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1.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (4): 1309-1316
in English | IMEMR | ID: emr-189698

ABSTRACT

Tranexamic Acid [TXA] is commonly administered in total knee arthroplasty for reducing blood loss. There has been a growing interest in the topical use of TXA except intravenous use for prevention of bleeding in TKA. The aim of this study was to develop and validate a HPLC-MS method to detect TXA and apply to compare the pharmacokinetic profile of TXA after intravenous [IV] and topical intra-articular [IA] application of TXA at a dose of 20 mg/kg in rabbits. In order to prove intra-articular administration is better than that of intravenous administration from the point of rabbit pharmacokinetic. Two groups of rabbits [n=6/group] respectively received TXA intra-articularly or intravenously. Blood samples were collected at scheduled time. The concentration of TXA in plasma was determined by a validated HPLC-MS method. Excellent linearity was found between 0.015 and 70.0microg/ml with a lower limit of quantitation [LLOQ]of 0.015microg/ml [r>0.99]; moreover, all the validation data including accuracy and precision [intra- and inter-day] were all within the required limits. The pharmacokinetic parameters in IA and IV group were: C[max]: 30.65+/-3.31 VS 54.05+/- 6.21 fig/ml [p<0.0l]; t[1/2]: 1.26+/-0.05 VS 0.68+/-0.13h [p<0.05]; AUC[0-t]: 42.98+/-7.73 VS 23.39+/-4.14microg/ml- h [p<0.0l], time above the minimum effective concentration [%T > MEC]: 1.5-2.2 VS 0.7-1.2h [p<0.05]. HPLC-MS method is suitable for TXA pharmacokinetic studies. The results demonstrated that topical intra-articular application of TXA showed a reduced peak plasma concentration and prolonged therapeutic drug level compared with intravenous TXA from the point of rabbit pharmacokinetic


Subject(s)
Animals , Injections, Intra-Articular , Administration, Intravenous , Rabbits , Chromatography, High Pressure Liquid
2.
Article in Chinese | WPRIM | ID: wpr-249254

ABSTRACT

<p><b>OBJECTIVE</b>To evaluate efficacy and safety of Baimai ointment (see symbol in text) in the treatment of wrist-dysfunction after distal radius fracture.</p><p><b>METHODS</b>From April, 2011 to June, 2012, 43 patients with distal radius fracture were treated with plaster fixation. All the patients were divided into two group: test group and control group. Twenty-one patients in test group and 22 in control group, and the baseline was balance (P > 0.05). The 21 patients in test group were treated with Baimai ointment (see symbol in text), fomentation, functional exercises. The 22 patients in control group were treated with placebo, fomentation, functional exercises. Foment affected side wrist with wet towel in 20 min before medication, with the temperature between 50 degrees C and 60 degrees C. Smear drugs uniformly in range of 3 cm in the vicinity of palm stripes after drying (about 3 g) and take functional exercises for the activities of wrist and hand. Continuous follow the program per 8 hours once and follow-up for 8 weeks. The Wrist's pain was assessed with VAS. The wrist's activities were measured with the protractor of orthopedic. Measure The grip strength was measured with dynamometer. The wrist's function were assessed with the table of Cooney.</p><p><b>RESULTS</b>The test group had a significantly better results than those of control group in the extent of wrist's pain throughout the treatment (P < 0.001), and grip strength on the 28th day and the 56th day (P < 0.05), and Cooney functional assessment on the 56th day (P < 0.05). Wrist's activities had no significane difference throughout the 8 weeks (P > 0.05). There were no drug adverse reactions occurred.</p><p><b>CONCLUSION</b>Tibetan Baimai ointment (see symbol in text) has the treatment of wrist-dysfunction after distal radius fracture for external use, which can reduce the extent of wrist's pain, promote grip strength recovery in the middle and late of process, promote wrist's function recovery latterly, and safety for external use.</p>


Subject(s)
Adult , Aged , Case-Control Studies , Double-Blind Method , Female , Humans , Male , Medicine, Tibetan Traditional , Middle Aged , Ointments , Radius Fractures , Drug Therapy , Recovery of Function , Wrist Joint
3.
Article in English | WPRIM | ID: wpr-296042

ABSTRACT

<p><b>OBJECTIVE</b>To analyze the relationship between malignant transformation and abnormal expression of eukaryotic initiation factor 3 (eIF3 p36) in human bronchial epithelial (16HBE) cells induced by cadmium chloride (CdCl2).</p><p><b>METHODS</b>16HBE cells were treated several times with different concentrations of CdCl2. Tumorigenic potential of transformed cells was identified by assays for anchorage-independent growth in soft agar and for tumorigenicity in nude mice after the 35th passage. Total RNA was isolated from 16HBE cells induced by CdCl2, including non-transformed, Cd-transformed, and Cd-tumorigenic cell lines. Special primers for eIF3 p36 were designed and the expression of eIF3 mRNA in different cell lines was detected with fluorescent quantitative-polymerase chain reaction technique (FQ-PCR).</p><p><b>RESULTS</b>The 35th passage of 16HBE cells transformed by CdCl2 exhibited overlapping growth. Compared with the non-transformed cells, colonies of transformed cell lines in soft agar showed statistically significant increases and dose-dependent effects (P<0.01). All Cd-induced transformed cell lines formed tumors in nude mice within 2 weeks of inoculation, but none of the mice injected with non-transformed cells showed tumors even after 3 weeks. All tumors were pathologically identified as poorly differentiated squamous cell carcinoma. The eIF3 p36 genes in different stages of 16HBE cells transformed by CdCl2 were elevated as compared with the non-transformed control (P<0.01), and the eIF3 expression increased with the degree of cell malignancy.</p><p><b>CONCLUSION</b>CdCl2 is capable of inducing morphological transformation in 16HBE cells and transformed cells are potentially tumorigenic. Over-expression of eIF3 p36 is positively correlated with malignant transformation of 16HBE cells induced by CdCl2 and may be one of the molecular mechanisms potentially responsible for carcinogenesis due to Cd.</p>


Subject(s)
Animals , Base Sequence , Bronchi , Cell Biology , Metabolism , Cadmium Chloride , Pharmacology , Cell Transformation, Neoplastic , DNA Primers , Epithelial Cells , Metabolism , Eukaryotic Initiation Factors , Metabolism , Humans , Mice , Mice, Nude , Polymerase Chain Reaction
4.
Article in Chinese | WPRIM | ID: wpr-638862

ABSTRACT

Objective To study the influence of vascular endothelial growth factor(VEGF) on development of alveolar epithelial cell Ⅱ (AECⅡ) and expression of pulmonary surfactant protein B(SP-B) in premature rats.Methods Wistar rats at 19 days gestation were paunched to get embryo and primary AECⅡculture.The rats were divided into 4 groups ,VEGF-165 group,Dexamethasone group,VEGF and Dexamethason group,control group. AECⅡ and SP-B expression were measured by immunology histochemistry.Results SP-B had positive expression in VEGF group, Dexamethason group, VEGF and Dexamethason group. SP-B had negative expression in control group.Conclusion VEGF-165 can increase SP-B positive expression and secret of AECⅡ.VEGF promotes lung maturity.

5.
Article in Chinese | WPRIM | ID: wpr-638853

ABSTRACT

Objective To investigate the expression of nerve growth factor(NGF) and slouble Fas(sFas) in children with viral myocarditis(VM),and the relationship with immunity,with the aim to provide evidence and basis for the diagnosis and treatment of VM.Methods The serum levels of NGF and sFas were detected by two-site enzyme-linked immunosorbent assy(ELISA) in 43 children with VM,and 20 normal heathy children as controls.Results The serum levels of both NGF and sFas in children with the acute stage(course in less than month and 1-2 months)and the procrastinate and chronic stages of VM were significantly higher than those of healthy children(P0.05).Conclusion The increased serum expression levels of NGF and sFas are related to the process of viral myocarditis,which confirms the relationship between the onset of VM and immune factors.

6.
Article in Chinese | WPRIM | ID: wpr-683352

ABSTRACT

Objective To study the effects of vascular endothelial growth factor(VEGF)on production of pulmonary surfactants.Method Fetal rat lungs were obtained at 19-day gestation.Primary culture of typeⅡalveolar epithelial cells(AECⅡ)was performed using IgG panning technique.The rats was divided into groups: VEGF,Dexamethasone,VEGF plus Dexamethasone and a control.Total phospholipids,phosphatidylcholine (PC),phosphatidyl glycerol(PG)and sphingornyelin(SM)were determined.Results expressed as mean?SEM. Comparison between groups were made with LSD-t test and one -way ANOVA.Result VEGF,Dexamethasone and VEGF plus Dexamethasone groups showed increased amount of total phospholipids and its compositions on the first day of culture.Conclusions VEGF-165 promotes the production and secretion of pulmonary surfactant. VEGF and Dexamethason may go through different mechanism for enhancement of synthesis of pulmonary surfactant,thereby improve biological function of AECⅡ.

7.
Article in English | WPRIM | ID: wpr-229725

ABSTRACT

<p><b>OBJECTIVE</b>To study the oncogenic potential of mouse translation initiation factor 3 (TIF3) and elongation factor-1delta (TEF-1delta) in malignant transformed human bronchial epithelial cells induced by crystalline nickel sulfide (NiS).</p><p><b>METHODS</b>Abnormal expressions of human TIF3 and TEF-1delta genes in two kinds of NiS-transformed cells and NiS-tumorigenic cell lines were investigated and analyzed by the reverse transcript polymerase chain reaction (RT-PCR) and fluorescent quantitative polymerase chain reaction (FQ-PCR), respectively.</p><p><b>RESULTS</b>RT-PCR analysis primarily showed that both human TIF3 and TEF-1delta mRNA expressions in two kinds of NiS-transformed cells and NiS-tumorigenic cell lines were increased as compared with controls. FQ-PCR assay showed that the levels of TIF3 expressions in the transformed cells and tumorigenic cells were 3 and 4 times higher respectively, and the elevated expressions of TEF-1delta cDNA copies were 2.7- to 3.5-fold in transformed cells and 4.1- to 5.2-fold in tumorigenic cells when compared with non-transformed cells, indicating that the over-expressions of human TIF3 and TEF-1delta genes were related to malignant degree of the cells induced by nickel.</p><p><b>CONCLUSIONS</b>These findings demonstrate that there are markedly abnormal expressions of TIF3 and TEF-1delta genes during malignant transformation of human bronchial epithelial cell lines induced by crystalline NiS. They seem to be the molecular mechanisms potentially responsible for human carcinogensis due to nickel.</p>


Subject(s)
Biomarkers , Bronchi , Cell Biology , Cell Line, Transformed , Cell Line, Tumor , Cell Transformation, Neoplastic , Metabolism , DNA, Complementary , Metabolism , Epithelial Cells , Gene Expression Regulation, Neoplastic , Humans , Nickel , Toxicity , Peptide Elongation Factor 1 , Genetics , Metabolism , Prokaryotic Initiation Factor-3 , Genetics , Metabolism
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