Preparation of ebastine dispersible tablets by hot-melt dispersion / 药学实践杂志

Objective To prepare ebastine dispersible tablets by hot-melt dispersion method using hypromellose as a carrier.Methods Ebastine was heated to melt and dispersed in hot solution of hypromellose.The mixture was adsorbed by mannitol and then used to prepare dispersible tablets.The characteristics of hot-melt dispersion were analyzed by the methods of differential scanning calorimetry and X-ray powder diffraction.A comparison of dissolution curves between self-made dispersible tablets and original ebastine tablets was performed.Results The analysis of X-ray diffraction and differential scanning calorimetry showed that the ebastine in solid matrix remained the main crystalline characteristics.The dissolution of ebastine hot-melt dispersion was 95.07％ in 15 min in vitro, which was significantly higher than that of micronized ebastine raw material.Moreover, the accumulative dissolution of ebastine dispersible tablets in 30 min was about 30％ higher than the original drug.Conclusion The method of hot-melt dispersion using hypromellose as a carrier improved the ebastine dissolution significantly.

CT appearance of thoracic lymphonodus in AIDS patients with immune reconstitution inflammatory syndrome / 实用放射学杂志

Objective To explore the CT appearance of thoracic lymphonodus in AIDS patients with immune reconstitution in-flammatory syndrome(IRIS)after highly active antiretroviral therapy (HAART).Methods The data of thoracic CT in 24 AIDS pa-tients after HAART with enlarged thoracic lymphonodus in IRIS were collected,and the chest CT appearance was analyzed.Results Of the 24 cases of AIDS patients with IRIS after HAART,1 9 cases were complicated with pulmonary tuberculosis,which includ-ed 5 cases with cervical tuberculous lymphadenitis,3 cases were co-infected with bacterium and fungi,1 case was infected by penicil-lium marneffei,1 case by pneumocystis carinii.The enlarged thoracic lymphonodus were primarily located in 4R region(20/24), secondly in 2R region(1 1/24)and 4L region(1 1/24),in which the density was uniform or non-uniform,edge clear or unclear,some parts of lymphonodus were fused together but not calcified.The minor axis of enlarged lymphonodus was 1 1.0-25.0 mm except X region,enhanced uniformly in 2 cases.Obstructive pneumonia and pulmonary consolidation were found in 2 cases with enlarged lym-phonodus,which were located in 10R region.Pleural effusion was found in 13 cases with greatest depth of about 22 mm,pericardial effusion was found in 5 cases with greatest depth of about 24 mm.Conclusion The enlarged thoracic lymphonodus in AIDS patients with IRIS affer HAART are mainly involved in the region of 4R,2R and 4L,with or without pleural effusion and pericardial effusion.

The therapeutic outcomes of surgery on senile patients with laryngeal carcinoma / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To investigate the therapeutic outcomes of Laryngectomy and prognostic factors in senile patients with laryngeal carcinoma.@*METHOD@#A retrospective study of long-term therapeutic outcomes was performed on 110 patients with laryngeal carcinoma over 65, treated mainly by surgery, from 1990 to 2005. Different kinds of operations were as follows: cordectomy(1 case) or stripping (2 cases) by suspended laryngoscope, laryngofissure (4 cases), vertical partial laryngectomy without tracheotomy (8 cases), vertical partial laryngectomy (8 cases), extended vertical partial laryngectomy (1 case), horizontal laryngectomy (4 cases), subtotal laryngectomy (4 cases), cricohyoidoepiglottopexy (30 cases), Arslan's procedure (8 cases), and total laryngectomy (40 cases). Forty-eight patients were treated with preoperative or postoperative radiotherapy, and five patients were treated with induction chemotherapy followed by radiotherapy.@*RESULT@#There were four missing cases among all 110 cases. The 5- and 10-year overall survival rate were 66.6% and 44.2%, respectively. The 5- and 10-year diseases-free survival rate were 57.0% and 38.4%, respectively. The median survival was 84 months. Decannulation rate was 87.1% (54/62). Well-differentiation, surgery alone, node-negative, glottic carcinoma, early stage, partial laryngectomy, non-recurrence and male were favorable prognostic factors with univariate analysis (P < 0. 05). Well-differentiation and surgery without combined therapy were also favorable prognostic factors with multivariate analysis.@*CONCLUSION@#Conservation laryngectomy was an efficient method to treat senile patients with laryngeal carcinoma. Combined therapy should better not be adopted to patients with negative surgical margins.

The building of multiple drug resistant human laryngeal cancer cell line and its characteristics / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To build the multiple drug resistant human laryngeal cancer cell line and investigate its characteristics.@*METHOD@#Human laryngeal cancer cells were exposed in stepwise escalating concentration of Taxol until the resistant cell line was developed. The IC50 and the resistance folds of multidrug resistance were detected by an ATP assay. The differences of cell cycle distribution, apoptosis, and Rhodamine accumulation between Hep-2 and Hep-2T cells were studied through flow cytometry. The MDR1 and MRP1 gene were detected through realtime quantitative RT-PCR, and the corresponding protein was detected through western-blotting.@*RESULT@#A multidrug resistance cell line-Hep-2T induced by Taxol was effectively developed, whose drug resistance was 104 times that of Hep-2 cells. Doxorubicin, Gemcitabine, 5-Fu, Cisplatin all increased the drug resistance by 46.78, 1.95, 2.50, 1.05 folds. The cell cycle distribution altered. The apoptosis of Hep-2 cells was quite greater than that of Hep-2T cells (45.32% vs 4.26%, P < 0.01, flow cytometry), (54.47 +/- 48.95 vs 9.84 +/- 12.53 P < 0.01, hoechst staining) after Hep-2 and Hep-2T exposed to Taxol at IC50 to Hep-2. The copy ratio of MDR1/GAPDH mRNA of Hep-2T was 64.2 +/- 36.7 times that of Hep-2 (P < 0.05), while MRP1/GAPDH of Hep-2T was only 1.20 +/- 0.09 folds more than that of Hep-2 (P < 0.05). The proteins of MDR1/P-gp were greatly over expressed in Hep-2T cells compared with Hep-2 cells (P < 0.01) whose was in the same trend (P < 0.05), while the elevated expression of MRP1 was lower than that of MDR1/P-gp.@*CONCLUSION@#When considering the possible methods to reverse MDR of SCCHN, more emphasis should be laid on MDR1/P-gp, and when combining this with chemotherapy the non-P-gp substrate chemotherapeutic agents should be considered. At the same time, more attention should be paid to the changes of cell cycle distribution during the drug selection.