The complex level of constructing biopharmaceutics classification system of Chinese materia medica CMMBCS) was the study of traditional Chinese compound, on the premise of insisting that the multicomponent simultaneous determination, when carrying out the study of intestinal permeability, the primary task was to define the source of the components that was absorbed through the intestinal wall, namely, which medicinal material the components belonged to in traditional Chinese compound. The technology of chemical fingerprint and in vitro everted gut sac model were used in this research to make multicomponent an intuitive source attribution which permeated the intestine in the classic formula Gegen Qinlian decoction, and to lay the foundation for the further qualitative and quantitative research of intestinal permeability.
Animals ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Intestines ; metabolism ; Male ; Permeability ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar

Background Glaucoma is primarily characterized by the damage of retinal ganglion cells.The macular ganglion cell complex (GCC)thickness can be quantitatively measured using spectral domain optical coherence tomography(SD-OCT). Objective This clinical study was to explore the macular GCC thickness change in primary open-angle glaucoma (POAG) patient with SD-OCT. Methods A serial case-controlled study was designed.A total 101 eyes of 101 POAG patients and 41 normal eyes of 41 age- and refract power-matched normal subjects were cnrolled in the study.POAG patients were assigned to normal perimetry POAG group,early stage POAG group,advanced POAG group and late stage POAG group.Average macular GCC thickness(GCC-Avg),superior GCC thickness(GCC-Sup) and inferior GCC thickness (GCC-Inf)of subjects were measured by SD-OCT and compared among POAG patients and normal controls.Peripapillary retinal nerve fiber layer(RNFL) thickness was measured with time domain OCT(TD-OCT).The correlation between GCC thickness with RNFL thickness or mean deviation(MD) of perimetry were evaluated and analyzed.Informed consent was obtained from each patient prior to entering this study.Results GCC-Avg thickness,GCC-Sup thickness and GCC-Inf thickness were significantly decreased in the normalperimetry POAG group and early stage POAG group compared with the normal control group (GCC-Avg:t =5.411,10.247,P ＜ 0.01 ; GCC-Sup:t =6.171,9.484,P＜ 0.01 ; GCC-Inf:t =5.281,8.592,P ＜ 0.01 ).Also,GCC-Avg thickness,GCC-Sup thickness and GCC-Inf thickness were significantly decreased in the advanced POAG group compared with the early stage POAG group ( GCC-Avg:t =4.246,P＜0.01 ; GCC-Sup:t - 2.419,P - 0.019 ; GCC-Inf:t =4.636,P＜0.01 ),and GCC-Avg thickness,GCC-Sup thickness and GCC-Inf thickness were significantly decreased in the late stage POAG group compared with the advanced POAG group (GCC-Avg:t=2.095,P=0.040;GCC-Sup:t=2.756,P＜0.01:GCC-Inf:t =2.018,P =0.040 ).The positive correlations were seen between GCC-Avg thickness,GCC-Sup thickness,GCC-Inf thickness and RNFL-Avg thickness,RNFL-Sup thickness,RNFL-Inf thickness respectively( r =0.802,0.825,0.856,P ＜ 0.01 ).MD value of perimetry was positive correlated with GCC-Avg thickness in POAG patients ( r =0.601,P ＜ 0.01 ). Conclusions SD-OCT can quantitatively measure and differentiate the GCC thickness in POAG patients.The GCC thickness gradually decreases with the development of POAG.There exist a well correlation between visual field defect and RNFL thinning.

Background Glaucoma is primarily characterized by the damage of retinal ganglion cells in the inner layer.Whether the outer retinal layers are involved is controversial.Although the functional abnormality of the outer retinal layers have been determined,structural studies present difierent outcomes.Objective This study measured and compared photoreceptor layer thickness between normal and glaucomatous eyes using spectral domain optical coherence tomography(OCT). Methods A case-control study was designed.The macular area of 38 eyes from 38 normal volunteers and 48 primary open-angle glaucomatous eyes(POAG)were imaged by spectral domain OCT(SD OCT).The outer nuclear layer(ONL)and inner and outer segments(IS/OS)layer thicknesses in fovea and parafovea(1.5 mm from the fovea) were measured by a single masked observer using an image analysis software (SigmaScan Pro version 5.0).Retinal nerve fiber layer(RNFL)thicknesses of the 86 eyes were measured by Stratus OCT.The photoreceptor layer thicknesses between normal and glaucomatous eyes were compared.The correlation of photoreceptor with RNFL thicknesses was evaluated with linear and non-linear regression models. Results The outer nuclear layer(ONL)thickness in the fovea in normal and glaucomatous eyes were 96.7±10.7μm and 103.7±13.3 μm,respectively,with a significant difference(P=0.011).The inner and outer segments(IS/OS)layer thicknesses in the fovea in the two groups were 59.3±5.5 μm and 59.5±5.5μm,respectively,without significant difference(P=0.890).The outer nuclear layer(ONL)thicknesses in the parafovea in normal and glaucomatous eyes were 70.9±14.0μm and 68.7 ±10.7μm,respectively,(P=0.410).The inner and outer segments(IS/OS)layer thicknesses in the parafovea in the two groups were 45.2±6.4 μm and 43.6±5.5μm,respectively(P=0.228).The relationship between ONL and RNFL thickness was best described with a second order polynomial regression model assoeiation(Y=-0.019X2+2.73X+10.34,R2=0.211,P=0.005). Conclusion The foveal ONL thickness is increased in glaucomatous eyes.The alteration of foveal ON L thickness is associated with the severity of the disease.

Background Fundus photography is a traditional method for detecting local retinal nerve fiber layer (RNFL) defects,but the evaluation of its result depends on the observer's experience.The spectral domain optical coherence tomography (OCT) exhibit the defects of RNFL very clearly.Objective This study was to evaluate the diagnosis value and correlation between topographic profiles of localized RNFL defects determined by spectral domain and time domain OCT with fundus photography.Methods Forty-one normal eyes of 41 subjects and 55 eyes of 55 glaucomatous patients with localized,wedge-shaped RNFL defects identified by two glaucoma specialists in fundus photographs were enrolled in the clinical study.The angular location and width of RNFL defects determined on the images of fundus photography,Cirrus HD-OCT and Stratus OCT were analyzed respectively using Pearson's correlation coefficient and linear regression analysis.This study followed the Helsinki declaration and was approved by Ethic Committee of Shenzhen Eye Hospital.Written informed consent was obtained from each individual before the clinical examination.Results Seventy-five RNFL defects were identified in 55 eyes by two glaucoma specialists unanimously with the defect position at superior-temporal and inferior-temporal quadrants.The sensitivity of Cirrus HD-OCT and Stratus OCT to determining RNFL defects were 88.0% and 69.3% respectively and their specificities were 92.7% and 97.6% respectively.The angular locations of RNFL defects by Cirrus HD-OCT and Stratus OCT were highly correlated with those by fundus photography(r=0.993,r=0.992,P＜0.001);while the angular widths of RNFL defects by Cirrus HD-OCT and Stratus OCT were moderately correlated with those by fundus photography(r=0.420,r=0.432,P=0.019,P=0.002).No significant differences were found in the defect width of RNFL between Cirrus HD-OCT or Stratus OCT and fundus photography(Cirrus HD-OCT:P=0.114;Stratus OCT:P=0.074),and significant difference was found in that between Cirrus HD-OCT and Stratus OCT(P=0.002).Conclusion Spectral domain OCT and time domain OCT can localize RNFL defects with high sensitivity and specificity.The measure value of Cirrus HD-OCT and Stratus OCT for RNFL defects shows a good diagnostic agreement with fundus photography.

Four salts of ticagrelor, ticagrelor-3,5-dinitrobenzoic acid, ticagrelor-pyrazinamide, ticagrelor-D-proline and ticagrelor-L-proline were prepared by solvent suspension and liquid-assisted grinding to improve the solubility of ticagrelor. The compounds were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, nuclear magnetic resonance spectroscopy, elemental analysis, and the intermolecular salt-bonding forces were analyzed. The equilibrium solubility of salts and pure drug in hydrochloride buffer pH 1.2 and phosphate buffer pH 6.8 were measured by high-performance liquid chromatography. Ticagrelor was salted with 3,5-dinitrobenzoic acid, pyrazinamide, D-proline, L-proline all in a stoichiometric ratio of 1∶1; with the exception of ticagrelor-D-proline, the solubility of the other three salts provided significantly improved solubility in hydrochloride buffer pH 1.2, and the equilibrium solubility of ticagrelor-3,5-dinitrobenzoic acid was increased by approximately 1.7 folds as compared to pure drug. Salt-forming technology is convenient and can improve the solubility of ticagrelor.

In order to improve the poor photostability of nifedipine, this study designed a cocrystal based on the principles of crystal engineering and prepared nifedipine-imidazole cocrystal by suspension method. The new cocrystal was characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TG) and infrared spectroscopy (IR) to confirm the formation of the cocrystal. The photostability of nifedipine and its cocrystal was measured by powder X-ray diffraction and high-performance liquid chromatography (HPLC). The results showed that the nifedipine-imidazole cocrystal improved the photostability of nifedipine to a certain extent. This study provides guidance for the development of nifedipine cocrystals and the improvement of its druggability.

To illustrate the solubility involved in biopharmaceutics classification system of Chinese materia medica (CMMBCS) , the influences of artificial multicomponent environment on solubility were investigated in this study. Mathematical model was built to describe the variation trend of their influence on the solubility of puerarin. Carried out with progressive levels, single component environment: baicalin, berberine and glycyrrhizic acid; double-component environment: baicalin and glycyrrhizic acid, baicalin and berberine and glycyrrhizic acid and berberine; and treble-component environment: baicalin, berberin, glycyrrhizic acid were used to describe the variation tendency of their influences on the solubility of puerarin, respectively. And then, the mathematical regression equation model was established to characterize the solubility of puerarin under multicomponent environment.
Berberine ; chemistry ; Biopharmaceutics ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Glycyrrhizic Acid ; chemistry ; Isoflavones ; chemistry ; Materia Medica ; chemistry ; Solubility

Piroxicam has polymorphism. Different crystalline forms can exhibit different physicochemical properties and biological activities. Analysis of the intermolecular interactions is essential to reveal the formation mechanism and differences of polymorphs. In this paper, Hirshfeld surface analysis and semi-empirical methods were used to calculate and analyze the intermolecular interactions in seven polymorphic forms of piroxicam. The results show that the Hirshfeld surface analysis method can clearly and intuitively reveal the intermolecular interactions, among which H…H, O…H/H…O and N…H/H…N interactions account for 95% of the total energy. There are differences in the proportion and distribution of the forces of different crystal forms. The energy calculation shows that the lattice energy of the hydrate is significantly lower than that of the anhydrous forms, and in the specific energy distribution, the contribution of the dispersion force is the most prominent. Further interaction energy analysis was found that within the distance of 3.8 Å from the center of the piroxicam molecule, different crystalline forms of piroxicam molecule have different interaction energies with surrounding molecules.

OBJECTIVETo provide an ideal animal model for exploring pathogenesis and experimental treatment of primary colonic lymphoma.

METHODSPrimary colonic and liver metastatic lymphoma tissues were obtained from the surgical specimens,and transplanted into colonic mucosa of nude mice respectively. The tumorigenesis, invasion, metastasis and morphology of the transplanted tumor were observed. Karyotype was analyzed and DNA content was measured.

RESULTSAccording to the new WHO classification of malignant lymphoma, two high metastatic models (HCBL-0303 from primary lymphoma and HCBL-0304 from live metastatic lesion) of human primary colonic non-Hodgkin's B cell lymphoma in nude mice were established successfully by orthotopic transplantation. Pathological examination showed poorly differentiated non-Hodgkin's B cell lymphoma of the transplanted tumors, and immunohistochemical staining showed positive expressions of CD19, CD20 and CD22, and negative expressions of CD3 and CD7. The number of chromosome ranged from 55 to 59, and DNA index (DI) was 1.59 - 1.71 (i.e. heteroploid). In HCBL-0303,liver metastasis rate was 63.7% and lymph node metastasis rate was 56.4%. However, in HCBL-0304, both metastasis rates of liver and lymph node were 100%. The transplanted tumors grew autonomously and invasively in nude mice, and further developed hematogenous, lymphatic metastasis and intraperitoneal seeding.

CONCLUSIONSHCBL-0303 and HCBL-0304 are the first established high metastatic models of primary colonic lymphoma, and can be applied to the research on pathogenesis, invasion,metastasis and experimental therapy of human primary colonic lymphoma.

Animals ; Colonic Neoplasms ; pathology ; Female ; Humans ; Liver Neoplasms ; secondary ; Lymphoma ; pathology ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Neoplasm Metastasis ; Neoplasms, Experimental ; Xenograft Model Antitumor Assays

OBJECTIVETo assess the clinical effect of combination of far with near acupoints, Chengshan (BL 57) and Changqiang (GV 1), for acupuncture treatment of hemorrhoidal pain.

METHODSOne hundred and twenty cases of hemorrhoids with pain were randomly divided into 2 groups, an electroacupuncture group and a medication group, 60 cases in each group. The electroacupuncture group were treated by electroacupuncture at Changqiang (GV 1) and Chengshan (BL 57) with sparse-dense wave, frequency 2/100 Hz; and the medication group with oral administration of Tramadol and rectal application of Mayinglong Shexiang Zhichuang Suppository. The two group were treated for five days. Changes of pain were assessed by Visual Analogue Scale (VAS) scores at the defecation each day.

RESULTSIn the electroacupuncture group, VAS score was 6.64 +/- 3.66 before treatment and 5.65 +/- 2.21 on the second day of treatment with a significant decrease (P < 0.05), and 1.85 +/- 1.24 on the fifth day after treatment end. In the medication group, VAS score was 6.58 +/- 3.18 before treatment and 4.86 +/- 2.04 on the third day after treatment with significant decrease compared with that before treatment, and 2.24 +/- 1.46 on the fifth day. There was no significant difference between the two groups in the pain score on the fifth day after the treatment end.

CONCLUSIONCombination of Chengshan (BL 57) with Changqiang (GV 1) is effective for improvement of hemorrhoidal pain in defecation.

Acupuncture Points ; Adult ; Electroacupuncture ; Female ; Hemorrhoids ; therapy ; Humans ; Male ; Middle Aged ; Pain Management