Synthesis and druggability study of triptolide stearate / 药学实践杂志

Objective To synthesize a lipophilic prodrug of triptolide (TP) and improve its druggability .Methods Trip-tolidestearate (TP-SA)was synthesized via the DMAP-catalyzed DCC method and identified by MS ,1H-NMR and 13C-NMR. The shake-flask method was used to study the oil/water partition coefficient .The preparations of TP and TP-SA liposomes and emulsions were compared .Their encapsulation efficiency and stability were investigated .Results TP-SA was synthesized suc-cessfully .Its log P in octanol/water system was 2 .33 .It was difficult to prepare TP liposome or emulsion .By contrast ,TP-SA liposome and emulsion can be prepared successfully with the same formulation process .The particle size of TP-SA lipo-somes were about 90 nm and TP-SA emulsions were about 110 nm .The encapsulation efficiency was above 95% .Their stabili-ty were studied at 4℃ and 25℃ .The preparation parameters ,such as particle size and encapsulation efficiency ,had no signif-icant change in a week .Conclusion Triptolide stearate enhanced drug lipophilicity .Its druggability was improved significant-ly .These data can be used for the TP related drug design and development .

Therapeutic value of endoscopical therapy for small gastric stromal tumor / 中华消化内镜杂志

Objective To investigate the safety and effectiveness of endoscopical therapy for small grastric stromal tumor( d<2 cm) . Methods Clinical records of 80 patients dignosed as having small grastric stromal tumor by pathology and immunohistochemistry were retrospectively analyzed. Endoscopic or laparo?scopic or open surgery was performed, so patients were divided into endoscopic treatment group ( n=37) and surgical treatment group ( n=43) accordingly. Perioperative period data, effectiveness and follow?up data were analysed. Results Thirty?five cases( 94?6%) of endoscopic treatment group were successfully treated by endoscopic surgery. Intraoperative perforation occurred in 8 cases, among which 2 cases transferred for conventional operations.Pneumoperitoneum occurred in 2 cases (better after symptomatic treatment), while no serious infection or perioperative death occurred. There were no significant differences in the complete re?section rate[ 91?89% ( 34/37) VS 100?0%( 43/43) , P=0?095) , the incidence of postoperative complica?tions[5?71%(2/35)VS 2?33%(1/43),P=0?855)or the improvement of postoperative symptoms[93?10%( 27/29) VS 85?71% ( 30/35) , P=0?589] ,while statistically significant differences were found in operation time[(37?41±13?45)min VS(84?56±38?37)min, P=0?000], intraoperative blood loss[(5?65±5?88)ml VS(31?48 ±39?57)ml, P=0?000], postoperative feeding time[(2?47±0?61)d VS(3?26 ±1?27)d, P=0?001], postoperative hospital stay[(5?76 ±2?28)d VS(7?64±2?99)d,P=0?022],and medical expenses [(18 554?4±9 736?45)yuan VS(31 138?11±1 206?24)yuan, P=0?000]. Conclusion Endoscopic re?section is safe and effective for small grastric stromal tumor with minimal invasion,simple procedure, faster recovery and less economic burden for the patients.

Simultaneously determining the contents of combretastatin A4 myristate and its active metabolite combretastatin A4 by HPLC / 国际药学研究杂志

Objective To develop a high performance liquid chromatography(HPLC)method for simultaneously determining the contents of combretastatin A4 myristate(CA4-14)and its active metabolite combretastatin A4(CA4)in rat plasma. Methods 1-Naphthol was used as internal standard. The analysis was performed on a Agilent Eclipse plus C18(4.6 mm × 250 mm,5μm )with gra?dient elution by using the mobile phase of acetonitrile(A)-0.4%formic acid solution(B). The column temperature was 30° C and the flow rate was 1.0 ml/min. The detection wavelength was 295 nm and the injection volume was 20μl. Results The calibration curves were linear within the range of 0.2-100μg/ml(r2=0.9980)for CA4-14,and 0.05-50μg/ml(r2=0.9999)for CA4,while the quantifica?tion limits of CA4-14 and CA4 were 0.2μg/ml and 0.01μg/ml,respectively. The recoveries of CA4-14 and CA4 were 93.79%(RSD=1.94%)and 96.81%(RSD=3.11%). Conclusion The method is convenient,fast,sensitive,with good precision,and can be used to determine the contents of CA4-14 and C A4 in rat plasma.

Clinical and pathologic features of small gastrointestinal stromal tumor / 中华消化内镜杂志

Objective To investigate the clinical and pathologic features of small gastrointestinal stromal tumors (small GISTs,d ＜ 2.0 cm).Methods Medical records of 95 patients undergoing surgery (endoscopic surgery,thoracoscopic/laparoscropic surgery and open surgery)and diagnosed as having GISTs by pathology and immunohistochemistry in Nanfang hospital from October 2003 to June 2014 were retrospectively analyzed.Based on clinical and pathological results,correlation analyses between risk factors for endoscopic ultrasonography(EUS) and Mitotic count(MI),clinicopathologic parameter and NIH risk classification were performed.Results Among 95 cases (104 lesions),88 were single,while 7 were multiple;81.7％ (85/104) small GISTs arose from stomach,including 87.1％ (74/85)in middle-upper stomach;5 cases (5.3％) presented calcification of different degrees,3 cases(3.2％) presented local necrosis and 2 cases (2.1％) with arrangement of epithelioid cells;88 cases (92.6％) were very low grade of NIH risk classification,6 cases (6.3％) were intermediate risk and 1 case(1.1％) was high risk.Positive rates of CD34 and CD117 were 95.8％ (91/95) and 96.8％ (92/95) respectively.The risk factors (border,mucosal surface,echo and heterogeneity) of EUS had no correlation with mitotic count(P＞0.05).The correlation analysis between clinicopathologic features and NIH risk classification revealed tumors more than 1.5 cm had a striking correlation with NIH risk classification (P＜ 0.05).Conclusion Most small GISTs,single or multiple,located at middle-upper stomach,were of very low or low risk,and have a favorable prognosis.But it has worse biological behavior and a higher grade risk when the diameter is more than 1.5 cm,intervention should be recommended.

Nanoformulations of the vascular inhibitors:combretastatin A4 and combretastatin A4 phosphate / 国际药学研究杂志

Combretastatin A4(CA4),a vascular inhibitor,can target tubulin and inhibit tubulin polymerization,thus it can inhibit the tumor blood vessels and has antitumor effect. But it is insoluble in water and has low bioavailability. CA 4 phosphate (CA4P),the derivative of CA4,can improve the solubility of CA4 and convert into CA4. CA4P is undergoing phaseⅡ/Ⅲclinical tri?als abroad. However,CA4P has several undesirable side effects and relative short half-life in vivo. Nanoformulations can increase the dissolution and absorption of the drug and obtain controlled release and targeting,prolong the efficacy and reduce side effects. Work?ing on the physical and chemical characteristics and biological pharmacy defects of CA4 and CA4P,nanoformulations may change the dissolution,absorption and distribution of the drug. This paper reviews the current nanoformulations of CA4 and CA4P,including den?drimer,polymeric micelle(PM),nanoparticles(NP),long-circulating liposome(LCL),and discusses the prospects of their nanofor?mulations.

Investigation about nurses'congnition of reporting adverse events and errors voluntarily in Guangxi Province / 中国实用护理杂志

Objective In order to know nurses'congnition of reporting adverse events and errors voluntarily by questionnaire,and then analyze the related factors. Methods Investigated 275 nurses from 25 hospitals in Guangxi Province by self-desinged questionnaire to know their cognition about reporting adverse events and errors voluntarily,analyzed the datum of invetigation. Results There was different ideas about reporting adverse events and errors voluntarily in nurses with different professional title and duty.Nurses'attitude was different under the different system of reporting adverse events and errors. Conclusions The safety awarness of nurses should be strengthened.The existing reporting system must be imported. It is necessary to establish a comprehensive reporting system of care mistakes and adverse events.