OBJECTIVE: To prepare high carbamazepine (CBZ) loading solid dispersion and investigate its solubilization mechanism and stability. METHODS: The effects of different drug-carrier ratios and preparation METHODS on dissolution were investigated by intrinsic dissolution rate. The existing form of CBZ in the solid dispersion was characterized by differential scanning calorimetry(DSC) and powder X-ray diffraction(PXRD). The micromorphology was observed with scanning electron microscopy and the solubilization mechanism was probed by wettability test and particle size measurement. RESULTS: The solid dispersion prepared by hot-melt extrusion with the drug/carrier ratio of 4∶1 demonstrated the highest dissolution, which was 327 fold that of the untreated drug. CBZ in the solid dispersion was small crystalline which had been transformed from polymorph III to . Wettability of the solid dispersion in hydrochloric acid solution was increased significantly, which could be rapidly dispersed into a nanometer-sized suspension. The solid dispersion was very stable without any changes for more than 6 months under accelerated test conditions. CONCLUSION: The CBZ solid dispersion with 80% drug loading prepared by hot melt extrusion with a hydrophilic polymer, Eudragit EPO, as carrier possesses satisfactory properties such as fast drug dissolution and excellent stability.

The optimum medium for Lactobacillus M7 was systematically studied with SAS system. Firstly, the prime factors affecting lactic acid yield were selected by means of Plackett-Burman design; secondly, the pnme facias were optimized by response rurface analysis. Under the optimum level determined, the yield is increased by 15%.

The characteristic fingerprint of conventional dairy Nanhanshuishi was established by X-ray diffraction (XRD), based on similarity of caculation on public peaks by MATLAB software, and the feasibility of new dairy technology of microwave method was explored between XRD and the dissolution rate in artificial simulation gastric juices. The result showed that similarity of shared peak in XRD of conventional dairy Nanhanshuishi was > 95%, This XRD characteristic fingerprint of conventional dairy Nanhanshuishi had strong specificity, could be used to provide a reference for identification and quality evaluation. This study also showed that the similarity of microware dairy products and conventional dairy products was good, and the sample of microwave 15 min was the best, and new dairy method by the microwave could replace the traditional method.
Animals ; Chemistry, Pharmaceutical ; instrumentation ; methods ; Drugs, Chinese Herbal ; chemistry ; Medicine, Tibetan Traditional ; Microwaves ; Milk ; chemistry ; Plants, Medicinal ; chemistry ; Quality Control ; X-Ray Diffraction

OBJECTIVETo establish a finite element model of canine segmental mandibular reconstruction by partial-cortical-cutting distraction osteogenesis.

METHODSThe geometry model was established by Mimics software via reading the data of DICOM format from CT and was cut with Magics software. The finite element model was established and was analyzed by MARC software.

RESULTSA finite element model of canine segmental mandibular reconstruction by partial-cortical-cutting distraction osteogenesis was established. The model was composed of five parts. These five parts were felted via Magics software. The Von Mises stress of the joint region of slice and the slide segment were 34.60 MPa when the slide segment was retained 1.4 mm width during distraction osteogenesis with the force of 12 N.

CONCLUSIONThe biomechanics analysis can be complated through the finite element model of canine segmental mandibular reconstruction by distraction osteogenesis that retains lingual cortical bone.

Finite Element Analysis ; Humans ; Mandible ; Mandibular Reconstruction ; Osteogenesis, Distraction ; Reconstructive Surgical Procedures

Objective To measure and analyze the set-up errors of postoperative intensity modulated radiation therapy of rectal cancer (PIMRTRC)with electronic portal imaging device (EPID),and to provide theoretical foundation for clinical realizing of accurate PIMRTRC.Methods Totally 30 patients after rectal carcinoma resection underwent sagittal and coronal photographing with EPID before the first time of therapy and one time per week during the treatment course.The obtained images were compared with DRR images in treatment planning system to get the setup errors at X(left-right),Y(head-foot) and Z (front-back)directions,and the extending margins of CTV and PTV in postoperative intensity modulated radiation therapy were calculated.EPID was used for setup correction,and SPSS 19.0 was involved in to execute statistical analysis. Results The linear displacement had the mean values plus/minus standard deviation at X, Y and Z directions before and after error correction being(-1.392 4±3.670 9)mm vs(-0.816 5±2.670 5)mm,(0.969 7±4.076 1)mm vs(0.418 2±2.911 4)mm, and(0.704 4±1.805 6)mm vs(0.471 7±1.641 3)mm respectively;the extending margin had the values being 7 mm vs 5 mm, 6 mm vs 4 mm, and 4 mm vs 3 mm respectively.Conclusion EPID ensures the correctness and accuracy in postoperative intensity modulated radiotherapy of rectal cancer,which makes target area gifted with maximized dose,the surrounding tissue and organs at risk protected adequately,and provides theoretical support for extending CTV margin.[Chinese Medical Equip-ment Journal,2018,39(5):59-63]

Acute Disease ; Adult ; Aged ; Aneurysm, Dissecting ; complications ; Aortic Aneurysm, Thoracic ; complications ; Coronary Artery Bypass ; Coronary Artery Disease ; surgery ; Female ; Humans ; Male ; Middle Aged

Objective To investigate the expressions of S100B and calcitonin gene related peptide (CGRP) and the pathologic alterations of the hippocampus in kainic acid (KA)-induced epileptic rats. Methods Male SD rats were randomly divided into control group (n=8) and model group (n=40).Animal models of temporal lobe epilepsy were established by intracerebroventricular injection of KA; the same volume of saline was injected into the rats in the control group. Hippocampal tissues within various phases after seizures (6, 12, 24 and 72 h, and 24 h after the success of model making) were performed Nissl staining, Timm staining and immunohistochemical staining. The expressions of S100B and CGRP were observed, and the pathologic alterations of the hippocampal neurons and glial cells were studied.Results All rat models were successfully induced with epileptic seizures. Nissl staining showed that pyknotic neuronal necrosis appeared in the CA3 area of the hippocampus in the model group with cell body atrophy and disappearance of Nissl bodies 1 week after the injection. Timm staining showed that brown particles showed stripped distribution in the CA3 area of the hippocampus and some brown particles in the molecular layer of fascia dentate. Immunohistochemical staining indicated that significant neurons lost and gliosis appeared after seizures with abundant expressions of S100B and CGRP.Conclusion KA-induced epileptic rats express abundant S100B and CGRP and appear such pathological changes as disappearance of Nissl bodies and mossy fiber sprouting, indicating that both S100B and CGRP participate in the onset of epilepsy.

OBJECTIVETo study the effect of siRNA targeting ADAM17 (ADAM17-siRNA) on the proliferation of prostate cancer PC-3 cells.

METHODSAfter transfecting PC-3 cells with ADAM17-siRNA 1 and ADAM17-siRNA 2, we detected the expressions of ADAM17 mRNA and protein by RT- PCR and Western blotting, respectively. We measured the changes in the proliferation and DNA synthesis of PC-3 cells by MTT and bromodeoxyuridine (BrdU) incorporation assay, examined the cell cycle profile by flow cytometry, and determined the expressions of the genes associated with PC-3 cell proliferation by Western blotting.

RESULTSBoth ADAM17-siRNA 1 and 2 effectively reduced the expressions of ADAM17 mRNA and protein in the PC-3 cells. Knockdown of ADAM17 with the two siRNAs significantly inhibited cell proliferation as compared with the control group (0.43 +/- 0.57 and 0.44 +/- 0.64 vs 0.80 +/- 0.51, P < 0.05) and down-regulated DNA synthesis (0.48 +/- 0.43 and 0.54 +/- 0.59 vs 0.79 +/- 0.72, P < 0.05). The cell cycle profile showed that the cell population of the G1 phase was markedly higher in both the ADAM17-siRNA groups than in the control ([61.83 +/- 2.41]% and [59.78 +/- 1.92]% vs [41.38 +/- 1.53]%, P < 0.05), but that of the S phase remarkably lower in the former two than in the latter ([23.64 +/- 2.56]% and [25.24 +/- 1.86]% vs [33.51 +/- 1.47]%, P < 0.05), with a concomitant decrease in the expression of the cell cycle protein cyclin D1 and increase in the cyclin-dependent kinase inhibitor p21.

CONCLUSIONADAM17-siRNA can effectively inhibit the proliferation of PC-3 cells by up-regulating cyclin D1 and down-regulating p21 protein, and ADAM17 has a potential value in the gene therapy of prostate cancer.

ADAM Proteins ; genetics ; metabolism ; ADAM17 Protein ; Cell Line, Tumor ; Cell Proliferation ; Cyclin D1 ; metabolism ; Cyclin-Dependent Kinase Inhibitor p21 ; metabolism ; Down-Regulation ; Humans ; Male ; Prostatic Neoplasms ; genetics ; metabolism ; pathology ; RNA Interference ; RNA, Messenger ; genetics ; RNA, Small Interfering ; genetics ; Signal Transduction ; Transfection

OBJECTIVETo establish the rat model of acute pulmonary embolism, and study the changes of vascular active substances in pulmonary embolism rats, and investigate the interventive effect of anticoagulant drugs on vascular active substances.

METHODSOne hundred and twenty-eight rats were randomly divided into four groups: control group, model group, low-molecular-weight heparin and warfarin treated group and rivaroxaban-treated group (n = 32 in each group). The method of autologous thrombosis was used to establish the animal model of acute pulmonary embolism. The animals were treated with saline or different anticoagulant drugs. The physiological and biochemical parameters were detected at different time points after embolization. The rats were killed after embolism of 24 h, 3 d, 5 d or 1 week respectively and the pathologic samples of lung tissues were collected to analyze the pulmonary pathological changes in different groups.

RESULTSRats in embolization group after blood clots injection showed shortness of breath, oral cyanosis; quicken heart rates and other symptoms. All embolization groups had pulmonary hypertension, the levels of type B natriuretic peptide (BNP) were increased significantly. The ratio of endothelin-1 (ET-1)/NO and thromboxane (TXB2) and prostacyclin (6-k-PGFla) were abnormal. After treated with effective anticoagulant drugs, the levels of BNP, ET-1, NO, TXB2 and 6-k-PGF1a were tended to the normal levels in the control group. The pulmonary hypertensions were gradually decreased. The efficacy of rivaroxaban on pulmonary embolism was the same as that of the low molecular weight heparin or warfarin.

CONCLUSIONAnticoagulation therapy can effectively improve endothelial function after pulmonary embolism, reduce pulmonary hypertension, and revise the increased BNP levels to normal levels. The efficacy of rivaroxaban is not inferior to that of low molecular weight heparin and warfarin.

Animals ; Anticoagulants ; pharmacology ; Disease Models, Animal ; Endothelin-1 ; metabolism ; Heparin, Low-Molecular-Weight ; pharmacology ; Hypertension, Pulmonary ; drug therapy ; metabolism ; Lung ; pathology ; Morpholines ; pharmacology ; Pulmonary Embolism ; drug therapy ; metabolism ; Rats ; Rivaroxaban ; Thiophenes ; pharmacology ; Warfarin ; pharmacology

OBJECTIVETo explore the differential expression of homeobox genes in the normal, wounded human fetal and adult skins and its significance in fetal scarless healing.

METHODSGene chips containing 14 000 human genes were used to investigate homeobox gene expressions of the normal, wounded human fetal and adult skins.

RESULTSThere were significant differences between the expression of homeobox genes, especially for PRX-2, HOXB13, HOXB6 and HOXB7.

CONCLUSIONSThe homeobox gene is in close relation to developmental biology. The different expressions and changes of homeobox genes in the normal, wounded human fetal and adult skin may be a primary cause of different wound healing between fetal and adult skin.

Adolescent ; Adult ; Animals ; Cells, Cultured ; Child ; Female ; Fetus ; Gene Expression ; Gene Expression Profiling ; Genes, Homeobox ; genetics ; Homeodomain Proteins ; genetics ; Humans ; Male ; Mice ; Mice, Inbred BALB C ; Oligonucleotide Array Sequence Analysis ; Skin ; Wound Healing ; genetics ; Young Adult