OBJECTIVE:To establish a HPLC method for the determination of dolastron mesylate.METHODS:The sample was separated on Diamonsil C18 column.The mobile phase consisted of acetonitrile-water-1mol? L-1 ammonium formate(450∶ 440∶ 110)(pH=8.0 adjusted with trithylamine)with a flow rate of 1.0mL? min-1.The UV detection wavelength was set at 285nm and the sample size was 20? L.RESULTS:The linear range of dolasetron mesylate was 24～ 56? g? min-1(r=0.999 6),with average recovery at 99.7%(RSD=0.74%).CONCLUSION:The established is simple,sensitive and reproducible,and suitable for the quality control of dolasetron mesylate.

OBJECTIVE:To prepare and characterize capreomycin sulfate liposomes(CSL).METHODS:Capreomycin sulfate was entrapped into liposomes using active loading that pH gradient methods,ammonium sulfate gradient methods and sodium acetate gradient methods respectively followed by lyophilization technique.The liposome was characterized by entrapment efficiency,particle size,? potential and the stability.RESULTS:The entrapment efficiency of CSL pre-and post-lyophilization prepared by three methods were 65.7% and 65.2 %,20.1% and 18.6%,34.6% and 32.4%,with particle size of 136 and 145 nm,144 and 153 nm,142 and 159 nm,? potential of —20.2 and —19.5 mV,—24.4 and —22.9 mV,—18.7 and —17.8 mV respectively.No obvious changes were found in all the indexes in the stability test.CONCLUSIONS:The pH gradient technique is suitable for preparing CSL in 3 kinds of methods.

OBJECTlVE To investigate the effect of stretch on muscarinic receptor- and 5-hydroxytryptamine( 5-HT)receptor-mediated contractiIe responses in isoIated circuIar muscIe strips taken from the rat stomach. METHODS The contractiIe responses to carbachoI(CCh)0.001-30 μmoI·L-1 or 5-HT 0.0001 -30 μmoI·L-1 administered cumuIativeIy were recorded in isoIated circuIar muscIe strips taken from the gastric fundus,body,cardia and pyIorus of rats under different preIoads of 1.0,1.5,2.0, 2.5 and 3. 0 g,but a singIe concentration of CCh 0. 3 μmoI·L-1 was administered to the antrum. RESULTS The -Log EC50 vaIue for CCh in the isoIated circuIar muscIe strips of the gastric fundus, body and pyIorus under 1.0 g preIoad was the Iargest,but decreased significantIy with higher preIoads (P﹤0.05,P﹤0.01). A simiIar resuIt was obtained in the isoIated circuIar muscIe strips of the gastric body when 5-HT was used as an agonist. The Emax vaIue of contractiIe responses to CCh and 5-HT in the cir-cuIar muscIe strips of the gastric cardia under 3.0 g preIoad was increased by 117.4% and 75.7% com-pared to that under 1.0 g preIoad. The Emax vaIue of contractiIe responses to 5-HT in the circuIar muscIe strips of the gastric body under 3.0 g preIoad was aIso increased by 115.9% when compared to 1.0 g preIoad. The Emax( g) vaIue of contractiIe responses to CCh in four types of muscIe strips was 10.453±2.956(cardia under 3.0 g preIoad),13.878±2.618(fundus under 2.5 g preIoad),10.244±1.843 (gastric body under 2.5 g preIoad)and 2.585±1.098(pyIorus under 2.5 g preIoad),respectiveIy. The Emax(g)vaIue of contractiIe responses to 5-HT in three types of muscIe strips was 4.363±1.705(cardia under 3.0 g preIoad),3.931±0.615(fundus under 3.0 g preIoad)and 3.161±0.680(gastric body under 3.0 g preIoad),respectiveIy. CONCLUSlON 0.5 g or 1.0 g preIoad is inadequate for accurate determi-nation of contractiIe responses mediated by muscarinic receptors and 5-HT receptors in isoIated circuIar muscIe strips taken from the rat gastric cardia,fundus,body and pyIorus,but 2.0 g preIoad is optimaI for investigating muscarine receptor- or 5-HT receptor-mediated contractiIe responses of isoIated gastric strips of rats.

The anti-tumor activity of folate receptor targeting docetaxel-loaded membrane-modified liposomes (FA-PDCT-L) was investigated in vitro and in vivo. FA-PDCT-L was prepared by organic solvent injection method. Transmission electron microscope, dynamic light scattering and electrophoretic light scattering were employed to study the physicochemical parameters of FA-PDCT-L. The inhibitory effects of docetaxel injection (DCT-I), non-modified DCT liposomes (DCT-L) and FA-PDCT-L on the growth of MCF-7 and A-549 cells at different incubation times were detected by CCK-8 assay; and the hemolytic test was employed in vitro. Tumor mice were randomized into 4 groups: DCT-I, DCT-L, FA-PDCT-L and control group (normal saline), and given drugs at 10 mg x kg(-1) x d(-1) through tail vein. The tumor volume, mice weight, inhibition rate of tumor and life span were measured at the end of experiments. The IC50 of the FA-PDCT-L for MCF-7 and A549 cell lines were significantly lower than that of DCT-I and DCT-L, without hemolysis reaction observed. Compared with control group, the weights of tumor in DCT-I, DCT-L and FA-PDCT-L were decreased, especially for FA-PDCT-L, with inhibitory rates at 79.03 % (P < 0.05). The life span and median survival time of FA-PDCT-L treated mice were significantly higher than that of DCT-I and DCT-L. In conclusion, FA-PDCT-L shows a good anti-tumor activity, indicating that it is potential carriers for DCT in the treatment of tumor.

OBJECTIVE:To prepare the levofloxacin(LEF)thermosensitive gel for ophthalmic drug delivery,and to study the drug release in vitro.METHODS:Poloxamer407was used as themosensitive material for the LEF eye drop,the best con?centration of poloxamer in prescription was selected according to the temperature of gel,a novel membraneless model was used to study the drug release.RESUTS:The detected concentration of LEF was in the linear range of3～11?g/ml(r=0.9991,n=6),the recovery was99.62%;The best concentration of poloxamer in prescription was18%;Drug release followed zero-order kinetics,and the quantity of drug release was controlled by that of gel dissolution.CONCLUSION:The preparation is simple in method and easy to control in dosage,therefore it shows a promising future in development.

OBJECTIVE: To establish a RP-HPLC method for the determination of pamidronate disodium. METHODS: The determination was performed on C18 column with acetonitrile-0.4% sodium hydroxide solution of EDTA-Na2 (14∶86) as mobile phase at a flow rate of 0.6mL?min-1,the sample size was 10?L and the detection was performed by fluorescence detector with excitation wavelength at 395nm and emission wavelength at 480nm. RESULTS: The linear range of pamidronate disodium was 7.2～16.8?g?mL-1(r=0.999 8,n=9),the recovery rate was 100.11%(RSD=0.7%, n=9). CONCLUSIONS: The established method is simple and accurate.

OBJECTIVE:To prepare coenzyme Q10 submicroemulsion and investigate its stability and physico-chemical properties.METHODS:Orthogonal experiment was designed to optimize the formulation and preparation procedure of coenzyme Q10 submicroemulsion.The content and entrapment efficiency of the preparation were determined by HPLC,and its properties such as particle size,? potential,pH value and stability were studied.RESULTS:The optimal formulation and preparation procedure of coenzyme Q10 submicroemulsion were as follows:the ratio of soybean oil to medium-chain triglyceride was 1∶2;the ratio of soybean phospholipids to poloxamer 188 was 3∶1;the high speed shearing emulsification time was 10min and the preparation temperature was 60℃.The mean entrapment efficiency of 3 batches of coenzyme Q10 submicroemulsions was 98.07%,with a ? potential of —28.4mV and a mean particle size of 168 nm.Illumination and freeze thawing should be avoided for the preparation in storing,which showed a satisfactory stability at 4℃.CONCLUSION:The prepared coenzyme Q10 submicroemulsion was up to the standards of intravenous injection preparations.

Oxaliplatin-loaded nanostuctured lipid carriers (OP-NLC) were prepared by ultrasonic emulsification method. And its optimal prescription was selected by orthogonal design. The laser light scattering technique, zeta potential analyzer, TEM, DSC, XRD and HPLC were employed to study the physicochemical parameters of OP-NLC, which displayed in terms of particle size, zeta potential, crystalline, drug loading and encapsulation efficiency. The results showed that OP-NLC had an average diameter of (111 +/- 20) nm, zeta potential of (-27.4 +/- 13.1) mV, encapsulation efficiency of (77.4 +/- 2.5) % and drug content of (0.8 +/- 1.5) mg mL(-1). TEM, DSC and XRD indicated that OP-NLC was spherical and the drug was dispersed as nanoparticles by means of non-crystalline. The in vitro release test showed that the drug could be sustained-released from NLC in buffer solution (pH 4.5) after a burst release in initial phase.

Objective To improve the stability of epirubicin long circulation liposomes via lyophilizing technology and preliminarily evaluate their quality. Methods The effect of the various cryoprotectant,different pre-freezing and total drying time on the preparation was analyzed. The stability of the lyophilized powder was tested at (25±2) ℃ and (60±10)% relative humidity for 3 months. Results The protective agent trehalose to liposomes was 31. The freeze-drying was conducted with pre-freezing temperature at -70 ℃,precooling for 8 h and total drying for 24 h. There were no significant differences in particle size,encapsulation efficiency and drug content of lyophilized long-circulating liposomes compared with those un-lyophilized. After 3 months under the accelerated condition,it had good redispersibility, entrapment rate (>94%) and drug content (>99%) . Conclusion Lyophilizing the long-circulation epirubicin liposomes can effectively improve the stability of the preparation.

Objective: Evidence supports the efficacy of coronary computed tomography angiography (CCTA)-based risk scores in cardiovascular risk stratification of patients with suspected coronary artery disease (CAD). We aimed to compare two CCTAbased risk score algorithms, Leiden and Confirm scores, in patients with diabetes mellitus (DM) and suspected CAD. Materials and Methods: This single-center prospective cohort study consecutively included 1241 DM patients (54.1% male, 60.2 ± 10.4 years) referred for CCTA for suspected CAD in 2015–2017. Leiden and Confirm scores were calculated and stratified as < 5 (reference), 5–20, and > 20 for Leiden and < 14.3 (reference), 14.3–19.5, and > 19.5 for Confirm. Major adverse cardiovascular events (MACE) were defined as the composite outcomes of cardiovascular death, nonfatal myocardial infarction (MI), stroke, and unstable angina requiring hospitalization. The Cox model and Kaplan–Meier method were used to evaluate the effect size of the risk scores on MACE. The area under the curve (AUC) at the median follow-up time was also compared between score algorithms. Results: During a median follow-up of 31 months (interquartile range, 27.6–37.3 months), 131 of MACE were recorded, including 17 cardiovascular deaths, 28 nonfatal MIs, 64 unstable anginas requiring hospitalization, and 22 strokes. An incremental incidence of MACE was observed in both Leiden and Confirm scores, with an increase in the scores (log-rank p < 0.001). In the multivariable analysis, compared with Leiden score < 5, the hazard ratios for Leiden scores of 5–20 and > 20 were 2.37 (95% confidence interval [CI]: 1.53–3.69; p < 0.001) and 4.39 (95% CI: 2.40–8.01; p < 0.001), respectively, while the Confirm score did not demonstrate a statistically significant association with the risk of MACE. The Leiden score showed a greater AUC of 0.840 compared to 0.777 for the Confirm score (p < 0.001). Conclusion CCTA-based risk score algorithms could be used as reliable cardiovascular risk predictors in patients with DM and suspected CAD, among which the Leiden score outperformed the Confirm score in predicting MACE.