chloroquine phosphate has the potential to be used in leukemic therapy.

Objective To investigate the awareness rate,treatment rate and control rate of mineral and bone disorder in patients with moderate or advanced stage chronic kidney disease (CKD). Methods The awareness rate,treatment rate and control rate of mineral and bone disorder were evaluated based on a questionnaire and related laboratory examinations in 503 CKD stage 3 to 5 patients. Results The awareness rate of mineral and bone disorder in patients with moderate or advanced stage CKD was highest in hemodialysis patients,moderate in peritoneal dialysis patients and lowest in non-dialyzed patients (all P ＜0.01).The total scores of the questionnaire were lowest in non-dialyzed patients [6 (5,8)] and were significantly higher in peritoneal dialysis [11 (9,12)] and hemodialysis patients [13 (11,15)] (P＜0.01).The extent of awareness was negatively correlated with age (r=-0.11,P＜0.05),and positively correlated with educational background (r=0.226,P＜0.01),duration of CKD (r=0.597,P＜0.01) and duration of dialysis (r=0.366,P＜0.01).The source of knowledge was mainly from publicity and education made by medical staff,which accounted for 94.0％,79.5％ and 69.4％ respectively in nondialyzed,peritoneal dialysis and hemodialysis patients.The treatment rate was significantly higher in peritoneal dialysis (88.6％) and hemodialysis patients (96.9％) than that in non-dialyzed patients (58.2％) (all P＜0.01).According to K/DOQI guideline,the control rate of serum calcium,phosphorus,calcium and phosphorus product and parathyroid hormone (PTH) were much better in non-dialyzed patients as compared to dialyzed ones.The percentage of number of lab indicators meeting the standard was significantly higher in non-dialyzed patients as compared to dialyzed ones (P＜0.01).According to KDIGO guideline,the control rate of serum phosphorus was significantly lower in hemodialysis patients (23.6％) than that in peritoneal dialysis (36.9％) and non-dialyzed patients (46.7％) (P＜0.01). Conclusions In non-dialyzed patients with moderate or advanced stage CKD,the awareness rate and treatment rate of mineral and bone disorder are relatively low,and the control rate is relatively high.Whereas in dialyzed patients,the awareness rate and treatment rate are relatively high,and the control rate is relatively low.

OBJECTIVETo isolate single chain antibody fragments (scFv) against cell surface molecules by pathfinder selection from an anti-KG1a cell scFv phage library.

METHODSThe anti-KG1a scFv library was enriched by KGla cell panning for three rounds, or unenriched, then processed for pathfinder selection respectively using anti-CD34 monoclonal antibody as pathfinder molecule. ScFv phage clones were randomly picked and identified by binding KG1a cells using immunofluorescein and flow cytometry. The KG1a+ clones were further identified by KG1a, HL60, U937, and CEM cell lines and ELISA. Their antigenic molecules on cell surface were digested by chymopapain and analyzed by flow cytometry. DNAs from ten positive clones were sequenced. The scFv clones with different primary structure were used to analyze the molecular weight of their antigens by Western blot.

RESULTSOne hundred and two KG1a+ scFv phage clones were isolated from 144 enriched and 96 unenriched scFv phage library respectively, among which 47 bound KG1a, HL60, U937, and CEM cells, 55 bound KG1a cells exclusively. None of 28 KG1a+, HL60-, U937-, and CEM- scFv clones bound to the CD34 antigen, as confirmed by ELISA, although most of their antigens were sensitive to chymopapain digestion. DNA sequences from ten positive clones showed that they were from four different clones. They bound antigens with different molecular weight.

CONCLUSIONSOne hundred and two scFv phage clones specific for hematopoietic stem and progenitor cells have been isolated from an anti-KG1a cell scFv phage library. The pathfinder selection has showed advantages to improve the screening efficacy of scFv phage clones against antigens, which present at very low densities on the cell surface.

Antibodies, Anti-Idiotypic ; immunology ; Antibodies, Monoclonal ; genetics ; Antibody Specificity ; Bacteriophages ; genetics ; Cloning, Molecular ; Hematopoietic Stem Cells ; immunology ; Humans ; Immunoglobulin Fc Fragments ; biosynthesis ; genetics ; immunology ; Immunoglobulin Fragments ; genetics ; immunology ; Immunoglobulin Variable Region ; genetics ; immunology ; Peptide Library ; Single-Chain Antibodies